Cellular and Molecular Research Center, Basic Health Sciences Institute, Shahrekord University of Medical Sciences, Rahmatiyeh, Shahrekord, Iran.
Department of Biology, University of Sistan and Baluchestan, Zahedan, Iran.
Appl Biochem Biotechnol. 2018 Aug;185(4):1132-1144. doi: 10.1007/s12010-017-2684-0. Epub 2018 Feb 22.
Cisplatin resistance is one of the main limitations in the treatment of ovarian cancer, which is partly mediated by long noncoding RNAs (lncRNAs). H19 is a lncRNA involving in cisplatin resistance in cancers. Valproic acid (VPA) is a commonly used drug for clinical treatment of seizure disorders. In addition, this drug may display its effects through regulation of noncoding RNAs controlling gene expression. The aim of the present study was the investigation of VPA treatment effect on H19 expression in ovarian cancer cells and also the relation of the H19 levels with apoptosis and cisplatin resistance. Briefly, treatment with VPA not only led to significant increase in apoptosis rate, but also increased the cisplatin sensitivity of A2780/CP cells. We found that following VPA treatment, the expression of H19 and EZH2 decreased, but the expression of p21 and PTEN increased significantly. To investigate the involvement of H19 in VPA-induced apoptosis and cisplatin sensitivity, H19 was inhibited by a specific siRNA. Our results demonstrate that H19 knockdown by siRNA induced apoptosis and sensitized the A2780/CP cells to cisplatin-induced cytotoxicity. These data indicated that VPA negatively regulates the expression of H19 in ovarian cancer cells, which subsequently leads to apoptosis induction, cell proliferation inhibition, and overwhelming to cisplatin resistance. The implication of H19→EZH2→p21/PTEN pathway by VPA treatment suggests that we could repurpose an old drug, valproic acid, as an effective drug for treatment of ovarian cancer in the future.
顺铂耐药性是卵巢癌治疗的主要限制因素之一,部分是由长链非编码 RNA(lncRNA)介导的。H19 是一种 lncRNA,涉及癌症中的顺铂耐药性。丙戊酸(VPA)是一种常用于治疗癫痫发作的临床药物。此外,这种药物可能通过调节控制基因表达的非编码 RNA 来发挥作用。本研究的目的是研究 VPA 治疗对卵巢癌细胞中 H19 表达的影响,以及 H19 水平与细胞凋亡和顺铂耐药性的关系。简而言之,VPA 治疗不仅导致细胞凋亡率显著增加,而且还增加了 A2780/CP 细胞对顺铂的敏感性。我们发现,VPA 治疗后,H19 和 EZH2 的表达降低,而 p21 和 PTEN 的表达显著增加。为了研究 H19 在 VPA 诱导的细胞凋亡和顺铂敏感性中的作用,我们使用特异性 siRNA 抑制 H19 的表达。我们的结果表明,H19 的 siRNA 敲低诱导了细胞凋亡,并使 A2780/CP 细胞对顺铂诱导的细胞毒性敏感。这些数据表明,VPA 负调控卵巢癌细胞中 H19 的表达,随后诱导细胞凋亡、抑制细胞增殖,并克服顺铂耐药性。VPA 处理通过 H19→EZH2→p21/PTEN 通路的作用表明,我们可以在未来将旧药物丙戊酸重新用作治疗卵巢癌的有效药物。