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Application of B ring methoxy substituted silybin to preparing glycosidase inhibitors

A technology of silibinin ester and methoxy group is applied in the field of pharmaceutical use of B-ring methoxy silibinin for preparing glycosidase inhibitors, which can solve the problems such as diabetes that have not been inhibited by glycosidase, and achieve industrial Clear prospects, convenient sources, huge social and economic benefits

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 ring methoxy substituted silybin to preparing glycosidase inhibitors
  • Application of B ring methoxy substituted silybin to preparing glycosidase inhibitors
  • Application of B ring methoxy substituted silybin to preparing glycosidase inhibitors

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Example 1: Compound of formula (1) (±)-2-[2,3-dihydro-3-(3-methoxy-4-hydroxyphenyl)-2-hydroxymethyl-8-methoxy-1,4 Preparation of -benzodioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[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-...

Embodiment 2

[0036] Example 2 : Compound (1) (±)-2-[2,3-dihydro-3-(3-methoxy-4-hydroxyphenyl)-2-hydroxymethyl-8-methoxy-1,4 Inhibitory activity of -benzodioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one on 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 the compound on α-glucosidase is determined by colorimetry: add phosphate buffer (67 mmol / liter, pH 6.8, 170 microliters), reduced glutathione (1 mg / ml, 5 microliter), α-D-glucosidase (diluted to 0.2U / ml with phosphate buffer, 25 microliters), compound (1) was dissolved in dimethyl sulfoxide, diluted with phosph...

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Abstract

The invention relates to application of B ring methoxy substituted silybin to preparing glycosidase inhibitors and in particular discloses application of B ring 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 75.6%. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 8 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 type flavonoid lignan substituted by a B-ring methoxy group 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 75.6%, and it is shown by measuring its half-maximum inhibitory concentration: the intensity of the flavonoid lignan to inhibit α-glucosidase is 8 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 i...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P3/10
Inventor 毛本勇徐艳何正春段利华巫秀美赵昱陈忠
Owner DALI UNIV
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