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Application of a lignan compound in the preparation of anti-hepatic fibrosis medicine

A technology of lignans and anti-hepatic fibrosis, which is applied in the preparation of sugar derivatives, drug combinations, sugar derivatives, etc., can solve the problems of lack of batch or large-scale preparation methods, lignans without a system, etc. Achieve good biological activity and strong anti-hepatic stellate cell proliferation effect

Active Publication Date: 2019-10-22
BEIJING INSTITUTE OF TECHNOLOGYGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the extraction and separation of lignans has not yet formed a systematic and standardized method, especially the lack of methods suitable for batch or large-scale preparation

Method used

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  • Application of a lignan compound in the preparation of anti-hepatic fibrosis medicine
  • Application of a lignan compound in the preparation of anti-hepatic fibrosis medicine
  • Application of a lignan compound in the preparation of anti-hepatic fibrosis medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation method of embodiment 1 compound

[0035] The lignan compounds described in this example are extracted from natural Bupleurum chinensis, and the specific process is as follows:

[0036] 1) Take 15 kg of dried bamboo-leaf Bupleurum chinensis (produced in Yunnan, China) and grind it into a coarse powder, heat and reflux extraction with 9 times the amount of 75% ethanol for 3 times, each time for 1 hour, filter, combine the filtrates, concentrate under reduced pressure to remove ethanol, Stir and add water to dilute to 40L, and sequentially extract with petroleum ether, ethyl acetate, n-butanol and water. The extracts were collected and rotovaped to obtain individual fractions.

[0037] 2) Dissolve the extracted part of ethyl acetate in ethyl acetate to make the concentration reach 20-50mg / ml, pass through 200-300 mesh silica gel column chromatography, use petroleum ether-ethyl acetate system at 4:1 (v / v) , 1:1 (v / v), 1:8 (v / v), 1:20 (v / v), pure methanol s...

Embodiment 2

[0052] Example 2 In vitro inhibition of activated hepatic stellate cells by MTT method

[0053] In this example, the hepatic stellate cell experiment of in vitro inhibition by MTT method was carried out for the lignan compounds described in the present invention.

[0054] Experimental materials: human hepatic stellate cell line LX-2, rat hepatic stellate cell line T-6

[0055] Drugs to be tested: 15 compounds were prepared with final concentration gradients of 100 μM, 20 μM, 4 μM, 0.8 μM and 0.16 μM.

[0056] Positive control: Saikosaponin d was prepared with final concentration gradients of 100 μM, 20 μM, 4 μM, 0.8 μM and 0.16 μM.

[0057] Taking human hepatic stellate cell line LX-2 as an example, the inhibitory effect of 15 compounds on activated hepatic stellate cells was determined by MTT method.

[0058] (1) Count the LX-2 human hepatic stellate cell line, and make the cells 5×10 4 cells / mL of cell suspension.

[0059] (2) Take the cell suspension and inoculate it in...

Embodiment 3

[0069] Example 3 Anti-hepatic fibrosis experiment in rats

[0070] In this example, an in vivo anti-hepatic fibrosis experiment in rats was carried out for the compound described in the present invention.

[0071] Experimental animals: male SD rats, SPF grade, 6-8 weeks old, weighing 180+-20, purchased from the Experimental Animal Center of the Chinese Academy of Military Medical Sciences, certificate number: SCXK-(Army) 2012-2004. Normal adaptive feeding Conditions: Breeding in independent isolation cages, temperature 18-21°C, humidity >40%, 150Pa pressurized air supply, cycle light (12h light, 12h dark), free access to water and food (standard pellet feed), change the pad every other day feed and fodder.

[0072] Experimental grouping: 265 experimental rats were randomly divided into 18 groups, which were normal group (10 rats), model group (15 rats), compound 1a group (15 rats), compound 1b group (15 rats), compound 1c group ( 15 rats), compound 1d group (15 rats), compou...

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Abstract

The invention provides the application of a lignan compound in the preparation of anti-hepatic fibrosis medicine. After in vitro, in vivo, and molecular level experiments, the lignan compounds described in the present invention prove that they have strong anti-hepatic stellate cell proliferation effects, anti-hepatic fibrosis effects, and anti-matrix metalloproteinase-2 (MMP2), matrix metalloproteinase-9 (MMP9) and transforming growth factor-β1 (TGF-β1) all have low IC50 values, have good binding and inhibit their biological activity, so they can be used as anti-hepatic fibrosis drugs .

Description

technical field [0001] The invention relates to the field of natural product chemical drugs, in particular to the application of a lignan compound in the preparation of anti-hepatic fibrosis drugs. Background technique [0002] Liver fibrosis is a pathological change caused by chronic liver damage caused by various reasons. It is characterized by excessive and abnormal deposition of extracellular matrix components in the liver, which affects the function of the liver. It is a necessary stage for the development of chronic liver disease to cirrhosis. Studies have shown that liver fibrosis may be reversed to normal, but if it progresses to liver cirrhosis, there is no possibility of reversal. Therefore, finding drugs for the treatment of liver fibrosis is a hot research topic of many scholars. Although some progress has been made in the diagnosis and treatment of liver fibrosis, there is still a lack of definitive and effective drugs. However, medicinal materials rich in lign...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K31/7048A61P1/16C07D307/33C07D407/06C07D307/58C07D307/92C07H15/26C07H1/08
CPCA61K31/365A61P1/16C07D307/58C07D407/06
Inventor 戴荣继刘秀洁邓玉林孟薇薇
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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