College of Oriental Medicine, Kyung Hee University, Dongdaemun-gu, Seoul, South Korea.
J Pineal Res. 2011 May;50(4):367-73. doi: 10.1111/j.1600-079X.2010.00852.x. Epub 2011 Jan 18.
Melatonin, a naturally occurring molecule, is produced by the pineal gland in a circadian manner to regulate biologic rhythms in humans. Recent studies report that melatonin may be an attractive candidate as an anticancer agent or for combined therapy because of its antioxidant, oncostatic and immunoregulatory activities. In this study, the potentiating effect of melatonin was evaluated on the apoptosis induced by puromycin as an anticancer drug in acute promyelocytic leukemia HL-60 cells. Melatonin did not show significant cytotoxicity against HL-60 cells compared to puromycin. However, melatonin significantly augmented the cytotoxicity of puromycin. Consistently, combined treatment of melatonin and puromycin reduced the expression of anti-apoptotic proteins, such as bcl-2 and bcl-x(L) , and also induced caspase-3 activation and poly (ADP-ribose) polymerase (PARP) cleavage compared to puromycin treatment alone. Furthermore, cell cycle analysis revealed that melatonin promoted puromycin-induced apoptosis by increasing the sub-G1 population, but suppressing G2/M arrest in HL-60 cells. Interestingly, melatonin activated the phosphorylation of 5'-adenosine monophosphate-activated kinase (AMPK) in combination with puromycin. Taken together, our results suggest that melatonin potentiates puromycin-induced apoptosis with caspase-3 and AMPK activation in HL-60 cells, and thus, melatonin treatment can be effectively applied to leukemia treatment as a potential sensitizer for chemotherapeutic agents.
褪黑素是一种内源性分子,由松果腺昼夜节律性地产生,以调节人体的生物节律。最近的研究报告称,褪黑素可能是一种有吸引力的抗癌药物或联合治疗候选药物,因为它具有抗氧化、抗肿瘤和免疫调节活性。在这项研究中,评估了褪黑素对作为抗癌药物的嘌呤霉素诱导的急性早幼粒细胞白血病 HL-60 细胞凋亡的增效作用。与嘌呤霉素相比,褪黑素对 HL-60 细胞没有显示出显著的细胞毒性。然而,褪黑素显著增强了嘌呤霉素的细胞毒性。一致地,与单独用嘌呤霉素处理相比,褪黑素和嘌呤霉素的联合治疗降低了抗凋亡蛋白,如 bcl-2 和 bcl-x(L) 的表达,并且还诱导了 caspase-3 激活和多聚(ADP-核糖)聚合酶(PARP)切割。此外,细胞周期分析表明,褪黑素通过增加亚 G1 群体,同时抑制 HL-60 细胞中 G2/M 阻滞,促进嘌呤霉素诱导的细胞凋亡。有趣的是,褪黑素与嘌呤霉素联合激活了 5'-腺苷单磷酸激活的蛋白激酶(AMPK)的磷酸化。总之,我们的结果表明,褪黑素通过 caspase-3 和 AMPK 的激活增强了嘌呤霉素诱导的 HL-60 细胞凋亡,因此,褪黑素治疗可以作为化疗药物的潜在增敏剂有效地应用于白血病治疗。