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Use of alkaloid compound 5-hydroxypyrrolidin-2-one in the preparation of anti-complement drugs

A technology of hydroxypyrrolidine and alkaloids, which is used in drug combinations, antipyretics, anti-inflammatory agents, etc.

Active Publication Date: 2020-02-07
SHIHEZI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there has been no report about the alkaloid compound 5-hydroxypyrrolidin-2-one having complement inhibitory activity

Method used

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  • Use of alkaloid compound 5-hydroxypyrrolidin-2-one in the preparation of anti-complement drugs
  • Use of alkaloid compound 5-hydroxypyrrolidin-2-one in the preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Preparation of alkaloid compounds

[0023] Take 16.5 kg of dried whole herb of Buglossis italicum, crush it, soak it in 95% ethanol at room temperature for 3 times, combine the extracts and concentrate until there is no alcohol smell to obtain 1 kg of the total extract, add water (1000 mL) to the extract to suspend , extracted three times with petroleum ether, ethyl acetate, and n-butanol in an equal-volume boiling range from 60°C to 90°C, respectively, to obtain 54 g, 160 g, and 385 g of extracts, respectively. The n-butanol extraction fraction (300 g) was separated by silica gel column chromatography, followed by chloroform, chloroform-methanol and methanol gradient elution, wherein the ratio of chloroform-methanol gradient elution was 50:1, 30:1, 15:1, 9:1, 7:1, 5:1, 3:1, 2:1 and 1:1, resulting in 9 fractions. Among them, the fraction Fr.2 (4 g) was subjected to MCI column chromatography with methanol-water in the ratio of 10:90, 30:70, 50:50, 70:30, and 9...

Embodiment 2

[0024] Example 2 Anti-complement classical pathway test in vitro

[0025] Take 0.1ml 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; take 1:1000 hemolysin, each concentration of complement and 2% sheep red blood cell (SRBC) each 0.1ml dissolved in 0.3ml BBS, mix well, 37 ℃ water bath for 30min, then put into low temperature Centrifuge in a high-speed centrifuge at 5000rpm and 4°C for 10min, take 0.2ml of the supernatant from each tube and put it in a 96-well plate, measure its absorbance at 405nm, and set up a full hemolysis group (0.1ml of 12% SRBC dissolved in 0.5ml of three Distilled water), using the absorbance of three-distilled water lysed blood vessels as the standard of full hemolysis, calculate the hemolysis rate, take the dilution of complement as the X-axis, and the percentage of hemolysis caused by each dilution of complement a...

Embodiment 3

[0026] Example 3 Anti-complement alternative pathway test in vitro

[0027] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH 7.4, containing 5 mMg 2+ , 8mMEGTA) was prepared into a 1:5 solution, and double-diluted into 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solutions, and each concentration of complement 0.15ml, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit red blood cells (RE), mix well, put in a low-temperature high-speed centrifuge after 30min in 37℃ water bath, centrifuge at 5000rpm, 4℃ for 10min, take each tube Put 0.2 ml of the supernatant in a 96-well plate, and measure the absorbance at 405 nm. At the same time, a complete hemolysis group (0.20 ml 0.5% RE dissolved in 0.3 ml triple-distilled water) was set up in the experiment. The absorbance of the three-distilled water lysed blood vessel was used as the standard of total hemolysis to calculate the hemolysis rate , with the complement dilution as the X-axis, the percentage of hemol...

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Abstract

The invention belongs to the field of preparation of traditional Chinese medicines, and relates to an application of an alkaloid compound namely 5-hydroxypyrrolidine-2-ketone in preparation of an anticomplement drug. According to the invention, the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone is separated from the n-butanol extraction part of an ethanol extract of a dried whole Borraginaceae plant namely Anchusaitalica Retz.; meanwhile, in-vitro anticomplement activity evaluation experiment results verify that the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has strong inhibitory effects on the classical pathway and the alternative pathway of a complement system. The alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has a CH50 value of 83 [mu]g / ml and an AP50 valueof 77 [mu]g / ml, and can be used as an active ingredient for preparation of the anticomplement drug.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the use of alkaloid compound 5-hydroxypyrrolidin-2-one isolated from Buglossum italiana in preparing anti-complement drugs. Background technique [0002] The prior art discloses that excessive activation of the complement system can lead to various serious diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. 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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/273A61K31/4015A61P37/02A61P19/04A61P19/02A61P29/00A61P11/00
Inventor 王琪戴沩候玉珍
Owner SHIHEZI UNIVERSITY
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