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新型放线菌素 A 和 B,一种具有 5H-噁唑并[4,5-b]吩嗪发色团的天然放线菌素,来源于海洋来源的链霉菌 IMB094。

Neo-actinomycins A and B, natural actinomycins bearing the 5H-oxazolo[4,5-b]phenoxazine chromophore, from the marine-derived Streptomyces sp. IMB094.

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China.

出版信息

Sci Rep. 2017 Jun 15;7(1):3591. doi: 10.1038/s41598-017-03769-8.

DOI:10.1038/s41598-017-03769-8
PMID:28620204
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5472614/
Abstract

Neo-actinomycins A and B (1 and 2), two new natural actinomycins featuring an unprecedented tetracyclic 5H-oxazolo[4,5-b]phenoxazine chromophore, were isolated from the marine-derived actinomycete Streptomyces sp. IMB094. Their structures were elucidated by spectroscopic analyses. The presence of this ring system was proposed to originate from a condensation between actinomycin D (3) with α-ketoglutarate and pyruvate, respectively. Compound 1 showed potent cytotoxic activities against human cancer HCT116 and A549 cell lines in the nanomolar range (IC: 38.7 and 65.8 nM, respectively) and moderate antibacterial activities against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) strains.

摘要

新型放线菌素 A 和 B(1 和 2)是从海洋来源放线菌 Streptomyces sp. IMB094 中分离得到的两种具有前所未有四环 5H-噁唑并[4,5-b]吩嗪发色团的新型天然放线菌素。通过光谱分析阐明了它们的结构。该环系的存在被认为是分别由放线菌素 D(3)与α-酮戊二酸和丙酮酸缩合而成。化合物 1 对人癌细胞 HCT116 和 A549 细胞系表现出强烈的细胞毒性,其 IC50 值分别为 38.7 和 65.8 nM,对耐甲氧西林金黄色葡萄球菌(MRSA)和耐万古霉素肠球菌(VRE)菌株也具有中等的抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/05cf2f1684c8/41598_2017_3769_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/a20e71ca57a5/41598_2017_3769_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/54f50aa51d18/41598_2017_3769_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/05cf2f1684c8/41598_2017_3769_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/a20e71ca57a5/41598_2017_3769_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/54f50aa51d18/41598_2017_3769_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/813e/5472614/05cf2f1684c8/41598_2017_3769_Fig3_HTML.jpg

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