JPH11246399A - Lipid metabolism improving composition - Google Patents

Abstract

(57) [Problem] To provide a composition for improving lipid metabolism which has a triglyceride lowering action and is safe even for a human body. A lipid metabolism-improving composition comprising at least one selected from curcumin and its derivatives as an active ingredient.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for improving lipid metabolism which has a triglyceride lowering action and is safe even for the human body.

[0002]

2. Description of the Related Art Conventionally, an increase in the concentration of lipids represented by triglycerides and cholesterol in blood and organs has been considered as a risk factor for inducing adult diseases such as arteriosclerosis and fatty liver.

[0003] Conventionally, as antilipidemic agents, for example, provastatin, clohibrate, nicomol, dextran sulfate, tocopherol nicotinate and the like are known, but all of them have satisfactory side effects and effects. It is hard to say that it does.

On the other hand, curcumin and its derivatives are turmeric (Curcuma longa), a perennial ginger.
L.) and are included in tropical and subtropical plants. Turmeric has been used as a coloring agent for edible spices, food and clothing, and has been used as a medicinal product especially in the Asian region. Its pharmacological effects include bile secretion promoting action (biliary action), (Liver, pancreas) function enhancement, anti-inflammatory, hemostatic,
Although the stomachic effect is known, the relationship between its medicinal effects and individual medicinal components has not yet been completely elucidated.

On the other hand, Japanese Unexamined Patent Publication No. 7-149628 discloses a ginger family perennial grass, Curcuma (Curcuma).
It is known that α-curcumene (C ₁₅ H ₂₂ ) derived from Xanthorrhiza has a triglyceride lowering effect,
Its chemical structure is clearly different from curcumin (C ₂₁ H ₂₀ O ₆ ). In addition, as the physiological functions of curcumin which have been known so far, reports of cholesterol-lowering action in addition to antioxidant action, carcinogenesis-suppressing action [Intern
at. J. Vit. Nutr. Res., Vol. 61, p364 (1991)], but it is not yet known that curcumin and its derivatives have a triglyceride lowering effect.

[0006]

DISCLOSURE OF THE INVENTION The present invention has been made in view of the above-mentioned conventional situation, and has been made to solve the above problems, and provides a composition for improving lipid metabolism which has a triglyceride lowering action and is safe even for the human body. The purpose is to do.

[0007]

Means for Solving the Problems The present inventors have conducted intensive studies in order to solve the above-mentioned problems and the like. As a result, specific components contained in turmeric plants, which are perennial ginger, are found in the liver. Has the effect of suppressing the accumulation of triglycerides, and has been found to be highly safe for the human body, and succeeded in obtaining the lipid metabolism-improving composition of the above object, and completed the present invention. It is. That is, the composition for improving lipid metabolism of the present invention is characterized by containing at least one selected from curcumin and its derivatives as an active ingredient.

[0008]

Embodiments of the present invention will be described below in detail. The lipid metabolism improving composition of the present invention is characterized by containing at least one selected from curcumin and its derivatives as an active ingredient.

The curcumin used in the present invention is 1,7-bis- (4-hydroxy-3-methoxyphenyl) hepta-1,6-diene-3,5-dione. , Demethoxycurcumin [4-hydroxy-cinnamoyl- (4-hydroxy-
3-methoxy-cinnamoyl) methane] and bisdemethoxycurcumin [bis- (4-hydroxy-cinnamoyl) methane]. These can be used chemically synthesized or derived from any plant. For example, the ginger perennial turmeric (Curcuma long
a L.), curcumin and / or a derivative thereof can be extracted from plants such as mangosh shija, Indian arrow root, gejut, yellow gejut, black gejut, and galangard. In the present invention, at least one selected from curcumin and its derivatives may be a pure compound, but is not limited thereto, and may be semi-purified unless it contains impurities unsuitable as pharmaceuticals and foods. Alternatively, crude curcumin and / or its derivatives can also be used. For example, the crude curcumin extract from the turmeric usually contains 3 curcumin.
7% by weight (hereinafter, simply referred to as “%”), 7% of demethoxycurcumin, 5% of bisdemethoxycurcumin,
This crude curcumin extract may be used, or curcumin or the like purified from this curcumin extract to 100% may be used.

As at least one preparation method selected from curcumin and its derivatives used in the present invention, for example, a conventionally known method can be adopted. For example, turmeric is pulverized to an average particle diameter of 250 to 500 μm, and an extract is obtained by a Soxhlet method or a cooling filtration method using a hydrophilic solvent, specifically, ethanol, acetone, ethylene dichloride, and the like. There are mentioned, for example, a method of purifying the present extract under reduced pressure and using a silica column.

The composition for improving lipid metabolism of the present invention comprises at least one selected from the above-mentioned curcumin and its derivatives as an active ingredient, that is, one (single) or two or more thereof as an active ingredient. Yes, for example, it can be used as pharmaceuticals or foods and drinks (products). When used as a medicament, curcumin and its derivatives may be used in combination with at least one selected from them or, if necessary, with other lipid metabolism-improving agents, by oral administration, intravenous injection, subcutaneous injection, intramuscular injection, or suppository. It can be administered by various methods such as rectal administration. In addition, since the dose can be controlled by the administration route and the number of times, it can be varied widely according to the symptoms. For example, when used as a pharmaceutical, 15 μg to 300 mg / kg body weight per adult per day,
Preferably, the dose is 1 mg to 30 mg / kg body weight.

Further, the lipid metabolism-improving composition of the present invention is prepared by mixing an effective amount of curcumin or the like with an appropriate amount of a non-toxic carrier and formulating the composition for administration using any conventional production method. Can be prepared. When prepared for oral administration, soft capsules, high capsules, tablets, granules, fine granules, powders, active ingredient sustained release agents, solutions, suspensions, etc. It is prepared into injections, drops and suppositories.

In this case, in formulating, non-toxic carriers include, for example, surfactants such as sucrose ester, fatty acid monoglyceride, propylene glycol fatty acid ester, sorbitan fatty acid ester and lecithin, arabic gum, gelatin, sorbit, tragacanth gum and the like. Binders such as polyvinylpyrrolidone, sucrose, lactose, starch, crystalline cellulose, mannitol, light anhydrous silicic acid, magnesium aluminate, magnesium aluminate metasilicate, synthetic aluminum silicate, calcium carbonate, sodium hydrogen carbonate, calcium hydrogen phosphate , Carboxymethylcellulose calcium, excipients, lubricants such as magnesium stearate, talc, hydrogenated oil, salt, saccharin, orange oil, licorice extract, citric acid, glucose, menthol, Li oil, malic acid, flavoring agents and the like,
Flavoring agent, coconut oil, olive oil, sesame oil, peanut oil, soybean oil, medium chain fatty acid triglycerides, safflower oil,
Suspending agents such as soybean phospholipids, wetting agents, cellulose such as cellulose acetate phthalate (CAP), carbohydrate derivatives such as sugars, polyvinyl derivatives such as methyl acrylate / methacrylic acid copolymers and dibasic acid monoesters And other components, such as a film-forming agent and a coating aid, are prepared by a conventional method and used.

[0014] Preparations for mucosal application and injections are also prepared by a conventional method. When a method of suspending or emulsifying in distilled water for injection is employed, a suspending agent is used.
For example, soybean oil, peanut oil, medium-chain fatty acid triglyceride and the like can be used. As the emulsifier, for example, sucrose fatty acid ester, fatty acid monoglyceride, propylene glycol fatty acid ester, sorbitan fatty acid ester, lecithin and the like can be used.

When at least one selected from curcumin and its derivatives as the active ingredient of the present invention is used as a food or drink, the effective amount of curcumin or the like, that is, 15 μg to 300 mg / kg body weight per adult per day, preferably Can be processed and manufactured by a general manufacturing method of food and drink, in addition to a food and drink raw material in an appropriate amount to an effective amount of 1 mg to 30 mg / kg body weight, in particular, a food and drink raw material essentially containing no curcumin. it can. At this time, the type and form of the food are not particularly limited, and for example, it can be prepared into beverages, frozen desserts, jellies, fried noodles, wiener sausages, fish meat sausages, and the like. In particular, curcumin and its derivatives, which are the active ingredients of the present invention, are selected for health foods, functional foods, dietary supplements, foods for specified insurance, etc. having a well-balanced composition of proteins, amino acids, lipids, vitamins, and trace elements. Those containing at least one of them are particularly preferable in terms of prevention and improvement of diseases such as hyperlipidemia, arteriosclerosis, diabetes, fatty liver, and myocardial infarction.

The composition for improving lipid metabolism of the present invention thus constituted has an excellent lipid metabolism improving effect of promoting lipid metabolism by enhancing the activity of a β-oxidation-promoting enzyme of lipids and reducing triglyceride in organs. (This point will be further described in Test Examples and the like). In addition, at least one selected from curcumin and its derivatives contained as an active ingredient is a component contained in turmeric and the like conventionally used as foods or crude drugs, so there is a particular problem in terms of safety. No worries about side effects. Further, the composition for improving lipid metabolism of the present invention can be administered in various ways and can be administered, so that the administration method and dosage can be adjusted. Combination with blood agents is also possible. Therefore, the composition for improving lipid metabolism of the present invention is effective for the prevention and treatment of diseases such as hyperlipidemia, arteriosclerosis, diabetes, fatty liver, and myocardial infarction. And so on.

[0017]

EXAMPLES Hereinafter, the present invention will be described more specifically with reference to Test Examples and Examples, but the present invention is not limited to these Examples. As the curcumin of the test examples and examples, purified products obtained by the following production methods were used. From 100 g of turmeric powder crushed to about 40 mesh, 4 g of a crude extract was obtained by Soxhlet extraction using acetone. The crude extract was subjected to silica column chromatography using an acetone-ethanol gradient to obtain 2.8 g of a purified product.

[Test Example 1] An 8-week-old male ddY mouse was acclimated to a normal diet (F-2, manufactured by Funabashi Farm) for 1 week,
A synthetic feed (AIN-76) containing 15% soybean oil was used as a basic feed, and a non-added group (control group), a 1% curcumin added group (inventive group), and a 1% red pepper hexane extract added group (comparative group 1). A group in which 1% rosemary hexane extract was administered (Comparative Group 2) was bred for 18 weeks in a freely ingestible dosage form with 18 animals per group. After 24 hours of fasting, the animals were sacrificed by cervical dislocation and the liver was removed, lipids were extracted according to the method of Folch et al., And the amount of triglyceride in the liver was measured using a commercially available analysis kit. The results are shown in Table 1 below.

[0019]

[Table 1]

(Consideration of Table 1) As is clear from Table 1 above, the invention group containing 1% curcumin, which falls within the scope of the present invention, suppresses the accumulation of triglide in the liver of mice,
The effect was found to be significantly higher than the spice extracts of the other comparative groups 1 and 2.

Test Example 2 An 8-week-old SD male rat was acclimated to a normal diet (F-2, manufactured by Funabashi Farm) for 1 week, and
A synthetic feed (AIN-93G) containing 5% soybean oil was used as a basic feed, and a non-addition group (control group), a 0.2% curcumin addition group (invention group 1), and a 1% curcumin addition group (invention group 2). Six groups were bred for 2 weeks in a freely ingestible dosage form. After 24 hours of fasting, the animals were sacrificed by cervical dislocation and the liver was removed, and the amount of triglyceride in the liver was measured as in Test Example 1. At the same time, the fatty acid synthase activity was measured by the amount of oxidized NADPH after the addition of the substrate (NADPH-oxd), and the amount of hydrogen peroxide generated after the addition of the substrate was determined by the acyl-CoA oxidase activity as a β-oxidation-promoting enzyme. Dichlorofluoroescein (LDCF-oxd)
Was measured by converting with the amount of color development. The results are shown in Table 2 below.

[0022]

[Table 2]

(Consideration of Table 2) As is clear from Table 2 above, those containing 0.2% and 1% of curcumin of Invention Groups 1 and 2, which are within the scope of the present invention, had higher fatty acids than the control group. While there was no significant change in synthase activity, β
-The effect of enhancing the activity of acyl-CoA oxidase, which is a pro-oxidant enzyme, and the effect of inhibiting triglyceride accumulation in rat liver were observed, and these effects were dependent on the concentration of curcumin added.

Examples 1 to 12 Injectables, suppositories, soft capsules, cookies, dressings, food additives (curcumin preparations) are described below as the lipid metabolism-improving composition containing curcumin used as an active ingredient in the present invention. , Beverage syrup, ice cream, jelly candy,
Examples include sea bream crackers, fried noodles, and wiener sausages.

Example 1 Preparation of Injection Curcumin 100 g Stearic acid monoglyceride 100 g Peanut oil 200 g Sucrose glycerin stearate ester 50 g Ascorbic acid stearate 20 g Distilled water for injection 9530 g 1 ampoule 10
ml.

[Example 2: Preparation of suppository] Methyl salicylate 0.0350 g Famazole T-115 (trade name, manufactured by Nissan Chemical Co., Ltd.) 2.0000 g Curcumin 0.0100 g A suppository having the above composition was prepared by a conventional method.

[Example 3: Preparation of soft capsules] Curcumin 10 g Corn oil 25 g Extracted tocopherol 1 g Ascorbic acid palmitate 5 g Gelatin 52 g Fifty soft capsules having the above composition were prepared by a conventional method.

Example 4: Preparation of Cookies Curcumin 0.1 g Soybean salad oil 263 g Sugar 225 g Egg 63 g Milk 20 g Milk flour 425 g Salt 2 g The above composition was used to prepare cookies by a conventional method.

[Example 5: Preparation of dressing] Rapeseed salad oil 65.5 g Vinegar 25 g Salt 0.6 g Sodium glutamate 0.4 g Pepper 0.1 g Pear 0.1 g Curcumin 0.1 g Onion juice 2.5 g Lemon juice 3 8 g A dressing was prepared with the above composition by a conventional method.

Example 6: Preparation of food additive (curcumin preparation) Curcumin 20 g Glycerin fatty acid ester 7 g Medium-chain fatty acid triglyceride 1.5 g Sorbitol 45 g Arabic gum 0.7 g Ethanol 6.5 g Water 19.3 g Curcumin preparation was prepared by the method.

[Example 7: Preparation of syrup for beverage] Apple juice 3 kg Fructose-glucose liquid sugar (75%) 30 kg Citric acid 0.2 kg DL-malic acid 0.05 kg Curcumin preparation (Example 6) 0.2 kg Water 16 .55 kg A syrup for beverage was prepared by the usual method with the above composition.

Example 8: Preparation of ice cream Whole fat-sweetened condensed milk 12.25 kg unsalted butter 7.5 kg fresh cream 3 kg skim milk powder 5.5 kg sugar 4 kg starch syrup 12.5 kg salt 0.05 kg stabilizer 0.3 kg emulsifier 0.35 kg banana essence 0.15 kg curcumin preparation (Example 6) 0.1 kg water 54.3 kg Ice cream was prepared by the usual method with the above composition.

[Example 9: Preparation of jelly candy] Agar powder 3 kg Granulated sugar 32 kg Water syrup 50 kg Water 1000 kg Orange essence 0.15 kg Citric acid 0.5 kg Curcumin preparation (Example 6) 0.1 kg Jelly with the above composition by a conventional method A candy was prepared.

[Example 10: Preparation of sea bream rice cracker] Sea bream surimi 300g shrimp surimi 60g salt 12g white sugar 15g sodium glutamate 10g starch 600g curcumin preparation (Example 6) 3g A sea bream cracker was prepared by the usual method using the above composition.

Example 11: Preparation of fried noodles Semi-strong flour 100 kg Salt 0.5 kg Brackish water 0.5 kg Curcumin preparation (Example 6) 0.3 kg Water 30 kg Fried noodles were prepared according to a conventional method with the above composition.

Example 12: Preparation of Wiener Sausage Pork 540 g Tallow 160 g Ice water 300 g Phosphate 3 g Salt 16 g Sodium nitrite 0.05 g L-ascorbate 0.4 g Sodium glutamate 2 g Starch 40 g Curcumin preparation (Example) 6) 0.5 g Wiener sausage was prepared by the usual method with the above composition.

[0037]

According to the present invention, there is provided a composition for improving lipid metabolism which has an excellent triglyceride lowering action and is safe for the human body.

Claims (1)

[Claims] 1. A lipid metabolism improving composition comprising as an active ingredient at least one selected from curcumin and its derivatives.