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Phenyl dilactone compounds and uses in preparation of anti-complement drugs

A compound and dilactone technology, applied in the field of traditional Chinese medicine pharmacy, can solve problems such as excessive activation of the autoimmune system, and achieve the effect of good anti-complement activity

Active Publication Date: 2019-06-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 dilactone compounds and uses in preparation of anti-complement drugs
  • Phenyl dilactone compounds and uses in preparation of anti-complement drugs
  • Phenyl dilactone compounds and uses in preparation of anti-complement drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Example 1. Preparation of phenyl dilactone compounds

[0028] Take 10kg of Polygonum chinense Linn., crush it, and extract with 95% ethanol for 3 times. The extract is concentrated and suspended in water, and then extracted with petroleum ether, ethyl acetate and n-butanol to obtain the active part. 300g of butanol, take 250g of the extract and wet process for the macroporous resin D101 with H 2 O / EtOH (30, 60, 95%, v / v) obtained three fractions Fr.B1-Fr.B3. The active fraction passes through ODS C 18 Medium pressure rapid preparation column with CH 3 OH-H 2 O(25:75 to 100:0) eluted to obtain 7 Fr.B2fractions(AG). 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 in Table 1.

Embodiment 2

[0030] Example 2. In vitro anti-complement classical pathway experiment

[0031] Take 0.1 mL of complement (guinea pig serum), add barbital buffer (BBS) to make a 1:10 solution, and use BBS to double-dilute it to 1:20, 1:40, 1:80, 1:160, 1: 320, 1:640 and 1:1280 solutions. Dissolve 0.1 mL each of 1:1000 hemolysin, each concentration of complement and 2% sheep red blood cells (SRBC) in 0.3 mL BBS, mix them, and put them in a low-temperature high-speed centrifuge after a water bath at 37°C for 30 minutes at 5000 rpm and 4°C Centrifuge for 10 min. Take 0.2mL of supernatant from each tube to 96-well plate, and measure the absorbance at 405nm. The experiment also set up a complete hemolysis group (0.1mL 2% SRBC dissolved in 0.5mL tri-distilled water). The absorbance of the three-distilled water-soluble blood vessel was used as the standard for total hemolysis to calculate the hemolysis rate. Plot the complement dilution on the x-axis and the percentage of hemolysis on the y-axis. ...

Embodiment 3

[0032] Example 3. In vitro anti-complement alternative pathway experiment

[0033] Take 0.2mL of complement (human serum), add AP diluent (barbital buffer, pH 7.4, containing 5mM Mg 2+ , 8mMEGTA) after diluting it to 8 concentration gradients (1:2, 1:4, 1:8, 1:16, 1:32, 1:64, 1:128, 1:256), add hemolysis In the reaction system, 0.15 mL of each concentration of complement and 0.2 mL of 0.5% RRBC were dissolved in 0.35 mL of AP diluent, mixed well, placed in a low-temperature high-speed centrifuge at 37°C for 30 minutes, and centrifuged at 5000 rpm, 4°C for 10 minutes. Take 0.2mL of supernatant from each tube to 96-well plate and measure the absorbance at 405nm. The experiment also set up a complete hemolysis group (0.5% RRBC 0.2mL dissolved in 0.5mL tri-distilled water). The absorbance of the three-distilled water-soluble blood vessel was used as the standard for total hemolysis to calculate the hemolysis rate. Take the complement dilution factor as the x-axis, and plot the perc...

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Abstract

The invention belongs to the technical field of traditional Chinese medicine pharmacy, and particularly relates to phenyl dilactone compounds and uses in preparation of anti-complement drugs. According to the present invention, the phenyl lactone compounds of maysedilactone C and maysedilactone D are separated and extracted from the whole plant of Polygonaceae plant Polygonum chinensis Linn by using an active guide separation method, and the anti-complement activity evaluation test results show that the compounds have strong inhibition effects on the classical and alternative pathways of the complement system, wherein the inhibition effect (CH50) on the classical pathway is 0.72-0.94 mM, and the inhibition effect (AP50) on the alternative pathway is 0.98-1.20 mM. The compounds of the present invention can be used for preparing anti-complement drugs and further preparing drugs for treating diseases associated with complement.

Description

Technical field [0001] The present invention belongs to the technical field of traditional Chinese medicine pharmacy, and relates to phenyl dilactone compounds separated and identified from traditional Chinese medicine fire charcoal, in particular to phenyl dilactone compounds separated and identified and their use in preparing anti-complement drugs Background technique [0002] The prior art discloses that Fotan is the dry aerial part of Polygonum chinensis Linn. It is a traditional heat-clearing and detoxifying Chinese medicine in southern my country, and it is also the main component medicine of Wanglaoji herbal tea. Taste pungent, bitter, cool in nature. It has the effects of clearing heat and dampness, cooling blood and detoxification, calming liver and improving eyesight, promoting blood circulation and relaxing muscles. Modern pharmacological studies have shown that this product has anti-pathogenic microorganisms, anti-inflammatory and analgesic effects, smooth muscle and...

Claims

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Application Information

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Patent Type & Authority Applications(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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