Department of Obstetrics and Gynecology, Ruijin Hospital, Shanghai Jiao Tong University, School of Medicine, Shanghai, P.R. China.
AntiCancer, Inc., San Diego, CA, U.S.A.
Anticancer Res. 2024 Apr;44(4):1399-1407. doi: 10.21873/anticanres.16936.
BACKGROUND/AIM: The prognosis of ovarian cancer (OC) patients is especially poor for patients with chemotherapy resistance. Anlotinib, a novel multi-targeted tyrosine kinase inhibitor, has shown encouraging clinical efficacy in several tumor types. The aim of the present study was to examine the inhibitory efficacy and mechanism of anlotinib on the proliferation and chemosensitivity of OC cells.
The inhibitory effects of Anlotinib on SKOV3 and OVCAR3 OC cells were examined using CCK-8 cell-viability, colony-formation, flow-cytometry, transwell-migration and sphere-formation assays. A xenograft mouse model was used for in vivo studies. RT-qPCR and western blotting were used to detect gene expression.
Molecular targets of anlotinib were elevated in OC patient tumors. Anlotinib significantly inhibited ovarian cancer cell proliferation and migration in vitro. Anlotinib enhanced the sensitivity of ovarian cancer cells to cisplatinum both in vitro and in vivo. Anlotinib suppressed sphere formation and the stemness phenotype of OC cells by inhibiting NOTCH2 expression.
Anlotinib inhibits ovarian cancer and enhances cisplatinum sensitivity, suggesting its future clinical promise.
背景/目的：化疗耐药的卵巢癌（OC）患者预后尤其差。安罗替尼是一种新型多靶点酪氨酸激酶抑制剂，在多种肿瘤类型中显示出令人鼓舞的临床疗效。本研究旨在探讨安罗替尼对 OC 细胞增殖和化疗敏感性的抑制作用及其机制。
采用 CCK-8 细胞活力、集落形成、流式细胞术、Transwell 迁移和球体形成实验检测安罗替尼对 SKOV3 和 OVCAR3 OC 细胞的抑制作用。利用异种移植小鼠模型进行体内研究。采用 RT-qPCR 和 Western blot 检测基因表达。
安罗替尼的分子靶点在 OC 患者肿瘤中上调。安罗替尼显著抑制 OC 细胞在体外的增殖和迁移。安罗替尼在体外和体内均增强了 OC 细胞对顺铂的敏感性。安罗替尼通过抑制 NOTCH2 表达抑制 OC 细胞的球体形成和干性表型。
安罗替尼抑制卵巢癌并增强顺铂敏感性，提示其具有未来的临床应用前景。
