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WO2008010663A1 - Composition contenant un sophoricoside pour la réduction de poids corporel ou de graisse corporelle - Google Patents

Composition contenant un sophoricoside pour la réduction de poids corporel ou de graisse corporelle Download PDF

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Publication number
WO2008010663A1
WO2008010663A1 PCT/KR2007/003458 KR2007003458W WO2008010663A1 WO 2008010663 A1 WO2008010663 A1 WO 2008010663A1 KR 2007003458 W KR2007003458 W KR 2007003458W WO 2008010663 A1 WO2008010663 A1 WO 2008010663A1
Authority
WO
WIPO (PCT)
Prior art keywords
weight
fat
sophoricoside
reducing
present
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.)
Ceased
Application number
PCT/KR2007/003458
Other languages
English (en)
Inventor
Song-Am Choi
Jae-Seung Choi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
EURAPHARM Inc
Original Assignee
EURAPHARM Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by EURAPHARM Inc filed Critical EURAPHARM Inc
Publication of WO2008010663A1 publication Critical patent/WO2008010663A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents

Definitions

  • the present invention relates to a composition for reducing body-weight or body-fat.
  • the present invention also relates to a method for reducing body-weight or body-fat.
  • Energy homeostasis means the balance of absorbed energy and consumed energy. The excess intake of energy breaks the balance, which is known to be able to cause metabolic disease like obesity or diabetes. Examples of representative drug for decreasing the body-weight in the obesity are sibutramine suppressing appetite, and orlistat decreasing the absorption of lipid in food by suppressing lipase in the body.
  • sibutramine often causes side effects such as the rise of blood pressure, insomnia, mouth dryness and dizziness, and sibutramine also has a drawback that the drug can not be used in patient having cardiovascular disease or uncontrolled hypertension. Orlistat very often causes side effects such as diarrhea, fatty stool and fecal incontinence. In addition, orlistat' s effect does not be apparent in Korean eating less fat than the amount the Westerner eats. There have been lots of efforts to find a drug candidate having a body-weight reducing effect in obesity patient. Procter & Gamble is developing Avasimibe as a therapeutic agent for obesity, which exhibits its body-weight reducing effect by taking part in ciliary neurotropic factor (neurotropic factor related with obesity) .
  • ciliary neurotropic factor neurotropic factor related with obesity
  • Korean patent issued No. 10-0498512 discloses onion peels extract for reducing or maintaining body-weight, and its manufacturing method.
  • Korean patent application No. KR2000- 0010156 discloses a method for extracting and purifying an effective agent from Gyrophora esculenta and plant compositions containing the extract.
  • the object of the present invention is to provide a composition being safe, that is, having little side effects, and having superior body-weight reducing effect and/or body-fat reducing effect, and the medicine or functional food comprising the composition.
  • Another object of the present invention is to provide a safe and effective method for reducing body-weight and/or body- fat.
  • the present invention provides a composition for reducing body-weight or body-fat, comprising sophoricoside represented by the chemical formula 1 below as effective agent.
  • the present invention also provides a medicine or functional food for reducing body-weight and/or body-fat, comprising the composition.
  • the present invention also provides a method for reducing body-weight and/or body-fat, comprising administering the sophoricoside to a subject in need of body-weight or body-fat reduction.
  • Sophoricoside is one of several ingredients included in Sophora japonica. Sophoricoside is known to inhibit the activity of interleukin-5 by acting on eosinophil and basophil playing an important roll in allergic reaction, and thereby treat inflammation reaction by allergy. Thus, based on these results, sophoricoside is being developed as anti-inflammatory drug. However, the fact that this sophoricoside has superior body- weight and/or body-fat reducing effect is not known until now.
  • composition for reducing body-weight or body-fat according to the present invention will be described in more detail.
  • the present inventors completed the present invention by confirming that the administration of sophoricoside effectively reduces the body-weight of high fat diet-induced obesity rat, and reduces peritoneal fat and suppresses the proliferation of adipocyte.
  • Sophoricoside comprised as effective agent in the composition for reducing body-weight or body-fat has a structure of the chemical formula 1.
  • This sophoricoside can be synthesized according to chemical synthesis methods well known in the art to which the present invention pertains, and can be extracted from fruits of Sophora japonica according to extraction methods well known in the art. Conventional solvent extraction method using ethanol, methanol, butanol, chloroform, dichloromethane, hexane, ethylacetate, etc. can be used, or supercritical extraction method can be used. In addition, extracts can be purified to get more pure sophoricoside.
  • sophoricoside is commercially available and for example, can be purchased from Sinobest Inc. (Shangbei Xincun, China) .
  • the sophoricoside has much better effect in reducing body- weight and body-fat than compounds having similar structures.
  • composition for reducing body-weight or body-fat according to the present invention can be formulated into forms of medicine and functional food. These medicine and functional food can comprise pharmaceutically acceptable excipient or additive.
  • the composition for reducing body-weight or body-fat according to the present invention may be administered alone or with any convenient carrier, diluent, etc. and the formulation for administration may be single-dose unit or multiple-dose unit.
  • the medicine and functional food comprising the composition for reducing body-weight or body-fat according to the present invention may be formulated in a solid or liquid form.
  • the solid formulation includes, but is not limited to, a powder, a granule, a tablet, a capsule, a suppository, etc.
  • the solid formulation may further include, but is not limited to, a diluent, a flavoring agent, a binder, a preservative, a disintegrating agent, a lubricant, a filler, etc.
  • the liquid formulation includes, but is not limited to, a solution such as water solution and propylene glycol solution, a suspension, an emulsion, etc., and may be prepared by adding suitable additives such as a coloring agent, a flavoring agent, a stabilizer, a thickener, etc.
  • a powder can be made by simply mixing the sophoricoside of the present invention and pharmaceutically acceptable excipients like lactose, starch, microcrystalline cellulose.
  • a granule can be prepared as follows: mixing the sophoricoside, a pharmaceutically acceptable diluent and a pharmaceutically acceptable binder such as polyvinylpyrrolidone, hydroxypropylcellulose, etc; and wet-granulating with adequate solvent like water, ethanol, isopropanol, etc, or direct- compressing with compressing power.
  • a tablet can be made by mixing the granule with a pharmaceutically acceptable lubricant such as magnesium stearate, and tabletting the mixture.
  • composition for reducing body-weight or body-fat according to the present invention may be administered in forms of, but not limited to, oral formulation, injectable formulation (for example, intramuscular, intraperitoneal, intravenous, infusion, subcutaneous, implant), inhalable, intranasal, vaginal, rectal, sublingual, transdermal, topical, etc. depending on the disorders to be treated and the patient's conditions.
  • injectable formulation for example, intramuscular, intraperitoneal, intravenous, infusion, subcutaneous, implant
  • inhalable intranasal, vaginal, rectal, sublingual, transdermal, topical, etc. depending on the disorders to be treated and the patient's conditions.
  • the composition of the present invention may be formulated in a suitable dosage unit comprising a pharmaceutically acceptable and non-toxic carrier, additive and/or vehicle, which all are generally used in the art, depending on the routes to be administered. Depot type of formulation being able to continuously release drug for desirable time also is included in the scope of the present invention.
  • the sophoricoside of the present invention may be administered daily at a dose of approximately 0.01 mg/kg to approximately 10 g/kg, preferably approximately 0.1 mg/kg to approximately 1 g/kg.
  • the dosage may be varied according to the patient's conditions (age, sex, body weight, etc.), the severity of patients in need thereof, the used effective components, diets, etc.
  • the composition of the present invention may be administered once a day or several times a day in divided doses, if necessary.
  • the present invention provides a method for reducing body-weight or body-fat, or maintaining body-weight, comprising administering sophoricoside represented by the chemical formula 1.
  • Figure 1 is an evaluation result showing that sophoricoside suppresses the proliferation of adipocyte.
  • ICR mice female, 4 weeks, Dae Han Biolink Co., Ltd.
  • 4 groups normal group; high fat diet group (15% fat); high fat diet group (15% fat) + Sophora japonica extract (10 mg/kg) treatment group; and high fat diet group (15% fat) + sophoricoside (1 mg/kg) treatment group
  • mice were raised for 8 weeks. Light and shade of the room was changed every 12 hours, and temperature and humidity were maintained to 22°C and 50-60%, respectively. Water was supplied without any restriction. The change of body-weight was recorded every one week for 8 weeks . Results were shown in the below table 1.
  • Sophora japonica methanol extract and sophoricoside significantly reduced the weight of peritoneal fat.
  • sophoricoside is thought to have much superior peritoneal fat reducing effect.
  • the cells were washed with PBS three times to remove the remaining fixing solution, and then stained in 0.2% Oil Red 0 solution for 1 hour.
  • the cells were washed with distilled water several times to remove the remaining staining reagent. Stained cells were observed with microscope (CKX41, Olympus, Japan), and stained lipid droplet was dissolved into isopropanol and its absorbance was observed at 510 nm. Cells were treated with 10 ug/ml of sophoricoside for 9 days after induction of fat cell differentiation. Results of Oil Red O staining were shown in figure 1. DMSO was used as control.
  • the present invention provides a composition having body-weight reducing effect, peritoneal fat reducing effect and suppressing effect in proliferation od adipocyte.
  • the present invention also provides a medicine or functional food for reducing body-weight and/or body-fat.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une composition sûre et présentant un effet supérieur de réduction de poids corporel et de réduction de graisse corporelle. la composition de la présente invention comprend un sophoricoside en tant qu'agent efficace. La composition de la présente invention peut être utilisée efficacement en tant que médicament ou aliment nutritionnel pour réduire le poids corporel ou la graisse corporelle.
PCT/KR2007/003458 2006-07-18 2007-07-18 Composition contenant un sophoricoside pour la réduction de poids corporel ou de graisse corporelle Ceased WO2008010663A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020060066841A KR100796004B1 (ko) 2006-07-18 2006-07-18 소포리코사이드를 함유하는 체중감소 또는 체지방감소용조성물
KR10-2006-0066841 2006-07-18

Publications (1)

Publication Number Publication Date
WO2008010663A1 true WO2008010663A1 (fr) 2008-01-24

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2007/003458 Ceased WO2008010663A1 (fr) 2006-07-18 2007-07-18 Composition contenant un sophoricoside pour la réduction de poids corporel ou de graisse corporelle

Country Status (2)

Country Link
KR (1) KR100796004B1 (fr)
WO (1) WO2008010663A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2454236C1 (ru) * 2008-08-07 2012-06-27 Нин ДУ Применение софорикозида для получения лекарственных средств
CN107126437A (zh) * 2016-02-29 2017-09-05 上海中医药大学 一种槐角苷的药物用途
EP3628177A1 (fr) * 2018-09-28 2020-04-01 Amorepacific Corporation Composition d'aliment liquide comprenant un extrait de japonica sophora
CN115997928A (zh) * 2022-12-06 2023-04-25 广东金骏康生物技术有限公司 一种可溶性槐米粉在减肥产品中的应用

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102337297B1 (ko) * 2014-08-12 2021-12-07 주식회사 엘지생활건강 소포리코시드 또는 이의 약학적으로 허용가능한 염을 포함하는 피부 탄력, 주름개선, 또는 보습용 화장료 또는 약학 조성물

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6555573B2 (en) * 2000-12-21 2003-04-29 The Quigley Corporation Method and composition for the topical treatment of diabetic neuropathy
US6753325B2 (en) * 2001-11-06 2004-06-22 The Quigley Corporation Composition and method for prevention, reduction and treatment of radiation dermatitis

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010037308A (ko) * 1999-10-15 2001-05-07 김영수 소포리코사이드를 포함하는 인터루킨 관련 면역질환 예방 및 치료용 조성물

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6555573B2 (en) * 2000-12-21 2003-04-29 The Quigley Corporation Method and composition for the topical treatment of diabetic neuropathy
US6753325B2 (en) * 2001-11-06 2004-06-22 The Quigley Corporation Composition and method for prevention, reduction and treatment of radiation dermatitis

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2454236C1 (ru) * 2008-08-07 2012-06-27 Нин ДУ Применение софорикозида для получения лекарственных средств
CN107126437A (zh) * 2016-02-29 2017-09-05 上海中医药大学 一种槐角苷的药物用途
EP3628177A1 (fr) * 2018-09-28 2020-04-01 Amorepacific Corporation Composition d'aliment liquide comprenant un extrait de japonica sophora
CN110959860A (zh) * 2018-09-28 2020-04-07 株式会社爱茉莉太平洋 含有槐树提取物的液体食品组合物
US11154078B2 (en) 2018-09-28 2021-10-26 Amorepacific Corporation Liquid food composition comprising Sophora japonica extract
CN110959860B (zh) * 2018-09-28 2024-06-04 株式会社爱茉莉太平洋 含有槐树提取物的液体食品组合物
CN115997928A (zh) * 2022-12-06 2023-04-25 广东金骏康生物技术有限公司 一种可溶性槐米粉在减肥产品中的应用

Also Published As

Publication number Publication date
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