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从红海海绵 Diacarnus erythraeanus 中分离出的诺特佩烷过氧化物对正常细胞和癌细胞的体外药理和毒理学作用。

In vitro pharmacological and toxicological effects of norterpene peroxides isolated from the Red Sea sponge Diacarnus erythraeanus on normal and cancer cells.

机构信息

Service de Neurochirurgie, Hôpital Erasme, ULB, Route de Lennik, 1070 Brussels, Belgium.

出版信息

J Nat Prod. 2013 Sep 27;76(9):1541-7. doi: 10.1021/np400107t. Epub 2013 Aug 26.

DOI:10.1021/np400107t
PMID:23977995
Abstract

Eight cyclic peroxide norterpenoids, compounds 1-8, have been isolated and characterized from the Red Sea sponge Diacarnus erythraeanus, including two new norsesterterpene derivatives (3, 4). Among these metabolites, (-)-muqubilin A (5) (nine cell lines analyzed) and the new compounds 3 and 4 (seven cell lines analyzed) displayed mean IC₅₀ growth inhibitory concentrations in vitro of <10 μM, while the remaining compounds (1, 6-8) were inactive in these cancer cell lines. Compound 5 displayed no selectivity between normal and cancer cells in terms of in vitro growth inhibition. Quantitative video microscopy analysis carried out on (-)-muqubilin A-treated cells validated the data obtained by means of the MTT colorimetric assay, while flow cytometry analysis revealed ROS production but no induction of apoptosis in cancer cells.

摘要

从红海海绵 Diacarnus erythraeanus 中分离得到了 8 种环过氧化物诺特培烯类化合物,化合物 1-8,包括 2 种新的诺甾萜烯衍生物(3、4)。在这些代谢产物中,(-)-muqubilin A(5)(分析了 9 种细胞系)和新化合物 3 和 4(分析了 7 种细胞系)在体外显示出平均 IC₅₀ 生长抑制浓度<10 μM,而其余化合物(1、6-8)在这些癌细胞系中没有活性。化合物 5 在体外生长抑制方面对正常细胞和癌细胞没有选择性。对(-)-muqubilin A 处理的细胞进行定量视频显微镜分析验证了通过 MTT 比色法获得的数据,而流式细胞术分析显示在癌细胞中产生了 ROS,但没有诱导细胞凋亡。

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