JP2005272456A - Hypoglycemic agent or cathartic agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a hypoglycemic agent capable of being ingested in a large amount at one time, excellent in safety, and having higher efficacy than ever, and to provide a cathartic agent. <P>SOLUTION: This hypoglycemic agent contains albedo of citrus fruits as an active ingredient. A hypoglycemic food or beverage contains the hypoglycemic agent. The cathartic agent contains the albedo of the citrus fruits as an active ingredient. A cathartic food or beverage contains the cathartic agent. A representative example of the citrus fruits containing the albedo is grapefruit. The albedo may be processed in such a degree that its pharmacological effect is not inhibited. The albedo used herein is given at a reduced cost and scarcely has a side effect. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to a citrus-derived hypoglycemic agent and a bowel movement improving agent.

Lifestyle-related illnesses called adult illnesses can occur in almost all Japanese people, including children, regardless of age. In recent years, the number of lifestyle-related disease patients and the reserve army has increased remarkably. It is a problem.
Lifestyle-related diseases are chronic diseases in which lifestyle habits such as eating habits, exercise habits, rest, smoking, and drinking are greatly involved in the onset and progression of diabetes, obesity, hyperlipidemia, hyperuricemia Disease, cardiovascular disease, colon cancer, hypertension, squamous cell lung cancer, chronic bronchitis, emphysema, alcoholic liver disorder, periodontal disease and the like.
Among them, the number of diabetic patients, who are representative of lifestyle-related diseases, has been increasing rapidly in recent years. In Japan, it is said that one out of 10 middle-aged and older people has diabetes. Diabetes mellitus is a disease in which the level of glucose in the blood (blood glucose level) rises above a certain level. If the state of high blood glucose level continues for a long time, the blood vessel wall is damaged and the whole body associated with various vascular complications. Complications of the organs occur. The basis of treatment of diabetes is to control blood sugar by diet therapy or exercise therapy, and diet therapy is particularly important. Therefore, various efforts have been made to improve eating habits in order to prevent lifestyle-related diseases in general households, and it is desired to develop foods and drinks having a lifestyle-safety-preventing action that is superior in safety.

On the other hand, food functions include a life-sustaining function (primary function) by food nutrients, a function in which food components appeal to living sensations (secondary function), and a function to adjust physical condition (tertiary function). Nutrition (primary function) and taste (secondary function) of food are well understood and recognized, but in recent years, tertiary functions such as food defense, physical condition rhythm control, disease prevention and recovery have attracted attention. Yes. Foods continue to be eaten every day, have a high potential for long-term effects on the body, and many researches and developments have been made on the functionality of foods. For example, many studies have been conducted on the action of flavonoids such as naringin and hesperidin, which are abundant in citrus fruits. Antioxidant activity, prevention of cardiovascular diseases, anti-inflammatory, antiallergic, antibacterial, antiviral There are many reports such as lowering of blood sugar level.
In addition, inhibitors of blood glucose level elevation, hyperleptinemia prevention / amelioration agent, hyperinsulinemia prevention / amelioration agent, peroxisome proliferator-activated receptor using plant extracts that have been ingested daily as food for many years (PPAR) -dependent gene transcription activators and lipid metabolism promoters are known (Patent Document 1). This gene consists of chlorogenic acids obtained from plants such as coffee, apple, grape, onion, etc., has an excellent PPAR-dependent gene transcription activation action, and has a PPR response element (PPRE) in the transcriptional regulatory region of the gene In particular, lipid metabolism is activated, thereby having an effect on various lifestyle-related diseases.
However, there are few things that are readily available at low cost, and there is a need for the development of familiar foods and drinks that are more safe.

  In addition, citrus peel has been used as a feed for its use because it is by-produced in large quantities in the production of juice and the like. However, it is not suitable for eating as it is because it is sensually bitter to humans.

JP 2003-34636 A

  An object of the present invention is to provide a hypoglycemic agent and a bowel movement improving agent that can be ingested in a large amount at once, is excellent in safety, and is more effective. Moreover, it is providing the food / beverage products which have the effect of a blood glucose level fall and a bowel movement improvement.

  Briefly describing the present invention, the first invention of the present invention is a hypoglycemic agent containing citrus albedo as an active ingredient, and the second invention of the present invention is an improvement of bowel movement containing citrus albedo as an active ingredient. The third invention of the present invention is a hypoglycemic agent in which the citrus fruit is grapefruit, and the fourth invention of the present invention is a bowel movement improving agent in which the citrus fruit is grapefruit. A fifth invention is a food or beverage for reducing blood sugar level containing the blood glucose level lowering agent, and a sixth invention of the present invention is a food for improving bowel movement containing the bowel movement improving agent Or a beverage.

  As a result of diligent research to solve the problems of the prior art, the present inventors have eaten albedo that is present in large amounts in citrus fruits, thereby reducing blood glucose levels, improving bowel movements, and lowering cholesterol. As a result, the present invention has been completed.

  The blood glucose level lowering agent and the bowel movement improving agent containing the citrus albedo of the present invention as an active ingredient can be taken in a large amount at a time, and a high effect is obtained. Moreover, since the skin peeled normally is utilized, it is inexpensive and has little worry about side effects.

The present invention will be specifically described below.
The citrus fruits in the present invention are not particularly limited as long as they are citrus fruits rich in albedo. For example, mandarin oranges such as Wenzhou mandarin, Ponkan, Sikhwasher, Sudachi, oranges such as Navel and Valencia, summer mandarin oranges, Hassaku, Iyokan, Daidai and other citrus fruits, other Bungtan, grapefruit, lemon, yuzu, kumquats In the present invention, it is particularly preferable to use grapefruit rich in albedo containing a large amount of flavonoids such as naringin. There are no particular limitations on the grapefruit varieties used, and examples include Duncan, Marsh, and Ruby.

  The albedo used as an active ingredient in the present invention includes a white portion of the skin which is a citrus mesocarp and contains many water-soluble dietary fibers such as pectin, flavonoids such as naringin and hesperidin. Say what you are.

  Albedo used as an active ingredient in the present invention may be albedo itself, but albedo is processed and used to the extent that the pharmacological effect (decrease in blood glucose level or improvement of bowel movement) intended in the present invention is not invalidated. May be. For example, (1) Albedo itself, with skin attached to it, whole fruit ground, (2) (1), soaked in water, ethanol, liquor, plum vinegar, honey, etc. (3 ) (1) made into syrup, jelly, paste, jam, etc., (4) dried from (1), (5) pulverized from (4), or fine powder, (6) those obtained by steam distillation or solvent extraction of (1), (4), (5) etc., or residues, (7) (1), (4) , (5), etc., and (8) any of the above, processed into a pharmaceutical form. In the case of a pharmaceutical form, it may be any commonly used dosage form, such as powders, tablets, powders, granules, capsules, troches, syrups, soft gelatin capsules, pastes, etc. Can be mentioned.

  The albedo used as an active ingredient in the present invention can be taken as it is or in addition to food or beverage. When added to food or beverage, the type of food or beverage used is not limited. Examples of the food include use for confectionery such as bread, cake, donut, chocolate, candy, biscuits, jelly, yogurt and manju, seasonings such as sauce and dressing, side dishes, processed foods and the like. . Prepared meals are cereals, potatoes, seeds, beans, seafood, animal fowls, eggs, vegetables, mushrooms, algae, and mixtures thereof, baked, roasted, fried, fried, steamed , Boiled, boiled and so on. Examples of beverages include beverages such as coffee, tea, green tea, Chinese tea, cocoa and other favorite beverages, soft drinks, juices such as apples, oranges, grapefruits and grapes, and liquors such as liqueurs. Can be mentioned.

The intake of a hypoglycemic agent and a bowel movement improving agent containing citrus albedo as an active ingredient in the present invention varies depending on various factors such as age, weight, and sex. For example, grapefruit albedo is ventilated at 60 ° C. for 24 hours. The dry powder obtained by 60 mesh pass is preferably 2 to 3 g per day for an adult (body weight 60 kg), preferably taken once to several times a day. As the intake period, a period exceeding 3 weeks is preferable, and 4 weeks or more is particularly preferable. As for acute toxicity, it is derived from natural products and is safe. The LD ₅₀ using a mouse is 2 g / kg or more.

  EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples, but the present invention is not limited to these examples.

Albedo powder was prepared using grapefruit. First, 400 g of fresh grapefruit fruit was washed and trimmed (peeled) to obtain 30 g of albedo, followed by hot air drying at 60 ° C. for 24 hours to obtain 7.4 g of dried albedo. It was finely pulverized and sieved to prepare a 60 mesh pass albedo powder.
Thirteen healthy adult men and women with a fasting blood glucose level of 110 mg / dl or higher and a BMI index of about 19-30, each with 2 grams of prepared grapefruit albedo powder after a daily lunch or dinner for 4 weeks And dissolved in water. On the day before the examination, eating and drinking after 9 pm was prohibited, and blood was collected from the vein on the side of the flexor arm. Test items are biochemical tests (blood glucose level, HbA ₁ c, fructosamine, glycoalbumin, insulin, total protein, total cholesterol, HDL-C, neutral fat, GOT, GPT, LDH, γ-GTP, creatinine, urea nitrogen, Uric acid, albumin, Na, K, Cl), general blood test (white blood cell count, red blood cell count, hemoglobin, hematocrit, platelet count), urine test (pH, protein, sugar, occult blood), others (height, weight, blood pressure, pulse) Number). Results of biochemical tests and body weight are shown in Table 1.

  From the results in Table 1, 10 out of 13 subjects showed a decrease in blood glucose level, and a significant decrease (P <0.01) was observed. Therefore, grapefruit albedo may have a blood glucose level lowering effect. It could be confirmed.

  In the same manner as in Example 1, the prepared grapefruit albedo powder was ingested by 13 healthy subjects by dissolving 2 g per day in a glass of water after lunch or dinner every day for 4 weeks. During the ingestion period, a diary was recorded on the number of defecations and stool tone. Table 2 shows the results of the number of defecations.

  From the results in Table 2, the number of bowel movements increased significantly in the second week, and the effect of improving bowel movement was confirmed.

  Using the grapefruit albedo powder prepared in Example 1, the raw materials were prepared based on the preparation recipe in Table 3, sterilized at 95 ° C., and then filled into a 190 g steel can to produce a grapefruit beverage. The charging composition is shown in Table 3.

  As a result of eating 190 g of the present invention 1 and 2 every day, a blood glucose level lowering action was observed, and stool communication was also improved. In 190 g, the present invention 1 includes 2.2 g of albedo powder, and the present invention 2 includes 3.0 g of albedo powder.

Grapefruit albedo powder prepared in Example 1 (920 g), crystalline cellulose (50 g), and sucrose fatty acid ester (30 g) were blended and compressed to produce grapefruit albedo tablets (present invention 3). One tablet is 200 mg. Tableting conditions are ^{1kg / cm 2 ~2kg / cm 2} .

  When the present invention 3 was eaten 4 to 5 tablets once a day and 2 to 3 times a day (approximately 11 tablets a day), a blood glucose level lowering action was also observed, and stool communication was also improved.

Grapefruit is washed and the outer skin is trimmed (peeled) to leave an albedo. At the same time, remove foreign matter and rot. Next, the enzyme is deactivated by dipping in boiling water at 98 ° C., and then rapidly frozen by a blow freezing method in which low-temperature cold air is passed through the fruit at high speed. The frozen grapefruit is roughly crushed with a hammer crusher and then ground using a super mass collider with a clearance adjusted to 200 μm. After grinding, the mixture was homogenized with a high-pressure homogenizer to obtain a grapefruit ground product. 1 kg of the obtained ground product contains 18.5 g of albedo in terms of dry matter.
This grapefruit ground product is used as the main ingredient, and the raw materials are prepared based on the preparation table in Table 4, sterilized at 95 ° C, filled into 2 liter PET bottles, and a grapefruit 50w / w% fruit juice beverage ( Invention 4) was prepared. The charging recipe is shown in Table 4.

  When 220 g of the present invention 4 was eaten every day, a blood glucose level lowering action was also observed, and stool communication was improved. In addition, in this invention 4, the albedo powder equivalent to 2.0g is contained in this invention 4.

Using diabetic mice (C57BLKS / J Iar− + Lepr ^db / Lepr ^db ), the hypoglycemic effect of grapefruit albedo powder prepared in the same manner as in Example 1 was examined.
Seventeen-week-old diabetic mice (C57BLKS / J Iar− + Lepr ^db / Lepr ^db ) were used for 21 weeks of acclimatization, blood was collected, and 7 groups were assigned to 3 groups according to blood glucose level.
Each dose of the test substance (grapefruit albedo powder) was mixed with a normal diet (powder feed CE-2, manufactured by CLEA Japan, Inc.) and allowed to freely ingest for 4 weeks. In the meantime, drinking water was freely consumed by public tap water. As the test group, one group consisted of 7 animals, and the control group, the low dose group, and the high dose group consisted of 3 groups.
The control group was fed only a normal diet without grapefruit albedo powder. The low dose group was fed with 2% grapefruit albedo powder as a normal diet, and the high dose group was fed with 5% diet as a feed.
After the start of administration, body weight is measured once a week, and blood sampling is performed 3 times in total at the start of administration (day 0), 2 weeks after the start of administration, and at the end of the administration (after 4 weeks of administration) to measure blood glucose levels Went.
Table 5 shows the average blood glucose level during the breeding period.

From the results shown in Table 5, a dose-dependent decrease in blood glucose level was observed 4 weeks after the start of administration when comparing the control group given only the normal diet with the grapefruit albedo powder administration group (low dose group, high dose group). .
In the control group, it increased from 170.4 mg / dl at the start of administration (day 0) to 255.3 mg / dl 4 weeks after the start of administration, whereas in the low dose group, 213.4 mg / dl. In the high dose group, it was 183.4 mg / dl, and it was confirmed that the grapefruit albedo powder has a blood glucose lowering effect.
In a very short period of 4 weeks after the start of administration, it showed a high blood glucose level lowering effect.

The hypoglycemic agent and the bowel movement improving agent comprising the citrus albedo of the present invention as an active ingredient can be ingested as they are, and are useful because the hypoglycemic agent and the bowel movement improving agent can be added to foods or beverages. It is. In addition, a large amount can be ingested at one time, which is excellent in safety and can be expected to lower blood glucose level and improve bowel movement more effectively. In addition, daily intake of this hypoglycemic agent and bowel movement-improving agent can be expected to reduce or prevent symptoms of lifestyle-related diseases caused by dietary habits, exercise habits, rest, smoking, drinking and other eating habits. In addition, the use of albedo, which is normally discarded, as an active ingredient is an industrially useful invention from the viewpoint of utilizing natural product waste.

Claims (6)

  A hypoglycemic agent comprising citrus albedo as an active ingredient.   A bowel movement improving agent comprising a citrus albedo as an active ingredient.   2. The hypoglycemic agent according to claim 1, wherein the citrus fruit is grapefruit.   The stool is a grapefruit, The bowel movement improving agent of Claim 2 characterized by the above-mentioned.   A food or beverage for lowering blood glucose, comprising the blood glucose lowering agent according to claim 1 or 3.   A food or beverage for improving bowel movements comprising the bowel movement improving agent according to claim 2 or 4.