WO2009138582A2 - Use of a composition containing 7-dehydrocholesterol or a natural extract of a vegetable or animal microorganism - Google Patents
Use of a composition containing 7-dehydrocholesterol or a natural extract of a vegetable or animal microorganism Download PDFInfo
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- WO2009138582A2 WO2009138582A2 PCT/FR2009/000463 FR2009000463W WO2009138582A2 WO 2009138582 A2 WO2009138582 A2 WO 2009138582A2 FR 2009000463 W FR2009000463 W FR 2009000463W WO 2009138582 A2 WO2009138582 A2 WO 2009138582A2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
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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
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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
- A61P17/16—Emollients or protectives, e.g. against radiation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
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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
- A61Q19/004—Aftersun preparations
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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
- A61Q19/08—Anti-ageing preparations
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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
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/52—Stabilizers
- A61K2800/522—Antioxidants; Radical scavengers
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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
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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
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/92—Oral administration
Definitions
- composition containing 7-dehydrochlolesterol or a natural extract of microorganism or plant or animal Use of a composition containing 7-dehydrochlolesterol or a natural extract of microorganism or plant or animal
- the present invention relates to the use of a composition containing 7-dehydrocholesterol or a natural extract of microorganism or plant or animal including, to protect skin cells and mucous membranes against the consequences of stress oxidative, such as exposure to ultraviolet radiation.
- 7-dehydrocholesterol is a precursor of vitamin D found naturally in the skin.
- GB-454260-A discloses the synthesis of 7-dehydrocholesterol from 7-oxo-cholesteryl acetate.
- JP-1261326-A relates to a cosmetic product containing 7-dehydrocholesterol to promote the formation of cutaneous pigments.
- the repeated exposure of the skin to ultraviolet radiation causes damage in the cells of the skin and mucous membranes, in particular in the cells called fibroblasts which are responsible for the renewal of the macromolecules constituting the extracellular matrix of the dermis (Goukassian D. et al,
- sun-exposed skin cells have long been known to lose their ability to reproduce more rapidly when introduced into in vitro culture (Gilchrest, BA, J Gerontol., 35 (4): 537-41, 1980). ). Cells that can no longer reproduce are called “senescent cells", and are characterized by the strong expression of an active beta-galactosidase at pH 6. More cells expressing this beta-galactosidase are found among the keratinocytes. or elderly skin fibroblasts, than in the cultures of cells aged by successive subcultures (Dimri GP et al, Proc Nat Acad Sci USA 92: 9363-67,1995), or in cultures having undergone repeated ultraviolet stress (Chainiaux F. et al., Int.J. Biochem., Cell Biol., 34 (11): 1331-9,2002).
- composition containing 7-dehydrocholesterol, a derivative of 7-dehydrocholesterol or a natural extract of a microorganism or plant or animal comprising comprising to protect the cells of the skin and mucous membranes against the consequences of oxidative stress such as exposure to ultraviolet radiation.
- the 7-dehydrocholesterol is in the form of a water-soluble derivative such as an ester of phosphoric acid, or succinic acid.
- this composition also comprises at least one antioxidant such as vitamin E 1 vitamin C, a carotenoid, a flavonoid, an isoflavonoid, a polyphenol, a procyanidin, resveratrol, epigallocatechin gallate, genistein , daidzein, formononetin, equol, a green tea extract.
- at least one antioxidant such as vitamin E 1 vitamin C, a carotenoid, a flavonoid, an isoflavonoid, a polyphenol, a procyanidin, resveratrol, epigallocatechin gallate, genistein , daidzein, formononetin, equol, a green tea extract.
- it comprises from 0.00001 to 95% by weight, and preferably from 0.001 to 1% by weight, of 7-dehydrocholesterol.
- composition according to the present invention is intended for application to the skin or the mucous membranes and / or to be ingested.
- this composition stimulates the activity of the p53 protein in the cells of the skin or mucous membranes.
- Example 1 Attenuation by 7-dehydrocholesterol of the damage caused to fibroblasts in culture, by repeated exposures to ultraviolet radiation.
- the 7-dehydrocholesterol used is a sample of greater than 96% purity provided by MMP Inc.
- Dermal fibroblasts of the same BJ strain as used by Chaines F. et al (2002, already cited) are cultured by conventional methods.
- the absence of cytotoxicity of 7-dehydrocholesterol over a period of 9 days is verified in the range 0.25 to 1 ⁇ g / ml.
- the fibroblasts are exposed once a day to a dose of ultraviolet B of 500 mJ / cm 2 .
- the culture medium is replaced by medium containing 0.25; 0.5; or 1 ⁇ g / ml of 7-dehydrocholesterol.
- the cells After the last irradiation, the cells are left for 72 hours in contact with a medium supplemented with 7-dehydrocholesterol, renewed every 24 hours.
- beta-galactosidase activity at pH6 (beta-galactosidase associated with senescence or SA beta-gal) is evaluated according to the method of Dimri GP et al (already cited), on at least 400 cells for each concentration of 7-dehydrocholesterol.
- a positive control was achieved by irradiating a culture of the same cells by a dose of 150 mJ / cm 2 of UVB. After these treatments the nuclear proteins were extracted from the fibroblasts.
- compositions are given below by way of example to illustrate the different modes of action or use of 7-dehydrocholesterol.
- Composition No. 1 Cosmetic cream for protection against oxidative stress.
- the procedure is as for the production of a conventional oil-in-water emulsion, that is to say, a hydrophobic phase containing 0.05% by weight of 7-dehydrocholesterol and an aqueous phase is mixed with stirring at 85 ° C. containing each of the raw materials intended to give the product the usual properties of use: stability, safety, easy spreading, pleasant final touch, etc.
- This cream is applied to the face, neck and hands, preferably in the morning to prepare the skin for daily aggression
- Composition No. 2 Cosmetic cream for protection against oxidative stress.
- an oil-in-water emulsion containing, in addition to alpha-tocopherol, as well as alpha-tocopherol acetate is carried out; and during cooling, at 45 ° C, vitamin C phosphate is added in an amount sufficient to achieve the concentrations by weight in the final composition of: - 7-dehydrocholesterol 0.05%
- This formulation is a day cream.
- Composition No. 3 Cosmetic cream for protection against oxidative stress and filter protection.
- composition No. 1 an oil-in-water emulsion is made with an addition of titanium oxide sufficient for the protection factor SPF to be equal to 6.
- SPF protection factor
- Composition No. 4 Cosmetic gel for protection against oxidative stress.
- a hydroalcoholic acrylic gel containing 0.02% by weight of 7-dehydrocholesterol and containing 2% by weight of a glycolic acid extract of Glycyrrhiza glabra is prepared.
- This gel is applied in the morning and during the day on skin areas exposed to the sun and pollution.
- Composition No. 5 Dietary supplement to protect the skin during exposure to the sun or pollution.
- Composition No. 6 Dietary supplement to prepare the skin for sun exposure.
- Capsules containing 60 mg of a 2% by weight powder formulation of 7-dehydrocholesterol, 15 mg of green tea extract and 25 mg of vitamin C per capsule are made.
- the recommended daily dose is 2 to 4 capsules per day, depending on the intensity of the exposure, in two doses in the morning and in the middle of the day with a little water at the time of the meal.
- Composition No. 7 Drink to protect the skin during sun exposure. A soy milk drink containing 0.01% by weight of 7-dehydrocholesterol is prepared.
- This drink is presented in doses of 100 ml.
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Abstract
Description
Utilisation d'une composition contenant le 7-déhydrochlolestérol ou un extrait naturel de micro-organisme ou végétal ou animal Use of a composition containing 7-dehydrochlolesterol or a natural extract of microorganism or plant or animal
La présente invention est relative à l'utilisation d'une composition contenant le 7-déhydrocholestérol ou un extrait naturel de micro-organisme ou végétal ou animal en comprenant, pour protéger les cellules de la peau et des muqueuses contre les conséquences d'un stress oxydatif tel qu'une exposition aux rayonnements ultraviolets.The present invention relates to the use of a composition containing 7-dehydrocholesterol or a natural extract of microorganism or plant or animal including, to protect skin cells and mucous membranes against the consequences of stress oxidative, such as exposure to ultraviolet radiation.
Le 7-déhydrocholestérol est un précurseur de la vitamine D trouvé naturellement dans la peau. Le document GB-454260-A décrit la synthèse du 7-déhydrocholestérol à partir de l'acétate de 7-oxo-cholestéryle.7-dehydrocholesterol is a precursor of vitamin D found naturally in the skin. GB-454260-A discloses the synthesis of 7-dehydrocholesterol from 7-oxo-cholesteryl acetate.
Le document JP-1261326-A concerne un produit cosmétique contenant du 7- déhydrocholestérol pour favoriser la formation des pigments cutanés.JP-1261326-A relates to a cosmetic product containing 7-dehydrocholesterol to promote the formation of cutaneous pigments.
Par ailleurs, l'exposition répétée de la peau aux rayonnements ultraviolets en- traîne des dommages dans les cellules de la peau et des muqueuses, en particulier dans les cellules appelées fibroblastes qui sont responsables du renouvellement des macromolécules constituant la matrice extracellulaire du derme (Goukassian D. et al,Furthermore, the repeated exposure of the skin to ultraviolet radiation causes damage in the cells of the skin and mucous membranes, in particular in the cells called fibroblasts which are responsible for the renewal of the macromolecules constituting the extracellular matrix of the dermis (Goukassian D. et al,
The FASEB J., 14 : 1325-34,2000).The FASEB J., 14: 1325-34,2000).
Ces dommages sont naturellement réparés. Mais, quand ce n'est pas le cas, cela peut avoir des conséquences pour le bon fonctionnement des cellules (Goukassian D.A. et Gilchrest B.A., Rejuvenation Res.7 (3) : 175-85,2004).This damage is naturally repaired. But when this is not the case, this can have consequences for the proper functioning of the cells (Goukassian D.A. and Gilchrest B.A., Rejuvenation Res.7 (3): 175-85,2004).
De plus, on sait depuis longtemps que les cellules de la peau exposée au soleil perdent plus vite leur capacité de reproduction lorsqu'on les introduit en culture in vitro (Gilchrest B.A., J Gerontol., 35(4) :537-41 ,1980). Les cellules qui ne peuvent plus se reproduire sont appelées « cellules sénes- centes », et sont caractérisées par la forte expression d'une bêta-galactosidase active à pH 6. On trouve plus de cellules exprimant cette bêta-galactosidase aussi bien parmi les kératinocytes ou fibroblastes de la peau de personnes âgées, que dans les cultures de cellules vieillies par repiquages successifs (Dimri G. P. et al, Proc. Nat. Acad. Sci. USA 92 :9363-67,1995), ou dans les cultures ayant subi des stress ultra-violets répétés (Chainiaux F. et al, Int. J. Biochem. CeII. Biol. 34(1 1 ) : 1331 -9,2002).In addition, sun-exposed skin cells have long been known to lose their ability to reproduce more rapidly when introduced into in vitro culture (Gilchrest, BA, J Gerontol., 35 (4): 537-41, 1980). ). Cells that can no longer reproduce are called "senescent cells", and are characterized by the strong expression of an active beta-galactosidase at pH 6. More cells expressing this beta-galactosidase are found among the keratinocytes. or elderly skin fibroblasts, than in the cultures of cells aged by successive subcultures (Dimri GP et al, Proc Nat Acad Sci USA 92: 9363-67,1995), or in cultures having undergone repeated ultraviolet stress (Chainiaux F. et al., Int.J. Biochem., Cell Biol., 34 (11): 1331-9,2002).
De plus, il a été récemment montré (Debacq-Chainiaux F. et al, J. CeII. Sci. 118(Pt4) :743-58, 2005) que les fibroblastes perdent avec l'âge une partie de leur capacité de réparation des dommages causés par les rayonnements ultra-violets (UV) (Goukassian D. et al, 2000, déjà cité). Enfin, il a été rapporté que les « cellules sénescentes » in vivo, ont des effets néfastes sur le tissu environnant (Funk W. D. et al, Exp CeII Res.258 :270-8, 2000), et il parait important de pouvoir disposer de moyens pour éviter leur apparition.Moreover, it has recently been shown (Debacq-Chainiaux F. et al., J. CeII, Sci 118 (Pt4): 743-58, 2005) that fibroblasts lose, with age, part of their ability to repair damage caused by ultraviolet (UV) radiation (Goukassian D. et al, 2000, cited above). Finally, it has been reported that the "senescent cells" in vivo have adverse effects on the surrounding tissue (Funk WD et al, Exp CeII Res.258: 270-8, 2000), and it seems important to have means to avoid their appearance.
Il apparaît donc qu'il serait très intéressant de pouvoir disposer de moyens pour éviter l'apparition de « cellules sénescentes » qui ont perdu la capacité de se reproduire, et qui, de plus, ont des effets néfastes sur les tissus environnants.It thus appears that it would be very interesting to be able to have means to avoid the appearance of "senescent cells" which have lost the ability to reproduce, and which, moreover, have adverse effects on the surrounding tissues.
Ainsi, l'un des buts de la présente invention est-il de fournir un moyen pour protéger les cellules cutanées contre l'apparition des « cellules sénescentes » qui est la conséquence d'un stress oxydatif tel qu'une exposition aux rayonnements ultra- violets.Thus, it is an object of the present invention to provide a means for protecting cutaneous cells against the appearance of "senescent cells" which is a consequence of oxidative stress such as ultraviolet radiation exposure. purples.
Ce but, ainsi que d'autres qui apparaîtront par la suite, est atteint par l'utilisation d'une composition contenant du 7-déhydrocholestérol, un dérivé de 7- déhydrocholestérol ou un extrait naturel de microorganisme ou végétal ou animal en comprenant pour protéger les cellules de la peau et des muqueuses contre les consé- quences d'un stress oxydatif tel qu'une exposition aux rayonnements ultraviolets.This aim, as well as others which will appear later, is achieved by the use of a composition containing 7-dehydrocholesterol, a derivative of 7-dehydrocholesterol or a natural extract of a microorganism or plant or animal comprising comprising to protect the cells of the skin and mucous membranes against the consequences of oxidative stress such as exposure to ultraviolet radiation.
Avantageusement, le 7-déhydrocholestérol est sous la forme d'un dérivé hydro- soluble tel qu'un ester de l'acide phosphorique, ou de l'acide succinique.Advantageously, the 7-dehydrocholesterol is in the form of a water-soluble derivative such as an ester of phosphoric acid, or succinic acid.
De préférence, cette composition comprend aussi au moins un antioxydant tel que la vitamine E1 la vitamine C, un caroténoïde, un flavonoïde, un isoflavonoïde, un polyphénol, une procyanidine, du resvératrol, du gallate d'épigallocatéchine, de la ge- nistéine, de la daidzéine, de la formononétine, de l'équol, un extrait de thé vert.Preferably, this composition also comprises at least one antioxidant such as vitamin E 1 vitamin C, a carotenoid, a flavonoid, an isoflavonoid, a polyphenol, a procyanidin, resveratrol, epigallocatechin gallate, genistein , daidzein, formononetin, equol, a green tea extract.
Avantageusement, elle comprend de 0,00001 à 95 % en poids, et de préférence de 0,001 à 1 % en poids, de 7-déhydrocholestérol.Advantageously, it comprises from 0.00001 to 95% by weight, and preferably from 0.001 to 1% by weight, of 7-dehydrocholesterol.
La composition, selon la présente invention, est destinée à une application sur la peau ou les muqueuses et/ou à être ingérée.The composition according to the present invention is intended for application to the skin or the mucous membranes and / or to be ingested.
Avantageusement, cette composition stimule l'activité de la protéine p53 dans les cellules de la peau ou des muqueuses.Advantageously, this composition stimulates the activity of the p53 protein in the cells of the skin or mucous membranes.
La description qui va suivre et qui ne présente aucun caractère limitatif, est en particulier relative à des exemples de réalisation de la présente invention qui permet- tront à l'homme du métier de mieux comprendre celle-ci.The following description, which is in no way limiting, relates in particular to embodiments of the present invention which will enable those skilled in the art to better understand it.
Il a maintenant été trouvé de façon tout à fait inattendue et surprenante,et comme le montrent les exemples ci-après, que si le milieu de culture des fibroblastes soumis à des expositions aux ultra-violets répétées, est supplémenté, avant les irradiations, par un ajout de 7-déhydrocholestérol, on diminue de façon très significative le nombre de cellules qui passent à l'état « sénescent » caractérisé par l'apparition de l'activité bêta-galactosidase qui lui est associée (« Sénescence Associated bêta- galactosidase » ou « SA bêta-gal »).It has now been found quite unexpectedly and surprisingly, and as shown by the examples below, that if the fibroblast culture medium subjected to repeated ultraviolet exposures, is supplemented, before the irradiations, by an addition of 7-dehydrocholesterol significantly decreases the number of cells that pass to the "senescent" state characterized by the appearance of the beta-galactosidase activity associated with it ("Senescence Associated Beta-galactosidase" or "SA Beta-gal").
Le 7-déhydrocholestérol utilisé dans les exemples et compositions ci-dessous est commercialisé par la société MMP Inc (USA).The 7-dehydrocholesterol used in the examples and compositions below is marketed by MMP Inc. (USA).
Exemple 1 : Atténuation par le 7-déhydrocholestérol des dommages causés à des fibroblastes en culture, par des expositions répétées à un rayonnement ultraviolet.Example 1: Attenuation by 7-dehydrocholesterol of the damage caused to fibroblasts in culture, by repeated exposures to ultraviolet radiation.
Le 7-déhydrocholestérol utilisé est un échantillon de pureté supérieure à 96% fourni par la société MMP Inc.The 7-dehydrocholesterol used is a sample of greater than 96% purity provided by MMP Inc.
Des fibroblastes de derme de la même souche BJ que celle utilisée par Chai- niaux F. et al (2002, déjà cité) sont mis en culture par les méthodes classiques.Dermal fibroblasts of the same BJ strain as used by Chaines F. et al (2002, already cited) are cultured by conventional methods.
L'absence de cytotoxicité du 7-déhydrocholestérol sur une durée de 9 jours, est vérifiée dans la gamme 0,25 à 1 μg /ml. Pendant 5 jours les fibroblastes sont exposés 1 fois par jour à une dose d'ultraviolets B de 500 mj/cm2.The absence of cytotoxicity of 7-dehydrocholesterol over a period of 9 days is verified in the range 0.25 to 1 μg / ml. For 5 days the fibroblasts are exposed once a day to a dose of ultraviolet B of 500 mJ / cm 2 .
A la suite de chaque irradiation, le milieu de culture est remplacé par du milieu contenant 0,25 ; 0,5 ; ou 1 μg /ml de 7-déhydrocholestérol.Following each irradiation, the culture medium is replaced by medium containing 0.25; 0.5; or 1 μg / ml of 7-dehydrocholesterol.
Avant chaque nouvelle irradiation, ces milieux sont remplacés par un milieu ne contenant pas de 7-déhydrocholéstérol.Before each new irradiation, these media are replaced by a medium containing no 7-dehydrocholesterol.
Après la dernière irradiation, les cellules sont laissées pendant 72 heures en contact avec un milieu supplémenté en 7-déhydrocholestérol, renouvelé toutes les 24 heures.After the last irradiation, the cells are left for 72 hours in contact with a medium supplemented with 7-dehydrocholesterol, renewed every 24 hours.
Au terme de cette dernière période de contact, l'activité bêta-galactosidase à pH6 (bêta-galactosidase associée à la sénescence ou SA bêta-gal) est évaluée suivant la méthode de Dimri G. P. et al (déjà cité), sur au moins 400 cellules pour chaque concentration en 7-déhydrocholestérol.At the end of this last period of contact, the beta-galactosidase activity at pH6 (beta-galactosidase associated with senescence or SA beta-gal) is evaluated according to the method of Dimri GP et al (already cited), on at least 400 cells for each concentration of 7-dehydrocholesterol.
L'expérience a été réalisée deux fois.The experiment was performed twice.
Les valeurs moyennes des pourcentages de cellules exprimant la SA bêta-gal sont regroupées dans le tableau I ci-après :The average values of the percentages of cells expressing beta-gal SA are summarized in Table I below:
On constate que :We observe that :
- les dommages causés par les expositions répétées aux rayons ultra-violets B ont entraîné une augmentation significative des fibroblastes présentant l'activité SA bêta- gal caractéristique des cellules qui ne peuvent plus se reproduire (qualifiées de « sé- nescentes »), le traitement des cellules par le 7-déhydrocholestérol après les irradiations, a permis une atténuation des dommages causés par les ultra-violets de façon significative dès la concentration de 0,25 μg/ml, ce qui se traduit par un nombre de fibroblastes « sé- nescents » qui reste inférieur à celui des cultures n'ayant subi aucune irradiation.- the damage caused by repeated exposure to ultraviolet B rays has led to a significant increase in fibroblasts exhibiting the characteristic beta-galatic activity of cells that can no longer reproduce (referred to as "sequencers"), the treatment of the cells with 7-dehydrocholesterol after the irradiations, made it possible to attenuate the damage caused by the ultraviolet rays significantly from the concentration of 0.25 μg / ml, which results in a number of fibroblasts - nescents "which remains lower than that of cultures which have not undergone any irradiation.
Tableau ITable I
II apparaît ainsi, que l'utilisation de 7-déhydrocholestérol, permet bien selon l'invention d'atténuer les dommages cellulaires causés par l'exposition aux rayonne- ments ultraviolets.It thus appears that the use of 7-dehydrocholesterol makes it possible, according to the invention, to attenuate the cellular damage caused by exposure to ultraviolet radiation.
Exemple 2 :Example 2
Pour protéger les cellules contre les stress oxydatifs, il est intéressant d'activer la protéine p53 (cf. de Magalhaes JP. et al, Expert Gerontol. 39(9) : 1379-89, 2004). On a évalué la stimulation de l'expression de la protéine p53 dans les fibroblastes de l'Exemple 1 sous l'influence de 1 μg/ml de 7-déhydrocholestérol dans le milieu de culture pendant 24 heures.To protect the cells against oxidative stress, it is interesting to activate the p53 protein (see Magalhaes JP et al., Expert Gerontol 39 (9): 1379-89, 2004). The stimulation of the expression of the p53 protein in the fibroblasts of Example 1 was evaluated under the influence of 1 μg / ml of 7-dehydrocholesterol in the culture medium for 24 hours.
Un contrôle positif a été réalisé en irradiant une culture des mêmes cellules par une dose de 150 mj/cm2 d'UVB. Après ces traitements on a extrait les protéines nucléaires des fibroblastes.A positive control was achieved by irradiating a culture of the same cells by a dose of 150 mJ / cm 2 of UVB. After these treatments the nuclear proteins were extracted from the fibroblasts.
Puis on a incubé 5μg de protéines nucléaires dans une microplaque recouverte d'un oligonucléotide portant la séquence d'ADN spécifique susceptible de lier la protéine p53. Enfin, la teneur en protéine p53 liée a été évaluée par colorimétrie au moyen d'un anti-corps spécifique de cette protéine et d'un anticorps conjugué à la peroxydase (test TransAM de Active Motif, Rixensart, Belgique).Then 5 .mu.g of nuclear proteins were incubated in a microplate coated with an oligonucleotide carrying the specific DNA sequence capable of binding the p53 protein. Finally, the content of bound p53 protein was evaluated by colorimetry using an antibody specific for this protein and a peroxidase-conjugated antibody (TransAM test of Active Motif, Rixensart, Belgium).
Les résultats obtenus sont regroupés dans le Tableau II ci-dessous :The results obtained are summarized in Table II below:
Tableau IITable II
On a ainsi trouvé de façon surprenante que le traitement au 7- déhydrocholestérol en l'absence d'UV a augmenté de 19% la teneur des fibroblastes en protéine p53.It has surprisingly been found that treatment with 7-dehydrocholesterol in the absence of UV increased by 19% the fibroblast content of p53 protein.
On a aussi confirmé que les expositions aux ultra-violets, en absence de 7- déhydrocholestérol, ont multiplié par 4 la teneur des fibroblastes en protéine p53.It has also been confirmed that ultraviolet exposures, in the absence of 7-dehydrocholesterol, have quadrupled the fibroblast content in p53 protein.
Cet exemple permet de mettre en évidence de façon surprenante que le 7- déhydrocholestérol stimule la protéine de défense p53 nécessaire à la prévention des dommages causés par les rayonnements ultra-violets tels que l'apparition de « cellules sénescentes » ayant perdu la capacité de se reproduire et qui ont des effets néfastes sur le tissu environnant.This example makes it possible to demonstrate, surprisingly, that 7-dehydrocholesterol stimulates the p53 defense protein necessary for the prevention of damage caused by ultraviolet radiation, such as the appearance of "senescent cells" having lost the ability to to reproduce and which have adverse effects on the surrounding tissue.
Différentes compositions sont données ci-après à titre d'exemple pour illustrer les différents modes d'action ou d'utilisation du 7-déhydrocholestérol.Various compositions are given below by way of example to illustrate the different modes of action or use of 7-dehydrocholesterol.
Composition N°1 : Crème cosmétique de protection contre les stress oxydât if s.Composition No. 1: Cosmetic cream for protection against oxidative stress.
On procède comme pour la réalisation d'une émulsion classique huile dans eau, c'est-à-dire qu'on mélange sous agitation à 850C une phase hydrophobe contenant 0,05% en poids de 7-déhydrocholestérol et une phase aqueuse contenant cha- cune des matières premières destinées à conférer au produit les propriétés d'usage habituelles : stabilité, sécurité, étalement facile, toucher final agréable, etc.The procedure is as for the production of a conventional oil-in-water emulsion, that is to say, a hydrophobic phase containing 0.05% by weight of 7-dehydrocholesterol and an aqueous phase is mixed with stirring at 85 ° C. containing each of the raw materials intended to give the product the usual properties of use: stability, safety, easy spreading, pleasant final touch, etc.
La teneur en 7-déhydrocholestérol dans cette crème est de 0,04% en poids. 6 T/FR2009/000463The content of 7-dehydrocholesterol in this cream is 0.04% by weight. 6 T / FR2009 / 000463
On refroidit ensuite sous agitation.It is then cooled with stirring.
Cette crème est appliquée sur le visage, le cou et les mains, de préférence le matin pour préparer la peau aux agressions quotidiennesThis cream is applied to the face, neck and hands, preferably in the morning to prepare the skin for daily aggression
Composition N°2 : Crème cosmétique de protection contre les stress oxydatifs.Composition No. 2: Cosmetic cream for protection against oxidative stress.
On réalise comme ci-dessus une émulsion huile dans eau contenant en plus de l'alpha-tocophérol ainsi que de l'acétate d'alpha-tocophérol ; et lors du refroidissement, à 45°C, on rajoute du phosphate de vitamine C en quantité suffisante pour arriver aux concentrations en poids dans la composition finale de : - 7-déhydrocholestérol 0,05 %As above, an oil-in-water emulsion containing, in addition to alpha-tocopherol, as well as alpha-tocopherol acetate is carried out; and during cooling, at 45 ° C, vitamin C phosphate is added in an amount sufficient to achieve the concentrations by weight in the final composition of: - 7-dehydrocholesterol 0.05%
- alpha-tocophérol 0,05 %- alpha-tocopherol 0.05%
- acétate d'alpha-tocophérol 0,2 %- alpha-tocopherol acetate 0.2%
- phosphate de Vitamine C, sel de Mg 0,2 %.- Vitamin C phosphate, 0.2% Mg salt.
Cette formulation est une crème de jour.This formulation is a day cream.
Composition N°3 : Crème cosmétique de protection contre les stress oxydatifs et de protection filtrante.Composition No. 3: Cosmetic cream for protection against oxidative stress and filter protection.
On réalise comme pour la Composition N°1 , une émulsion huile dans eau avec un ajout d'oxyde de titane suffisant pour que le facteur de protection SPF soit égal à 6. Le produit ainsi obtenu est destiné à être appliqué le matin sur les zones de peau non couvertes, et si possible l'application doit être renouvelée en milieu de journée.As for Composition No. 1, an oil-in-water emulsion is made with an addition of titanium oxide sufficient for the protection factor SPF to be equal to 6. The product thus obtained is intended to be applied in the morning to the zones of skin not covered, and if possible the application must be renewed in the middle of the day.
Composition N°4 : Gel cosmétique de protection contre les stress oxydatifs. On réalise un gel acrylique hydroalcoolique contenant 0,02 % en poids de 7- déhydrocholestérol et contenant en outre 2 % en poids d'un extrait hydroglycolique de Glycyrrhiza glabra.Composition No. 4: Cosmetic gel for protection against oxidative stress. A hydroalcoholic acrylic gel containing 0.02% by weight of 7-dehydrocholesterol and containing 2% by weight of a glycolic acid extract of Glycyrrhiza glabra is prepared.
Ce gel est appliqué le matin et en cours de journée sur les zones de peau exposées au soleil et aux pollutions.This gel is applied in the morning and during the day on skin areas exposed to the sun and pollution.
Composition N°5 : Complément alimentaire pour protéger la peau lors des expositions au soleil ou à la pollution.Composition No. 5: Dietary supplement to protect the skin during exposure to the sun or pollution.
On réalise par les techniques classiques des comprimés dosés à 10 μg de 7- déhydrocholestérol par comprimé, d'une formulation de poudre comprenant 0,1% en poids de 7-déhydrocholestérol. Ces comprimés sont à prendre avec un peu d'eau au cours des repas du matin et de milieu de journée, à raison de un à deux comprimés par prise suivant l'intensité et la durée d'exposition attendue.10 μg of 7-dehydrocholesterol per tablet, a powder formulation comprising 0.1% by weight of 7-dehydrocholesterol are produced by conventional techniques. These tablets should be taken with a little water during the morning and mid-day meals, one to two tablets per dose depending on the intensity and duration of exposure expected.
Composition N°6 : Complément alimentaire pour préparer la peau à l'exposition au soleil.Composition No. 6: Dietary supplement to prepare the skin for sun exposure.
On réalise des capsules contenant 60 mg d'une formulation de poudre à 2 % en poids de 7-déhydrocholestérol, 15 mg d'extrait de thé vert et 25 mg de vitamine C par capsule. La dose quotidienne conseillée est de 2 à 4 capsules par jour, en fonction de l'intensité de l'exposition, en deux prises le matin et en milieu de journée avec un peu d'eau au moment du repas.Capsules containing 60 mg of a 2% by weight powder formulation of 7-dehydrocholesterol, 15 mg of green tea extract and 25 mg of vitamin C per capsule are made. The recommended daily dose is 2 to 4 capsules per day, depending on the intensity of the exposure, in two doses in the morning and in the middle of the day with a little water at the time of the meal.
Composition N°7 : Boisson pour protéger la peau lors des expositions au soleil. On réalise une boisson à base de lait de soja contenant 0,01 % en poids de 7- déhydrocholestérol.Composition No. 7: Drink to protect the skin during sun exposure. A soy milk drink containing 0.01% by weight of 7-dehydrocholesterol is prepared.
Cette boisson est présentée en doses de 100 ml.This drink is presented in doses of 100 ml.
Il est conseillé d'en boire une dose le matin et une dose en milieu de journée au moment des repas. It is advisable to drink a dose in the morning and a dose in the middle of the day at mealtimes.
Claims
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0802400A FR2930445B1 (en) | 2008-04-29 | 2008-04-29 | USE OF A COMPOSITION CONTAINING 7-DEHYDROCHOLESTEROL OR A NATURAL EXTRACT OF MICROORGANISM OR PLANT VEGETABLE OR ANIMAL |
| FR0802400 | 2008-04-29 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2009138582A2 true WO2009138582A2 (en) | 2009-11-19 |
| WO2009138582A3 WO2009138582A3 (en) | 2010-03-11 |
Family
ID=39831610
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/FR2009/000463 Ceased WO2009138582A2 (en) | 2008-04-29 | 2009-04-21 | Use of a composition containing 7-dehydrocholesterol or a natural extract of a vegetable or animal microorganism |
Country Status (2)
| Country | Link |
|---|---|
| FR (1) | FR2930445B1 (en) |
| WO (1) | WO2009138582A2 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017218853A1 (en) * | 2016-06-15 | 2017-12-21 | Ojai Energetics Pbc | Methods and compositions for reducing oxidative stress |
| CN113967174A (en) * | 2021-11-11 | 2022-01-25 | 上海澄穆生物科技有限公司 | A kind of whitening and anti-wrinkle composition and application thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4310511A (en) * | 1980-10-02 | 1982-01-12 | Massachusetts General Hospital | Sunscreen compositions containing Δ5,7 steroidal dienes |
| CA2374763C (en) * | 2000-04-04 | 2008-09-30 | Color Access, Inc. | Composition for improving skin lipid barrier function |
| CA2494156A1 (en) * | 2002-07-31 | 2004-02-19 | Procyte Corporation | Compositions containing peptide copper complexes and phytochemical compounds, and methods related thereto |
| JP2004175744A (en) * | 2002-11-28 | 2004-06-24 | Kose Corp | Dermopathy inhibitor or dermopathy improving agent, and skin care preparation for external use containing the same |
-
2008
- 2008-04-29 FR FR0802400A patent/FR2930445B1/en not_active Expired - Fee Related
-
2009
- 2009-04-21 WO PCT/FR2009/000463 patent/WO2009138582A2/en not_active Ceased
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017218853A1 (en) * | 2016-06-15 | 2017-12-21 | Ojai Energetics Pbc | Methods and compositions for reducing oxidative stress |
| CN113967174A (en) * | 2021-11-11 | 2022-01-25 | 上海澄穆生物科技有限公司 | A kind of whitening and anti-wrinkle composition and application thereof |
| CN113967174B (en) * | 2021-11-11 | 2023-10-20 | 上海澄穆生物科技有限公司 | Whitening and anti-wrinkle composition and application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2930445B1 (en) | 2012-06-08 |
| FR2930445A1 (en) | 2009-10-30 |
| WO2009138582A3 (en) | 2010-03-11 |
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