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Triterpene compound and application thereof in preparation of anti-complementary medicament

A technology of triterpene compounds and compounds, which is applied in the field of new applications in the preparation of anti-complement drugs, and can solve problems such as Prunella vulgaris compounds that have not yet been seen

Inactive Publication Date: 2012-07-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, there have been many studies on the chemical constituents and biological activities of Prunella vulgaris, but so far there has been no report on Prunella vulgaris as a complement inhibitory compound

Method used

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  • Triterpene compound and application thereof in preparation of anti-complementary medicament
  • Triterpene compound and application thereof in preparation of anti-complementary medicament
  • Triterpene compound and application thereof in preparation of anti-complementary medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1. Preparation of triterpenoids

[0022] Take 15 kg of Prunella vulgaris fruit ears, cold-soak with 95% ethanol at room temperature (50 L × 5 times), combine the extracts and concentrate until there is no alcohol smell, and dilute the extract (700 g) to 2 L with water; -90 °C) and ethyl acetate extraction (each 2 L × 3 times), the ethyl acetate extracts were combined and concentrated to dryness to obtain 160 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel column chromatography, and petroleum ether (60-90 °C), petroleum ether (60-90 °C)-acetone, acetone gradient elution, the obtained petroleum ether (60-90 °C)- Acetone (10:1) fractions were purified by repeated silica gel column chromatography using petroleum ether (60-90 °C)-ethyl acetate as eluent to obtain compound 1 (16 mg), compound 2 (17 mg), 3 (9 mg) and 4 (8 mg). Their structures were analyzed by spectroscopic methods and identified as 2α,3α-dihydroxy-olean-1...

Embodiment 2

[0028] Example 2. Anti-complement classical pathway test in vitro

[0029] Take 0.1 ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:5 solution, and double-dilute with BBS to 1:10, 1:20, 1:40, 1:80, 1: 160, 1:320 and 1:640 solutions. Dissolve 0.1 ml of 1:1000 hemolysin, various concentrations of complement and 2% sheep red blood cells (SRBC) in 0.3 ml BBS, mix well, put in a low-temperature high-speed centrifuge at 5000 rpm, 4 oC Centrifuge for 10 min under conditions. Take 0.2 ml of the supernatant from each tube in a 96-well plate, and measure the absorbance at 405 nm. A full hemolysis group (0.1 ml 2% SRBC dissolved in 0.5 ml triple distilled water) was also set up in the experiment. The absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of co...

Embodiment 3

[0031] Example 3. Anti-complement alternative pathway test in vitro

[0032] Take 0.2 ml of complement (human serum), add AP diluent to prepare a 1:5 solution, and double-dilute to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solution. Take 0.15 ml of complement of each concentration, 0.15 ml of AP diluent and 0.20 ml of 0.5% rabbit erythrocyte (RE), mix well, place in a low-temperature high-speed centrifuge at 5000 rpm and 4 oC for 10 min in a water bath at 37 oC . Take 0.2 ml of the supernatant from each tube in a 96-well plate, and measure the absorbance at 405 nm. A full hemolysis group (0.20 ml 0.5% RE dissolved in 0.3 ml triple distilled water) was also set up in the experiment. The absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of complement is plotted as the Y-axis. The l...

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Abstract

The invention belongs to the field of Chinese medicine pharmacy, and relates to a triterpene compound shown as a formula I and a novel application thereof to preparation of an anti-complementary medicament, in particular to an application of a novel compound 3beta,13beta-dihydroxyolic-11-ene-28-oic acid in preparation of an anti-complementary medicament and a preparation method of the novel compound. Four triterpene compounds are separated from an acetic ether extracting position of a labiate selfheal spike dried ear ethanol extract, and are proved to have suppressing effects on a classical path and a bypath of a complementary system. The suppressing effect CH50 of the compound on the classical path of the complementary system is 198-449 mug / ml, and the suppressing effect AP50 of the compound on the bypath is 357-602 mug / ml. The triterpene compound disclosed by the invention can be used for preparing an anti-complementary medicament and further preparing a medicament for treating complement-related diseases. The formula I is shown in the specification.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to triterpenoids in Prunella vulgaris and its new application in preparing anti-complement drugs. Background technique [0002] Studies have reported that excessive activation of the complement system can lead to many major diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. However, there is still a lack of ideal therapeutic drugs for such diseases. Therefore, there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors in clinical practice. Therefore, the research on anti-complement drugs has been the focus and focus of pharmaceutical research in the world for many years. The research and development of complement inhibitors from natural products is an important research field that has received more and more attention in recent years, and it has the characteristics of l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P37/02A61P19/04A61P29/00A61P11/00
Inventor 程志红陈道峰杜冬生金家宏
Owner FUDAN UNIV
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