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RK-1355A 和 B,新型醌霉素衍生物,从基于 NPPlot 筛选的微生物代谢产物部分文库中分离得到。

RK-1355A and B, novel quinomycin derivatives isolated from a microbial metabolites fraction library based on NPPlot screening.

机构信息

1] Antibiotics Laboratory, RIKEN, Saitama, Japan [2] Industrial Biotechnology Research Laboratory, School of Biological Sciences, Universiti Sains Malaysia, Penang, Malaysia.

RIKEN Center for Sustainable Research Science, Saitama, Japan.

出版信息

J Antibiot (Tokyo). 2014 Apr;67(4):323-9. doi: 10.1038/ja.2013.144. Epub 2014 Feb 5.

Abstract

Two novel quinomycin derivatives, RK-1355A (1) and B (2), and one known quinomycin derivative, UK-63,598 (3), were isolated from a microbial metabolites fraction library of Streptomyces sp. RK88-1355 based on Natural Products Plot screening. The structural elucidation of 1 and 2 was established through two-dimensional NMR and mass spectrometric measurements. They belong to a class of quinomycin antibiotics family having 3-hydroxyquinaldic acid and a sulfoxide moiety. They are the first examples for natural products as a quinoline type quinomycin having a sulfoxide on the intramolecular cross-linkage. They showed potent antiproliferative activities against various cancer cell lines and they were also found to exhibit moderate antibacterial activity.

摘要

从链霉菌 RK88-1355 的微生物代谢产物部分库中,基于天然产物绘图筛选,分离到两个新型醌霉素衍生物 RK-1355A(1)和 B(2)以及一个已知的醌霉素衍生物 UK-63,598(3)。通过二维 NMR 和质谱测量确定了 1 和 2 的结构。它们属于具有 3-羟基邻苯二甲酸和亚砜部分的醌霉素抗生素家族的一类。它们是天然产物作为具有分子内交联亚砜的喹啉型醌霉素的第一个例子。它们对各种癌细胞系表现出很强的抗增殖活性,并且还具有中等的抗菌活性。

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