Uses of lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol in preparation of anti-complement drugs

A technology of lignans and compounds, applied in the field of medicine, can solve the problems that have not yet been seen

Inactive Publication Date: 2016-04-27
FUDAN UNIV
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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 on the anti-complement activity of lignans (7S,8R)-dihydrodehydrodisconiferyl alcohol

Method used

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  • Uses of lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol in preparation of anti-complement drugs
  • Uses of lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol in preparation of anti-complement drugs
  • Uses of lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol in preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1 Preparation of (7S, 8R)-dihydrodehydrodisconiferyl alcohol

[0014] Take 25kg of dry roots of Sesame chinensis, crush them, and reflux extract with 95% ethanol for 3 times (50L×3), each time for 2h, combine the extracts and concentrate to obtain 0.95kg of extract, add water (4L) to suspend, and add an equal volume of petroleum Extracted 5 times with ether, ethyl acetate and n-butanol, combined the extracts and concentrated to dryness to obtain 200 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, and sequentially eluted with dichloromethane-methanol (50:1-0:1) gradient to obtain 11 fractions (Fr.1-11) , wherein the fraction Fr.3 (32g) was subjected to silica gel column chromatography (dichloromethane-methanol, 30:1, 20:1, 10:1, 5:1, 3:1, 1:1), MPLC (methanol - water, 20:80-80:20 gradient elution) and sephadexLH-20 column chromatography and other means to purify, isolate and obtain c...

Embodiment 2

[0016] Example 2 Anti-complement classical pathway activation test in vitro

[0017] 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 1:1000 hemolysin, 0.1ml of 2% sheep red blood cells (SRBC) and 0.2ml of complement of each concentration, dissolve them in 0.2ml of BBS, mix well, put them in a low-temperature high-speed centrifuge at 4000rpm and 4℃ Centrifuge 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 complement on the X-axis...

Embodiment 3

[0018] Example 3 Anti-complement Alternative Pathway Activation Test in Vitro

[0019] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mMMg 2+ ,8mMEGTA) 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 t...

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PUM

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Abstract

The present invention belongs to the field of medicine, and relates to uses of a lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol in preparation of anti-complement drugs. According to the present invention, a lignan compound (7S,8R)-dihydrodehydrodiconiferyl alcohol is separated from the dried root of a Helicteres plant Helicteres angustifolia L, and the modern pharmacological research method results confirm that the method provides strong inhibition effects for complement activation in the complement system classical pathway and the alternative pathway, wherein the CH50 value is 0.0032 mg / ml, the AP50 is 0.0077 mg / ml, and the compound can be used as the active component so as to be used for preparing anti-complement drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the use of a lignan compound (7S, 8R)-dihydrodehydrodisconiferyl alcohol isolated from the medicinal plant Sesame chinensis in the preparation of anti-complement drugs. Background technique [0002] Studies have shown that overactivation of the complement system can lead to systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other major diseases. High efficiency, low toxicity, specific new complement inhibitor. 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 low cost and low toxicity. Scholars at home and abroad have isolated a variety of monomeric compounds with inhibitory effects on the complement system from various natural products including marine organisms, which provides broad prospects for the...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61P37/02C07D307/80
Inventor 陈道峰殷翔卢燕
Owner FUDAN UNIV
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