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Buckwheat husk flavonoid extractive and applications as DPP4 inhibitor

A buckwheat husk flavonoid and extract technology is applied in the field of buckwheat husk flavonoids extract and as DPP4 inhibitor, can solve the problems of high price, large side effects and the like, and achieves the effect of strong inhibitory activity and obvious protective effect

Active Publication Date: 2015-09-16
JILIN AGRICULTURAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to solve the problem that DPP4 inhibitors in the market are all chemically synthesized drugs, which are expensive and have great side effects, and provide a pure natural and cheap buckwheat husk flavonoid extract

Method used

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  • Buckwheat husk flavonoid extractive and applications as DPP4 inhibitor
  • Buckwheat husk flavonoid extractive and applications as DPP4 inhibitor
  • Buckwheat husk flavonoid extractive and applications as DPP4 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Grind the dried buckwheat husks with a high-speed grinder, pass through a 60-mesh sieve, put them into a clean beaker, add distilled water 10 times the mass of the coarse powder, heat at 121°C for 20 minutes, then filter, and repeat the extraction of the filter residue twice . The filtrates were combined, concentrated in vacuum at 60°C to a paste, and freeze-dried for 24 hours to obtain the buckwheat husk flavonoids crude extract (BHEs), which was brown in color. The supernatant was prepared into a 1% stock solution, which was diluted for use in the test.

[0019] Take 25mg of BHEs and add 50ml of distilled water to dissolve, add 2 g of D101 macroporous resin treated by conventional methods, and place it in a shaker at 100 r / min for 24 h at room temperature; use 70% ethanol with 50ml of 70% ethanol to absorb the macroporous resin After soaking, place in a 100 r / min shaker at room temperature for 24 hours, filter out the macroporous resin, and the remaining liquid is...

Embodiment 2

[0021] Example 2 A buckwheat husk flavonoid extract BHEs-A Determination of DPP4 inhibitory activity

[0022] The BHEs-A inhibitor liquid and the standard solution were serially diluted to prepare 1.0, 0.5, 0.1, 0.05, and 0.01 mg / mL respectively for later use. Determined according to the method used in the DPP4 inhibitor kit of SIGMA company. Set up blank group, negative control group, positive control group, positive blank group, test group and color control group respectively. Sitagliptin inhibitor, DPP4 enzyme and substrate were diluted with buffer. A black 96-well plate was used for detection, and the total reaction system was 100 μL. Add 25 μL of sample to each group first, replace the blank group and negative control group with buffer, add Sitagliptin inhibitor to the positive control and positive blank group; then add 50 μL of diluted DPP4 enzyme to each group, add buffer to the blank group, positive blank and color control group Replace with 50 μL of buffer, mix...

Embodiment 3

[0027] Example 3 Study on the Improvement of Buckwheat Hull Extract (BHE) on Type Ⅱ Diabetes

[0028] Preparation of Type Ⅱ Diabetic Rat Model

[0029] Rats were raised in a standardized animal room with no food or water restrictions. One week later, several rats were randomly selected as the normal group. The rest of the rats were fed a high-fat and high-sugar diet for 4 weeks. After 4 weeks, fast for 12 hours, intraperitoneally inject streptozotocin (STZ) 30mg / kg, and inject again 1 week later. The control group was given 1% buffer solution 30 mg / kg as a placebo, and the fasting blood glucose value > 11.0 mmol / L after 72 hours was the modeling standard.

[0030] Test grouping and administration

[0031]The diabetic rats successfully modeled were randomly divided into 5 groups, plus the normal control group, a total of 6 groups. Fasting blood glucose was measured before the experiment. The rats in each group were grouped and gavaged as follows:

[0032] Normal gr...

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Abstract

The invention discloses a buckwheat husk flavonoid extractive. The extractive is prepared after steps: buckwheat husks are subjected to drying and crushing, water is added, high temperature high pressure extraction is carried out, filtering is carried out, and filtrate macroporous resin dynamic adsorption-elution is carried out. Experiments prove that after mice with II type diabetes are administrated with the extractive, a hypoglycemic effect is achieved. The level of INS in serum of mice with II type diabetes can be raised substantially, and the facts are proved that the buckwheat husk flavonoid extractive has an obvious function to pancreatic beta cells and promotes secretion of insulin to a normal level. The buckwheat husk flavonoid extractive shows strong inhibition activity to a DPP4 enzyme, and the effect is better than effects of rutin, quercetin and isoquercitrin, the buckwheat husk flavonoid extractive is a mixture, which illustrates that the buckwheat husk flavonoid extractive contains other effective components besides flavonoid compounds and can be employed as a natural DPP4 inhibitor. Buckwheat husks provide a new raw material source for auxiliary medicines preventing the II type diabetes, and the purified buckwheat husk flavonoid extractive can become a novel, safe and natural target medicine treating II type diabetes.

Description

technical field [0001] The invention belongs to the field of health food and medicine, and in particular relates to a buckwheat husk flavonoid extract and its use as a DPP4 inhibitor. Background technique [0002] Diabetes is a systemic metabolic disorder dominated by glucose metabolism disorders, and is listed as the third largest disease in the world. According to the onset characteristics, it can be divided into type Ⅰ (insulin-dependent) and type Ⅱ (non-insulin-dependent) diabetes, and the number of patients with type Ⅱ diabetes accounts for more than 90%. At present, oral hypoglycemic drugs are mainly biguanides, sulfonylureas, α-glucosidase inhibitors and other drugs. These drugs are likely to cause hypoglycemia in patients, with large side effects and limited tolerance. In recent years, with the deepening of research, a series of new antidiabetic drugs that can act on new targets and can continuously control blood sugar levels have emerged. [0003] DPP4, dipeptidyl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/70A23L1/29A61P3/10
Inventor 朴春红张羽胡耀辉王玉华于寒松刘俊梅代伟长李想李鹏程赵梓瀛
Owner JILIN AGRICULTURAL UNIV
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