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Application of 4-cinnamoyl chloride substituted silybin in preparing glycosidase inhibitors

A technology of silibinin ester and glucosidase, which is applied in the direction of drug combination and metabolic diseases, can solve the problems of diabetes without glucosidase inhibition, and achieve clear industrialization prospects, strong inhibition of α-glucosidase, The effect of mass production on energy saving and emission reduction

Inactive Publication Date: 2012-10-10
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 4-cinnamoyl chloride substituted silybin in preparing glycosidase inhibitors
  • Application of 4-cinnamoyl chloride substituted silybin in preparing glycosidase inhibitors
  • Application of 4-cinnamoyl chloride substituted silybin in preparing glycosidase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 : the preparation of formula (1) compound

[0020] 1.1 Instruments and reagents:

[0021] 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 internal standard); Electrospray mass spectrometry ESI-MS is measured by Bruker Esquire3000+mass spectrometer, column chromatography uses silica gel ( 100-200, 200-300 and 300-400 mesh) and silica gel GF254 (10-40 mesh) for thin-layer chromatography are produced by Qingdao Ocean Chemical Factory; all reagents used are analytically pure; preparative thin-layer chromatography (PTLC) Aluminum foil silica gel plates from Merck were used; Sephadex LH-20 for column chromatography was produced by Amersham Pharmacia Biotech AB in Sweden; reverse-phase silica gel RP-18 was produced by Chromatorex fro...

Embodiment 2

[0026] Example 2 : The inhibitory activity detection of formula (1) compound to α-glucosidase

[0027] 2.1 Instruments and reagents

[0028] 2.1.1 Experimental Instruments

[0029] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)

[0030] 2.1.2 Reagents

[0031] 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).

[0032] 2.2 Test method

[0033] 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 a...

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Abstract

The invention relates to application of 4-cinnamoyl chloride substituted silybin to preparing glycosidase inhibitors and in particular discloses application of 4-cinnamoyl chloride substituted silybin ester 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 92.1%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 30 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 invention relates to the technical field of medicine, in particular, the invention relates to a silybin ester flavonoid lignan substituted with 4-chlorocinnamoyl or a pharmaceutically acceptable salt thereof for the preparation of inhibitors of α-glucosidase, prevention and treatment of Type II diabetes, that is, non-insulin-dependent diabetes mellitus, the flavonoid lignan has extremely significant inhibitory activity of α-glucosidase, and its inhibitory activity to α-glucosidase at a concentration of 40 μg / ml The intensity has reached 92.1%, and it is shown by measuring its half maximal inhibitory concentration: the intensity of the flavonoid lignan to inhibit α-glucosidase is 30 times that of the positive control drug acarbose, so the compound or its pharmaceutically acceptable salt, And the pharmaceutical composition prepared with pharmaceutical excipients or carriers allowed by the formulation can be expected to be used as a glycosidase inhibito...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P3/10
Inventor 申元英董晓武李海波武有聪巫秀美赵昱郑汉其
Owner DALI UNIV
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