NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2022, Vol. 34 ›› Issue (6): 1038-1046.doi: 10.16333/j.1001-6880.2022.6.017

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Determination of anti-Mycobacterium tuberculosis components of Caulis Euonymi Alati and Cinnamomi Cortex by reverse bioassay guided isolation

ZHANG yue1,XIA Meng-yu1,WANG Lei1,ZHAO Xin1,YANG Zai-chang1,2,3 *   

  1. 1School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;2State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medcial University,Guiyang 550014,China;3Key Laboratory of Molecular Design for Plant Cell Factory of Guangdong Higher Education Institutes,Institute of Plant and Food Science,Department of Biology,Southern University of Science and Technology,Shenzhen 518055,China
  • Online:2022-06-28 Published:2022-06-30

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Abstract:

In this study,reverse bioassay guided isolation was used to discover the anti-Mycobacterium tuberculosis (Mbt) components of Caulis Euonymi Alati and Cinnamomi Cortex.The results indicated that usnic acid and cinnamaldehyde were the strongest anti-Mycobacterium tuberculosis components of Caulis Euonymi Alati and Cinnamomi Cortex,respectively.The structure of usnic acid and cinnamaldehyde was modified to obtain 7 derivatives(compounds 1-7),which have strong anti-Mtb activity.Among them,2-(2-benzofuranylmethylene)hydrazinecarbothioamide(1) showed the strongest activity against Mbt (MIC=1 μg/mL).Through molecular docking,quantitative PCR,microscopic imaging,and bactericidal tests,it is speculated that the mechanism of action of compound 1 anti-Mtb is related to the intervention of β-ketoacyl-ACP condensase III of Mbt.

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