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伯克酸,一种从酸性矿山废弃物真菌嗜极菌中提取的具有选择性抗癌活性的新型螺环缩酮。

Berkelic acid, a novel spiroketal with selective anticancer activity from an acid mine waste fungal extremophile.

作者信息

Stierle Andrea A, Stierle Donald B, Kelly Kal

机构信息

Department of Chemistry, Montana Tech of University of Montana, Butte, MT 59701, USA.

出版信息

J Org Chem. 2006 Jul 7;71(14):5357-60. doi: 10.1021/jo060018d.

Abstract

Berkeley Pit Lake is an abandoned open-pit copper mine filled with 30 billion gallons of acidic, metal-contaminated water. This harsh environment is proving to be a source of unusual microorganisms that produce novel bioactive metabolites. Bioassay-guided fractionation using signal transduction enzyme assays led to the isolation of the novel spiroketal, berkelic acid 1, and of the known gamma-pyrone, spiciferone A 4. Berkelic acid has shown selective, nanomolar activity against OVCAR-3, an ovarian cancer cell line in the National Cancer Institute cell line screen. The isolation and characterization of these compounds are reported here.

摘要

伯克利矿坑湖是一个废弃的露天铜矿,里面充满了300亿加仑酸性的、受金属污染的水。事实证明,这种恶劣环境是产生新型生物活性代谢物的异常微生物的来源。使用信号转导酶测定法进行生物测定引导的分级分离,导致分离出新型螺缩酮伯克利酸1和已知的γ-吡喃酮斯皮西弗酮A 4。在国立癌症研究所细胞系筛选中,伯克利酸对卵巢癌细胞系OVCAR-3显示出选择性的纳摩尔活性。本文报道了这些化合物的分离和表征。

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