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Application of Eupalinolide K in preparing anticomplement drugs

An anti-complement and wild horse technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations containing active ingredients, etc., to achieve the effect of shortening the separation cycle and improving the separation effect

Inactive Publication Date: 2014-01-22
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At the same time, there is no report about whether Eupalinolide K has the effect of inhibiting complement activation in the prior art

Method used

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  • Application of Eupalinolide K in preparing anticomplement drugs
  • Application of Eupalinolide K in preparing anticomplement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Yemachai lactone K

[0025] Take 75 g of dried Ye Ma Zhui medicinal material, add 750 mL of ethanol and water mixed solution with a volume ratio of 80:20 for reflux extraction each time, extract twice, each time for 2 hours, filter the extract while it is hot, combine the filtrates, and recover ethanol under reduced pressure , to obtain 100 mL of aqueous suspension; extract 3 times with petroleum ether, each time with 200 mL of petroleum ether, evaporate the water layer to dryness, add 100 mL of methanol, dissolve it by ultrasonication for 15 minutes, reflux extraction for 1 hour, filter while hot, and recover the filtrate; The filtrate was left to settle at 4 °C for 2 hours, filtered, the filtrate was recovered to dryness under reduced pressure, and 4.936 g of sample was obtained by weighing; 4.936 g of sample was dissolved in 20 mL of a mixed solution of methanol and water with a volume ratio of 30:70. Phases were separated and purified, spec...

Embodiment 2

[0027] Example 2: Eupalinolide K Classical Pathway Complement Inhibition Experiment

[0028] 1. Experimental principle

[0029] Complement can hemolyze red blood cells sensitized by hemolysin. When the concentration of sensitized red blood cells is constant, the degree of hemolysis is proportional to the complement content. Therefore, after diluting the test product at different concentrations, mix it with complement, react with red blood cells, and measure the degree of hemolysis, so as to cause the minimum concentration of the test product required for 50% hemolysis (CH 50 ) to evaluate the anti-complement activity of the test article.

[0030] 2. Solution preparation

[0031] Barbitol buffer solution (BBS): take 2.875 g of barbital sodium, dissolve it in 250 mL of hot water, and ultrasonically vibrate to accelerate the dissolution, then add 42.5 g of NaCl, MgCl 2 ·6H 2 O 0.84 g, CaCl 2 0.14 g, 1.0 g of barbiturate, supplemented with triple distilled water to 1000 ml t...

Embodiment 3

[0044] Example 3: Eupalinolide K alternative pathway complement inhibition experiment

[0045] 1. Experimental principle

[0046] The Ca in the serum to be tested was chelated with ethylene glycol diethyl ether diamine tetraacetic acid (EGTA) 2+ , block the role of C1, block the classic activation pathway of complement, add rabbit red blood cells that can activate factor B, lead to activation of the alternative pathway of complement, rabbit red blood cells are damaged and hemolysis occurs. The relationship between the degree of hemolysis and the anti-complement activity of the test article is similar to the classic route, so the minimum concentration of the test article required to cause 50% hemolysis (AP 50 ) to evaluate the anti-complement activity of the test article.

[0047] 2. Solution preparation

[0048] 0.1M EGTA: Dissolve 3.5g of NaOH in 85mL of distilled water, add 19g of EGTA, dissolve, add distilled water to 500mL.

[0049] AP Diluent: 0.1 M EGTA 80 mL, Barbit...

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Abstract

The invention discloses application of Eupalinolide K in preparing anticomplement drugs. The related research indicates that the Eupalinolide K has high anticomplement activity by complement classical pathway and bypass pathway and can be used for preparing anticomplement drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicines, and relates to the application of yemazulide K, in particular to the application of yomazolide K in the preparation of anti-complement drugs. Background technique [0002] The complement system is one of the important immune defense systems of the human body. The normal activation of the complement system can eliminate foreign microorganisms, remove damaged or dead cells and tissues in the body, and maintain the balance of the body; but abnormal activation of the complement system can cause the immune system to and participate in the pathological process of various diseases, such as: rheumatoid arthritis, senile dementia, systemic lupus erythematosus, ischemic reperfusion, acute myocardial infarction, acute respiratory distress syndrome, etc. Studies have found that severe atypical pneumonia (SARS) is also associated with overactivation of the complement system. In view of the import...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P7/00
Inventor 张健褚纯隽夏龙陈道峰吴双庆李显伦严彪
Owner SUZHOU UNIV
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