Symplostatin 3，一种来自海洋蓝藻Symploca sp. VP452的新型多拉司他汀10类似物。

Symplostatin 3, a new dolastatin 10 analogue from the marine cyanobacterium Symploca sp. VP452.

作者信息

Luesch Hendrik, Yoshida Wesley Y, Moore Richard E, Paul Valerie J, Mooberry Susan L, Corbett Thomas H

机构信息

Department of Chemistry, University of Hawaii at Manoa, Honolulu, Hawaii 96822, USA.

出版信息

J Nat Prod. 2002 Jan;65(1):16-20. doi: 10.1021/np010317s.

DOI:10.1021/np010317s

PMID:11809057

Abstract

Symplostatin 3 (1), a new analogue of dolastatin 10 (2), has been isolated from a tumor selective extract of a Hawaiian variety of the marine cyanobacterium Symploca sp. VP452. Compound 1 differs from 2 only in the C-terminal unit; the dolaphenine unit is substituted by a 3-phenyllactic acid residue. Symplostatin 3 (1) possesses IC(50) values for in vitro cytotoxicity toward human tumor cell lines ranging from 3.9 to 10.3 nM. It disrupts microtubules, but at a higher concentration than 2, correlating with the weaker in vitro cytotoxicity.

摘要

Symplostatin 3（1）是多拉司他汀10（2）的一种新类似物，已从夏威夷海洋蓝藻Symploca sp. VP452的肿瘤选择性提取物中分离出来。化合物1与2的区别仅在于C末端单元；多拉芬宁单元被一个3-苯基乳酸残基取代。Symplostatin 3（1）对人肿瘤细胞系的体外细胞毒性IC50值在3.9至10.3 nM之间。它会破坏微管，但所需浓度比2高，这与较弱的体外细胞毒性相关。