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Application of penthorum chinense pursh monomer in preparation of liver protection medicine

A technology for liver protection and drugs, which is applied in the field of preparation of liver protection drugs, can solve the unseen problems of insufficient enrichment of active ingredients, etc., and achieve excellent effects, good clinical application prospects, and definite curative effects

Active Publication Date: 2015-12-30
四川古蔺肝苏药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported in the literature that C. chinensis has the pharmacological activity of preventing and treating hepatitis and protecting the liver, but so far there has been no report on the active ingredients of C. chinensis on the prevention and treatment of ischemia-reperfusion liver injury and chemical liver injury.
In addition, the "Gansu Granules" series of Ganhuangcaocheng prescription preparations currently in clinical use, because the production process is still the traditional water extraction and alcohol precipitation, the active ingredients are not fully enriched, and they are mostly used in clinical adjuvant treatment of liver diseases, so further research is needed. improvement

Method used

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  • Application of penthorum chinense pursh monomer in preparation of liver protection medicine
  • Application of penthorum chinense pursh monomer in preparation of liver protection medicine
  • Application of penthorum chinense pursh monomer in preparation of liver protection medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 macrocyclic polyphenol compound

[0031] Take 30kg of root vegetables, crush them, add 10-15 times of water to decoct twice, each time for 2 hours, combine the extracts, concentrate under reduced pressure (60°C) to get the crude extract (relative density is 1.12-1.18), centrifuge ( 5000rpm / min), to obtain 3.5kg of precipitated parts. Take 3.0kg of the precipitation part, add 3.0kg100-200 mesh silica gel, carry out silica gel column chromatography, use dichloromethane:methanol (50:1-0:1) gradient elution, detect through TLC (silica gel thin-layer plate), get 13 fractions (Fr 1 -Fr 13 ). Merge Fr 10 and Fr 11 Two parts, concentrated, suspended in water and centrifuged (5000rpm / min), subjected to MCI-CHP20P gel column chromatography, gradient elution with methanol: water (1:9~1:0), and TLC (silica gel thin layer plate) Detected and obtained 10 fractions (Fr 1 -Fr 10 ). Fraction Fr 8 Segmented by a reverse-phase silica gel column (O...

experiment example 1

[0034] Experimental example 1 in vitro liver cell protection experiment

[0035] 1 Materials and methods

[0036] 1.1 Test drugs

[0037] Example 1 Preparation of the obtained monomeric compound joconin dihydrochalcone-7-O-[3"-O-galloyl-4", 6"-hexahydroxybiphenyldiformyl]-β-D-glucoside, The structural formula is as follows I:

[0038]

[0039] Experimental Materials

[0040] Hydrogen peroxide (H 2 o 2 ), analytically pure, purchased from Shanghai Sinopharm Chemical Reagent Co., Ltd.; cell culture: DMEM medium (Dulbecco'sModifiedEagle'sMedium) dry powder, PRMIMedium1640 medium dry powder, fetal bovine serum (fetalbovineserum, FBS) are all products of Gibco, USA; Trypsin (Trypsin), product of Amresco Company; Cytotoxicity and proliferation test: CellCountingKit-8 (CCK-8 kit), purchased from Beyontien Institute of Biotechnology; cell line: human normal liver cell line (HL-7702), Purchased from Shanghai Cell Bank, Chinese Academy of Sciences; main equipment: PowerWaveXS m...

experiment example 2

[0057] Experimental example 2 Experiment of prevention and treatment of ischemia-reperfusion liver injury by macrocyclic polyphenol monomer compound in vivo

[0058] 1 Materials and methods

[0059] 1.1 Test drugs

[0060] Example 1 Preparation of the obtained monomeric compound joconin dihydrochalcone-7-O-[3"-O-galloyl-4", 6"-hexahydroxybiphenyldiformyl]-β-D-glucoside, The structural formula is as follows I:

[0061]

[0062] 1.2 Experimental materials

[0063] SD rats (Shanghai Slack Experimental Animal Co., Ltd., animal certificate number: SYXK (Shanghai) 2013-0005; body weight: about 250g; gender: male; 6 rats per group); MDA, T-SOD kit

[0064] 1.3 Establishment of rat liver ischemia-reperfusion injury model:

[0065] The rat was anesthetized with 10% chloral hydrate, and after about one minute, the rat was unconscious. The rat was fixed on the operating table, and 75% alcohol was sprayed on the abdomen for disinfection. Cut the endothelium from the midline of the...

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Abstract

The invention provides an application of pinocembrin dihydrogen chalcone-7-O-[3'-O-galloyl-4',6'-hexahydroxydiphenodicarboxy]-beta-D-glucoside in preparation of a liver protection medicine. The penthorum chinense pursh macrocyclic polyphenol monomer namely pinocembrin dihydrogen chalcone-7-O-[3'-O-galloyl-4',6'-hexahydroxydiphenodicarboxy]-beta-D-glucoside has a liver protection effect, can be used for preventing and treating liver injuries, and has a definite curative effect on hepatic ischemia-reperfusion injuries and chronic liver injuries, and the effect is superior to that of positive medicine namely Gansu Granules, so that the penthorum chinense pursh macrocyclic polyphenol monomer can be used for replacing the Gansu Granules and has a good clinical application prospect.

Description

technical field [0001] The present invention relates to the use of C. chinensis monomer in the preparation of liver protection drugs, specifically, chopinenine dihydrochalcone-7-O-[3"-O-galloyl-4", 6"-hexahydroxybiphenyl Use of formyl]-β-D-glucoside in the preparation of liver protection drugs. Background technique [0002] Common liver injuries include ischemia-reperfusion liver injury and chemical liver injury. Among them, ischemia-reperfusion injury (ischemiareperfusioninjury, IRI) is one of the most common problems in clinical surgery. Ischemic injury occurs when the blood perfusion flow of tissues and organs is reduced due to various reasons, and after the blood perfusion is restored, the cell function metabolism and structural damage are aggravated, resulting in ischemia-reperfusion injury. Today, as the technology of liver transplantation is becoming more and more mature, after the transplanted liver undergoes ischemic injury, with the opening of the blood, it will ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P1/16
Inventor 江云陈万生孙连娜张大永黄豆豆兰泽伦刘静
Owner 四川古蔺肝苏药业有限公司
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