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来自澳大利亚海棉Pipestela candelabra的强效细胞毒性肽。

Potent cytotoxic peptides from the Australian marine sponge Pipestela candelabra.

作者信息

Tran Trong D, Pham Ngoc B, Fechner Gregory A, Hooper John N A, Quinn Ronald J

机构信息

Eskitis Institute for Drug Discovery, Griffith University, Brisbane, Queensland 4111, Australia.

出版信息

Mar Drugs. 2014 Jun 4;12(6):3399-415. doi: 10.3390/md12063399.

Abstract

Two consecutive prefractionated fractions of the Australian marine sponge extract, Pipestela candelabra, were identified to be selectively active on the human prostate cancer cells (PC3) compared to the human neonatal foreskin fibroblast non-cancer cells (NFF). Twelve secondary metabolites were isolated in which four compounds are new small peptides. Their structures were characterized by spectroscopic and chemical analysis. These compounds inhibited selectively the growth of prostate cancer cells with IC50 values in the picomolar to sub-micromolar range. Structure-activity relationship of these compounds is discussed.

摘要

与人类新生儿包皮成纤维非癌细胞(NFF)相比,澳大利亚海洋海绵提取物烛台管海绵(Pipestela candelabra)的两个连续预分馏部分被鉴定为对人类前列腺癌细胞(PC3)具有选择性活性。分离出了12种次生代谢产物,其中4种化合物是新的小肽。通过光谱和化学分析对它们的结构进行了表征。这些化合物以皮摩尔至亚微摩尔范围内的IC50值选择性抑制前列腺癌细胞的生长。讨论了这些化合物的构效关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dce1/4071583/b4a82fdf0244/marinedrugs-12-03399-g001.jpg

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