Combretastatin A-4 and Derivatives: Potential Fungicides Targeting Fungal Tubulin

文献类型: 外文期刊

第一作者: Zhao, Lei

作者: Zhao, Lei;Zhou, Jiu-jiu;Pang, Wan;Kai, Zhen-peng;Wu, Fan-hong;Yan, Xiao-jing;Wu, Fan-hong

作者机构:

关键词: combretastatin;fungicide;resistance;tubulin;molecular modeling

期刊名称:JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY ( 影响因子:5.279; 五年影响因子:5.269 )

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收录情况: SCI

摘要: Combretastatin A-4, first isolated from the African willow tree Combretum caffrum, is a tubulin polymerization inhibitor in medicine. It was first postulated as a potential fungicide targeting fungal tubulin for plant disease control in this study. Combretastatin A-4 and its derivatives were synthesized and tested against Rhizoctonia solani and Pyricularia oryzae. Several compounds have EC50 values similar to or better than that of isoprothiolane, which is widely used for rice disease control. Structure activity relationship study indicated the the cis configuration and hydroxyl group in combretastatin A-4 are crucial to the antifungal effect. Molecular modeling indicated the binding sites of combretastatin A-4 and carbendazim on fungal tubulin are totally different. The bioactivity of combretastatin A-4 and its derivatives against carbendazim-resistant strains was demonstrated in this study. The results provide a new approach for fungicide discovery and fungicide resistance management.

分类号: R15`S

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