KR20090125918A - Antidiabetic composition and method of manufacturing the same - Google Patents

Abstract

PURPOSE: An antidiabetes composition containing isoquercetin and a method for preparing the same are provided to treat diabete due to pancreatic beta cell by streptozotocin and suppress diabetes. CONSTITUTION: An antidiabetes composition contains isoquercetin, rutin, quercetinin, quercetin or quercetin glydoside. The total amount of isoquercetin and quercetin glydoside is over 90%. A method for preparing the composition comprises: a step of adding water to plant containing isoquercetin, rutin, quercetinin, quercetin or quercetin glydoside, pulverizing and concentrating; a step of mixing water and methylacetate then shaking; a step of removing precipitate by centrifuging and decompress-concentrating supernatant to remove methylacetate; a step of falling temperature to obtain precipitate; and a step of drying the precipitate.

Description

Antidiabetic composition and method of manufacturing the same {Antidiabetic composition and method of manufacturing the same}

The present invention relates to an anti-diabetic composition and a method for producing the same, and more particularly, to an anti-diabetic composition containing isoquecetin, which is a quercetin glycoside, and a method for producing the same.

Diabetes mellitus is an adult disease that includes the most risk factors at present, and the number of patients is increasing as the diet of Korea becomes westernized. Diabetes is a type 1 diabetes (insulin-dependent diabetes mellitus) caused by the breakdown of pancreatic beta cells caused by genetics, viruses, or harmful compounds. Type 2 diabetes (type 2 diabetes, noninsulin-dependent diabetes mellitus), which is inefficient in insulin due to abnormalities in receptors and signaling related substances, can be classified as diabetic retinopathy if it lasts for a long time without proper treatment. Causes severe damage to the eyes, diabetic nephropathy, and kidneys, and diabetic neuropathy, to nerves, and eventually to death Disease (see Harrison, TR, Diabetes Mellitus: Principles of internal medicine 11th ed. 1778-1797, 1987; Mahler, RJ, and Adler, M.L., Type 2 Diabetes Mellitus: Update on diagnosis, pathophysiology, and treatement. J. Clin. Endocrinol. Metab. 84 (4), 1165-1169, 1999). Patent Registration 10-0354912)

In Korea, type 2 diabetes is distributed at a ratio of 1: 9 type 1 diabetes rather than type 1 diabetes, and the incidence rate is rising exponentially. Therefore, the onset of diabetes and mortality due to diabetes are increasing every year. The prevalence of diabetes was estimated to be less than 1% in Korea in 1970, about 3% in the late 1980s and 5-8% in the 1990s (Korean Diabetes Association, Diabetes, Seoul, Korea Medicine). , 1998).

Type 1 diabetes can be solved by insulin administration because of the lack of insulin in the pancreas, but there are limitations (Ramiya, VK, Maraist, M., Arfors, KE, Schatz, DA, Peck, AB, Cornelius, JG). , Reversal of insulin-dependent diabetes using islets generated in vitro from pancreatic stem cells.Nat Med 6 (3), 278-282, 2000).

Treatment of type 2 diabetes is first. By reducing the absorption of fats and carbohydrates due to dietary control, diabetes is being prevented and treated. Second, exercise therapy can increase blood sugar and increase the sensitivity to insulin by aerobic exercise. (American Diabetes Association.Care of children with diabetes in the school and day care setting.Diabetes Care, 22 (1), 163-6, 1999). Third, oral hypoglycemic agents that promote insulin secretion of sulfonyl urea lines, biguanides that increase insulin sensitivity, and direct insulin application and other methods are widely used as drug therapy.

These methods are mainly parallel with the diet and are representative of alpha-glucosidase inhibitors. However, these drugs, which are currently used for the treatment of diabetes, are not fully effective in treating diabetes and do not act at all on secondary complications. (Mahler, R. J., Adler, M, L., Type 2 Diabetes Mellitus: Update on diagnosis, pathophysiology, and treatement. J. Clin. Endocrinol. Metab. 84 (4), 1165-1169, 1999).

Conventionally, there has been an experimental report on diabetes using herbal medicine in Korea. Kim et al. Reported that Baek-Ho-Tang inhibits hypoglycemic and insulin secretion, and decreases the activity of various enzymes. (1, 5, 1983), Lee et al., A study on the effect of goji berry on the activity of blood sugar and various enzymes. Seoul, 250-268, 1980). In addition, Huh et al., The Effect of Gamiyukmiji Hwang-tang (加味 六味 地 黃 湯, 許 鍾 會, 加味 六味 地 黃 湯) on the Concentration of Streptozotocin Whites, 慶 熙 大 學校 校 文集, 7, 135-152, 1984) Cheongshimyeonjaum lowers blood sugar levels in streptozotocin-treated rats (萬 浣 萬 浣, 淸 心 蓮子 飮 Extract acid on the effects of 消渴. 東 国 大 學校 大院, 1987), Kwak has reported that YIMJi Hwangtang acid medicine lowers blood sugar levels in alloxan-induced diabetic rats (桂 桂, 六味 地 黄 湯加 山藥) Impact, Graduate School, Daejeon University, 1992).

In the manufacture of the decoctions described above, vegetable antioxidants are often used. Therefore, it has been shown that quercetin, a plant antioxidant, is administered at a dose of 15 mg / kg / day for 4 weeks to suppress the diabetes induced by streptozotocin. ( Pharmacol Res , 51 (2): 117-23.2005. Coskun O, Kanter M, Korkmaz A, Oter S)

However, quercetin is administered intraperitoneally, but its efficacy is shown in oral administration. This is because quercetin itself has a disadvantage in that the absorption rate of the human body falls.

Also, the most easily consumed foods are drinks such as drinks. In addition, various beverages currently on the market use both white sugar and liquid fructose, which is highly likely to cause diabetes, and when the diabetic is ingested, there is a high possibility of blood sugar shock.

Therefore, it does not affect blood sugar, and screens for substances that can prevent diabetes in the long term and have anti-diabetic activity, and manufactures 'Active-X', which is a group of additives that combine them, and develops beverages containing them. It will have a great effect on prevention and suppression.

Accordingly, an object of the present invention is to provide an antidiabetic composition and a method for producing the same, which have superior effects to quercetin in preventing and inhibiting diabetes and controlling blood sugar.

The antidiabetic composition according to the present invention for achieving the above object, at least one selected from the group consisting of quercetin glycosides other than isoquecetin, rutin, quercetinin, quercetin, isoquecetin, wherein the isoquecetin is the main component It is necessarily included as.

In this case, it is preferable that content of the sum of the said isoquircetin and quercetin glycosides other than the said isoquircetin is 90% or more.

In addition, the method for producing an antidiabetic composition according to the present invention for achieving the above object,

Adding at least one selected from the group consisting of quercetin glycosides other than isoquircetin, rutin, quercetinin, quercetin, and isoquircetin, and pulverizing and concentrating water by adding water to a target plant which isoquecetin must include as a main component Wow;

Mixing and shaking methyl acetate and water in the concentrated product;

Centrifuging the shaken product to remove the precipitate, and concentrating the supernatant under reduced pressure to remove methyl acetate;

Rapidly cooling the resultant from which the methyl acetate has been removed to form a precipitate;

Drying the precipitate;

Characterized in having a.

According to the present invention, streptozotocin is responsible for the destruction of the pancreatic beta cells or the autoimmune reaction and the pancreatic beta cells. Bring it. In addition, even when the composition according to the present invention is administered prior to the administration of the streptozotocin, a diabetes-inducing drug, it is very useful in the biopharmaceutical industry because it has an excellent effect of preventing beta cell destruction of the pancreas by streptozotocin and inhibiting diabetes. .

Hereinafter, with reference to the accompanying drawings, preferred embodiments of the present invention will be described in detail. The following examples are only presented to understand the content of the present invention, and those skilled in the art will be capable of many modifications within the technical spirit of the present invention. Therefore, the scope of the present invention should not be construed as limited to these examples.

[Formula of the substance used in the Example of this invention]

The antidiabetic composition of the present invention includes at least one selected from the group consisting of isoquecetin, rutin, quercetinin or quercetin, and isoquecetin is necessarily included as a main component. The chemical formula of these materials is shown in FIG.

[Preparation of Plant Extract Containing Quercetin Glycosides]

Quercetin glycoside isoquecetin, rutin or quercetinin, arure, onion and rooibos known to have high content of quercetin were extracted according to the following method. The extraction process is as follows.

1) To about 500 grams of the target plant, add about 1000 ml of water and grind completely.

2) Concentrate them.

3) Mix the concentrated plant paste with methyl acetate / water (9: 1) and shake at 45 ° C. for 4 hours.

4) The resultant of 3) is centrifuged to remove the precipitate, and the supernatant is concentrated under reduced pressure to remove methyl acetate.

5) When the resultant product of 4) is rapidly reduced to 10 ° C, a precipitate is formed.

6) Dry the precipitate.

When using this dried product, it was dissolved in calcium carbonate buffer (pH 9.0) and used.

[Anti-diabetic beverage composition]

A basic composition for making an antidiabetic beverage was prepared as follows.

Base composition of the anti-diabetic beverage is as follows.

matter Drinks 1 Drinks 2 Drinks 3 Drinks 4 Drinks 5 Drinks 6 Drinks 7 Acesulfame K 0.8 0.8 0.8 0.8 0.8 0.8 0.8 Sucralose 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Amino acid complexes 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Isoquercetin 0.1 Routine 0.1 Arbor extract 0.1 Rooibos extract 0.1 Onion Extract 0.1 Soybean Extract 0.1 Calcium carbonate A reasonable amount A reasonable amount A reasonable amount A reasonable amount A reasonable amount A reasonable amount A reasonable amount water system 100 100 100 100 100 100 100

Experimental Example 1. Effect of Inhibition of Diabetes Induction by Streptozotocin of Quercetin and Quercetin Glycosides

Quercetin and isoquircetin, rutin, quercetinin were applied to experimental mice (Balb / c) at mg / kg orally once a day for 7 days, and then streptozotocin 250 mg / kg was administered to the abdominal cavity of the mouse to induce diabetes. I was. After 48 hours, the change in blood glucose was measured according to each administration group to confirm the occurrence of diabetes.

At this time, it was determined that the mouse blood sugar was 120 mg / dL or less, and it was determined that diabetes was 200 mg / dL or more, and it is summarized in Table 1 below. Table 1 shows the diabetes-induced inhibition rate for each substance, and the result of pre-administration of each substance and the induction of diabetes. (QU: Quercetin. IQ: Isoquecetin, RU: Routine, QN: Quercetinin)

No addition QU IQ RU QN IQ + RU IQ + QN RU + QN IQ + RU + QN Suppression rate 0% 0% 80% 70% 20% 100% 90% 60% 90%

In addition, Figure 2 shows a bar graph showing the diabetes-induced inhibition rate of the complex of isoquecetin, rutin and quercetinin, quercetin isoquecetin, rutin and quercetin.

Experimental Example 2: Diabetes-induced Inhibitory Effect of Quercetin and Quercetin Glycosides 2

Immediately after administering streptozotocin 250mg / kg to the mouse abdominal cavity, quercetin and isoquecetin, rutin, and quercetinin were applied to experimental mice (Balb / c) at 5mg / kg once a day for 7 days after oral administration. Diabetes mellitus was measured by measuring the change in blood glucose according to the administration group.

At this time, the standard was determined that the mouse blood sugar is less than 120mg / dL, and it is determined that the induction of diabetes more than 200mg / dL is shown in Table 2 and Figure 3, unlike the Experimental Example 1 and induced diabetes first, respectively Post-administration of the material is shown. (QU: Quercetin. IQ: Isoquecetin, RU: Routine, QN: Quercetinin)

No addition QU IQ RU QN IQ + RU IQ + QN RU + QN IQ + RU + QN Suppression rate 0% 0% 70% 50% 0% 40% 30% 10% 20%

Experimental Example 3: Effect of Inhibiting Diabetic Induction of Isoquercein and Plant Extracts]

Arsenal, rooibos, and onion (dried) are extracted by the same method as described in the section `` Preparation of plant extracts containing quercetin glycosides '', and the extract is calibrated to 5mg / kg once a day orally for 7 days. Diabetes was induced by streptozotocin 250 mg / kg intraperitoneally.

Diabetes induction was confirmed by measuring blood glucose levels in mice 48 hours after streptozotocin administration. At this time, it was determined that the mouse blood sugar was 120 mg / dL or less, and it was determined that diabetes was 200 mg / dL or more. The results are shown in Table 3 and FIG.

No addition IQ Thrust Rooibos onion bean Content of Quercetin Glycosides 0 > 90% > 90% > 90% > 90% > 90% % Inhibition 0 90 100 80 100 100

Experimental Example 4: Diabetes-induced Inhibitory Activity of Mice According to the Dose of Isoquecetin and Rutin]

Isocercetin and rutin were orally administered to the mice once a day for 7 days at each concentration, and then streptozotocin 250 mg / kg was administered to the mouse abdominal cavity to induce diabetes. Diabetes induction was confirmed by measuring blood glucose levels in mice 48 hours after streptozotocin administration. At this time, it was determined that the mouse blood sugar was 120 mg / dL or less, and it was determined that diabetes was 200 mg / dL or more. The results are shown in Table 4 and FIG.

Dosage concentration (mg / kg) 0 One 2 3 4 5 6 7 8 9 10 Isoquercetin 0 20% 50% 80% 90% 90% 90% 90% 90% 90% 90% Routine 0 0 30% 50% 70% 80% 90% 90% 90% 90% 90%

Experimental Example 5: Glucose tolerance after ingesting a prepared beverage containing isoquecetin, rutin and plant extract

Streptozotocin was administered to mice at a concentration of 250 mg / kg, and 48 hours later, mice with diabetes mellitus with a blood sugar level of 200 mg / dL or higher were intraperitoneally administered at 100 mg / 100 grams based on the mouse's weight. After applying oral administration of each plant extract to the beverage formulation according to Example 2 and oral administration by 0.1mL, glucose tolerance was measured by each glycemic reaction, but the hypoglycemic ability of the ingested food was not found. Therefore, in the present invention, it was determined that there is no effect of inhibiting blood glucose absorption in the case of the plant extract containing isoquecetin or isoquecetin. The results are shown in Table 5 below.

No addition IQ Thrust Rooibos onion bean Content of Quercetin Glycosides 0 > 90% > 90% > 90% > 90% > 90% % Inhibition 0 Less than 10% Less than 5% 0 0 Less than 21%

Experimental Example 6: Changes in Blood Glucose after Long-term Ingestion of Prepared Drinks Containing Isoquecetin, Rutin and Onion Extracts after Induction of Diabetes]

Streptozotocin was administered to mice at a concentration of 250 mg / kg, and after 48 hours, mice with diabetes mellitus with blood sugar levels of 200 mg / dL or higher were treated with mice receiving a beverage containing onion extract containing isoquecetin and isoquecetin. The blood glucose change over two months was observed while taking twice daily at a concentration of 5 mg / kg. The diet of the mice was free diet. The results are shown in FIG. As can be seen with reference to Figure 6, when the long-term administration of both isoquecetin and onion extracts containing isoquecetin, blood sugar was significantly reduced after about 15 days and one month was found to return to almost normal blood sugar.

However, the mice that did not take the mice began to die from the 7th day of the experiment and all died within 10 days. The average blood glucose of the mice until just before death was 472 ± 81 mg / dL.

Judging from the results of the above experiments, at least one selected from the group consisting of quercetin glycosides other than isoquecetin, rutin, quercetinin, quercetin, and isoquecetin, characterized in that the isoquecetin is necessarily included as a main component. The anti-diabetic composition was confirmed to show an excellent effect in restoring the blood sugar level to the normal level, or inhibit the development of diabetes itself when diabetes occurs. In the anti-diabetic composition, when the content of isoquecetin and a combination of quercetin glycosides other than isoquecetin is greater than 90%, a better effect was obtained. Therefore, when the beverage is made using such an anti-diabetic composition, both the diabetic patient and the general public can enjoy the effect of being free from the pain of blood sugar while taking it comfortably.

1 is a view showing the chemical structure of the material contained in the antidiabetic composition of the present invention;

2 is a graph showing the results of experiments to determine the effects of streptozotocin-induced diabetes of quercetin and quercetin glycosides;

Figure 3 is a graph showing the results of another experiment to determine the effect of inhibiting diabetes induced quercetin and quercetin glycosides;

Figure 4 is a graph showing the results of the experiment to determine the effect of inhibiting the diabetes-induced diabetic quercetin (Isoquercein) and each plant extract;

Figure 5 is a graph showing the results of the experiment to determine the effect of diabetic induction according to the dosage of isoquecetin and rutin;

Figure 6 is a graph showing the results of experiments to determine the long-term blood glucose changes according to the administration of isoquecetin and onion extracts.

Claims (3)

An antidiabetic composition, characterized in that it contains at least one selected from the group consisting of quercetin glycosides other than isoquircetin, rutin, quercetinin, quercetin, and isoquircetin, and the isoquecetin is necessarily included as a main component. 2. The antidiabetic composition according to claim 1, wherein the content of the sum of the isoquircetin and quercetin glycosides other than the isoquircetin is 90% or more. Adding at least one selected from the group consisting of quercetin glycosides other than isoquircetin, rutin, quercetinin, quercetin, and isoquircetin, and pulverizing and concentrating water by adding water to a target plant which isoquecetin must include as a main component Wow; Mixing and shaking methyl acetate and water in the concentrated product; Centrifuging the shaken product to remove the precipitate, and concentrating the supernatant under reduced pressure to remove methyl acetate; Rapidly cooling the resultant from which the methyl acetate has been removed to form a precipitate; Drying the precipitate; Method for producing an antidiabetic composition comprising a.

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