IF 1.9 3区 化学 Q3 CHEMISTRY, APPLIED
He Duan, Meifang Zhang, Xin Wang, Fei Xiao, Wenli Li
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引用次数: 0

摘要

抗霉素是一类具有多种生物活性的去肽化合物。然而,它们潜在的临床应用却受到高细胞毒性的阻碍。糖基化通常会对天然产物的理化性质、生物活性和毒性产生深远影响。在这项研究中,我们在深海萃取的白链霉菌 ZH66 中过表达了人工糖基转移酶(GT)基因 sbmGT1,从而发现了三种新的抗霉素衍生物葡糖基抗霉素 A、B 和 C(1-3)。这些衍生物的结构是通过高分辨率电喷雾离子化质谱(HRESIMS)和核磁共振(NMR)分析等光谱方法确定的。糖基化显著提高了抗霉素的水溶性,但同时降低了抗霉素对人宫颈表皮样癌(HeLa)和人肝癌(HepG2)细胞系的细胞毒性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Generation of glucosylantimycins by heterologous expression of a promiscuous glycosyltransferase in a deepsea-derived Streptomyces.

Antimycins are a class of depsipeptide compounds that exhibit diverse bioactivities. However, their potential clinical applications are hampered by high cell toxicities. Glycosylation usually has profound impacts on the physicochemical properties, bioactivities and toxicities of natural products. In this study, we overexpressed an artificial glycosyltransferase (GT) gene sbmGT1 in deepsea-derived Streptomyces albus ZH66, leading to the discovery of three new antimycin derivatives glucosylantimycins A, B and C (1-3). Their structures were determined by a combination of spectroscopic methods, including high resolution electrospray ionisation mass spectrometry (HRESIMS) and nuclear magnetic resonance (NMR) analysis. The glycosylation remarkably improved the water solubility but simultaneously reduced the cytotoxicities of antimycins towards human cervix epidermoid carcinoma (HeLa) and human hepatic carcinoma (HepG2) cell lines.

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来源期刊
Natural Product Research
Natural Product Research 化学-医药化学
CiteScore
5.10
自引率
9.10%
发文量
605
审稿时长
2.1 months
期刊介绍: The aim of Natural Product Research is to publish important contributions in the field of natural product chemistry. The journal covers all aspects of research in the chemistry and biochemistry of naturally occurring compounds. The communications include coverage of work on natural substances of land and sea and of plants, microbes and animals. Discussions of structure elucidation, synthesis and experimental biosynthesis of natural products as well as developments of methods in these areas are welcomed in the journal. Finally, research papers in fields on the chemistry-biology boundary, eg. fermentation chemistry, plant tissue culture investigations etc., are accepted into the journal. Natural Product Research issues will be subtitled either ""Part A - Synthesis and Structure"" or ""Part B - Bioactive Natural Products"". for details on this , see the forthcoming articles section. All manuscript submissions are subject to initial appraisal by the Editor, and, if found suitable for further consideration, to peer review by independent, anonymous expert referees. All peer review is single blind and submission is online via ScholarOne Manuscripts.
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