Soini Tea, Pihlajoki Marjut, Kyrönlahti Antti, Andersson Leif C, Wilson David B, Heikinheimo Markku
1 Children's Hospital, University of Helsinki and Helsinki University Hospital, Helsinki, Finland.
2 Department of Pediatrics, School of Medicine, Washington University in St. Louis and St. Louis Children's Hospital, St. Louis, MO, USA.
Tumour Biol. 2017 Mar;39(3):1010428317695016. doi: 10.1177/1010428317695016.
Hepatoblastoma, the most common type of pediatric liver cancer, is treated with a combination of surgery and chemotherapy. An essential drug in the treatment of hepatoblastoma is doxorubicin, which in high doses is cardiotoxic. This adverse effect is due to downregulation of cardiac expression of transcription factor GATA4, leading in turn to diminished levels of anti-apoptotic BCL2 (B-cell lymphoma 2) protein family members. GATA4 is also expressed in early fetal liver, but absent from normal postnatal hepatocytes. However, GATA4 is highly expressed in hepatoblastoma tissue. In this study, we assessed the role of GATA4 in doxorubicin-induced apoptosis of hepatoblastoma cells. Herein, we demonstrate that doxorubicin decreases GATA4 expression and alters the expression pattern of BCL2 family members, most profoundly that of BCL2 and BAK, in the HUH6 hepatoblastoma cell line. Silencing of GATA4 by siRNA prior to doxorubicin treatment sensitizes HUH6 cells to the apoptotic effect of this drug by further shifting the balance of BCL2 family members to the pro-apoptotic direction. Specifically, expression levels of anti-apoptotic BCL2 were decreased and pro-apoptotic BID were increased after GATA4 silencing. On the whole, our results indicate that since high endogenous levels of transcription factor GATA4 likely protect hepatoblastoma cells from doxorubicin-induced apoptosis, these cells can be rendered more sensitive to the drug by downregulation of GATA4.
肝母细胞瘤是最常见的儿童肝癌类型,采用手术和化疗相结合的方法进行治疗。治疗肝母细胞瘤的一种关键药物是阿霉素,高剂量使用时具有心脏毒性。这种不良反应是由于转录因子GATA4的心脏表达下调,进而导致抗凋亡BCL2(B细胞淋巴瘤2)蛋白家族成员水平降低。GATA4在胎儿早期肝脏中也有表达,但在正常出生后的肝细胞中不存在。然而,GATA4在肝母细胞瘤组织中高度表达。在本研究中,我们评估了GATA4在阿霉素诱导的肝母细胞瘤细胞凋亡中的作用。在此,我们证明阿霉素降低了GATA4的表达,并改变了BCL2家族成员的表达模式,在HUH6肝母细胞瘤细胞系中,对BCL2和BAK的影响最为显著。在阿霉素治疗前通过小干扰RNA使GATA4沉默,可使HUH6细胞对该药物的凋亡作用更加敏感,方法是进一步将BCL2家族成员的平衡向促凋亡方向转移。具体而言,GATA4沉默后,抗凋亡BCL2的表达水平降低,促凋亡BID的表达水平升高。总体而言,我们的结果表明,由于转录因子GATA4的高内源性水平可能保护肝母细胞瘤细胞免受阿霉素诱导的凋亡,通过下调GATA4可使这些细胞对该药物更敏感。