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Application of B/E ring changed silybin to preparing glycosidase inhibitors

A technology of silybin esters and compounds, which is applied in the field of pharmaceutical use of silibinin with changes in the B/E ring for the preparation of glycosidase inhibitors, can solve the problems of diabetes without glycosidase inhibition, and achieve industrialization Clear prospect, beneficial to energy saving and emission reduction, simple and easy preparation method

Inactive Publication Date: 2011-04-06
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But it is obvious: the above studies have only focused on the antioxidant and cytoprotective effects of silybin flavonoid lignans
[0007] Although the flavonoid lignan compounds represented by silibinin and dehydrosilibinin have the above-mentioned antioxidant effects, there are no reports on their use in inhibiting glycosidase and treating diabetes

Method used

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  • Application of B/E ring changed silybin to preparing glycosidase inhibitors
  • Application of B/E ring changed silybin to preparing glycosidase inhibitors
  • Application of B/E ring changed silybin to preparing glycosidase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Preparation of formula (1)

[0022] 1.1 Instruments and reagents:

[0023] The ultraviolet spectrum was measured with a Shimadzu UV-240 ultraviolet spectrophotometer; the hydrogen nuclear magnetic resonance spectrum 1 H-NMR is measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS is the internal standard); (100-200, 200-300 and 300-400 mesh) and silica gel GF254 (10-40 mesh) for thin-layer chromatography are all produced by Qingdao Ocean Chemical Factory; the reagents used are all analytically pure; thin-layer preparative chromatography (PTLC ) uses the aluminum foil silica gel plate of Merck Company; Sephadex LH-20 used for column chromatography adopts the product of Amersham Pharmacia Biotech AB Company of Sweden; Reversed-phase silica gel RP-18 adopts the Chromatorex product of Fuji Silysia Chemical Company of Japan; MCI is the product of Mitsubishi, Japan Chemical company produc...

Embodiment 2

[0036] Example 2 : Compound (1) is tested for the inhibitory activity of α-glucosidase

[0037] 2.1 Instruments and reagents

[0038] 2.1.1 Experimental Instruments

[0039] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)

[0040] 2.1.2 Reagents

[0041] α-glucosidase is α-D-glucosidase (Sigma, 500U / ml); 4-nitrophenol-α-D-glucopyranoside (PNPG, Merck), reduced glutathione (Shanghai Shenggong) , Acarbose is Baitangping (Bayer Healthcare Co., Ltd., Beijing).

[0042] 2.2 Test method

[0043] The inhibitory effect of compounds on α-glucosidase was determined by colorimetric method. Add phosphate buffer (67 mmol / L, pH6.8, 170 microliters), reduced glutathione (1 mg / ml, 5 microliters), α-D-glucosidase (diluted with phosphate buffer into 0.2U / ml, 25 microliters), compound (1) was dissolved in dimethyl sulfoxide, diluted with phosphate buffer, 25 microliters per well, so that the final concentration was 0.04 mg / ml, 0.004 mg / ml, 0.0004 mg / ml, finally add the ...

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Abstract

The invention relates to application of B / E ring changed silybin to preparing glycosidase inhibitors and in particular discloses application of B ring ethyoxyl or E ring de-methoxy substituted silybin ester-type flavonolignans or pharmaceutical salt thereof to preparing drugs for inhibiting alpha-glycosidase and preventing and treating type II diabetes. The flavonolignans has extremely obvious activity for inhibiting alpha-glycosidase and the intensity of activity of the 40mcg / ml flavonolignans for inhibiting alpha-glycosidase reaches 54.3%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 2.5 times that of the positive control drug acarbose. The pharmacodynamics result shows that the flavonolignans or pharmaceutical salt thereof can be expected to be applied to preparing glycosidase inhibitors, especially the drugs for preventing and treating type II diabetes.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a kind of silybin ester type flavonoid lignan or its pharmaceutically acceptable salt which is substituted by B ring ethoxy group and E ring demethoxy group is used for the preparation of inhibitory α-glucosidase, prevention and treatment of type II diabetes, that is, the application of non-insulin-dependent diabetes mellitus drugs, the flavonoid lignans have a significant activity of inhibiting α-glucosidase, and it has an effect on α-glucosidase at a concentration of 40 micrograms / ml. The inhibitory activity intensity of glucosidase has reached 54.3%, shows by measuring its half maximal inhibitory concentration: the intensity of this flavonoid lignan inhibiting α-glucosidase is 2.5 times that of positive control drug acarbose, so this compound or its The pharmaceutically acceptable salt and the pharmaceutical composition prepared with pharm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P3/10
Inventor 巫秀美张丽娟陈可欣杨淬陶巧凤赵昱曾苏
Owner DALI UNIV
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