Department of Thoracic Surgery, The First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu, 210009 China.
Department of Radiotherapy, Nantong Tumor Hospital, Nantong, Jiangsu, 226361 China.
Biomed Pharmacother. 2018 Feb;98:694-700. doi: 10.1016/j.biopha.2017.12.106. Epub 2018 Jan 4.
Gastric cancer is a common cancer in the world with high morbidity and mortality. Here, we report that FPHPB (4-(4-(2-fluoropyridin-3-yl)phenyl)-N-(4-hydroxyphenyl)), a derivative of CMPD-1/MK2a Inhibitor, had anti-tumor activities by inhibiting gastric tumor SNU-16 and SGC7901 cells. FPHPB dose-dependently inhibited cell proliferation, induced cell apoptosis and arrested SNU-16 and SGC7901 cells in G2-M cell cycle checkpoint. Upon treatment with FPHPB, apoptotic proteins cleaved PARP and cleaved caspase-3 were remarkably increased, and G2-M regulatory molecules, the phosphorylation of Cdc2 and Chk2, were significantly accentuated. Collectively, FPHPB has anti-tumor activities and may be a potential candidate for treating gastric cancers.
胃癌是一种常见的癌症，发病率和死亡率都很高。在这里，我们报告说，FPHPB（4-（4-（2-氟吡啶-3-基）苯基）-N-（4-羟基苯基）），CMPD-1/MK2a 抑制剂的衍生物，通过抑制胃肿瘤 SNU-16 和 SGC7901 细胞具有抗肿瘤活性。FPHPB 呈剂量依赖性抑制细胞增殖，诱导细胞凋亡，并使 SNU-16 和 SGC7901 细胞停滞在 G2-M 细胞周期检查点。用 FPHPB 处理后，凋亡蛋白 cleaved PARP 和 cleaved caspase-3 明显增加，G2-M 调节分子 Cdc2 和 Chk2 的磷酸化明显增强。总之，FPHPB 具有抗肿瘤活性，可能是治疗胃癌的潜在候选药物。
