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Medicinal use of dinitrobenzoylsilybin for preparing glycosidase inhibitor

A technology of dinitrobenzoyl and silybin esters, which is applied in the field of pharmaceutical use of dinitrobenzoyl silybin for the preparation of glycosidase inhibitors, and can solve diabetes without glycosidase inhibition, etc. problems, to achieve the effect of clear industrialization prospects, strong inhibition of α-glucosidase, energy saving and emission reduction in large-scale production

Inactive Publication Date: 2012-12-05
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 use of dinitrobenzoylsilybin for preparing glycosidase inhibitor
  • Medicinal use of dinitrobenzoylsilybin for preparing glycosidase inhibitor
  • Medicinal use of dinitrobenzoylsilybin for preparing glycosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 : Formula (1) compound (±)-3,5-dinitrobenzoic acid [3-(4-hydroxyl-3-methoxyphenyl)-6-(2,3-dihydro-3,5, Preparation of 7-trihydroxy-4-oxo-benzopyran-2)-2,3-dihydro-1,4-benzodioxane-2]-methyl ester

[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; Sepha...

Embodiment 2

[0026] Example 2 : Formula (1) compound (±)-3,5-dinitrobenzoic acid [3-(4-hydroxyl-3-methoxyphenyl)-6-(2,3-dihydro-3,5, Inhibition of α-glucosidase by 7-trihydroxy-4-oxo-chromen-2)-2,3-dihydro-1,4-benzodioxane-2]-methyl ester Activity detection

[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 (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 s...

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Abstract

The invention relates to medicinal use of dinitrobenzoylsilybin for preparing a glycosidase inhibitor, in particular discloses use of 3,5-dinitrobenzoyl substituted silybin ester type flavonolignan and pharmaceutically acceptable salts thereof for the preparation of medicaments for inhibiting alpha-glucuroide and controlling type 2 diabetes. The flavonolignan has extremely obvious activity for inhibiting alpha-glucuroide and has the activity strength for inhibiting the alpha-glucuroide of 71.19 percent at the concentration of 40mg / ml, and by measuring median inhibitory concentration, the strength of the flavonolignan for inhibiting the alpha-glucuroide is 9.5 times that of a positive control medicament acarbose. Pharmacodynamic results prove that the flavonolignan or the pharmaceutically acceptable salts thereof can be expectedly used as a glycosidase inhibitor medicament, particularly a medicament for controlling the type 2 diabetes.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to a 3,5-dinitrobenzoyl substituted silybin ester type flavonoid lignan or a pharmaceutically acceptable salt thereof for the preparation of inhibitors of 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 very significant activity of inhibiting α-glucosidase, and it is effective for α-glucose at a concentration of 40 micrograms / ml. The inhibitory activity intensity of glucosidase has reached 71.19%. It shows by measuring its half maximal inhibitory concentration: the intensity of this flavonoid lignan inhibiting α-glucosidase is 9.5 times that of the positive control drug acarbose, so the compound or its The pharmaceutically acceptable salt and the pharmaceutical composition prepared with pharmaceutical excipients or carriers allowed by the formul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P3/10
Inventor 王鹏杨柳青焦春香郭利军巫秀美赵昱郝小江
Owner DALI UNIV
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