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Phenyl bis-lactone compounds and their use in the preparation of anti-complement drugs

A compound, dilactone technology, applied in the field of traditional Chinese medicine pharmaceuticals, can solve problems such as excessive activation of the autoimmune system

Active Publication Date: 2021-09-07
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Studies have shown that the above-mentioned diseases and pharmacological activities related to the treatment of Huo Tanmu are mostly related to the complement system, and the complement system plays a very important role in maintaining the body's immune balance and eliminating foreign microorganisms. Studies have shown that some pathogenic microorganisms can cause The overactivation of the autoimmune system in the human body leads to serious consequences, such as SARS, influenza, rheumatoid arthritis, etc. Therefore, it has been aroused in the art to find low-toxicity and high-efficiency complement inhibitors from traditional Chinese medicines for the treatment of related diseases. personnel concern

Method used

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  • Phenyl bis-lactone compounds and their use in the preparation of anti-complement drugs
  • Phenyl bis-lactone compounds and their use in the preparation of anti-complement drugs
  • Phenyl bis-lactone compounds and their use in the preparation of anti-complement drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Embodiment 1. Preparation of phenyl bis lactone compounds

[0028] Take Polygonum chinense Linn. 10kg medicinal material, pulverize it, and extract it by cold immersion in 95% ethanol for 3 times. After the extract is concentrated, it is suspended in water, and extracted with petroleum ether, ethyl acetate, and n-butanol respectively to obtain the active part positive Butanol 300g, get the extractant 250g and wet the macroporous resin D101 with H 2 O / EtOH (30, 60, 95%, v / v) obtained three fractions Fr.B1-Fr.B3. The active fraction passed through ODS C 18 Medium pressure flash preparative column with CH 3 OH-H 2 O (25:75 to 100:0) was eluted to obtain 7 Fr.B2fractions (A-G). All fractions were purified by semi-preparative column, and compound maysedilactone C (1) and compound maysedilactone D (2) were obtained from Fr. B2fraction A (CH 3 CN-H 2 O-CH 3 COOH 25:75:0.05);

[0029] After further identification, the NMR data of the obtained compounds 1 and 2 are shown...

Embodiment 2

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

[0031]Take 0.1 mL 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 each concentration of complement and 2% sheep red blood cells (SRBC) and dissolve them in 0.3mL BBS, mix well, put them in a low-temperature high-speed centrifuge at 5000rpm and 4℃ in a 37℃ water bath for 30min Centrifuge for 10 min. Take 0.2 mL of the supernatant from each tube and place it in a 96-well plate, and measure its absorbance at 405 nm. At the same time, a complete hemolysis group (0.1 mL 2% SRBC dissolved in 0.5 mL 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...

Embodiment 3

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

[0033] Take complement (human serum) 0.2mL, add AP diluent (barbital buffer, pH 7.4, containing 5mM Mg 2+ , 8mMEGTA) was double-diluted into 8 concentration gradients (1:2, 1:4, 1:8, 1:16, 1:32, 1:64, 1:128, 1:256), and then hemolyzed In the reaction system, 0.15mL of various concentrations of complement and 0.2mL of 0.5% RRBC were dissolved in 0.35mL of AP diluent, mixed evenly, placed in a low-temperature high-speed centrifuge at 5000rpm, 4°C for 10min in a 37°C water bath for 30min. Take 0.2 mL of the supernatant from each tube and place it in a 96-well plate, and measure the absorbance at 405 nm. At the same time, a complete hemolysis group (0.5% RRBC 0.2mL dissolved in 0.5mL 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. Take the dilution factor ...

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Abstract

The invention belongs to the technical field of traditional Chinese medicine pharmacy, and in particular relates to phenyl bis-lactone compounds and their application in the preparation of anti-complement drugs. The present invention adopts the activity-oriented separation method to separate and extract the phenyl lactone compounds maysedilactone C and maysedilactone D from the whole herb of Polygonaceae (Polygonaceae) plant Polygonum chinensis Linn, and through the anti-complement activity evaluation test, the results show that, The compound has a strong inhibitory effect on the classical and alternative pathways of the complement system, wherein the inhibitory effect on the classical pathway (CH 50 ) is 0.72 ~ 0.94mM, the inhibitory effect on the alternative pathway (AP 50 ) is 0.98 to 1.20 mM. The compounds of the present invention can be used to prepare anti-complement drugs and further prepare drugs for treating complement-related diseases.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine pharmacy, and relates to phenyl bis-lactone compounds isolated and identified from the traditional Chinese medicine Huotanmu, in particular to the isolated and identified phenyl bis-lactone compounds and their use in the preparation of anti-complement drugs Background technique [0002] It is disclosed in the prior art that Fotanmu is the dry above-ground part of Polygonum chinensis Linn., a plant of the genus Polygonum in the family Polygonaceae. It is a traditional heat-clearing and detoxifying traditional Chinese medicine in southern my country, and it is also a main component of Wanglaoji herbal tea and the like. Spicy, bitter, cool in nature. It has the effects of clearing heat and dampness, cooling blood and detoxifying, calming liver and improving eyesight, promoting blood circulation and relaxing tendons. Modern pharmacological studies have shown that this product has...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61P11/00A61P31/12A61P31/16A61P29/00A61P19/02A61P37/02
Inventor 陈道峰郑昊钏卢燕
Owner FUDAN UNIV
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