KR100573592B1 - Imperatae rhizoma Extract for Treatment and Prevention of Obesity - Google Patents

Abstract

The present invention relates to anti-obesity and obesity-containing drugs and health functional foods containing the extract of Imperatae rhizoma .

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.

Anti-obesity, obesity treatment, herbal medicine, extract, hyperlipidemia, white hair root

Description

Imperatae rhizoma Extract for Treatment and Prevention of Obesity             

1 is an electrophoretic photograph and a diagram showing the effect of the white hair root extract according to the present invention on the β3AR activity of the cells.

The present invention relates to a herbal composition for inhibiting obesity treatment obtained from the extract of 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, in particular, the establishment of a high-protein-oriented diet is becoming prominent due to the establishment of a restaurant culture. 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 consumption 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 sugar, the sugar in the food is digested and becomes monosaccharide and absorbed into the body through the small intestine. Will be accepted by the fat cells to change fat. In addition, fat (triglycerides), which is the highest calorie among the food ingredients, is broken down by lipase and absorbed through the small intestine. 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.

Glycolytic digestive enzyme inhibition, which inhibits the path to obesity due to over-glucose intake, hyperglycemia, or monosaccharide absorption inhibition, or cholic acid adsorption excretion that inhibits the path to obesity by over-ingestion of fat, cholesterol lowering 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 anti-arteriosclerosis 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 and clinical trials, the effects of elevated postprandial blood sugar levels were confirmed, and the effectiveness of anti-obesity and anti-diabetic disease was also reported (Res. Exp. Med. Vol. 175, 8 7 (1979), Japanese Journal of Agricultural Chemistry vol. 63, 217 (1989), New Current vol. 6, 2 (199 5).

In addition, fat (triglyceride) intake to inhibit the path to obesity, such as the excretion 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 that 9 g is taken in 100 mL of water, so that the dose is very large, and when taken, the rough unpleasant texture of the resin remains in the mouth, making it very difficult for the patient to take it. There was a problem.

As described above, a number of chemical synthetic compounds having respective actions have been reported and used as medicines, but they have a problem in that they have a large amount 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 expenditure and significantly reduce mortality from cardiovascular disease. However, due to the characteristics of modern society, which is difficult to continuously exercise, the main efforts for suppressing obesity are focused on the consumption of natural ingredients, diet foods, or dietary supplements that are effective in preventing obesity and improving constipation. Products are being developed and marketed.

In particular, Cocis semen , Sanos ( Dioscoreae rhizoma ), Gilkyung ( Platycodi radix ), Bellflower, Schizandrae fructus , Citrus unshiu Markovich , Aloe vera and 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.

Therefore, the present inventors have diligently studied and analyzed many traditional herbal medicines known to directly affect the digestion, sugar metabolism, lipid metabolism, etc. of sugar, and find the most effective anti-obesity and hyperlipidemic drugs. .

Therefore, an object of the present invention is to provide a herbal ingredient that is inexpensive, easy to obtain, and exhibits an excellent anti-obesity effect.                         

Another object of the present invention is to provide a drug and a food containing the herbal ingredient for inhibiting obesity.

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

The present invention for achieving the above object, the present invention relates to anti-obesity and obesity treatment herbal composition containing the extract of Imperatae rhizoma .

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 extracts according to the present invention may be prepared by first obtaining and drying the white hair roots, which were selected according to a conventional method and trimmed to an appropriate size, respectively, by cold water extraction, hot water extraction or solvent extraction. For example, it can be manufactured by the following method. First, an appropriate amount of pure water is added to the selected white hair roots, followed by hot water extraction at 100 ° C. for 3 hours, and then rapidly frozen at minus 40 ° C. for 10-20 hours, vacuum-dried for at least 35 hours at a pressure of 0.23 Torr or less, and then pulverized to dry. Powder can be obtained.

The present invention also relates to a medicament for inhibiting obesity and health functional food containing the white hair root extract as an active ingredient. In addition to the white hair root extract, the pharmaceutical and health functional food for inhibiting obesity treatment may contain various auxiliary herbal medicines, vitamins, minerals, dietary fiber and other medicinal-food supplements (eg, excipients, enhancers, coatings, etc.). Can be.

The present invention also relates to a pharmaceutical composition for increasing intracellular β3AR activity while containing the white hair root extract 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

A 10-fold weight of water was mixed with 5 Kg of dried white hair roots, which were previously screened and cut to an appropriate size, and then heated to perform hot water extraction at 100 ° C. for 3 hours. Subsequently, the solution was rapidly frozen 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 pulverized to obtain a dry powder.

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

β3AR (β-3-adrenergic receptor) is mainly expressed in adipocytes 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 fatty 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 the β3AR gene mutation (Kim-Motoyama, Diabetologia 40: 469-4 72, 1997). This is the result of fat loss and heat dissipation suppressed by fat diet due to loss or loss of function of this gene.

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 prepare fat cells ( After differentiation into adipocytes, the white hair root extract according to the present invention per 1 ml of cell culture solution, Reductyl R (Sibutramine HCL, Ilsung New Drug), which is currently marketed as an anti-obesity agent, and Gil-kyung extract known to have an anti-obesity effect (according to the present invention) Obtained in the same manner as the method for extracting extracts) 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. By using the same amount of the extracted mRNA reverse transcription-polymerase chain reaction (reverse transcription-polymerase chain reaction) was investigated the expression level of β3AR (Fig. 1: above the electrophoresis picture of the PCR product). In addition, the expression level of beta-actin (β-actin), which is an internal control that can be seen that the same amount of total mRNA is present in each treatment group was examined together (Fig. 1: electrophoresis picture of the 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.

As mentioned above, obesity is the accumulation of fat in adipocytes through a number of mechanisms, the white hair root extract according to the present invention using an in vitro cell system that differentiates into adipocytes by treating insulin and indomethacin to undifferentiated adipocytes 3T3L1 The effect on the expression level of this β3AR was seen.

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, when the white hair root extract according to the present invention 200, 100, 10 ㎍ / ㎖ concentration, the expression level for β3AR which plays an important role in the control of obesity is a commercial obesity inhibitor reductil It was higher than about 60 ~ 70%, and showed a better expression effect than a single group treated with Gilpyeong extract. 1a As can be seen in the figure below, there was no significant difference in the expression level of beta-actin (β-actin) significant in all treatments. 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, the white hair root extract for obesity inhibition according to the present invention was confirmed to show an excellent anti-obesity effect compared to other chemical synthesis products or herbal ingredients.

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

(1) Four weeks of c57BL / 6 mice were divided into four groups: 10 control groups, 5 groups of white hair root extracts according to the present invention, 10 groups of reductil, a chemical diet drug, and 5 groups of ginslim diets, a famous Korean diet food. While fed a high fat diet (Diet # 101556ccl, Dyets Inc., US), each sample was administered orally 600 mg / kg body weight once a day. 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, after 8 weeks of administration, the weight gain of the white hair root extract group according to the present invention was slightly increased than that of the synthetic drug reductil. In the case of reductile, however, the increase was minimal with an average increase of 0.3g, but the gap between the minimum and maximum 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.

On the contrary, the group of white hair root extract according to the present invention showed an excellent weight loss effect evenly compared to the case of administration of reductil or gin slim diet (that is, the interval between minimum weight increase and maximum weight increase is narrow). Meaning = low standard deviation value for weight loss).

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

As can be seen in Table 2a and Table 2b, in the case of the white hair root extract 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, while the total cholesterol content is lower than other administration groups, the levels of triglyceride (TG) and low-density lipoprotein cholesterol (LDL-cholesterol), which precipitate cholesterol on arterial vessel walls and promote atherosclerosis, are relatively lower than those of the control group.

Thereby, the white hair root extract according to the present invention was confirmed that it 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 extract according to the present invention 2

(1) normal animal feed (Samyang blended feed, Samyang Corp. product) divided into 7 control animals and 6 control group of white hair root extract, 6 reductil-treated group, 6 slimmed diet-treated group of disease animal model DB / DB mouse Samples were orally administered in the same manner as in (1) of Application Example 2, and 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, the white hair root extract administration group according to the present invention showed a relatively small standard deviation while reducing or decreasing the weight gain compared to the other drug administration group. As a result, the extract 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 nerve, increases dietary intake and insulin secretion, and increases the expression of obesity genes in WAT (white adipocyte tissue). 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 (Tables 4a and 4b).

As can be seen in Table 4a and Table 4b, GOT, GPT, Glucose, and creatinine were significantly increased in the obese mice of the control group, and these serum substances were significantly reduced in the white hair root extract administration group according to the present invention. In addition, insulin and leptin secretion were increased in the control group by the activation of adipocytes, whereas the expression of obesity gene was regulated by administration of white hair root extract, which significantly reduced the secretion of insulin and leptin.

In addition, the group administered the white hair root extract according to the present invention showed a significantly higher serum test value than the control group, and compared with the reductil or gin slim diet.

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

In conclusion, in the group of white hair root extract administration according to the present invention, almost all blood-related values are superior to other administration groups.

Thereby, the white hair root extract according to the present invention was confirmed that it can be usefully applied to the treatment and prevention of diseases associated with obesity.

As discussed above, the white hair root extract according to the present invention promotes the expression of genes related to the prevention of obesity and the treatment of obesity in cells, and very high weight gain inhibitory effect and the amount of fat in the blood in mice administered high fat diet. And improve the composition, even when administered to obese mice.

When the white hair root extract according to the present invention is used as an active ingredient of an anti-obesity and obesity treatment drug or health functional food, natural ingredients are applied, so that the user's rejection can be eliminated. It is possible to provide excellent products without negative effects.

Claims (4)

Herbal composition for the treatment and suppression of obesity, containing the extract of Imperatae rhizoma . An agent for the treatment and suppression of obesity, comprising the composition according to claim 1 as an active ingredient. Health functional food for obesity treatment and suppression containing the composition according to claim 1 as an active ingredient. A pharmaceutical composition comprising the composition of claim 1 as an active ingredient, which has an effect on the treatment and inhibition of obesity through the enhancement of intracellular β3AR expression and activity.

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