European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2017-08-24 , DOI: 10.1016/j.ejmech.2017.08.022 Peihong Qiu , Shanshan Zhang , Yangyang Zhou , Min Zhu , Yanting Kang , Dahui Chen , Jiabing Wang , Peng Zhou , Wulan Li , Qing Xu , Rong Jin , Jianzhang Wu , Guang Liang
NF-κB is a critical target for cancer treatment due to its central role in facilitating cancer progression and desensitizing cancer cells to chemotherapeutic drugs. In this study, a series of chemically modified asymmetric curcuminoid analogs named S01–S15 were synthesized and evaluated for NF-κB inhibitory activity in gastric cancer cell lines. Cell growth inhibition assays revealed that most of these analogs effectively inhibited the growth of BGC-823, SGC-7901, and MFC cells. S06 was selected for further research. MTT assay, clonogenic assay, Hoechst 33258 staining assay, and western blotting revealed that S06 could exert anti-gastric cancer effects by downregulating NF-κB activity. Moreover, via its effects on NF-κB, S06 effectively enhanced the sensitivity of the gastric cancer cells to irinotecan. Together, this study provide a series of new curcuminoid analogs as promising cancer therapeutic agents.
中文翻译:
非对称姜黄素类似物的合成和评估作为潜在的抗癌剂,可下调NF-κB活化并增强胃癌细胞系对伊立替康化疗的敏感性
NF-κB是癌症治疗的重要靶标,因为它在促进癌症进展和使癌细胞对化学治疗药物脱敏方面起着核心作用。在这项研究中,合成了一系列化学修饰的不对称姜黄素类似物S01–S15,并评估了它们在胃癌细胞系中的NF-κB抑制活性。细胞生长抑制试验表明,大多数类似物均能有效抑制BGC-823,SGC-7901和MFC细胞的生长。选择S06进行进一步研究。MTT法,克隆形成法,Hoechst 33258染色法和western blotting显示,S06可通过下调NF-κB活性来发挥抗胃癌作用。此外,通过对NF-κB的作用,S06有效地增强了胃癌细胞对伊立替康的敏感性。一起,