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Benzo-macrolactam indole alkaloid and application thereof in preparation of anti-complement medicines

A technology of macrolactam and indole alkaloids, which can be used in drug combination, organic chemistry, allergic diseases, etc., and can solve problems such as lack of therapeutic drugs

Active Publication Date: 2016-10-05
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still a lack of ideal therapeutic drugs for such diseases, so there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors in clinical practice.

Method used

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  • Benzo-macrolactam indole alkaloid and application thereof in preparation of anti-complement medicines
  • Benzo-macrolactam indole alkaloid and application thereof in preparation of anti-complement medicines
  • Benzo-macrolactam indole alkaloid and application thereof in preparation of anti-complement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 prepares cinnamonine C

[0017] Take 5kg of Qingdai powder, 95% ethanol reflux extraction 3 times (50L×3), 2h each time, combine the extracts and concentrate to get 0.25kg of extract, add water (4L) to suspend, add equal volume petroleum ether, ethyl acetate Extract with n-butanol 5 times, combine the extracts and concentrate to dryness to obtain 50 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, followed by gradient elution with dichloromethane-methanol (50:1-0:1) to obtain 8 fractions (Fr.1-8) , wherein the fraction Fr.5 (4g) was subjected to silica gel column chromatography (dichloromethane-methanol, 30:1, 20:1, 10:1, 5:1, 3:1, 1:1), Sephadex LH- 20 column chromatography (chloroform-methanol, 1:1) and reversed-phase HPLC (methanol-water, 20:80-80:20 gradient elution) and other means of purification, and the compound incindaline C was isolated.

[0018] The compound incindai...

Embodiment 2

[0019] Example 2 Anti-complement classical pathway test in vitro

[0020] Take 0.04ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:10 320, 1:640 and 1:1280 solutions, take 0.1ml of 1:1000 hemolysin, 2% sheep red blood cell (SRBC) and 0.2ml of complement of each concentration, dissolve in 0.2ml BBS, mix well, and bathe in 37℃ water for 30min Put it into a low-temperature high-speed centrifuge, and centrifuge at 4000rpm and 4°C for 5min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure its absorbance at 405nm. At the same time, a complete hemolysis group (0.1ml 2% SRBC, 0.1ml hemolysin dissolved in 0.4ml triple distilled water) was 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. Plot the dilution of comple...

Embodiment 3

[0021] Example 3 Anti-complement alternative pathway test in vitro

[0022] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mMMg 2+,8mM EGTA) was prepared as a 1:5 solution, and double-diluted into 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solutions. Take 0.15ml of complement of each concentration, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit erythrocytes (RE), mix them evenly, put them in a low-temperature high-speed centrifuge at 37°C for 30min, and centrifuge at 4000rpm and 4°C for 5min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure the absorbance at 405nm. At the same time, a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple distilled water) was 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. Plot the dilution of complement on the X-axis a...

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PUM

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Abstract

The invention belongs to the field of preparation of traditional Chinese medicines and relates to a benzo-macrolactam indole alkaloid, indigo naturalis alkaloid C, and an application thereof in preparation of anti-complement medicines. In the invention, the benzo-macrolactam indole alkaloid, indigo naturalis alkaloid C, is separated from powder of indigo naturalis, wherein the compound has a novel and unique structure and is formed by complexing two 3-carbonyl indole groups on benzo-macrolactam. A modern pharmacological experiment proves that the compound has strong inhibition effects on both a classic pathway and a bypass pathway of a complement system, wherein the CH50 value and the AP50 value of the compound are respectively 0.018 + / - 0.004 mg / ml and 0.042 + / - 0.014 mg / ml. The compound can be used for preparing a complement inhibitor.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a benzomacrocyclic lactam indole alkaloid in Qingdai and its application in preparing anti-complement drugs. Background technique [0002] Studies have disclosed that excessive activation of the complement system can lead to many major diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), and acute respiratory distress syndrome (ARDS). The study of anti-complement drugs has been the focus and focus of the world's pharmaceutical research for many years. However, there is still a lack of ideal therapeutic drugs for such diseases at present, so there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors in clinical practice. 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 th...

Claims

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Application Information

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IPC IPC(8): C07D487/20A61P37/02
Inventor 陈道峰范明松黄成钢
Owner FUDAN UNIV
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