KR20040012110A - Lipase inhibitor and functional food preventing from an obesity containing the same - Google Patents

Abstract

PURPOSE: Provided are a lipase inhibitor and a functional food containing the same for preventing obesity. The lipase inhibitor contains dioscin or its derivatives as an active ingredient and the food containing it for the prevention of obesity inhibits lipid uptake. CONSTITUTION: A lipase inhibitor is characterized by containing, an active ingredient, dioscin represented by the formula(1) or its derivatives, such as diosgenin, gracillin, prosapogenin A and prosapogenin C. The dioscin is preferably extracted from Dioscrea batatas, Dioscrea japonica, Dioscrea bulbifera, Dioscrea nipponica, Dioscrea tokoro, Dioscrea tenuipes, Dioscrea septemloba, Dioscrea quinqueloba and the like.

Description

Lipase inhibitor and functional food preventing from an obesity containing the same

The present invention relates to a lipase inhibitor and an anti-obesity functional food containing the same, and more particularly, by containing a lipase inhibitor that inhibits degradation of lipids and the lipase inhibitor, thereby inhibiting absorption of fat into the body to prevent and treat obesity. It relates to a functional food for preventing obesity that can be used as.

Fats are high in energy density and easily accumulated in the body, which is a major cause of obesity. Fat accumulates mainly in the subcutaneous tissue, and it can accumulate around the heart and interfere with heart function. Obesity, a condition characterized by excess body fat, is known as a risk factor for diseases such as diabetes, arteriosclerosis, heart disease, hypertension, liver disease, gallstones, gout, kidney disease, and breast cancer. As described above, obesity is not only a health problem directly related to life, but especially for women, the cost of losing weight every year is a social problem.

To control obesity, it is necessary to reduce food intake, increase energy consumption, and suppress fat accumulation in the body. While it is well known that suppressed diets can induce weight loss, they do not effectively reduce food intake unless accompanied by the intake of chemical appetite reducers, and in many cases do not promote long term weight loss. Therefore, increasing energy consumption rather than reducing food intake is effective in suppressing obesity. However, due to the characteristics of modern society, which is difficult to continuously exercise, the main efforts for suppressing obesity are focused on the intake of drugs and supplements having an anti-obesity effect.

Drugs used as therapeutic agents for obesity include drugs that act on the central nervous system such as noradrenaline receptors, serotonin receptors, dopamine receptors, histamine receptors and the like. These drugs are effective by inducing appetite suppression, but are accompanied by side effects such as headache and insomnia. Indeed, in the West, anti-obesity drugs have been developed to inhibit fat digestion, and pancreatic lipase-inhibiting drugs are predominant (Tsuji M. et al ., Nippon Yakurigaku Zassh i, 118 (5): 340-). 346 (2001).

Lipase is an enzyme secreted by the pancreas of the human body and is involved in the digestion of fat. In other words, it is involved in converting triglycerides into monoglycerides and free fatty acids which are easily absorbed, and inhibiting them is known to have an effect of inhibiting the concentration of triglycerides in the blood.

Drugs that inhibit pancreatic lipases, such as orlistat (Generic), are drugs that inhibit the absorption of fat in food. These drugs remain only in the gastrointestinal tract and are excreted, are not absorbed into the body at all, and 97% of the dose is excreted in the stool, so there are no side effects like central nervous system drugs. In addition, it can prevent diabetes, hypertension and cholesterol deposition due to obesity, and also reduces the concentration of triglycerides in the blood. In addition, after weight loss in dietary suppression regimens, there is no weight re-expansion (yo-yo) phenomenon that appears when discontinuation. However, side effects such as disturbing the absorption of vitamins or bowel movements are also a problem.

Examples of reported obesity-inhibiting activity from plant materials include alginic acid in seaweeds (Jin, Jin-ho et al., Journal of the Korean Fisheries Society, 19: 303-311 (1986)), and extracts of ogal skin (Son Kyu-mok, et al., Korean Journal of Food and Nutrition Science, 21: 9 (1992). ), Bellflower Extract (Han LK et al., J. Nutr. , 130: 2760-4 (2000)).

However, there has been a continuing need for development of new plant materials and materials that can exhibit an anti-obesity effect without exhibiting side effects.

On the other hand, the perennial plant is a perennial herb, vine-like, and has starch-rich storage roots. The leaves are attached to the stems as a symbiosis or symbiosis, usually divided into heart-shaped or intestine, and have reticular veins. The flowers are ear-shaped, and the fruits are grains or berries. The active ingredient contains a lot of saponin (saponin), steroid saponin (steroid saponin) contains diosin (dioscin), diosgenin (diosgenin) and the like. It is known that 12 species grow in Korea (Korea Society of Pharmaceutical Botanicals, New Drug Botany, Hakchangsa, 228-229 (1991)).

The medicinal effect of the plant, Ma and Pan-ma, is written in "Agreement Gagam", saying, "Har and gods are strengthened, and the five intestines are strengthened to strengthen energy, strengthen muscles and bones, and control the stomach to relieve diarrhea and relax the mind." It is generally used as a rejuvenating medicine and used for fatigue fatigue, chronic cough, and loss of appetite.

The present inventors completed the present invention by finding that the dioxins contained in the apple plants are excellent in the results, as a result of searching for a substance that inhibits the digestion of fats and evaluating the degree of lipase inhibition, like Zenical.

The present invention has been made in view of the above demands, and an object of the present invention is to provide a lipase inhibitor capable of controlling the rise of triglyceride concentration in the blood by regulating lipid metabolism.

Another object of the present invention to provide a functional food for preventing obesity, characterized in that it comprises the lipase inhibitor.

1 is a graph showing the change in plasma lipid concentration (mg / d) with time in mice after administration of diosin according to the concentration.

◆: Control ■: Diosin (50mg / ㎏)

▲: Diosin (100mg / kg) ●: Zenical (5mg / kg)

Figure 2 is a graph showing the change in plasma lipid concentration (mg / d) over time in mice after administration of diosgenin according to the concentration.

◆: Control ■: Diosgenin (50mg / kg)

▲: Diosgenin (100mg / kg) ●: Zenical (5mg / kg)

Figure 3 is a weekly intake (g) of the mice's intake (g) for the diet containing 2% by weight and 5% by weight of diocin-containing fan fan powder.

◆: Control ■: Fan Hemp 2% by weight

▲: 5% by weight fan

Figure 4 shows the weight increase rate (%) of the mice on a weekly basis after administering the fan-containing powder containing diocin to the mouse.

◆: Control ■: Fan Hemp 2% by weight

▲: 5% by weight fan

In order to achieve the above object, the present invention provides a lipase inhibitor containing diocin or a derivative thereof as an active ingredient. The present invention also provides a lipase inhibitor containing fanza extract as an active ingredient.

In the lipase inhibitor according to the present invention, it is preferable to use the dioxins or derivatives thereof, which are extracted from an asteraceae, and more preferably, those extracted from fan horses.

In order to achieve another object of the present invention, the present invention provides a functional food for preventing obesity comprising the lipase inhibitor.

Hereinafter, the present invention will be described in detail.

The present invention is characterized by providing a lipase inhibitor containing a dioxin represented by the following formula (1) or a derivative thereof as an active ingredient.

Specifically, the diosin is hemp (Dioscrea Batatas), yam (Dioscrea Japonica), round horse (Dioscrea Bulbifera), fan fan (Dioscrea Nipponica), big horse (Dioscrea Tokoro), kelp (Dioscrea Tenuipes), chrysanthemum (Dioscrea Septembloba) ), It is preferable to be extracted from an apple plant, such as Dioscrea Quinqueoloba, more preferably from a hemp or fan.

In addition to the diosin, in the basic skeleton of the diosin represented by the following formula (2),

Diosgenin, wherein R is H,

Gracillin,

Phosphorus prosapogenin A and

Derivatives of diosin, such as phosphorus prosapogenin C, may also be used, and these derivatives may be obtained by hydrolysis of diosin or may be extracted directly from an asteraceae and isolated.

In addition, the present invention is characterized by providing a lipase inhibitor containing a fan fan extract as an active ingredient.

In one embodiment of the present invention, to obtain diocin or its derivatives, diocin was extracted from the fan. Extraction method can be extracted with water or an organic solvent from the skin, root, stem, leaf of the plant, using a conventional method known in the art, specifically in the present invention extracted with methanol from fan . The extract thus obtained is filtered, concentrated under reduced pressure, chromatographed, the substance is separated and recrystallized to obtain diosine or a derivative thereof. Specifically, silica gel column chromatography was used, and methanol was used as a recrystallization solvent.

In another embodiment of the present invention, the lipase inhibitory activity of dioxin or its derivatives and fanica extract was measured according to the change in concentration. The substrate may be used without limitation as long as the lipase acts as a substance capable of breaking down lipids into monoglycerides and fatty acids. Specifically, 4-methylumbelliferyl oleate was used in the present invention.

The lipase inhibitor according to the present invention may contain the dioxins or derivatives thereof extracted as an active ingredient, or may contain fanza extract, and according to the pharmaceutical preparation methods known in the art, Acceptable carriers may also be added to prepare the pharmaceutical compositions.

Examples of the carrier in the above, lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, microcrystalline cellulose, poly Vinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. In addition, the lipase inhibitor may further include fillers, anti-coagulants, lubricants, wetting agents, fragrances, emulsifiers or preservatives.

The composition containing the lipase inhibitor of the present invention can be used clinically for the prevention and treatment of obesity, control of triglycerides in blood, lowering cholesterol levels, improving blood pressure, treating hyperlipidemia and diabetes.

In the lipase inhibitor according to the present invention, the effective amount of diocin is 50 mg to 500 mg / kg, preferably 100 to 200 mg / kg. Dosage may be determined by the expert taking into account various factors such as the severity of obesity, the condition of the patient, age, complications and the like.

On the other hand, the present invention provides a functional food for preventing obesity comprising the lipase inhibitor. The lipase inhibitor according to the present invention may be used alone or in addition, but may be synergistic by adding a known substance or a new substance used to prevent or treat obesity. In addition, general additives such as food colorings, food flavorings, herbal medicines, fruits, oligosaccharides, chitosan, citric acid and the like may be used to give good taste and aroma.

Functional foods containing the lipase inhibitor of the present invention include, but are not limited to, confectionery such as bread, rice cakes, dried fruits, candy, chocolates, chewing gum, and nuts; Ice cream products such as ice creams, ice creams, and ice cream powders; Dairy products such as milk, low-fat milk, lactose-decomposed milk, processed milk, goat milk, fermented milk, butter milk, concentrated milk, milk cream, butter oil, natural cheese, processed cheese, milk powder, whey; Meat products such as meat products, processed products, and hamburgers; Fish meat products such as fish meat products such as fish paste, ham, sausage and bacon; Noodles such as ramen noodles, dried noodles, raw noodles, fried noodles, deluxe dried noodles, refined noodles, frozen noodles and pasta; Beverages such as fruit drinks, vegetable drinks, carbonated drinks, lactic acid bacteria drinks such as soy milk and yogurt, mixed drinks; Seasoning foods such as soy sauce, miso, red pepper paste, chunjang, cheongukjang, mixed soy sauce, vinegar, sauce, tomato ketchup, curry, and dressing; Margarine, shortening; And pizza, but are not limited thereto.

Hereinafter, the present invention will be described in detail by way of examples.

However, the following examples are merely to illustrate the invention, but the content of the present invention is not limited to the following examples.

Example 1 Isolation and Purification of Diosin and Its Derivatives

(1-1) Isolation and Purification of Diosin

After cutting 3 kg of root diameter of Dioscorea nipponica , the mixture was extracted three times for 72 hours with 5000 ml of methanol at 25 ° C. using a reflux condenser. The obtained methanol extract was filtered with a funnel using filter paper, and then concentrated under reduced pressure at 76 cmHg to obtain 115.1 g of Methanol extract. 25 g of Fanoma methanol extract was added to a silica gel column (90 × 6 cm, Merck 7734 silica gel 900 g), CHCl ₃ : CH ₃ OH: H ₂ O = 7: 3: 1 (mixed in the above ratio in a separatory funnel to use the lower layer) It was developed using a solvent of. After the start of development, eight fractions of 2000 ml were obtained after 60 minutes. Fraction 5 of this step was increased in polarity from the solvent of water saturated CH ₃ COOCH ₂ CH ₃ : CH ₃ OH = 98: 2 to the solvent of water saturated CH ₃ COOCH ₂ CH ₃ : CH ₃ OH = 95: 5. , Silica gel column chromatography was performed (at this time, water-saturated CH ₃ COOCH ₂ CH ₃ means the upper layer after mixing CH ₃ COOCH ₂ CH ₃ and distilled water in a separating funnel 1: 1 and left for 6 hours). . After the start of development, 60 fractions of 500 ml were obtained after 30 minutes. Diosine was obtained from fractions 35 to 50 of the fractions obtained, and TLC and NMR analysis was used to confirm that this material was diosin. Diosin was recrystallized from methanol to obtain colorless needle crystals. Dioxin measurements are as follows.

Melting Point: 290 ~ 292 ℃

[α] _D ²⁵ : -112.3 ° (c, 0.3 in MeOH)

IR (KBr, cm ^-1 ) 3420, 1640, 1100-1000, 920, 900, 866, 838 (900> 920, 25 (R) -spiroketal), 811

¹ H NMR (300 MHz, pyridine-d ₅ ) δ 0.81 (s), 1.01 (s), 1.09 (d, J = 6.9 Hz), 0.69 (d, J = 5.2 Hz), 5.30 (brd, J = 4.6 Hz), 1.52 (d, J = 6.2 Hz), 1.66 (d, J = 6.1 Hz), 4.82 (d, J = 7.4 Hz), 5.62 (brs), 6.17 (s).

¹³ C NMR (75.5 MHz, pyridine-d ₅ ) δ 37.4, 29.9, 78.0, 38.8, 140.7, 121.5, 32.0, 31.6, 50.6, 37.0, 20.9, 39.8, 40.3, 56.5, 32.2, 80.9, 62.8, 16.2, 19.3, 41.8, 14.8, 109.0, 31.7, 29.1, 30.4, 66.7, 17.1

(1-2) Isolation and Purification of Diosgenin

Part 1 of the eight fractions of Example (1-1) was subjected to silica gel column chromatography with a solvent of CH ₃ COOCH ₂ CH ₃ . After starting the development, 15 small fractions were obtained in 500 ml from 20 minutes afterwards, and dioxenin was obtained from 5 to 14 small fractions of which, using TLC and MS analysis, determined that the substance was diosgenin. Confirmed. Diosgenin was recrystallized from methanol to obtain colorless needle crystals. The measured value of diosgenin is as follows.

Melting Point: 298 ~ 300 ℃

[α] _D ²⁵ : -41.7 ° (c, 0.2 in pyridine)

IR (KBr, cm ^-1 ) 3420, 1650, 1075, 1025, 835, 800

MS (30 eV), m / z (rel. Int.) 414 (13.1), 412 (6.7), 397 (60.4), 396 (100), 396 (44.5), 382 (28.5), 381 (17.1), 329 (7.0), 303 (10.7), 275 (20.8), 273 (16.7), 271 (10.8), 255 (69.8), 229 (13.5), 213 (38.0)

(1-3) Isolation and Purification of Gracillin

Gracillin was obtained from subfractions 52 to 59 of the 60 subfractions of Example (1-1), using TLC and NMR analysis, it was confirmed that the substance is gracillin. Gracillin was recrystallized from methanol to obtain colorless needle crystals. The measurement of gracillin is as follows.

Melting Point: 296 ~ 298 ℃

[α] _D ²⁵ : -95 ° (c, 0.4 in pyridine)

IR (KBr, cm ^-1 ) 3420, 1640, 1100-1000, 920, 900, 866, 836 (900> 920, 25 (R) -spiroketal), 812

¹ H NMR (300 MHz, pyridine-d ₅ ) δ 0.82 (s), 1.04 (s), 1.11 (d, J = 6.9 Hz), 0.71 (d, J = 5.7 Hz), 5.32 (brd, J = 4.8 Hz), 1.66 (d, J = 6.1 Hz), 4.84 (d, J = 7.3 Hz), 4.97 (d, J = 7.7 Hz), 6.18 (s).

¹³ C NMR (75.5 MHz, pyridine-d ₅ ) δ 37.5, 30.0, 78.4 ^a , 38.7, 140.8, 121.7, 32.2 ^b , 31.8, 50.3, 37.1, 21.1, 39.9, 40.4, 56.7, 32.3 ^b , 81.0, 62.9 , 16.2, 19.3, 41.9, 14.9, 109.2, 31.7, 29.2, 30.5, 66.8, 17.2

(1-4) Isolation and Purification of Prosapogenin A

Fraction 4 of the eight fractions of Example (1-1) was used as a solvent of CHCl ₃ : CH ₃ OH: H ₂ O = 7: 3: 1 (using the lower layer after being left in a separatory funnel for 10 hours). Silica gel column chromatography was carried out, and prosapogenin A was obtained from the small fractions 6 to 12 of the 15 small fractions which were separated by 500 ml from 15 minutes after the development. Prosapogenin A was recrystallized from methanol to obtain colorless needle crystals. Measured values of prosapogenin A are as follows.

Melting Point: 238 ~ 240 ℃

[α] _D ²⁵ : -12.5 ° (c, 0.4 in MeOH)

IR (KBr, cm ^-1 ) 3410, 1650, 1100-1000, 920, 900, 865, 837 (900> 920, 25 (R) -spiroketal), 811

¹ H NMR (300 MHz, pyridine-d ₅ ) δ0.80 (s), 1.01 (s), 1.09 (d, J = 6.9Hz), 0.68 (d, J = 5.7Hz), 5.28 (brd, J = 4.8 Hz), 1.67 (d, J = 6.3 Hz), 4.92 (d, J = 7.2 Hz), 6.20 (s).

¹³ C NMR (75.5 MHz, pyridine-d ₅ ) δ 37.4, 30.0, 77.9, 38.8, 140.8, 121.5, 32.0, 31.6, 50.2, 37.0, 20.9, 39.8, 40.3, 56.5, 32.2, 80.9, 62.8, 16.1, 19.2, 41.8, 14.8, 109.0, 31.7, 29.1, 30.4, 66.7, 17.1

(1-5) Isolation and Purification of Prosapogenin C

Fraction 2 of the eight fractions of Example (1-1) was used as a solvent of CHCl ₃ : CH ₃ OH: H ₂ O = 8: 2: 0.5 (using the lower layer after being left in a separatory funnel for 10 hours). Silica gel column chromatography was performed, and prosapogenin C was obtained from the small fractions 7 to 16 of the 24 small fractions which were separated from 30 minutes to 500 ml after development. Prosapogenin C was recrystallized from methanol to obtain colorless needle crystals. Measured values of prosapogenin C are as follows.

Melting Point: 247 ~ 249 ℃

IR (KBr, cm ^-1 ) 3450, 1650, 1070, 1045, 1025, 920, 900, 865, 835 (900> 920, 25 (R) -spiroketal), 810

¹ H NMR (300 MHz, pyridine-d ₅ ) δ0.70 (3H, d, J = 5.2 Hz, 27-CH ₃ ), 0.83 (3H, s, 18-CH ₃ ), 0.92 (3H, s, 19 -CH ₃ ), 1.13 (3H, d, J = 6.9 Hz, 21-CH ₃ ), 5.01 (1H, d, J = 7.7 Hz, anomeric H), 5.31 (1H, brd, J = 4.4 Hz, H- 6)

¹³ C NMR (75.5 MHz, pyridine-d ₅ ) δ37.3, 30.0, 78.3 ^* , 39.1, 140.7, 121.5,32.0, 31.5, 50.1, 36.9, 20.9, 39.7, 40.3, 56.5, 32.1, 80.9, 62.7, 16.2 , 19.2, 41.8, 14.8, 109.1, 31.6, 29.1, 30.4, 66.7, 17.1, 102.4, 75.1, 78.0 ^* , 71.5, 78.2 ^* , 62.7

Example 2 Measurement of Pancreatic Lipase Inhibitory Activity

(2-1) Determination of Pancreatic Lipase Inhibitory Activity of Fanica Extracts

Porcine pancreatic lipase used in this experiment was purchased from Sigma (St Louis, MO, USA), and 4-methylumbelliferyl oleate was used as a substrate. Meanwhile, as a positive control, Xenical (Xenical ^?, Roche, Switzerland), which is clinically used as a lipase inhibitor, was used.

The Fanza extract obtained in Example 1 was dissolved in dimethyl sulfoxide (DMSO) at a concentration of 0.05 mg / mL, 0.5 mg / mL, 5 mg / mL and 50 mg / mL to prepare a solution, which contained pancreatic lipase and a substrate. The degree of inhibition of lipase was investigated by Kawaguchi et al. (Kawaguchi K. et al. , Biosci. Biotechnol. Biochem. , Jan. 61 (1): 102-104 (1997)). The measurement was repeated three times, and the results are shown in Table 1 below as the average value ± standard deviation.

(2-2) Measurement of Pancreatic Lipase Inhibitory Activity of Diosin

Porcine pancreatic lipase, substrate, and positive control were used in this experiment the same as in Example 2-1.

The diocin obtained in Example 1-1 was dissolved in dimethyl sulfoxide at 0.05 mg / mL, 0.5 mg / mL, 5 mg / mL and 50 mg / mL concentrations to prepare a solution, and this was an enzyme containing pancreatic lipase and a substrate. Into the reaction solution, the inhibition of lipase was examined according to methods such as Kawaguchi. The measurement was repeated three times, and the results are shown in Table 1 below as the average value ± standard deviation.

Concentration (µg / ml) Lipase inhibition degree (%) Fan Methanol Extract Diosin Zenical 0.05 - 37 ± 8 77 ± 4 0.5 52 ± 4 20 ± 22 67 ± 16 5 60 ± 9 83 ± 2 86 ± 6 50 90 ± 1 88 ± 0 97 ± 0

As shown in Table 1, 60 mg, dioxin, 83%, and Zenical 86% inhibitory activity was shown in Methanol extract of 5% at 5 ㎍ / ㎖ concentration. In addition, diosin or fanza extract was found to have the ability to inhibit lipolytic enzymes even at 0.5 ug / ml, which is slightly lower in terms of activity than jenical, but is considered to have a significant inhibition of fat digestion as a natural product.

(2-3) Measurement of Pancreatic Lipase Inhibitory Activity of Diosin Derivatives

Porcine pancreatic lipase, substrate, and positive control were used in this experiment the same as in Example 2-1.

Diosgenin, gracillin, prosapogenin A and prosapogenin C, which are diosine derivatives obtained in the same manner as in Example 1-2, were added to dimethyl sulfoxide, respectively. A solution was prepared by dissolving at a concentration of 5.00 µg / ml, 12.50 µg / ml, 25.00 µg / ml, 50.00 µg / ml, and 125 µg / ml, and then, it was added to an enzyme reaction solution containing pancreatic lipase and a substrate. The inhibition of lipase was investigated according to the method of. The results are shown in Table 2 below.

Concentration (µg / ml) Lipase inhibition degree (%) Diosgenin Gracillin Prosapogenin A Prosapogenin C 5.00 11.52 11.61 61.91 12.37 12.50 36.27 45.45 70.37 33.20 25.00 44.32 58.13 75.71 44.88 50.00 61.87 64.29 87.61 49.16 125.00 83.69 - - - IC ₅₀ (Μg / ml) 27.99 28.87 1.81 42.21

As shown in Table 2, the saponin-based diosin derivatives of diosgenin, gracillin, prosapogenin A and prosapogenin C showed lipase inhibitory effects of 11% to 87% depending on the concentration of administration. In particular, prosapogenin A showed strong inhibitory activity even at 5 µg / ml. From these results, it was found that the diosin derivative has lipase inhibitory activity.

<Example 3> Blood triglyceride concentration lowering effect in the mouse

(3-1) Effects of Dermabrasion Extracts on Blood Triglycerides in Mice

Sprague-Dawley rats (230-240 g) were divided into a control group, 2% by weight fan group, and 5% by weight fan group, and 7 animals of each group were raised for 8 weeks, and blood was collected. Blood was drawn from the heart, and total triglycerides, total cholesterol, HDL (high density lipoprotein), VLDL (ultra low density lipoprotein), low density lipoprotein (LDL), AI, GOT, GPT, and the like were obtained using a sigma kit (St Louis, USA). Measured.

As a result, as shown in Table 3, the control group without the fan fan extract showed a triglyceride concentration of 59 mg / 반면 while 35 mg / ㎗, 41 mg / respectively in the 2% and 5% fan fan intake group, respectively 중 showed triglyceride concentration in blood, and it was confirmed that fan intake significantly lowered total triglyceride concentration in blood.

Comparison of Blood Lipids and Hematological Indicators in Rats After Infant Powder (8 Weeks) ^* Control 2% by weight fan Fan weight 5% by weight Total triglyceride (mg / ㎗) 59 ± 14 ^a 35 ± 9 ^b 41 ± 11 ^b Total Cholesterol (TC) (mg / dl) 110 ± 13 ^a 93 ± 6 ^b 82 ± 9 ^b HDL cholesterol (mg / cc) 16 ± 2 ^a 21 ± 3 ^b 22 ± 2 ^b VLDL Cholesterol (mg / dl) 12 ± 3 ^a 7 ± 2 ^b 8 ± 2 ^b LDL cholesterol (mg / dl) 82 ± 15 ^a 65 ± 8 ^b 52 ± 10 ^b HDL / TC 0.15 ± 0.03 ^a 0.22 ± 0.04 ^b 0.27 ± 0.04 ^b AL ^** 6.1 ± 1.6 ^a 3.6 ± 0.9 ^b 2.8 ± 0.6 ^b GOT (Karmen / mL) 62.8 ± 15.9 ^a 64.3 ± 6.1 ^a 63.1 ± 6.4 ^a GPT (Karmen / mL) 17.8 ± 8.2 ^a 20.4 ± 7.0 ^a 18.1 ± 9.9 ^a

^* Values with the same subscript in the same column do not differ significantly at 5%

^** AI (atherogenic index) = (Total Cholesterol-HDL Cholesterol) / HDL Cholesterol

(3-2) Dioxin-induced Blood Neutral Fat Drop in Mouse

Overnight fasted mice (ICR mouse, 40 ± 5g) was administered orally with a 200-dilution of fat-diocin suspension based on 40g body weight of the mouse. The fat-diocin suspension may contain 15 mg of cholic acid, 100 μl of dimethylsulfoxide, 1000 μl of corn oil, 1000 μl of saline, and different concentrations of diosin (50 mg / kg, 100 mg / kg) or Xenical (5 mg / kg) was added and prepared by sonication for 5 minutes. The serum triglyceride concentration was collected from the tail of rats every 30 minutes, 1 hour, 2 hours, 3 hours and 4 hours before oral administration of the suspension (0 min), and the kit for triglyceride measurement (Sigma 336). -10, St Louis, USA).

As a result, as shown in FIG. 1, the control group without diocin showed a rapid increase in blood triglyceride concentration after 1 hour of oral administration of lipid suspension, while dioxin was mixed with lipid suspension orally at 100 mg / kg body weight. In the case of the mice administered, the lipid triglyceride concentration increased by the administration of the lipid suspension was shown to be slower than the control group.

(3-3) Effects of Diosine Derivatives on the Lowering of Triglyceride Levels in Blood

Overnight overnight fasted mice (ICR mouse, 40 ± 5g) was administered orally 100 mg of fat-diosgenin suspension based on 1kg of the mouse body weight. The suspension of fat-diogeninine is 15 mg of cholic acid (cholic acid), 100 μl of dimethyl sulfoxide, 1000 μl of corn oil, 1000 μl of physiological saline, and different concentrations of diosgenin (50 mg / kg, 100 mg / kg). Alternatively, Zenical (5 mg / kg) was added and sonicated for 5 minutes. The serum triglyceride concentration was collected from the tail of the rat every 1 hour, 2 hours, 3 hours and 4 hours before oral administration of the suspension (0 min), and the kit for measuring triglycerides (Sigma 336-10, St Louis, USA).

As a result, as shown in Figure 2, the control group containing no diocin showed a sharp increase in blood triglyceride concentration 1 hour after oral administration of lipid suspension, while diosin oral at 50 mg / kg body weight mixed with lipid suspension In the case of the mice administered, the lipid triglyceride concentration increased by the administration of the lipid suspension was shown to be slower than the control group.

These results indicate that diosin, diosin derivatives, and panaxima extract inhibit lipase, which effectively inhibited triglycerides, resulting in less triglycerides and less triglycerides absorbed into the body. have. In particular, as the dioxin concentration increased from 50 mg / kg to 100 mg / kg it was found that the inhibitory effect of the increase in the blood lipid concentration. The experimental data is the average of the results obtained using 7 mice per treatment.

This example shows that diosin and fanica extracts exert lipolysis inhibitory effects not only in vitro but also in vivo.

<Example 4> Weight loss measurement of fan horse extract

In this experiment, 7 Sprague-Dawley rats (230 ± 10 g) were used for each experiment. At this time, the fan-containing powder tank was AIN-76 feed (ICN, Costa Mesa, CA, USA). ) Was fed to a high fat diet in which tallow was added so that fat was 64% of total calories. The experiment was divided into three groups, the control group containing no fan, 2% by weight and 5% by weight fan fan powder treatment group. Dietary intake and body weight were measured at intervals of 2-3 days while feeding the experimental diet. The dietary intake was less than the control group at the beginning of the experiment compared to the control group, but from the second week all three groups were found to consume almost the same amount (see Figure 3). As a result, there was a big difference in the weight gain rate from 1 week after the experimental diet, and the weight increase rate up to 4 weeks was lower than that of the control group (see FIG. 4). All experimental data are mean and standard deviation for seven rats.

On the other hand, in addition to the decrease in weight gain rate in the intake experiment up to 4 weeks, no apparent toxic symptoms such as fatality, hair color change and behavioral abnormalities were observed.

Hereinafter, a production example of a functional food containing a diosin or fan horse extract according to the present invention.

The following preparation examples merely exemplify the present invention, and may be prepared by adding dioxins, dioxins derivatives, or fanza extracts according to the present invention in the preparation of conventional foods.

Preparation Example 1 Preparation of Ice Cream

Milkfat 10.0%

Non-fat solids 10.8%

Sugar 12.0%

Starch syrup 3.0%

Emulsifying stabilizer (span) 0.5%

Spices (Strawberries) 0.15%

Water 63.45∼ 63.54%

Diosin 0.01 to 0.1%

Ice cream was prepared using conventional methods with the above composition and content.

Preparation Example 2 Preparation of Beverage

522 mg of honey

Chioctosanamide 5 mg

Nicotinamide 10 mg

Riboflavin Sodium Hydrochloride 3 mg

Pyridoxine hydrochloride 2 mg

Inositol 30 mg

Orthoic acid 50 mg

Diosin 5-50 mg

200 ml of water

The beverage was prepared by the conventional method with the said composition and content.

Production Example 3 Production of Sausage

Pork 63.6%

Chicken 27.5%

Starch 3.5%

Soy Protein 1.7%

Saline 1.62%

Glucose 0.5%

Other additives (glycerine) 1.08 ~ 1.48%

Fancha Extract 0.1-0.5%

Sausages were prepared using conventional methods with the above compositions and contents.

As such, the present invention can provide a functional food having an effect of preventing obesity by preparing various foods (eg, ice cream, beverages, sausages, etc.) containing the fan extract.

Diosin or its derivatives, extracted from cabbage plants, inhibit lipase, an enzyme that breaks down fat, thereby preventing fat from being broken down and absorbed into the body. Therefore, it is also effective in preventing and treating obesity, alleviating the rapid rise of triglycerides in blood, preventing the deposition of cholesterol and adult diseases such as hyperlipidemia, hypertension, diabetes, and cardiovascular diseases. In addition, it is not addictive compared to a drug that is chemically synthesized and sold, and there is no phenomenon of losing weight again even after discontinuation. Moreover, even when a large amount is administered, it does not show any acute toxicity at all, and can be used as an adjuvant to treat various adult diseases while preventing normal obesity while eating a normal meal without a special diet.

Claims (8)

A lipase inhibitor containing diosin represented by the following formula (1) or a derivative thereof as an active ingredient. <Formula 1> The lipase inhibitor of claim 1, wherein the diosin derivative is diosgenin, gracillin, prosapogenin A or prosapogenin C. The lipase inhibitor according to claim 1 or 2, wherein the diosin or derivative thereof is extracted from an asteraceae. 4. The lipase inhibitor according to claim 3, wherein the quince is a fan. Functional food for preventing obesity, comprising diosin or derivatives thereof. 6. The functional food for preventing obesity according to claim 5, wherein the food is confectionary, ice cream, dairy products, meat products, fish products, noodles, beverages, seasonings, margarine, shortening or pizza. Lipase inhibitor containing fanza extract as an active ingredient. Functional food for preventing obesity, comprising diosin or derivatives thereof.