帕尔默内酯A，一种源自南极被囊动物阿代尔海鞘的细胞毒性大环内酯。

Palmerolide A, a cytotoxic macrolide from the antarctic tunicate Synoicum adareanum.

作者信息

Diyabalanage Thushara, Amsler Charles D, McClintock James B, Baker Bill J

机构信息

Department of Chemistry, University of South Florida, 4202 East Fowler Avenue CHE205, Tampa, Florida 33620, USA.

出版信息

J Am Chem Soc. 2006 May 3;128(17):5630-1. doi: 10.1021/ja0588508.

DOI:10.1021/ja0588508

PMID:16637618

Abstract

Palmerolide A, a 20-membered macrocyclic polyketide bearing carbamate and vinyl amide functionality, was isolated from the tunicate Synoicum adareanum collected from the vicinity of Palmer Station on the Antarctic Peninsula. Palmerolide A displays potent and selective cytotoxicity toward melanoma (UACC-66 LC50 = 0.018 muM) and appears to operate via inhibition (IC50 = 2 nM) of V-ATPase.

摘要

帕尔默内酯A是一种含有氨基甲酸酯和乙烯基酰胺官能团的20元大环聚酮化合物，它是从南极半岛帕尔默站附近采集的被囊动物阿达雷海鞘中分离出来的。帕尔默内酯A对黑色素瘤表现出强效且具有选择性的细胞毒性（UACC - 66，半数致死浓度LC50 = 0.018 μM），并且似乎是通过抑制V - ATP酶（半数抑制浓度IC50 = 2 nM）来发挥作用的。