KR101778227B1 - Composition for anti-obesity comprising extract of Morus alba as effective component - Google Patents

Abstract

The present invention relates to a composition for anti-obesity comprising an extract of Morus alba as an effective component. A leaf extract of Morus alba of a Cheong-ol variety and a fruit extract of Morus alba of a Dae-shim variety have the most excellent effect of inhibiting the differentiation of adipocytes among extracts of the Morus alba varieties, and thus, can be used more effectively as a medicine or health functional food for preventing and treating obesity.

Description

TECHNICAL FIELD The present invention relates to an anti-obesity composition comprising an extract of Morus alba as an active ingredient,

The present invention relates to an anti-obesity composition containing mulberry extract as an active ingredient.

Recent improvements in living standards have resulted in a new eating culture in which the intake of fat and sugar is increased and the intake of fiber is reduced. Especially, preference for high protein-based diet is becoming more pronounced due to the establishment of eating-out culture. On the contrary, it is a reality that obesity population is rapidly increasing with the lifestyle of modern people with little physical activity. Obesity, especially abdominal obesity, is emerging as a serious social problem as the intake of high calorie foods increases and the intake of fiber decreases. Obesity refers to the state of overgrowth of fat tissue, and the increase in body weight due to obesity is mostly due to the increase in fat.

Obesity is a metabolic disorder caused by an imbalance in the intake and consumption of calories, and refers to a state of abnormally increased fat tissue due to excessive calories. It is known that when obesity develops and persists, it induces various diseases, such as hypertension, elevated blood cholesterol, diabetes, kidney disease, stroke, arteriosclerosis, fatty liver, arthritis, cancer, sleep and apnea.

Obesity is caused by accumulation of triglyceride (TG) in the adipocyte by differentiation and adipogenesis of preadipocyte, and regulating this lipogenesis mechanism is called obesity inhibition It is known as an effective treatment method. However, existing obesity remedies are used only by a small number of obese patients because of their ineffective effect or various side effects. The appetite suppressant that acts on the central nervous system includes the noradrenergic drug phentermine, the serotonin drug fluoxetine, the noreadrenaline and serotonin mixed drug sibutramine, Orlistat, the endogenous cannabinoid receptor antagonist rimonabant, and taranabant. However, the above-mentioned obesity treatment drugs have side effects such as nausea, dizziness, diarrhea, constipation and hypertension due to mental disorders such as depression, anxiety and insomnia. In particular, rimonabant and sibutramine are not commercially available due to side effects At present, only orlistat, belviq and qsymia are approved by the FDA. Therefore, it is required to develop a drug for obesity which has a high anti-obesity effect and a low side effect among natural products expected to minimize the possibility of a safety problem. That is, it is required to develop a substance derived from a natural substance, which inhibits the differentiation process of the adipocyte and has a low side effect.

Morus alba ) is a plant of the Rosaceae Mulberry, and has been known to have various pharmacological activities such as leaves, roots, and fruits. It is recorded in Donguibogam that "mulberry leaves are warm and poisonous, and that they eliminate each and every species, and benefit the large and small intestine (remove energy or excitement) and eliminate the windpipe." In Chinese books, It heals the fever, headache, and coughs of the cold, removes the phlegm, cleanses the eyes and liver, heals the eye diseases caused by the hallucinations and fever, and heals the redness, dryness and pain of the eyes. " have. In addition, recent studies have shown that 1-DNJ (1-deoxynojirimycin) and derivatives thereof, which have AIDS virus infection inhibitory effect and anti-cancer effect, dietary fiber and neurotransmitter which have constipation improving effect and heavy metal detoxifying effect (GABA), and it is known to contain Mulberrin, which has anti-inflammatory action and diuretic action, and other flavonoids such as Rutin and Quercetin.

In the case of mulberry berries (hereinafter "Odyssey"), Dongwoo Bohm is also noted that "Black Audi is a gathering spirit of mulberry, and is beneficial to diabetes and the five days. "It has the effect of boosting the liver and kidneys and enhancing the blood of the blood (tack), and it acts as a blood-sucking breeze." Even now, due to its various physiological activities, it is possible to use food such as jam, jelly, juice, syrup, It is widely used as a material or as a medicine.

Korean Patent Laid-Open Publication No. 2015-0083622 discloses an anti-obesity composition using an oak tree and mulberry, and Korean Patent No. 0645385 discloses a composition for inhibiting obesity. However, no anti-obesity composition containing the mulberry extract of the present invention as an active ingredient has been disclosed yet.

The present invention has been made in view of the above needs. In the present invention, when mulberry leaves and fruit extracts of the various cultivars were treated with 3T3-L1 lipid precursor cells, the mulberry leaf extract and the mulberry fruit extract The present inventors have completed the present invention by confirming that the differentiation inhibition activity of lipid precursor cells is remarkably excellent in comparison with the mulberry leaf extract and the fruit extract of other varieties.

In order to solve the above problems, the present invention provides a pharmaceutical composition for preventing or treating obesity, which comprises mulberry extract as an active ingredient.

The present invention also provides a health functional food composition for preventing or ameliorating obesity containing mulberry extract as an active ingredient.

The mulberry leaf extract and the mulberry fruit extract of the mulberry leaf extract of the present invention have the greatest inhibitory effect on the differentiation of adipocytes among the extracts of the mulberry varieties, so they are more useful as medicines or health functional foods for preventing and treating obesity .

FIG. 1 shows the result of measurement of the differentiation rate of lipid precursor cells of the mulberry leaf extract according to an embodiment of the present invention. The control was treated with MDI (IBMX, Dexametason, Insulin), an inducer of lipid differentiation.
FIG. 2 is a result of measuring the differentiation rate of lipid precursor cells of the mulberry fruit extract according to one embodiment of the present invention. The control was treated with MDI (IBMX, Dexametason, Insulin), an inducer of lipid differentiation.

In order to accomplish the object of the present invention, the present invention provides a pharmaceutical composition for preventing or treating obesity comprising mulberry extract as an active ingredient.

In the pharmaceutical composition for preventing or treating obesity of the present invention, the mulberry can be a mulberry leaf of a blueberry variety or a mulberry fruit of a major variety, but is not limited thereto.

The mulberry extract is extracted with a solvent selected from the group consisting of water, lower alcohols having 1 to 4 carbon atoms, and a mixed solvent thereof, preferably ethanol.

In addition, the composition may inhibit the differentiation of adipocytes, but is not limited thereto.

The pharmaceutical compositions of the present invention may further comprise suitable carriers, excipients or diluents conventionally used in the manufacture of pharmaceutical compositions.

The pharmaceutical dosage forms of the compositions according to the invention may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable set.

The pharmaceutical composition according to the present invention may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like, oral preparations, suppositories and sterilized injection solutions according to a conventional method . Examples of carriers, excipients and diluents that can be contained in the pharmaceutical composition containing the mulberry extract include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate , Calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. have. In the case of formulation, a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, or a surfactant is usually used. The solid preparation for oral administration includes at least one excipient such as starch, calcium carbonate, sucrose or lactose, gelatin, and the like to the mulberry extract. The solid preparation for oral administration includes tablets, pills, powders, granules, capsules, . In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Examples of liquid formulations for oral use include suspensions, solutions, emulsions and syrups. In addition to water and liquid paraffin, which are commonly used simple diluents, various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like have. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Examples of the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. Examples of the suppository base include withexol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.

The preferred dosage of the pharmaceutical composition of the present invention varies depending on the condition and the weight of the patient, the degree of disease, the drug form, the administration route and the period, but can be appropriately selected by those skilled in the art.

The mulberry extract of the present invention can be administered to mammals such as rats, mice, livestock, and humans in various routes. All modes of administration may be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intra-uterine or intracerebroventricular injections.

The present invention also provides a health functional food composition for preventing or ameliorating obesity containing mulberry extract as an active ingredient.

In the health functional food composition for prevention or amelioration of obesity of the present invention, the mulberry can be mulberry leaf of a blueberry variety or mulberry fruit of a major variety, but is not limited thereto.

The composition of the present invention may be prepared in any form of powder, granule, ring, tablet, capsule, candy, syrup and beverage, but is not limited thereto.

When the health functional food composition of the present invention is used as a food additive, the health functional food composition may be added as it is, or may be used together with other food or food ingredients, and suitably used according to a conventional method. The active ingredient may be suitably used depending on its intended use (prevention or improvement). Generally, the health functional food composition of the present invention is added in an amount of not more than 15 parts by weight, preferably not more than 10 parts by weight based on the raw material, when the food or beverage is produced. However, in the case of long-term intake intended for health, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount of more than the above range.

There is no particular limitation on the kind of the health functional food. Examples of the foods to which the health functional food composition can be added include dairy products including meat, sausage, bread, chocolate, candy, snacks, confectionery, pizza, ramen and other noodles, gums, ice cream, soups, Drinks, alcoholic beverages, and vitamin complexes, all of which include health foods in a conventional sense.

In addition, the health functional food composition of the present invention can be produced as a food, particularly a functional food. The functional food of the present invention may contain ingredients that are conventionally added. For example, proteins, carbohydrates, fats, nutrients, and seasonings. For example, in the case of a drink, a natural carbohydrate or a flavoring agent may be included as an additional ingredient in addition to the active ingredient. The natural carbohydrate may be selected from the group consisting of monosaccharides (e.g., glucose, fructose, etc.), disaccharides (e.g., maltose, sucrose etc.), oligosaccharides, polysaccharides (e.g., dextrin, cyclodextrin, , Xylitol, sorbitol, erythritol, etc.). The flavoring agent may be a natural flavoring agent (e.g., tau Martin, stevia extract, etc.) and a synthetic flavoring agent (e.g., saccharin, aspartame, etc.).

In addition to the above health functional food composition, it is also possible to use various nutrients, vitamins, electrolytes, flavors, colorants, pectic acids and salts thereof, alginic acid and its salts, organic acids, protective colloid thickening agents, pH adjusting agents, stabilizers, preservatives, glycerin, A carbonating agent used in beverages, and the like. Although the ratio of the above-mentioned ingredients is not critical, it is generally selected in the range of 0.01 to 0.1 part by weight based on 100 parts by weight of the health functional food composition of the present invention.

Hereinafter, the present invention will be described in more detail with reference to Examples. It is to be understood by those skilled in the art that these embodiments are merely illustrative of the present invention and that the scope of the present invention is not limited thereto.

Materials and methods

1. Preparation of Mulberry Extract by Varieties

Mulberry ( Morus ), distributed by the Department of Agricultural Biology, Rural Development Administration alba L.) leaves and fruit (audi). In the case of the mulberry leaves, 500 g of 50% (v / v) ethanol was added to 25 g of mulberry leaf powder, and the mixture was ultrasonically extracted for 30 minutes. After standing for 30 minutes, filter paper (Hyundai micro, No. 20, ). The extracts were concentrated under reduced pressure at 38 ℃ and 10, 50, 100 and 500 ㎍ / ml of mulberry leaf extract were added to distilled water. In the case of fruit (OD), 70% (v / v) alcohol (citric acid) containing 10% 0.1% citric acid was added to 10 g of the sesame powder and ultrasonically extracted at 38 to 40 ° C for 30 minutes. (5,000 g, 4 ° C, and 15 minutes). The supernatant was collected by filtration through a filter paper, concentrated under reduced pressure at 38 ° C using a rotary evaporator, Drying was carried out using a dryer. 500 times, 100 times and 50 times, respectively.

2. 3T3-L1 Lipocytic cells  differentiation

Effect of Mulberry Leaf Extract and Fruit Extract Treatment In order to confirm the lipid differentiation inhibitory activity of 3T3-L1 adipose precursor cells, the cells were fixed with 10% formaldehyde for 30 minutes, and then the cells were stained with Oil red-O solution for 1 hour, And then stained cells were observed under a microscope. After observation, the cells were treated with 100% isopropanol to elute fat accumulated in the cells, and the absorbance was measured at 510 nm using a multilabel reader (VICTOR ^TM X3, PerkinElmer). The absorbance was compared with the absorbance value of the control group and expressed as a percentage And the experiment was repeated three times to show the mean ± SD (mean ± SD) value.

Example  1. 3T3-L1 by mulberry extract treatment Lipocytic cells  Identification of inhibition of differentiation

In Example 1, mulberry leaf extracts of sub-image, yulbone, chrysanthemum, and blueberry varieties were treated with 3T3-L1 lipid precursor cells to inhibit lipid progenitor differentiation. As a result, as shown in FIG. 1, when the mugwort foliar extracts of 500 μg / ml were treated on the lipid precursor cells, the differentiation rates of the lipid precursor cells were significantly different from each other, and the sub-image cultivar was 68.68% 66.09% in Yulbon, 84.85% in Cheongil, and 42.10% in Cheongol, respectively. It was confirmed that the differentiation rate of lipid precursor cells was the lowest in Cheongol varieties.

 When 3T3-L1 adipocyte precursor cells were treated with fruit extracts of supernumerum 2, supernatant, chrysanthemum and wisteria, the effect of inhibiting lipid progenitor cell differentiation was confirmed. As a result, when the mulberry fruit extracts treated with 100-fold diluted extracts as shown in FIG. 2 were treated, the degree of differentiation of the lipid precursor cells was significantly different from that of the cultured mulberry fruit extracts treated with 50-fold diluted mulberry fruit extracts , 93.86% of the second grade, 87.44% of the second grade, 86.81% of the winged varieties showed the differentiation rate of the fat precursor cells, whereas the major variety showed the differentiation rate of 67.70% It was confirmed that the activity of inhibiting the differentiation of lipid precursor cells was remarkably excellent.

Claims (9)

A pharmaceutical composition for preventing or treating obesity, which contains mulberry leaf extract as an active ingredient at a concentration of 500 μg / ml. delete The pharmaceutical composition for preventing or treating obesity according to claim 1, wherein the mulberry leaf extract of the blueberry variety is extracted using water, a lower alcohol having 1 to 4 carbon atoms, or a mixed solvent thereof. The pharmaceutical composition for preventing or treating obesity according to claim 1, wherein the composition inhibits differentiation of adipocytes. The pharmaceutical composition for preventing or treating obesity according to claim 1, further comprising a pharmaceutically acceptable carrier, excipient or diluent in addition to the active ingredient. The pharmaceutical composition for preventing or treating obesity according to claim 1, wherein the composition is prepared from any one of capsules, powders, granules, tablets, suspensions, emulsions, syrups and aerosols. A health functional food composition for prevention or amelioration of obesity containing mulberry leaf extract of 500 쨉 g / ml of a blueberry variety as an active ingredient. delete The health functional food composition for preventing or improving obesity according to claim 7, wherein the composition is prepared from one of powder, granule, ring, tablet, capsule, candy, syrup and beverage.

Images