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Medicinal application of flavanonol lignan in preparation glycosidase inhibitors

A dihydroflavonol lignan and drug technology, which is applied in drug combination, metabolic diseases, etc., can solve the problems of diabetes without glycosidase inhibition, and achieve clear industrialization prospects, low pollution, and huge social and economic benefits Effect

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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  • Medicinal application of flavanonol lignan in preparation glycosidase inhibitors
  • Medicinal application of flavanonol lignan in preparation glycosidase inhibitors
  • Medicinal application of flavanonol lignan in preparation glycosidase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Formula (1) compound (±)-2-[2,3-dihydro-3-(3-benzyloxy-4-hydroxyphenyl)-2-hydroxymethyl-1,4 benzodioxane -5] Preparation of -2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0022] 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 ge...

Embodiment 2

[0042] Example 2 : Compound (1) is (±)-2-[2,3-dihydro-3-(3-benzyloxy-4-hydroxyphenyl)-2-hydroxymethyl-1,4 benzodioxane Inhibitory activity of cyclo-5]-2,3-dihydro-3,5,7-trihydroxy-4H-1-chromen-4-one on α-glucosidase

[0043] 2.1 Instruments and reagents

[0044] 2.1.1 Experimental Instruments

[0045] Microplate reader: ELISA plate reader (Bio-Tek Instruments, USA)

[0046] 2.1.2 Reagents

[0047] α-glucosidase (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).

[0048] 2.2 Test method

[0049] 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 to 0.2U / ml, 25 μl), compound (1) was dissolved in DMSO, diluted with phosphate buffer, 25 μl per well, so that the final c...

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Abstract

The invention relates to medicinal application of flavanonol lignan in preparing glycosidase inhibitors, in particular to application of B-ring dioxane flavanonol lignan or pharmaceutically acceptable salts thereof in preparation medicines for inhibiting alpha-glucosidase and preventing type 2 diabetes. The flavone lignan has extremely obvious activity of inhibiting the alpha-glucosidase and has the activity strength of inhibiting the alpha-glucosidase at the concentration of 40 micrograms / milliliter of 93 percent; and a half inhibitory concentration test shows that: the strength of the flavone lignan of inhibiting the alpha-glucosidase is 1.2 times that of a positive contrast medicine acarbose. A pharmacodynamic result shows that the flavone lignan or the pharmaceutically acceptable salts thereof can be expected to serve as the glycosidase inhibitors, particularly serve as medicines for preventing the type 2 diabetes.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a dihydroflavonol lignan of B-ring dioxane or a pharmaceutically acceptable salt thereof for the preparation of inhibiting α-glucosidase and preventing and treating type II diabetes That is, the application in non-insulin-dependent diabetes mellitus drugs, the flavonoid lignans have extremely significant activity of inhibiting α-glucosidase, and its inhibitory activity to α-glucosidase at a concentration of 40 μg / ml has reached 93%, showing by measuring its half inhibitory concentration: the intensity of this flavonoid lignan inhibiting α-glucosidase is 12 times that of the positive control drug acarbose, so this compound or its pharmaceutically acceptable salt, and the preparation The pharmaceutical composition prepared from the permissible pharmaceutical excipients or carriers can be expected to be used as a glycosidase inhibitor drug, espe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P3/10
Inventor 莽朝勇来亦刚罗廷顺刘卫红巫秀美赵昱董心齐
Owner DALI UNIV
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