阿来环素，一种由海洋链霉菌 ICN19 产生的新型广谱噻肽抗生素。

Ala-geninthiocin, a new broad spectrum thiopeptide antibiotic, produced by a marine Streptomyces sp. ICN19.

机构信息

International Centre for Nanobiotechnology (ICN), Centre for Marine Science and Technology (CMST), Manonmaniam Sundaranar University, Rajakkamangalam-629502, Kanyakumari District, Tamil Nadu, India.

Microbial Strain Collection, Helmholtz Centre for Infection Research GmbH (HZI), Inhoffenstrasse 7, 38124, Braunschweig, Germany.

出版信息

J Antibiot (Tokyo). 2019 Feb;72(2):99-105. doi: 10.1038/s41429-018-0115-2. Epub 2018 Oct 24.

DOI:10.1038/s41429-018-0115-2

PMID:30356080

Abstract

Bioassay-guided screening of antibacterial compounds from the cultured marine Streptomyces sp. ICN19 provided Ala-geninthiocin (1), along with its known analogs geninthiocin (2) and Val-geninthiocin (3) and the indolocarbazole staurosporine (4). The structure of 1 was determined on the basis of 1D and 2D NMR spectra and ESI-HRMS. The absolute configurations of the amino acid residues were determined by enantioselective GC-MS analysis. Compound 1 exhibited potent activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus subtilis, Mycobacterium smegmatis, and Micrococcus luteus, as well as cytotoxicity against A549 human lung carcinoma cells with an IC value of 6 nM.

摘要

从培养的海洋链霉菌 ICN19 中进行的基于生物测定的抗菌化合物筛选提供了 Ala-geninthiocin（1），以及其已知类似物 geninthiocin（2）和 Val-geninthiocin（3）和吲哚咔唑类 staurosporine（4）。基于 1D 和 2D NMR 光谱和 ESI-HRMS 确定了 1 的结构。通过对映选择性 GC-MS 分析确定了氨基酸残基的绝对构型。化合物 1 对革兰氏阳性菌包括金黄色葡萄球菌、枯草芽孢杆菌、耻垢分枝杆菌和藤黄微球菌具有很强的活性，对 A549 人肺癌细胞也具有细胞毒性，IC 值为 6 nM。