Department of Pathogen Biology and Immunology, Medical College of Nanchang University, Nanchang, 330006, China.
Department of Gastroenterology and Hepatology, Second Affiliated Hospital of Nanchang University, Nanchang, 330006, China.
Naunyn Schmiedebergs Arch Pharmacol. 2021 May;394(5):1009-1018. doi: 10.1007/s00210-020-02018-6. Epub 2020 Nov 18.
Apatinib is a novel, highly selective small-molecule inhibitor of the tyrosine kinase VEGFR-2. Although its safety and efficacy in the treatment of advanced gastric cancer (GC) and other solid tumors have been confirmed, the precise molecular mechanism underlying its efficacy remains unclear. The purpose of this study was to investigate the mechanism by which apatinib regulates the biological functions of GC cells in vitro. The CCK-8 assay was used to detect the inhibitory effect of apatinib at different concentrations on the proliferation of SGC7901 and MKN45 human GC cells. The effects of apatinib on apoptosis, autophagy, and cell cycle-related genes in SGC7901 and MKN45 cells were detected by Western blotting and real-time quantitative PCR (RT-qPCR). JC-1 staining, flow cytometry, Hoechst 33342 staining, dansylcadaverine (MDC) staining, and Transwell assays were used to detect the effects of apatinib on apoptosis, the cell cycle, autophagy, and invasion and migration capacities, respectively, in SGC7901 and MKN45 cells. The inhibitory effect of apatinib on the proliferation of GC cells was dependent on concentration. Apatinib significantly promoted apoptosis and autophagy. It also altered the cell cycle distribution and inhibited the invasion and migration of GC cells. In general, apatinib inhibited the proliferation of GC cells by promoting apoptosis and autophagy, regulating the cell cycle and inhibiting the invasion and migration capacities of GC cells.
阿帕替尼是一种新型、高度选择性的酪氨酸激酶 VEGFR-2 小分子抑制剂。尽管其在治疗晚期胃癌（GC）和其他实体瘤中的安全性和疗效已得到证实，但其确切疗效机制仍不清楚。本研究旨在探讨阿帕替尼体外调节 GC 细胞生物学功能的机制。CCK-8 检测不同浓度阿帕替尼对人 GC 细胞 SGC7901 和 MKN45 增殖的抑制作用。Western blot 和实时定量 PCR（RT-qPCR）检测阿帕替尼对 SGC7901 和 MKN45 细胞凋亡、自噬和细胞周期相关基因的影响。JC-1 染色、流式细胞术、Hoechst 33342 染色、丹磺酰尸胺（MDC）染色和 Transwell 检测分别用于检测阿帕替尼对 SGC7901 和 MKN45 细胞凋亡、细胞周期、自噬和侵袭迁移能力的影响。阿帕替尼对 GC 细胞增殖的抑制作用依赖于浓度。阿帕替尼显著促进细胞凋亡和自噬。它还改变了细胞周期分布，抑制了 GC 细胞的侵袭和迁移。总的来说，阿帕替尼通过促进细胞凋亡和自噬、调节细胞周期和抑制 GC 细胞的侵袭和迁移能力来抑制 GC 细胞的增殖。
