Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Pharmaceutical application of B ring methoxy substituted silybin in preparing glycosidase inhibitors

A technology of silibinin and methoxy, which is applied in the field of pharmaceutical use of B-ring methoxy silibinin for the preparation of glycosidase inhibitors, can solve the problems of diabetes without glycosidase inhibition, and achieve industrialization Clear prospect, strong inhibition of α-glucosidase, energy saving and emission reduction effect of large-scale production

Inactive Publication Date: 2012-12-26
DALI UNIV
View PDF2 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical application of B ring methoxy substituted silybin in preparing glycosidase inhibitors
  • Pharmaceutical application of B ring methoxy substituted silybin in preparing glycosidase inhibitors
  • Pharmaceutical application of B ring methoxy substituted silybin in preparing glycosidase inhibitors

Examples

Experimental program
Comparison scheme
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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com