Rhopaladins类似物RPDPRH抗肝癌细胞增殖的实验研究

Experimental Study of Rhopaladins Analogue RPDPRH Against Hepatoma Cell Proliferation

目的:选用肝癌HepG2和7402细胞株,探讨海洋生物碱Rhopaladins类似物(2E,4E)-N-环己基-1-对氟苯基-2-对氯苯乙烯基-4-对氯苄叉基-5-吡咯烷酮-2-酰胺(简称RPDPRH)对肝癌细胞的增殖抑制和周期阻滞的影响。方法:采用CCK-8实验检测Rhopaladins类似物RPDPRH对肝LO2细胞以及肝癌HepG2和7402细胞的增殖抑制。平面克隆实验评估Rhopaladins类似物RPDPRH对肝癌HepG2和7402细胞克隆形成的影响。通过周期实验检测Rhopaladins类似物RPDPRH对肝癌HepG2和7402细胞的周期阻滞情况。采用Hoechst 33258染色法荧光观察经Rhopaladins类似物RPDPRH作用后的肝癌HepG2和7402细胞的凋亡情况。结果:CCK-8实验结果表明Rhopaladins类似物RPDPRH对肝LO2细胞的增殖抑制作用较小,但对肝癌HepG2和7402细胞的增殖具有显著的抑制作用;通过克隆形成实验和细胞周期检测验证了Rhopaladins类似物RPDPRH能够抑制肝癌HepG2和7402细胞的克隆形成,并将肝癌细胞周期阻滞在G0/G1期;Hoechst 33258染色实验发现,经Rhopaladins类似物RPDPRH干预后,在荧光显微镜下可以明显观察到肝癌细胞的凋亡。结论:Rhopaladins类似物RPDPRH对肝LO2细胞具有较小的抑制作用,但其能够表现出很好地抑制人肝癌HepG2和7402两种细胞系的细胞增殖的作用,并且可能与将肝癌细胞周期阻滞在G0/G1期有关。

Objctive To examine the effects of the analogue of marine alkaloids Rhopaladins(2E,4E)-4-(4-chloro⁃benzylidene)-2-(4-chlorostyryl)-N-cyclohexyl-1-(4-fluorophenyl)-5-oxopyrrplidine-2-carboxamide(RPDPRH)on proliferation inhibition and cycle arrest of human hepatoma HepG2 and Bel-7402 cell lines.Methods Growth inhibition by RPDPRH on HepG2 and Bel-7402 cells was assessed by a CCK-8 assay.The effects on colony formation of these cells were evaluated,along with cell cycle analysis to understand the potential blockage induced by RPDPRH.Hoechst 33258 staining was employed to observe the apoptotic changes in treated cells under a fluorescence microscope.Results CCK-8 results indicated that RPDPRH had a modest inhibitory effect on the proliferation of liver LO2 cells,while it significantly suppressed the proliferation of HepG2 and Bel-7402 cells.Colony formation assay and cell cycle analysis confirmed that RPDPRH inhibited colony formation in HepG2 and Bel-7402 cells and arrested the cell cycle in the G0/G1 phase.Hoechst 33258 staining revealed significant hepatic cell apoptosis after RPDPRH intervention.Conclusion RPDPRH shows minimal inhibition on LO2 cells but exhibits potent anti-proliferative effects on HepG2 and Bel-7402 cell lines,which may be relat⁃ed to the arrest of cell cycle in the G0/G1 phase.