KR20220071066A - Composition for anti-obesity - Google Patents

Abstract

The present invention relates to an anti-obesity composition containing a Perilla frutescens var. crispa extract. More specifically, the present invention relates to an anti-obesity composition, in which the Perilla frutescens var. crispa extract itself has effects such as inhibition of adipocyte differentiation and changes in blood lipids. The anti-obesity composition further contains extracts of Alpinia officinarum, Phyllostachys nigra var. henonis, Trigonella foenum-graecum, Platycodon grandiflorum, and the like to enhance the effects of the Perilla frutescens var. crispa extract.

Description

Anti-obesity composition {Composition for anti-obesity}

The present invention relates to an anti-obesity composition comprising a chazugi extract, which has effects such as inhibition of adipocyte differentiation and changes in blood lipids by itself. It relates to an anti-obesity composition further comprising Gilgyeong extract and the like.

Obesity is a condition in which adipose tissue is accumulated in the body excessively. In the case of obesity, a person usually has a lot of weight, but even people with a lot of muscle can gain a lot of weight even if they are not obese. do. Obesity is induced by energy imbalance when excessive intake of nutrients compared to energy consumption over a long period of time, and other factors such as hormonal changes, genetics, mental health problems, and socioeconomic factors are complexly related. As the obesity population is increasing worldwide, it is recently pointed out as an important factor in causing adult diseases, and the severity of obesity is emerging as an important problem.

On the other hand, type 2 diabetes among diabetes mellitus is highly correlated with obesity. One of the transcription factors, peroxisome proliferation activated receptor (PPAR), is known to regulate gene expression of enzymes involved in lipid and glucose homeostasis and promote adipose tissue production. In addition, it is known that this change in donation of PPAR causes obesity. In addition, PPARγ is expressed in adipocytes and is a major transcription factor that converts preadipocytes into adipocytes, and is known to induce obesity by this mechanism.

In order to prevent and improve obesity and maintain a healthy weight, it is necessary to continuously manage it throughout life through a balanced diet and regular exercise. In particular, fat cells can be reduced in size once made, but it is impossible to remove them naturally, so it is important to prevent obesity from the beginning because they remain in the body permanently. For the prevention, improvement, or treatment of obesity, methods of reducing intake of calories, increasing activity and exercise, and taking drugs such as reducing fat absorption have been used.

Current treatments for obesity include fenfluramine, which inhibits the serotonin nervous system, ephedrine and caffeine via the noradrenergic nervous system, sibutramine, which acts simultaneously on the serotonin and noradrenergic nervous system, and orli, which reduces fat absorption by inhibiting lipase produced in the pancreas There are drugs such as start. However, among the previously used drugs, fenfluramine was banned because it caused side effects such as primary pulmonary hypertension or heart valve lesions. There is a problem that cannot be done.

Drugs for diet are divided into two mechanisms: inhibiting fat accumulation (appetite suppressants, lipogenesis inhibitors, etc.) or increasing fat activity (thermogenesis, lipolysis, etc.). Although it can be prescribed and taken after treatment, side effects such as digestive disorders and insomnia occur, so the need to develop natural raw materials to replace them is increasing.

On the other hand, Chazugi (蘇葉; Perilla frutescens (L.) Britton var. acuta (Thunb.) Kudo) is an annual medicinal plant belonging to the angiosperm phylum, Dicotyledon, and Lamiaceae, distributed in Korea and China. do. Stems are upright and square, with purple color on the entire pole, fragrant, and the leaves are opposite, broad ovate, pointed at the tip, round or somewhat wedge-shaped at the bottom, with serrated edges, hairs on both sides, and especially veins. It has long hairs on top and the petiole is long. Flowers bloom in August-September in light purple and hang in raceme at the tips of stems and branches, and in the interstitial space of the upper leaves. The calyx is split into two, the upper one has 3 rows again, the lower one has 2 rows, and there are hairs inside and out of the tube. The corolla is short, usually pure, and the lower lip is slightly longer than the upper lip, and the stamens are two-fold. The whole species is purple, and the branches are round and have a net pattern. The leaves and stems are used for medicinal purposes, and the young leaves and seeds are edible. The young leaves are so similar to perilla leaves that it is difficult to distinguish them, and the sugar made from perylaldehyde contained in chaiseki is a sweetener 2,000 times stronger than normal sugar, so it is used for cigarettes, paste, and toothpaste. Those whose leaves are green instead of purple are called for. viridis. The green leaves have white flowers and have a stronger scent than chazugi, and are often used medicinally.

It was confirmed that the chazugi of the present invention is an effective ingredient that can suppress obesity, and in addition, an excellent combination for anti-obesity was developed by conducting an experiment to increase its efficacy.

An object of the present invention is to provide a highly effective anti-obesity composition.

The present invention is an anti-obesity composition containing chazugi extract as an active ingredient. Furthermore, it may be an anti-obesity composition containing chazugi extract and goryanggang extract as active ingredients, and may also be an anti-obesity composition containing chazugi extract, goryanggang extract and bamboo leaf extract as active ingredients.

In addition, it is preferable that the composition of the present invention further comprises fenugreek to gilgyeong extract as an active ingredient.

On the other hand, the fenugreek extract to gilgyeong extract is preferably 25 to 75 parts by weight based on 100 parts by weight of the chazugi extract, and the goryanggang extract and the bamboo leaf extract are 50 to 150 parts by weight based on 100 parts by weight of the chazugi extract. desirable.

And, the content of chazugi in the composition is more effective to be administered at a dose of 3 to 9 mg/kg based on chazugi extract.

The anti-obesity composition of the present invention can maximize the anti-obesity function through synergy between the compositions.

1 is a graph showing the results of a pre-adipocyte growth inhibition experiment.
2 is a graph showing the results of a differentiated adipocyte growth inhibition experiment.
3 is a graph showing changes in body weight as a result of an animal test administered in an embodiment of the present invention.

Chazugi is also called leaflet, when the tips of leaves and stems are used, it is also called perilla, and the seed part is called perilla, and in the present invention, it means perilla. Phenolic compounds, flavonoid glycosides, triterpenoids, and phytosterols have been reported as major components of chazugi. The glomerulonephritis inhibition, antioxidant effect, and b-secretase inhibitory effect were reported for rosmarinic acid isolated from Chazugi, and the antidepressant effect of apigenin was reported. In addition, studies on various physiological activities such as anti-allergic effect, anti-inflammatory effect, anticancer effect, and antibacterial effect have been reported.

The present inventors confirmed that the tea extract itself had effects such as inhibition of adipocyte differentiation and changes in blood lipids, and presented an anti-obesity composition comprising the tea extract as an active ingredient.

In addition, to identify a combination of additional extracts that increase the anti-obesity effect, and to provide an anti-obesity composition further comprising it. Furthermore, effective usage was confirmed.

When chazugi extract is used together with goryanggang extract, it may exhibit a more effective anti-obesity effect. Goryanggang ( Alpinia officinarum Hance) used in the present invention is a perennial herb with a height of about 1 meter belonging to the ginger family, and uses dried rhizomes harvested in autumn. Galangal, called Asian ginger, is slightly different from general ginger ( Zingiber officinale Roscoe). Ordinary ginger (healthy) does not show as much synergistic effect as goryanggang.

In consent treatment, it is effective for abdominal pain, vomiting, and diarrhea, and it is said that it has a high therapeutic response to abdominal pain and diarrhea caused by eating cold foods, drinks, and fruits, and is effective in reducing energy due to kidney weakness and poor circulation, diarrhea, and dysentery. The main components of essential oil include cineol, methylcinnamate, eugenol, pinene, and cardinene. In addition, flavonoids include galangin, kaemperide, kaampferol, quercetin, isoramnetine, and galanzine-3-methyl ether, and galangol, etc., as a new ingredient. It is known that major pharmacological actions include gastric juice secretion promoting action, analgesic action, antioxygen deprivation action, antithrombotic action, anticoagulant action, and peripheral circulation improvement action.

Furthermore, bamboo leaves may be additionally used in the present invention. In the case of the combination of chazugi and bamboo leaves, the synergistic effect did not reach that of goryanggang. However, the effect was excellent when chazugi, goryanggang and bamboo leaves were used together. Goryanggang and bamboo leaves can be used within the range of 50 to 150 parts by weight based on 100 parts by weight of the chazugi extract, but if used too little, the synergistic efficiency is not good, and if too much is used more than necessary, the effect does not increase proportionally. . The preferred amount was 100 parts by weight, and it was effective to use it in a similar specific gravity.

Bamboo leaves are dried leaves of Chamdae, that is, Wangdae. Chamdae grows in the south central part of our country. In summer, the green leaves are picked and dried in a well-ventilated shade. The taste is bitter and the nature is cold. It works on the heart, menopause, stomach, and liver. Relieves fever, relieves chest tightness, removes phlegm, and soothes cramps. It is used for fever, chest tightness, and thirst, for vomiting with stomach fever, coughing with sputum, colds of breath, spasms, laryngitis, and tongue ulcers.

In addition, fenugreek and gilgyeong can be used in the present invention. From the point of view of oriental medicine, this was selected and tested, and it was effective to use fenugreek and gilgyeong together with chazugi. The amount of fenugreek and gilgyeong is preferably 25 to 75 parts by weight based on 100 parts by weight of chazugi, and preferably a ratio of about half of chazugi was appropriate. When used too little, the auxiliary synergistic effect is not large, and the effect does not increase proportionally even if used more than necessary.

The scientific name of Fenugreek (胡蘆巴, Trigonellae Semen) is Trigonella foenum-graecum L, which is also called Fenugreek. The country of origin is India, China, Southeast Asia, Europe, Egypt, Sudan, the United States, Lebanon, and Argentine. Fenugreek seeds are usually dried in the sun and used for medicinal purposes. Since fenugreek is warm in nature and non-toxic, it has been used to treat bladder and kidney diseases since ancient times in Africa, the Middle East, and India, and is also used to treat people with cold sweats or a cold. It is said to cure sore throat, sore knees, damp scrotum, eliminate all 虛寒證 and numbness, treat frequent urination, and treat cold stomach symptoms. Recently, it has been reported that it is effective in maintaining the balance of blood sugar and insulin in the body, so research is being actively conducted.

Gilgyeong is a medicinal material made by removing the root or bark of the bellflower ( Platycodon grandiflorum A. De Candolle) of the bellflower family. This medicine has a slight odor, and the taste is bitter and bitter, and its properties are not biased toward either side. Gilkyung acts on the lungs to treat symptoms of difficulty in breathing with a lot of seawater and sputum, clears the lungs, relieves a stuffy chest, releases cold energy in the stomach, stops coughing and removes phlegm. It is also used when there is general edema due to inability to urinate and the amount of urine is small. It is used for sore throat, cough due to cold, phlegm, nasal congestion, asthma, bronchitis, pleurisy, headache, chills, and tonsillitis. As pharmacological action, expectorant action, blood sugar lowering action, cholesterol lowering action, and antibacterial action were reported.

The shape is irregularly thin and long fusiform or conical, sometimes branched, and the outer surface is grayish brown, light brown or white. The straight root has a concave mark at the top end of which the stem has been removed, and there are thin horizontal folds and vertical grooves near it, and some are slightly bent. Most of the roots except for the upper part have rough vertical folds and horizontal grooves, and there are horizontal lines in the shape of bark. The quality is firm but easy to break. Broken sides are not fibrous and sometimes have large gaps. Other names are Gil Kyung-geun (桔梗根), Gyeongcho (梗草), Kogyeong (苦梗), Ko Gil-gyeong (苦桔梗), Li Yeo (利如), Bangdo (房圖), Baekyak (白藥), and Fubu (符扈). etc.

In the present invention, the key active ingredient is chazugi extract. Additional extracts have a synergistic effect on the anti-obesity effect. The synergistic effect of goryanggang and bamboo leaves is particularly excellent. Furthermore, it is more effective when goryanggang and bamboo leaves are used together. Fenugreek and fenugreek showed excellent effects when used together and added. In the case of chazugi, a key active ingredient, when administered at a dose of 3 to 9 mg/kg based on chazugi extract, a practical effect was shown.

Meanwhile, in the present invention, the term "extract" refers to an active ingredient separated from a natural product. The extract can be obtained by an extraction process using water, an organic solvent, or a mixed solvent thereof, and includes an extract, a dry powder thereof, or any form formulated using the same. In the present invention, the gilgyeong extract may be extracted using water, an organic solvent, or a mixed solvent thereof. Preferably, it is an extract soluble in a lower alcohol having 1 to 4 carbon atoms or a mixed solvent thereof, and it is particularly preferable to extract using ethanol. The extracted liquid may be used directly or concentrated and/or dried. In case of extraction using an organic solvent, methanol, ethanol, isopropanol, butanol, ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, dichloromethane, N, N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol, or an organic solvent that is a mixed solvent thereof is used, and extraction can be performed at room temperature or by heating under conditions in which the active ingredient of the herbal medicine is not destroyed or minimized. Depending on the organic solvent to be extracted, the degree of extraction and loss of the active ingredient of the drug may be different, so an appropriate organic solvent should be selected and used. The extraction method is not particularly limited, and examples thereof include cold extraction, ultrasonic extraction, and reflux cooling extraction. Filtration is a process of removing suspended solid particles from the extract, and may use cotton, nylon, etc. to filter out particles, ultrafiltration, cryofiltration, centrifugation, etc., but is not limited thereto. Methods such as reduced pressure concentration, reverse osmosis concentration, etc. may be used for concentration of the extract. The drying step after concentration includes, but is not limited to, freeze drying, vacuum drying, hot air drying, spray drying, reduced pressure drying, foam drying, high frequency drying, infrared drying, and the like. In some cases, a process of pulverizing the final dried extract may be added. In addition, the extract may be subjected to an additional fractionation process.

Hereinafter, the present invention will be described in more detail through Examples and Test Examples. However, these examples and the like are used for the purpose of illustration to help the understanding of the present invention, and the scope and scope of the present invention is not limited thereto.

<Example 1>

3 kg of chazugi purchased from the Seoul Pharmacy Store was dried and pulverized in the shade and at room temperature for 5 days. The pulverized charzugi was immersed in 30 ℓ of 40% alcohol (ethanol) and extracted at 50° C. for 24 hours. This was filtered through filter paper, dried under reduced pressure, and concentrated to obtain a total extract of 605 g.

<Example 2>

The extraction was performed in the same manner as in Example 1 using 2 kg of goryanggang purchased from the Seoul Pharmacopeia to obtain a total extract of 310 g.

<Example 3>

Using 2 kg of bamboo leaves purchased from Seoul Pharmacopoeia, extraction was performed in the same manner as in Example 1 to obtain a total extract of 290 g.

<Example 4>

It was extracted in the same way using 3 kg of fenugreek purchased from Seoul Pharmacy Store, to obtain a total extract of 530 g.

<Example 5>

It was extracted in the same way using 3 kg of gilgyeong purchased from the Seoul Pharmacy Store, to obtain a total extract of 510 g.

<Example 6>

The composition was constituted in a ratio of 100 parts by weight of the goryanggang extract of Example 2 to 100 parts by weight of the chazugi extract of Example 1.

<Example 7>

The composition was constituted in a ratio of 100 parts by weight of the bamboo leaf extract of Example 3 to 100 parts by weight of the chazugi extract of Example 1.

<Example 8>

The composition was constituted in a ratio of 100 parts by weight of the goryanggang extract of Example 2 and 100 parts by weight of the bamboo leaf extract of Example 3 with respect to 100 parts by weight of the chazugi extract of Example 1.

<Example 9>

The composition was constituted in a ratio of 100 parts by weight of the fenugreek extract of Example 4 to 100 parts by weight of the chazugi extract of Example 1.

<Example 10>

The composition was constituted in a ratio of 100 parts by weight of the gilgyeong extract of Example 5 to 100 parts by weight of the chazugi extract of Example 1.

<Example 11>

In addition to Example 6, 50 parts by weight of the fenugreek extract of Example 4 and 50 parts by weight of the Gilkyong extract of Example 5 were added to constitute a composition.

<Example 12>

In addition to Example 7, 50 parts by weight of the fenugreek extract of Example 4 and 50 parts by weight of the Gilkyong extract of Example 5 were added to constitute a composition.

<Example 13>

In addition to Example 8, 50 parts by weight of the fenugreek extract of Example 4 and 50 parts by weight of the Gilkyong extract of Example 5 were added to constitute a composition.

<Toxicity evaluation>

MTT analysis was performed to confirm the effect of the Examples on the viability of 3T3-L1 preadipocytes. 3T3-L1 preadipocytes were seeded in 96-well plates at a concentration of 1Х10 ⁵ cells/ml. Thereafter, the cells differentiated through differentiation induction were treated with DW in Examples and a negative control at a concentration of 50 to 250 ppm and cultured for 2 days. After 2 days, the medium was replaced with a medium containing 0.5 mg/ml of MTT reagent and cultured for 1 hour. After that, the medium was discarded and 100 μl of DMSO was dispensed to dissolve the generated formazan, and absorbance was measured at a wavelength of 540 nm.

At all concentrations, there was no significant difference compared to the negative control group, so it was judged that cytotoxicity was not a problem.

<Experiment to inhibit growth of preadipocytes>

3T3-L1 preadipocytes were incubated in a 96-well plate at a density of 1x10 ⁴ cells/ml. Except for the negative control (DMSO solvent control), Garcinia cambogia extract (positive control) and Examples were treated in the cells at a concentration of 100 ppm. It was repeated three times for each group and the average value was used. Garcinia cambogia extract is a health functional food ingredient that has been recognized for its ability to inhibit body fat accumulation. After administration and incubation for 48 hours, the cell growth status was recorded, and the growth inhibitory effect of each test substance on 3T3-L1 preadipocytes was analyzed by MTT analysis.

The results are shown in FIG. 1 compared to the control group. The chazugi extract showed better results than the garcinia cambogia extract, which is a positive control, and the goryanggang extract itself showed similar effects to the garcinia cambogia extract. Although fenugreek and gilkyung of Examples 4 and 5 had no significant effect on their own, synergistic effects were confirmed in Examples 11 to 13 in which fenugreek and gilkyung were used together. The effect of Example 1 alone is also significant, and it was confirmed that Examples 6 and 8, and the combination using fenugreek and gilgyeong together in them, were more effective.

<Experiment to inhibit the growth of differentiated adipocytes>

3T3-L1 cells were incubated in 12-well plates at a density of 1× ^{10 5} cells/well. 3T3-L1 preadipocytes were cultured in a medium containing 10% BCS and 1% P/S, and the culture environment was maintained at 37°C and 5% carbon dioxide. Two days after cell confluency was reached (Day 0), it was replaced with a differentiation induction medium containing 5 μg/ml insulin, 1 dexamethasone, 0.5 mM IBMX, and 10% FBS. From Day 2, the medium containing only 5 μg/ml insulin and 10% FBS was replaced with a new medium once every two days and cultured for 8 days. Cells were treated with the extract from Day 0, and the final concentration of cells treated was 250 ppm based on the concentration of chazugi.

The results are shown in FIG. 2 compared to the control group. The tea extract showed better results than the Garcinia cambogia extract as a positive control. Also, the garcinia cambogia extract itself showed similar effects, confirming that the goryanggang extract itself has a significant meaning. Overall, it showed a trend similar to the results of the preadipocyte growth inhibition experiment.

<Experiment of weight change after induction of obesity>

In this experiment, 8-week-old female B6 mice were used. In this experiment, it was divided into a normal control group, an obese control group, and a group administered with the extract of Example. This experiment was performed using 5 female mice in each group. During the experimental period, with the exception of mice in the normal control group fed a normal-fat diet, other groups of mice were continuously fed a high-fat diet for 8 weeks to induce obesity. At the same time, the test substance was orally administered daily for 8 weeks. Reflecting the results obtained through the preadipocyte growth inhibition experiment and the differentiated adipocyte growth inhibition experiment, Garcinia cambogia extract was used as a positive control group, and the combinations of Examples 1, 2, 6, 8, 11, and 13 were evaluated. Differences in body weight and body fat between mice in groups were evaluated, and the body weight and average food intake of each animal were recorded weekly for the duration of the experiment.

The final weight change is shown in FIG. 3 . The normal control group showed an increase in body weight of 9 g, and the obese control group fed a high-fat diet increased the body weight by 33.5 g. When Garcinia cambogia extract, which is a positive control, was administered, a weight gain of 14.8 g was shown, showing that there was an anti-obesity effect. On the other hand, the chazugi extract showed better results than the positive control, and it showed better results when adding goryanggang, further adding goryanggang and bamboo leaves together, and adding a combination of fenugreek and gilkyong. .

<Changes in blood biochemical indicators>

Fasting (water is supplied) for more than 16 hours before and 8 weeks after the start of the animal experiment, after primary anesthesia through isoflurane (Baxter, USA) inhalation, fasting blood is collected from the inferior vena cava total cholesterol (Total-cholesterol; Total-C), triglyceride (TG), free fatty acid (FFA), high-density lipoprotein-cholesterol (HDL-cholesterol; HDL-C), And the amount of non-high-density lipoprotein-cholesterol (nonHDL-cholesterol; nonHDL-C) was measured. The content of all five lipids was increased in the obese control group compared to the normal control group. In the case of the positive control group, the contents of TG, Total-C and FFA were slightly decreased compared to the obese control group, but did not show much difference, HDL-C showed a similar level, and the content of nonHDL-C was significantly decreased. did. On the contrary, the Examples of the present invention showed more effective results overall, and in particular, the effects of Examples 8 and 13 were excellent.

<Sensory evaluation>

Since the composition of the present invention is a safe material that can be used as a food composition, weight measurement and subjective feeling (fatigue, defecation effect) were evaluated for 25 adult males and 25 adult females (40s to 50s). For the composition of placebo, Garcinia cambogia extract, Example 1, Example 8, and Example 13, 5 adult males and 5 adult females were assigned to each. Those of Examples showed higher satisfaction than the Garcinia cambogia extract used as a positive control.

Claims (6)

An anti-obesity composition containing chazugi extract as an active ingredient. Anti-obesity composition containing chazugi extract and goryanggang extract as active ingredients, An anti-obesity composition containing chazugi extract, goryanggang extract and bamboo leaf extract as active ingredients. 4. The method according to any one of claims 1 to 3,
The composition is an anti-obesity composition, characterized in that it further comprises fenugreek extract and Gilkyung extract as active ingredients. 5. The method of claim 4,
The anti-obesity composition, characterized in that the fenugreek extract to gilgyeong extract is 25 to 75 parts by weight based on 100 parts by weight of the chazugi extract. 4. The method according to any one of claims 2 to 3,
The anti-obesity composition, characterized in that the goryanggang extract to the bamboo leaf extract is 50 to 150 parts by weight based on 100 parts by weight of the chazugi extract.

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