EP1401383A2 - Use of at least an oil extracted from the seeds of the gourd family for preparing a composition for inhibiting 5-alpha-reductase activity - Google Patents
Use of at least an oil extracted from the seeds of the gourd family for preparing a composition for inhibiting 5-alpha-reductase activityInfo
- Publication number
- EP1401383A2 EP1401383A2 EP02767537A EP02767537A EP1401383A2 EP 1401383 A2 EP1401383 A2 EP 1401383A2 EP 02767537 A EP02767537 A EP 02767537A EP 02767537 A EP02767537 A EP 02767537A EP 1401383 A2 EP1401383 A2 EP 1401383A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- composition
- oil
- seeds
- luffa
- skin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
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- 239000002076 α-tocopherol Substances 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/42—Cucurbitaceae (Cucumber family)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61Q19/00—Preparations for care of the skin
- A61Q19/008—Preparations for oily skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61Q19/00—Preparations for care of the skin
- A61Q19/10—Washing or bathing preparations
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q3/00—Manicure or pedicure preparations
- A61Q3/02—Nail coatings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/008—Preparations for oily hair
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/02—Preparations for cleaning the hair
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
- A61Q7/02—Preparations for inhibiting or slowing hair growth
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
Definitions
- the present invention relates to the use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, for the preparation of a composition intended to inhibit the activity of 5 ⁇ -reductase, as well as the use of such an oil for the preparation of a composition intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia, and hirsutism.
- the invention also relates to cosmetic treatment methods, in particular for oily skin.
- the subject of the invention is also the use of at least one oil of cucurbit seeds in a food for humans and / or animals as an additive acting to inhibit the activity of 5-alpha reductase.
- the tropical cucurbits belonging to the three genera Lagenaria, Luffa and Momordica are plants cultivated in particular on Reunion Island or in India.
- these tropical cucurbits one can cite in particular the long calabashes, scabies and bottle (Lagenaria leucaritha), the ribbed pipangaille (Luffa acutanguld), the smooth pipangaille (Luffa cylindrica) and the margoze (Momordica charantia).
- Calabashes of the genus Lagenaria leucaritha are plants generally cultivated in Asia, especially in China and Japan. They are also found around the Indian Ocean. These plants are annual herbaceous plants from 8 to 10 meters. The fertilization of their flowers leads to cylindrical fruits, swollen at their base, called calabashes. There are, for example, on the island of Reunion, three types of gourds of the genus Lagenaria leucaritha, the long gourds, scabies and bottle. These fleshy fruits contain in their center flat and elongated seeds with a lipid content of between 12 and 25% by weight.
- the margoze of the genus Momordica charantia comes from India but is also cultivated on the island of Reunion. It is an annual herb, which can give lianas of 2 meters, and whose oblong fruits of green color contain flat seeds. The lipid content of these seeds is approximately 30% by weight.
- patent application EP 359 196 describes cosmetic formulations for the treatment of the skin, comprising at least one adjuvant and from 1 to 90% by weight of an extract of luffa cylindrica, the extract being an aqueous or alcoholic extract. obtained for example by percolation.
- the oil extracted from the seeds of tropical cucurbits advantageously chosen from the group consisting of Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia
- a cosmetic composition advantageously administered by topical external route, intended to inhibit the activity of 5-alpha reductase and to act in particular on oily or shiny skin or hair, on skin prone to acne, on the areas of the scalp affected by alopecia of non-pathological origin or on areas of the skin with excess hairiness.
- oils extracted from the seeds of tropical cucurbits appear to be cosmetically acceptable compounds, non-aggressive for the skin, non-toxic and hypoallergenic.
- the Applicant has also surprisingly discovered that the oil extracted from the seeds of tropical cucurbits according to the present invention could be used in a pharmaceutical or food composition intended to inhibit the activity of 5-alpha reductase.
- 5 ⁇ -reductase is a microsomal NADPH dependent enzyme which exists in the form of two isoenzymes synthesized from two different genes.
- the type 1 isoenzyme of 5-reductase is found mainly in the liver and skin, more particularly in the sebaceous glands of non-genital skin and scalp, and appears at puberty.
- the type 2 isoenzyme is predominant in the prostate and in the skin of the differentiated sexual territories: genital area, beard, and plays a role in sexual differentiation.
- the distribution of type 1 and 2 isoenzymes of 5 ⁇ -reductase in the skin and the cutaneous appendages in humans can be illustrated by the following table 1.
- Table 1 Distribution of type 1 and 2 isoenzymes of 5 ⁇ -reductase in the skin and skin appendages in humans
- this enzyme 5 ⁇ -reductase mainly located in the genital tissues and in the skin, catalyzes the hydroxylation of testosterone to 5 ⁇ -reductase dihydrotestosterone (DHT).
- DHT 5 ⁇ -reductase dihydrotestosterone
- Too high 5 ⁇ -reductase activity therefore causes too much androgen in the form of DHT elevated in the prostate, resulting in overstimulation of the latter resulting in an undesirable growth which can lead to the pathology of prostatic hypertrophy, or even to prostatic adenoma, most often requiring surgical intervention.
- Other pathologies, of dermatological type can be observed in men or women as resulting from an overactivity of 5 ⁇ -reductase, namely, in particular acne, hirsutism or even alopecia.
- the activity of 5-reductase is greater in the sebaceous gland than in other structures.
- the seborrheic glands show a more active 5 ⁇ -reductase than those in other skin areas. Therefore, the level of physiological sebaceous secretion seems closely related to the activity of this enzyme.
- Oily skin in addition to its unsightly appearance, constitutes a field on which complications can arise. It reaches the areas where the sebaceous glands are numerous and results mainly from an androgenic overstimulation of the sebaceous production by these specific glands. Hyperseborrhea participates in the occurrence of acne vulgaris lesions.
- the type 1 isoenzyme of 5 ⁇ -reductase in the sebaceous glands, as well as in the hair follicle.
- the 5 ⁇ -reductase type 2 isoenzyme is localized mainly at the level of the internal epithelial sheath, as well as at the level of the dermal papilla of the hair. However, this latter location remains to be specified.
- Androgenic alopecia whose pathophysiology is very close to that of acne, is the most common alopecia and probably the one where the demand for therapy is the highest. 5 ⁇ -reductase seems to play a key role in this pathology. In fact, men suffering from a genetic deficiency in the 5cc-reductase type 2 isoenzyme do not develop androgenetic alopecia. In view of the above, research has focused on the development of 5 ⁇ -reductase inhibitors. Some steroids like progesterone have been tested for this, but its rapid metabolism makes it ineffective in vivo. To be active, the 5 ⁇ -reductase inhibitor must be stable enough to block the activity of the enzyme in vitro.
- Finasteride a competitive steroidal inhibitor, fulfills this condition, but it is more active on the type 2 isoenzyme than on the type 1 isoenzyme and these two isoenzymes have only 50% homology on the sequence of their acids. amines. It is therefore especially in benign prostatic hyperplasia that finasteride has already been tested.
- Serenoa Repens extract is also known, as a reference as a 5 ⁇ -reductase inhibitor, the Serenoa Repens extract having the advantage, compared to the finasteride, of being of natural origin in as a plant extract allowing a better comparison for tested products also of natural origin.
- Serenoa Repens also known as Sabal serrulatum, is a small palm that can be found in the United States (Florida) in North Africa and in Spain.
- the Applicant has now found, quite surprisingly and unexpectedly, that the use of the oil extracted from cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica allows a remarkable inhibition effect to be obtained. the activity of 5 ⁇ -reductase, thus in particular providing a new response for the treatment of the dermatological pathologies and / or disorders mentioned above.
- the oil according to the present invention can thus be incorporated into a pharmaceutical composition, into a food product or into a food supplement, or even into a cosmetic composition.
- a subject of the present invention is therefore the use of at least one oil of cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, for the preparation of a composition intended to inhibit the activity of 5-alpha reductase.
- cucurbit seed oil to prepare a composition according to the present invention intended to inhibit the type 1 isoenzyme and / or the type 2 isoenzyme of 5 ⁇ -reductase is particularly advantageous according to the present invention.
- the composition is advantageously intended for topical external use. It may also contain a cosmetically acceptable support.
- compositions which is advantageously used according to the present invention can be in all the dosage forms usually used for a topical external application.
- the composition is in the form of an aqueous, hydroalcoholic or oily solution, an oil-in-water or water-in-oil or multiple emulsion, an aqueous or oily gel, a liquid, pasty or solid anhydrous product, or an oil dispersion in an aqueous phase using spherules, the spherules possibly being polymeric nanoparticles such as nanospheres and nanocapsules or better lipid vesicles of ionic type and / or non-ionic.
- the composition can be more or less fluid, be in the form of a white or colored cream, ointment, milk, lotion, ointment, serum, paste, foam, aerosol or stick.
- composition used according to the present invention may also contain the adjuvants customary in the cosmetic field, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters, pigments, chelating agents, odor absorbers and coloring matters.
- the amounts of these various adjuvants are those conventionally used in cosmetics, and for example from 0.01% to 20% by weight, relative to the total weight of the composition.
- These adjuvants depending on their nature, can be introduced into the fatty phase, into the aqueous phase, into the lipid vesicles and / or into the nanoparticles.
- the proportion of the fatty phase can range from 5% to 80% by weight, and preferably from 5% to 50% by weight, relative to the total weight of the composition.
- the oils, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the field under consideration.
- the emulsifier and the coemulsifier are present in the composition in a proportion ranging from 0.3% to 30% by weight, and preferably from 0.5% to 20% by weight, relative to the total weight of the composition .
- mineral oils other oils of vegetable origin (apricot oil, sunflower oil, plum oil), oils of animal origin, synthetic oils , silicone oils and fluorinated oils (perfluoropolyethers).
- Fatty alcohols such as cetyl alcohol, fatty acids, or waxes such as beeswax can also be used as fats according to the present invention.
- emulsifiers and coemulsifiers which can be used according to the present invention, there may be mentioned in particular fatty acid esters of polyethylene glycol, such as PEG-40 stearate or PEG-100 stearate, esters of fatty acid and of polyol, such as glyceryl stearate and sorbitan tristearate.
- hydrophilic gelling agents which can be used according to the present invention, mention may in particular be made of carboxyvinyl polymers (carbomer), acrylic copolymers such as acrylate / alkylacrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays.
- carboxyvinyl polymers carboxyvinyl polymers (carbomer)
- acrylic copolymers such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- polyacrylamides such as acrylate / alkylacrylate copolymers
- the composition also contains at least one compound chosen from the group consisting of hydrophilic active agents, lipophilic active agents, agents modulating differentiation and / or proliferation and / or skin pigmentation, antibacterial agents, agents modulating bacterial adhesion to the skin and / or mucous membranes, antifungal agents, soothing agents, anti-pruritic agents, keratolytic agents, free anti-radical agents, anti-seborrheic agents, anti-dandruff agents , agents with anti-acne activity, anti-irritant agents, moisturizing agents, vitamins, anti-inflammatory agents, UNA and UVB filters, matting agents, light-reflecting pigments, anti-wrinkle active agents, anti-glycation agents, Heat Shock Protein modulators and enzyme inhibitors.
- hydrophilic active agents e.g., lipophilic active agents, agents modulating differentiation and / or proliferation and / or skin pigmentation
- antibacterial agents agents modulating bacterial adhesion to the skin and / or mucous membranes
- lipophilic active agents which can be used according to the present invention, there may be mentioned in particular retinol (vitamin A) and its derivatives, tocopherol (vitamin E) and its derivatives, essential fatty acids, ceramides, essential oils, salicylic acid and its derivatives.
- composition used according to the present invention may also contain other active agents intended in particular for the prevention and / or treatment of skin conditions.
- active agents there may be mentioned in particular agents modulating differentiation and / or proliferation and / or skin pigmentation such as retinoic acid and its isomers, retinol and its esters, vitamin D and its derivatives, phyto -estrogens and kojic acid; antibacterial agents such as octanediol and conventional preservatives (quaternary ammonium, ...); agents modulating bacterial adhesion to the skin and / or mucous membranes such as certain sugar derivatives; antifungal agents, in particular compounds belonging to the class of imidazoles or their salts, compounds of the allylamine family, glycine derivatives (sodium hydroxymethylglycinate for example), piroctone olamine or even octopirox; soothing agents such as salicylic acid, lupeol, allantoin, blueberry water, Silaned
- anti-pruritic agents such as glycine
- keratolytic agents such as alpha and beta-hydroxycarboxylic or beta-ketocarboxylic acids, their salts, amides or esters and more particularly hydroxy acids such as glycolic acid, lactic acid, salicylic acid, acid citric and in general fruit acids
- anti-free radical agents such as alpha-tocopherol or its esters, carotenoids, isoflavones, OPCs, flavonoids, superoxide dismutases, certain metal chelators or ascorbic acid and its esters
- anti-seborrheic agents such as retinoids, sabal, Pygeum Africanum extract, zinc salts.
- anti-dandruff agents such as octopirox, zinc pyrithione or piroctone olamine ; agents having anti-acne activity such as retinoids, retinol, retinaldehyde, vitamins PP, benzoyl peroxides, erythromycin; anti-irritant agents such as thermal waters, polysaccharides, in particular with regard to irritant compounds possibly present in the compositions of the present invention; moisturizers such as polyols (eg glycerin); vitamins (for example D-panthenol or vitamins C, D, B6); anti-inflammatory agents such as thermal waters, polysaccharides; UNA and UNB filters of the organic and mineral screen type; mattifying agents and light-reflecting pigments such as mixtures of titanium and mica; anti-wrinkle active ingredients such as retinol and its derivatives (retinal
- the oil of the seeds of cucurbits is capable of being obtained according to the method consisting in extracting the total lipids from the seeds of cucurbits previously dried and ground, using a solvent oils, then evaporate the solvent.
- the cucurbit seeds according to the present invention are ground for example using a cylinder or hammer mill.
- the solvent for oils, used to extract the total lipids from the seeds forming the oil is a conventional organic solvent for extracting lipids.
- the solvent is advantageously chosen from the group consisting of aliphatic alkanes, aromatic alkanes, aliphatic alcohols and their halogen derivatives. Even more advantageously according to the present invention, the organic solvent is hexane.
- the extraction of the total lipids from the seeds of cucurbits is advantageously carried out by a soxhlet extraction which is a technology well known to those skilled in the art.
- the organic solvent is evaporated, preferably by evaporation under vacuum.
- the oil of the cucurbit seeds is capable of being obtained according to the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure of the seeds cold, advantageously using of a continuous screw press, to lead, after filtration, to virgin oils of first pressure.
- the cucurbit oils according to the present invention can be used raw or refined.
- refining is meant within the meaning of the present invention, the unitary operations for the purification of lipids of plant origin well known to those skilled in the art, among which there may be mentioned in particular chemical neutralization, degumming, bleaching, deodorization and refrigeration.
- the oil extracted from the seeds of cucurbits is present at a concentration of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
- the composition prepared using the oil of the seeds of cucurbits is intended for the treatment of pathologies and / or skin disorders linked to a congenital exaggeration or acquired from the activity of 5 ⁇ -reductase.
- the composition is intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
- the composition used according to the present invention can be a cosmetic, pharmaceutical, dermatological or nutraceutical composition.
- the composition is a pharmaceutical or dermatological composition.
- the therapeutic use of the oil according to the present invention makes it possible to treat forms of acne, hyperseborrhea, alopecia or hirsutism having a pathological character.
- the present invention also relates to the use of at least one seed oil of cucurbits chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, for the preparation of a composition, advantageously pharmaceutical or dermatological, intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
- the present invention also relates to a cosmetic treatment method, characterized in that one applies to the skin, mucous membranes, nails or hair at least one oil of cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in order to inhibit the activity of 5 ⁇ -reductase.
- the cosmetic composition is applied to oily skin and / or to oily hair, to shiny skin and / or to shiny hair, on the skin having pimples, dots. black, or blackheads, on oily skin prone to acne, on oily skin with imperfections, on the areas of the scalp affected by alopecia or on the areas of the skin with excess hairiness.
- the cosmetic treatment methods for oily and / or shiny skin or hair, skin with pimples, blackheads, or blackheads, oily skin prone to acne or blemishes, areas of the scalp affected by alopecia or areas of the skin with excess hair growth make it possible to improve the appearance of human beings by visibly reducing unsightly phenomena and aesthetically annoying linked to hyperseborrhea, which gives in particular a greasy and / or shiny appearance to the skin and / or hair and which can cause the appearance of pimples, blackheads or blackheads, alopecia which manifests itself by hair loss or hirsutism which is manifested by excess body hair.
- hyperseborrhea, alopecia or hirsutism is not of pathological origin, but comes, for example, in the case of alopecia, external aggressions (discoloration, dyeing) or even old age.
- the subject of the present invention is the use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in a nutraceutical composition or a food for humans and / or animals as an additive acting to inhibit the activity of 5-alpha reductase.
- the oil of the seeds of cucurbits is extracted according to the process consisting in extracting the total lipids from the seeds of cucurbits previously dried and ground, using a solvent oils, advantageously by extraction with a soxhlet, then evaporating the said solvent or by the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure from the seeds when cold, advantageously using a continuous screw press, to lead, after filtration, to virgin oils of first pressure.
- the oil extracted from the seeds of cucurbits is used in a proportion of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
- Example 1 Composition of the Oil Extracted from Cucurbit Seeds
- Example 1.1 composition of the oil extracted from the seeds of bottle, scab and long calabash (Lagenaria leucaritha)
- Example 1.2 composition of the oil extracted from the seeds of smooth pipangailles (Luffa cylindrica) and ribbed (Luffa acutangula) and margoze (Momordica charantia)
- Example 2 Cosmetic Compositions Example 2.1 Cream for Acne-prone Skin No. 1
- Example 2.6 Foaming washing emulsion for acne-prone skin no. 3
- Example 2.8 Matifying emulsion n ° 2
- Example 2.9 Matifying emulsion n ° 3
- Example 2.10 Tinted matifying emulsion No. 1
- Example 2.11 Tinted matifying emulsion n ° 2
- Example 3 In Vitro Evaluation of the Activity of Margoze Oil 5-Reductase on the Conversion of Testosterone to 5-Dihydrotestosterone in Cultures of Normal Human Dermal Fibroblasts.
- MCF fibroblast culture medium
- MEM designation given to the culture medium, Minimum Essential medium
- MIF fibroblast incubation medium
- SNF fetal calf serum
- 5 ⁇ -DHT 5 ⁇ -DiHydroTestosterone
- Margoze oil was supplied by Pharmascience Laboratories and was stored at + 4 ° C until the time of use. The effects of the test product were compared with those obtained in the presence of Finasteride, used as a reference product (Finasteride, active ingredient in CHIBRO-PROSCAR tablets: MERCK SHARP & DOHME CHIBRET).
- Radioactive testosterone (labeled with tritium in position 1, 2, 6 and 7, specific activity 95 Ci / mmol) was supplied by AMERSHAM, non-radiolabelled testosterone was supplied by SIGMA.
- the analytical quality reagents came from SIGMA, MERCK, BDH,
- the fibroblast culture medium consisted of MEM / M199 (3: 1, v / v) supplemented with penicillin (50 IU / ml), streptomycin (50 ⁇ g / ml), sodium bicarbonate (0 , 2%, w / v) and S VF (10%, v / v).
- the test system consisted of normal human dermal fibroblasts grown in a monolayer.
- the fibroblasts were isolated from a residue of tummy tuck performed in a 30-year-old woman (subject no. I0006).
- the cells were used in the third passage, they were cultured until the monolayers converge in the MCF medium at 37 ° C. in a humid atmosphere containing 5% CO 2 .
- the fibroblast incubation medium consisted of MCF supplemented with tritiated testosterone (1.6 ⁇ 10 ⁇ 7 M, ie 6.32 ⁇ Ci / ml) and non-radiolabelled testosterone (3.84 x 10 "6 M). Finasteride was extracted from the tablets by grinding, stirring in DMSO, centrifugation then collection of the supernatant (theoretical concentration of this solution: 1 mg / ml of finasteride), tested at 30 ng / ml.
- MIF fibroblast incubation medium
- Margoze oil was dissolved at 2 mg / ml in MCF medium containing 2.5% ethanol, then dilution in MCF medium in contact with the cells so as to obtain final concentrations of margoze oil of 5 and 10 ⁇ g / ml.
- the fibroblast cultures were incubated in the presence of the test product or of the reference product prepared in the MIF medium for 24 hours at 37 ° C. in a humid atmosphere containing 5% CO 2 . Control cultures were incubated in the MIF medium in the absence of test product and of reference product.
- the migration solvent was a mixture of dichloromethane and ether (7: 3, v / v)
- the silica plates were read using a BERTHOLD radioactivity scanner.
- the non-radiolabelled standards were demonstrated by spraying 5% (v / v) sulfuric acid on the chromatography plates then heated to 100 ° C for 10 minutes.
- the metabolism of testosterone to 5 -dihydrotestosterone under the various experimental conditions was calculated: the results (areas of the peaks of 5 ⁇ -dihydrotestosterone counted by the BERTHOLD scanner) are expressed in pmol of 5 ⁇ -DHT formed by ⁇ g of DNA. They were also expressed as a percentage of the 5 ⁇ -reductase activity present in the “control cells” group.
- the determination of the total DNA content was carried out using a fluorecent nuclear dye (Hoechst 33258) by fluorometry (excitation 356 nm, emission .458 nm).
- control group and treated groups were treated by a factor analysis of variance (ANONA 1, p ⁇ 0.05), followed by a DU ⁇ ETT test (p ⁇ 0.05). The effect of the test product and the reference product was compared with the 'control cells' group.
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Abstract
The invention concerns the use of at least an oil derived from the seeds of the gourd family selected from the group consisting of Lagenaria, Luffa and Momordica, for preparing a composition designed to inhibit 5α-reductase activity, and the use of said oil for preparing a composition for treating prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia, and hirsutism. The invention also concerns cosmetic treatment methods, in particular for greasy skin. The invention further concerns the use of at least an oil derived from seeds of the gourd family in a nutritional food composition for humans and/or animals as additive for inhibiting 5α reductase activity.
Description
« Utilisation d'au moins une huile extraite de graines de cucurbitacées pour la préparation d'une composition destinée à inhiber l'activité de la 5α-réductase »"Use of at least one oil extracted from cucurbit seeds for the preparation of a composition intended to inhibit the activity of 5α-reductase"
La présente invention se rapporte à l'utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, pour la préparation d'une composition destinée à inhiber l'activité de la 5α-réductase, ainsi qu'à l'utilisation d'une telle huile pour la préparation d'une composition destinée au traitement de l'hypertrophie prostatique, de l'adénome prostatique, de l'acné, de Phyperséborrhée, de l'alopécie, et de l'hirsutisme. L'invention se rapporte également à des méthodes de traitement cosmétique, notamment de la peau grasse. L'invention a également pour objet l'utilisation d'au moins une huile de graines de cucurbitacées dans un aliment pour l'être humain et/ou l'animal en tant qu'additif agissant pour inhiber l'activité de la 5-alpha reductase.The present invention relates to the use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, for the preparation of a composition intended to inhibit the activity of 5α -reductase, as well as the use of such an oil for the preparation of a composition intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia, and hirsutism. The invention also relates to cosmetic treatment methods, in particular for oily skin. The subject of the invention is also the use of at least one oil of cucurbit seeds in a food for humans and / or animals as an additive acting to inhibit the activity of 5-alpha reductase.
Les cucurbitacées tropicales appartenant aux trois genres Lagenaria, Luffa et Momordica sont des végétaux cultivés notamment sur l'île de la Réunion ou en Inde. Parmi ces cucurbitacées tropicales, on peut citer notamment les calebasses longue, gale et bouteille (Lagenaria leucaritha), le pipangaille à côtes (Luffa acutanguld), le pipangaille lisse (Luffa cylindrica) et la margoze (Momordica charantia).The tropical cucurbits belonging to the three genera Lagenaria, Luffa and Momordica are plants cultivated in particular on Reunion Island or in India. Among these tropical cucurbits, one can cite in particular the long calabashes, scabies and bottle (Lagenaria leucaritha), the ribbed pipangaille (Luffa acutanguld), the smooth pipangaille (Luffa cylindrica) and the margoze (Momordica charantia).
Les calebasses du genre Lagenaria leucaritha sont des plantes généralement cultivées en Asie, notamment en Chine et au Japon. On les retrouve également sur le pourtours de l'Océan Indien. Ces plantes sont des herbacées annuelles de 8 à 10 mètres. La fécondation de leurs fleurs conduit à des fruits cylindiques, enflés à leur base, appelés calebasses. On trouve par exemple, sur l'île de la Réunion, trois types de calebasses du genre Lagenaria leucaritha, les calebasses longue, gale et bouteille. Ces fruits charnus contiennent en leur centre des graines plates et allongées présentant une teneur en lipides comprise entre 12 et 25 % en poids.Calabashes of the genus Lagenaria leucaritha are plants generally cultivated in Asia, especially in China and Japan. They are also found around the Indian Ocean. These plants are annual herbaceous plants from 8 to 10 meters. The fertilization of their flowers leads to cylindrical fruits, swollen at their base, called calabashes. There are, for example, on the island of Reunion, three types of gourds of the genus Lagenaria leucaritha, the long gourds, scabies and bottle. These fleshy fruits contain in their center flat and elongated seeds with a lipid content of between 12 and 25% by weight.
Les pipangailles appartenant aux genres Luffa cylindrica et Luffa acutangula, respectivement du type lisse ou à côtes, sont originaires de l'Inde. Ce sont des herbacées annuelles, constituées de tiges rampantes pouvant atteindre 5 mètres de long.
Les fruits renferment des graines noires et ovales dont la teneur en lipides est comprise entre 20 et 30% en poids.The pipangailles belonging to the genera Luffa cylindrica and Luffa acutangula, respectively of the smooth or ribbed type, originate from India. They are annual herbs, made up of creeping stems up to 5 meters long. The fruits contain black and oval seeds whose lipid content is between 20 and 30% by weight.
La margoze du genre Momordica charantia provient de l'Inde mais est aussi cultivée sur l'île de la Réunion. C'est une herbacée annuelle, qui peut donner des lianes de 2 mètres, et dont les fruits oblongs de couleur verte contiennent des graines plates. La teneur en lipides de ces graines est de 30% environ en poids.The margoze of the genus Momordica charantia comes from India but is also cultivated on the island of Reunion. It is an annual herb, which can give lianas of 2 meters, and whose oblong fruits of green color contain flat seeds. The lipid content of these seeds is approximately 30% by weight.
Les cucurbitacées tropicales telles que le Luffa cylindrica ont déjà été utilisées dans des applications cosmétiques, mais l'huile extraite des graines de ces cucurbitacées, contenant les lipides totaux de ces graines, n'a jamais été utilisée dans des formulations cosmétiques. Ainsi, la demande de brevet EP 359 196 décrit des formulations cosmétiques pour le traitement de la peau, comprenant au moins un adjuvant et de 1 à 90 % en poids d'un extrait de luffa cylindrica, l'extrait étant un extrait aqueux ou alcoolique obtenu par exemple par percolation.Tropical cucurbits such as Luffa cylindrica have already been used in cosmetic applications, but the oil extracted from the seeds of these cucurbits, containing the total lipids of these seeds, has never been used in cosmetic formulations. Thus, patent application EP 359 196 describes cosmetic formulations for the treatment of the skin, comprising at least one adjuvant and from 1 to 90% by weight of an extract of luffa cylindrica, the extract being an aqueous or alcoholic extract. obtained for example by percolation.
La demanderesse a ainsi découvert de manière surprenante que l'huile extraite des graines des cucurbitacées tropicales, avantageusement choisies dans le groupe constitué par le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, pouvait être utilisée dans une composition cosmétique, avantageusement administrée par voie externe topique, destinée à inhiber l'activité de la 5-alpha reductase et à agir notamment sur la peau ou les cheveux gras ou luisants, sur les peaux à tendance acnéique, sur les zones du cuir chevelu affectées d'alopécie d'origine non pathologique ou sur les zones de la peau présentant des excès de pilosité.The Applicant has thus surprisingly discovered that the oil extracted from the seeds of tropical cucurbits, advantageously chosen from the group consisting of Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, could be used in a cosmetic composition, advantageously administered by topical external route, intended to inhibit the activity of 5-alpha reductase and to act in particular on oily or shiny skin or hair, on skin prone to acne, on the areas of the scalp affected by alopecia of non-pathological origin or on areas of the skin with excess hairiness.
En outre, les huiles extraites des graines des cucurbitacées tropicales s'avèrent être des composés cosmétiquement acceptables, non agressifs pour la peau, non toxiques et hypoallergéniques. La demanderesse a également découvert de manière surprenante que l'huile extraite des graines des cucurbitacées tropicales selon la présente invention pouvait être utilisée dans une composition pharmaceutique ou alimentaire destinée à inhiber l'activité de la 5-alpha reductase.In addition, the oils extracted from the seeds of tropical cucurbits appear to be cosmetically acceptable compounds, non-aggressive for the skin, non-toxic and hypoallergenic. The Applicant has also surprisingly discovered that the oil extracted from the seeds of tropical cucurbits according to the present invention could be used in a pharmaceutical or food composition intended to inhibit the activity of 5-alpha reductase.
La 5α-réductase est une enzyme microsomiale NADPH dépendante qui existe sous forme de deux isoenzymes synthétisées à partir de deux gènes différents.
L' isoenzyme de type 1 de la 5 -réductase est retrouvée essentiellement dans le foie et la peau, plus particulièrement dans les glandes sébacées de la peau non génitale et du cuir chevelu, et apparaît à la puberté. L'isoenzyme de type 2 est prédominante dans la prostate et au niveau de la peau des territoires sexuels différenciés : région génitale, barbe, et joue un rôle dans la différenciation sexuelle. La répartition des isoenzymes de type 1 et 2 de la 5α-réductase au niveau de la peau et des annexes cutanées chez l'homme peut être illustrée par le tableau 1 suivant.5α-reductase is a microsomal NADPH dependent enzyme which exists in the form of two isoenzymes synthesized from two different genes. The type 1 isoenzyme of 5-reductase is found mainly in the liver and skin, more particularly in the sebaceous glands of non-genital skin and scalp, and appears at puberty. The type 2 isoenzyme is predominant in the prostate and in the skin of the differentiated sexual territories: genital area, beard, and plays a role in sexual differentiation. The distribution of type 1 and 2 isoenzymes of 5α-reductase in the skin and the cutaneous appendages in humans can be illustrated by the following table 1.
Tableau 1 : répartition des isoenzymes de type 1 et 2 de la 5α-réductase au niveau de la peau et des annexes cutanées chez l'hommeTable 1: Distribution of type 1 and 2 isoenzymes of 5α-reductase in the skin and skin appendages in humans
Il existe un certain nombre de pathologies pour lesquelles une exagération congénitale ou acquise de l'activité de la 5 -réductase est responsable en totalité ou en majorité des troubles observés.There are a certain number of pathologies for which a congenital or acquired exaggeration of the activity of 5-reductase is responsible in whole or in majority for the disorders observed.
Par exemple, chez l'homme, cette enzyme 5α-réductase, principalement localisée dans les tissus génitaux et dans la peau, catalyse l'hydroxylation de la testostérone en 5α-réductase dihydrotestostérone (DHT). Or, comme la DHT est un androgène bien plus actif que la testostérone (environ 2 fois plus), les effets de cette dernière sont amplifiés dans les tissus où est produite la DHT. Une activité trop élevée de la 5α-réductase provoque ainsi des teneurs en androgène sous forme de DHT trop
élevées dans la prostate, d'où une surstimulation de cette dernière se traduisant en une croissance indésirable pouvant mener à la pathologie de l'hypertrophie prostatique, voire à l'adénome prostatique, nécessitant le plus souvent une intervention chirurgicale. D'autres pathologies, de type dermatologique, peuvent être observées chez l'homme ou la femme comme résultant d'une suractivité de la 5α-réductase à savoir, en particulier l'acné, l'hirsutisme ou encore l'alopécie.For example, in humans, this enzyme 5α-reductase, mainly located in the genital tissues and in the skin, catalyzes the hydroxylation of testosterone to 5α-reductase dihydrotestosterone (DHT). However, as DHT is a much more active androgen than testosterone (about twice as much), the effects of the latter are amplified in the tissues where DHT is produced. Too high 5α-reductase activity therefore causes too much androgen in the form of DHT elevated in the prostate, resulting in overstimulation of the latter resulting in an undesirable growth which can lead to the pathology of prostatic hypertrophy, or even to prostatic adenoma, most often requiring surgical intervention. Other pathologies, of dermatological type, can be observed in men or women as resulting from an overactivity of 5α-reductase, namely, in particular acne, hirsutism or even alopecia.
Dans la peau, l'activité de la 5 -réductase est plus importante dans la glande sébacée que dans les autres structures. Par ailleurs, les glandes séborrhéiques montrent une activé 5α-réductase plus importante que celles des autres territoires cutanés. Par conséquent, le niveau de sécrétion sébacée physiologique semble étroitement lié à l'activité de cette enzyme.In the skin, the activity of 5-reductase is greater in the sebaceous gland than in other structures. In addition, the seborrheic glands show a more active 5α-reductase than those in other skin areas. Therefore, the level of physiological sebaceous secretion seems closely related to the activity of this enzyme.
Chez Pacnéïque, il existe une hyperactivité de la 5α-réductase. Plus qu'une augmentation des taux sériques des androgènes, c'est une augmentation des précurseurs en DHT, facteur principal de la fonction sébacée, qui participent à l'acné.In Pacneic, there is an overactivity of 5α-reductase. More than an increase in serum androgen levels, it is an increase in the precursors of DHT, the main factor in sebaceous function, which participate in acne.
La peau grasse (ou séborrhée), outre son aspect disgracieux, constitue un terrain sur lequel peuvent survenir des complications. Elle atteint les zones où les glandes sébacées sont nombreuses et résulte principalement d'une surstimulation androgénique de la production sébacée par ces glandes spécifiques. L'hyperséborrhée participe à la survenue des lésions d'acné vulgaire.Oily skin (or seborrhea), in addition to its unsightly appearance, constitutes a field on which complications can arise. It reaches the areas where the sebaceous glands are numerous and results mainly from an androgenic overstimulation of the sebaceous production by these specific glands. Hyperseborrhea participates in the occurrence of acne vulgaris lesions.
Dans le cuir chevelu, on retrouve l' isoenzyme de type 1 de la 5α-réductase au niveau des glandes sébacées, ainsi qu'au niveau du follicule pileux. L'isoenzyme de type 2 de la 5α-réductase est localisée majoritairement au niveau de la gaine épithéliale interne, ainsi qu'au niveau de la papille dermique du cheveu. Cependant cette dernière localisation reste à préciser.In the scalp, we find the type 1 isoenzyme of 5α-reductase in the sebaceous glands, as well as in the hair follicle. The 5α-reductase type 2 isoenzyme is localized mainly at the level of the internal epithelial sheath, as well as at the level of the dermal papilla of the hair. However, this latter location remains to be specified.
L'alopécie androgénique, dont la physiopathogénie est très voisine de celle de l'acné, est la plus fréquente des alopécies et sans doute celle où la demande de thérapeutique est la plus forte. La 5α-réductase semble jouer un rôle primordial dans cette pathologie. En effet, les hommes atteints d'un déficit génétique en isoenzyme de type 2 de la 5cc-réductase ne développent pas d'alopécie androgénétique.
Compte tenu de ce qui précède, la recherche s'est orientée vers la mise au point d'inhibiteurs de la 5α-réductase. Certains stéroïdes comme la progestérone ont été testés dans ce sens, mais sa métabolisation rapide la rend inefficace in vivo. Pour être actif, l'inhibiteur de 5α-réductase doit être suffisamment stable pour bloquer l'activité de l'enzyme in vitro. Le finastéride, inhibiteur compétitif stéroïdien, remplit cette condition, mais il est plus actif sur l'isoenzyme de type 2 que sur l'isoenzyme de type 1 et ces deux isoenzymes n'ont que 50 % d'homologie sur la séquence de leurs acides aminés. C'est donc surtout dans Fhyperplasie bénigne de la prostate que le finastéride a déjà été testé. Par ailleurs, on connaît également l'extrait de Serenoa Repens, comme référence en tant qu'inhibiteur de la 5α-réductase, l'extrait de Serenoa Repens présentant l'avantage, par rapport au finastéride, d'être d'origine naturelle en tant qu'extrait végétal permettant une meilleure comparaison pour des produits testés également d'origine naturelle. Serenoa Repens, également connu sous la dénomination Sabal serrulatum, est un petit palmier que l'on peut trouver aux Etats-Unis (Floride) en Afrique du Nord et en Espagne.Androgenic alopecia, whose pathophysiology is very close to that of acne, is the most common alopecia and probably the one where the demand for therapy is the highest. 5α-reductase seems to play a key role in this pathology. In fact, men suffering from a genetic deficiency in the 5cc-reductase type 2 isoenzyme do not develop androgenetic alopecia. In view of the above, research has focused on the development of 5α-reductase inhibitors. Some steroids like progesterone have been tested for this, but its rapid metabolism makes it ineffective in vivo. To be active, the 5α-reductase inhibitor must be stable enough to block the activity of the enzyme in vitro. Finasteride, a competitive steroidal inhibitor, fulfills this condition, but it is more active on the type 2 isoenzyme than on the type 1 isoenzyme and these two isoenzymes have only 50% homology on the sequence of their acids. amines. It is therefore especially in benign prostatic hyperplasia that finasteride has already been tested. Furthermore, the Serenoa Repens extract is also known, as a reference as a 5α-reductase inhibitor, the Serenoa Repens extract having the advantage, compared to the finasteride, of being of natural origin in as a plant extract allowing a better comparison for tested products also of natural origin. Serenoa Repens, also known as Sabal serrulatum, is a small palm that can be found in the United States (Florida) in North Africa and in Spain.
La demanderesse a maintenant trouvé de manière tout à fait surprenante et inattendue que l'utilisation de l'huile extraite de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica permettait d'obtenir un effet remarquable d'inhibition de l'activité de la 5α-réductase, procurant ainsi notamment une nouvelle réponse pour le traitement des pathologies et/ou désordres dermatologiques évoqués ci-dessus. L'huile selon la présente invention peut ainsi être incorporée dans une composition pharmaceutique, dans un produit alimentaire ou dans un complément alimentaire, ou encore dans une composition cosmétique.The Applicant has now found, quite surprisingly and unexpectedly, that the use of the oil extracted from cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica allows a remarkable inhibition effect to be obtained. the activity of 5α-reductase, thus in particular providing a new response for the treatment of the dermatological pathologies and / or disorders mentioned above. The oil according to the present invention can thus be incorporated into a pharmaceutical composition, into a food product or into a food supplement, or even into a cosmetic composition.
La présente invention a ainsi pour objet l'utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, pour la préparation d'une composition destinée à inhiber l'activité de la 5-alpha reductase.A subject of the present invention is therefore the use of at least one oil of cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, for the preparation of a composition intended to inhibit the activity of 5-alpha reductase.
L'utilisation de l'huile des graines de cucurbitacées pour préparer une composition selon la présente invention destinée à inhiber l'isoenzyme de type 1 et/ou
l'isoenzyme de type 2 de la 5α-réductase est particulièrement avantageuse selon la présente invention.The use of cucurbit seed oil to prepare a composition according to the present invention intended to inhibit the type 1 isoenzyme and / or the type 2 isoenzyme of 5α-reductase is particularly advantageous according to the present invention.
Selon la présente invention, la composition est avantageusement destinée à un usage externe topique. Elle peut par ailleurs contenir un support cosmétiquement acceptable.According to the present invention, the composition is advantageously intended for topical external use. It may also contain a cosmetically acceptable support.
La composition qui est mise en œuvre avantageusement selon la présente invention peut se présenter sous toutes les formes galéniques usuellement utilisées pour une application externe topique. Avantageusement selon la présente invention, la composition se présente sous forme d'une solution aqueuse, hydroalcoolique ou huileuse, d'une émulsion huile-dans-eau ou eau-dans-huile ou multiple, d'un gel aqueux ou huileux, d'un produit anhydre liquide, pâteux ou solide, ou d'une dispersion d'huile dans une phase aqueuse à l'aide de sphérules, les sphérules pouvant être des nanoparticules polymériques telles que les nanosphères et les nanocapsules ou mieux des vésicules lipidiques de type ionique et/ou non-ionique. La composition peut être plus ou moins fluide, se présenter sous forme de crème blanche ou colorée, de pommade, de lait, de lotion, d'onguent, de sérum, de pâte, de mousse, d'aérosol ou de stick.The composition which is advantageously used according to the present invention can be in all the dosage forms usually used for a topical external application. Advantageously according to the present invention, the composition is in the form of an aqueous, hydroalcoholic or oily solution, an oil-in-water or water-in-oil or multiple emulsion, an aqueous or oily gel, a liquid, pasty or solid anhydrous product, or an oil dispersion in an aqueous phase using spherules, the spherules possibly being polymeric nanoparticles such as nanospheres and nanocapsules or better lipid vesicles of ionic type and / or non-ionic. The composition can be more or less fluid, be in the form of a white or colored cream, ointment, milk, lotion, ointment, serum, paste, foam, aerosol or stick.
La composition mise en œuvre selon la présente invention peut par ailleurs contenir les adjuvants habituels dans le domaine cosmétique, tels que les gélifiants hydrophiles ou lipophiles, les actifs hydrophiles ou lipophiles, les conservateurs, les antioxydants, les solvants, les parfums, les charges, les filtres, les pigments, les agents chélateurs, les absorbeurs d'odeur et les matières colorantes. Les quantités de ces différents adjuvants sont celles classiquement utilisées en cosmétique, et par exemple de 0,01% à 20% en poids, par rapport au poids total de la composition. Ces adjuvants, selon leur nature, peuvent être introduits dans la phase grasse, dans la phase aqueuse, dans les vésicules lipidiques et/ou dans les nanoparticules.The composition used according to the present invention may also contain the adjuvants customary in the cosmetic field, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters, pigments, chelating agents, odor absorbers and coloring matters. The amounts of these various adjuvants are those conventionally used in cosmetics, and for example from 0.01% to 20% by weight, relative to the total weight of the composition. These adjuvants, depending on their nature, can be introduced into the fatty phase, into the aqueous phase, into the lipid vesicles and / or into the nanoparticles.
Lorsque la composition selon la présente invention est une émulsion, la proportion de la phase grasse peut aller de 5% à 80% en poids, et de préférence de 5% à 50% en poids, par rapport au poids total de la composition. Les huiles, les émulsionnants et les coémulsionnants utilisés dans la composition sous forme d'émulsion sont choisis parmi ceux classiquement utilisés dans le domaine considéré.
L'émulsionnant et le coémulsionnant sont présents, dans la composition, en une proportion allant de 0,3 % à 30 % en poids, et de préférence de 0,5 % à 20 % en poids, par rapport au poids total de la composition.When the composition according to the present invention is an emulsion, the proportion of the fatty phase can range from 5% to 80% by weight, and preferably from 5% to 50% by weight, relative to the total weight of the composition. The oils, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the field under consideration. The emulsifier and the coemulsifier are present in the composition in a proportion ranging from 0.3% to 30% by weight, and preferably from 0.5% to 20% by weight, relative to the total weight of the composition .
Parmi les huiles utilisables selon la présente invention, on peut citer notamment les huiles minérales, d'autres huiles d'origine végétale (huile d'abricot, huile de tournesol, de prune), les huiles d'origine animale, les huiles de synthèse, les huiles siliconées et les huiles fluorées (perfluoropolyéthers). Des alcools gras, tels que l'alcool cétylique, des acides gras, ou des cires telles que la cire d'abeilles peuvent également être utilisées en tant que matières grasses selon la présente invention. Parmi les émulsionnants et coémulsionnants utilisables selon la présente invention, on peut citer notamment les esters d'acide gras et de polyéthylène glycol, tels que le stéarate de PEG-40 ou le stéarate de PEG-100, les esters d'acide gras et de polyol, tels que le stéarate de glycéryle et le tristéarate de sorbitane.Among the oils which can be used according to the present invention, there may be mentioned in particular mineral oils, other oils of vegetable origin (apricot oil, sunflower oil, plum oil), oils of animal origin, synthetic oils , silicone oils and fluorinated oils (perfluoropolyethers). Fatty alcohols, such as cetyl alcohol, fatty acids, or waxes such as beeswax can also be used as fats according to the present invention. Among the emulsifiers and coemulsifiers which can be used according to the present invention, there may be mentioned in particular fatty acid esters of polyethylene glycol, such as PEG-40 stearate or PEG-100 stearate, esters of fatty acid and of polyol, such as glyceryl stearate and sorbitan tristearate.
Parmi les gélifiants hydrophiles utilisables selon la présente invention, peuvent notamment être cités les polymères carboxyvmyliques (carbomère), les copolymères acryliques tels que les copolymères d'acrylate/alkylacrylate, les polyacrylamides, les polysaccharides, les gommes naturelles et les argiles. Parmi les gélifiants lipophiles, peuvent notamment être cités les argiles modifiées telles que les bentones, les sels métalliques d'acides gras, la silice hydrophobe et les polyéthylènes. Avantageusement selon la présente invention, la composition contient en outre au moins un composé choisi dans le groupe constitué par les actifs hydrophiles, les actifs lipophiles, les agents modulant la différenciation et/ou la prolifération et/ou la pigmentation cutanée, les agents antibactériens, les agents modulant l'adhésion bactérienne sur la peau et/ou les muqueuses, les agents antifongiques, les agents apaisants, les agents anti-prurigineux, les agents kératolytiques, les agents antiradicaux libres, les agents anti-séborrhéiques, les agents anti-pelliculaires, les agents présentant une activité anti-acnéique, les agents anti-irritants, les agents hydratants, les vitamines, les agents anti-inflammatoires, les filtres UNA et UVB, les agents matifiants, les pigments réflecteurs de lumière, les actifs antirides, les agents anti- glycation, les modulateurs de Heat Shock Protein et les inhibiteurs enzymatiques.Among the hydrophilic gelling agents which can be used according to the present invention, mention may in particular be made of carboxyvinyl polymers (carbomer), acrylic copolymers such as acrylate / alkylacrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays. Among the lipophilic gelling agents, mention may in particular be made of modified clays such as bentones, metal salts of fatty acids, hydrophobic silica and polyethylenes. Advantageously according to the present invention, the composition also contains at least one compound chosen from the group consisting of hydrophilic active agents, lipophilic active agents, agents modulating differentiation and / or proliferation and / or skin pigmentation, antibacterial agents, agents modulating bacterial adhesion to the skin and / or mucous membranes, antifungal agents, soothing agents, anti-pruritic agents, keratolytic agents, free anti-radical agents, anti-seborrheic agents, anti-dandruff agents , agents with anti-acne activity, anti-irritant agents, moisturizing agents, vitamins, anti-inflammatory agents, UNA and UVB filters, matting agents, light-reflecting pigments, anti-wrinkle active agents, anti-glycation agents, Heat Shock Protein modulators and enzyme inhibitors.
Parmi les actifs hydrophiles utilisables selon la présente invention, on peut citer notamment les protéines ou les hydrolysats de protéine, les peptides tels que les
peptides de lupin, les acides aminés, les polyols, l'urée, l'allantoine, les sucres et leurs dérivés, les vitamines hydrosolubles, les extraits végétaux et les hydroxy-acides.Among the hydrophilic active agents which can be used according to the present invention, mention may in particular be made of proteins or protein hydrolysates, peptides such as lupine peptides, amino acids, polyols, urea, allantoin, sugars and their derivatives, water-soluble vitamins, plant extracts and hydroxy acids.
Parmi les actifs lipophiles utilisables selon la présente invention, on peut citer notamment le rétinol (vitamine A) et ses dérivés, le tocophérol (vitamine E) et ses dérivés, les acides gras essentiels, les céramides, les huiles essentielles, l'acide salicylique et ses dérivés.Among the lipophilic active agents which can be used according to the present invention, there may be mentioned in particular retinol (vitamin A) and its derivatives, tocopherol (vitamin E) and its derivatives, essential fatty acids, ceramides, essential oils, salicylic acid and its derivatives.
La composition mise en œuvre selon la présente invention peut également contenir d'autres agents actifs destinés notamment à la prévention et/ou au traitement des affections cutanées. Parmi ces agents actifs, on peut citer notamment les agents modulant la différenciation et/ou la prolifération et/ou la pigmentation cutanée tels que l'acide rétinoique et ses isomères, le rétinol et ses esters, la vitamine D et ses dérivés, les phyto-oestrogènes et l'acide kojique ; les agents antibactériens tels que l'octanediol et les conservateurs classiques (ammonium quaternaire,...) ; les agents modulant l'adhésion bactérienne sur la peau et/ou les muqueuses tels que certains dérivés de sucres ; les agents antifongiques, en particulier les composés appartenant à la classe des imidazoles ou leurs sels, les composés de la famille des allylamines, les dérivés de glycine (hydroxyméthylglycinate de sodium par exemple), la piroctone olamine ou encore l'octopirox ; les agents apaisants tels que l'acide salicylique, le lupeol, l'allantoine, l'eau de bleuet, le Silanediol Salicylate, les dérivés de réglisse et Penexolone.The composition used according to the present invention may also contain other active agents intended in particular for the prevention and / or treatment of skin conditions. Among these active agents, there may be mentioned in particular agents modulating differentiation and / or proliferation and / or skin pigmentation such as retinoic acid and its isomers, retinol and its esters, vitamin D and its derivatives, phyto -estrogens and kojic acid; antibacterial agents such as octanediol and conventional preservatives (quaternary ammonium, ...); agents modulating bacterial adhesion to the skin and / or mucous membranes such as certain sugar derivatives; antifungal agents, in particular compounds belonging to the class of imidazoles or their salts, compounds of the allylamine family, glycine derivatives (sodium hydroxymethylglycinate for example), piroctone olamine or even octopirox; soothing agents such as salicylic acid, lupeol, allantoin, blueberry water, Silanediol Salicylate, licorice derivatives and Penexolone.
Parmi les agents actifs destinés notamment à la prévention et/ou au traitement des affections cutanées éventuellement présents dans la composition selon la présente invention, peuvent également être cités : les agents anti-prurigineux comme la glycine ; les agents kératolytiques tels que les acides alpha et bêta-hydroxycarboxyliques ou bêta-cétocarboxyliques, leurs sels, amides ou esters et plus particulièrement les hydroxy-acides tels que l'acide glycolique, l'acide lactique, l'acide salicylique, l'acide citrique et de manière générale les acides de fruits ; les agents anti-radicaux libres, tels que l'alpha-tocophérol ou ses esters, les caroténoïdes, les isoflavones, les OPC, les flavonoïdes, les superoxyde dismutases, certains chélatants de métaux ou l'acide ascorbique et ses esters ; les agents anti-séborrhéiques tels que les rétinoïdes, le sabal, l'extrait de Pygeum Africanum, les sels de zinc.
Peuvent également être ajoutés en tant qu'agents actifs destinés notamment à la prévention et/ou au traitement des affections cutanées dans la composition selon la présente invention, les agents anti-pelliculaires tels que l'octopirox, la pyrithione de zinc ou la piroctone olamine ; les agents présentant une activité anti-acnéique tels que les rétinoïdes, le rétinol, le rétinaldéhyde, les vitamines PP, les peroxydes de benzoyle, l'erythromycine ; les agents anti-irritants tels que les eaux thermales, les polysaccharides, en particulier vis-à-vis de composés irritants éventuellement présents dans les compositions de la présente invention ; les agents hydratants tels que les polyols (par exemple la glycérine) ; les vitamines (par exemple le D-panthénol ou les vitamines C, D, B6) ; les agents anti-inflammatoires tels que les eaux thermales, les polysaccharides ; les filtres UNA et UNB de type écrans organiques et minéraux ; les agents matifiants et les pigments réflecteurs de lumière tels que des mélanges de titane et de mica ; les actifs antirides tels que le rétinol et ses dérivés (rétinaldéhyde) ; les agents anti-glycation ; les modulateurs de Heat Shock Protein ; et les inhibiteurs enzymatiques.Among the active agents intended in particular for the prevention and / or treatment of skin conditions possibly present in the composition according to the present invention, the following may also be mentioned: anti-pruritic agents such as glycine; keratolytic agents such as alpha and beta-hydroxycarboxylic or beta-ketocarboxylic acids, their salts, amides or esters and more particularly hydroxy acids such as glycolic acid, lactic acid, salicylic acid, acid citric and in general fruit acids; anti-free radical agents, such as alpha-tocopherol or its esters, carotenoids, isoflavones, OPCs, flavonoids, superoxide dismutases, certain metal chelators or ascorbic acid and its esters; anti-seborrheic agents such as retinoids, sabal, Pygeum Africanum extract, zinc salts. Can also be added as active agents intended in particular for the prevention and / or treatment of skin conditions in the composition according to the present invention, anti-dandruff agents such as octopirox, zinc pyrithione or piroctone olamine ; agents having anti-acne activity such as retinoids, retinol, retinaldehyde, vitamins PP, benzoyl peroxides, erythromycin; anti-irritant agents such as thermal waters, polysaccharides, in particular with regard to irritant compounds possibly present in the compositions of the present invention; moisturizers such as polyols (eg glycerin); vitamins (for example D-panthenol or vitamins C, D, B6); anti-inflammatory agents such as thermal waters, polysaccharides; UNA and UNB filters of the organic and mineral screen type; mattifying agents and light-reflecting pigments such as mixtures of titanium and mica; anti-wrinkle active ingredients such as retinol and its derivatives (retinaldehyde); anti-glycation agents; Heat Shock Protein modulators; and enzyme inhibitors.
Dans un mode de réalisation particulier selon la présente invention, l'huile des graines de cucurbitacées est susceptible d'être obtenue selon le procédé consistant à extraire les lipides totaux des graines de cucurbitacées préalablement séchées et broyées, à l'aide d'un solvant des huiles, puis à évaporer le solvant.In a particular embodiment according to the present invention, the oil of the seeds of cucurbits is capable of being obtained according to the method consisting in extracting the total lipids from the seeds of cucurbits previously dried and ground, using a solvent oils, then evaporate the solvent.
Les graines de cucurbitacées selon la présente invention sont broyées par exemple à l'aide d'un broyeur à cylindre ou à marteaux. Le solvant des huiles, utilisé pour extraire les lipides totaux des graines formant l'huile, est un solvant organique classique d'extraction de lipides. Le solvant est avantageusement choisi dans le groupe constitué par les alcanes aliphatiques, les alcanes aromatiques, les alcools aliphatiques et leurs dérivés halogènes. De manière encore plus avantageuse selon la présente invention, le solvant organique est Phexane. L'extraction des lipides totaux des graines de cucurbitacées est avantageusement réalisée par une extraction au soxhlet qui est une technologie bien connue de l'homme de métier. Après extraction des lipides contenus dans les graines de cucurbitacées selon la présente invention, le solvant organique est évaporé, de préférence par évaporation sous vide.
Dans un autre mode de réalisation particulier selon la présente invention, l'huile des graines de cucurbitacées est susceptible d'être obtenue selon le procédé consistant à extraire les lipides des graines de cucurbitacées par pression mécanique des graines à froid, avantageusement à l'aide d'une presse à vis continue, pour conduire, après filtration, à des huiles vierges de première pression.The cucurbit seeds according to the present invention are ground for example using a cylinder or hammer mill. The solvent for oils, used to extract the total lipids from the seeds forming the oil, is a conventional organic solvent for extracting lipids. The solvent is advantageously chosen from the group consisting of aliphatic alkanes, aromatic alkanes, aliphatic alcohols and their halogen derivatives. Even more advantageously according to the present invention, the organic solvent is hexane. The extraction of the total lipids from the seeds of cucurbits is advantageously carried out by a soxhlet extraction which is a technology well known to those skilled in the art. After extraction of the lipids contained in the seeds of cucurbits according to the present invention, the organic solvent is evaporated, preferably by evaporation under vacuum. In another particular embodiment according to the present invention, the oil of the cucurbit seeds is capable of being obtained according to the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure of the seeds cold, advantageously using of a continuous screw press, to lead, after filtration, to virgin oils of first pressure.
Les huiles de cucurbitacées selon la présente invention peuvent être utilisées brutes ou raffinées. Par raffinage, on entend au sens de la présente invention, les opérations unitaires de purification des lipides d'origine végétale bien connues de l'homme de métier, parmi lesquelles on peut citer notamment la neutralisation chimique, la démucilagination, la décoloration, la désodorisation et la frigélisation.The cucurbit oils according to the present invention can be used raw or refined. By refining, is meant within the meaning of the present invention, the unitary operations for the purification of lipids of plant origin well known to those skilled in the art, among which there may be mentioned in particular chemical neutralization, degumming, bleaching, deodorization and refrigeration.
Avantageusement selon la présente invention, l'huile extraite des graines de cucurbitacées est présente à une concentration comprise entre 0,01 et 95 %, de préférence entre 0,1 et 30 % en poids, par rapport au poids total de la composition.Advantageously according to the present invention, the oil extracted from the seeds of cucurbits is present at a concentration of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
Avantageusement selon la présente invention, la composition préparée en utilisant l'huile des graines de cucurbitacées est destinée au traitement des pathologies et/ou des désordres cutanés liés à une exagération congénitale ou acquise de l'activité de la 5α-réductase. De manière encore plus avantageuse selon la présente invention, la composition est destinée au traitement de l'hypertrophie prostatique, de l'adénome prostatique, de l'acné, de l'hyperséborrhée, de l'alopécie ou de l'hirsutisme.Advantageously according to the present invention, the composition prepared using the oil of the seeds of cucurbits is intended for the treatment of pathologies and / or skin disorders linked to a congenital exaggeration or acquired from the activity of 5α-reductase. Even more advantageously according to the present invention, the composition is intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
La composition mise en œuvre selon la présente invention peut être une composition cosmétique, pharmaceutique, dermatologique ou nutraceutique. Dans un mode de réalisation particulier selon la présente invention, la composition est une composition pharmaceutique ou dermatologique. Contrairement aux méthodes de traitement cosmétique selon la présente invention selon lesquelles l'hyperséborrhée, l'alopécie ou encore l'hirsutisme ne sont pas d'origine pathologique et se manifestent par des phénomènes esthétiquement gênants sur la peau et/ou les cheveux, l'utilisation thérapeutique de l'huile selon la présente invention permet de traiter des formes d'acné, d'hyperséborrhée, d'alopécie ou d'hirsutisme présentant un caractère pathologique.
La présente invention a également pour objet l'utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, pour la préparation d'une composition, avantageusement pharmaceutique ou dermatologique, destinée au traitement de l'hypertrophie prostatique, de l'adénome prostatique, de l'acné, de l'hyperséborrhée, de l'alopécie ou de l'hirsutisme.The composition used according to the present invention can be a cosmetic, pharmaceutical, dermatological or nutraceutical composition. In a particular embodiment according to the present invention, the composition is a pharmaceutical or dermatological composition. Unlike the cosmetic treatment methods according to the present invention according to which hyperseborrhea, alopecia or even hirsutism are not of pathological origin and are manifested by aesthetically annoying phenomena on the skin and / or the hair, the therapeutic use of the oil according to the present invention makes it possible to treat forms of acne, hyperseborrhea, alopecia or hirsutism having a pathological character. The present invention also relates to the use of at least one seed oil of cucurbits chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, for the preparation of a composition, advantageously pharmaceutical or dermatological, intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
La présente invention a également pour objet une méthode de traitement cosmétique, caractérisée en ce qu'on applique sur la peau, les muqueuses, les ongles ou les cheveux au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, afin d'inhiber l'activité de la 5α-réductase.The present invention also relates to a cosmetic treatment method, characterized in that one applies to the skin, mucous membranes, nails or hair at least one oil of cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in order to inhibit the activity of 5α-reductase.
Avantageusement selon la méthode de traitement cosmétique de la présente invention, on applique la composition cosmétique sur la peau grasse et/ou sur les cheveux gras, sur la peau luisante et/ou sur les cheveux luisants, sur la peau présentant des boutons, des points noirs, ou des comédons, sur la peau grasse à tendance acnéique, sur la peau grasse à imperfections, sur les zones du cuir chevelu affectées d'alopécie ou sur les zones de la peau présentant des excès de pilosité.Advantageously according to the cosmetic treatment method of the present invention, the cosmetic composition is applied to oily skin and / or to oily hair, to shiny skin and / or to shiny hair, on the skin having pimples, dots. black, or blackheads, on oily skin prone to acne, on oily skin with imperfections, on the areas of the scalp affected by alopecia or on the areas of the skin with excess hairiness.
En effet, selon la présente invention, à l'opposé des traitements médicaux hormonaux, les méthodes de traitement cosmétique de la peau ou des cheveux gras et/ou luisants, de la peau présentant des boutons, des points noirs, ou des comédons, de la peau grasse à tendance acnéique ou à imperfections, des zones du cuir chevelu affectées d'alopécie ou des zones de la peau présentant des excès de pilosité permettent d'améliorer l'apparence de l'être humain en réduisant de manière visible les phénomènes disgracieux et esthétiquement gênants liés à l'hyperséborrhée, qui donne notamment un aspect gras et/ou luisant à la peau et/ou aux cheveux et qui peut provoquer l'apparition de boutons, comédons ou points noirs, à l'alopécie qui se manifeste par une chute des cheveux ou des poils et à l'hirsutisme qui se manifeste par des excès de pilosités. Il s'agit ici des cas où l'hyperséborrhée, l'alopécie ou encore
l'hirsutisme ne sont pas d'origine pathologique, mais proviennent par exemple, dans le cas de l'alopécie, des agressions extérieures (décoloration, teinture) ou encore de la vieillesse.In fact, according to the present invention, in contrast to hormonal medical treatments, the cosmetic treatment methods for oily and / or shiny skin or hair, skin with pimples, blackheads, or blackheads, oily skin prone to acne or blemishes, areas of the scalp affected by alopecia or areas of the skin with excess hair growth make it possible to improve the appearance of human beings by visibly reducing unsightly phenomena and aesthetically annoying linked to hyperseborrhea, which gives in particular a greasy and / or shiny appearance to the skin and / or hair and which can cause the appearance of pimples, blackheads or blackheads, alopecia which manifests itself by hair loss or hirsutism which is manifested by excess body hair. These are cases where hyperseborrhea, alopecia or hirsutism is not of pathological origin, but comes, for example, in the case of alopecia, external aggressions (discoloration, dyeing) or even old age.
Enfin, la présente invention a pour objet l'utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, dans une composition nutraceutique ou un aliment pour l'être humain et/ou l'animal en tant qu'additif agissant pour inhiber l'activité de la 5-alpha reductase. Selon un mode de réalisation avantageux de l'utilisation selon la présente invention, l'huile des graines de cucurbitacées est extraite selon le procédé consistant à extraire les lipides totaux des graines de cucurbitacées préalablement séchées et broyées, à l'aide d'un solvant des huiles, avantageusement par une extraction au soxhlet, puis à évaporer ledit solvant ou selon le procédé consistant à extraire les lipides des graines de cucurbitacées par pression mécanique des graines à froid, avantageusement à l'aide d'une presse à vis continue, pour conduire, après filtration, à des huiles vierges de première pression.Finally, the subject of the present invention is the use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in a nutraceutical composition or a food for humans and / or animals as an additive acting to inhibit the activity of 5-alpha reductase. According to an advantageous embodiment of the use according to the present invention, the oil of the seeds of cucurbits is extracted according to the process consisting in extracting the total lipids from the seeds of cucurbits previously dried and ground, using a solvent oils, advantageously by extraction with a soxhlet, then evaporating the said solvent or by the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure from the seeds when cold, advantageously using a continuous screw press, to lead, after filtration, to virgin oils of first pressure.
Selon un autre mode de réalisation avantageux de l'utilisation selon la présente invention, l'huile extraite des graines de cucurbitacées est utilisée selon une proportion comprise entre 0,01 et 95 %, de préférence entre 0,1 et 30 % en poids, par rapport au poids total de la composition.According to another advantageous embodiment of the use according to the present invention, the oil extracted from the seeds of cucurbits is used in a proportion of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
Les exemples suivants sont donnés à titre non limitatif et illustrent la présente invention. A moins qu'il n'en soit précisé autrement, les pourcentages indiqués dans les exemples suivants sont des pourcentages en poids. Dans les exemples suivants, toutes les huiles de graines de cucurbitacées ont été extraites par Phexane, en partant d'une quantité d'environ 500 g de graines de cucurbitacées.The following examples are given without limitation and illustrate the present invention. Unless otherwise specified, the percentages given in the following examples are percentages by weight. In the following examples, all the cucurbit seed oils were extracted with Phexane, starting from an amount of about 500 g of cucurbit seeds.
Exemple 1 : Composition de l'huile extraite de graines de cucurbitacées
Exemple 1.1 : composition de l'huile extraite des graines de calebasses bouteille, gale et longue (Lagenaria leucaritha)Example 1 Composition of the Oil Extracted from Cucurbit Seeds Example 1.1: composition of the oil extracted from the seeds of bottle, scab and long calabash (Lagenaria leucaritha)
Exemple 1.2 : composition de l'huile extraite des graines de pipangailles lisse (Luffa cylindrica) et à côtes (Luffa acutangula) et de margoze (Momordica charantia)Example 1.2: composition of the oil extracted from the seeds of smooth pipangailles (Luffa cylindrica) and ribbed (Luffa acutangula) and margoze (Momordica charantia)
Exemple 2 : Compositions cosmétiques
Exemple 2.1 : Crème pour peaux à tendance acnéique n°lExample 2 Cosmetic Compositions Example 2.1 Cream for Acne-prone Skin No. 1
% en poids% in weight
Eau QSP 100Water QSP 100
Isononanoate d'Isononyle 7 Malate de di-C12-13 Alkyle 7Isononyle Isononanoate 7 di-C12-13 Malate Alkyl 7
Stéarate d'Isocétyle 5Isocetyl 5 stearate
Butylène Glycol 3Butylene Glycol 3
Oriza Sativa 2,5Oriza Sativa 2.5
Huile de margoze 0,1 à 30 Ether de Dicaprylyle 2Margoze oil 0.1 to 30 Dicaprylyle ether 2
Salicylate de Silanediol 2Silanediol salicylate 2
Alcool arachidylique ,6Arachidyl alcohol, 6
Trométhamine ,2Tromethamine, 2
Alcool cétylique Acide SalicyliqueCetyl alcohol Salicylic acid
Glucoside d'ascorbyleAscorbyle glucoside
Glycinewistaria
Acétate deTocophéryleTocopheryl acetate
Alcool Béhénylique 0,9 Squalane 0,8Behenyl Alcohol 0.9 Squalane 0.8
Citrate de Sodium 0,7Sodium Citrate 0.7
Copolymère PPG-12/SMDI 0,5PPG-12 / SMDI 0.5 copolymer
Glucoside d'Arachidyle 0,4Arachidyl glucoside 0.4
Parfum 0,4 Gomme de sclérote 0,2Perfume 0.4 Sclerotia gum 0.2
Alcool cétéarylique 0,1Cetearyl alcohol 0.1
Acide citrique 0,1Citric acid 0.1
Sepigel 305* 0,1Sepigel 305 * 0.1
Système conservateur QS *produit commercialisé par la société Seppic
Exemple 2.2 : Crème pour peaux à tendance acnéique n°2QS preservative system * product marketed by Seppic Example 2.2 Cream for Acne-prone Skin No. 2
% en poids% in weight
Eau QSP 100Water QSP 100
Isononanoate d'Isononyle 7 Malate de di-C12-13 Alkyle 7Isononyle Isononanoate 7 di-C12-13 Malate Alkyl 7
Stéarate d'Isocétyle 5Isocetyl 5 stearate
Butylène Glycol 3Butylene Glycol 3
Oriza Sativa 2,5Oriza Sativa 2.5
Huile de pipangaille lisse 0,1 à 30 Ether de Dicaprylyle 2Smooth pipangaille oil 0.1 to 30 Dicaprylyle ether 2
Salicylate de Silanediol 2Silanediol salicylate 2
Alcool arachidylique 6Arachidyl alcohol 6
Trométhamine 2Tromethamine 2
Alcool cétylique Acide SalicyliqueCetyl alcohol Salicylic acid
Glucoside d'ascorbyleAscorbyle glucoside
Glycinewistaria
Acétate deTocophéryleTocopheryl acetate
Alcool Béhénylique 0,9 Squalane 0,8Behenyl Alcohol 0.9 Squalane 0.8
Citrate de Sodium 0,7Sodium Citrate 0.7
Copolymère PPG-12/SMDI 0,5PPG-12 / SMDI 0.5 copolymer
Glucoside d'Arachidyle 0,4Arachidyl glucoside 0.4
Parfum 0,4 Gomme de sclérote 0,2Perfume 0.4 Sclerotia gum 0.2
Alcool cétéarylique 0,1Cetearyl alcohol 0.1
Acide citrique 0,1Citric acid 0.1
Sepigel 305* 0,1Sepigel 305 * 0.1
Système conservateur QS *produit commercialisé par la société Seppic
Exemple 2.3 : Crème pour peaux à tendance acnéique n°3QS preservative system * product marketed by Seppic EXAMPLE 2.3 Cream for Acne-Prone Skins No. 3
% en poids% in weight
Eau QSP 100Water QSP 100
Isononanoate d'Isononyle 7 Malate de di-C12-13 Alkyle 7Isononyle Isononanoate 7 di-C12-13 Malate Alkyl 7
Stéarate d'Isocétyle 5Isocetyl 5 stearate
Butylène Glycol 3Butylene Glycol 3
Oriza Sativa 2,5Oriza Sativa 2.5
Huile de calebasse bouteille 0,1 à 30 Ether de Dicaprylyle 2Calabash oil bottle 0.1 to 30 Ether of Dicaprylyle 2
Salicylate de Silanediol 2Silanediol salicylate 2
Alcool arachidylique 6Arachidyl alcohol 6
Trométhamine 2Tromethamine 2
Alcool cétylique Acide SalicyliqueCetyl alcohol Salicylic acid
Glucoside d'ascorbyleAscorbyle glucoside
Glycinewistaria
Acétate deTocophéryleTocopheryl acetate
Alcool Béhénylique 0,9 Squalane 0,8Behenyl Alcohol 0.9 Squalane 0.8
Citrate de Sodium 0,7Sodium Citrate 0.7
Copolymère PPG-12/SMDI 0,5PPG-12 / SMDI 0.5 copolymer
Glucoside d'Arachidyle 0,4Arachidyl glucoside 0.4
Parfum 0,4 Gomme de sclérote 0,2Perfume 0.4 Sclerotia gum 0.2
Alcool cétéarylique 0,1Cetearyl alcohol 0.1
Acide citrique 0,1Citric acid 0.1
Sepigel 305* 0,1Sepigel 305 * 0.1
Système conservateur QS *produit commercialisé par la société Seppic
Exemple 2.4 : Emulsion moussante lavante pour peaux à tendance acnéique n°lQS preservative system * product marketed by Seppic Example 2.4: Foaming washing emulsion for acne-prone skin No. 1
% en poids% in weight
Eau QSP 100Water QSP 100
Arlatone duo* 20 Glucoside de noix de coco 12Arlatone duo * 20 Glucoside of coconut 12
Guar Hydroxypropylé 2Guar Hydroxypropylé 2
Huile de margoze 0,1 à 30Margoze oil 0.1 to 30
Palmate de PEG-200 Glycéryle hydrogéné 1,1PEG-200 palmate Hydrogenated glyceryl 1.1
Cocoate de PEG-7 Glycéryle 1,1 Salicylate de Silanediol 1PEG-7 cocoate Glyceryl 1,1 Silanediol salicylate 1
Cocamide DEA 1Cocamide DEA 1
Glycine de Caprylyole 0,5Caprylyole glycine 0.5
Sorbate de Potassium 0,5Potassium Sorbate 0.5
Polyquaternium 10 0,4 Parfum 0,4Polyquaternium 10 0.4 Perfume 0.4
Acide citrique 0,3Citric acid 0.3
Zinc PCA 0,2Zinc PCA 0.2
*produit commercialisé par la société Quimasso* product marketed by Quimasso
Exemple 2.5 : Emulsion moussante lavante pour peaux à tendance acnéique n°2EXAMPLE 2.5 Washing Foaming Emulsion for Acne-Prone Skins No. 2
% en poids% in weight
Eau QSP 100Water QSP 100
Arlatone duo* 20Arlatone duo * 20
Glucoside de noix de coco 12 Guar Hydroxypropylé 2Coconut glucoside 12 Guar Hydroxypropylé 2
Huile de calebasse longue 0,1 à 30Calabash oil long 0.1 to 30
Palmate de PEG-200 Glycéryle hydrogéné 1,1PEG-200 palmate Hydrogenated glyceryl 1.1
Cocoate de PEG-7 Glycéryle 1 , 1PEG-7 Glyceryl Cocoate 1, 1
Salicylate de Silanediol 1 Cocamide DEA 1Silanediol salicylate 1 Cocamide DEA 1
Glycine de Caprylyole 0,5Caprylyole glycine 0.5
Sorbate de Potassium 0,5
Polyquaternium 10 0,4Potassium Sorbate 0.5 Polyquaternium 10 0.4
Parfum 0,4Perfume 0.4
Acide citrique 0,3Citric acid 0.3
Zinc PCA 0,2 *produit commercialisé par la société QuimassoZinc PCA 0.2 * product marketed by the company Quimasso
Exemple 2.6 : Emulsion moussante lavante pour peaux à tendance acnéique n°3Example 2.6: Foaming washing emulsion for acne-prone skin no. 3
% en poids% in weight
Eau QSP 100 Arlatone duo* 20Eau QSP 100 Arlatone duo * 20
Glucoside de noix de coco 12Coconut glucoside 12
Guar Hydroxypropylé 2Guar Hydroxypropylé 2
Huile de pipangaille à côtes 0,1 à 30Rib pipangaille oil 0.1 to 30
Palmate de PEG-200 Glycéryle hydrogéné 1 , 1 Cocoate de PEG-7 Glycéryle 1 , 1PEG-200 palmate Hydrogenated glyceryl 1, 1 PEG-7 cocoate Glyceryl 1, 1
Salicylate de Silanediol 1Silanediol salicylate 1
Cocamide DEA 1Cocamide DEA 1
Glycine de Caprylyole 0,5Caprylyole glycine 0.5
Sorbate de Potassium 0,5 Polyquaternium 10 0,4Potassium Sorbate 0.5 Polyquaternium 10 0.4
Parfum 0,4Perfume 0.4
Acide citrique 0,3Citric acid 0.3
Zinc PCA 0,2Zinc PCA 0.2
*produit commercialisé par la société Quimasso* product marketed by Quimasso
Exemple 2.7 : Emulsion matiβante n°lExample 2.7: Matting emulsion n ° l
% en poids% in weight
Eau QSP 100Water QSP 100
Malate de di-C12-13 Alkyle 10Di-C12-13 Malate Alkyl 10
Glycérol 5Glycerol 5
Oryza Sativa 4
Huile de margoze 0,1 à 30Oryza Sativa 4 Margoze oil 0.1 to 30
Stéarate de PEG -5 Glycéryle 3,5PEG -5 Glyceryl 3,5 stearate
Sepigel* 2,5Sepigel * 2.5
Butylène Glycol 2,4Butylene Glycol 2.4
Salicylate de Silanediol 2Silanediol salicylate 2
Stéarate de Glycéryle ,5Glyceryl stearate, 5
Cérésine ,5Ceresin, 5
Stéarate de PEG-40 ,5PEG-40 stearate, 5
Stéarate de SorbitaneSorbitan stearate
Nylon-6Nylon-6
Zinc PCAZinc PCA
Alcool cétyliqueCetyl alcohol
Glycol caprylylique 0,6Caprylylic glycol 0.6
Parfum 0,5Perfume 0.5
Piroctone Olamine 0,3Piroctone Olamine 0.3
Pyridoxine HC1 0,2Pyridoxine HC1 0.2
Tocophérol 0,2Tocopherol 0.2
''produit commercialisé par la société Seppic'' product marketed by the company Seppic
Exemple 2.8 : Emulsion matiflante n°2Example 2.8: Matifying emulsion n ° 2
% en poids% in weight
Eau QSP 100Water QSP 100
Malate de di-C12-13 Alkyle 10Di-C12-13 Malate Alkyl 10
Glycérol 5Glycerol 5
Oryza Sativa 4Oryza Sativa 4
Huile de pipangaille lisse 0,1 à 30Smooth pipangaille oil 0.1 to 30
Stéarate de PEG -5 Glycéryle 3,5PEG -5 Glyceryl 3,5 stearate
Sepigel* 2,5Sepigel * 2.5
Butylène Glycol 2,4Butylene Glycol 2.4
Salicylate de Silanediol 2Silanediol salicylate 2
Stéarate de Glycéryle 1,5
Cérésine ,5Glyceryl stearate 1.5 Ceresin, 5
Stéarate de PEG-40 ,5PEG-40 stearate, 5
Stéarate de SorbitaneSorbitan stearate
Nylon-6Nylon-6
Zinc PCAZinc PCA
Alcool cétyliqueCetyl alcohol
Glycol caprylylique 0,6Caprylylic glycol 0.6
Parfum 0,5Perfume 0.5
Piroctone Olamine 0,3Piroctone Olamine 0.3
Pyridoxine HC1 0,2Pyridoxine HC1 0.2
Tocophérol 0,2Tocopherol 0.2
"produit commercialisé par la société Seppic"product marketed by the company Seppic
Exemple 2.9 : Emulsion matiflante n°3Example 2.9: Matifying emulsion n ° 3
% en poids% in weight
Eau QSP 100Water QSP 100
Malate de di-C12-13 Alkyle 10Di-C12-13 Malate Alkyl 10
Glycérol 5Glycerol 5
Oryza Sativa 4Oryza Sativa 4
Huile de calebasse bouteille 0,1 à 30Calabash oil bottle 0.1 to 30
Stéarate de PEG -5 Glycéryle 3,5PEG -5 Glyceryl 3,5 stearate
Sepigel* 2,5Sepigel * 2.5
Butylène Glycol 2,4Butylene Glycol 2.4
Salicylate de Silanediol 2Silanediol salicylate 2
Stéarate de Glycéryle 1,5Glyceryl stearate 1.5
Cérésine 1,5Ceresin 1.5
Stéarate de PEG-40 1,5PEG-40 stearate 1.5
Stéarate de Sorbitane 1Sorbitan 1 stearate
Nylon-6 1Nylon-6 1
Zinc PCA 1Zinc PCA 1
Alcool cétylique 1Cetyl alcohol 1
Glycol caprylylique 0,6
Parfum 0,5Caprylylic glycol 0.6 Perfume 0.5
Piroctone Olamine 0,3Piroctone Olamine 0.3
Pyridoxine HC1 0,2Pyridoxine HC1 0.2
Tocophérol 0,2Tocopherol 0.2
*produit commercialisé par la société Seppic* product marketed by the company Seppic
Exemple 2.10 : Emulsion matiflante teintée n°lExample 2.10: Tinted matifying emulsion No. 1
% en poids% in weight
Eau QSP 100Water QSP 100
Malate de di-C12-13 Alkyle 10Di-C12-13 Malate Alkyl 10
Glycérol 5Glycerol 5
Oryza Sativa 4Oryza Sativa 4
Huile de margoze 0,1 à 30Margoze oil 0.1 to 30
Stéarate de PEG -5 Glycéryle 3,5PEG -5 Glyceryl 3,5 stearate
Sepigel* 2,5Sepigel * 2.5
Butylène Glycol 2,4Butylene Glycol 2.4
Salicylate de Silanediol 2Silanediol salicylate 2
Stéarate de Glycéryle 1,5Glyceryl stearate 1.5
Cérésine 1,5Ceresin 1.5
Stéarate de PEG-40 1,5PEG-40 stearate 1.5
Stéarate de Sorbitane 1Sorbitan 1 stearate
Nylon-6 1Nylon-6 1
Zinc PCA 1Zinc PCA 1
Alcool cétylique 1Cetyl alcohol 1
Glycol caprylylique 0,6Caprylylic glycol 0.6
Parfum 0,5Perfume 0.5
Oxyde de fer brun 0,3Brown iron oxide 0.3
Piroctone Olamine 0,3Piroctone Olamine 0.3
Pyridoxine HC1 0,2Pyridoxine HC1 0.2
Oxyde de fer 0,1Iron oxide 0.1
Tocophérol 0,2Tocopherol 0.2
Oxyde de fer noir 0,1
*produit commercialisé par la société Seppic0.1 black iron oxide * product marketed by the company Seppic
Exemple 2.11 : Emulsion matiflante teintée n°2Example 2.11: Tinted matifying emulsion n ° 2
% en poids Eau QSP 100% by weight Water QSP 100
Malate de di-C12-13 Alkyle 10 Glycérol 5Di-C12-13 Malate Alkyl 10 Glycerol 5
Oryza Sativa 4Oryza Sativa 4
Huile de calebasse bouteille 0,1 à 30 Stéarate de PEG -5 Glycéryle 3,5Calabash oil bottle 0.1 to 30 PEG -5 stearate Glyceryl 3.5
Sepigel* 2,5Sepigel * 2.5
Butylène Glycol 2,4Butylene Glycol 2.4
Salicylate de Silanediol 2Silanediol salicylate 2
Stéarate de Glycéryle 1,5 Cérésine 1,5Glyceryl stearate 1.5 Ceresin 1.5
Stéarate de PEG-40 1,5PEG-40 stearate 1.5
Stéarate de Sorbitane 1Sorbitan 1 stearate
Nylon-6 1Nylon-6 1
Zinc PCA 1 Alcool cétylique 1Zinc PCA 1 Cetyl alcohol 1
Glycol caprylylique 0,6Caprylylic glycol 0.6
Parfum 0,5Perfume 0.5
Oxyde de fer brun 0,3Brown iron oxide 0.3
Piroctone Olamine 0,3 Pyridoxine HC1 0,2Piroctone Olamine 0.3 Pyridoxine HC1 0.2
Oxyde de fer 0,1Iron oxide 0.1
Tocophérol 0,2Tocopherol 0.2
Oxyde de fer noir 0,10.1 black iron oxide
*produit commercialisé par la société Seppic* product marketed by the company Seppic
Exemple 2.12 : Shampooing n°lExample 2.12: Shampoo No. 1
% en poids
Eau QSP 100% in weight Water QSP 100
Lauroamphoacétate de Sodium 11Sodium 11 Lauroamphoacetate
Glucoside de noix de coco 11Coconut glucoside 11
Sulfate de Magnésium Laureth 6Laureth 6 Magnesium Sulfate
Huile de margoze 0,1 à 30Margoze oil 0.1 to 30
Cocoate de PEG-40 Glycéryle 2,4PEG-40 Glyceryl Cocoate 2,4
Distéarate de PEG-150 1,2PEG-150 distearate 1,2
Sulfate de Sodium Coceth 1,1Sodium sulfate Coceth 1.1
Acide salicylique 1Salicylic acid 1
Disodium EDTA 0,3Disodium EDTA 0.3
Parfum 0,2Perfume 0.2
Hydroxyde de Sodium QS pH=6,5Sodium hydroxide QS pH = 6.5
Système conservateur QSQS conservative system
Exemple 2.13 : Shampooing n °2Example 2.13: Shampoo No. 2
% en poids% in weight
Eau QSP 100Water QSP 100
Lauroamphoacétate de Sodium 11Sodium 11 Lauroamphoacetate
Glucoside de noix de coco 11Coconut glucoside 11
Sulfate de Magnésium Laureth 6Laureth 6 Magnesium Sulfate
Huile de calebasse longue 0,1 à 30Calabash oil long 0.1 to 30
Cocoate de PEG-40 Glycéryle 2,4PEG-40 Glyceryl Cocoate 2,4
Distéarate de PEG-150 1,2PEG-150 distearate 1,2
Sulfate de Sodium Coceth 1,1Sodium sulfate Coceth 1.1
Acide salicylique 1Salicylic acid 1
Disodium EDTA 0,3Disodium EDTA 0.3
Parfum 0,2Perfume 0.2
Hydroxyde de Sodium QS pH=6,5Sodium hydroxide QS pH = 6.5
Système conservateur QSQS conservative system
Exemple 2.14 : Shampooing n°3Example 2.14: Shampoo No. 3
% en poids
Eau QSP 100% in weight Water QSP 100
Lauroamphoacétate de Sodium 11Sodium 11 Lauroamphoacetate
Glucoside de noix de coco 11Coconut glucoside 11
Sulfate de Magnésium Laureth 6Laureth 6 Magnesium Sulfate
Huile de pipangaille à côtes 0,1 à 30Rib pipangaille oil 0.1 to 30
Cocoate de PEG-40 Glycéryle 2,4PEG-40 Glyceryl Cocoate 2,4
Distéarate de PEG- 150 1,2PEG-150 distearate 1.2
Sulfate de Sodium Coceth 1,1Sodium sulfate Coceth 1.1
Acide salicylique 1Salicylic acid 1
Disodium EDTA 0,3Disodium EDTA 0.3
Parfum 0,2Perfume 0.2
Hydroxyde de Sodium QS pH=6,5Sodium hydroxide QS pH = 6.5
Système conservateur QSQS conservative system
Exemple 3 : Evaluation in vitro de l'activité de la 5 -reductase de l'huile de margoze sur la conversion de la testostérone en 5 -dihydrotestostérone dans des cultures de fibroblastes dermiques humains normaux.Example 3: In Vitro Evaluation of the Activity of Margoze Oil 5-Reductase on the Conversion of Testosterone to 5-Dihydrotestosterone in Cultures of Normal Human Dermal Fibroblasts.
Abréviations utilisées dans les exemples suivants :Abbreviations used in the following examples:
EtOH : éthanolEtOH: ethanol
DMSO : diméthyl sulfoxydeDMSO: dimethyl sulfoxide
Ml 99 : appellation donnée à un milieu de culture standardMl 99: name given to a standard culture medium
MCF : milieu de culture des fibroblastesMCF: fibroblast culture medium
MEM : appellation donnée au milieu de culture, Minimum Essential médiumMEM: designation given to the culture medium, Minimum Essential medium
MIF : milieu d'incubation des fibroblastesMIF: fibroblast incubation medium
Rf : facteur de rétention relatifRf: relative retention factor
SNF : sérum de veau fœtalSNF: fetal calf serum
5α-DHT : 5α-DiHydroTestostérone
On se propose d'évaluer l'effet de l'huile solide (beurre) extraite de graines de margoze (Momordica charantia) extraite par solvant (hexane) sur l'activité de la 5α- réductase. Un modèle in vitro de cultures de fibroblastes dermiques humains normaux a été retenu. 1. Matériels et méthodes5α-DHT: 5α-DiHydroTestosterone We propose to evaluate the effect of solid oil (butter) extracted from margoze seeds (Momordica charantia) extracted by solvent (hexane) on the activity of 5α-reductase. An in vitro model of normal human dermal fibroblast cultures was chosen. 1. Materials and methods
1.1 Produit à l'essai, produit de référence, et réactifs1.1 Test product, reference product, and reagents
L'huile de margoze a été fournie par les Laboratoires Pharmascience et a été conservée à +4°C jusqu'au moment de son utilisation. Les effets du produit à l'essai ont été comparés à ceux obtenus en présence du Finastéride, utilisé comme produit de référence (Finastéride, principe actif des comprimés CHIBRO-PROSCAR : MERCK SHARP & DOHME CHIBRET).Margoze oil was supplied by Pharmascience Laboratories and was stored at + 4 ° C until the time of use. The effects of the test product were compared with those obtained in the presence of Finasteride, used as a reference product (Finasteride, active ingredient in CHIBRO-PROSCAR tablets: MERCK SHARP & DOHME CHIBRET).
La testostérone radioactive (marquée au tritium en position 1, 2, 6 et 7, activité spécifique 95 Ci/mmol) était fournie par AMERSHAM, la testostérone non- radiomarquée était fournie par SIGMA. Les réactifs de qualité analytique provenaient de chez SIGMA, MERCK, BDH,Radioactive testosterone (labeled with tritium in position 1, 2, 6 and 7, specific activity 95 Ci / mmol) was supplied by AMERSHAM, non-radiolabelled testosterone was supplied by SIGMA. The analytical quality reagents came from SIGMA, MERCK, BDH,
ALDRICH ou CARLO ERBA sauf indication contraire.ALDRICH or CARLO ERBA unless otherwise indicated.
1.2 Système d'essai1.2 Test system
Le milieu de culture des fibroblastes (MCF) était constitué par du MEM/M199 (3:1, v/v) additionné de pénicilline (50 Ul/ml), de streptomycine (50 μg/ml), de bicarbonate de sodium (0,2 %, p/v) et de S VF (10 %, v/v).The fibroblast culture medium (MCF) consisted of MEM / M199 (3: 1, v / v) supplemented with penicillin (50 IU / ml), streptomycin (50 μg / ml), sodium bicarbonate (0 , 2%, w / v) and S VF (10%, v / v).
Le système d'essai était constitué de fibroblastes dermiques humains normaux cultivés en monocouche. Les fibroblastes ont été isolés à partir d'un résidu de plastie abdominale réalisée chez une femme de 30 ans (sujet n°i0006). Les cellules ont été utilisées au troisième passage, elles ont été cultivées jusqu'à confluence des monocouches dans le milieu MCF à 37°C dans une atmosphère humide contenant 5 % de CO2.The test system consisted of normal human dermal fibroblasts grown in a monolayer. The fibroblasts were isolated from a residue of tummy tuck performed in a 30-year-old woman (subject no. I0006). The cells were used in the third passage, they were cultured until the monolayers converge in the MCF medium at 37 ° C. in a humid atmosphere containing 5% CO 2 .
1.3 Préparation des produits et incubation avec le système d'essai Le milieu d'incubation des fibroblastes (MIF) était constitué de MCF additionné de testostérone tritiée (1,6 x 10"7 M, soit 6,32 μCi/ml) et de testostérone non radiomarquée (3,84 x 10"6 M).
Le Finastéride a été extrait des comprimés par broyage, agitation en DMSO, centrifugation puis recueil du surnageant (concentration théorique de cette solution : 1 mg/ml de finastéride), testé à 30 ng/ml. L'huile de margoze a été solubilisée à 2 mg/ml dans le milieu MCF contenant 2,5% d'éthanol, puis dilution dans le milieu MCF en contact avec les cellules de manière à obtenir des concentrations finales en huile de margoze de 5 et 10 μg/ml.1.3 Preparation of the products and incubation with the test system The fibroblast incubation medium (MIF) consisted of MCF supplemented with tritiated testosterone (1.6 × 10 −7 M, ie 6.32 μCi / ml) and non-radiolabelled testosterone (3.84 x 10 "6 M). Finasteride was extracted from the tablets by grinding, stirring in DMSO, centrifugation then collection of the supernatant (theoretical concentration of this solution: 1 mg / ml of finasteride), tested at 30 ng / ml. Margoze oil was dissolved at 2 mg / ml in MCF medium containing 2.5% ethanol, then dilution in MCF medium in contact with the cells so as to obtain final concentrations of margoze oil of 5 and 10 μg / ml.
Echelle de temps : T-2 To T 4 • • « HeuresTime scale: T -2 To T 4 • • “Hours
: élimination du milieu MCF: elimination of the MCF medium
1 pré-incubation des produits à l'essai et du produit de référence préparés dans le milieu MCF Ψ: élimination des milieux MCF contenant le produit à l'essai ou le produit de référence : incubation du produit à l'essai et du produit de référence préparés dans le milieu1 pre-incubation of the test products and of the reference product prepared in the MCF medium Ψ: elimination of the MCF media containing the test product or the reference product: incubation of the test product and of the reference prepared in the middle
MIFMIF
*>: détermination de l'activité de la 5α -reductase. Les cultures de fibroblastes ont été pré-incubées en présence du produit à l'essai ou du produit de référence pendant 2 heures avant l'ajout du substrat, la testostérone. Pour cette étape, le produit à l'essai et le produit de référence ont été préparés dans le milieu MCF.*>: determination of the activity of 5α-reductase. The fibroblast cultures were pre-incubated in the presence of the test product or the reference product for 2 hours before the addition of the substrate, testosterone. For this step, the test product and the reference product were prepared in the MCF medium.
Après la pré-incubation, les cultures de fibroblastes ont été incubées en présence du produit à l'essai ou du produit de référence préparés dans le milieu MIF pendant 24 heures à 37°C dans une atmosphère humide contenant 5 % de CO2. Des cultures témoins ont été incubées dans le milieu MIF en absence de produit à l'essai et de produit de référence.After the pre-incubation, the fibroblast cultures were incubated in the presence of the test product or of the reference product prepared in the MIF medium for 24 hours at 37 ° C. in a humid atmosphere containing 5% CO 2 . Control cultures were incubated in the MIF medium in the absence of test product and of reference product.
Chaque condition expérimentale a été testée en triplicate.Each experimental condition was tested in triplicate.
1.4 Evaluation des effets
Après la période d'incubation, les cellules ont été soumises à l'action des ultrasons dans le milieu MIF. Les lysats cellulaires ainsi obtenus ont été extraits par du dichlorométhane. Après évaporation, les résidus secs ont été repris dans du méthanol et ont été déposés sur des plaques de silice 60F254 (MERCK, référence 5554). Des standards non radiomarqués, la testostérone, la 5α-dihydrotestostérone et l'androstènedione, ont été déposés sur chacune des plaques.1.4 Assessment of effects After the incubation period, the cells were subjected to the action of ultrasound in the MIF medium. The cell lysates thus obtained were extracted with dichloromethane. After evaporation, the dry residues were taken up in methanol and were deposited on silica plates 60F 254 (MERCK, reference 5554). Non-radiolabelled standards, testosterone, 5α-dihydrotestosterone and androstenedione, were deposited on each of the plates.
Le solvant de migration était un mélange de dichlorométhane et d'éther (7:3, v/v) A la fin de la migration, les plaques de silices ont été lues à l'aide d'un scanner de radioactivité BERTHOLD. Les standards non radiomarqués ont été mis en évidence par pulvérisation d'acide sulfurique à 5 % (v/v) sur les plaques de chromatographie chauffées ensuite à 100°C pendant 10 minutes.The migration solvent was a mixture of dichloromethane and ether (7: 3, v / v) At the end of the migration, the silica plates were read using a BERTHOLD radioactivity scanner. The non-radiolabelled standards were demonstrated by spraying 5% (v / v) sulfuric acid on the chromatography plates then heated to 100 ° C for 10 minutes.
La comparaison des Rf (facteur de rétention relatif) déterminés pour les standards avec ceux obtenus pour les différents métabolites radioactifs a permis l'identification de ces derniers.The comparison of the Rf (relative retention factor) determined for the standards with those obtained for the different radioactive metabolites allowed the identification of the latter.
La métabolisation de la testostérone en 5 -dihydrotestostérone dans les différentes conditions expérimentales a été calculée : les résultats (aires des pics de 5α- dihydrotestostérone comptés par le scanner BERTHOLD) sont exprimés en pmol de 5α-DHT formées par μg d'ADN. Ils ont aussi été exprimés en pourcentage de l'activité 5α-réductase présente dans le groupe 'cellules témoin'. Le dosage du contenu total en ADN a été effectué à l'aide d'un colorant nucléaire fluorecent (Hoechst 33258) par fluorométrie (excitation 356 nm, émission .458 nm).The metabolism of testosterone to 5 -dihydrotestosterone under the various experimental conditions was calculated: the results (areas of the peaks of 5α-dihydrotestosterone counted by the BERTHOLD scanner) are expressed in pmol of 5α-DHT formed by μg of DNA. They were also expressed as a percentage of the 5α-reductase activity present in the “control cells” group. The determination of the total DNA content was carried out using a fluorecent nuclear dye (Hoechst 33258) by fluorometry (excitation 356 nm, emission .458 nm).
1.5 - Traitement des données1.5 - Data processing
Les groupes de données (groupe témoin et groupes traités) ont été traités par une analyse de la variance à un facteur (ANONA 1, p<0,05), suivie par un test de DUΝΝETT (p<0,05). L'effet du produit à l'essai et du produit de référence a été comparé au groupe 'cellules témoin'.The data groups (control group and treated groups) were treated by a factor analysis of variance (ANONA 1, p <0.05), followed by a DUΝΝETT test (p <0.05). The effect of the test product and the reference product was compared with the 'control cells' group.
2. Résultats et discussion
Le finastéride utilisé comme produit de référence et testé à 30 ng/ml inhibe l'activité de la 5α-réductase de 70% (p<0,05). Ce résultat était attendu et valide notre test (tableau 2).2. Results and discussion Finasteride used as a reference product and tested at 30 ng / ml inhibits the activity of 5α-reductase by 70% (p <0.05). This result was expected and validates our test (Table 2).
L'huile de margoze testée à 5 et 10 μg/ml inhibe respectivement l'activité de la 5α-réductase de 39 et 50%) (P<0,1 et p<0,05 respectivement) (tableau 3).Margoze oil tested at 5 and 10 μg / ml respectively inhibits the activity of 5α-reductase by 39 and 50%) (P <0.1 and p <0.05 respectively) (Table 3).
3. Tableaux3. Tables
3.1 - Effet du Finastéride sur l'activité de la 5α-réductase dans des cultures de fibroblastes dermiques humains normaux après 24 heures d'incubation3.1 - Effect of Finasteride on the activity of 5α-reductase in cultures of normal human dermal fibroblasts after 24 hours of incubation
Tableau 2Table 2
** moyenne statistiquement différente de celle du groupe témoin (p<0,05)** mean statistically different from that of the control group (p <0.05)
3.2 - Effet de l'huile de margoze sur l'activité de la 5α-réductase dans des cultures de fibroblastes dermiques humains normaux après 24 heures d'incubation.3.2 - Effect of margoze oil on the activity of 5α-reductase in cultures of normal human dermal fibroblasts after 24 hours of incubation.
Tableau 3Table 3
** moyenne statistiquement différente de celle du groupe témoin (p<0,05) *moyenne statistiquement différente de celle du groupe témoin (p<0,l)
** mean statistically different from that of the control group (p <0.05) * mean statistically different from that of the control group (p <0, l)
Claims
1. Utilisation d'au moins une huile extraite de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, pour la préparation d'une composition destinée à inliiber l'activité de la 5-alpha reductase. 1. Use of at least one oil extracted from cucurbit seeds chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia 'a composition intended to inhibit the activity of 5-alpha reductase.
2. Utilisation selon la revendication 1, caractérisée en ce que la composition est destinée à inhiber l'isoenzyme de type 1 et/ou l'isoenzyme de type 2 de la 5α- réductase.2. Use according to claim 1, characterized in that the composition is intended to inhibit the type 1 isoenzyme and / or the type 2 isoenzyme of 5α-reductase.
3. Utilisation selon la revendication 1 ou 2, caractérisée en ce que la composition est adaptée pour une administration par voie topique externe. 3. Use according to claim 1 or 2, characterized in that the composition is suitable for administration by external topical route.
4. Utilisation selon l'une quelconque des revendications 1 à 3, caractérisée en ce que la composition se présente sous forme d'une solution aqueuse, hydroalcoolique ou huileuse, d'une émulsion huile-dans-eau ou eau-dans-huile ou multiple, d'un gel aqueux ou huileux, d'un produit anhydre liquide, pâteux ou solide, ou d'une dispersion d'huile dans une phase aqueuse à l'aide de sphérules. 4. Use according to any one of claims 1 to 3, characterized in that the composition is in the form of an aqueous, hydroalcoholic or oily solution, of an oil-in-water or water-in-oil emulsion or multiple, an aqueous or oily gel, a liquid, pasty or solid anhydrous product, or an oil dispersion in an aqueous phase using spherules.
5. Utilisation selon l'une quelconque des revendications précédentes, caractérisée en ce que l'huile des graines de cucurbitacées est susceptible d'être obtenue selon le procédé consistant à extraire les lipides totaux des graines de cucurbitacées préalablement séchées et broyées, à l'aide d'un solvant des huiles, puis à évaporer ledit solvant ou selon le procédé consistant à extraire les lipides des graines de cucurbitacées par pression mécanique des graines à froid.5. Use according to any one of the preceding claims, characterized in that the oil of the cucurbit seeds is capable of being obtained according to the process consisting in extracting the total lipids from the cucurbit seeds previously dried and ground, with using an oil solvent, then evaporating said solvent or according to the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure from the seeds when cold.
6. Utilisation selon l'une quelconque des revendications précédentes, caractérisée en ce que l'huile extraite des graines de cucurbitacées est présente à une concentration comprise entre 0,01 et 95 %, de préférence entre 0,1 et 30 % en poids, par rapport au poids total de la composition. 6. Use according to any one of the preceding claims, characterized in that the oil extracted from the seeds of cucurbits is present at a concentration of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
7. Utilisation selon l'une quelconque des revendications précédentes, caractérisée en ce que la composition est destinée au traitement des pathologies et/ou des désordres cutanés liés à une exagération congénitale ou acquise de l'activité de la 5α-réductase. 7. Use according to any one of the preceding claims, characterized in that the composition is intended for the treatment of pathologies and / or skin disorders linked to a congenital exaggeration or acquired from the activity of 5α-reductase.
8. Utilisation selon l'une quelconque des revendications précédentes, caractérisée en ce que la composition est destinée au traitement de l'hypertrophie prostatique, de l'adénome prostatique, de l'acné, de l'hyperséborrhée, de l'alopécie ou de l'hirsutisme. 8. Use according to any one of the preceding claims, characterized in that the composition is intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
9. Utilisation selon l'une quelconque des revendications précédentes, caractérisée en ce que la composition est une composition pharmaceutique ou dermatologique.9. Use according to any one of the preceding claims, characterized in that the composition is a pharmaceutical or dermatological composition.
10. Utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, pour la préparation d'une composition destinée au traitement de l'hypertrophie prostatique, de l'adénome prostatique, de l'acné, de l'hyperséborrhée, de l'alopécie ou de l'hirsutisme.10. Use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, for the preparation of a composition intended for the treatment of prostatic hypertrophy, prostatic adenoma, acne, hyperseborrhea, alopecia or hirsutism.
11. Méthode de traitement cosmétique, caractérisée en ce qu'on applique sur la peau, les muqueuses, les ongles ou les cheveux au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, afin d'inhiber l'activité de la 5-alpha reductase.11. Cosmetic treatment method, characterized in that at least one oil of cucurbit seeds selected from the group consisting of Lagenaria, Luffa and Momordica is advantageously applied to the skin, mucous membranes, nails or hair. Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in order to inhibit the activity of 5-alpha reductase.
12. Méthode de traitement cosmétique selon la revendication 11, caractérisée en ce qu'on applique l'huile de graines de cucurbitacées sur la peau grasse et/ou sur les cheveux gras, sur la peau luisante et/ou sur les cheveux luisants, sur la peau présentant des boutons, des points noirs, ou des comédons, sur la peau grasse à tendance acnéique, sur la peau grasse à imperfections, sur les zones du cuir chevelu affectées d'alopécie ou sur les zones de la peau présentant des excès de pilosité. 12. Cosmetic treatment method according to claim 11, characterized in that the oil of cucurbit seeds is applied to oily skin and / or to oily hair, to shiny skin and / or to shiny hair, on skin with pimples, blackheads, or comedones, on oily skin prone to acne, on oily skin with blemishes, on areas of the scalp affected by alopecia or on areas of skin with excess hair.
13. Utilisation d'au moins une huile de graines de cucurbitacées choisies dans le groupe constitué par le Lagenaria, le Luffa et le Momordica, avantageusement le Lagenaria leucaritha, le Luffa acutangula, le Luffa cylindrica et le Momordica charantia, dans une composition nutraceutique pour l'être humain et/ou l'animal en tant qu'additif agissant pour inhiber l'activité de la 5-alpha reductase. 13. Use of at least one cucurbit seed oil chosen from the group consisting of Lagenaria, Luffa and Momordica, advantageously Lagenaria leucaritha, Luffa acutangula, Luffa cylindrica and Momordica charantia, in a nutraceutical composition for humans and / or animals as an additive which acts to inhibit the activity of 5-alpha reductase.
14. Utilisation selon la revendication 13, caractérisée en ce que l'huile des graines de cucurbitacées est extraite selon le procédé consistant à extraire les lipides totaux des graines de cucurbitacées préalablement séchées et broyées, à l'aide d'un solvant des huiles, puis à évaporer ledit solvant ou selon le procédé consistant à extraire les lipides des graines de cucurbitacées par pression mécanique des graines à froid.14. Use according to claim 13, characterized in that the oil from the cucurbit seeds is extracted according to the process consisting in extracting the total lipids from the cucurbit seeds previously dried and ground, using a solvent for the oils, then evaporating the said solvent or according to the process consisting in extracting the lipids from the cucurbit seeds by mechanical pressure from the seeds when cold.
15. Utilisation selon la revendication 13 ou 14, caractérisée en ce que l'huile des graines de cucurbitacées est présente selon une proportion comprise entre 0,01 et 95 %, de préférence entre 0,1 et 30 % en poids, par rapport au poids total de la composition. 15. Use according to claim 13 or 14, characterized in that the oil of the cucurbit seeds is present in a proportion of between 0.01 and 95%, preferably between 0.1 and 30% by weight, relative to the total weight of the composition.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0108648 | 2001-06-29 | ||
| FR0108648A FR2826579B1 (en) | 2001-06-29 | 2001-06-29 | COSMETIC COMPOSITION CONTAINING AT LEAST ONE OIL EXTRACTED FROM CUCURBITACEOUS SEEDS, ITS COSMETIC, THERAPEUTIC AND FOOD USE |
| PCT/FR2002/002277 WO2003002088A2 (en) | 2001-06-29 | 2002-07-01 | Use of an oil of the gourd family for inhibiting 5$g(a)-reductase activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP1401383A2 true EP1401383A2 (en) | 2004-03-31 |
Family
ID=8864944
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP02767537A Withdrawn EP1401383A2 (en) | 2001-06-29 | 2002-07-01 | Use of at least an oil extracted from the seeds of the gourd family for preparing a composition for inhibiting 5-alpha-reductase activity |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7238377B2 (en) |
| EP (1) | EP1401383A2 (en) |
| JP (1) | JP2005502612A (en) |
| KR (1) | KR100901056B1 (en) |
| CN (1) | CN100558340C (en) |
| AU (1) | AU2002330544A1 (en) |
| FR (1) | FR2826579B1 (en) |
| MX (1) | MXPA04000015A (en) |
| WO (1) | WO2003002088A2 (en) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004103321A2 (en) * | 2003-05-16 | 2004-12-02 | Johnson & Johnson Consumer Companies, Inc. | Topical treatment of ingrown hairs |
| US20050031571A1 (en) * | 2003-05-16 | 2005-02-10 | Khaiat Alain V. | Topical treatment of ingrown hairs |
| US20040228822A1 (en) * | 2003-05-16 | 2004-11-18 | Khaiat Alain V. | Topical treatment of skin conditions |
| FR2873295B1 (en) * | 2004-07-26 | 2006-12-01 | Expanscience Sa Lab | USE OF AT LEAST ONE CONJUGATED FATTY ACID TRIENE FOR THE PREPARATION OF A MEDICAMENT FOR THE TREATMENT OF INFLAMMATION |
| KR101131685B1 (en) * | 2004-10-18 | 2012-03-28 | 애경산업(주) | Cosmetic compositions having sebosuppressive effect |
| JP4630102B2 (en) * | 2005-03-30 | 2011-02-09 | 株式会社ナリス化粧品 | Hyaluronic acid production promoter and cosmetics containing the same |
| US20070243154A1 (en) * | 2006-04-13 | 2007-10-18 | L'oreal | Solubilization of acid ingredients |
| US20080075798A1 (en) * | 2006-08-30 | 2008-03-27 | Rosemarie Osborne | Personal care compositions comprising pear seed extract |
| US8071844B1 (en) | 2007-09-13 | 2011-12-06 | Nutritional Health Institute Laboratories, Llc | Cultivated momordica species and extract thereof |
| EP2378872A4 (en) | 2008-12-18 | 2012-05-16 | B Eugene Guthery | Acne vulgaris treatment regimen |
| FR2966042B1 (en) * | 2010-10-18 | 2012-11-09 | Clarins Lab | USE OF A COSMETIC COMPOSITION COMPRISING AN EXTRACT OF DIANTHUS CARTHUSIANORUM |
| WO2012104240A2 (en) * | 2011-01-31 | 2012-08-09 | LUCOLAS-M.D. Ltd | Cosmetic use |
| US11850451B2 (en) | 2011-01-31 | 2023-12-26 | Lucolas-M.D. Ltd. | Cosmetic compositions and methods for improving skin conditions |
| US20140178496A1 (en) * | 2012-12-14 | 2014-06-26 | Annuary Healthcare Inc. | Endospore compositions and uses thereof |
| WO2017055943A1 (en) * | 2015-07-15 | 2017-04-06 | Bakel Srl | Cosmetic composition |
| JP6646528B2 (en) * | 2016-01-14 | 2020-02-14 | 日本メナード化粧品株式会社 | Keratin plug decomposition accelerator |
| CN106072221A (en) * | 2016-06-22 | 2016-11-09 | 安徽金豪生态农业科技有限公司 | A kind of Flammulina velutiper (Fr.) Sing nourishing healthy fruit jelly helping beauty treatment and preparation method thereof |
| CN105911593A (en) * | 2016-06-24 | 2016-08-31 | 北京金双狐油气技术有限公司 | Tilted model layer velocity calculation method |
| FR3123210B1 (en) * | 2021-05-28 | 2023-12-15 | Oreal | Use of ascorbyl glucoside to prevent the coloring of skin blackheads. |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3881000A (en) * | 1971-09-08 | 1975-04-29 | Mundipharma Ag | Bis-(phosphorylated anthralin) compounds in the treatment of psoriasis and arthritis |
| JPS5251033A (en) * | 1975-10-16 | 1977-04-23 | Koichi Ogawa | Cosmetics |
| US4789749A (en) * | 1984-06-18 | 1988-12-06 | The Regents Of The University Of California | Manoalide analogs |
| FR2567402B1 (en) * | 1984-07-12 | 1988-07-01 | Cird | NOVEL PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING DIHYDROXY-1,8 PHENYL-10 ANTHRONE-9 AS ACTIVE INGREDIENT, AND PROCESS FOR PREPARING THE ACTIVE INGREDIENT |
| JPS6293214A (en) * | 1985-10-18 | 1987-04-28 | Shiseido Co Ltd | Hair tonic |
| IT1225405B (en) | 1988-09-13 | 1990-11-13 | Mariko Kawamura | COSMETIC FORMULATION FOR SKIN CARE. |
| JPH0725660B2 (en) * | 1990-05-29 | 1995-03-22 | サンスター株式会社 | Cosmetics with anti-inflammatory properties against sunburn |
| DE4111569A1 (en) * | 1991-04-10 | 1992-10-15 | Zimzik Henry | Cosmetic compsns. contg. Luffa extract - e.g. soaps, lotions, creams or oils, have antibacterial activity against skin and hair fungi |
| JP2722164B2 (en) * | 1993-07-22 | 1998-03-04 | 株式会社セレスコスメプラン | Hair growth and hair growth cosmetics |
| DE4429747A1 (en) * | 1994-08-22 | 1996-02-29 | Willige Zimzik Elfriede | Cosmetic ointment and cream bases |
| US6183747B1 (en) * | 1999-07-14 | 2001-02-06 | Kaijun Ren | Use of plant Momordica charactia extracts for treatment of acne acid |
| WO2001005416A1 (en) * | 1999-07-15 | 2001-01-25 | Pushpa Khanna | Oil from momordica charantia l., its method of preparation and uses |
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2001
- 2001-06-29 FR FR0108648A patent/FR2826579B1/en not_active Expired - Lifetime
-
2002
- 2002-07-01 KR KR1020037017110A patent/KR100901056B1/en not_active Expired - Fee Related
- 2002-07-01 AU AU2002330544A patent/AU2002330544A1/en not_active Abandoned
- 2002-07-01 CN CNB02813074XA patent/CN100558340C/en not_active Expired - Fee Related
- 2002-07-01 MX MXPA04000015A patent/MXPA04000015A/en unknown
- 2002-07-01 WO PCT/FR2002/002277 patent/WO2003002088A2/en not_active Ceased
- 2002-07-01 EP EP02767537A patent/EP1401383A2/en not_active Withdrawn
- 2002-07-01 JP JP2003508328A patent/JP2005502612A/en active Pending
- 2002-07-01 US US10/482,280 patent/US7238377B2/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| See references of WO03002088A2 * |
Also Published As
| Publication number | Publication date |
|---|---|
| KR100901056B1 (en) | 2009-06-04 |
| FR2826579B1 (en) | 2005-08-05 |
| FR2826579A1 (en) | 2003-01-03 |
| CN1529578A (en) | 2004-09-15 |
| AU2002330544A1 (en) | 2003-03-03 |
| MXPA04000015A (en) | 2004-05-21 |
| KR20040030716A (en) | 2004-04-09 |
| US20040234632A1 (en) | 2004-11-25 |
| WO2003002088A2 (en) | 2003-01-09 |
| JP2005502612A (en) | 2005-01-27 |
| CN100558340C (en) | 2009-11-11 |
| WO2003002088A3 (en) | 2003-04-17 |
| US7238377B2 (en) | 2007-07-03 |
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