新型喜树碱衍生物PCC0208021的合成及其体外抗人结直肠癌细胞增殖作用  

Synthesis and in vitro Anti-proliferation Activity against Colorectal Cancer Cells of PCC0208021,One Novel Camptothecin Derivatives

作　　者：李敏[1] 魏颖杰 刘宗亮[1] 邹方霞 王洪波[1] 田京伟[1] LI Min;WEI Ying-jie;LIU Zong-liang;ZOU Fang-xia;WANG Hong-bo;TIAN Jing-wei(School of Pharmacy,Key Laboratory of Molecular Pharmacology and Drug Evaluation(Yantai University),Ministry of Education,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,Yantai University,Yantai 264005,China)

机构地区：[1]烟台大学药学院,新型制剂与生物技术药物研究山东省高校协同创新中心,分子药理和药物评价教育部重点实验室(烟台大学),山东烟台264005

出　　处：《烟台大学学报（自然科学与工程版）》2021年第4期436-441,共6页Journal of Yantai University(Natural Science and Engineering Edition)

基　　金：国家自然科学基金资助项目NSFC(82073888);山东省高等学校优秀青年创新团队资助项目(2019KJM009)。

摘　　要：通过成酯反应合成了一种新型喜树碱类衍生物,并将其命名为PCC0208021。PCC0208021对4种结直肠癌细胞株(LS180、HCT116、HT-29和CT-26)显示出良好的体外生长抑制活性,并能有效抑制2种结直肠癌细胞株(LS180和HCT116)的集落形成;它在体外酶学水平可抑制拓扑异构酶Ⅰ(Topo Ⅰ)的活性;分子对接研究表明PCC0208021与Topo Ⅰ具有较高的结合亲和力。新型喜树碱衍生物PCC0208021有望成为治疗结直肠癌的先导化合物。A novel camptothecin derivative,designed PCC0208021 is synthesized via esterification reaction.PCC0208021 inhibits the proliferation in vitro against 4 colorectal cancer cell lines( LS180,HCT116,HT-29 and CT-26),and inhibits the colony formation in vitro against 2 colorectal cancer cell lines( LS180 and HCT116). Also,it can suppress the activity of Topo Ⅰ and display a high binding affinity in the molecular docking study,and thus is expected to become a lead compound for the treatment of colorectal cancer.

关 键 词：新型喜树碱衍生物 结直肠癌 体外抗肿瘤活性 TopoⅠ抑制剂 

分 类 号：R966[医药卫生—药理学]