Stilbene compound for treating liver injury as well as preparation method and application thereof

A technology of stilbene compounds and liver damage, applied in the field of medicinal chemistry

Inactive Publication Date: 2019-03-26
BEIJING INSTITUTE OF TECHNOLOGYGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no FDA-approved anti-hepatic fibrosis drug. Therefore, starting from the mechanism of hepatic fibrosis, it is very important to find relevant targets that may treat hepatic fibrosis to reverse and control the pathological process of hepatic fibrosis.

Method used

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  • Stilbene compound for treating liver injury as well as preparation method and application thereof
  • Stilbene compound for treating liver injury as well as preparation method and application thereof
  • Stilbene compound for treating liver injury as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0101] Due to the complex operation and small content of the stilbene compounds separated from Baibangjie, the modification and transformation of the group cannot be carried out, so a series of stilbene compounds will be synthesized by using the chemical synthesis method with the phenanthrene compound as the mother nucleus, and tested. Experiments have verified that this type of compound also has anti-hepatic fibrosis activity.

[0102] Synthesis of a series of stilbene compounds

[0103]

[0104] Among them, R1 is H, OBn, p-hydroxybenzyl or isopentenyl, R2 is OH, OCH 3 , OBn, H, p-hydroxybenzyl or isopentenyl, R3, R4, R5, R7 are H, OCH respectively 3 or OH, R6 is OH or OCH 3 , R8 is H.

[0105] Preferably, the stilbene compounds described in the general formula (I) are:

[0106]

[0107]

[0108] Described stilbene compound is:

[0109]

[0110] Among them, R1, R3 are H, OH or OCH respectively 3 , R2 is OH, OCH 3 , R4 is H, R5-R7 are H or OCH 3 .

[0111]...

Embodiment 3

[0131] 1. Pharmacological action of the compound:

[0132] 1) MTT method:

[0133] Accurately weigh the dry samples of the ethanol extract, petroleum ether extract, chloroform extract, ethyl acetate extract, and n-butanol extract respectively, dissolve in DMSO and add 1640 medium to dilute to 1000, 500, 250, 100, 50, 10, 5, 1 μg / mL, the final concentration of DMSO should not exceed 0.1%; 2 Routine subculture in an incubator. Take HSCs in the logarithmic growth phase and adjust the concentration to 1×10 5 / mL inoculated in a 96-well plate, 90 μL per well. Place the 96-well plate at 37°C, 5% CO 2 In the incubator, after culturing for 24 hours, 10 μL of samples from each of the above groups was added, and 6 parallels were set up in each group, and 0.1% DMSO was used as a blank control. After culturing for 24 hours, the absorbance was measured on a microplate reader at 570 nm by the MTT method (tetramethylazolate microenzyme reaction colorimetry). The inhibition rate of each...

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PUM

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Abstract

The invention provides a stilbene compound for treating liver injury as well as a preparation method and an application thereof. The stilbene compound is separated and extracted from a natural product, namely arundina graminifolia or is artificially synthesized. Verification results show that the stilbene compound is capable of treating hepatic fibrosis.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a stilbene compound and its derivatives for treating liver damage, its preparation method and its application. Background technique [0002] Baogan No. 1 is a compound preparation in the Dai Hospital of Xishuangbanna Prefecture. It is composed of ten ingredients, bamboo leaf orchid, hawthorn, schisandra, salvia miltiorrhiza, gentian, and Bupleurum. Anti-inflammatory and anti-oxidant effects. At present, it is mainly used clinically in the treatment of liver fibrosis, chronic hepatitis B and liver cirrhosis. The research work on Baogan No. 1 includes: scale-up research on the water extraction process of Baogan No. 1 semi-finished products and the formulation of quality control standards for semi-finished products, including the establishment and methods of moisture control, thin layer identification (TLC) and content determination (HPLC) methods Scientific investigation; "Baog...

Claims

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Application Information

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IPC IPC(8): C07C43/23C07C41/34C07C46/10C07C50/34A61P1/16
CPCC07C43/23C07C50/34
Inventor 戴荣继高梦旦刘青青王慧婷吕芳刘秀洁邓玉林
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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