KR20050078601A - New herbal composition for treatment and prevention of obesity - Google Patents

Abstract

The present invention is a mixture of 1.0 parts by weight of Platycodi radix extract, 0.8-1.2 parts by weight of Citus unshiu Markovich extract, 1.4-3.5 parts by weight of Imperatae rhizoma extract and 1.1-1.7 parts by weight of Liriopsis tuber extract. It relates to a herbal composition containing and an anti-obesity and obesity treatment agent and health functional food containing the same as an active ingredient.

According to the present invention, it is possible to provide an excellent natural water-derived obesity suppression and obesity treatment agent or health functional food without user's rejection and other side effects.

Description

New Herbal Composition for Treatment and Prevention of Obesity

The present invention relates to a herbal composition for treating and suppressing obesity, which is obtained by extracting from a mixture of Platycodi radix , Citus unshiu Markovich , Liriopsis tuber , and Imperatae rhizoma .

Recently, with the improvement of living standards due to the modernization of the economy, a new dietary culture, in which fat and sugar intake is increased and fiber intake is reduced, especially eating out, has become a preference for high protein-oriented diets. The reality is that the obese population is rapidly increasing due to the few lifestyles of modern people. As the consumption of high-calorie foods increases and fiber intake decreases, obesity, especially abdominal obesity, is becoming a serious social problem. Obesity refers to a state in which fat tissue is excessively increased, and weight gain due to obesity is mostly due to an increase in fat.

Obesity is a problem that obesity itself causes a lot of constipation, indigestion, gastrointestinal disorders due to the pressure of the abdomen by the fat tissue, as well as the risk factors of many adult diseases. Obesity is known to cause all kinds of complications such as cancer, arteriosclerosis, heart disease, high blood pressure, diabetes and other complications, and in 1996, the World Health Organization (WHO) warned that obesity is a disease that needs treatment. A study of 750,000 people reported a 1.9-fold increase in mortality in men and women who were 40% or more above average body weight than those of normal weight.

Obesity is a state in which excess fat is accumulated in the body, and the cause of fat accumulation in the body is excessive intake of sugar (carbohydrate) or excess intake of fat. The mechanism of reaching obesity is that by over-ingesting the sugars, the sugars in the food are digested and become monosaccharides and absorbed into the body through the small intestine.Increase the blood sugar and insulin secreted by the stimulus acts on fat cells to release the monosaccharides in the blood. Fat cells are taken in and converted into fat. In addition, fat (triglyceride), which is the highest calorie among food ingredients, is broken down by pancreatic lipase and absorbed through the small intestine, resulting in an increase in stored calories due to excess calories. That is, obesity is caused by excess fat intake.

Therefore, studies on various anti-obesity agents are currently being conducted based on the idea of generating anti-obesity effects by inhibiting a part of certain pathways that cause obesity.

Cholesterol adsorption excretion, cholesterol lowering, inhibiting glycolysis digestive enzyme inhibition, hyperglycemia inhibition, or monosaccharide absorption inhibition or excess fat ingestion It is thought that obesity can be prevented and improved by the action, the blood triglyceride lowering action, or the lipase inhibitory action, and the research on the pharmaceutical component which has these actions is continuing.

Rapid postprandial blood sugar rise and excessive insulin secretion due to excessive intake of carbohydrates (sugars) can lead to diabetes or hyperlipidemia in addition to obesity (Pharmacology and Treatment Vol. 19, No. 10 Oct. 274, 1991), Inhibition is known to prevent and improve diabetes or hyperlipidemia. Therefore, glycosylated digestive enzyme inhibitors, monosaccharide absorption inhibitors, or blood glucose elevation inhibitors are considered to be useful as antidiabetic agents, antihyperlipidemic agents, or antiarteriosclerosis agents. Glycolytic digestive enzyme inhibitors currently used in medicine include acarbose (Acarbose, Bayer Pharmaceutical Co., Ltd.) and Bogriboose (AO-128, Daeda Pharmaceutical Co., Ltd.), a post-prandial hyperglycemic improver. In animal studies or clinical trials, the effect of suppressing postprandial blood sugar levels was confirmed, and the effectiveness of anti-obesity and anti-diabetic disease was also reported (Res. Exp. Med. Vol. 175, 87 (1979), Japanese Journal of Agricultural Chemistry vol. 63, 217 (1989), New Current vol. 6, 2 (1995).

In addition, fat (triglyceride) intake to inhibit the path to obesity, such as exclusion of cholic acid adsorption, cholesterol lowering, blood triglyceride lowering, lipase inhibition and the like. Drugs with cholic acid excretion include cholstyramine, a hypercholesterolemic drug, which is an anion exchange resin. By oral administration of the anion exchange resin, the anion exchange resin adsorbs cholic acid in the intestinal circulatory organs (Makino Isaora, Taisha, vol. 24, No. 8, 685-692, 1987). Fixing interferes with the resorption of cholic acid and promotes the conversion of cholesterol into cholic acid in the liver, resulting in a lowering of cholesterol levels in the blood. However, the usage of cholestyramine is to take 9 g in 100 mL of water, so the dose is very high, and when taken, the rough uncomfortable texture of the resin remains in the mouth, which is very often taken by the patient. There was a difficult problem.

As described above, a number of chemical synthetic compounds having respective actions have been reported and used as medicines, but these have a problem in that they have a high dose or are unpleasant at the time of taking them, and because they are chemically synthesized compounds, the test subjects have no effect on the human body at the time of administration. In some cases, safety was anxiety.

In order to suppress obesity and improve constipation, it is important to reduce the body's accumulation of fat by reducing the consumption of food, especially high-calorie foods, and increasing energy consumption. In particular, increasing energy consumption rather than reducing food intake is known to be effective in suppressing obesity. Regular exercise has also been shown to increase energy consumption and significantly reduce mortality from cardiovascular disease. However, due to the nature of the modern society, which is difficult to continuously exercise, the main efforts to control obesity are focused on the consumption of drugs derived from natural materials, diet foods, or dietary supplements that are effective in suppressing obesity and improving constipation. Are developed and marketed.

In particular, Cocis semen , Dioscoreae rhizoma , Gilkyung ( Pycycodi radix ), Bellflower, Schizandrae fructus , Citus unshiu Markovich, Aloe vera , Adenophorae radix Some anti-obesity drugs have been developed, which consist of extracts of several herbal drugs or mixtures.

However, in the case of products derived from such natural materials so far known, the materials are very expensive, and in order to obtain a proper effect, they have to be consumed in large quantities, or the effects of preventing obesity and preventing hyperlipidemia are often insignificant.

Therefore, there is a need to research and develop a new herbal composition that can be easily obtained even though it is a natural material and can have a more complex effect.

Accordingly, the present inventors have studied and analyzed many traditional herbal medicines known to directly affect the digestion, sugar metabolism, lipid metabolism, and the like, directly and indirectly, and the combination of herbal ingredients showing the best anti-obesity and hyperlipidemic effect. I found their grant.

Therefore, an object of the present invention is to provide a composition exhibiting an excellent anti-obesity effect by presenting an optimal combination and optimal composition ratio of herbal medicines that are inexpensive and easy to obtain, and excellent in effectiveness.

It is another object of the present invention to provide a drug and a food containing the composition for inhibiting obesity.

That is, an object of the present invention is to provide a composition that can effectively prevent and suppress obesity and related diseases.

The present invention for achieving the object as described above, 1.0 parts by weight of Platycodi radix extract, 0.8 to 1.2 parts by weight of Citus unshiu Markovich extract, 1.4 to 3.5 parts by weight of white hair root ( Imperia rhizoma ) extract and pulse moon dong ( Liriopsis tuber ) relates to a herbal composition for the control of obesity and obesity containing 1.1 to 1.7 parts by weight of extract.

As a result of many experiments and studies, the present inventors have confirmed that the best herbal composition is obtained only with the above content ratio.

The herbal composition according to the present invention exhibits an excellent anti-obesity and safe anti-obesity effect as compared to other conventional herbal or commercial chemical synthetic anti-obesity medicines as shown in the following Examples and Applications.

The herbal composition according to the present invention may be prepared by first obtaining a herbal medicine each of the compositions according to a conventional method by cold water extraction, hot water extraction or solvent extraction, drying, and then mixing in the above ratios. In this case, each herbal may be extracted in different ways. For example, it can be manufactured by the following method. First, prepare dried gilyeong, tangerine, white hairy root and pulsatile sinus, which have been screened and trimmed to an appropriate size. A suitable amount of pure water is added to the herbal medicine, hot water extraction is performed at 100 ° C. for 3 hours, and then rapidly frozen at minus 40 ° C. for 10-20 hours, vacuum dried at a pressure of 0.23 Torr or less for 35 hours, and then ground to prepare a dry powder. Subsequently, the dry powder of each herbal medicine is mixed by the said ratio, and the herbal composition powder which concerns on this invention is obtained. Of course, the solids content of each herbal extract before drying may be investigated in advance, and then the extracts may be mixed so as to have the above ratio and then dried in a batch to obtain the herbal composition powder according to the present invention.

On the other hand, the herbal composition according to the present invention may be obtained by first mixing each herbal dry matter of the calculated ratio so as to finally be the ratio and then extracted in a batch. To this end, a mixture of 1.0 parts by weight of dry path length, 0.8 to 1.2 parts by weight of dried tangerine, 2.3 to 3.5 parts by weight of dried white hair root and 0.8 to 1.2 parts by weight of dried Macmundong according to a conventional method, such as cold water extraction, hot water extraction or solvent extraction The mixture of each component is extracted, and then filtered and used as it is, or used by concentration, or lyophilized to be used as a powder. For example, it can be manufactured by the following method. First, the selected dried and cured gilyeong, tangerine, white hair root and pulmonary dong are appropriately mixed to the mixing ratio. The crude drug composition according to the present invention is added to the mixture with an appropriate amount of pure water, followed by hot water extraction at 100 ° C. for 3 hours, then rapidly freezing at 40 ° C. for 10-20 hours, vacuum drying at a pressure of 0.23 Torr or less for 35 hours, and then pulverizing. Obtain a powder.

The present invention also relates to a medicament for obesity treatment and suppression and a health functional food containing the herbal composition as an active ingredient. In addition to the herbal composition, various supplemental herbal medicines, vitamins, minerals, dietary fiber and other medicinal-food supplements (e.g., excipients, enhancers, coatings, etc.) may be used for the obesity treatment / inhibitory agent and health functional food. It may be contained.

The present invention also relates to a pharmaceutical composition which increases the intracellular β3AR activity while containing the herbal composition as an active ingredient. The pharmaceutical composition may also contain various supplemental herbal medicines, vitamins, minerals, dietary fiber and other medicinal-food supplements (eg, excipients, enhancers, coatings, etc.) as needed.

Hereinafter, the present invention will be described in more detail in Examples and Application Examples. The following examples are merely illustrative of the present invention in detail, and thus, the nature of the technical idea of the present invention is not changed or reduced in scope. It will be apparent to those skilled in the art that various embodiments and applications not shown in the following examples are possible.

Example: Preparation of herbal composition according to the present invention

(1) 10 times weight of water was mixed in each of 5 Kg of dried Kilkyung, Kalpipi, White Hairy root and Macmundong, which were previously screened and cut to an appropriate size, followed by heating and performing hot water extraction at 100 ° C. for 3 hours. Subsequently, rapid freezing was carried out at minus 40 ° C. for 15 hours, vacuum dried for at least 35 hours under a pressure of 0.23 Torr or less, and then ground to obtain respective dry powders.

The obtained gilyeong, tangerine peel, white hair root and pulmonary pulverized extract powder were mixed in a ratio of 1: 1: 1.8: 1.4 to obtain the herbal composition powder of the present invention.

(2) The extraction efficiency of each herbal medicine was analyzed in advance, and then each dried herbal medicine was mixed so that the ratio of each component in the final extract was Gilkyung: Gangpi: White hair root: Mangmun-dong = 1: 1: 1.8: 1.4. In other words, 1kg of dry length, 1kg, tangerine peel 1kg, white hair root 2.9kg, and 1kg of gingimun dong, which were selected and cut in advance, were mixed, poured with 10 times the weight of water, and heated to extract hot water at 100 ° C. for 3 hours. Subsequently, the solution was rapidly frozen at 40 ° C. for 15 hours, vacuum-dried at least 35 hours under a pressure of 0.23 Torr or less, and then ground to obtain 0.83 kg of the herbal composition powder of the present invention.

(3) Results of various in vitro and in vivo experiments (not shown in the data), the herbal compositions according to the present invention prepared by the above two methods were identified as the same. Therefore, in the following experiment, it used for the application example, not distinguishing by the two methods.

Application Example 1: Analysis of the effect of the composition according to the invention through in vitro experiments using 3T3L1 cell

β-3-AR (β-3-adrenergic receptor) is mainly expressed in fat cells and is well known as a gene involved in the process of lipolysis and heat dissipation. For example, mice that have lost this gene have been shown to have a slight obesity due to a decrease in metabolism in normal diets and a significant increase in obesity in fat diets (Bachman, E. S, Science 297: 843-845, 2002). In addition, Japanese studies on normal and obese people have reported differences in abdominal obesity according to β3AR gene mutations (Kim-Motoyama, Diabetologia 40: 469-472, 1997). This is a result of the loss or function of this gene, resulting in suppressed fat breakdown and heat dissipation due to fat diet.

Accordingly, in this application example, the effect of various drug treatment groups on the expression of β3AR involved in obesity control was analyzed.

In a conventional manner, 3T3L1 cells, which are pre-adipocytes, are cultured to a concentration of about 2 × 10 ⁶ cells / ml, and then treated with insulin (Insulin) and indomethasin (Indomathasin) to adipocytes. After differentiation into (adipocyte), each medicinal herb composition according to the present invention per 1ml of cell culture medium and the components of the medicinal composition, ie, ductilum, gilyeong, Megmundong and white hair root extracts (medicines were obtained in the same manner as the method of obtaining a composition according to the present invention) were treated with 10, 100 and 200 µg, respectively, and cultured at 37 ° C for 24 hours, and then mRNA was extracted from the cells. The expression level of β3AR (FIG. 1: above the electrophoretic image of the PCR product) was investigated by using reverse transcription-polymerase chain reaction. In addition, the expression level of beta-actin (β-actin), which is an internal control that shows the presence of the same amount of total mRNA in each treatment group, was examined together (Fig. 1: electrophoresis picture of PCR product) that). Beta-actin is a gene that is commonly used to see the same level of expression in cells and is measured to see that the total amount of mRNA is the same in each treatment group.

As mentioned above, since obesity is known to accumulate fat in adipocytes through various mechanisms, the present invention uses an in vitro cell system that differentiates into adipocytes by treating insulin and indomethacin to undifferentiated adipocytes 3T3L1. We have seen the effect of "composition" on the expression level of β3AR.

In Figure 1a, the top is β3AR, the bottom is an electrophoretic picture of the PCR product of beta-actin (β-actin), Figure 1b is the intensity (intensity) of the lanes as a quantitative value. As can be seen in the photos and diagrams of Figure 1, 200, 100, 10ug / ml of the herbal composition according to the present invention, the expression level for β3AR that plays an important role in the control of obesity is about 2 than the commercially available obesity inhibitor reductil It was about twice as high, and showed better expression effect in single treatment group of Kippi or white hair root. 1a As can be seen in the figure below, there was no significant difference in the expression level of beta-actin (β-actin) in all treatment groups. This means that there is a difference in the expression of β3AR for each drug treatment group for the same amount of total mRNA. Therefore, the difference in effect of each treatment group was not due to the difference in the total mRNA, but was due to the mRNA expression difference of the β3AR specific gene.

Therefore, it was confirmed that the herbal composition for inhibiting obesity according to the present invention showed superior anti-obesity effect compared to other chemical synthesis products or single herbal medicines.

Application Example 2 Analysis of the weight loss and hemostatic improvement effect of the composition according to the present invention 1

(1) A total of 35 c57BL / 6 mice were divided into four groups: 10 control groups, 10 herbal drug administration groups according to the present invention, 6 reductil-administered groups, and 5 Ginslim diet-administered groups, which are well-known domestic diet foods, for 4 weeks. A high fat diet (Diet # 101556ccl, Dyets Inc., US) was administered orally 600 mg / kg body weight once daily. Four weeks thereafter the dose was increased to 1 g / kg and body weight change was measured. The results are shown in Table 1.

As can be seen in Table 1, during the first four weeks of administration, the composition-administered group according to the present invention slightly increased the weight gain than the synthetic drug reductil-administered group, but the average weight was decreased during the later four-week administration period. In the case of reductil, the average increase was 0.3g, but the increase was small, but the gap between the minimum value and the maximum value was very large (and therefore the standard deviation was very large). A large standard deviation means that the drug is different for each individual and that the drug is less significant.

In the case of administering the composition according to the present invention, the average weight loss effect is superior to that in the case of administration of other chemical synthesis obesity inhibitors or obesity inhibitory health foods, but the effect is shown evenly (that is, the minimum and maximum weight gains) Meaning that the interval is narrow = means that the standard deviation value for weight change is small).

(2) Eight weeks after the experiment in the above-described experiment (1), blood of each mouse was collected and serologically performed (Table 2).

As can be seen in Table 2, in the case of the composition administration group according to the present invention, it can be seen that almost all blood-related values are superior to other administration groups. In particular, the ratio of HDL-cholesterol, a useful cholesterol, was lower than that of other administration groups.

Thereby, it was confirmed that the herbal composition according to the present invention can be usefully applied to the prevention and treatment of hyperlipidemia.

Application Example 3 Analysis of the weight loss and hemostatic improvement effect of the composition according to the present invention 2

(1) The disease animal model DB / DB mouse is divided into seven control groups and six herbal composition administration groups according to the present invention, six reductyl administration groups, six Ginslim diet administration groups, and six Samyang compound feeds (for mice). While the feeds were orally administered in the same manner as in the above (1) of Application Example 2, the weight gain of each group was analyzed by the same method (Table 3).

As can be seen in Table 3, the same results as in the previous application example 2 also appeared in this application model of the diseased animal. That is, in the case of the composition administration group according to the present invention, the amount of weight gain was decreased or decreased, but the standard deviation was relatively smaller than that of the other drug administration group. As a result, the composition according to the present invention was confirmed to be effective in the treatment of obese patients.

(2) In obese mice, the concentration of NPY (neuropeptide Y) is increased in the hypothalamus, which stimulates the central nervous system, increases dietary intake and insulin secretion, and increases the expression of obesity genes in white adipocyte tissue (WAT). do. Insulin plays a physiological role in up- and down-regulation of obesity genes in WAT, which stimulates triglyceride accumulation and leptin secretion in adipocytes, leading to proliferation of adipocytes in the abdominal cavity and an increase in WAT. Excessive dietary intake and hormone secretion in obese mice lead to hepatic dysfunction by increasing blood glucose, cholesterol, and triglyceride proteins due to the proliferation and activation of hepatocytes. This impairment of liver function leads to an increase in GPT, GOT, and creatinine, and the suppression of overmetabolism is suppressed and the degree of obesity continues to increase (Meinders, AE, AC Toornvliet, H. Pijl. Leptin, Netherlands journal of medicine 49 (1996) 247-252).

In this regard, after eight weeks of the experiment in the above-described experiment (1), blood of each mouse was collected and serologically performed (see Table 4).

As shown in Table 4, GOT, GPT, Glucose, and creatinine were significantly increased in obese mice of the control group, but it was confirmed that the composition administration group according to the present invention is significantly reduced. The activation of adipocytes increased the secretion of insulin and leptin in the control group, whereas the expression of the obesity gene was regulated by the administration of the composition, indicating that insulin and leptin secretion were significantly reduced.

In addition, the group administered with the composition according to the present invention showed an excellent overall serum test results compared to the control group as well as other chemotherapy drugs.

That is, the composition administration group according to the present invention shows that blood glucose levels and insulin levels closely related to obesity and diabetes are similar to reductyl. On the other hand, the level of creatinine in the composition treatment group of the present invention is similar to the control group, which confirms that the composition of the present invention does not place a specific burden on the kidney (kidney).

In conclusion, in the case of the composition administration group according to the present invention, it can be seen that almost all blood-related values are superior to other administration groups.

Accordingly, it was confirmed that the herbal composition according to the present invention can be usefully applied to the treatment and prevention of diseases associated with obesity.

As discussed above, the herbal composition according to the present invention promotes the expression of genes related to the prevention of obesity and the treatment of obesity in cells. The amount and composition are improved to show an excellent effect even when administered to obese mice.

When the herbal composition according to the present invention is used as an active ingredient of anti-obesity and anti-obesity drugs or health functional foods, natural ingredients are applied so that the user's rejection can be eliminated. It is possible to provide excellent products without negative effects.

1 is an electrophoretic photograph and a diagram showing the effect of the herbal composition according to the present invention on the β3AR activity of the cells.

Claims (6)

It contains a mixture of 1.0 parts by weight of Platycodi radix extract, 0.8-1.2 parts by weight of Citus unshiu Markovich extract, 1.4-3.5 parts by weight of Imperatae rhizoma extract, and 1.1-1.7 parts by weight of Liriopsis tuber extract. Anti-obesity and obesity treatment composition. The method of claim 1, The composition for inhibiting obesity and treating obesity, characterized in that for extracting and drying each herbal medicine. The method of claim 1, A composition for inhibiting obesity and treating obesity, which is obtained from an extract of a mixture of 1.0 parts by weight of dry path length, 0.8 to 1.2 parts by weight of dried tangerine, 2.3 to 3.5 parts by weight of dried white hair root, and 0.8 to 1.2 parts by weight of dried Macmundong. An agent for the treatment of obesity and suppression containing the composition according to claim 1 as an active ingredient. Obesity treatment-suppressing health functional food containing the composition according to claim 1 as an active ingredient. A pharmaceutical composition comprising increased intracellular β3AR expression and activity, comprising the composition according to claims 1 to 3 as an active ingredient.