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The food-grade antimicrobial xanthorrhizol targets the enoyl-ACP reductase (FabI) in Escherichia coli
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-10-29 , DOI: 10.1016/j.bmcl.2020.127651
Yogiara 1 , Elena A Mordukhova 2 , Dooil Kim 3 , Won-Gon Kim 3 , Jae-Kwan Hwang 4 , Jae-Gu Pan 5
Affiliation  

Xanthorrhizol, isolated from the Indonesian Java turmeric Curcuma xanthorrhiza, displays broad-spectrum antibacterial activity. We report herein the evidence that mechanism of action of xanthorrhizol may involve FabI, an enoyl-(ACP) reductase, inhibition. The predicted Y156V substitution in the FabI enzyme promoted xanthorrhizol resistance, while the G93V mutation originally known for triclosan resistance was not effective against xanthorrhizol. Two other mutations, F203L and F203V, conferred FabI enzyme resistance to both xanthorrhizol and triclosan. These results showed that xanthorrhizol is a food-grade antimicrobial compound targeting FabI but with a different mode of binding from triclosan.



中文翻译:

食品级抗菌药黄草醇靶向大肠杆菌中的烯酰-ACP还原酶(FabI)

从印尼爪哇姜黄姜黄提取物中分离得到的黄药酚具有广谱抗菌活性。我们在这里报告的证据表明,黄药的作用机制可能涉及FabI,一种烯酰-(ACP)还原酶,抑制作用。FabI酶中预测的Y156V取代促进了黄曲唑的抗药性,而最初以三氯生抗性而闻名的G93V突变对黄曲唑无效。其他两个突变,F203L和F203V,赋予FabI酶对黄藻唑和三氯生的抗性。这些结果表明,黄药酚是靶向FabI的食品级抗菌化合物,但与三氯生的结合方式不同。

更新日期:2020-11-06
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