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从印度尼西亚海绵 Haliclona sp. 中分离得到的巴普胺和海鞘素胺抑制人癌细胞系的增殖。

Papuamine and haliclonadiamine, obtained from an Indonesian sponge Haliclona sp., inhibited cell proliferation of human cancer cell lines.

机构信息

Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, Sendai , Japan.

出版信息

Nat Prod Res. 2013;27(11):1012-5. doi: 10.1080/14786419.2012.688050. Epub 2012 May 11.

Abstract

The extract of an Indonesian marine sponge Haliclona sp. showed potent cytotoxicity against human solid cancer cell lines, MCF-7 (breast), LNCap (prostate), Caco-2 (colon) and HCT-15 (colon) cells. Study on nuclear morphological changes and flow cytometric analysis suggested that the component(s) in the extract would induce an apoptosis to these cancer cells. Bioassay-guided isolation yielded two pentacyclic alkaloids, papuamine (1) and haliclonadiamine (2), which inhibited cell proliferation of six human cancer cell lines with IC50 values of 0.93-1.50 and 1.00-4.44 µM, respectively. Compounds 1 and 2 accumulated lymphoma U937 cells at sub-G1 phase and induced a condensation of chromatin and fragmentation of nucleus.

摘要

印度尼西亚海绵 Haliclona sp. 的提取物对 MCF-7(乳腺癌)、LNCap(前列腺癌)、Caco-2(结肠癌)和 HCT-15(结肠癌)等人体实体癌细胞系具有很强的细胞毒性。核形态变化和流式细胞术分析研究表明,提取物中的成分会诱导这些癌细胞凋亡。基于生物测定的分离得到了两种五环生物碱,papuamine(1)和 haliclonadiamine(2),它们对六种人类癌细胞系的细胞增殖具有抑制作用,IC50 值分别为 0.93-1.50 和 1.00-4.44 μM。化合物 1 和 2 将淋巴瘤 U937 细胞积累在亚 G1 期,并诱导染色质凝聚和核碎裂。

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