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Application of flavonoids compounds in preparation of anticomplement medicaments

A technology of flavonoids and anti-complement, which is applied in the directions of pharmaceutical combinations, pharmaceutical formulations, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2011-06-22
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, more and more studies have shown that the flavonoids in Sophora flavescens have good pharmacological effects such as anti-tumor, anti-oxidation, antipruritic, and inhibition of cGMP phosphodiesterase. Reports with inhibitory effects

Method used

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  • Application of flavonoids compounds in preparation of anticomplement medicaments
  • Application of flavonoids compounds in preparation of anticomplement medicaments
  • Application of flavonoids compounds in preparation of anticomplement medicaments

Examples

Experimental program
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Embodiment 1

[0021] The preparation of embodiment 1 flavonoids

[0022] Take 17 kg of dried roots of Sophora flavescens, repeatedly cold soak and percolate extraction with 95% ethanol at room temperature for several times, and concentrate the extract under reduced pressure to obtain 2.7 kg of extract. Take 1.2kg of extract, suspend in distilled water, extract with petroleum ether, ethyl acetate and n-butanol successively, and concentrate to dryness respectively, among which 460g of ethyl acetate extract. Take 160g of the extract from the ethyl acetate fraction, perform silica gel column chromatography (column specification: 11x85cm, silica gel: 200-300 mesh, 1.8kg), elute with petroleum ether-acetone gradient, and then perform silica gel column chromatography with different eluents. And Sephadex LH-20 column chromatography, concrete steps are as follows:

[0023] The fractions eluted with petroleum ether-acetone (10:1) were subjected to silica gel column chromatography with petroleum ethe...

Embodiment 2

[0024] Example 2 Anti-complement classical pathway test in vitro

[0025] Take 0.04mL of complement (guinea pig serum), add 0.36mL of BBS to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solution. Dissolve 0.1 mL each of 1:1000 hemolysin, 2% SRBC, and 0.2 mL of each concentration of complement in 0.2 mL BBS, mix well, put in a low-temperature high-speed centrifuge at 37 °C for 30 min, and centrifuge at 4000 rpm and 4 °C for 5 min . 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. A full hemolysis group (0.1 mL 2% SRBC dissolved in 0.5 mL triple distilled water) was also 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. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of complement is plot...

Embodiment 3

[0026] Example 3 Anti-complement alternative pathway test in vitro

[0027]Take 0.06mL of complement (human serum), add 0.24mL of AP diluent to prepare a 1:5 dilution solution, and double-dilute to 1:10, 1:20, 1:40, 1:80, 1:160, 1 :320 and 1:640 solutions. Take 0.15mL of each concentration of complement, 0.15mL of AP diluent and 0.20mL of 0.5% RE, mix them evenly, place them in a low-temperature high-speed centrifuge after 30 minutes in a 37°C water bath, and centrifuge at 4000rpm and 4°C for 5 minutes. 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. A complete hemolysis group (0.20 mL of 0.5% RE dissolved in 0.3 mL of triple distilled water) was also 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. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by ea...

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Abstract

The invention belongs to the field of Chinese pharmaceutical technology, and relates to application of flavonoids compounds(formula I) in the preparation of anticomplement medicaments. The flavonoids compounds are extracted from ethyl acetate of Sophora flavescens, and in vitro anticomplementary activity screening tests of the flavonoids compounds prove that the flavonoids compounds have quite good effect of inhibiting the classical pathway and the alternative pathway of a complement system. The CH50 of the effect of the flavonoids compounds in inhibiting the classical pathway is 0.12+ / -0.02mg / mL to 0.35+ / -0.03mg / mL, and the AP50 of the effect of the flavonoids compounds in inhibiting the alternative pathway is 0.45+ / -0.05mg / mL. The flavonoids compounds can be furthered used for preparing the anticomplement medicaments.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy and relates to new uses of medicines, in particular to new uses of flavonoids in Sophora flavescens in preparing anti-complement medicines. Background technique [0002] It is known that the complement system is one of the important immune defense systems of the human body, and plays an important role in physiological processes such as eliminating foreign microorganisms and maintaining the balance of the body. Excessive activation of the complement system can lead to systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases. At present, there is no ideal drug for the treatment of such diseases, so there is an urgent need for a new type of complement inhibitor with high efficiency, low toxicity and specificity in clinical practice. The cost of researching and developing complement inhibitors directly from natural products is low,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P37/02
Inventor 陈道峰何常明
Owner FUDAN UNIV
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