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Use of bisabolane type sesquiterpene compounds in preparing anti-complement drugs

A technology of bisabolane and sesquiterpenoids, applied in the field of preparation of anti-complement drugs and bisabolane-type sesquiterpenoids

Active Publication Date: 2019-07-16
SHIHEZI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there has been no report on the discovery of bisabolane-type sesquiterpenoids with complement inhibitory effects

Method used

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  • Use of bisabolane type sesquiterpene compounds in preparing anti-complement drugs
  • Use of bisabolane type sesquiterpene compounds in preparing anti-complement drugs
  • Use of bisabolane type sesquiterpene compounds in preparing anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of bisabolane-type sesquiterpenoids

[0029] Take 3.5 kg of dried roots and rhizomes of L. tekesi, crush them, and use petroleum ether: ether: methanol = 1:1:1 to repeatedly cold soak and extract 3 times at room temperature, soaking each time for 7 days. The solvent was recovered under reduced pressure to obtain 130 g of the total extract. 130g of total extract and 100-200 mesh silica gel 1:1 mixed sample, wet column (5 kg SiO 2 ), petroleum ether-acetone gradient elution (50:1, 30:1, 15:1, 9:1, 7:1, 5:1, 3:1, 2:1, 1:1) fractions were subjected to TLC The detection was pooled into 11 fractions (Fr.1-11). Fraction Fr.7 (2.5g), was loaded on a forward silica gel column by dry method, eluted with petroleum ether-acetone (10:1), obtained fractions, sampled, detected by TLC and concentrated sulfuric acid-vanilla The aldehyde reagent was used for color observation, and the samples were combined to obtain 3 parts, which were eluted by silica gel column...

Embodiment 2

[0030] Example 2 Anti-complement classical pathway test in vitro

[0031] 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

[0032] Example 3 Anti-complement alternative pathway test in vitro

[0033] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH 7.4, containing 5 mMg 2+ , 8 mMEGTA) 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 was taken Complement 0.15ml, AP diluent 0.15ml and 0.5% rabbit erythrocyte (RE) 0.20ml, mix well, put in a low-temperature high-speed centrifuge at 37°C for 30 minutes, centrifuge at 5000 rpm and 4°C for 10 minutes, take Put 0.2 ml of the supernatant in each tube into 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 triple-distilled water-lyzed blood vessels was used as the standard for full hemolysis. Hemolysis rate, take the dilution of complement as the X-axis, and the percentage of hemolysis c...

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Abstract

The present invention belongs to the field of traditional Chinese medicine pharmacy and relates to bisabolane type sesquiterpene compounds and a use thereof in preparing anti-complement drugs. The bisabolane type sesquiterpene compounds are obtained by being separated from extracts of dried roots and rhizomes of a compositae plant of ligularia knorringiana Pojark by petroleum ether, diethyl etherand methanol at a ratio of 1:1:1. Besides, in vitro anti-complement activity evaluation experiments prove that the bisabolane type sesquiterpene compounds have relatively strong inhibitory effects onclassical pathways and alternative pathways of a complement system. The bisabolane type sesquiterpene compounds can be used to prepare the anti-complement drugs and further prepare the drugs for treating complement-related diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to alkane-type sesquiterpene compound of Ligularia tekesii and its new application in the preparation of 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 ha...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/704C07C45/78C07C45/79C07C49/513C07H15/203C07H1/08A61P37/06A61P19/02A61P29/00A61P11/00
CPCA61K31/122A61K31/704C07C45/78C07C45/79C07C49/513C07H1/08C07H15/203
Inventor 王琪戴沩元思文
Owner SHIHEZI UNIVERSITY
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