Department of Biotechnology, Yonsei University, 50-Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea; Faculty of Biotechnology, Atma Jaya Catholic University of Indonesia, Jalan Jenderal Sudirman 51, Jakarta 12930, Indonesia.
GenoFocus Inc., 65 Techno 1-ro, Gwanpyeong-dong, Yuseong-gu, Daejeon 34014, Republic of Korea.
Bioorg Med Chem Lett. 2020 Dec 15;30(24):127651. doi: 10.1016/j.bmcl.2020.127651. Epub 2020 Oct 29.
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.
姜黄醇，从印度尼西亚爪哇姜黄 Curcuma xanthorrhiza 中分离出来，具有广谱抗菌活性。我们在此报告证据表明，姜黄醇的作用机制可能涉及 FabI，一种烯酰-（ACP）还原酶的抑制。FabI 酶中的预测 Y156V 取代促进了姜黄醇的耐药性，而最初已知对抗菌剂三氯生耐药的 G93V 突变对姜黄醇则无效。另外两个突变，F203L 和 F203V，使 FabI 酶对姜黄醇和三氯生都具有耐药性。这些结果表明，姜黄醇是一种食品级抗菌化合物，针对 FabI，但与三氯生的结合方式不同。
