马文他霉素 A 是一种很有前途的抗生素，可用于治疗复杂的传染病。
Mavintramycin A is a promising antibiotic for treating complex infectious disease.
机构信息
Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Drug Discovery Laboratory, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
出版信息
Antimicrob Agents Chemother. 2024 Mar 6;68(3):e0091723. doi: 10.1128/aac.00917-23. Epub 2024 Feb 9.
complex (MAC) is a serious disease that is mainly caused by infection with the non-tuberculous mycobacteria (NTM), and . Seven new compounds, designated mavintramycins A-G (-), were isolated along with structurally related compounds, including amicetin () and plicacetin (), from the culture broth of sp. OPMA40551 as anti-MAC compounds that were active against and . Among them, mavintramycin A showed the most potent and selective inhibition of and . Furthermore, mavintramycin A was active against more than 40 clinically isolated , including multidrug-resistant strains, and inhibited the growth of in a persistent infection cell model using THP-1 macrophages. Mavintramycin A also exhibited efficacy in silkworm and mouse infection assays with NTM. An experiment to elucidate its mechanism of action revealed that mavintramycin A inhibits protein synthesis by binding to 23S ribosomal RNA in NTM. Mavintramycin A, with a different chemical structure from those of clinically used agents, is a promising drug candidate for the treatment of MAC infectious disease.
马文他汀 A（Mavintramycin A）是一种新型的非结核分枝杆菌（NTM）核糖体 RNA 靶向抗生素，对结核分枝杆菌（Mycobacterium tuberculosis）和 MAC 具有强效和选择性抑制作用。
马文他汀 A 是从 sp. OPMA40551 的发酵液中分离得到的，与结构相关的化合物包括阿米卡星（Amicetin）和普里卡汀（Plicacetin）等，具有抗 MAC 活性。
在这些化合物中，马文他汀 A 对 结核分枝杆菌和 MAC 的抑制作用最强。此外，马文他汀 A 对 40 多种临床分离株均有活性，包括耐多药菌株，并且能够抑制 THP-1 巨噬细胞中持续感染细胞模型中 MAC 的生长。马文他汀 A 在 NTM 感染的家蚕和小鼠模型中也表现出良好的疗效。
作用机制研究表明，马文他汀 A 通过与 NTM 的 23S rRNA 结合，抑制蛋白质合成。马文他汀 A 与临床使用的药物具有不同的化学结构，是一种有前途的治疗 MAC 感染性疾病的候选药物。
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