WO2014157865A1

WO2014157865A1 - Composition for preventing, ameliorating, or treating obesity containing extracts of litchi chinensis and artemisia iwayomogi as active ingredients

Info

Publication number: WO2014157865A1
Application number: PCT/KR2014/002241
Authority: WO
Inventors: 이재걸; 고찬영; 김대훈; 김소라
Original assignee: 현대약품 주식회사
Priority date: 2013-03-29
Filing date: 2014-03-17
Publication date: 2014-10-02
Also published as: KR20140118531A

Abstract

The present invention provides a composition for preventing, ameliorating, or treating obesity containing extracts of Litchi chinensis and Artemisia iwayomogi as active ingredients. The composition of the present invention, which is a mixture of the extracts of Litchi chinensis and Artemisia iwayomogi, exhibits a stronger effect in losing body weight compared with individual extracts of Litchi chinensis and Artemisia iwayomogim, thereby ultimately exhibiting activity to prevent or treat obesity. The present invention provides foundational data as medicine and food of the extracts of Litchi chinensis and Artemisia iwayomogim which have efficacies in preventing and treating obesity.

Description

【Specification】

[Name of invention]

Composition for the prevention, improvement or treatment of obesity, including fibroblasts and Haninjin extract as an active ingredient

[Technical field]

The present invention relates to a composition for the prevention, improvement or treatment of obesity, including fibroblasts and Haninjin extract as an active ingredient. [Related Patent Application]

This patent application claims priority to Korean Patent Application No. 10—2013-0034647 filed with the Korean Patent Office on March 29, 2013, the disclosure of which is incorporated herein by reference. [Background technology]

The World Health Organization has warned that over 1 billion people who are overweight and obese (more than 30 in BMI) will produce 50% in 2015, up to 1.5 billion people, producing serious health problems (September 22, 2005). ). Obesity is a cause of various diseases, 80¾ of diabetic patients, 21% of heart diseases are caused by obesity, and the socioeconomic loss caused by obesity is huge [US $ 117 billion annually; In Korea, the amount has increased from 1.17 trillion won in 2020 years to 1.8 trillion won in 2005 (direct cost KRW 1.1 trillion, KRW 8.87 billion, indirect cost KRW 720.2 billion). Therefore, the development of safe and effective treatment for obesity can reduce the enormous socioeconomic loss. However, the drugs that can solve the market situation are limited to appetite suppressants and fat absorption inhibitors, which are not as expected, and there are various side effects shown below. Xenical (Roche) inhibits fat absorption by inducing lipase inhibition in the pancreas and digestive system, accompanied by low weight loss effects of 2–3¾ and frequent side effects such as frequent diarrhea and fatty bowel movements. In addition, reductil (Abbott) suppresses appetite by inhibiting resorption of serotonin and noradrenaline, which has a 5-10% weight loss effect, but has side effects of cardiovascular diseases such as stroke and myocardial infarction. The European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) have been taken out of the market with prescriptions, suspensions, and voluntary recall recommendations, and were discontinued by the Korea Food and Drug Administration in October 2010. In addition, many products developed as anti-obesity drugs have been banned due to serious side effects. For example, aminophylline has been reported to have a wide range of side effects in the mental nervous system, circulatory system, and digestive system, despite its excellent body fat breakdown effect.Fenfuramine, dexfenfluramine, topirame, ephedrine, etc. It was determined that the sale was prohibited. As Western medicine has shown limitations in overcoming side effects and chronic diseases of synthetic drugs, the value of natural food products is emerging. Throughout this specification, numerous papers and patent documents are referenced and their citations are indicated. The disclosures of cited papers and patent documents are incorporated herein by reference in their entirety, so that the level of the technical field to which the present invention belongs and the contents of the present invention are more clearly explained.

[Content of invention]

[Problem to solve]

The present inventors made an intensive study to develop an effective substance to treat or prevent obesity and to develop a substance that is safe for the human body, especially plant-derived substances. As a result, the extract of Yeogi-nucleus and Haninjin, which has been conventionally used as a herbal medicine, prevents and improves obesity. Or by discovering that it is very effective in treating the present invention.

Accordingly, it is an object of the present invention to provide a composition for the prevention, improvement or treatment of obesity, which has the extract of Lilium nucleus and Hanjinjin as an active ingredient.

Another object of the present invention is to provide a pharmaceutical composition for the prevention or treatment of obesity, which has an extract of Yeogeruk Nucleus and Haninjin as an active ingredient.

Still another object of the present invention is to provide a food composition for preventing or improving obesity, which has an extract of Yeogeruk Nucleus and Haninjin as an active ingredient. Other objects and advantages of the present invention are detailed description of the invention, claims The above makes it clearer.

[Measures of problem]

According to one aspect of the present invention, the present invention provides a composition for the prevention, improvement or treatment of obesity, including fibroblasts and Hanjinjin extract as an active ingredient. The present inventors made an intensive study to develop an effective material for treating or preventing obesity, and especially to develop a substance that is safe for the human body, especially plant-derived substances. As a result, the extract mixture of Yeogi-nucleus and Han-injin, which has been conventionally used as a herbal medicine, prevents obesity. It was found to be very effective in improving or treating the disease.

Fibrin nucleus used as an active ingredient in the composition of the present invention means a seed of Litchi chinensis Sonn.

Haninjin used as an active ingredient in the composition of the present invention is a deciduous broad-leaved shrub belonging to the Asteraceae, it is also called heather, white wormwood, ulsan wormwood.

When the filtrate nucleus and Haninjin extract used in the composition of the present invention is obtained by treating the filtrate and the extraction solvent to the filtrate nucleus and Haninjin, various extraction solvents may be used. Preferably, a polar solvent or a nonpolar solvent can be used. Suitable polar solvents include (i) water, (ii) alcohols (preferably methanol, ethanol, propanol, butane, normal-propane, iso-propane, normal-butane, 1-pentanol , 2-butoxyethanol or ethylene glycol), (iii) acetic acid, (iv) dimethyl-formamide (DMFO) and (v) dimethyl sul foxide (DMS0). Suitable non-polar solvents are acetone, acetonitrile, ethyl acetate, methyl acetate, fluoroalkane, pentane, hexane, 2,2,4-trimethylpentane, decane, cyclonucleic acid, cyclopentane, diisobutylene, 1- Pentene, 1-chlorobutane, 1-chloropentane, 0-xylene, diisopropyl ether, 2-chloropropane, toluene, 1-chlorotropane chlorobenzene benzene, diethyl ether, diethyl sulfide, chloroform , Dichloromethane, 1,2-dichloroethane, anneal, diethylamine, ether, carbon tetrachloride and THF.

According to one embodiment of the present invention, the extraction solvent used in the present invention

(a) water, (b) anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms (methanol, ethanol Propane, butane, etc.), (c) a mixed solvent of the lower alcohol and water, (d) acetone, (e) ethyl acetate, (f) chloroform, ( _g ) butyl acetate, (h) 1,3 Butylene glycol, (i) nucleic acid and (j) diethyl ether.

According to another embodiment of the present invention, the extract of the present invention is obtained by treating water, methanol ethanol or a combination thereof with fibroblasts and Hanjin.

According to a particular embodiment of the present invention, the extract of the present invention is obtained by treating fermented liquor and water with a combination of fermented core and Hanjin, respectively, and then mixed.

As used herein, the term 'extract' has a meaning commonly used as a crude extract in the art as described above, but broadly includes a fraction additionally extracting the extract. That is, the nucleus nucleus and Haninjin extract includes not only those obtained by using the aforementioned extraction solvent, but also those obtained by additionally applying a purification process thereto. For example, fractions obtained by passing the extract through an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity), etc. Fractions obtained through various purification methods can be included in the extract of the fibrils and Hanjinjin of the present invention.

Fibrils and Hanjinjin extract used in the present invention may be prepared in a powder state by an additional process such as distillation under reduced pressure and freeze drying or spray drying.

The composition of the present invention works very effectively in the prevention or treatment of obesity.

As used herein, the term "obesity" refers to the accumulation of excessive body fat in the body. Obesity not only reduces social activities, but also indicates psychological disorders such as anxiety and depression, including cardiovascular disease, lipid metabolism, hypercholesterolemia, fatty liver, angina pectoris, myocardial infarction, arteriosclerosis, coronary artery disease, stroke, It is a factor that increases the risk of adult diseases such as high blood pressure and diabetes.

The composition of the present invention reduces weight. According to one embodiment of the present invention, when the composition of the present invention is fed to a test animal, it was found that the effect of inhibiting weight gain is greater as compared to the diet of the high fat diet control group, mononucleus mononuclear extract and Hanjinjin single extract diet group (Table 5). . The composition of the present invention may be prepared as a pharmaceutical composition. According to a preferred embodiment of the present invention, the composition of the present invention comprises (a) a pharmaceutically effective amount of the fibrinomegaly and Haninjin extract of the present invention described above; And (b) a pharmaceutically acceptable carrier. As used herein, the term "pharmaceutically effective amount" means an amount sufficient to achieve the efficacy or activity of the above-mentioned fibrinomegaly and Hanjinjin extract.

When the composition of the present invention is made into a pharmaceutical composition, the pharmaceutical composition of the present invention includes a pharmaceutically acceptable carrier. Pharmaceutically acceptable carriers included in the pharmaceutical compositions of the present invention are those commonly used in the preparation of lactose, dextrose, sucrose, sorbbi, mantle, starch, acacia gum, phosphate, alginate , Gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and minerals Oils and the like, but are not limited thereto. The pharmaceutical composition of the present invention may further include lubricants, wetting agents, sweeteners, flavoring agents, emulsifiers, suspending agents, preservatives, and the like, in addition to the above components. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington's Pharmaceutical Sciences (19th ed., 1995).

The pharmaceutical composition of the present invention may be administered orally or parenterally, and preferably applied by oral administration.

Suitable dosages of the pharmaceutical compositions of the present invention vary depending on factors such as formulation method, mode of administration, age, weight, sex, morbidity, food, time of administration, route of administration, rate of excretion and response sensitivity of the patient. Can be prescribed. Typical dosages of the pharmaceutical compositions of the invention are in the range of 0.001-100 nig / kg on an adult basis.

The pharmaceutical composition of the present invention may be formulated in a unit dose form by using a pharmaceutically acceptable carrier and / or excipient according to a method which can be easily carried out by a person of ordinary skill in the art. It can be made or prepared by incorporating into a multi-dose container. The formulation may be in the form of a solution, suspension, syrup or emulsion in an oil or aqueous medium. Or it may be in the form of extracts, powders, powders, granules, tablets or accelerators, and may further include a dispersant or stabilizer. The composition of the present invention may be provided as a food composition.

According to a preferred embodiment of the present invention, the composition of the present invention comprises (a) a food-effective amount of the above-mentioned fibrinomegalo and Haninjin extract of the present invention; And (b) a food acceptable composition.

When the composition of the present invention is made of a food composition, as an active ingredient, as well as the extract of fibrils and Korean jinjin, as well as ingredients commonly added during food production, for example, proteins, carbohydrates, fats, nutrients, seasonings And flavoring agents. Examples of the above carbohydrates include monosaccharides such as glucose, fructose, and the like; Disaccharides such as maltose, sucrose, oligosaccharides and the like; And sugar alcohols such as polysaccharides such as conventional sugars such as textulin and cyclotextile dung, xylyl, sorbitol and erythritol. As flavoring agents, natural flavoring agents [tautin, stevia extract (for example, rebaudioside A, glycyrrhizin, etc.) and synthetic flavorings (saccharin, aspartame, etc.) can be used. When the food composition of the preparation is made with a drink, the citric acid, liquid fructose, sugar, glucose, acetic acid, malic acid, fruit juice, two-layer extract, jujube extract, licorice extract, etc. may be further included in addition to the fibrils and extracts of Hanjinjin of the present invention. .

【Effects of the Invention】

The features and advantages of the present invention are summarized as follows:

(i) The present invention provides a composition for the prevention, improvement or treatment of obesity, including fibroblasts and Hanjinjin extract as an active ingredient.

(ii) The composition of the present invention is a mixture of fibroblasts and Hanjin jin extracts, shows a high weight reduction effect compared to the extracts of fibroblasts and Hanjin jin, and ultimately exhibits prophylactic or therapeutic activity of obesity.

(Hi) The present invention provides basic data as medicines and foods of fibrinomegaly and Hanjinjin extract complexes having efficacy of preventing and treating obesity. [Brief Description of Drawings]

Figure 1 is the result of measuring the change in body weight after dieting fibroblasts and Haninjin extract in experimental animals.

Figure 2 is a result showing the increased body weight after dieting fibroblasts and Haninjin extract in experimental animals. Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, it will be apparent to those skilled in the art that the scope of the present invention is not limited by these examples in accordance with the gist of the present invention. .

EXAMPLE

Example 1 Preparation of Fibroblast and Haninjin Extract

1-1. Extraction method

Fibroblasts (500 g) and Hanjin (600 g) were respectively ground and chilled in 3 L of 95¾ »fermented alcohol for 48 hours, respectively, to obtain an extract. After drying under reduced pressure, the dried product was recovered and the yield was measured. Total extraction was repeated three times per drug to increase the yield.

1-2. Extraction results

Nucleus

Filtration nuclei (500 g) were extracted to recover 15.26 g as a solid.

■ [Table 1]

* Domestic registered patent: Composition for the prevention or treatment of fatty liver or obesity, including fibromyalgia extract (Deoktook: 10-0969170)

Haninjin (600 g) was extracted to recover 27.87 g as a solid with high viscosity.

Table 2

* Domestic patent: Novel use of scopoline and its derivatives (Registration No .: 10-0981350) Example 2: Test for weight loss effect of fibroblast and Haninjin natural products

2-1. Breeding of Experimental Animals

Sprague-Dawley rats, 4 weeks old, were supplied to Nara Biotech every 100 males, and fed to the environment by feeding them with solid feed and water. For one week, high-fat feed was administered and administered temporarily, and the experiment was conducted at the age of five weeks.

Feed was freely consumed with high-fat feed Kcal 60% fat (D12492, Research diet, New Brunswick, NJ 08901). . 23 ± 3 ° C, Humidity 55 土 15, Roughness 150-300 Lux, Experimental animals were bred at 10-20 times / hour ventilation at 8 am-8 pm.

2-2. Test substance, natural product

The amount of natural product dissolved in CMC (0.5% carboxymethyl cellulose; Sigma-Aldrich, USA) was prepared at 10 ml / kg and the concentration of the test substance to be tested was changed. The reagents used are shown in Table 3.

Table 3

Major reagents

Table 4

Composition of test group

2-3. Test Methods

After group separation by body weight, test substance and control substance were administered once a day, and weight and feed were measured twice a week to measure weight change and feed intake.

2-4. Test result

Changes in body weight of experimental animals dieted with fibrinomegaly and Hanjin extract were measured (Tables 5 and 6). Body weight gain was decreased in the experimental animals dieted with the fibrils and Hanjin extracts compared to the experimental animals fed the mononucleus or Haninjin single extract.

Table 5

Change in Body Weight of Laboratory Animal

Having described the specific part of the present invention in detail, it is apparent to those skilled in the art that such a specific technology is only a preferred embodiment, and the scope of the present invention is not limited thereto. Accordingly, the substantial scope of the invention will be defined by the appended claims and equivalents thereof.

Claims

[Range of request]

[Claim 1]

A composition for preventing, ameliorating or treating obesity, comprising an extract of Lichchi chinensis Sonn and Artemisiae Iwayomogi i Herba. As an active ingredient.

[Claim 2]

The composition of claim 1, wherein the fibrinomegaly and Haninjin extract are extracted with an organic solvent, water, or a mixture thereof.

[Claim 3]

The composition of claim 2, wherein the organic solvent is selected from the group consisting of ethane, methanol, acetone, nucleic acid, ethyl acetate and methylene chloride.

[Claim 4]

The composition of claim 1, wherein said composition reduces weight.

[Claim 5]

(a) a therapeutically effective amount of the composition of any one of claims 1 or 4 above; And (b) a pharmaceutical composition for the prevention or treatment of obesity comprising a pharmaceutically acceptable carrier.

[Claim 6]

(a) a food-effective amount of the composition of any one of the preceding claims; And (b) food composition for the prevention or improvement of obesity comprising a food acceptable carrier.

[Claim 7]

A method of preventing or treating obesity, comprising administering to a subject a composition comprising Lichichi chinensis Sonn. And Artemisiae Iwayomogi i Herba.

[Claim 8]

8. The method according to claim 7, wherein the fibrinomegaly and Hanjinjin extract are extracted with an organic solvent, water or a combination thereof.

[Claim 9]

The method of claim 8, wherein the organic solvent is selected from the group consisting of ethanol, methanol, acetone, hexane, ethyl acetate and methylene chloride.

[Claim 10]

8. The method of claim 7, wherein said composition reduces weight.