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Application of dehydrobiconidyl alcohol in the preparation of anti-liver damage medicine

A technology of coniferyl alcohol and medicine, which is applied in the field of monomer compounds of traditional Chinese medicine, and can solve the problems such as no report on liver protection activity

Active Publication Date: 2021-10-22
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It, but there is no report about the hepatoprotective activity of the lignan dehydrobiconiferyl alcohol (Dehydrodiconify alcohol) in the melon seeds

Method used

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  • Application of dehydrobiconidyl alcohol in the preparation of anti-liver damage medicine
  • Application of dehydrobiconidyl alcohol in the preparation of anti-liver damage medicine
  • Application of dehydrobiconidyl alcohol in the preparation of anti-liver damage medicine

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 the pulverized melon seeds are soaked in ethanol with a volume fraction of 95% for 24 hours, extracted by leakage for 5 to 6 times, the extracts are combined, and the extracts are respectively extracted 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 the sample, 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 7...

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 of co-culture, 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 rates. The results showed that dehydroconiferyl alcohol at a concentration lower than 50 μ...

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] Get 48 SD rats, divide them into 6 groups according to the principle of random distribution, 8 in every group: normal control group, model group ANIT (isothiocyanate-A-naphthyl ester, 60mg / Kg), positive drug UDCA group (100mg / kg), the dehydrobiconiferyl alcohol low-dose group (10mg / kg), the dehydrobiconiferyl alcohol middle-dose group (20mg / kg) and the dehydrobiconiferyl alcohol high-dose group (40mg / kg), placed in Southwest University After 7 days of adaptive feeding in the animal cleaning room of the School of Pharmacy, the animals were administered orally. 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...

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Abstract

The present invention relates to the preparation method of dehydrodiconify alcohol or the ethyl acetate extract of pollen melon seeds with dehydrodiconify alcohol as the main active ingredient and the application in the medicine for preventing or treating liver damage. The extraction method is as follows: the pollen melon seeds are crushed and extracted with ethanol, the extract is extracted with ethyl acetate, concentrated under reduced pressure to obtain an extract. The present invention finds through experiments that dehydrobiconiferyl alcohol can significantly reverse the increase of liver function levels such as ALT and AST in the serum of SD rats with cholestasis induced by ANIT, the decrease of bile flow, and liver lesions, and has a significant protective effect on liver damage; and mainly It functions based on the activation of FXR targets to regulate the expression of its downstream genes. The invention broadens the scope of application of dehydrobiconiferyl alcohol and the ethyl acetate extract of the sunflower seeds, and has important application value and economic benefits for the development of FXR agonist drugs or liver damage protection 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 levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), and bilirubin. Indexes such as superoxide dismutase (SOD), reduced glutathione (GSH) and catalase (CAT) in the liver also increased significantly. Intrahepatic cholestasis, referred t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/343A61K36/42A61P1/16
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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