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2'-O-rhamnosyl swertisin, preparation of analogues thereof, and application thereof

A rhamnose-based and analog technology, applied in the field of natural medicinal chemistry, can solve problems that have not yet been reported, and achieve the effects of promoting absorption and utilization, inhibiting the rise of blood sugar, and enhancing translocation.

Active Publication Date: 2011-05-11
北京理工亘舒科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main pharmacological effects are anti-inflammatory, anti-viral, antibacterial, eliminating free radicals, choleretic, anti-diarrhea, anti-thrombotic, inhibiting the synthesis of TXA2 (thromboxane A2) and promoting the generation of PGI2 (prostacyclin), etc. Reports on the use of 2”-O-rhamnosyl as a drug and its analogues isolated and purified from the dried leaves of radishes as drugs for the treatment of type II diabetes and its complications

Method used

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  • 2'-O-rhamnosyl swertisin, preparation of analogues thereof, and application thereof
  • 2'-O-rhamnosyl swertisin, preparation of analogues thereof, and application thereof
  • 2'-O-rhamnosyl swertisin, preparation of analogues thereof, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation and structure identification of 2"-O-rhamnosyl as drug

[0049] 1. Preparation of 2”-O-rhamnosyl as drug

[0050] (1) Take 2kg of dried leaves and cut them into small sections;

[0051] (2) Add 20L of distilled water to the dried leaf fragments, heat and reflux to extract for 1 hour, filter, and repeat the above operation twice for the filter residue, combine the filtrate, recover the solvent to 5L, add ethanol until the alcohol content is 70%, let stand, filter, and obtain For the filtrate, the solvent was recovered under reduced pressure until there was no alcohol smell, and diluted with water to 20 L, filtered, the filtrate was separated with HP20 macroporous adsorption resin, eluted with 40% ethanol aqueous solution, and the solvent was recovered to obtain about 50 g of dry extract;

[0052] (3) 50g extract is separated by polyamide chromatographic column, eluted with 30% ethanol aqueous solution, followed by polyamide thin-layer chromatograph...

Embodiment 2

[0063] Example 2 2”-O-rhamnosyl as a drug enhances mouse GLUT4 translocation experiment

[0064] 1. Sample

[0065] 2"-O-rhamnosyl as drug (prepared in Example 1)

[0066] 2. Reagents

[0067] Collagenase VIII, the fifth fraction of bovine serum, rabbit anti-GLUT4 (primary antibody), goat anti-rabbit-HRP (secondary antibody), dibromoethylamine, and other drugs are of analytical grade.

[0068] 3. Experimental method

[0069] Add the sample to the mouse adipocyte suspension, incubate in a water bath at 37°C for 40min, then ultrasonically disrupt the cell suspension at 4°C, centrifuge (3000×g, 15min, 4°C), and discard the white fat layer suspended on the surface , the suspension continued to be centrifuged (12000×g, 25 min, 4° C.), and the precipitate was diluted with Medium I (10 mM Tris-HCl, 1 mM EDTA, 250 mM sucrose, pH=7.4) to form a solution as the cell membrane sample solution to be tested.

[0070] The content of GLUT4 was determined by Western blot method, and the sp...

Embodiment 3

[0083] Example 3 Effect of 2"-O-rhamnosyl as a drug on blood sugar in diabetic rats

[0084] 1. Animal modeling

[0085] Select 50 adult male rats with a body weight of 200±10g. After fasting for 12 hours before the experiment, alloxan was injected into the tail vein at a dose of 35mg / kg. The above operation was repeated once the next day. The experimental environment required a constant temperature of 25°C. On the seventh day after the injection of alloxan, the blood was taken from the tail, and the fasting blood glucose value of the rats after fasting for 12 hours was measured with a blood glucose meter. Rats were used as blank control, and the control group was injected with normal saline 10 mL / kg through the tail vein.

[0086] 2. Grouping, administration and index determination

[0087] The 30 rats with successful modeling were divided into three groups, namely the model control group, the positive control group and the drug administration group, with 10 rats in each gr...

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Abstract

The invention relates to 2'-O-rhamnosyl swertisin, preparation of analogues thereof, and application thereof. The 2'-O-rhamnosyl swertisin and the analogues thereof can obviously enhance the transposition of a glucose transporter GLUT4, accelerate absorption and utilization of glucose, obviously inhibit the rise of blood sugar, can be singly applied or are mixed with pharmaceutically acceptable medicinal auxiliary materials to form medicinal compositions or preparations, serve as medicaments for resisting type II diabetes and complications thereof, and are applied via gastrointestinal tracts or not. The preparation method comprises the steps of: separating from natural plant raw materials, chemically synthesizing and performing other means; and performing crushing, solvent extraction, weak-polarity macroporous adsorption resin separation, polyamide chromatographic column separation, sephadex gel chromatographic column separation, semi-preparative high performance liquid chromatograph purification and performing other processes.

Description

technical field [0001] The present invention relates to the preparation and use of 2"-O-rhamnosyl antidote and its analogues, in particular to the 2"-O-rhamnosyl antidote isolated and purified from natural plants and its The application of analogs in the preparation of medicines for treating type II diabetes and its complications belongs to the field of natural medicinal chemistry. Background technique [0002] What the present invention researches is the leaf of Shegan Belamcanda chinensis (L.) DC. The rhizome of Shegan is a commonly used traditional Chinese medicine, which was first recorded in "Shen Nong's Materia Medica". It is cultivated all over the country. Shegan medicinal material is bitter and cold in nature and taste, enters the liver and lung meridians, has the effects of clearing away heat and detoxification, relieving sore throat and reducing inflammation. It is mainly used for sore throat, lung abscess, phlegm, cough and asthma. [0003] At present, more re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04C07H1/00C07H1/08C07D407/04A61K31/7048A61K31/352A61P3/10
Inventor 邓玉林戴荣继张良孟薇薇李玉娟林凡凯李良陈艳吴崇明
Owner 北京理工亘舒科技有限公司
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