KR100773246B1 - Composition comprising of trillium kamtschaticum extracts as an effective ingredient for decreasing weight gain and lowering plasma glucose level - Google Patents

Abstract

A composition comprising an ethanol extract of Trillium Kamtschaticum is provided to inhibit the increase of body weight and lower the blood sugar, thereby inducing the decrease of weight and the health of body. A composition for inhibiting obesity and lowering blood sugar comprises an ethanol extract of Trillium Kamtschaticum extract as an effective ingredient, which is prepared by crushing dried aerial parts of Trillium Kamtschaticum and extracting the powder with 50% ethanol at room temperature for 2-3 days.

Description

Composition comprising of Trillium Kamtschaticum extracts as an effective ingredient for decreasing weight gain and lowering plasma glucose level}

1 is a graph showing the effect of inhibiting fat absorption by the concentration of ethanol extract of age.

Figure 2 is a graph showing the percentage inhibition rate of the ethanol extract of the age of the age based on the activity of alpha-glucocosidase of the control group.

Figure 3 is a graph showing the amount of change in body weight after feeding the high fat diet mixed with high fat diet and orilstat and ethanol extract of age.

Figure 4 is a graph showing the average blood glucose of the experimental group by measuring the fasting blood glucose after dieting the experimental animals for 8 weeks.

The present invention relates to a composition for inhibiting obesity and lowering blood sugar, containing an ethanol extract of Trillium Kamtschaticum as an active ingredient having lipid energy and glycemic control efficacy. More specifically, the composition for inhibiting obesity, which inhibits energy accumulation in adipocytes by using fatty acid absorption inhibitory effect of ethanol extract of age-age and the activity of alpha-glucosidase of ethanol extract of age-age It relates to a blood sugar lowering composition having a blood sugar strengthening activity by the effect of inhibiting.

Globally, the number of obese people is about 150 million, and in Korea, the proportion of obese people is about 30% in 2004 and the rate is increasing every year. Accordingly, with the improvement of economic level and the increasing interest in beauty, obesity has been treated by various methods ranging from conventional diet or exercise to drug treatment. However, some of the obesity inhibitors and diet ingredients that are inundated in Korea have not been scientifically verified.

Obesity patients are not only directly tired or fatigued, but also suffer from fatal complications such as diabetes, hypertension, and coronary artery disease. Recently, diabetes mellitus, arteriosclerosis, and other symptoms occur simultaneously to the disease called metabolic syndrome (metabolic syndrome), and their pathogenesis and comprehensive treatment methods are on the move. Given the fact that obesity should be managed with other diseases, not individual diseases, a reduction in body fat should be considered first, rather than simple weight loss, leading to weight loss by preventing the accumulation of digested fat and sugar in the body. It will be an important way of treating obesity.

Diabetes is a metabolic disorder caused by dysfunction and lack of action of insulin secreted by pancreatic cells, which leads to overproduction of glucose, breakdown of body fat, and waste of protein and abnormally accelerates glucagon secretion, leading to metabolic disruption. . Diabetes is divided into pediatric diabetes (type 1 diabetes) and adult diabetes (type 2 diabetes), which is responsible for more than 90% of diabetics and is more likely to develop after age 40, especially in obese people. Insulin resistance is characterized. People with insulin resistance develop hyperinsulinemia because they regulate high blood sugar to normal blood sugar by releasing too much insulin.

Oral hypoglycemic agents currently used in diabetics include alpha-glycosidase inhibitors, sulfonylureas and biguyanide, and alpha-glycosidase inhibitors It delays the digestion and absorption of carbohydrates in the diet, thereby reducing the elevation of postprandial blood sugar and blood insulin, thus showing the therapeutic effect of diabetes. Alpha-glucosidase has the advantage of promoting the secretion of glucagon-like peptide-1, which promotes insulin secretion and suppresses glucagon secretion without causing hyperinsulinemia or hypoglycemia. Have. However, long-term use may have side effects such as abdominal bloating and vomiting diarrhea in some patients, which may limit their use.

As such, obesity and diabetes are steadily increasing due to the development of modern society and westernization of dietary life, which causes various fatal complications. Eating foods raises blood sugar and stimulates insulin production and secretion. Insulin that travels through the blood stimulates glucose transporter 4 (GLUT4) in muscles and adipose tissues to absorb glucose in the blood, and raises the concentration of cAMP in the cell to increase protein Kinase A (PKA). Activate it. PKA stimulates hormone-sensitive lipase to break down fats in cells into fatty acids and glycerol, which are then secreted out of the cells. Fatty acids released into the blood are converted to acyl-CoA and used in the liver or flow into the mitochondria and are oxidized and used as energy sources. However, excess fatty acids are moved back to other tissues by the blood and absorbed into fat cells or lipid droplets and accumulate in the form of triglycerides.

Age herb ( Trillium Kamtschaticum ) according to the present invention is a perennial herb of the monocotyledonous genus Liliaceae, also known as Birthroot. It is mainly distributed in Korea (northern), northeastern China, eastern Siberia, Japan, and Kamchatka. It lives in the forest and grows in columnar shape in thick and short root stems. Three leaves without petioles grow and are 20 ~ 40cm high. Stems are 1 ~ 3, leaves are wide egg-shaped, square-like, 7 ~ 17cm long and butterfly, flat and 3 ~ 5 veins developed. In China, the age group is called age-cho, the root stem is called age-cho root, and it is used as a gastrointestinal drug, astringent, irritation, pain, and expectorant.

However, the fact that ethanol extract of early age is effective in inhibiting obesity and lowering blood sugar has not been disclosed or taught in any of the literature.

The present inventors confirmed that ethanol extract of Trillium Kamtschaticum among 400 kinds of natural product extracts has the effect of inhibiting the absorption of fat from adipocytes and the activity of alpha-glucosidase. And through animal experiments to verify the efficacy and hypoglycemic effect of inhibiting obesity was completed the present invention.

SUMMARY OF THE INVENTION An object of the present invention is to provide a composition for inhibiting obesity and for enhancing blood sugar, which contains an ethanol extract of early age that can induce weight loss and body health by inhibiting an increase in body fat and lowering blood sugar.

In order to achieve the above object, ethanol of early age having the effect of inhibiting the absorption of fatty acids occurring in adipocytes by using insulin as a signal to inhibit the accumulation of fat in the body, and lowering blood sugar by inhibiting the activity of alpha-glucosidase It provides a composition for inhibiting obesity and lowering blood sugar containing the extract as an active ingredient.

Hereinafter, the present invention will be described in detail.

The ethanol extract of age seconds of the present invention is collected only after drying the ground part of age seconds, crushed and extracted by reacting for 2 to 3 days at room temperature by adding 50% ethanol of 1L per unit mass (kg). The extract obtained therefrom is filtered through filter paper and then lyophilized to powder.

The present invention provides a composition for inhibiting obesity and lowering blood sugar, including an ethanol extract of age-old obtained in the extraction step as an active ingredient.

The composition for inhibiting obesity and lowering blood sugar containing ethanol extract of age group according to the present invention as an active ingredient may be administered orally at the time of clinical administration, and a pharmaceutically acceptable carrier according to a pharmaceutical preparation method known in the art may be used. It can be added to prepare a pharmaceutical composition.

The anti-obesity and hypoglycemic composition containing the ethanol extract of the early age as an active ingredient can be administered in various oral dosage forms at the time of actual clinical administration, and when formulated, commonly used fillers, extenders, binders, humectants, It is prepared using diluents or excipients such as disintegrants and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and such solid preparations include at least one excipient such as starch, calcium carbonate, water It is prepared by mixing sucrose or lactose, gelatin and the like. In addition, magnesium, thiarate, in addition to simple excipients. Lubricants such as talc are also used. Liquid preparations for oral use include suspensions, solvents, emulsions, and syrups.In addition to commonly used simple diluents, water and liquid paraffin, various excipients, for example, wetting agents, sweeteners, fragrances, and preservatives may be included. have.

A typical daily dose of the composition for inhibiting obesity and lowering blood sugar containing ethanol extract of age group according to the present invention as an active ingredient is 1 to 30 mg / kg body weight, and may be administered once or in several divided doses. However, the actual dosage should be determined in light of several relevant factors such as the route of administration, the age, sex, weight of the patient and the severity of the patient and the dosage does not limit the scope of the invention in any aspect.

In addition, ethanol extract of the age of the present invention has little toxicity and side effects, so can be used with confidence even when taking for preventive purposes.

Hereinafter, the present invention will be described in detail with reference to Examples. However, these examples are merely to illustrate the invention, but the content of the present invention is not limited to the following examples.

Example 1

Preparation of Ethanol Extracts from Early Ages

Age group used only leaves and stems, not roots. The leaves and stems of Nachos were dried, crushed and extracted by adding 1L of 50% ethanol per unit mass (kg) and reacting at room temperature for 2 to 3 days. The extract obtained therefrom was filtered with a filter paper (Whaatman No. 41), the filtrate was concentrated under reduced pressure with a vacuum rotary concentrator (Eyela NE, Japan), lyophilized using a freeze dryer, and powdered by lyophilization. An extract was prepared.

Example 2

Determination of Fatty Acid Absorption in Adipose Cells by Ethanol Extract of Early Ages

The degree of fatty acid uptake in adipocytes was measured using a fluorescent fatty acid analogue developed by Molecular Devices. Rat precursor adipocytes (3T3-L1 preadipocytes) were previously differentiated into adipocytes. On the day of the experiment, 96-well black wall / clear bottom plate was passaged to 50,000 to 80,000 cells / well, and then incubated in 10% FBS / DMEM medium for 5 hours. After 5 hours, when the cells were completely settled on a plate, 10 μl of 0.25 mg / ml age ethanol extract prepared in Example 1 was added and replaced with 90 μl of DMEM medium, followed by incubation for 1 hour. Subsequently, insulin (insulin) was added to 100 nM and incubated for 30 minutes, and then the absorption of fatty acids was measured using a QBT fatty acid uptake assay kit (Molecular Devices, product # R8132). The results are shown in FIG.

As shown in Figure 1, when the fatty acid is absorbed into the cell, the amount of fatty acid absorbed by the fluorescent material attached to the fatty acid can be measured with a fluorescence detector. It was confirmed that the absorption of fatty acids into the cell is inhibited. That is, as the fatty acid is absorbed into the adipocytes with time, the fluorescence amount increases, and as the concentration of ethanol extract of the early age added increases, the fluorescence amount decreases, indicating that the absorption of the fatty acid into the cells is inhibited.

Example 3

Determination of Activity of Alpha-Glycosidase of Ethanol Extracts from Early Ages

0.1 g of intestinal acetone powder (small intestine acetone extract) was dissolved in 10 ml of 0.9% NaCl and centrifuged to separate the supernatant and coenzyme solution containing alpha-glucosidase (α-glucosidase). Can be obtained. The activity of alpha-glycosidase was measured in 40 μl of 20 mM sodium phosphate (pH 7.0) buffer solution with 20 μl of coenzyme solution and 6 mM p-nitrophenyl α-D-glucopyranoside as substrate. It can be measured by reacting 50 µl of a solution of (p-nitrophenyl α-D-glucopyranoside; PNPG). Herein, the solvent diluted with ethanol extract of age group was used as a control, and the ethanol extract of age group prepared in Example 1 was prepared by concentration (0.125 mg / ml, 0.25 mg / ml, 0.5 mg / ml, 1.0 mg / ml). 20 µl each was added to react. The reaction was carried out at 37 ° C. for 30 minutes, and 100 μl of 1M glycine buffer (pH9.0) was added and the absorbance was compared at 405 nm to measure the activity of alpha-glucosidase. The results are shown in Figure 2, Figure 2 shows the value converted in percentage the degree of inhibition of the activity of alpha-glycosidase (α-glucosidase) of the control group ethanol extract by age.

As shown in Figure 2, the ethanol extract of the early age was confirmed in vitro (in vitro) inhibit the activity of alpha-glycosidase by 60-70%.

Example 4

Obesity Inhibitory Effects of Ethanol Extracts from Early Ages on Male C57BL / 6 Mice

In order to investigate the anti-obesity effect of the ethanol extract of the early age was made a feed as shown in Table 1 below and fed to the experimental animals. The experimental animals were adapted to feed three weeks-old male C57BL / 6 mice with a high-fat diet for one week, and then feed according to the experimental group. The experimental group was high-fat diet, high-fat diet olistat added group [high-fat diet + orlistat (add 0.1% of the total feed)], high-fat diet ethanol extract of the age group [high fat diet + ethanol extract (age) 0.62% of the total feed)], ethanol extract of the age group to the high fat diet (ethanol extract of the high fat diet + age vinegar (add 1.25% of the total feed)]. Orlistat is an active ingredient in obesity treatments that is currently widely used. Seven experimental animals were placed in each group. The diets were D12451 (45% fat, 5.252 cal / g) from Research diets.

Experimental group Number of objects Feed composition It's a high-fat diet. 7 High fat (45%) diet orlistat group 7 High fat (45%) diet + orlistat (0.1%) Ethanol added group at the beginning of age (0.62%) 7 High fat (45%) diet + age herb extract (0.62%) Ethanol-added group at the beginning of age (1.25%) 7 High fat (45%) diet + age herb extract (1.25%)

The diet was fed for a total of eight weeks, and body weight and feed intake were measured twice a week. The results are shown in FIG.

As shown in Figure 3, the experimental group ingested feed containing ethanol extract of the age group was found that the weight gain was significantly suppressed compared to the experimental group ingested only high fat diet. In addition, considering that the ethanol extract of the age group was used in an unpurified state, the experimental group added only the ethanol extract of the age group compared to the experimental group to which only the positive control (orlistat) was added {high fat diet + age group Ethanol extract (0.62%), high fat diet + ethanol extract (1.25%) of the early age} was confirmed that the anti-obesity effect is obvious.

Example 5

Measurement of hypoglycemic effect of ethanol extract of early age on male C57BL / 6 mouse

The male C57BL / 6 mouse prepared in the same manner as in Example 4 was fasted for 12 hours before sacrificing the experimental animals to observe whether the blood biochemical indices were changed by the experimental diet for 8 weeks, and blood glucose was measured by heart blood collection. . The results are shown in Figure 4 (* P <0.05, ** P <0.01, compared with the high fat diet).

As shown in Figure 4, the experimental group intake of ethanol extract of the age group (high fat diet + ethanol extract (0.62%), high fat diet + age ethanol extract (1.25%)} of the negative control high fat diet It was confirmed that the blood glucose was significantly lower than the experimental group to which only this was added and the experimental group to which only the positive control orlistat was added.

Example 6

Preparation of Pharmaceutical Compositions Using Ethanol Extracts from Early Ages

Hereinafter, an example of preparation of a composition for inhibiting obesity and for enhancing blood sugar containing an ethanol extract of age vinegar according to the present invention as an active ingredient will be described.

Powder  Produce

According to the preparation method of powder in the Pharmacopoeia General Formulation, it is prepared in the following component content per packet.

Ethanol Extract (Dry Powder) of Early Ages ... 300 mg

Lactose ... Mg

Talc ... Mg

Manufacture of tablets

According to the preparation method of tablets in the Pharmacopoeia General Formulation, it is prepared in the following component contents per tablet.

Ethanol Extract (Dry Powder) of Early Age ........................ 300mg

Corn starch ........................... 100 mg

Lactose ... 100mg

Magnesium Stearate ......................................... 2 mg

Manufacture of capsule

According to the preparation method of capsules in the pharmacopeia formulation, it is prepared in the following component content per capsule.

Ethanol Extract (Dry Powder) of Early Ages ............ 300mg

Corn starch ........................... 100 mg

Lactose ... 100mg

Magnesium Stearate ......................................... 2 mg

Liquid  Produce

According to the method for preparing a liquid formulation in the Pharmacopoeia General Formulation, it is prepared in the following component content per 100 ml of liquid formulation.

Ethanol Extract (Dry Powder) of Early Ages ........................ 1g

Isomerized sugar ... 10 g

Mannitol ... 5 g

Purified water................................................. Appropriate amount

As described above, the ethanol extract of Trillium Kamtschaticum of the present invention has the effect of inhibiting the activity of alpha-glucosidase that degrades disaccharides in the intestine, thereby inhibiting the absorption of sugar into the intestine. Efficacy in lowering blood sugar, and inhibiting the absorption of fatty acids in adipocytes, thereby preventing the accumulation of fat in the cells. The composition comprising the same is useful as a medicine or health functional food for preventing obesity and preventing diabetes. Can be.

Claims (4)

A composition for inhibiting obesity, containing ethanol extract of Nachocho as an active ingredient. A composition for lowering blood sugar, which contains ethanol extract of early age as an active ingredient. The method of claim 1, The ethanol extract of the early age is a composition for inhibiting obesity, characterized in that it inhibits the absorption of fatty acids in fat cells. The method of claim 2, The ethanol extract of the early age lowers blood sugar by inhibiting the activity of alpha-glucosidase composition.

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