Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa

被引：24

作者：

Davis, Rohan A. ^{[1
]}

Sykes, Melissa ^{[1
]}

Avery, Vicky M. ^{[1
]}

Camp, David ^{[1
]}

Quinn, Ronald J. ^{[1
]}

机构：

[1] Griffith Univ, Eskitis Inst, Brisbane, Qld 4111, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 22期

基金：

澳大利亚研究理事会;

关键词：

Marine bryozoan; Convolutamines; Antitrypanosomal; Trypanosoma brucei brucei; ANTINEOPLASTIC AGENTS; FLUSTRA-FOLIACEA; BUGULA-NERITINA; BROMINATED ALKALOIDS; MARINE ALKALOIDS; DRUG DISCOVERY;

D O I：

10.1016/j.bmc.2011.06.006

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Mass-directed isolation of the CH(2)Cl(2)/CH(3)OH extract from the marine bryozoan Amathia tortusa resulted in the purification of two new brominated alkaloids, convolutamines I (1) and J (2). The structures of 1 and 2 were determined following spectroscopic data analysis. Both compounds were isolated during a drug discovery program aimed at identifying new antitrypanosomal leads from a prefractionated natural product library. Compounds 1 and 2 were shown to be active toward the parasite Trypanosoma brucei brucei with IC(50) values of 1.1 and 13.7 mu M, respectively. Preliminary toxicity profiling was also performed on both 1 and 2 using the human embryonic kidney cell line, HEK293. Compound 1 was shown to exhibit cytotoxicity against HEK293 with an IC(50) of 22.0 mu M whilst 2 was inactive at 41.0 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：6615 / 6619

页数：5

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