KR20140024582A - Composition containing hedyotis diffusa extract for treating or preventing obesity - Google Patents

Abstract

The present invention relates to a composition containing an extract or a fraction of Hedyotis diffusa as an active ingredient for preventing or treating obesity. The extract or fraction of Hedyotis diffusa according to the present invention does not have in vivo toxicity and side effects and has outstanding therapeutic effects for the obesity in animal models, thereby can be valuably used for preventing or treating the obesity.

Description

[0001] The present invention relates to a composition for preventing or treating obesity,

The present invention relates to a composition for preventing or treating obesity comprising an acnes extract or fraction as an active ingredient.

Recent changes in diet and eating habits have been accompanied by changes in economic growth and lifestyle. Especially, busy modern people are overweight and obese because of high calorie diet such as fast food and low exercise amount. Weight overweight means that the body mass index (BMI, obesity index divided by the square of body weight) is 25 or more and less than 30, and obesity means the body mass index is 30 or more.

Two-thirds of US adults are overweight or obese, and overweight increases blood pressure and cholesterol levels, increasing the incidence of various adult diseases, including heart disease. The effects of obesity on various diseases are so severe that it is known that 80% of diabetics worldwide and 21% of heart disease are caused by obesity. In addition, various cancers such as uterine cancer, kidney cancer, and breast cancer are directly or indirectly related to obesity. Obesity and overweight also have higher incidences of sleep apnea, osteoarthritis, and gallstone disease than normal people (Stein CJ, Colditz GA. The epidemic of obesity. J Clin Endocrinol Metab 2004; 89: 2522-2525. ; Kopelman PG. Obesity as a medical problem. Nature 2000 Apr 6; 404 (6778): 635-43.).

Obesity is not caused by a single cause, but by a combination of genetic, environmental, social, and mental factors. Current methods of treating obesity include diet, exercise, and behavioral therapy, as well as methods of correcting lifestyle, drug therapy, and surgical treatment. Although active efforts should be made to correct lifestyle prior to medication or surgical treatment, it is not easy to correct lifestyle habits, and there is a limit to the weight that can be reduced by lifestyle correction alone. Therefore, in many cases, lifestyle correction and medication are necessary.

Although many anti-obesity agents are being developed every year for the treatment of obesity, there are not many obesity agents available at present, and most of them are limited to digestive or appetite-suppressing agents. In the case of digestive or appetite control agents, they are classified as psychotropic drugs because of habit, and digestion inhibitors show side effects such as diarrhea and constipation. By 2010, the US FDA approved long-term obesity treatment drugs include sibutramine (Reductil), which suppresses the reuptake of norepinephrine and serotonin, and lipase, which is secreted from the pancreas and digestive system (orlistat; Xenical), which has the effect of inhibiting lipase (Yanovski SZ, Yanovski JA, Obesity, N Engl J Med 2002; 346: 591-602).

However, sibutramine has been withdrawn in the US and Korea in October 2010 due to the risk of cardiovascular events such as myocardial infarction and stroke, which are common with side effects such as elevated blood pressure, insomnia, dry mouth, and dizziness. In addition, Orlistat has been reported to have side effects such as diarrhea, fatty liver, loss of gold, and the use of these drugs is limited because of the lack of efficacy of drugs when the fat intake is lower than that of westerners (Korean. The Korean Journal of Obesity 1998; 7 (4): 287-92.).

Accordingly, there is a need for a preventive or therapeutic agent for obesity, which is excellent in the effect of inhibiting obesity and has been confirmed to be safe for long-term use.

On the other hand, baekunpul (Hedyotis diffusa ; Is a year-old seedling with a twin-spotted plant. Chinese corymbosa ( H. corymbosa ), which has a similar appearance, has been used as an anticancer agent in civilian for decades, and domestic domestic white pine was endangered. Soon Jong-moo collected the seeds of native Bae whirlpool, which was naturally grown throughout the country, and confirmed the cultivation method in 2006 after several trial and error. However, the anti-obesity effect of the Acanthopanax acanthus extract has not been reported yet.

Accordingly, the inventors of the present invention have found that, while continuing the research for searching for anti-obesity agents derived from natural products having no toxicity or side effects in vivo and having excellent stability, it has been confirmed that the white flour extract or fractions have excellent anti- Thereby completing the invention.

Korean patent application number: 10-2002-0004551

The present invention is intended to provide a pharmaceutical composition for preventing or treating obesity, comprising an acnes extract or fraction as an active ingredient.

The present invention also provides a food composition for preventing or ameliorating obesity, comprising an acnes extract or fraction as an active ingredient.

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

The present invention also provides a food composition for prevention or amelioration of obesity comprising an acnes extract or fraction as an active ingredient.

The acne extract or fraction according to the present invention has an excellent effect of treating obesity in obesity animal models without toxicity or side effects in vivo, and thus can be usefully used for prevention or treatment of obesity.

FIG. 1 is a diagram showing a separation process of an Acanthopanax acnes extract and a fraction.
Fig. 2 shows the AMPK and ACC activity of the aflatoxin ethanol (50%, 75% or 95%) extract.
Figure 3 is a diagram showing AMPK and ACC activity of the albumin fraction (dichloromethane, ethyl acetate, butanol or water).
FIG. 4 is a view showing a separation process of the fractions of dichloromethane.
Figures 5 and 6 show AMPK and ACC activities of each fraction (Fr. 1-5) isolated from the dolomucetum dichloromethane fraction.
7 shows the separation process of fraction 3 (Fr. 3) isolated from the fractions of dichloromethane.
8 is a diagram showing the separation process of the fractions of the maleic acid ethyl acetate fraction.
FIG. 9 shows the TLC result of HD1, an active substance isolated from the fragrance of aflatoxin.
FIG. 10 is a graph showing ¹³ C-NMR results of HD1 which is an active substance isolated from the fragrance of viscose.
11 is a graph showing mass spectral results of HD1 which is an active substance isolated from the fragrance of aflatoxin.
12 is a graph showing the ¹ H-NMR results of HD2, which is an active substance isolated from the fractions of aflatoxin.
13 shows ¹³ C-NMR results of HD2 which is an active substance isolated from the fragrance of viscose.
Fig. 14 is a graph showing mass spectral results of HD2, which is an active substance isolated from the fragrance of aflatoxin.
15 is a graph showing the ¹ H-NMR results of HD3, which is the active substance isolated from the fragrance of aflatoxin.
16 is a graph showing ¹³ C-NMR results of HD3, which is an active substance isolated from the fragrance of aflatoxin.
17 is a graph showing the mass spectral results of HD3, which is an active substance isolated from the aflatoxin fraction.
Figures 18 and 19 show the AMPK and ACC activities of the dolomach dichloromethane fraction, fraction 3, HD1, HD2 and HD3 isolated therefrom.
FIG. 20 is a graph showing the effect of the ethanol extract of Whiteness on the weight gain in an obesity animal model. FIG.
FIG. 21 is a graph showing the effect of the ethanol extract of Baeknuhul on the abdominal fat increase in the obese animal model.
FIG. 22 is a graph showing the effect of the ethanol extract of Baeknuhul on blood cholesterol concentration in an obesity animal model.
FIG. 23 is a graph showing the effect of the ethanol extract of Baeknuhul on fat accumulation in liver tissue in an obesity animal model.

The present invention provides a composition for preventing or treating obesity comprising an acnes extract or fraction as an active ingredient.

The composition comprises a pharmaceutical composition or a food composition.

Hereinafter, the present invention will be described in more detail.

In the composition of the present invention, an acne extract or fraction, which is an active ingredient, can be obtained by the following method.

First, the whitewash is washed with water to remove foreign matter, dried in the shade, and pulverized. Paeonpul can be used without restrictions such as cultivated or marketed. An appropriate amount of solvent is added to the crushed vials to allow them to be completely immersed. The extraction solvent is preferably a solvent selected from water, an alcohol having 1 to 4 carbon atoms or a mixed solvent thereof, more preferably 50 to 99% ethanol. The extraction method can be performed at room temperature or by heating, more preferably by reflux extraction at 60 to 95 ° C for 2 to 10 hours, and the above process can be repeated. The extract is filtered and concentrated to give the final whitening extract.

The extract was suspended in water and then sequentially fractionated with dichloromethane (CH ₂ Cl ₂ ), ethyl acetate (EtOAc) and butanol ( n- BuOH), and the fractions were concentrated to give a dichloromethane fraction, ethyl acetate fraction, Butanol fraction and water fraction are obtained.

Among the above fractions, the fractions of dichloromethane and white viscose ethyl acetate, which exhibited excellent AMPK and ACC activities, were separated by silica gel column chromatography to obtain 5 fractions and 6 fractions, respectively. It was confirmed that AMPK and ACC activities were most excellent among fractions 3 and 5 obtained from the fractions of dichloromethane, fractions 1 and 5 of the fractions obtained from the fractions of ethyl acetate from the whitewater.

Thus, the active components (HD1, HD2, HD3) were separated from these fractions and these components were respectively dissolved in ursolic acid of formula 1, 2-hydroxy-3-methyl-anthraquinone of formula -3-methyl-anthraquinone or 2-hydroxy-1-methoxy-3-methyl-anthraquinone, digitolutein of formula (3).

The acne extract or fraction according to the present invention accelerates the activity of AMPK in cells without toxicity or side effects in vivo, and is also excellent in weight loss, body fat reduction, total cholesterol reduction and inhibition of fat accumulation in liver tissue It has the effect of treating obesity.

As described above, the acne extract or fraction according to the present invention is excellent in the effect of treating obesity, and thus can be used as a medicine or a health functional food useful for prevention or treatment of obesity.

The composition of the present invention may contain at least one known active ingredient having an effect of treating obesity together with the acne extract or fraction.

The compositions of the present invention may further comprise suitable carriers, excipients and diluents conventionally used in the manufacture of pharmaceutical compositions. In addition, it can be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, oral preparations such as syrups and aerosols, external preparations, suppositories and sterilized injection solutions according to a conventional method. Suitable formulations known in the art are preferably those as disclosed in Remington ' s Pharmaceutical Science, recently, Mack Publishing Company, Easton PA. Examples of carriers, excipients and diluents that can be included in the composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose , Microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. When the composition is formulated, it is prepared using a diluent such as a filler, an extender, a binder, a wetting agent, a disintegrant, a surfactant, or an excipient usually used. Solid formulations for oral administration include tablets, pills, powders, granules, capsules and the like, which may contain at least one excipient such as starch, calcium carbonate, sucrose, lactose, Gelatin and the like. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral administration include suspensions, solutions, emulsions, syrups and the like. Various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included in addition to water and liquid paraffin, which are simple diluents commonly used. have. Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Examples of the non-aqueous solvent and suspension include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. Examples of the suppository base include witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin and the like.

The term "administering" as used herein is meant to provide any desired composition of the invention to a subject in any suitable manner.

The preferred dosage of the pharmaceutical composition of the present invention varies depending on the condition and the weight of the patient, the degree of disease, the drug form, the administration route and the period, and can be appropriately selected by those skilled in the art. For a desired effect, the composition of the present invention may be administered in an amount of 1 mg / kg to 300 mg / kg per day. The composition may be administered once a day, or divided into several doses.

The pharmaceutical composition of the present invention can be administered to a subject by various routes. All modes of administration may be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intra-uterine dural or intracerebral injection.

The composition of the present invention can be used alone or in combination with methods using surgery, radiation therapy, hormone therapy, chemotherapy, and biological response modifiers for the prevention or treatment of obesity.

In the present invention, a health functional food refers to a food having a biological control function such as prevention and improvement of disease, bio-defense, immunity, recovery of disease and aging, and is harmless to human body when taken over a long period of time.

The white floret extract or fraction of the present invention can be added to a health functional food for the purpose of preventing or improving obesity. When the white floret extract or fraction of the present invention is used as a food additive, the white floret extract or fraction may be directly added or used together with other food or food ingredients, and may be suitably used according to a conventional method. The amount of the active ingredient to be mixed can be suitably determined according to the intended use (prevention, health or therapeutic treatment). Generally, in production of foods or beverages, the whitewash extract or fraction of the present invention is added in an amount of not more than 15% by weight, preferably not more than 10% by weight based on the raw material. However, in the case of long-term intake for the purpose of health and hygiene or for the purpose of controlling health, the amount may be less than the above range, and since there is no problem in terms of safety, the active ingredient may be used in an amount exceeding the above range.

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

The health beverage composition of the present invention may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. The natural carbohydrates may be monosaccharides such as glucose and fructose, disaccharides such as maltose and sucrose, natural sweeteners such as dextrin and cyclodextrin, synthetic sweeteners such as saccharine and aspartame, and the like. The ratio of the natural carbohydrate is generally about 0.01 to 10 g, preferably about 0.01 to 0.1 g per 100 ml of the composition of the present invention.

In addition to the above, the composition of the present invention may further contain various nutrients, vitamins, electrolytes, flavors, colorants, pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, A carbonating agent used in a carbonated beverage, and the like. In addition, the composition of the present invention may comprise flesh for the production of natural fruit juices, fruit juice drinks and vegetable drinks. These components may be used independently or in combination. Although the ratio of such additives is not critical, it is generally selected in the range of 0.01 to 0.1 parts by weight per 100 parts by weight of the composition of the present invention.

Hereinafter, preferred embodiments, experimental examples, and production examples are provided to facilitate understanding of the present invention. However, the following examples, experimental examples and production examples are provided only for the purpose of easier understanding of the present invention, and the present invention is not limited by the examples, experimental examples and production examples.

Example  One. Baekwunpo  Ethanol extract and Fraction  Produce

The whitewash was cleaned with water to remove foreign matter, and then dried. 10.8 kg of dried whitewash was reflux-extracted twice with 95% ethanol at 80 DEG C for 5 hours. After filtration, the filtrate was concentrated under reduced pressure to obtain 1327.3 g of an aflatoxin ethanol extract.

The whitewater ethanol extract was suspended in water and then sequentially fractionated using dichloromethane (CH ₂ Cl ₂ ), ethyl acetate (EtOAc) and butanol ( n- BuOH). The obtained dichloromethane layer was washed with brine, dried over anhydrous Na ₂ SO ₄ and then filtered. The filtrate was dehydrated and concentrated under reduced pressure to obtain an albumin dichloromethane fraction (343.1 g). (84.96 g), the whitewash butanol fraction (208.6 g) and the whitewash water fraction were obtained in the same manner.

The process of obtaining the acne extract and the fractions is shown in Fig.

Example  2. Baekwunpo  Preparation of ethanol extract

In the same manner as in Example 1, except for using 50% or 75% ethanol instead of 95% ethanol in Example 1, a 50% ethanol extract or a 75% ethanol extract of the whitewater was obtained.

Experimental Example  One. Baekwunpo  Ethanol extract or The fraction AMPK  And ACC  Analysis of impact on activity

1-1. Baekwunpo  Ethanol extract AMPK  And ACC  Effect on activity

The following experiments were carried out to confirm the effect of the extract of the whitewater ethanol obtained in Examples 1 and 2 on AMPK and ACC activity. First, L6 myotube cells were cultured on a medium of 10% FBS α-MEM for 12 hours or more at 37 ° C. and 5% CO _2. After confirming that the cells were fixed, the cells were cultured in 2% FBS α- Were replaced and cultured. Cells were cultured for a total of 10 days with medium exchanged every 48 hours and then exchanged with α-MEM medium without FBS. After 5 hours, the white flake extract (50%, 75% or 95% ethanol extract, 60 μg / mL) obtained in the above Examples 1 and 2 was treated for 2 hours and the cell lysis buffer After the proteins were separated, Western blotting was performed. Metformin (2 mM), an AMPK active substance known as a positive control, was used, and all experiments were repeated twice. The results are shown in Fig.

As shown in FIG. 2, the acne extract had the AMPK and ACC phosphorylation activities. Especially, when 95% ethanol was used as the extraction solvent, it was confirmed that AMPK activity promoting activity was similar to that of the positive control group, metformin.

1-2. Baekwunpo The fraction AMPK  And ACC  Effect on activity

The same experiments as in Experimental Example 1-1 were conducted to confirm the effect of the dichloromethane fraction, the whitewash ethyl acetate fraction, the whitewash fraction, and the white fraternity fraction obtained in Example 1 on AMPK and ACC activity. The results are shown in Fig.

As shown in FIG. 3, it was confirmed that the dolomatous dichloromethane fraction and the white floret ethyl acetate fraction had excellent AMPK phosphorylation activity among the four kinds of aflatoxin fractions.

Example  3. Baekwunpo In the fraction  Isolation of active ingredient

Silica gel column chromatography (Ø 11 × 53 cm) was carried out in order to isolate the active component from the viscous dichloromethane fraction and the whitewash ethyl acetate fraction having excellent AMPK phosphorylation activity in Experimental Example 1.

3-1. Baekwunpo  Dichloromethane In the fraction  Isolation of active ingredient

The fractions of dichloromethane (9.26 g) were obtained from five fractions (Fr: 50: 1 to 1: 1, dichloromethane: methanol = 20: 1 to 1: 1 to 5). The separation process is shown in FIG.

The effect of each fraction (30 or 60 μg / mL) on AMPK and ACC activity was confirmed in the same manner as in Experimental Example 1 above. The results are shown in Fig. 5 and Fig.

As shown in FIG. 5 and FIG. 6, the highest AMPK and ACC phosphorylation activity was observed in fraction 3 (Fr. 3) among the five fractions isolated from the fractions of the dolomucetum dichloromethane.

Further, fraction 3 (Fr. 3, 1.21 g) isolated from the fractions of dolomum dichloromethane was again subjected to silica gel column chromatography (Φ 3 × 45 cm) to obtain HD3 (4.3 mg) from fraction 3-2 . Further, the fraction 3-4 (1.04 g) was subjected again to silica gel column chromatography (Φ 3 × 57 cm) to obtain HD2 (60 mg) and HD1 (220 mg). The separation process is shown in Fig.

3-2. Baekwunpo  Ethyl acetate In the fraction  Isolation of active ingredient

The fractions (84.96 g) of the bisphosphoric acid ethyl acetate were fractionated in six fractions using an elution solvent (hexane: CHCl ₃ = 1: 1, CHCl ₃ 100%, CHCH ₃ : methanol = 100: 1 to 50: 1, methanol 100% (Fr. 1 to 6), and HD1 (5.35 g) was obtained from fraction 1 (Fr. Further, fraction 5 (Fr. 5, 17.26 g) was subjected to silica gel column chromatography (8 x 42 cm) again to obtain HD2 (2.4 g). The separation process is shown in FIG.

Example  4. Baekwunpo In the fraction  Identification of isolated active ingredients

4-1. HD1 Structure identification

TLC, mass spectrum and < ¹³ > C-NMR analysis were performed to identify the structure of HD1 obtained in Example 3 above. The results are shown in Fig. 9 to Fig.

As shown in FIG. 9, as a result of TLC analysis, HD1 did not absorb UV, but it appeared red in the color reaction using 10% sulfuric acid and was expected to be a triterpenoid or steroid compound Could. In addition, it was confirmed that Rf value was the same as that of ursolic acid, which is a typical triterpenoid compound, which has been separated from the whitewash.

As shown in Figs. 10 and 11, the results of mass spectrometry and ¹³ C-NMR analysis were compared with literature values, and ultimately HD1 was identified as ursolic acid.

¹³ C-NMR analysis The summary results are shown below.

¹³ C-NMR (100 MHz, DMSO- d ₆ ) ?: 178.67 (C-28), 138.54 (C-13), 124.93 (C-12), 77.17 (C-18), 47.34 (C-17), 47.17 (C-9), 41.99 (C-14), 38.85 10), 38.55 (C-1), 36.87 (C-4), 36.66 (C-22), 33.04 (C-7), 30.76 ), 27.32 (C-2), 24.14 (C-16), 23.62 (C-27), 23.19 (C-11), 21.45 , 17.26 (C-29), 16.45 (C-25), 15.58 (C-24)

[Chemical Formula 1]

4-2. HD2 Structure identification

¹ H-NMR, ¹³ C-NMR and mass spectral analyzes were carried out to identify the structure of HD2 obtained in Example 3 above. The results are shown in Figs. 12 to 14. Fig.

As shown in Fig. 12, as a result of ¹ H-NMR analysis, a peak corresponding to the integral 3 by the methyl group was observed at δ 2.29, and a peak due to the hydroxy group of the integral 1 was confirmed at δ 11.08.

As shown in FIG. 13, ¹³ C-NMR analysis showed that the peak was observed at? 182.95 and? 181.77, and thus it was found to have a ketone structure. The peaks at? 16.57 revealed that one methyl group .

Further, as shown in Fig. 14, the mass spectral results were compared with the literature values, and finally HD2 was identified as 2-hydroxy-3-methyl-anthraquinone.

¹ H-NMR and ¹³ C-NMR analysis The results are summarized as follows.

^{1 H-NMR (400 MHz,} DMSO- d 6) δ: 11.08 (1H, s, OH), 8.14 - 8.18 (2H, m, 5,8-Hs), 7.97 (1H, s, 4-H), 7.86 (1H, s, 1 H), 2.29 (3H, s, CH ₃ )

¹³ C-NMR (100 MHz, DMSO- d ₆ )?: 182.95 (C-10), 181.77 (C- 9), 161.74 (C-8a), 133.53 (C-10a), 133.43 (C-4a), 132.34 (C-2), 126.92 (C-4), 16.57 ( CH 3)

(2)

4-3. HD3 Structure identification

¹ H-NMR, ¹³ C-NMR and mass spectral analyzes were performed for the structure identification of HD3 obtained in Example 3 above. The results are shown in Fig. 15 to Fig.

As shown in Fig. 15, ¹ H-NMR analysis showed that a peak corresponding to the integral 3 by the methyl group was observed at? 4.03, a peak due to the methyl group at? 2.41 was confirmed, 1 < / RTI >

Further, as shown in FIG. 16, as a result of ¹³ C-NMR analysis, it was confirmed that the characteristic pattern of the anthraquinone shown in the ¹³ C-NMR spectrum of HD 2 was the same, and the peak of the methoxy group As shown in Fig.

Further, as shown in Fig. 17, the results of mass spectrometry were compared with literature values, and HD3 was finally converted to 2-hydroxy-1-methoxy-3-methyl-anthraquinone methyl-anthraquinone, digitolutein).

¹ H-NMR and ¹³ C-NMR analysis The results are summarized as follows.

¹ H-NMR (400 MHz, CDCl ₃ )?: 8.24-8.26 (2H, m, 5-H and 8-H), 7.99 -H and 7-H), 6.75 (1H, s, OH), 4.03 (3H, s, OCH3), 2.41 (3H, s, CH 3)

¹³ C-NMR (100 MHz, CDCl ₃ )?: 182.55 (C-9), 182.44 (C-10), 153.76 (C-3), 146.02 C-6), 133.67 (C-7), 132.98 (C-8a), 131.33 (C-2), 126.98 -9a), 123.52 (C-4a ), 62.16 (OCH 3), 16.34 (CH 3)

(3)

Experimental Example  2. Baekwunpo In the fraction  Activity analysis of isolated active ingredients

The effect of the dichloromethane fraction of dolmen, its fraction 3, HD1, HD2 and HD3 (30 or 60 μg / mL) on AMPK and ACC activity was confirmed in the same manner as in Experimental Example 1 above. The results are shown in Fig. 18 and Fig.

As shown in FIG. 18 and FIG. 19, it was confirmed that the fractions of dichloromethane and the three compounds separated from the fractions had potent AMPK activity and effectively promoted the phosphorylation of ACC as a sub-mechanism thereof.

Experimental Example  3. In animal models Baekwunpo  Effect of ethanol extracts on the anti-obesity effect

Animal experiments were carried out to examine the anti-obesity effect of the ethanol extract of the aflatoxins prepared in Example 1 above. To induce obesity in mice, high fat diet (HFD) was fed for 8 weeks. The experimental group was orally administered with a high fat diet and a 100% ethanol extract at a concentration of 150 mg / kg or 300 mg / kg daily. In order to check whether the induction of obesity was normal, the control group fed a general diet.

At the end of the drug administration period, body weights of each mouse, abdominal fat analysis, blood analysis, and oil red O staining of liver tissue were performed. The results are shown in Figs. 20 to 23, respectively.

As shown in FIG. 20, the body weight of each mouse was increased by about 30% in the control group which was fed with the high-fat diet compared with the normal diet group, (** P> 0.01; * P> 0.05), respectively.

In addition, as shown in Fig. 21, the abdominal fat analysis of each mouse showed that abdominal fat of the control group with a high-fat diet was significantly increased compared to that of the normal diet group, and the ethanol extract of Baeknu One group showed inhibition of abdominal fat increase.

As shown in FIG. 22, the total cholesterol level of the control group in which the high-fat diet was higher than that in the normal diet group was significantly increased in the blood analysis of each mouse, and the group treated with the high- This increase in total cholesterol was statistically significantly inhibited (* P> 0.05). There was no significant difference in LDL-cholesterol levels among the groups.

As shown in Fig. 23, the liver tissues of the mice were stained with oil red ocher. As a result, the fat was significantly increased in the liver tissues of the control group which was fed with high fat compared to the normal group, Showed a marked inhibition of the increase in fat in liver tissues

From the above results, it was confirmed that the Acanthopanax acnes extract has an anti-obesity effect that suppresses the increase of total cholesterol and inhibits the accumulation of fat in the liver, showing excellent effects on weight loss and body fat reduction.

Hereinafter, a pharmaceutical composition containing the composition of the present invention and a preparation example of a health functional food will be described, but the present invention is not limited thereto but is specifically described.

Formulation example  1. Preparation of pharmaceutical compositions

1-1. Manufacture of Powder

Acupuncture extract or fraction 20 mg

Lactose 100 mg

Talc 10 mg

The above components are mixed and filled in airtight bags to prepare powders.

1-2. Manufacture of tablets

Acupuncture extract or fraction 10 mg

Corn starch 100 mg

Lactose 100 mg

Magnesium stearate 2 mg

After mixing the above components, tablets are prepared by tableting according to the usual preparation method of tablets.

1-3. Preparation of capsules

Acupuncture extract or fraction 10 mg

Crystalline cellulose 3 mg

Lactose 14.8 mg

Magnesium stearate 0.2 mg

The above components are mixed according to a conventional capsule preparation method and filled in gelatin capsules to prepare capsules.

1-4. Injection preparation

Acupuncture extract or fraction 10 mg

180 mg mannitol

Sterile sterilized water for injection 2974 mg

Na ₂ HPO ₄ .2H ₂ O 26 mg

(2 ml) per 1 ampoule in accordance with the usual injection preparation method.

1-5. Manufacture of liquid agent

Acupuncture extract or fraction 20 mg

10 g per isomer

5 g mannitol

Purified water quantity

Each component was added and dissolved in purified water according to the usual liquid preparation method, and the lemon flavor was added in an appropriate amount. Then, the above components were mixed, and purified water was added thereto. The whole was added with purified water to adjust the total volume to 100 ml, And sterilized to prepare a liquid preparation.

Formulation example  2. Preparation of food composition

2-1. Manufacture of health food

Acupuncture extract or fraction 100 mg

Vitamin mixture quantity

Vitamin A acetate 70 μg

Vitamin E 1.0 mg

Vitamin B1 0.13 mg

0.15 mg of vitamin B2

Vitamin B6 0.5 mg

Vitamin B12 0.2 μg

Vitamin C 10 mg

Biotin 10 μg

Nicotinic acid amide 1.7 mg

Folic acid 50 μg

Calcium pantothenate 0.5 mg

Mineral mixture quantity

1.75 mg of ferrous sulfate

0.82 mg of zinc oxide

Magnesium carbonate 25.3 mg

Potassium monophosphate 15 mg

Secondary calcium phosphate 55 mg

Potassium citrate 90 mg

Calcium carbonate 100 mg

Magnesium chloride 24.8 mg

Although the composition ratio of the above-mentioned vitamin and mineral mixture is comparatively mixed with a composition suitable for health food as a preferred embodiment, the compounding ratio may be arbitrarily modified, and the above ingredients are mixed according to a conventional method for producing healthy foods , Granules can be prepared and used in the manufacture of health food compositions according to conventional methods.

2-2. Manufacture of health drinks

Acupuncture extract or fraction 100 mg

Vitamin C 15 g

Vitamin E (powder) 100 g

19.75 g of ferrous lactate

3.5 g of zinc oxide

Nicotinic acid amide 3.5 g

Vitamin A 0.2 g

Vitamin B1 0.25 g

Vitamin B2 0.3g

Water quantification

The above components were mixed according to a conventional health drink manufacturing method, and the mixture was stirred and heated at 85 DEG C for about 1 hour. The solution thus prepared was filtered and sterilized in a sterilized 2 liter container, It is used in the production of the health beverage composition of the invention.

Although the compositional ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the compounding ratio according to the regional or national preference such as the demand class, the demanding country, and the use purpose.

Claims (11)

Pharmaceutical composition for the prevention or treatment of obesity, containing baekwoon extract or fraction as an active ingredient.
The method of claim 1, wherein the extract of the dolomite powder is characterized in that the powder is extracted from any one or more solvents selected from the group consisting of water, alcohol having 1 to 4 carbon atoms and mixed solvents thereof, obesity prevention or treatment pharmaceutical composition .
The pharmaceutical composition of claim 2, wherein the alcohol is 50 to 95% ethanol.
The method according to claim 1, wherein the dolomite fraction is
(a) extracting the powder of the dolomite powder with one or more solvents selected from the group consisting of water, alcohols having 1 to 4 carbon atoms and mixed solvents thereof; And
(b) suspending the extract of step (a) in water, and then sequentially dividing with dichloromethane, ethyl acetate and butanol; characterized in that the pharmaceutical composition for preventing or treating obesity.
The pharmaceutical composition for preventing or treating obesity according to claim 4, wherein the fraction is a fraction of distillate or distillate ethylacetate.
Ursolic acid of formula 1, 2-hydroxy-3-methyl-anthraquinone of formula 2 and 2-hydroxy-1-methoxy-3 of formula 3 -Methyl-anthraquinone (2-hydroxy-1-methoxy-3-methyl-anthraquinone, digitolutein) A pharmaceutical composition for preventing or treating obesity, comprising any one or more compounds selected from the group consisting of active ingredients.
[Chemical Formula 1]

(2)

(3)

The pharmaceutical composition for preventing or treating obesity, according to claim 6, wherein the compound of Chemical Formulas 1 to 3 is obtained by extracting and separating from the dolomite.
Food composition for the prevention or improvement of obesity, including baekwool extract or fraction as an active ingredient.
The method of claim 8, wherein the dolomite extract is characterized in that the dolomite ethanol extract, obesity prevention or improvement food composition.
The method according to claim 8, wherein the fraction of the dolomite fraction is a dolomite dichloromethane fraction or dolomite ethyl acetate fraction, characterized in that the food composition for preventing or improving obesity.
Ursolic acid of formula 1, 2-hydroxy-3-methyl-anthraquinone of formula 2 and 2-hydroxy-1-methoxy-3 of formula 3 -Methyl-anthraquinone (2-hydroxy-1-methoxy-3-methyl-anthraquinone, digitolutein) A food composition for preventing or improving obesity comprising any one or more compounds selected from the group consisting of as an active ingredient.
[Chemical Formula 1]

(2)

(3)

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