WO2007111306A1 - Lipid metabolism ameliorating agent - Google Patents
Lipid metabolism ameliorating agent Download PDFInfo
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- WO2007111306A1 WO2007111306A1 PCT/JP2007/056226 JP2007056226W WO2007111306A1 WO 2007111306 A1 WO2007111306 A1 WO 2007111306A1 JP 2007056226 W JP2007056226 W JP 2007056226W WO 2007111306 A1 WO2007111306 A1 WO 2007111306A1
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- food
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- disease
- lipid metabolism
- lipid
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- 206010033675 panniculitis Diseases 0.000 description 1
- 210000002824 peroxisome Anatomy 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- VWBQYTRBTXKKOG-IYNICTALSA-M pravastatin sodium Chemical compound [Na+].C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC([O-])=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 VWBQYTRBTXKKOG-IYNICTALSA-M 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000000574 retroperitoneal space Anatomy 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 150000004671 saturated fatty acids Chemical class 0.000 description 1
- 235000003441 saturated fatty acids Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 235000021127 solid diet Nutrition 0.000 description 1
- 235000021055 solid food Nutrition 0.000 description 1
- 235000013555 soy sauce Nutrition 0.000 description 1
- 210000000952 spleen Anatomy 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 210000004003 subcutaneous fat Anatomy 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000007910 systemic administration Methods 0.000 description 1
- 235000019640 taste Nutrition 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 235000004835 α-tocopherol Nutrition 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/42—Cucurbitaceae (Cucumber family)
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the present invention relates to cut chlor, which is a plant of the Cucurbitaceae family. More specifically, the present invention relates to a new function of kicrol as a lipid metabolism improving agent. The present invention is useful in the field of food and pharmaceutical products.
- Non-patent Documents 1 and 2 are traditionally used as a medicinal plant for treatment of diabetes in South Asia. Recent studies have reported that serum and liver TGs are reduced to prevent fatty liver (Non-patent Documents 1 and 2). Furthermore, although the mechanism of action is not yet elucidated, an action to improve diabetes has been recognized (Non-patent Document 3, Patent Document 1). Thus, Nigauri is a useful vegetable that has been recognized for its various high functions such as diabetes and improvement of hyperlipidemia.
- Kakrol Momordica dioica Roxb.
- Kakrol Momordica dioica Roxb.
- Nigauri a vegetable that is harvested in the rainy season around Bangladesh. It belongs to the cucurbitaceae like Nigauri and has a shape similar to Nigauri, but it is not as bitter as Nigauri.
- katschlor research has been conducted on surface strength such as cultivation method, parthenocarpy, plant regeneration from tissue culture callus, and morphological characteristics (non-patent documents 4 to 7).
- Katstrol is known to have a high vitamin content.
- Patent Document 1 JP-A-11-59692 (Patent No. 3261090)
- Non-Patent Document 1 Gamarallage V. K. Senanayake, et al., J. Nutr. Sci. VitaminoL, 50 253 -257, 2004
- Non-Patent Document 2 Gamarallage V. K. Senanayake, et al., J. Ethnoparmacology, 91 257-2 62, 2004
- Non-Patent Document 3 Dhanasekar S., et al., Biol. Pharm. Bull., 28 (6) 978-983, 2005
- Non-Patent Document 4 Mohammad Ali, et al., Scientia Horticulturae, 47 335-343, 1991
- Non-Patent Document 5 Mohammad Nazmul Islam Mnik, et al., J. Fac. Agr., Kyushu Univ., 45 (2) 459-463, 2001
- Non-Patent Document 6 Shaila Arifa Nabi, et al "J. Fac. Agr., Kyushu Univ., 46 (2) 303-309, 2 002
- Non-Patent Document 7 Mohammad Golam Rasul, et al., J. Fac. Agr., Kyushu Univ., 49 (1) 1-11, 2004
- the present inventors examined the effect of a diet containing 3% katstrol powder on fat metabolism in SD rats. As a result, it was confirmed that the group fed with katstrol showed a significant improvement in the index related to lipid metabolism and the amount of fatty acid excreted in feces was significantly higher than the control group. Discovered and completed the present invention.
- the present invention provides a food or pharmaceutical composition comprising a cutlet knollole and a food or pharmaceutically acceptable additive.
- Katakrol (scientific name: Momordica dioica Roxb.) Is a plant belonging to the genus Morordica belonging to the same family as Nigauri.
- Katsura is a perennial perennial and sexually different strain that forms tuberous roots in the underground (see Figures 1-4). It is said to be native to the Bengal region of the Indian subcontinent, suitable for hot and humid climates, and easy to grow.
- Bandaradesh it is an important vegetable during the rainy season. The fruit is lemon-shaped, covered with small protrusions, and each piece weighs 50 to 100 g, and has no bitterness like that of two gourds.
- katschlor When katschlor is used in the food or pharmaceutical composition of the present invention, any variety can be used regardless of the cultivation method, morphological characteristics and physiological characteristics.
- cultivation method and morphological 'physiological characteristics of katstrol those skilled in the art can refer to the above-mentioned Non-Patent Documents 4 to 7 and the like.
- cut crawl refers to the whole or a part of the cut crawl plant, except in special cases, and includes the cut crawl fruit (at a stage suitable for eating).
- Fruits fruits and vegetables are sometimes referred to as “cut crawls”.
- Pulp skin, seeds, leaves, stems, roots, flowers, buds.
- Fruit is suitable as a raw material for the food or pharmaceutical composition of the present invention. Fruit In fact, it may be used as it is without removing the skin and seeds. At the fruit stage (fruit and vegetables) suitable for eating katstrol, the seeds can still be eaten with soft flesh. If necessary, pulp, skin or seed may be used alone or in combination.
- cut crawl refers to an extract, extract residue, fractionated product, or isolated from kat crawl as a raw material, regardless of whether or not it is processed, unless otherwise specified. Products, concentrates, additives, and dried products.
- the dried product includes a freeze-dried powder.
- the extract includes an extract with water or an aqueous solvent, and an extract with an organic solvent such as methanol, ethanol, hexane, or acetone.
- fruits and vegetables can be used as a dried product.
- the food or pharmaceutical composition of the present invention is useful for treating a disease or condition associated with lipid metabolism. More particularly, it is useful for treating diseases or conditions associated with serum lipid levels or liver lipid levels.
- Serum lipids and liver lipids include cholesterol (free and ester), triacinoleglycerol (TG) (triglycerides, triglycerides, and sometimes phospholipids (PL), non-esters.
- Type fatty acids include cholesterol (free and ester), triacinoleglycerol (TG) (triglycerides, triglycerides, and sometimes phospholipids (PL), non-esters.
- Type fatty acids The food or pharmaceutical composition of the present invention is particularly effective in reducing serum total cholesterol concentration, liver cholesterol concentration, triacylglycerol (TG) concentration, and / or phospholipid (PL) concentration. is there.
- the food or pharmaceutical composition of the present invention includes hyperlipidemia (primary (familial, sporadic) and secondary.
- Hypercholesterolemia hypertriglyceridemia, high Including cholesterol hypertriglyceridemia
- arteriosclerosis ischemic heart disease (angina, myocardial infarction)
- cerebrovascular disorder Cerebral infarction, cerebral hemorrhage
- fatty liver diabetes, obesity, lifestyle-related disease (sugar (Urine disease, stroke, heart disease, hyperlipidemia, hypertension, obesity).
- the pharmaceutical or food composition of the present invention is suitable for diseases or conditions related to oxidative stress (eg, arteriosclerosis). ) Is considered particularly useful.
- the dietary efficiency, liver weight, and spleen weight were determined for the group ingested dried chopped fruits and vegetables.
- the experimental results showed that serum amylase activity was higher than that of the control group (see Example 3).
- a high dietary efficiency means that energy metabolism has been made more efficient, and an increase in liver weight suggests the possibility of hypermetabolism not in fatty liver.
- the increase in visceral weight has the potential to efficiently perform blood glucose regulating actions such as digestive enzymes, insulin, and glucagon, and serum amylase increases as the visceral weight increases. It means the vigorous activity of Katsu. Therefore, the food or pharmaceutical composition of the present invention is also useful for the treatment of diseases or conditions that are ameliorated by the action of such katschlor.
- the pharmaceutical or food composition of the present invention has an action of inhibiting the absorption of diet-derived lipids, and is also useful for the treatment of diseases or conditions ameliorated by the action of such katstrol.
- lipid refers to simple lipids (for example, fats and oils; fats and oils are trivalent esters that also have fatty acid and glycerin power) unless otherwise specified.
- Triglycerides TG
- les sometimes
- complex lipids eg phospholipids, glycolipids
- Simple fats and complex lipids contain unsaturated fatty acids or saturated fatty acids as constituents. Inhibition of lipid absorption is usually assessed by measuring the amount of fatty acids excreted or absorbed. That power S.
- Treatment includes fundamental therapy and includes long-term prevention and / or therapy.
- the food composition of the present invention includes those in the form of beverages.
- the food composition of the present invention can be a nutritional functional food, a food for specified health use, a health food, a dietary supplement, a drink, a juice, a concentrated juice, or the like.
- the food composition may also be in the form of dried products, processed products (eg pickles, salted pickles, soy sauce pickles, miso pickles, nuka miso pickles, pickled pickles, pickled pickles, seasoned pickles, pickles), extracts.
- the pharmaceutical composition described below it can be in the form of capsules, tablets, pills, tablets, powders, granules, etc. containing extracts and concentrates.
- the amount of katchlor taken as a food composition can be appropriately determined according to the pharmaceutical composition described below.
- the food composition of the present invention includes various food-acceptable additives such as sweeteners, colorants, preservatives, antioxidants, flavors, acidulants, seasonings, fungicides (anti-bacterial agents). Agent), pH adjuster, nutrient enhancer, emulsifier, thickener, stabilizer, gelling agent, glue, color former, bleaching agent.
- various food-acceptable additives such as sweeteners, colorants, preservatives, antioxidants, flavors, acidulants, seasonings, fungicides (anti-bacterial agents).
- Agent pH adjuster, nutrient enhancer, emulsifier, thickener, stabilizer, gelling agent, glue, color former, bleaching agent.
- the amount, duration, and interval of katstrol as an active ingredient should be appropriately determined according to the purpose, symptoms, subject's age, weight, etc. You can.
- a clinically effective amount can be administered continuously for weeks to months. More specifically, an amount equivalent to 10 g to 1000 g (preferably 25 g to 500 g, more preferably 50 g to 250 g) as a dried product of fruits and vegetables per day is given to an adult patient once a day. Or it can be divided into multiple doses (eg, 3 times).
- a formulation designed to contain such amounts of 1/10 to 1/1 (eg 1/3) in a unit dosage form is one of the preferred embodiments of the present invention.
- administering in a smaller amount or amount may be effective. More specifically, for adult subjects, lg to 100 g (preferably 2.5 g to 50 g, more preferably 5 g to An amount corresponding to 25 g) can be administered in single or divided doses. Formulations designed to contain such amounts of 1/10 to 1/1 in one unit dosage form are also a preferred embodiment of the present invention.
- the amount corresponding to the dried product of fruits and vegetables can be determined by those skilled in the art with reference to the examples and the like of the present specification, whole fruits and vegetables, extracts of fruits and vegetables, residue of extracts, fractions, and isolation. Products, concentrates or processed products, or part of fruits and vegetables (for example, pulp, skin, seeds), dried products, extracts, extract residues, fractions, isolates, concentrates or processed products, etc. Each can be determined.
- the administration route and dosage form can also be designed as appropriate, for example, it can be formulated for systemic administration or for local administration, and is used as an internal preparation, external preparation, solid preparation, liquid preparation. , Powders, granules, capsules, tablets, pills, tablets, extracts, ointments, plasters, haps, lotions, liniments, or suppositories. Further, it can be a sustained release preparation or a controlled release preparation. Formulation can be performed according to conventional methods.
- the pharmaceutical composition of the present invention comprises various pharmaceutically acceptable additives such as excipients, binders, disintegrants, lubricants, coating agents, suspending agents, emulsifiers, stabilizers, storages.
- An agent or buffer may be included.
- the food or pharmaceutical composition of the present invention may be used in other dietary therapies (fat restriction, carbohydrate'alcohol restriction, high intake of dietary fiber, etc.), drug therapy (cholestyramine, nicotinic acid, mevalotin, etc.) Anti-cholesterol medication)), can be used in combination with exercise therapy.
- dietary therapies fat restriction, carbohydrate'alcohol restriction, high intake of dietary fiber, etc.
- drug therapy cholestyramine, nicotinic acid, mevalotin, etc.
- Anti-cholesterol medication Anti-cholesterol medication
- composition of the present invention has a specific use (for example, prevention of lifestyle-related diseases, improvement of constitution, long-term treatment, etc.) and / or specific use thereof. (E.g., amount, number of times, continuous use, period, etc.) can be displayed.
- the present invention also relates to a method for treating a disease or condition related to lipid metabolism in a human or non-human animal, which improves lipid metabolism by ingesting katchlor, an agent for improving lipid metabolism, including katchlor, And products that include guidelines for using katstrol to improve lipid metabolism (eg, specific uses and information about Z or its specific use, a document containing such information) . Also provided are a method for inhibiting lipid absorption, which comprises ingesting bonito crepes, and a lipid absorption inhibitor comprising katschlor. Brief Description of Drawings [0028] [Fig. 1] Fig. 1 is a photograph of the entire cut crawl.
- FIG. 2 is a photograph of cutlet fruits.
- FIG. 3 is a photograph of cutlet fruits.
- FIG. 4 is a photograph of Katsukuro tuberous root.
- Cut and chopped fruits and vegetables were cut into 3 cm squares, freeze-dried, and ground with a mixer. From 1004 g of fruits and vegetables, 131.3 g of pale green powder was obtained. The obtained dried product resembled the taste of cucumber without bitterness and had a blue odor. This was used in the following examples.
- Vitamin mixture (AIN-76) 10 10
- liver, knee, white adipose tissue (around testes, mesentery, retroperitoneal cavity) and muscle were removed.
- Liver lipids are chemical (cholesterol: Spe rry S., J. Biol. Chem., 187, 97-106, 1950, Triglyceride: Fletcher S "Clin. Chim. Act a.
- Serum gnolecose was measured using an enzyme method kit (glucose C-II-Test Koichi, Wako Pure Chemical Industries, Ltd.) Serum amylase concentration was measured using a kit (Amylase test Koichi, Wako Pure Chemical Industries, Ltd.) In addition, the enzyme activity of the fatty acid synthesis system (fatty acid oxidation system) of the liver was measured.
- One unit is defined as an activity that l OOmL serum
- Glucose level (mg / dL) 149.4 ⁇ 4,6 147.3 ⁇ 1.0
- Values are means SE (n; 6)
- Liver (mg / g Liver)
- the total cholesterol concentration and HDL-cholesterol concentration in serum were significantly decreased in the Kakrol group compared to the Control group. Since the decrease in HDL-cholesterol concentration is small compared to the decrease in total cholesterol concentration, LDL-cholesterol + VLDL-cholesterol is considered to have decreased.
- the cholesterol concentration, triacylglycerol (TG) concentration and phospholipid (PL) concentration in the liver were significantly decreased in the Kakrol group as compared to the Control group. There was no significant difference between the groups in serum TG concentration and serum gnolecose concentration.
- Kakrol has an effect of lowering serum cholesterol concentration and contains substances that show an action of lowering liver lipids.
- the ability of food ingredients to have the same effect is the ability of soy protein.
- the percentage of soy protein in the diet is 20%.
- mice SD rats or apo E-deficient mice were ingested with katschlor freeze-dried powder, and the effects of katschlor on lipid metabolism and its mechanism of action were investigated.
- control food containing 10% lard (Control group, 8 males and females) and A katsukuro diet (Kakrol group, 6 males, 7 females) containing 10% lard and 3% katsukuro freeze-dried powder was bred for 9 weeks by Pair feeding.
- the diet composition is shown in the table below.
- Vitamin mixture (AIN-76) 10 10
- the diets are formulated according to the AIN-76 formula.
- liver, heart, white adipose tissue testicles around the nest, around the mesentery, retroperitoneal space * around the kidney, subcutaneous
- aorta aorta
- Liver lipids were measured by chemical methods, and serum lipids were measured using an enzymatic method kit (see Example 3).
- Serum thiobarbituric acid reactant (TBARS) in serum was measured by a chemical method.
- Total fat weight, mesentery and subcutaneous adipose tissue weight were significantly lower in the Kakrol group than in the Control group. There was no significant difference between the groups in the weight of adipose tissue around the retroperitoneal cavity, around the kidney, and around the testicle / ovary.
- Serum TBARS concentrations were significantly lower in the Kakrol group compared to the Control group. It was suggested that the effect of Katstrol on lowering liver lipid and serum cholesterol levels was due to suppression of TG absorption. Therefore, in the future, in order to clarify the mechanism of inhibition of lipid absorption by katschlor, the effect on lipid transport in small intestinal absorptive cells will be examined. In addition, we plan to make aortic sections of apo E-deficient mice reared this time and evaluate the effect of katchlor on the progression of arteriosclerosis.
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Abstract
Disclosed is a food or pharmaceutical composition comprising kakrol (Momordica dioica Roxb.). Kakrol, which is a vegetable originally produced in Bangladesh, resembles balsam pear. The food or pharmaceutical composition is useful for the treatment of a disease or condition associated with lipid metabolism, hyperlipemia (including primary (familial, sporadic) and secondary hyperlipemia, hypercholesterolemia and hyper(LDL)cholesteremia), arteriosclerosis, ischemic heart disease (including angina pectoris and cardiac infarction), cerebrovascular disease (including cerebral infarction and cerebral hemorrhage) or lifestyle-related disease. The food or pharmaceutical composition can prevent the absorption of a lipid.
Description
明 細 書 Specification
脂質代謝改善剤 Lipid metabolism improver
技術分野 Technical field
[0001] 本発明は、ゥリ科の植物であるカツクロールに関する。より詳細には、本発明は、力 ックロールの脂質代謝改善剤としての新たな機能に関する。本発明は食品及び医薬 品の分野で有用である。 [0001] The present invention relates to cut chlor, which is a plant of the Cucurbitaceae family. More specifically, the present invention relates to a new function of kicrol as a lipid metabolism improving agent. The present invention is useful in the field of food and pharmaceutical products.
背景技術 Background art
[0002] 二ガウリの果肉や種子は南アジアにおいて、伝統的に薬効のある植物として糖尿病 治療に利用されている。近年の研究により、血清及び肝臓中の TGを減少させ、脂肪 肝を予防する作用があるという報告がある (非特許文献 1、 2)。さらに、作用機構は未 解明であるが、糖尿病改善作用が認められてきている（非特許文献 3、特許文献 1)。 このように、二ガウリは糖尿病や高脂血症の改善など、様々な高機能性が認められて レ、る有用な野菜である。 [0002] Nigauri pulp and seeds are traditionally used as a medicinal plant for treatment of diabetes in South Asia. Recent studies have reported that serum and liver TGs are reduced to prevent fatty liver (Non-patent Documents 1 and 2). Furthermore, although the mechanism of action is not yet elucidated, an action to improve diabetes has been recognized (Non-patent Document 3, Patent Document 1). Thus, Nigauri is a useful vegetable that has been recognized for its various high functions such as diabetes and improvement of hyperlipidemia.
[0003] 一方、カツクロール（Kakrol、 Momordica dioica Roxb.)は、バングラデイシュ周辺で 雨季に収穫される野菜である。二ガウリと同様ゥリ科に属し、二ガウリに類似した形を しているが、二ガウリほどには苦味がない。カツクロールについては、これまで、栽培 法、単為結実、組織培養カルスからの植物体再生、及び形態学上'生理学上の特徴 等の面力 研究されてきた (非特許文献 4〜7)。 [0003] On the other hand, Kakrol (Momordica dioica Roxb.) Is a vegetable that is harvested in the rainy season around Bangladesh. It belongs to the cucurbitaceae like Nigauri and has a shape similar to Nigauri, but it is not as bitter as Nigauri. Regarding katschlor, research has been conducted on surface strength such as cultivation method, parthenocarpy, plant regeneration from tissue culture callus, and morphological characteristics (non-patent documents 4 to 7).
[0004] さらにカツクロールはビタミン高含有であることが知られている力 多くの機能性につ いて検討の余地がある。 [0004] Furthermore, Katstrol is known to have a high vitamin content.
特許文献 1 :特開平 11-59692 (特許第 3261090号） Patent Document 1: JP-A-11-59692 (Patent No. 3261090)
非特許文献 1： Gamarallage V. K. Senanayake, et al., J. Nutr. Sci. VitaminoL, 50 253 -257, 2004 Non-Patent Document 1: Gamarallage V. K. Senanayake, et al., J. Nutr. Sci. VitaminoL, 50 253 -257, 2004
非特許文献 2 : Gamarallage V. K. Senanayake, et al., J. Ethnoparmacology,91 257-2 62， 2004 Non-Patent Document 2: Gamarallage V. K. Senanayake, et al., J. Ethnoparmacology, 91 257-2 62, 2004
非特許文献 3 : Dhanasekar S.， et al., Biol. Pharm. Bull., 28(6) 978-983， 2005 非特許文献 4 : Mohammad Ali, et al., Scientia Horticulturae, 47 335-343， 1991
非特許文献 5 : Mohammad Nazmul Islam Mnik, et al., J. Fac. Agr., Kyushu Univ., 45 (2) 459-463, 2001 Non-Patent Document 3: Dhanasekar S., et al., Biol. Pharm. Bull., 28 (6) 978-983, 2005 Non-Patent Document 4: Mohammad Ali, et al., Scientia Horticulturae, 47 335-343, 1991 Non-Patent Document 5: Mohammad Nazmul Islam Mnik, et al., J. Fac. Agr., Kyushu Univ., 45 (2) 459-463, 2001
非特許文献 6 : Shaila Arifa Nabi, et al" J. Fac. Agr., Kyushu Univ., 46(2) 303-309， 2 002 Non-Patent Document 6: Shaila Arifa Nabi, et al "J. Fac. Agr., Kyushu Univ., 46 (2) 303-309, 2 002
非特許文献 7 : Mohammad Golam Rasul, et al. , J. Fac. Agr., Kyushu Univ., 49(1) 1- 11， 2004 Non-Patent Document 7: Mohammad Golam Rasul, et al., J. Fac. Agr., Kyushu Univ., 49 (1) 1-11, 2004
発明の開示 Disclosure of the invention
[0005] 本発明者らは、 SDラットにおいて、カツクロール粉末を 3%含む食餌を与えた際の脂 質代謝に及ぼす影響について検討した。その結果、カツクロールを含む食事を与え た群が、コントロール群に比較して、脂質代謝に関連した指標において有意な改善 が見られること、また糞中への脂肪酸排泄量が有意に高いことを発見し、本発明を完 成した。 [0005] The present inventors examined the effect of a diet containing 3% katstrol powder on fat metabolism in SD rats. As a result, it was confirmed that the group fed with katstrol showed a significant improvement in the index related to lipid metabolism and the amount of fatty acid excreted in feces was significantly higher than the control group. Discovered and completed the present invention.
[0006] 本発明は、すなわち、カツクローノレ、及び食品又は医薬として許容可能な添加物を 含む、食品又は医薬組成物を提供する。 [0006] The present invention provides a food or pharmaceutical composition comprising a cutlet knollole and a food or pharmaceutically acceptable additive.
[0007] カツクロール（kakrol、学名： Momordica dioica Roxb.)は、二ガウリと同じゥリ科モモ ルディカ属の植物である。カツクロールは、蔓性多年草、雌雄異株であり、地下部に 塊根を作る（図 1〜4参照）。インド亜大陸ベンガル地方原産といわれており、高温多 湿気候に適し、栽培は容易である。バンダラデシュ国では雨季の重要な野菜となって いる。果実はレモン型で、小突起に覆われ、 1個の重さは 50〜100gであり、二ガウリの ような苦みを全く持たない。 [0007] Katakrol (scientific name: Momordica dioica Roxb.) Is a plant belonging to the genus Morordica belonging to the same family as Nigauri. Katsura is a perennial perennial and sexually different strain that forms tuberous roots in the underground (see Figures 1-4). It is said to be native to the Bengal region of the Indian subcontinent, suitable for hot and humid climates, and easy to grow. In Bandaradesh, it is an important vegetable during the rainy season. The fruit is lemon-shaped, covered with small protrusions, and each piece weighs 50 to 100 g, and has no bitterness like that of two gourds.
[0008] 本発明の食品又は医薬組成物に、カツクロールを用レ、る場合、栽培法、形態学上' 生理学上の特徴によらず、あらゆる品種を用いることができる。カツクロールの栽培法 及び形態学上'生理学上の特徴に関しては、当業者は、上述の非特許文献 4〜7等 を参照、すること力 Sできる。 [0008] When katschlor is used in the food or pharmaceutical composition of the present invention, any variety can be used regardless of the cultivation method, morphological characteristics and physiological characteristics. As for the cultivation method and morphological 'physiological characteristics of katstrol, those skilled in the art can refer to the above-mentioned Non-Patent Documents 4 to 7 and the like.
[0009] 本明細書で「カツクロール」というときは、特別な場合を除き、カツクロールの植物体 の全体又は一部を指し、これには、カツクロール果実 (食するのに適した段階の果実 (青果）を指して「カツクロール」とレ、うこともある。）、果肉、皮、種子、葉、茎、根、花、 蕾が含まれる。本発明の食品又は医薬組成物の原料として、果実が適している。果
実は、果皮及び種子を除くことなぐそのまま用いてもよい。カツクロールの食するの に適した果実の段階 (青果）では種子はまだ柔らかぐ果肉とともに食することができ る。必要に応じ、果肉、皮若しくは種子を、単独又は組み合わせて用いてもよい。 [0009] In this specification, the term "cut crawl" refers to the whole or a part of the cut crawl plant, except in special cases, and includes the cut crawl fruit (at a stage suitable for eating). Fruits (fruits and vegetables) are sometimes referred to as “cut crawls”.), Pulp, skin, seeds, leaves, stems, roots, flowers, buds. Fruit is suitable as a raw material for the food or pharmaceutical composition of the present invention. Fruit In fact, it may be used as it is without removing the skin and seeds. At the fruit stage (fruit and vegetables) suitable for eating katstrol, the seeds can still be eaten with soft flesh. If necessary, pulp, skin or seed may be used alone or in combination.
[0010] 本明細書で「カツクロール」というときは、特別な場合を除き、加工の有無、程度を問 わず、カツクロールを原料とした抽出物、抽出物残滓、分画物、単離物、濃縮物、加 ェ物、乾燥物を含む。 [0010] In the present specification, the term "cut crawl" refers to an extract, extract residue, fractionated product, or isolated from kat crawl as a raw material, regardless of whether or not it is processed, unless otherwise specified. Products, concentrates, additives, and dried products.
[0011] 乾燥物には、凍結乾燥物の粉末が含まれる。抽出物には、水又は水系溶媒による 抽出物、メタノーノレ、エタノール、へキサン、アセトン等の有機溶媒による抽出物が含 まれる。 [0011] The dried product includes a freeze-dried powder. The extract includes an extract with water or an aqueous solvent, and an extract with an organic solvent such as methanol, ethanol, hexane, or acetone.
[0012] 本発明の食品又は医薬組成物には、青果を乾燥物にして用いることができる。 [0012] In the food or pharmaceutical composition of the present invention, fruits and vegetables can be used as a dried product.
[0013] 本発明の食品又は医薬組成物は、脂質代謝に関連した疾患又は状態を処置する ために有用である。より特定すると、血清脂質濃度又は肝臓脂質濃度に関連した疾 患又は状態を処置するために有用である。血清脂質及び肝臓脂質には、コレステロ ール (遊離型、エステル型）、トリアシノレグリセロール (TG) (トリグリセリド、中性脂肪と レ、うこともある。）、リン脂質 (PL)、非エステル型脂肪酸が含まれる。本発明の食品又 は医薬組成物は、特に、血清中の総コレステロール濃度、肝臓中のコレステロール 濃度、トリァシルグリセロール (TG)濃度、及び/又はリン脂質 (PL)濃度を低減させる のに効果がある。本発明の食品又は医薬組成物は、より具体的には、高脂血症 (原 発性 (家族性、散発性）、二次性を含む。高コレステロール血症、高中性脂肪血症、 高コレステロール高中性脂肪血症を含む。）、動脈硬化、虚血性心疾患 (狭心症、心 筋梗塞)、脳血管障害 (脳梗塞、脳出血)、脂肪肝、糖尿病、肥満、生活習慣病 (糖 尿病、脳卒中、心臓病、高脂血症、高血圧、肥満）を処置するために有用である。な お、本発明者らの検討によると、 9〜18週齢の雌雄アポ E欠損マウスでの評価におい ては、カツクロール青果の乾燥物を摂取した群力 血清中の血清中のチォバルビッ ール酸反応物（TBARS)濃度がコントロール群と比較して低くなつた（実施例 4参照）こ とから、本発明の医薬又は食品組成物は、酸化ストレスに関連した疾患又は状態（例 えば動脈硬化）を処置するために、特に有用であると考えられる。 [0013] The food or pharmaceutical composition of the present invention is useful for treating a disease or condition associated with lipid metabolism. More particularly, it is useful for treating diseases or conditions associated with serum lipid levels or liver lipid levels. Serum lipids and liver lipids include cholesterol (free and ester), triacinoleglycerol (TG) (triglycerides, triglycerides, and sometimes phospholipids (PL), non-esters. Type fatty acids. The food or pharmaceutical composition of the present invention is particularly effective in reducing serum total cholesterol concentration, liver cholesterol concentration, triacylglycerol (TG) concentration, and / or phospholipid (PL) concentration. is there. More specifically, the food or pharmaceutical composition of the present invention includes hyperlipidemia (primary (familial, sporadic) and secondary. Hypercholesterolemia, hypertriglyceridemia, high Including cholesterol hypertriglyceridemia), arteriosclerosis, ischemic heart disease (angina, myocardial infarction), cerebrovascular disorder (cerebral infarction, cerebral hemorrhage), fatty liver, diabetes, obesity, lifestyle-related disease (sugar (Urine disease, stroke, heart disease, hyperlipidemia, hypertension, obesity). According to the study by the present inventors, in the evaluation in 9-18 week-old male and female apo E-deficient mice, the group strength that ingested dry matter of katsukuru fruits and vegetables Serum thiobarbiel in serum Since the acid reactant (TBARS) concentration was lower than that in the control group (see Example 4), the pharmaceutical or food composition of the present invention is suitable for diseases or conditions related to oxidative stress (eg, arteriosclerosis). ) Is considered particularly useful.
[0014] 本発明者らの検討によると、 5週齢の雄 SDラットでの評価においては、カツクローノレ
青果の乾燥物を摂取した群は、血清中の総コレステロール濃度が、コントロール群に 比較して低くなり、特に LDL-コレステロール及び VLDL-コレステロールがかなり低下 したと考察された（実施例 3参照）。また、 9〜18週齢の雌雄アポ E欠損マウスでの評 価においては、カツクロール青果の乾燥物を摂取した群は、血清中の総コレステロ一 ル濃度、 VLDL及び LDL濃度がコントロール群と比較して有意に低かった力 HDL濃 度は群間に有意差は見られなかった (実施例 4参照）。したがって、本発明の医薬又 は食品組成物は、特に、高コレステロール血症及び/又は高 LDL-コレステロール血 症を処置するために有用である。 [0014] According to the study by the present inventors, in the evaluation with 5-week-old male SD rats, In the group that ingested dried fruits and vegetables, the total cholesterol concentration in serum was lower than that in the control group, and it was considered that LDL-cholesterol and VLDL-cholesterol were particularly lowered (see Example 3). In addition, in the evaluation of male and female apo E-deficient mice aged 9 to 18 weeks, the group that ingested dried katstrol fruits and vegetables compared the total cholesterol concentration, VLDL, and LDL concentrations in the serum with those in the control group. There was no significant difference in the HDL concentration between the groups (see Example 4). Therefore, the pharmaceutical or food composition of the present invention is particularly useful for treating hypercholesterolemia and / or high LDL-cholesterolemia.
[0015] また、本発明者らの検討によると、 5週齢の雄 SDラットでの評価においては、カツクロ ール青果の乾燥物を摂取した群には、食効率、肝臓重量、瞎臓重量、血清アミラー ゼ活性においてコントロール群に比較して高いとの実験結果が得られた（実施例 3参 照）。食効率が高いことは、エネルギー代謝の効率化が行われていることを指し、また 、肝臓重量の増加は脂肪肝ではなぐ代謝亢進の可能性を示唆する。さらに、勝臓 重量の増加は、消化酵素、インシュリン、グルカゴンなどの血糖調節作用が効率的に 行える可能性を有し、血清アミラーゼは、勝臓重量の増加に伴って増加していること から、勝臓の活発な活動を意味する。したがって、本発明の食品又は医薬組成物は 、このようなカツクロールの作用により改善される疾患又は状態の処置にも有用である [0015] Further, according to the study by the present inventors, in the evaluation with 5-week-old male SD rats, the dietary efficiency, liver weight, and spleen weight were determined for the group ingested dried chopped fruits and vegetables. The experimental results showed that serum amylase activity was higher than that of the control group (see Example 3). A high dietary efficiency means that energy metabolism has been made more efficient, and an increase in liver weight suggests the possibility of hypermetabolism not in fatty liver. In addition, the increase in visceral weight has the potential to efficiently perform blood glucose regulating actions such as digestive enzymes, insulin, and glucagon, and serum amylase increases as the visceral weight increases. It means the vigorous activity of Katsu. Therefore, the food or pharmaceutical composition of the present invention is also useful for the treatment of diseases or conditions that are ameliorated by the action of such katschlor.
[0016] さらに本発明者らの検討によると、 7週齢の雄 SDラットでの評価においては、カツクロ ール青果の乾燥物を摂取した群の糞中への脂肪酸排泄量は、コントロール群と比較 して有意に高かった（実施例 4参照）。したがって、本発明の医薬又は食品組成物は 、食餌由来の脂質の吸収を阻害する作用があり、そのようなカツクロールの作用によ り改善される疾患又は状態の処置にも有用である。なお、本明細書において、生体 内での吸収に関連して「脂質」というときは、特別な場合を除き、単純脂質 (例えば油 脂；油脂は、脂肪酸とグリセリン力も成る 3価のエステルであり、トリグリセリド (TG)とレ、 うこともある。）、複合脂質 (例えばリン脂質、糖脂質)、コレステロールを含む。単純脂 質と複合脂質には、構成成分として不飽和脂肪酸又は飽和脂肪酸が含まれる。脂質 の吸収阻害は、通常、排泄又は吸収された脂肪酸量を測定することにより、評価する
こと力 Sできる。 [0016] Further, according to the study by the present inventors, in the evaluation of 7-week-old male SD rats, the amount of fatty acid excreted in the feces of the group ingested dried katsukaru fruits and vegetables was as high as that in the control group. It was significantly higher (see Example 4). Therefore, the pharmaceutical or food composition of the present invention has an action of inhibiting the absorption of diet-derived lipids, and is also useful for the treatment of diseases or conditions ameliorated by the action of such katstrol. In this specification, “lipid” refers to simple lipids (for example, fats and oils; fats and oils are trivalent esters that also have fatty acid and glycerin power) unless otherwise specified. ), Triglycerides (TG) and les (sometimes), complex lipids (eg phospholipids, glycolipids), cholesterol. Simple fats and complex lipids contain unsaturated fatty acids or saturated fatty acids as constituents. Inhibition of lipid absorption is usually assessed by measuring the amount of fatty acids excreted or absorbed. That power S.
[0017] 本明細書において、疾患又は状態を「処置 (する）」というときは、特別な場合を除き 、対象となる疾患もしくは状態を、予防もしくは治療すること、軽度に抑えること、又は 進行を抑えることを意味する。「処置」には、根本的な治療が含まれ、また長期的な予 防及び/又は治療とが含まれる。 [0017] In the present specification, when a disease or condition is referred to as "treating", except for special cases, the target disease or condition is prevented or treated, mildly suppressed, or progressed. It means to suppress. “Treatment” includes fundamental therapy and includes long-term prevention and / or therapy.
[0018] 本発明の食品組成物は、飲料の形態であるものも含む。本発明の食品組成物は、 栄養機能食品、特定保健用食品、健康食品、栄養補助食品、ドリンク剤、ジュース、 濃縮ジュース等とすることができる。食品組成物はまた、乾燥品、加工品（例えば、漬 け物。塩漬、しょうゆ漬、みそ漬、ぬかみそ漬、粕漬、麹漬、調味漬、酢漬）、エキスの 形態とすることもでき、以下で説明する医薬組成物である場合に準じて、エキス、濃 縮物等を含むカプセル剤、錠剤、丸剤、タブレット、散剤、顆粒剤等の形態とすること もできる。食品組成物として摂取するカツクロールの量は、以下で説明する医薬組成 物である場合に準じて、適宜とすることができる。 [0018] The food composition of the present invention includes those in the form of beverages. The food composition of the present invention can be a nutritional functional food, a food for specified health use, a health food, a dietary supplement, a drink, a juice, a concentrated juice, or the like. The food composition may also be in the form of dried products, processed products (eg pickles, salted pickles, soy sauce pickles, miso pickles, nuka miso pickles, pickled pickles, pickled pickles, seasoned pickles, pickles), extracts. According to the pharmaceutical composition described below, it can be in the form of capsules, tablets, pills, tablets, powders, granules, etc. containing extracts and concentrates. The amount of katchlor taken as a food composition can be appropriately determined according to the pharmaceutical composition described below.
[0019] 本発明の食品組成物は、食品として許容可能な種々の添加物、例えば甘味料、着 色料、保存料、酸化防止剤、香料、酸味料、調味料、防かび剤（防ばい剤）、 pH調整 剤、栄養強化剤、乳化剤、増粘剤、安定剤、ゲル化剤、糊剤、発色剤、漂白剤を含 んでもよい。 [0019] The food composition of the present invention includes various food-acceptable additives such as sweeteners, colorants, preservatives, antioxidants, flavors, acidulants, seasonings, fungicides (anti-bacterial agents). Agent), pH adjuster, nutrient enhancer, emulsifier, thickener, stabilizer, gelling agent, glue, color former, bleaching agent.
[0020] 本発明の組成物を医薬組成物とする場合、有効成分であるカツクロールの量、投 与期間、間隔は、 目的、症状、対象者の年齢、体重等に応じて適宜とすることができ る。治療の目的では、例えば、臨床上有効量を、数週間〜数ケ月の間、継続して投 与することができる。より具体的には、成人患者に対して、一日当たり、青果の乾燥物 (実施例参照）として 10g〜1000g (好ましくは 25g〜500g、より好ましくは 50g〜250g) に相当する量を、単回又は複数回（例えば 3回）に分割して投与することができる。こ のような量の 1/10〜1/1 (例えば 1/3)を一単位剤形中に含むように設計された製剤は 、本発明の好ましい態様の一つである。 [0020] When the composition of the present invention is used as a pharmaceutical composition, the amount, duration, and interval of katstrol as an active ingredient should be appropriately determined according to the purpose, symptoms, subject's age, weight, etc. You can. For therapeutic purposes, for example, a clinically effective amount can be administered continuously for weeks to months. More specifically, an amount equivalent to 10 g to 1000 g (preferably 25 g to 500 g, more preferably 50 g to 250 g) as a dried product of fruits and vegetables per day is given to an adult patient once a day. Or it can be divided into multiple doses (eg, 3 times). A formulation designed to contain such amounts of 1/10 to 1/1 (eg 1/3) in a unit dosage form is one of the preferred embodiments of the present invention.
[0021] また、健康維持及び/又は発症予防等の目的では、より少なレ、量での投与が効果 的である場合がある。より具体的には、成人である対象者に対して、一日当たり、青 果の乾燥物（実施例参照）として lg〜100g (好ましくは 2.5g〜50g、より好ましくは 5g〜
25g)に相当する量を、単回又は複数回に分割して投与することができる。このような 量の 1/10〜1/1を一単位剤形中に含むように設計された製剤もまた、本発明の好まし い態様の一つである。 [0021] Further, for the purpose of maintaining health and / or preventing onset, administration in a smaller amount or amount may be effective. More specifically, for adult subjects, lg to 100 g (preferably 2.5 g to 50 g, more preferably 5 g to An amount corresponding to 25 g) can be administered in single or divided doses. Formulations designed to contain such amounts of 1/10 to 1/1 in one unit dosage form are also a preferred embodiment of the present invention.
[0022] 青果の乾燥物に相当する量は、当業者であれば、本明細書の実施例等を参考に して、青果全体、青果の抽出物、抽出物残滓、分画物、単離物、濃縮物もしくは加工 物、又は青果の一部（例えば、果肉、皮、種子）、その乾燥物、抽出物、抽出物残滓 、分画物、単離物、濃縮物もしくは加工物等について、それぞれ求めることができる。 [0022] The amount corresponding to the dried product of fruits and vegetables can be determined by those skilled in the art with reference to the examples and the like of the present specification, whole fruits and vegetables, extracts of fruits and vegetables, residue of extracts, fractions, and isolation. Products, concentrates or processed products, or part of fruits and vegetables (for example, pulp, skin, seeds), dried products, extracts, extract residues, fractions, isolates, concentrates or processed products, etc. Each can be determined.
[0023] 投与経路、剤形も適宜設計することができ、例えば、全身的な投与のため、又は局 所投与のために製剤化することができ、内服剤、外用剤、固形剤、液状製剤、散剤、 顆粒剤、カプセル剤、錠剤、丸剤、タブレット、エキス剤、軟膏剤、硬膏剤、ハツプ剤、 ローション剤、リニメント剤、又は坐剤とすることができる。また、除放化製剤、放出制 御型製剤とすることもできる。製剤化は、従来の方法にしたがって行うことができる。 [0023] The administration route and dosage form can also be designed as appropriate, for example, it can be formulated for systemic administration or for local administration, and is used as an internal preparation, external preparation, solid preparation, liquid preparation. , Powders, granules, capsules, tablets, pills, tablets, extracts, ointments, plasters, haps, lotions, liniments, or suppositories. Further, it can be a sustained release preparation or a controlled release preparation. Formulation can be performed according to conventional methods.
[0024] 本発明の医薬組成物は、医薬として許容できる種々の添加物、例えば、附形剤、 結合剤、崩壊剤、滑沢剤、コーティング剤、懸濁化剤、乳化剤、安定剤、保存剤、緩 衝剤を含んでもよい。 [0024] The pharmaceutical composition of the present invention comprises various pharmaceutically acceptable additives such as excipients, binders, disintegrants, lubricants, coating agents, suspending agents, emulsifiers, stabilizers, storages. An agent or buffer may be included.
[0025] 本発明の食品又は医薬組成物は、他の食事療法 (脂肪制限、糖質'アルコール制 限、食物繊維を多く摂取する等。）、薬物療法（コレスチラミン、ニコチン酸、メバロチ ン等の抗コレステロール剤の投薬。）、運動療法と併用して用いることができる。 [0025] The food or pharmaceutical composition of the present invention may be used in other dietary therapies (fat restriction, carbohydrate'alcohol restriction, high intake of dietary fiber, etc.), drug therapy (cholestyramine, nicotinic acid, mevalotin, etc.) Anti-cholesterol medication)), can be used in combination with exercise therapy.
[0026] 本発明の組成物には、その具体的な用途 (例えば、生活習慣病予防のため、体質 改善のため、長期的な治療のため、等。）、及び/又はその具体的な用い方 (例えば 、量、回数、継続的に使用すべき旨、期間、等。）を表示することができる。 [0026] The composition of the present invention has a specific use (for example, prevention of lifestyle-related diseases, improvement of constitution, long-term treatment, etc.) and / or specific use thereof. (E.g., amount, number of times, continuous use, period, etc.) can be displayed.
[0027] 本発明はまた、カツクロールを摂取させることにより脂質代謝を改善する、ヒト又は非 ヒト動物における脂質代謝に関連した疾患又は状態の処置方法、カツクロールを含 む、脂質代謝改善剤、及びカツクロールを脂質代謝改善のために用いるための指針 (例えば、具体的な用途、及び Z又はその具体的な用い方に関する情報、そのような 情報を記載した書面）を含む、製品も提供する。また、カツクローノレを摂取させること を含む、脂質吸収の阻害方法、カツクロールを含む、脂質吸収阻害剤も提供する。 図面の簡単な説明
[0028] [図 1]図 1は、カツクロール全体の写真である。 [0027] The present invention also relates to a method for treating a disease or condition related to lipid metabolism in a human or non-human animal, which improves lipid metabolism by ingesting katchlor, an agent for improving lipid metabolism, including katchlor, And products that include guidelines for using katstrol to improve lipid metabolism (eg, specific uses and information about Z or its specific use, a document containing such information) . Also provided are a method for inhibiting lipid absorption, which comprises ingesting bonito crepes, and a lipid absorption inhibitor comprising katschlor. Brief Description of Drawings [0028] [Fig. 1] Fig. 1 is a photograph of the entire cut crawl.
[図 2]図 2は、カツクロール果実の写真である。 [FIG. 2] FIG. 2 is a photograph of cutlet fruits.
[図 3]図 3は、カツクロール果実の写真である。 [FIG. 3] FIG. 3 is a photograph of cutlet fruits.
[図 4]図 4は、カツクロール塊根の写真である。 [FIG. 4] FIG. 4 is a photograph of Katsukuro tuberous root.
実施例 Example
[0029] 〔実施例 1 :成分比較等〕 [Example 1: Component comparison, etc.]
九州大学内で栽培したカツクロールの青果について、成分及び脂肪酸組成を比較 した。対照として、二ガウリ（佐土原 3号)を用いた。 Ingredients and fatty acid composition were compared for the fruits and vegetables of Katsuraru grown in Kyushu University. As a control, Nigauri (Sadohara No. 3) was used.
[0030] カツクロール及び二ガウリの成分を下表に示した。 [0030] The ingredients of Katsukurol and Nigauri are shown in the table below.
[0031] [表 1] [0031] [Table 1]
Kakrol Bitter gourd Kakrol Bitter gourd
Crude protein (mg/g d.w.)' 101.4 - Crude protein (mg / g d.w.) '101.4-
Total lipid (mg/g d.w.)2 35.0 100.4 Total lipid (mg / g dw) 2 35.0 100.4
α-Tocopherol ( g g d.w.)" 121.5 196.1 α-Tocopherol (g g d.w.) "121.5 196.1
β-caroten ^g/g d.w.) x 10.5 36.4 β-caroten ^ g / g dw) x 10.5 36.4
Ascorbic acid (mg/g d.w.)5 25.1 11.0Ascorbic acid (mg / g dw) 5 25.1 11.0
jcldahl method. jcldahl method.
Holch's method. Holch's method.
HPLC. HPLC.
Hydrajin method また、脂肪酸組成を下表に示した。 Hydrajin method The fatty acid composition is shown in the table below.
[0032] [表 2] [0032] [Table 2]
Kakrol Bitter gourd Kakrol Bitter gourd
(%) (%)
16:0 23.4 10.7 16: 0 23.4 10.7
18:0 5.7 51.0 18: 0 5.7 51.0
18:1 9.7 10.3 18: 1 9.7 10.3
18:2 (n-6) 43.3 13.5 18: 2 (n-6) 43.3 13.5
18:3 (n-3) 17.9 14.7 測定は、 Folch法（クロ口ホルム/メタノール =2 : 1)で抽出後、けん化し、脂肪酸画分 をガスクロマトグラフィーで行った。 18: 3 (n-3) 17.9 14.7 Measurements were carried out by extraction using the Folch method (black mouth form / methanol = 2: 1), saponification, and the fatty acid fraction was measured by gas chromatography.
二ガウリに比べてカツクロールは、脂質量が少ない（カロリーが低レ、）割には- tocoph
erol (ビタミン E)量が多ぐまた、血清コレステロール低下作用の強いリノール酸が多く 含まれていた。なお、カツクロールのコレステロール低下作用について後述するが、 含有量からすると、このリノール酸が効いてコレステロールを下げているのではなレ、。 Katstrol compared to Nigauri has less fat (low calories), but -tocoph In addition, the amount of erol (vitamin E) was high and linoleic acid, which has a strong serum cholesterol-lowering effect, was contained in a large amount. The cholesterol-lowering action of katschlor will be described later. From the viewpoint of its content, this linoleic acid is effective in lowering cholesterol.
[0034] 〔実施例 2：凍結乾燥粉末の調製〕 [Example 2: Preparation of freeze-dried powder]
カツクロール青果を 3cm角に切り凍結乾燥し、ミキサーで粉砕した。青果 1004gから、 淡緑色の粉末 131.3gを得た。得られた乾燥物は、苦みはなぐキユウリの味に似てお り、青臭い匂いを有した。これを以下の実施例で用いた。 Cut and chopped fruits and vegetables were cut into 3 cm squares, freeze-dried, and ground with a mixer. From 1004 g of fruits and vegetables, 131.3 g of pale green powder was obtained. The obtained dried product resembled the taste of cucumber without bitterness and had a blue odor. This was used in the following examples.
[0035] 〔実施例 3 :脂質代謝に与える影響の評価〕 [Example 3: Evaluation of influence on lipid metabolism]
5週齢の雄 SDラットを市販の固形食で 1週間予備飼育後、体重により 2群に分け、 1 群 6匹とした。 AIN-76 (米国国立栄養研究所（American Institute of Nutrition, AIN) ) 組成に準じ、 5%コーン油を含むコントロール食（コントロール群）、及び 5。 /。のコーン 油と 3%の kakrol凍結乾燥粉末 (実施例 2)を含むカツクロール食 (カツクロール群）を、 摂食量を調節しながら与え、 2週間飼育した。 Five week old male SD rats were preliminarily raised on a commercially available solid diet for 1 week, and then divided into 2 groups according to body weight. AIN-76 (American Institute of Nutrition, AIN) According to the composition, a control diet containing 5% corn oil (control group), and 5. /. Of corn oil and 3% kakrol freeze-dried powder (Example 2) were fed while controlling the amount of food to be fed for 2 weeks.
[0036] 食餌組成を下表に示した。 [0036] The diet composition is shown in the table below.
[0037] [表 3] [0037] [Table 3]
Control Kakrol Control Kakrol
(g kg diet) (g kg diet)
Cornstarch 150 150 Cornstarch 150 150
Casein 200 200 Casein 200 200
Sucrose 500 470 Sucrose 500 470
Corn oil 50 50 Corn oil 50 50
Cellulose 50 50 Cellulose 50 50
凍結乾燥粉末 （実施例 2) - 30 Freeze-dried powder (Example 2)-30
Mineral mixture (A1N-76) 35 35 Mineral mixture (A1N-76) 35 35
Vitamin mixture (AIN-76) 10 10 Vitamin mixture (AIN-76) 10 10
DI, Methionine 3 3 DI, Methionine 3 3
Coline bitartrate 2 2 Coline bitartrate 2 2
Total 1000 1000 絶食をさせずに断頭により屠殺後、肝臓、膝臓、白色脂肪組織 (睾丸周辺、腸間膜 周辺、腹膜後腔周辺)及び筋肉を摘出した。肝臓脂質は化学法 (コレステロール: Spe
rry S., J. Biol. Chem., 187， 97-106, 1950,トリグリセリド： Fletcher S" Clin. Chim. Act a. 22， 393-397, 1968,リン脂質： Rouser S., Lipids, 1， 85-86, 1966)により測定し、血 清脂質は酵素法キット（コレステロール:デターミナ一 TC555、協和メディクス、 HDL分 画試薬:簡易 DCM測定法，トリグリセリド：トリグリセライド E-テストヮコ一、和光純薬ェ 業）、血清グノレコースは酵素法キット（グルコース C-II-テストヮコ一、和光純薬工業） を用いて測定した。血清アミラーゼ濃度はキット（アミラーゼテストヮコ一、和光純薬ェ 業)を用いて測定した。また、肝臓の脂肪酸合成系'脂肪酸酸化系の酵素活性を測 定した。 Total 1000 1000 After sacrifice by decapitation without fasting, liver, knee, white adipose tissue (around testes, mesentery, retroperitoneal cavity) and muscle were removed. Liver lipids are chemical (cholesterol: Spe rry S., J. Biol. Chem., 187, 97-106, 1950, Triglyceride: Fletcher S "Clin. Chim. Act a. 22, 393-397, 1968, Phospholipid: Rouser S., Lipids, 1, 85-86, 1966), and serum lipids were measured using enzyme method kits (cholesterol: Determina TC555, Kyowa Medics, HDL fractionation reagent: simple DCM assay, triglyceride: Triglyceride E-Test Sakai, Wako Pure Chemical Industries, Ltd. Serum gnolecose was measured using an enzyme method kit (glucose C-II-Test Koichi, Wako Pure Chemical Industries, Ltd.) Serum amylase concentration was measured using a kit (Amylase test Koichi, Wako Pure Chemical Industries, Ltd.) In addition, the enzyme activity of the fatty acid synthesis system (fatty acid oxidation system) of the liver was measured.
[0038] 結果: [0038] Results:
結果を下表に示した。 The results are shown in the table below.
[0039] [表 4] [0039] [Table 4]
Table 4 成長に関連したパラメ一 -タ Table 4 Parameters related to growth
Control akrol Control akrol
Initial body weight ^g) 201.7±3.0 201.8±2.9 Initial body weight ^ g) 201.7 ± 3.0 201.8 ± 2.9
rinal bodv weight ^g) 283.9±3.3 293.7±4.2 rinal bodv weight ^ g) 283.9 ± 3.3 293.7 ± 4.2
Body weight gain (g) 82.3±1.9 1.9±4.2 Body weight gain (g) 82.3 ± 1.9 1.9 ± 4.2
Food intake (g/day) 21.0±0.2 20.9±0.5 Food intake (g / day) 21.0 ± 0.2 20.9 ± 0.5
Food efficiency 279.9±6.1 313.7±12.8* Food efficiency 279.9 ± 6.1 313.7 ± 12.8 *
(mg weight gain/g food intake) (mg weight gain / g food intake)
Values are means ± SE (n=6) Values are means ± SE (n = 6)
Significantly different from the control rats at /?<0.05 Significantly different from the control rats at /?<0.05
[0040] [表 5] [0040] [Table 5]
Table 5 白色脂肪組織 (White adipose tissue WAT) 重量 Table 5 White adipose tissue WAT Weight
Control Kakrol Control Kakrol
Total WAT (g) 9.12±0.50 8.72±0.76 Total WAT (g) 9.12 ± 0.50 8.72 ± 0.76
Retroperitoneal WAT (g) 2.96±0.13 2.58±0.33 Retroperitoneal WAT (g) 2.96 ± 0.13 2.58 ± 0.33
Mesenteric WAT (g) 3.08±0.26 3.25±0.27 Mesenteric WAT (g) 3.08 ± 0.26 3.25 ± 0.27
Epididymal WAT (g) 3.08±0.18 2.88±0.29 Epididymal WAT (g) 3.08 ± 0.18 2.88 ± 0.29
Relative WAT weight 3.22±0.20 2.97±0.26 Relative WAT weight 3.22 ± 0.20 2.97 ± 0.26
(g/lOOg body weight) (g / lOOg body weight)
Values are means±SE (n=6) Values are means ± SE (n = 6)
[0041] [表 6]
Table 6 大腿筋重 [0041] [Table 6] Table 6 Thigh muscle weight
Control Kakrol Control Kakrol
Total muscle weight ^g) 4.04±0.09 3,91士 0.12 Total muscle weight ^ g) 4.04 ± 0.09 3,91 people 0.12
Right muscle weight (g) 2.02士 0.05 1.96±0.01 Right muscle weight (g) 2.02 people 0.05 1.96 ± 0.01
Left muscle weight (g) 2.02±0.04 1.96±0.05 Left muscle weight (g) 2.02 ± 0.04 1.96 ± 0.05
Relative muscle weight 1.42±0.02 1.33±0.03* Relative muscle weight 1.42 ± 0.02 1.33 ± 0.03 *
(g/lOOg body weight) (g / lOOg body weight)
Values are means士 SE (n=6) Values are meansshi SE (n = 6)
'Significantly different from the control rats at ?<0.05 'Significantly different from the control rats at? <0.05
[0042] [表 7] [0042] [Table 7]
Table 7 肝臓重量および睇臓重量 Table 7 Liver weight and visceral weight
Control Kakrol Control Kakrol
Total liver weight (g) 13.73±0.43 15.62±0.55* Total liver weight (g) 13.73 ± 0.43 15.62 ± 0.55 *
Relative liver weight 4.84±0.14 5.32±0.14* Relative liver weight 4.84 ± 0.14 5.32 ± 0.14 *
(g liver/ l OOg body weight) (g liver / l OOg body weight)
Total pancreas weight (g) 0.46±0.02 Ο·55±0.03' Total pancreas weight (g) 0.46 ± 0.02 Ο55 ± 0.03 '
Relative pancreas weight 0.16±0.01 0.19±0.01* Relative pancreas weight 0.16 ± 0.01 0.19 ± 0.01 *
(g pancreas/ 1 OOg body weight) (g pancreas / 1 OOg body weight)
Values are means±SE (n=6) Values are means ± SE (n = 6)
Significantly different from the control rats at /><0.05 体重増加量、終体重、摂食量及び脂肪組織重量に群間に有意差は見られなかつ たが、食効率、肝臓重量及び膝臓重量は Control群と比較して Kakrol群が有意に増 加した。また、相対筋重量は有意に減少した。 Significantly different from the control rats at /><0.05 There was no significant difference between the groups in weight gain, final body weight, food intake and adipose tissue weight, but food efficiency, liver weight and knee weight were different from those in the Control group. In comparison, the Kakrol group increased significantly. In addition, the relative muscle weight was significantly reduced.
[表 8] [Table 8]
Table 8 血清中の GOTレベルおよびアミラーゼレベル Table 8 GOT and amylase levels in serum
Control Kakrol Control Kakrol
GOT (lU'/L) 193.9±16.8 175.3±12.9 GOT (lU '/ L) 193.9 ± 16.8 175.3 ± 12.9
Amylase (unit2) 1474.2±50.8 1761.8士 93.7' Amylase (unit 2 ) 1474.2 ± 50.8 1761.8 people 93.7 '
Values are means±SH (n=6) Values are means ± SH (n = 6)
Significantly different from the control rats at ^><0,05 Significantly different from the control rats at ^> <0,05
1 IU= 1 ιηοΙ-L-glutanate/min 1 IU = 1 ιηοΙ-L-glutanate / min
One unit is defined as an activity that l OOmL serum One unit is defined as an activity that l OOmL serum
decompose 10 mg starch within 30 minutes at 37°C. 血清中の GOT活性は群間に有意差は見られなかった力 血清中のアミラーゼ活性 は Control群と比較して Kakrol群が有意に増加した。 decompose 10 mg starch within 30 minutes at 37 ° C. GOT activity in serum was not significantly different between groups. Amylase activity in serum was significantly increased in Kakrol group compared to Control group.
[0044] [表 9]
Table 9 血清グルコースレベル [0044] [Table 9] Table 9 Serum glucose levels
Control Kakrol Control Kakrol
Glucose level (mg/dL) 149.4±4,6 147.3±1.0 Glucose level (mg / dL) 149.4 ± 4,6 147.3 ± 1.0
Values are means SE (n;6) Values are means SE (n; 6)
[0045] [表 10] [0045] [Table 10]
Table 10 脂質レベル (血清、肝臓) Table 10 Lipid levels (serum, liver)
Control Kakrol Control Kakrol
Serum (mg/dL) Serum (mg / dL)
Total-Cholesterol 1 10.7±8.2 76.7±6.5** Total-Cholesterol 1 10.7 ± 8.2 76.7 ± 6.5 **
HDL-Cholesterol 62.5±3.9 44.3±3.9** HDL-Cholesterol 62.5 ± 3.9 44.3 ± 3.9 **
Triacylglycerol 261.7±37.4 236.4±35.3 Triacylglycerol 261.7 ± 37.4 236.4 ± 35.3
Liver (mg/g Liver) Liver (mg / g Liver)
Cholesterol Cholesterol
Total 4.72士 0.48 2.21±0.24" Total 4.72 0.48 2.21 ± 0.24 "
Free 2.53±0.22 1.49±0.07** Free 2.53 ± 0.22 1.49 ± 0.07 **
Esterified 2.18±0.42 0.72±0.26" Esterified 2.18 ± 0.42 0.72 ± 0.26 "
Triacylglycerol 56.14±12.57 20.27±4.31 * Triacylglycerol 56.14 ± 12.57 20.27 ± 4.31 *
Phospholipid 34.72±1.19 27.49±0.92** Phospholipid 34.72 ± 1.19 27.49 ± 0.92 **
Values are means土 SE (n=6) Values are means Sat SE (n = 6)
' Significantly different from the control rats at /?<0.05 'Significantly different from the control rats at /?<0.05
and /3<0.01 , respectively 血清中の総コレステロール濃度、 HDL-コレステロール濃度は Control群と比較して Kakrol群が有意に減少した。 HDL-コレステロール濃度の低下が総コレステロール濃 度の低下に比較して少ないことから、 LDL-コレステロール +VLDL-コレステロールが 力、なり低下したと考えられる。 and /3<0.01, respectively The total cholesterol concentration and HDL-cholesterol concentration in serum were significantly decreased in the Kakrol group compared to the Control group. Since the decrease in HDL-cholesterol concentration is small compared to the decrease in total cholesterol concentration, LDL-cholesterol + VLDL-cholesterol is considered to have decreased.
[0046] また、肝臓中のコレステロール濃度、トリァシルグリセロール (TG)濃度及びリン脂質 ( PL)濃度は、 Control群と比較して Kakrol群が有意に減少した。なお、血清 TG濃度及 び血清グノレコース濃度においては、群間に有意差は見られなかった。 [0046] Further, the cholesterol concentration, triacylglycerol (TG) concentration and phospholipid (PL) concentration in the liver were significantly decreased in the Kakrol group as compared to the Control group. There was no significant difference between the groups in serum TG concentration and serum gnolecose concentration.
[0047] [表 11]
Table 1 1 脂肪酸の合成および 酸化に関連する酵素の活性 [0047] [Table 11] Table 1 1 Activity of enzymes related to fatty acid synthesis and oxidation
Control akrol Control akrol
(nmol/min/mg protein) (nmol / min / mg protein)
Fatty acid synthesis Fatty acid synthesis
FAS 26.34±2.02 26.89±1.86 FAS 26.34 ± 2.02 26.89 ± 1.86
Malic Enzyme 113.66±10.92 120.11±12.02 Malic Enzyme 113.66 ± 10.92 120.11 ± 12.02
G6PDH 148.10±12.89 113.62±13.26 G6PDH 148.10 ± 12.89 113.62 ± 13.26
β-oxidation β-oxidation
Mitochondoria Mitochondoria
CPT 1.92±0.17 2.35土 0.21 CPT 1.92 ± 0.17 2.35 Sat 0.21
Peroxisome Peroxisome
ACO 1.37±0.07 1.0l±0.07* ACO 1.37 ± 0.07 1.0l ± 0.07 *
Values are means土 SE (n=6) Values are means Sat SE (n = 6)
Significantly different from the control rats at p<0.05 Significantly different from the control rats at p <0.05
FAS、 Malic Enzyme及び G6PDH活性は群間に有意差は見られな力、つた。また、 CP T活性も群間に有意差は見られなかった。一方、 AC〇活性は、 Control群と比較して K akrol群が有意に減少した。 FAS, Malic Enzyme, and G6PDH activities showed no significant difference between groups. In addition, CPT activity was not significantly different between groups. On the other hand, AC0 activity decreased significantly in the Kakrol group compared to the Control group.
[0048] 考察: [0048] Discussion:
Kakrolには血清コレステロール濃度の低下作用があり、肝臓脂質の低下作用を示 す物質が含まれていることが示唆された。食品成分で同様の作用が見られるものとし ては、大豆タンパク質が挙げられる力 その際の食餌中の大豆タンパク質の割合は 2 0%である。 3%カツクロール食における本実施例での結果は従来の食品成分からは 予 ¾|できなレ、顕著なものであるとレ、える。 It was suggested that Kakrol has an effect of lowering serum cholesterol concentration and contains substances that show an action of lowering liver lipids. The ability of food ingredients to have the same effect is the ability of soy protein. The percentage of soy protein in the diet is 20%. The results in this example for a 3% cut crawl meal are unpredictable and conspicuous from conventional food ingredients.
[0049] 〔実施例 4：脂質代謝に与える影響の評価〕 [Example 4: Evaluation of influence on lipid metabolism]
SDラット又はアポ E欠損マウスにカツクロール凍結乾燥粉末を摂取させ、カツクロー ルが脂質代謝に及ぼす影響と、その作用機構について検討した。 SD rats or apo E-deficient mice were ingested with katschlor freeze-dried powder, and the effects of katschlor on lipid metabolism and its mechanism of action were investigated.
[0050] 方法: [0050] Method:
[実験 1 糞中への脂肪酸排泄量の測定] [Experiment 1 Measurement of Fatty Acid Excretion in Feces]
AIN-76組成に準じて 5%コーン油を含む食餌 (Control群)と 5%コーン油及び 3%力 ックロール凍結乾燥粉末を含む食餌 (Kakrol群)、 5%コーン油及び 3%二ガウリ凍結 乾燥粉末を含む食餌 (Bitter gourd群)を与えた 7週齢の雄 SDラットの糞を 3日間回収 し、滴定により脂肪酸量を測定した。
[0051] [実験 2 アポ E欠損マウスにおける脂質代謝の評価] A diet containing 5% corn oil according to AIN-76 composition (Control group), a diet containing 5% corn oil and 3% hard-rolled lyophilized powder (Kakrol group), 5% corn oil and 3% digauri freeze-dried Feces from 7-week-old male SD rats fed a diet containing powder (Bitter gourd group) were collected for 3 days and the amount of fatty acid was measured by titration. [0051] [Experiment 2 Evaluation of lipid metabolism in apo E-deficient mice]
9〜18週齢の雌雄アポ E欠損マウス 29匹を市販固形食で 1週間予備飼育した後、 AI N-76組成に準じ、 10%ラードを含む Control食（Control群、雄雌 8匹）及び 10%ラードと 3%のカツクロール凍結乾燥粉末を含むカツクロール食（Kakrol群、雄 6匹、雌 7匹）を P air feedingで 9週間飼育した。 After pre-bred 29 male and female apo E deficient mice aged 9-18 weeks on a commercial solid food for 1 week, according to AI N-76 composition, control food containing 10% lard (Control group, 8 males and females) and A katsukuro diet (Kakrol group, 6 males, 7 females) containing 10% lard and 3% katsukuro freeze-dried powder was bred for 9 weeks by Pair feeding.
[0052] 食餌組成を下表に示した。 [0052] The diet composition is shown in the table below.
[0053] [表 12] [0053] [Table 12]
Control Kakrol Control Kakrol
(g kg diet) (g kg diet)
Sucrose 450 420 Sucrose 450 420
Casein 200 200 Casein 200 200
Cornstarch 150 150 Cornstarch 150 150
Lard 100 100 Lard 100 100
Cellulose 50 50 Cellulose 50 50
Kakrol - 30 Kakrol-30
Mineral mixture CAIN-76) 35 35 Mineral mixture CAIN-76) 35 35
Vitamin mixture (AIN-76) 10 10 Vitamin mixture (AIN-76) 10 10
DL-Methionine 3 3 DL-Methionine 3 3
Coline bitartrate 2 2 Coline bitartrate 2 2
The diets are formulated according to the AIN-76 formula. The diets are formulated according to the AIN-76 formula.
6時間絶食させた後、動脈採血により屠殺し、肝臓、心臓、白色脂肪組織 (睾丸 '卵 巣周辺、腸間膜周辺、腹膜後腔 *腎周辺、皮下)及び大動脈を摘出した。肝臓脂質 は化学法により測定し、血清脂質は酵素法キットを用いて測定した（実施例 3参照）。 血清中のチォバルビツール酸反応物（TBARS)は化学法により測定した。 After fasting for 6 hours, the blood was sacrificed by arterial blood sampling, and the liver, heart, white adipose tissue (testicles around the nest, around the mesentery, retroperitoneal space * around the kidney, subcutaneous) and the aorta were removed. Liver lipids were measured by chemical methods, and serum lipids were measured using an enzymatic method kit (see Example 3). Serum thiobarbituric acid reactant (TBARS) in serum was measured by a chemical method.
[0054] 結果: [0054] Results:
[実験 1 糞中への脂肪酸排泄量の測定] [Experiment 1 Measurement of Fatty Acid Excretion in Feces]
[0055] [表 13] [0055] [Table 13]
Table 13 糞中への脂肪酸排泄量 Table 13 Fatty acid excretion in feces
Control Kakrol Bitter gourd Control Kakrol Bitter gourd
Fatty acids in feces (mg day) 34.50 ± 3.74a 83.44 ± 4.73b 37.31 ± 4.17a FA extraction rate (%/day) 4.56士 0.50a 13.99 ± 0.76b 5.90士 0.64a Fatty acids in feces (mg day) 34.50 ± 3.74 a 83.44 ± 4.73 b 37.31 ± 4.17 a FA extraction rate (% / day) 4.56 0.50 a 13.99 ± 0.76 b 5.90 0.64 a
Values are mean±SE (n=6〜8) Values are mean ± SE (n = 6-8)
Different superscript letters are significantly different at pく 0.01 by Tukey-Kramer 糞中への脂肪酸排泄量は、 Control群及び Bitter gourd群と比較して Kakrol群で有
意に咼かった。 Different superscript letters are significantly different at p 0.01 0.01 by Tukey-Kramer Fecal fatty acid excretion is higher in the Kakrol group compared to the Control group and Bitter gourd group It was ugly.
[0056] [実験 2 アポ E欠損マウスにおける脂質代謝の評価] [0057] [表 14] [0056] [Experiment 2 Evaluation of lipid metabolism in apo E-deficient mice] [0057] [Table 14]
Kkll C Clttoaronoroonr Kkll C Clttoaronoroonr
68Ό干 68
22031339 2340509071h) Il bdi ( 235 ± ± ±ttoniiay wegg...... loo 167οτ οεv千d 22031339 2340509071h) Il bdi (235 ± ± ± ttoniiay wegg ...... loo 167οτ οεv thousandd
I49022 2 36150Z Fil bdih ()31土 ±tnaogy weg).... < S£019 OS 11 Ζ1OΛίΖ ξ9£ 901W)8干干干F =''''' ζΛ 01 I49022 2 36150Z Fil bdih () 31 Sat ± tnaogy weg) .... <S £ 019 OS 11 Ζ1OΛίΖ ξ9 £ 901W) 8 Dried F = '' '' 'ζΛ 01
2 Ζd Bh)ty weig gaino ΖSMΌ 600ャΓ. . ^ 2 Ζd Bh) ty weig gaino ΖSMΌ 600 Γ.
390013dk () F id ±tonaegayo.. 390013dk () F id ± tonaegayo ..
844911dffii24832 17 F ± ±ocnco eey.... 844911dffii24832 17 F ± ± ocnco eey ....
; ί i/ T (hil f i)dktttomg wengeaoonag ga ; ί i / T (hil f i) dktttomg wengeaoonag ga
Ζ Ζ 2 V N SN S 9Γ0 i 9095干干. V Ζ 2 V N SN S 9Γ0 i 9095
429i61 3008402 Rli lih ± ±ttaeeregevv w,,,. 429i61 3008402 Rli lih ± ± ttaeeregevv w ,,.
[1, [1,
m m
-H -H
. .
O
O
初体重、終体重、体重 加量、摂食量及び体重あたりの肝臓重量は群間に有意差 は見られなかったが、食 率は Control群と比較して Kakrol群で有意に低かった。 There was no significant difference between the groups in initial body weight, final body weight, body weight gain, food intake, and liver weight per body weight, but the food rate was significantly lower in the Kakrol group than in the Control group.
[表 15] [Table 15]
s家9 ¾!ズ！!tr Π： 9lql9e C D s house 9 ¾! ! tr Π: 9lql9e C D
Z Z
νΛοζν 3 νΛοζν 3
I 1O l¾リUUSC0J5I I 1O l¾ Li UUSC0J5I
S0ュ loo Όειί 6ε s l13トς r Γ616Vvΐ τiち¾&do3 B... S0 loo looειί 6ε s l13 ς r Γ616Vvΐ τi ¾ & do3 B ...
Γι 968 iuoH ί ΊΟΊΛi τpsol Γι 968 iuoH ί ΊΟΊΛi τpsol
o llqu一 drtsj,siosao o, o llqu drtsj, siosao o,
0一£Γ6ζΤ, 0 ££ 6ζΤ,
J!is N SN SちSIus：.. J! Is N SN S Chius: ..
血清中の総 Choi濃度、 VLDL及び LDL濃度は Control群と比較して Kakrol群で有意 に低かったが、 HDL濃度は群間に有意差は見られなかった。一方、肝臓中の総 Choi
濃度、 TG濃度は群間に有意差は見られなかった力 リン脂質は Control群と比較して Total serum Choi, VLDL, and LDL concentrations were significantly lower in the Kakrol group than in the Control group, but no significant differences were observed in the HDL concentration between the groups. Meanwhile, total Choi in the liver Concentration and TG concentration showed no significant difference between groups.
Claims
[1] カツクローノレ、及び食品又は医薬として許容可能な添加物を含む、食品又は医薬 組成物。 [1] A food or pharmaceutical composition comprising bonito and a food or pharmaceutically acceptable additive.
[2] 脂質代謝に関連した疾患又は状態を処置するための、請求項 1に記載の食品又は 医薬組成物。 [2] The food or pharmaceutical composition according to claim 1, for treating a disease or condition associated with lipid metabolism.
[3] 疾患又は状態が、高脂血症 (原発性 (家族性、散発性)、二次性を含む。また、高コ レステロール血症を含む。）、脂肪肝、動脈硬化、虚血性心疾患 (狭心症、心筋梗塞 を含む。）、脳血管障害 (脳梗塞、脳出血を含む。）又は生活習慣病である、請求項 2 に記載の食品又は医薬組成物。 [3] The disease or condition is hyperlipidemia (including primary (familial, sporadic), secondary, and hypercholesterolemia), fatty liver, arteriosclerosis, ischemic heart The food or pharmaceutical composition according to claim 2, which is a disease (including angina pectoris and myocardial infarction), cerebrovascular disorder (including cerebral infarction and cerebral hemorrhage) or a lifestyle-related disease.
[4] カツクロール力 カツクロール青果、その乾燥物、抽出物、分画物、単離物、もしくは 濃縮物又はそれらのいずれかの加工物である、請求項：!〜 3のいずれか 1項に記載 の食品又は医薬医薬組成物。 [4] Katscrawl force Katskraur fruits and vegetables, dried products, extracts, fractions, isolates, concentrates thereof, or processed products of any one of claims:! To 3 Or a pharmaceutical or pharmaceutical composition according to 1.
[5] カツクロールを摂取させることにより脂質代謝を改善する、脂質代謝に関連した疾患 又は状態の処置方法。 [5] A method for treating a disease or condition related to lipid metabolism, which improves lipid metabolism by ingesting katschlor.
[6] カツクロールを含む、脂質代謝改善剤。 [6] A lipid metabolism improving agent containing katschlor.
[7] カツクローノレ、及びカツクロールを脂質代謝改善のために用いるための指針を含む 、製品。 [7] A product that includes guidelines for using katsukuro nore and katsukuro to improve lipid metabolism.
[8] カツクロールを、青果の乾燥物として 10g〜1000g (好ましくは 25g〜500g、より好ましく は 50g〜250g)に相当する量で含む、請求項 4に記載の食品又は医薬組成物。 [8] The food or pharmaceutical composition according to claim 4, comprising katstrol in an amount corresponding to 10 g to 1000 g (preferably 25 g to 500 g, more preferably 50 g to 250 g) as a dried product of fruits and vegetables.
[9] カツクロールを摂取させることを含む、脂質吸収の阻害方法。 [9] A method for inhibiting lipid absorption, comprising ingesting katstrol.
[10] カツクロールを含む、脂質吸収阻害剤。
[10] A lipid absorption inhibitor containing katstrol.
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| JP2008507493A JP5256456B2 (en) | 2006-03-24 | 2007-03-26 | Lipid metabolism improver |
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| JP2006-083581 | 2006-03-24 |
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| WO (1) | WO2007111306A1 (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001278804A (en) * | 2000-03-30 | 2001-10-10 | Miyazaki Prefecture | Lipid metabolism-improving agent and food containing the same |
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2007
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001278804A (en) * | 2000-03-30 | 2001-10-10 | Miyazaki Prefecture | Lipid metabolism-improving agent and food containing the same |
Non-Patent Citations (5)
| Title |
|---|
| DATABASE MEDLINE [online] KAMESWARARAO B. ET AL.: "Evaluation of antidiabetic effect of Momordica cymbalaria fruit in alloxan-diabetic rats", XP003018314, accession no. STN Database accession no. (2003115484) * |
| FERNANDOPULLE B.M.R.: "Oral hypoglycaemic effects of Momordica dioica in the rat", MEDICAL SCIENCE RESEARCH, vol. 22, no. 2, 1994, pages 137 - 139, XP003018312 * |
| FITOTERAPIA, vol. 74, no. 1-2, 2003, pages 7 - 13 * |
| KAMESWARARAO B. ET AL.: "Antidiabetic and hypolipidemic effects of Momordica cymbalaria Hook fruit powder in alloxan-diabetic rats", JOURNAL OF ETHNOPHARMACOLOGY, vol. 67, no. 1, 1999, pages 103 - 109, XP003018313 * |
| REDDY G. ET AL.: "Antihyperglycemic activity of Momordica dioica fruits in alloxan-induced diabetic rats", NIGERIAN JOURNAL OF NATURAL PRODUCTS AND MEDICINE, vol. 9, 2005, pages 33 - 34, XP003018311 * |
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