Application of dehydrodiconify alcohol or extract with dehydrodiconify alcohol as main active ingredient in preparation of anti-liver damage drugs

A technology of active ingredient and coniferyl alcohol, applied in the field of traditional Chinese medicine monomer compounds, can solve problems such as no report on hepatoprotective activity

Active Publication Date: 2019-09-17
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report about the hepatoprotective activity of the lignan dehydrodiconify alcohol (Dehydrodiconify alcohol) in Boling melon seeds

Method used

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  • Application of dehydrodiconify alcohol or extract with dehydrodiconify alcohol as main active ingredient in preparation of anti-liver damage drugs
  • Application of dehydrodiconify alcohol or extract with dehydrodiconify alcohol as main active ingredient in preparation of anti-liver damage drugs
  • Application of dehydrodiconify alcohol or extract with dehydrodiconify alcohol as main active ingredient in preparation of anti-liver damage drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1, the preparation of dehydrobiconiferyl alcohol

[0027] The preparation method of dehydrobiconiferyl alcohol, the specific steps are as follows: after pulverizing the watermelon seeds, soak them in ethanol with a volume fraction of 95% for 24 hours, extract by leakage for 5 to 6 times, combine the extracts, and separate the extracts with petroleum Ether, ethyl acetate and n-butanol organic solvents were extracted successively, each extracted 3 times, respectively combined and sequentially obtained petroleum ether extract, ethyl acetate extract and n-butanol extract, which were concentrated under reduced pressure to obtain extracts of different extraction parts. Take 192 g of ethyl acetate extract, mix the sample with silica gel (100-200 mesh) of equal weight, dry it, and load the sample by dry method. Chloroform:methanol (20:80) eluted fraction was subjected to silica gel column chromatography, and eluted with chloroform:acetone 70:30, crystals were precipi...

Embodiment 2

[0029] Example 2, the protective effect of the compound dehydrobiconiferyl on stesterone-induced L-02 cells

[0030] 1. Dehydrobiconiferyl alcohol was used to determine the survival rate of L-02 cells

[0031] Add dehydrobiconiferyl alcohol at a concentration of 25 μmol / L, 50 μmol / L and 100 μmol / L to L-02 cells for 24 hours and then add MTT (20 μL, 0.5 mg / mL) at 37 °C, 5% CO 2 After incubating in the incubator for 4 hours, discard the MTT, add PBS to wash each well once, add 100 μL DMSO to dissolve formazan, place in a microplate reader and shake for 10 minutes, and measure the absorbance at a wavelength of 570 nm. The results are as follows: figure 1 shown. Taking the absorbance of the blank group as a reference, the cell survival rate was 100%, and the absorbance values ​​of other groups were compared with the absorbance values ​​of the blank group to obtain the survival rate. The results showed that dehydroconiferyl alcohol at a concentration lower than 50 μmol / L could ...

Embodiment 3

[0037] Example 3. Anti-ANIT-induced acute liver injury effect and mechanism of the compound dehydrobiconiferyl in SD rats

[0038] 1. Animal grouping, modeling, and drug administration methods

[0039] 48 SD rats were taken and divided into 6 groups according to the principle of random distribution, 8 rats in each group: normal control group, model group ANIT (A-naphthyl isothiocyanate, 60 mg / Kg), positive drug UDCA group ( 100 mg / kg), dehydroconiferyl alcohol low dose group (10 mg / kg), dehydroconiferyl alcohol medium dose group (20 mg / kg) and dehydroconiferyl alcohol high dose group (40 mg / kg) , placed in the animal clean room of the School of Pharmacy, Southwest University, and fed for 7 days after adaptive feeding. Except the rats in the normal control group and the model group were fed with the same amount of CMC-Na solution every day, the rats in the other groups were fed with their respective doses for 4 consecutive days. On the fifth day, except the rats in the normal...

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Abstract

The invention relates to a method for preparing dehydrodiconify alcohol or an ethyl acetate extract of semen hertospermi with dehydrodiconify alcohol as the main active ingredient and application thereof in hepatoprotective drugs for preventing or treating liver damage. The extraction method includes the following steps that pulverized semen hertospermi is pulverized and extracted with ethanol, the extract is extracted with ethyl acetate, and concentration under reduced pressure is conducted to form the extract. It is found through experiments that dehydrodiconify alcohol can significantly reverse the increase of liver function levels such as ALT and AST in the serum of ANIT-induced cholestasis SD rats, the decrease of bile flow and liver lesions, and has a significant anti-liver damage protective effect; dehydrodiconify alcohol acts mainly by modulating downstream gene expression based on activation of an FXR target. The application range of dehydrodiconify alcohol and the ethyl acetate extract of semen hertospermi is broadened, and the method for preparing dehydrodiconify alcohol or the ethyl acetate extract of semen hertospermi with dehydrodiconify alcohol as the main active ingredient and the application thereof in the hepatoprotective drugs for preventing or treating liver damage have important application value and economic benefit for the development of FXR agonistic drugs and anti-liver damage protective drugs.

Description

technical field [0001] The invention relates to a traditional Chinese medicine monomer compound, in particular to the application of dehydrobiconiferyl alcohol or an extract whose main active ingredient is dehydrobiconiferyl alcohol in the preparation of anti-liver damage medicine. Background technique [0002] Cholestasis in modern medicine refers to a pathological state in which bile formation, secretion and (or) excretion disorders in the liver are caused by various reasons, resulting in bile not flowing normally into the duodenum and back into the blood circulation. It can be manifested clinically as itching, fatigue, dark urine, jaundice, etc. It can also cause a sharp increase in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), bilirubin and other indicators. Indexes such as superoxide dismutase (SOD), reduced glutathione (GSH) and catalase (CAT) in the liver also increased significantly. Intrahepatic cholestasis, ref...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/42A61K31/343A61P1/16
CPCA61K31/343A61K36/42A61K2236/333A61K2236/55A61P1/16
Inventor 陈敏廖志华魏小东马英雄
Owner SOUTHWEST UNIV
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