脂盘菌素 A-C，来自 Discodermia kiiensis 的新型细胞毒性脂肽。

Lipodiscamides A-C, new cytotoxic lipopeptides from Discodermia kiiensis.

机构信息

Graduate School of Pharmaceutical Sciences, The University of Tokyo , 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Org Lett. 2014 Jun 20;16(12):3256-9. doi: 10.1021/ol501271v. Epub 2014 Jun 6.

Abstract

Lipodiscamides A-C, three new lipodepsipeptides, were characterized from the marine sponge Discodermia kiiensis. These structurally rare cyclic lipodepsipeptides were found to possess an unprecedented dilactone macrocycle and, thus, represent a new family of lipopeptides. They are the only lipopeptides bearing 4S-hydroxy-trans-2-enoate, and noncanonical amino acids, l-3-ureidoalanine (Uda), E-dehydronorvaline (Denor), and d-citrulline (Cit). MTT assays against P388 and HeLa cells revealed the moderate cytotoxicity of all three compounds.

摘要

脂盘菌素 A-C，三种新型的脂酰二肽，从海洋海绵 Discodermia kiiensis 中被鉴定出来。这些结构罕见的环状脂酰二肽被发现具有前所未有的双内酯大环，因此代表了一个新的脂肽家族。它们是唯一带有 4S-羟基反式-2-烯酸盐、非典型氨基酸 l-3-脲基丙氨酸（Uda）、E-去甲缬氨酸（Denor）和 d-瓜氨酸（Cit）的脂肽。对 P388 和 HeLa 细胞的 MTT 检测表明，所有三种化合物都具有中等的细胞毒性。