Acylated flavonoid glycoside compounds and application thereof in preparation of complement inhibitor medicines

A technology of acylated flavone glycoside compounds and compounds, which is applied in the application field of acylated flavone glycoside compounds and preparation of anti-complement drugs, can solve the problems such as no anti-complement reports of acylated flavone glycosides, and achieve great clinical application value and raw materials The effect of abundant sources and low effective concentration

Inactive Publication Date: 2012-01-04
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

These compounds have pharmacological effects such as antifungal and cytotoxicity, but so far no acylated flavone glycosides with flavone aglycone-4'-sugar-aromatic ring structure or flavone aglycone-7-sugar-aromatic ring structure have anti-complement and anti-complement agents. Report on the Preparation of Complement Inhibitory Drugs

Method used

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  • Acylated flavonoid glycoside compounds and application thereof in preparation of complement inhibitor medicines
  • Acylated flavonoid glycoside compounds and application thereof in preparation of complement inhibitor medicines
  • Acylated flavonoid glycoside compounds and application thereof in preparation of complement inhibitor medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of acylated flavonoid glycoside compounds

[0038] 25 kg of dry whole herb of S. sageii (purchased from Bozhou medicinal material market, Anhui, China) was pulverized, extracted three 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 total S. Extract 2.9kg of extract, take 2.5kg of total extract and suspend with water (15L), extract with equal volume of petroleum ether, ethyl acetate, n-butanol for 3 times in turn, combine ethyl acetate extract and concentrate at 60°C under reduced pressure 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 to dichloromethane: methanol (70:1, 50:1, 30:1, 20:1, 10:1, 5:1, 3:1, 1:1) gradient elution, 20L of each gradient elution, collected dichloromethane:methanol (10:1) elution ...

Embodiment 2

[0044] Example 2 Classical pathway complement inhibition test

[0045] 1 Instruments and reagents

[0046] 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.

[0047] 2 Test drugs

[0048] The total sage extract prepared in Example 1 and the acylated flavonoid glycosides isolated therefrom

[0049] 3 Experimental methods

[0050] 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; the sheep red blood cells were treated with VBS 2+ The buf...

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Abstract

The invention discloses acylated flavonoid glycoside compounds shown as a formula I and application thereof in preparation of complement inhibitor medicines. Acylated flavonoid glycosides extracted and separated from cudweed herb are proved to inhibit hemolysis caused by activation of a complement system in a classical pathway through in vitro experiments, and have complement inhibition effect; the activity of each monomericcompound is higher than that of a total extract of cudweed herb; and the acylated flavonoid glycoside compounds are good complement inhibitors and have low effective concentration, can serve as active ingredients to prepare novel complement inhibitor medicines for treating various diseases caused by abnormal activation of complements, are low in toxicity, safe in administration and rich in raw material sources and have great clinical application value. The structure of the formula I is shown as the specifications, wherein R1 and R2 are same or different, and respectively H, OH or OCH3; and R3 and R4 are respectively H or groups shown in the specifications.

Description

technical field [0001] The invention relates to a complement inhibitor drug, in particular to an acylated flavone glycoside compound and its application in the preparation of an anti-complement drug. Background technique [0002] The complement system is one of the important immune defense systems of the human body. Under normal physiological conditions, the function of complement is mainly to attack foreign pathogens, remove immune complexes, and maintain the balance of the body. However, the abnormal activation of the complement system will cause the excessive response of the human immune system, leading to the damage and inflammatory response of the normal tissue of the human body, which is an important mediator of autoimmune inflammatory response. More and more evidence shows that the occurrence and development of inflammatory diseases are related to the activation of complement. Therefore, how to interfere and inhibit the damage caused by complement activation has bec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/26C07H17/07A61K31/7048A61P37/04
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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