Effects of Thymoquinone-Fatty Acid Conjugates on Cancer Cells

被引：39

作者：

Breyer, Sandra ^{[1
]}

Effenberger, Katharina ^{[1
]}

Schobert, Rainer ^{[1
]}

机构：

[1] Univ Bayreuth, Organ Chem Lab, D-95440 Bayreuth, Germany

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 05期

关键词：

antitumor agents; conjugates; docosahexaenoic acid; fatty acids; thymoquinones; ANTITUMOR-ACTIVITY; 518A2; MELANOMA; NIGELLA-SATIVA; CYTOCHROME-C; IN-SITU; APOPTOSIS; ACTIVATION; INHIBITION; DRUG; CYTOTOXICITY;

D O I：

10.1002/cmdc.200800430

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Acylhydrazones and 6-alkyl derivatives of thymoquinone (TQ) were tested for growth inhibition of human HL-60 leukemia, 518A2 melanoma, KB-V1/Nbl cervix, and MCF-7/Topo breast carcinoma cells. Unsaturated side chains conferred greater activities than equally long saturated chains. The number of C=C bonds was less decisive than chain length. The 6-hencosahexaenyl conjugate 3 e was most active in all resistant tumor cells, with IC(50) (72 h) values as low as 30 nm in MCF-7/Topo cells. The conjugates are likely to operate by mechanisms different from that of TQ. For instance, 3 e induced distinct caspase-independent apoptosis in HL-60 and 518A2 cells concomitant with a loss of mitochondrial membrane potential and a subsequent rise in the levels of reactive oxygen species.

引用

页码：761 / 768

页数：8

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