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一种拟茎点霉属真菌的Versiol衍生物对结肠癌细胞和黑色素瘤细胞的生长抑制作用

Growth Inhibition of Colon Cancer and Melanoma Cells by Versiol Derivatives from a Paraconiothyrium Species.

作者信息

Cho Namki, Ransom Tanya T, Sigmund Janet, Tran Trong, Cichewicz Robert H, Goetz Michael, Beutler John A

机构信息

Molecular Targets Laboratory, Center for Cancer Research, National Cancer Institute , Frederick, Maryland 21702, United States.

Natural Products Discovery Institute , Doylestown, Pennsylvania 18902, United States.

出版信息

J Nat Prod. 2017 Jul 28;80(7):2037-2044. doi: 10.1021/acs.jnatprod.7b00170. Epub 2017 Jun 27.

Abstract

Bioassay-guided fractionation of a colon cancer growth inhibitory extract of the fungus Paraconiothyrium sp. led to the isolation of eight new versiol derivatives (1, 3-8, 10) along with two known compounds. The structures were elucidated by interpretation of combined MS and 2D NMR spectroscopic data. Compounds 8, 9, and 10 showed cell growth inhibition against COLO205 and KM12 cells, and both 8 and 9 displayed selectivity in their inhibition of melanoma cell lines in the NCI 60 one-dose test. In addition, compound 8 and the crude Paraconiothyrium sp. extract showed potent dose-dependent inhibitory effects in the five-dose NCI 60 cell line assay.

摘要

对真菌拟盾壳霉(Paraconiothyrium sp.)的结肠癌生长抑制提取物进行生物测定导向的分级分离,得到了八个新的versiol衍生物(1、3 - 8、10)以及两种已知化合物。通过综合质谱和二维核磁共振光谱数据的解析确定了其结构。化合物8、9和10对COLO205和KM12细胞具有细胞生长抑制作用,并且在NCI 60单剂量试验中,8和9对黑色素瘤细胞系的抑制均表现出选择性。此外,在NCI 60细胞系五剂量试验中,化合物8和拟盾壳霉粗提取物表现出强效的剂量依赖性抑制作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7a27/6684033/0be1e50d50e5/nihms-1039686-f0002.jpg

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