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Sesquiterpenoid anti-ulcer drug, preparation method and application

A sesquiterpene anti-ulcer technology, which is applied to a class of sesquiterpene anti-ulcer drugs, can solve the problems of lack of scientific data and insufficient support for the development, utilization and protection of Zijinsha medicinal resources.

Inactive Publication Date: 2016-03-09
CHINA THREE GORGES UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The curative effect of folk application is definite, and it has a wide range of application in our province. It has been included as an official variety in the "Quality Standards of Traditional Chinese Medicinal Materials in Hubei Province" (2009 edition), but domestic and foreign scholars have only conducted preliminary research on its pharmacological activity and chemical components. , the scientific information obtained is less, which is not enough to support the development, utilization and protection of Zijinsha medicinal resources

Method used

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  • Sesquiterpenoid anti-ulcer drug, preparation method and application
  • Sesquiterpenoid anti-ulcer drug, preparation method and application
  • Sesquiterpenoid anti-ulcer drug, preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Antiulcer Activity Evaluation of Sesquiterpene Derivatives

[0048] experimental animals

[0049] Kunming mice, weighing 18-22g; provided by the Department of Experimental Zoology, Tongji Medical College, Huazhong University of Science and Technology, certificate number: SCXK (E) 2004-2007.

[0050]

[0051] experimental reagent

[0052] h + / K + - ATPase activity assay kit (Nanjing Jiancheng Institute of Bioengineering); 95% ethanol (Wuhan Chemical Plant, chemically pure). Base solution: PBS, trypsin (0.5%), DMEM medium.

[0053] in vitro H + / K + -ATPase inhibitory activity protocol:

[0054] in vitro H + / K + -ATPase inhibitory activity test process: Take the gastric mucosa of mice with gastric ulcer, add normal saline to make gastric mucosa homogenate, and obtain H-containing + / K + - supernatant of ATPase microsomes. Transfer to a cell culture plate, add the drug to be tested and incubate for a certain period of time, then use commercially available ...

Embodiment 2

[0071] Molecular docking experiment of active sesquiterpene derivatives

[0072] (1) Selection of research strategies for molecular docking

[0073] Molecular docking refers to the process of ligand and receptor molecules recognizing each other through geometric matching and energy matching, which is of great significance in drug design. In the process of producing drug effect, the drug molecule needs to combine with the target enzyme, and then obtain a stable complex conformation through proper conformational adjustment. The molecular docking method puts the ligand molecule at the active site of the receptor, and then evaluates the interaction between the drug ligand and the receptor according to the principles of geometric complementarity, energy complementarity and chemical environment complementarity, and finds out the difference between the two molecules. the best combination mode. The binding strength of ligand and receptor depends on the change of free energy during t...

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Abstract

The invention relates to a sesquiterpenoid anti-ulcer drug which is prepared from bisabolangelone and derivatives thereof. The invention further provides a preparation method of the bisabolangelone and the derivatives thereof, and the sesquiterpenoid anti-ulcer drug is applied to preparation of a drug for preventing and treating a gastric ulcer and a duodenal ulcer. Experimental results prove that the sesquiterpenoid anti-ulcer drug has the better inhibition ratio on an H<+> / K<+>-ATP enzyme.

Description

technical field [0001] The present invention relates to the synthesis method, structure identification and its development of sesquiterpene derivative anti-gastric cancer drugs + / K + -ATPase inhibitory activity, can be used as an acid-suppressing drug for the treatment of related diseases such as gastric ulcer and duodenal ulcer. Background technique [0002] Gastric ulcer is a common disease, frequently-occurring disease, and is distributed worldwide, and the incidence rate in my country accounts for more than 10% of the population. At present, it is believed that the imbalance between aggressive factors and defensive factors of the mucosa is the basis of the pathogenesis of peptic ulcer, and gastric acid has been confirmed as one of the most important pathogenic factors of peptic ulcer. Reducing gastric acid secretion has become the most commonly used method to promote ulcer healing Yu Jieping. Diagnosis and treatment of gastric diseases [M]. Beijing: People's Health Pu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61P1/04A61P31/04C07D307/83
CPCA61K31/343C07D307/83
Inventor 黄年玉汪鋆植邹坤罗华军陈雷王文彬张凡
Owner CHINA THREE GORGES UNIV
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