一种源自雪白链霉菌，通过[4+6]环加成反应得到的独特大环内酯衍生物。

A unique macrolactam derivative via a [4+6]-cycloaddition from Streptomyces niveus.

作者信息

Li Liya, Cai Yaping, Jiang Yi, Liu Jiang, Ma Jian, Yuan Chunhui, Mu Yu, Han Li, Huang Xueshi

机构信息

Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, PR China.

Yunnan Institute of Microbiology, Yunnan University, Kunming 650091, PR China.

出版信息

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1599-1604. doi: 10.1016/j.bmcl.2016.02.002. Epub 2016 Feb 2.

DOI:10.1016/j.bmcl.2016.02.002

PMID:26874404

Abstract

One new macrolactam derivative, nivelactam (1) and one new polyenoic acid derivative, niveamide (2), along with two other known 20-atom macrolactams (3 and 4) were isolated from the fermentation broth of Streptomyces niveus, which obtained from the forest soil in northeastern China. The structures of 1 and 2 were elucidated on the basis of HRESIMS, IR, and NMR spectroscopic data analyses. Compound 1 was proposed as an intramolecular [4+6]-cycloaddition product of 3 by S. niveus, and displayed moderate cytotoxic activity against a panel of human tumor cell lines in vitro, with IC50 values ranging from 3.76 ± 0.58 to 15.02 ± 2.81 μM.

摘要

从中国东北森林土壤中分离得到的雪白链霉菌发酵液中，分离出一种新的大环内酯衍生物尼韦拉坦（1）、一种新的多烯酸衍生物尼韦酰胺（2）以及另外两种已知的20元大环内酯（3和4）。通过高分辨电喷雾电离质谱（HRESIMS）、红外光谱（IR）和核磁共振光谱（NMR）数据分析阐明了1和2的结构。化合物1被认为是雪白链霉菌对3进行分子内[4+6]环加成的产物，并且在体外对一组人肿瘤细胞系显示出中等的细胞毒性活性，IC50值范围为3.76±0.58至15.02±2.81μM。