Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, CA 92093-0204, USA.
Department of Chemistry and Biochemistry, University of California, San Diego, CA 92093, USA.
Mar Drugs. 2020 Nov 5;18(11):549. doi: 10.3390/md18110549.
A new cytotoxic thiodepsipeptide, verrucosamide (), was isolated along with the known, related cyclic peptide thiocoraline, from the extract of a marine-derived actinomycete, a sp., our strain CNX-026. The new peptide, which is composed of two rare seven-membered 1,4-thiazepane rings, was elucidated by a combination of spectral methods and the absolute configuration was determined by a single X-ray diffraction study. Verrucosamide () showed moderate cytotoxicity and selectivity in the NCI 60 cell line bioassay. The most susceptible cell lines were MDA-MB-468 breast carcinoma with an LD of 1.26 µM, and COLO 205 colon adenocarcinoma with an LD of 1.4 µM. Also isolated along with verrucosamide were three small 3-hydroxy(alkoxy)-quinaldic acid derivatives that appear to be products of the same biosynthetic pathway.
一种新型细胞毒性硫代二肽，疣孢菌胺（），与已知的相关环状肽硫珊瑚胺一起从海洋来源放线菌的提取物中分离出来，为 属，我们的菌株 CNX-026。新的肽由两个罕见的七元 1,4-噻唑烷环组成，通过光谱方法的组合阐明，绝对构型通过单个 X 射线衍射研究确定。疣孢菌胺（）在 NCI 60 细胞系生物测定中表现出中等的细胞毒性和选择性。最敏感的细胞系是 MDA-MB-468 乳腺癌，LD 为 1.26 μM，COLO 205 结肠腺癌，LD 为 1.4 μM。与疣孢菌胺一起分离出的还有三种小的 3-羟基（烷氧基）喹哪啶酸衍生物，它们似乎是同一生物合成途径的产物。
