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11-氧代气硫素:一种源自加勒比海海洋海绵多孔海绵属的具有细胞毒性的抗肿瘤溴酪氨酸衍生生物碱。

11-oxoaerothionin: a cytotoxic antitumor bromotyrosine-derived alkaloid from the Caribbean marine sponge Aplysina lacunosa.

作者信息

Acosta A L, Rodríguez A D

机构信息

Department of Chemistry, University of Puerto Rico, Río Piedras 00931.

出版信息

J Nat Prod. 1992 Jul;55(7):1007-12. doi: 10.1021/np50085a031.

DOI:10.1021/np50085a031
PMID:1402952
Abstract

A new cytotoxic bromotyrosine-derived secondary metabolite, 11-oxoaerothionin [3], was isolated from the Caribbean sea sponge Aplysina lacunosa. The structure of 3 was argued on the basis of detailed spectroscopic analysis and by chemical conversion to the known antibiotic compound 11-hydroxyaerothionin [2]. When screened against a panel of four human cell lines, 11-oxoaerothionin [3] showed pronounced as well as selective antitumor activity toward the human colon (HCT 116) cell line within the limited concentration range of 0.01-0.1 microgram/ml.

摘要

一种新的细胞毒性溴酪氨酸衍生的次生代谢产物,11-氧代气硫素[3],从加勒比海绵Aplysina lacunosa中分离得到。通过详细的光谱分析以及化学转化为已知的抗生素化合物11-羟基气硫素[2],确定了3的结构。在针对四种人类细胞系进行筛选时,11-氧代气硫素[3]在0.01-0.1微克/毫升的有限浓度范围内,对人结肠(HCT 116)细胞系显示出显著且选择性的抗肿瘤活性。

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