草酸-甘油交联物的合成及抗肿瘤活性研究  

Synthesis and Anti tumor Activity of Conjugate of Oxalic Acid and Glycerol

作　　者：戴一[1] 许飞 盛志敏 吴亚东 DAI Yi;XU Fei;SHENG Zhi-min;WU Ya-dong(Pharmacology College,Anhui Xinhua University,Hefei 230088,China;The Storehouse of Chinese Herbal Medicine,The General Hospital of Dingyuan County,Chuzhou 233290,China)

机构地区：[1]安徽新华学院药学院,安徽合肥230088 [2]定远县总医院中草药药库,安徽滁州233290

出　　处：《宜春学院学报》2024年第12期11-14,70,共5页Journal of Yichun University

基　　金：安徽省高等学校科研计划重点项目(编号:2024AH050624);安徽新华学院药物研究所(编号:yjs202107);抗肿瘤先导物研究团队项目(编号:kytd202211);国家级大学生创新创业训练计划项目(编号:202312216051,202312216052)。

摘　　要：细胞内钙离子的浓度与肿瘤的发生发展有着重要的联系,打破肿瘤细胞内钙离子稳态具有抑制肿瘤细胞生长的潜力。本实验以草酰氯为起始原料通过与甘油反应制得草酸-甘油交联物,该交联物可以自组装成水合粒径约为140 nm的纳米颗粒。噻唑兰(MTT)法测定结果显示相比于单独的草酸,该纳米颗粒对肝癌HepG2细胞的细胞毒性显著强于草酸,而对正常肝LO2细胞的细胞毒性甚微,比单独的草酸具有更高的安全性,细胞凋亡测试也显示出该交联物能更强的诱导肿瘤细胞凋亡,通过钙离子荧光探针Fluo-4 AM显示,该交联物纳米颗粒可以降低肿瘤细胞内的钙离子浓度,说明草酸的钙螯合能力具有潜在的药用开发价值。The concentration of intracellular calcium ions is closely related to the occurrence and progression of tumors,and disturbing the homeostasis of calcium ions in tumor cells has the potential to inhibit growth of tumor cells.This experiment used oxalyl chloride as the starting material to react with glycerol for preparing oxalic acid-glycerol conjugate.Oxalic acid-glycerol conjugate could self-assemble into nanoparticles with a hydrated particle size of approximately 140 nm.The result of thiazolium tetrazolium(MTT)method showed that the nanoparticles had a stronger cytotoxicity to human hepatoma HepG2 cells than that of oxalic acid.In addition,the cytotoxicity of the nanoparticles toward normal human liver LO2 cells was minimal,showing they had high safety.The apoptosis assay also showed that oxalic acid-glycerol conjugate more strongly induced apoptosis of HepG2 cells.The underlying mechanism was investigated,showing that the concentration of intracellular calcium ion demonstrated by fluorescence probe Fluo-4 AM,was decreased by the nanoparticles.It can be seen that the ability to chelate calcium of oxalic acid has a potential value for drug development.

关 键 词：草酸 甘油 交联物 抗肿瘤活性 

分 类 号：R284.3[医药卫生—中药学]