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Application of E ring bromine substituted silybin to preparing glycosidase inhibitors

A technology of silybin ester and bromine substitution, which is applied in the direction of drug combination and metabolic diseases, can solve the problems of diabetes without glycosidase inhibition, achieve clear industrialization prospects, benefit energy saving and emission reduction, and effectively inhibit α- The effect of glucosidase

Inactive Publication Date: 2012-08-22
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 E ring bromine substituted silybin to preparing glycosidase inhibitors
  • Application of E ring bromine substituted silybin to preparing glycosidase inhibitors
  • Application of E ring bromine substituted silybin to preparing glycosidase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Formula (1) (±)-2-[2,3-dihydro-3-(3-bromo-4-hydroxyl-5-methoxyphenyl)-2-hydroxymethyl-1,4-benzo Preparation of dioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0023] 1.1 Instruments and reagents:

[0024] 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 ...

Embodiment 2

[0032] Example 2 : Compound (1) (±)-2-[2,3-dihydro-3-(3-bromo-4-hydroxyl-5-methoxyphenyl)-2-hydroxymethyl-1,4-benzene Inhibitory activity of dioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-chromen-4-one on α-glucosidase

[0033] 2.1 Instruments and reagents

[0034] 2.1.1 Experimental Instruments

[0035] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)

[0036] 2.1.2 Reagents

[0037] 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).

[0038] 2.2 Test method

[0039]The inhibitory effect of compounds on α-glucosidase was determined by colorimetric method. Add phosphate buffer (67 mmol / L, pH 6.8, 170 microliters), reduced glutathione (1 mg / ml, 5 microliters), α-D-glucosidase (diluted into 0.2U / ml, 25 μl), compound (1) was dissolved in DMSO, diluted with phosphate buffer, 25 μl per well, so that the fi...

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Abstract

The invention relates to application of E ring bromine substituted silybin to preparing glycosidase inhibitors and in particular discloses application of E ring bromine 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 flavonolignans for inhibiting alpha-glycosidase reaches 77.1% under the condition of 4mcg / ml concentration. The measured half-inhibitory concentration of the flavonolignans shows that the intensity of activity of the flavonolignans for inhibiting alpha-glycosidase is 32 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 silibinin ester type flavonoid lignan substituted by E-ring bromine or a pharmaceutically acceptable salt thereof for the preparation of α-glucosidase-inhibiting, prevention and treatment type II Diabetes is also the application in non-insulin-dependent diabetes mellitus medicine, and this flavonoid lignan has extremely significant activity of inhibiting α-glucosidase, and its inhibitory activity intensity to α-glucosidase has already been obtained at a concentration of 40 micrograms / ml. Reach 77.1%, show by measuring its half maximal inhibitory concentration: the intensity that this flavonoid lignan inhibits α-glucosidase is 32 times that of positive control drug acarbose, so this compound or its pharmaceutically acceptable salt, and with The pharmaceutical composition prepared from the pharmaceutical excipients or carriers allowed by the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P3/10
Inventor 杨自忠周琪王琳杨明慧巫秀美赵昱谭仁祥
Owner DALI UNIV
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