Novel use of oridonin derivatives in preparing antituberculosis drugs

A technology of Rubescensine A and its derivatives, which is applied in the field of medicine and can solve the problems of no anti-tuberculosis Mycobacterium

Inactive Publication Date: 2014-07-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Rubescensin A is a natural organic compound of kaurene diterpenoids extracted and separated from Rubescens japonicus. Over the past 30 years, with the in-depth research on it, scholars at home and abroad have found that it is effective in esophageal cancer, gastric cancer, liver cancer, and lung cancer. , nasopharyngeal cancer, colon cancer, bladder cancer, cervical cancer and leukemia all have a certain therapeutic effect, and the study of its pharmacological activity has attracted much attention, but there has been no report of anti-mycobacterium tuberculosis

Method used

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  • Novel use of oridonin derivatives in preparing antituberculosis drugs
  • Novel use of oridonin derivatives in preparing antituberculosis drugs
  • Novel use of oridonin derivatives in preparing antituberculosis drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1. Anti-mycobacterium tuberculosis activity experiment of oridonin

[0031] The MIC experiment was carried out in a 96-well plate. The test compound was dissolved in an appropriate amount of DMSO to make a solution with a concentration of 12.8 mg / ml, and then added to the 7H9-OADC culture medium to make a stock solution with a final concentration of 128 μg / ml. , and then diluted with liquid medium to the concentration required for the experiment. The final concentration of the tested drug was set as follows: 128, 64, 32, 16, 8, 4, 2, 1, 0.5, 0.25, 0.125 μg / ml, a total of 11 concentration gradients.

[0032] During the detection, 100 μL of the above-mentioned drug solutions were each taken in a 96-well plate, and three groups of parallel controls were set up at the same drug dilution. Mycobacterium phlei M.phlei, Mycobacterium smegmatis M.smegmatis, Mycobacterium marinum M.marinum and Mycobacterium tuberculosis standard strain H 37 Rv was added to the culture w...

Embodiment 2

[0038] tablet

[0039]

[0040] Get above-mentioned prescription, prepare into tablet with conventional method.

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PUM

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Abstract

The invention relates to the field of pharmaceutical chemistry and specifically relates to oridonin and an ent-6, 7-ring opening kaurene type derivative thereof. The invention discloses oridonin derivatives and use of the oridonin derivatives in preparing antituberculosis drugs.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to the new use of oridonin and its derivatives or pharmaceutically acceptable salts thereof in the preparation of anti-tuberculosis drugs. technical background: [0002] Lamiaceae Coriander is a plant of the genus Cordyceps, which mainly includes tablets and syrups, as well as compound Donglingcao tablets, oridonium buccal tablets, etc. It is mainly used clinically for the treatment of inflammation and tumors, and has a certain curative effect. Rubescensin A is a natural organic compound of kaurene diterpenoids extracted and separated from Rubescens japonicus. Over the past 30 years, with the in-depth research on it, scholars at home and abroad have found that it is effective in esophageal cancer, gastric cancer, liver cancer, and lung cancer. , nasopharyngeal cancer, colon cancer, bladder cancer, cervical cancer and leukemia all have a certain therapeutic effect, and the study of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/366A61P31/06
Inventor 徐进宜徐盛涛李达翃蔡浩裴玲玲姚鸿张恒源周志文王超磊姚和权吴晓明谢唯佳
Owner CHINA PHARM UNIV
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