Versulin derivative and its use in treatment of diabetes and its complication

A kind of technology of apigenin and derivatives, applied in the field of apigenin derivatives

Active Publication Date: 2007-11-21
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far there is no report about apigenin and its derivatives anti-diabetes and complications

Method used

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  • Versulin derivative and its use in treatment of diabetes and its complication
  • Versulin derivative and its use in treatment of diabetes and its complication
  • Versulin derivative and its use in treatment of diabetes and its complication

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1. Extraction and separation of apigenin derivatives

[0025] The 95% alcohol extract of fenugreek seeds is sequentially extracted with petroleum ether, ethyl acetate and n-butanol to obtain n-butanol extraction parts. The extraction part is first subjected to silica gel column chromatography, then separated by AB-8 macroporous resin column chromatography and polyamide column chromatography, and finally purified by ODS preparative chromatography to obtain 4 apigenin derivatives, which are as follows:

[0026] Compound 1: 6-C-D-xylose-8-C-D-galactosyl-apigenin glycoside, which has the following structure:

[0027]

[0028] Compound 2: 6-D-D-galactose-8-D-D-glucose-pigenin glycoside;

[0029] Compound 3: 6-C-D-arabinose-8-C D-galactosyl-apigenin glycoside; and

[0030] Compound 4: 6,8-di-D-galactosyl-apigenin glycoside.

[0031] Compound 1 is a yellow powder. HCl-Mg reaction was positive, phenol-H 2 SO 4 The reaction was positive. according to 1 H-NMR a...

Embodiment 2

[0038] Embodiment 2. Biological activity experiment

[0039] Effect of compound 1 on blood sugar in diabetic mice

[0040]Fifty Kunming mice were randomly divided into normal control group (10 mice) and to-be-made model group (40 mice). After fasting for 24 hours (without water), the mice in the model group to be established were rapidly injected with alloxan physiological saline solution at a dose of 60 mg / kg through the tail vein. After 72 hours, blood was taken from the tip of the tail to measure the blood glucose of the mice. The mice with a blood glucose value > 20.0mmol / L were selected as diabetic mice, and were divided into model group (10 mice), compound I group (50mg / kg, 10 mice), and The gliclazide positive drug group (80 mg / kg, 10 rats) was administered by intragastric administration for 18 consecutive days, and the blood glucose was measured on the 7th and 18th days, respectively. The data are represented by X±SD, and the difference between the means of the two g...

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PUM

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Abstract

An apiin derivative, its production, medicinal composition containing it and its usage in treatment of diabetes and its complication are disclosed. It can also be used to prepare hypoglycemic, hypolipidemic and cholesterol-lowering medicines with aldose reductase activity inhibiting function.

Description

technical field [0001] The present invention relates to apigenin derivatives, a preparation method thereof, a pharmaceutical composition containing apigenin derivatives and medicines for treating diabetes and complications thereof, especially for lowering blood sugar, blood fat, cholesterol and inhibiting aldose reductase active drug use. technical background [0002] Fenugreek seeds are a traditional Chinese herbal medicine, which has the effects of warming the kidney, dispelling cold and relieving pain. It has been reported that various components such as steroidal saponins, flavonoids, and alkaloids have been isolated from fenugreek. The use of fenugreek for the treatment of diabetes has already been reported at home and abroad (G. Ribes, Proceedings of the Society for Experimental Biology and Medicine, 1986, 182: 159-166; M.A. Riyad, Planta Med., 1988, 54: 286 ; R.D.Sharma, Nutrition Res., 1996, 16(8): 1331; L.Ali, Planta Med., 1995, 61: 358; Zhu Zhenhai, Sichuan Tradi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07H17/07C07D311/40A61K31/355A61K31/7048A61K9/20A61K9/48A61K9/70A61K9/08A61P3/06A61P3/10
Inventor 单俊杰任晋玮赵毅民
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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