来自链霉菌 RAL404 的新型细胞毒抗生素奎诺霉素 H1 和 H2。

Quinomycins H1 and H2, new cytotoxic antibiotics from Streptomyces sp. RAL404.

机构信息

Department of Medicinal and Life Science, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba, 278-8510, Japan.

出版信息

J Antibiot (Tokyo). 2018 Oct;71(10):898-901. doi: 10.1038/s41429-018-0083-6. Epub 2018 Jul 17.

DOI:10.1038/s41429-018-0083-6

PMID:30018424

Abstract

Two new cytotoxic antibiotics designated quinomycins H1 (2) and H2 (3) were isolated from the culture broth of Streptomyces sp. RAL404. The molecular formula of both compounds was established as CHNOS by electrospray ionization mass spectrometry (ESI-MS). Their structures were determined as echinomycin (1) derivatives containing a 3-hydoxyquinaldic acid molecule in place of one of the two quinoxaline-2-carboxylic acid chromophores. Quinomycins H1 (2) and H2 (3) showed selective cytotoxicity against RG-E1-4 cells bearing the adenovirus oncogenes with ICs of 11 nM and 12 nM, respectively.

摘要

两种新的细胞毒性抗生素，命名为醌霉素 H1（2）和 H2（3），从链霉菌 RAL404 的发酵液中分离得到。通过电喷雾电离质谱（ESI-MS）确定这两个化合物的分子式均为 CHNOS。它们的结构被确定为含有 3-羟基喹哪啶酸分子取代两个喹喔啉-2-羧酸发色团之一的埃希霉素（1）衍生物。醌霉素 H1（2）和 H2（3）对携带腺病毒癌基因的 RG-E1-4 细胞具有选择性细胞毒性，其 ICs 分别为 11 nM 和 12 nM。