Centro de Investigaciones Biomédicas-CIB, Escuela de Medicina, Universidad de Valparaíso, Av. Hontaneda N° 2664, Valparaíso, Chile.
Molecules. 2013 May 10;18(5):5348-59. doi: 10.3390/molecules18055348.
In this study, we examined the cytotoxic effects of seven ent-labdane derivatives 1-7 (0-100 μM) in different human cancer cell lines. Our results showed that compounds 1-3 exhibited significant dose-dependent inhibition on the growth of the three different human cell lines, according to the sulphorhodamine B assay and produced morphological changes consistent with apoptosis, as confirmed by Hoestch 3342 staining analysis. They induced apoptosis in various cancer cell lines, as shown by nuclear condensation and fragmentation and caspase 3 activation. Such induction was associated with the depletion of mitochondrial membrane potential. These activities led to the cleavage of caspases and the trigger of cell death process. Overall, the compounds showed potent proapoptotic effects on the two different cancer cell lines, suggesting that the compounds deserve more extensive investigation of their potential medicinal applications.
在这项研究中,我们研究了 7 种 ent-labdane 衍生物 1-7(0-100μM)在不同人类癌细胞系中的细胞毒性作用。根据磺酰罗丹明 B 分析,我们的结果表明,化合物 1-3 对三种不同的人类细胞系的生长表现出显著的剂量依赖性抑制作用,并产生与凋亡一致的形态变化,经 Hoechst 3342 染色分析证实。它们在各种癌细胞系中诱导凋亡,表现为核浓缩和碎裂以及 caspase 3 的激活。这种诱导与线粒体膜电位的耗竭有关。这些活性导致半胱天冬酶的切割和细胞死亡过程的触发。总的来说,这些化合物对两种不同的癌细胞系表现出强烈的促凋亡作用,表明这些化合物值得更广泛地研究其潜在的药用应用。