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开发塞来昔布衍生的抗真菌剂用于作物保护。

Development of celecoxib-derived antifungals for crop protection.

机构信息

Plant Protection Institute, Henan Academy of Agricultural Sciences, Zhengzhou 450002, China.

Plant Protection Institute, Henan Academy of Agricultural Sciences, Zhengzhou 450002, China.

出版信息

Bioorg Chem. 2020 Apr;97:103670. doi: 10.1016/j.bioorg.2020.103670. Epub 2020 Feb 15.

Abstract

Selective COX-2 inhibitor celecoxib was found directly inhibiting the growth of tested phytopathogenic fungi with the inhibitory rate ranging from 30 to 40% at 100 µg/ml. Lead optimization of celecoxib led to the identification of compound 12 among its derivatives as the most active antifungal candidate. The antifungal effect of compound 12 was supposed to be independent of COX-2 inhibition. Transcriptome profiling analysis of Fusarium graminearium (PH-1) treated with compound 12 brought about 406 up-regulated and 572 down-regulated differentially express genes (DEGs) respectively.

摘要

选择性环氧化酶-2(COX-2)抑制剂塞来昔布被发现直接抑制测试的植物病原真菌的生长,在 100μg/ml 时抑制率为 30%至 40%。塞来昔布的先导化合物优化导致其衍生物中的化合物 12 被鉴定为最具活性的抗真菌候选物。化合物 12 的抗真菌作用可能不依赖于 COX-2 抑制。用化合物 12 处理的禾谷镰刀菌(PH-1)的转录组谱分析分别导致 406 个上调和 572 个下调的差异表达基因(DEGs)。

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