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
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Examples
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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Application Information
- IPC
- C07D487/20; A61P37/02
- Inventors
- 陈道峰; 范明松