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Application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs

A technology of caffeoylquinic acid and caffeoylquinic acid methyl ester, which is applied in the field of application of caffeoylquinic acid and its derivatives in the preparation of anti-complementary drugs, and can solve the problems that have not been reported on caffeoylquinic acid, etc. problems, to achieve the effect of great clinical application value, rich sources of raw materials, and drug safety

Inactive Publication Date: 2011-12-07
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Caffeoylquinic acid compounds are widely distributed in plants and have a variety of pharmacological activities. However, there are no reports of caffeoylquinic acid and its derivatives anti-complement and preparation of complement inhibitory drugs.

Method used

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  • Application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs
  • Application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs
  • Application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of caffeoylquinic acid and derivatives thereof

[0042] 25 kg of dry whole herb of S. sageii (purchased from the medicinal material market in Haozhou, Anhui, China) was pulverized, extracted 3 times under 80% ethanol hot reflux (200L×3), combined the extracts to recover ethanol, and concentrated to dryness under reduced pressure at 60°C to obtain S. sativa Grass total extract 2.9kg, take total extract 2.5kg and suspend with water (15L), sequentially extract with equal volume of petroleum ether, ethyl acetate, n-butanol for 3 times, combine ethyl acetate extract and concentrate under reduced pressure at 60°C To dryness, 450 g of ethyl acetate extract was obtained. Take 400 g of the ethyl acetate extract and pass through a silica gel column (4 kg, 100-200 mesh, 10 cm × 100 cm) chromatography, and dichloromethane: methanol (70:1, 50:1, 30:1, 20:1, 10:1 , 5:1, 3:1, 1:1) gradient elution, each gradient elution 20L, collect dichloromethane:methanol (3:1...

Embodiment 2

[0051] Example 2 classical pathway complement inhibition test

[0052] 1 Instruments and reagents

[0053] Low-temperature high-speed centrifuge (Jouan MR22i), microplate reader (Thermo Labsystems, well scanMK3), sheep red blood cells, anti-sheep red blood cell antibodies (sigma company), human serum, barbiturate-barbital sodium buffered saline (BBS 2+ , pH=7.4, containing 0.5mM Mg 2+ and 0.15mM Ca 2+ ), triple distilled water, heparin sodium, and a constant temperature water bath.

[0054] 2 test drugs

[0055] The total sage extract prepared in Example 1 and the caffeoylquinic acid compounds 1-7 isolated therefrom

[0056] 3 Experimental methods

[0057] Take human serum to VBS 2+ Buffer (barbital buffer, pH=7.4, containing 0.5mM Mg 2+ and 0.15mM Ca 2+ ) diluted 1:10, as a source of "complement" in the classical pathway. Antibodies against goat erythrocytes in VBS 2+ The buffer was diluted 1:1000 as hemolysin; sheep red blood cells were treated with VBS 2+ The buf...

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Abstract

The invention provides the application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs. The present invention extracts and separates the caffeoylquinic acid compounds obtained from Shamrock, through in vitro experiments, it is confirmed that the cell hemolysis caused by the activation of the classic pathway of the complement system is inhibited, indicating that there is an anti-complement effect. The activity is stronger than that of the total extract of S. sageris, and it is a kind of good complement inhibitor, which can be used to prepare new anti-complement drugs and treat various diseases caused by abnormal activation of complement, and has low effective concentration and low toxicity. The drug is safe, the source of raw materials is abundant, and it has great clinical application value. Caffeoylquinic acid and its derivatives are shown in the following structural formula I: Formula I wherein R1, R2, R3, or R4 can be the same or different, and they are H or caffeoyl respectively, provided that they cannot be H at the same time; R5 is H , CH3, CH2CH3 or CH2CH2CH2CH3.

Description

technical field [0001] The invention relates to anti-complement drugs, in particular to the application of caffeoylquinic acid and derivatives thereof 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, but activated complement has both physiological and pathological effects: the normal activation of the complement system is used to eliminate foreign microorganisms, remove damaged or dead cells and tissues in the body, and maintain the balance of the body It plays an important role; the abnormal activation of the complement system will cause the excessive reaction of the human immune system, cause damage to the normal tissues of the human body, and participate in the pathological process of various diseases. It has been proven that many diseases such as rheumatoid arthritis, stroke, nephritis, systemic lupus erythematosus, senile dementia, ischemic reperfusion, acut...

Claims

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Application Information

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IPC IPC(8): A61K31/216A61P37/02
Inventor 孙连娜席忠新孙蕾李霞赵贵钧王燕陈伟陈万生
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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