Application of 5-hydroxy-2-decenoic acid in preparation of drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer

An anti-hepatic fibrosis and chronic liver disease technology, applied in the field of medicine, can solve the problems of few reports on pharmacological effects, achieve the effect of reducing the deposition of collagen fibers in the liver, reducing the expression of type 1 collagen, and good therapeutic effect

Inactive Publication Date: 2019-11-05
SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

5-Hydroxy-2-decenoic acid is the product after hydrolysis of the lactone ring of massoia lactone (chemical structure see figure 1 ), which are only reported in the synthesis process of some compounds at present, and there are few reports on relevant pharmacological and pharmacodynamic studies
[0009] However, there are no reports of massoia lactone and 5-hydroxy-2-decenoic acid in the treatment of liver diseases

Method used

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  • Application of 5-hydroxy-2-decenoic acid in preparation of drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer
  • Application of 5-hydroxy-2-decenoic acid in preparation of drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer
  • Application of 5-hydroxy-2-decenoic acid in preparation of drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 1 Experiment purpose

[0041] Study on the anti-fibrosis effect of massoia lactone and 5-hydroxy-2-decenoic acid

[0042] 2 Experimental methods

[0043] Experimental animals: The experimental animals used in the present invention are C57BL / 6 mice, weighing 20-22 g, male, provided by the Experimental Animal Center of Shanghai University of Traditional Chinese Medicine.

[0044] Carbon tetrachloride (CCL4) and olive oil used in the experiment were purchased from Sinopharm Chemical Reagent Co., Ltd.; massoia lactone was isolated from fermented Cordyceps mycelium powder in the laboratory, and 5-hydroxy-2-decenoic acid was The massoia lactone is hydrolyzed and converted by base and prepared by column chromatography, the structure is determined by NMR and MS, and the purity is greater than 98% by HPLC area normalization method.

[0045] Forty C57BL mice, SPF grade, were divided into normal group (Control, n=10), liver fibrosis model group (CCL4, n=10), massoia lactone group ...

Embodiment 2

[0070] 1 Experiment purpose

[0071] Investigation of the Anticirrhosis Effects of Massoia Lactone and 5-Hydroxy-2-Decenoic Acid

[0072] 2 Experimental methods

[0073] Experimental animals: The experimental animals used in the present invention are C57BL / 6 mice, weighing 20-22 g, male, provided by the Experimental Animal Center of Shanghai University of Traditional Chinese Medicine.

[0074] Carbon tetrachloride (CCL4) and olive oil used in the experiment were purchased from Sinopharm Chemical Reagent Co., Ltd.; massoia lactone was isolated from fermented Cordyceps mycelium powder in the laboratory, and 5-hydroxy-2-decenoic acid was The massoia lactone is hydrolyzed and converted by base and prepared by column chromatography, the structure is determined by NMR and MS, and the purity is greater than 98% by HPLC area normalization method.

[0075] Forty C57BL mice, SPF grade, were divided into normal group (Control, n=10), liver cirrhosis model group (CCL4, n=10), massoia la...

Embodiment 3

[0100] 1 Experiment purpose

[0101] To investigate the anti-liver cancer effect of massoia lactone and 5-hydroxy-2-decenoic acid.

[0102] 2 Experimental methods

[0103] Experimental animal: The experimental animal used in this experiment is BALB / C (nu / nu) Nude mice, weighing 15-20 g, 4-5 weeks old, were purchased from Shanghai Bangyao Biotechnology Co., Ltd.

[0104] Cell line: Liver cancer HepG-2 cell line was purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences, using DMEM medium containing 10% fetal bovine serum, at 37°C, with a volume fraction of 5% CO 2 , Routine culture under fully saturated humidity conditions, and the cells in the logarithmic growth phase were taken for experiments.

[0105] Massoia lactone is isolated from fermented Cordyceps mycelium powder in the laboratory. 5-Hydroxy-2-decenoic acid is obtained by hydrolysis of massoia lactone base and prepared by column chromatography. The structure is obtained by NMR and MS, the purity ...

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Abstract

The invention relates to an application of 5-hydroxy-2-decenoic acid in preparation of a drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer. The animal model tests show that for CCL4-induced liver fibrosis and cirrhosis in mice, intervention with 5-hydroxy-2-decenoic acid can significantly improve abnormal liver function and reduce serum aspartate aminotransferase, glutamate pyruvate transaminase and total bilirubin levels, reduces liver tissue hydroxyproline content, inhibits liver stellate cell activation, reduces type I collagen expression, and inhibits liver tissue collagen deposition; and for a HepG-2 nude-mouse transplanted tumor model, the use of 5-hydroxy-2-decenoic acid significantly inhibites the growth of the weight and volume of the transplanted tumor. Therefore, the 5-hydroxy-2-decenoic acid can be used for the preparation of the drug for anti-liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer.

Description

[0001] This application is a divisional application, the filing date of the original application: 20170725, the application number: 2017106112818, the name of the invention: a new use of massoia lactone and 5-hydroxy-2-decenoic acid. technical field [0002] The invention relates to the technical field of medicine, in particular to the application of massoia lactone and 5-hydroxy-2-decenoic acid in the preparation of drugs for resisting liver fibrosis, chronic liver disease, liver cirrhosis and liver cancer. Background technique [0003] The Chinese name of Massoia lactone is 5,6-dihydro-6-pentyl-2H-pyran-2-one (see the chemical structure figure 1 ), present in Masoya osmanthus oil, fermented Cordyceps mycelia, liquor, wine, sweet-scented osmanthus and sugar cane molasses, and has antibacterial, anti-infective, and immune-regulating effects. In addition, because of its creamy, coconut, spicy, and celery aroma, it is also often used as a precious spice for butter, cream, vani...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/201A61P1/16A61P35/00
CPCA61K31/201A61P1/16A61P35/00
Inventor 刘平刘伟徐莹戚胜兰陈佳美肖准胡永红
Owner SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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