Weng Jing-Ru, Bai Li-Yuan, Chiu Shih-Jiuan, Chiu Chang-Fang, Lin Wei-Yu, Hu Jing-Lan, Shieh Tzong-Ming
Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 80424, Taiwan.
Department of Medical Research, China Medical University Hospital, Taichung 40447, Taiwan.
Comput Struct Biotechnol J. 2019 Jan 26;17:151-159. doi: 10.1016/j.csbj.2019.01.004. eCollection 2019.
Cardiac glycosides (CGs), prescribed to treat congestive heart failure and arrhythmias, exert potent antitumor activity. In this study, divaricoside (DIV), a CG isolated from was examined for its antitumor potency in oral squamous cell carcinoma (OSCC) cells. Cell growth was inhibited by DIV in a dose- and time-dependent manner in SCC2095 and OECM-1 OSCC cells using MTT assays. DIV induced S and G2/M phase arrest accompanied by downregulation of phosphorylated CDC25C, CDC25C, and CDC2 in SCC2095 cells. In addition, DIV induced apoptosis by activating caspase-3 and downregulating the expression of Mcl-1. Furthermore, overexpression of Mcl-1 partially reversed DIV-induced death in SCC2095 cells. Additionally, western blot and transmission electron microscopy analyses also indicated that DIV induced autophagy in SCC2095 cells. However, the combination of autophagy inhibitor did not affect DIV-mediated apoptosis in SCC2095 cells. Together, these findings suggest that translational potential of DIV to be developed as a therapeutic agent for OSCC treatment.
用于治疗充血性心力衰竭和心律失常的强心苷（CGs）具有强大的抗肿瘤活性。在本研究中，对从[具体来源未给出]分离出的一种强心苷——双花苷（DIV）在口腔鳞状细胞癌（OSCC）细胞中的抗肿瘤效力进行了检测。使用MTT法，DIV以剂量和时间依赖性方式抑制了SCC2095和OECM - 1 OSCC细胞的生长。DIV诱导S期和G2/M期阻滞，同时伴有SCC2095细胞中磷酸化CDC25C、CDC25C和CDC2的下调。此外，DIV通过激活caspase - 3和下调Mcl - 1的表达诱导细胞凋亡。此外，Mcl - 1的过表达部分逆转了DIV诱导的SCC2095细胞死亡。另外，蛋白质印迹和透射电子显微镜分析也表明DIV诱导了SCC2095细胞的自噬。然而，自噬抑制剂的联合使用并不影响DIV介导的SCC2095细胞凋亡。总之，这些发现表明DIV具有开发成为OSCC治疗药物的转化潜力。
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