Department Pharmaceutical Sciences, College of Pharmacy, The University of Jordan , Amman, 11942, Jordan.
J Nat Prod. 2017 Jun 23;80(6):1827-1836. doi: 10.1021/acs.jnatprod.7b00034. Epub 2017 May 23.
A family of 2,2-dimethyl-3-hydroxy-7-octynoic acid (Dhoya)-containing cyclic depsipeptides, named dudawalamides A-D (1-4), was isolated from a Papua New Guinean field collection of the cyanobacterium Moorea producens using bioassay-guided and spectroscopic approaches. The planar structures of dudawalamides A-D were determined by a combination of 1D and 2D NMR experiments and MS analysis, whereas the absolute configurations were determined by X-ray crystallography, modified Marfey's analysis, chiral-phase GCMS, and chiral-phase HPLC. Dudawalamides A-D possess a broad spectrum of antiparasitic activity with minimal mammalian cell cytotoxicity. Comparative analysis of the Dhoya-containing class of lipopeptides reveals intriguing structure-activity relationship features of these NRPS-PKS-derived metabolites and their derivatives.
从巴布亚新几内亚采集的蓝细菌 Moorea producens 中，采用生物测定指导和光谱方法分离到了一组含有 2,2-二甲基-3-羟基-7-辛炔酸（Dhoya）的环状脂肽家族，命名为 dudawalamides A-D（1-4）。通过 1D 和 2D NMR 实验和 MS 分析相结合，确定了 dudawalamides A-D 的平面结构，而绝对构型则通过 X 射线晶体学、改良的 Marfey 分析、手性相 GCMS 和手性相 HPLC 确定。Dudawalamides A-D 具有广谱抗寄生虫活性，对哺乳动物细胞的细胞毒性最小。对含有 Dhoya 的脂肽类化合物的比较分析揭示了这些 NRPS-PKS 衍生代谢物及其衍生物的有趣的结构-活性关系特征。
