摘要
目的为了深入研究稀土配合物的抗肿瘤活性,将稀土配合物开发成抗癌新药,本实验对钐、钇配合物抑制胃癌细胞BGC-823细胞增殖的活性作用及其机制作了探讨。方法磺酰罗丹明B(SRB)法测定钇、钐配合物及硝酸盐对人胃癌细胞株BGC-83增殖的影响;观察稀土配合物诱导BGC-823细胞凋亡,采用流式细胞仪检测稀土配合物对BGC-823细胞周期的影响,运用彗星微凝胶单细胞电泳观察其对BGC-823细胞DNA剪切作用。结果钇、钐配合物明显抑制BGC-823的增殖,并能诱导BGC-823凋亡;经不同浓度钐、钇配合物处理BGC-823细胞的细胞周期发生明显变化并损伤细胞的DNA。结论稀土配合物的体外抗肿瘤活性可能是在5-Fu配体的细胞毒性基础上,稀土离子发挥了协同作用;钐、钇稀土配合物可能通过将胃癌BGC-823细胞阻滞于G0/G1期或直接切断肿瘤细胞DNA诱导细胞凋亡,从而发挥其抗肿瘤活性作用。
OBJECTIVE To investigate the anti-tumor activity and their mechanism of Yttrium and Samarium complexes in vitro. METHODS The cytotoxicity of Sm and Yttrium complexes, Sm ion, Yttrium ion and 5-Fliorouracil （ligand） in BGC-823 was measured by SRB assay. The induction of apoptosis in BGC-823 cell was detected with fluorescent microscope. The alteration of cell cycle was assayed by flow cytometry, and DNA damage in cell was observed by SCGE. RESULTS The growth of BGC-823 was inhibited significantly by Yttrium, Samarium complexes. A considerable number of BGC-823 cells treated with these complexes underwent apoptosis, the alteration of cell cycle and DNA damage were obviously observed by fluorescent microscope in BGC-823 cells treated with Samarium, Yttrium complexes. CONCLUSION It is suggested that the antitumor activities of these lanthanide complexes may be the cooperative effect of 5-Fliorouracil and lanthanide ions, which were probably realized by blocking cells in G0/G1 phase or inducing apoptosis by damaging cells DNA.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第15期1150-1152,1153,1154,共5页
Chinese Pharmaceutical Journal
基金
云南省应用基础研究项目(1999C0066M)
关键词
稀土配合物
人胃癌细胞
抗肿瘤活性
机制
lanthanide complexes
human gastric carcinoma cell
anti-tumor activity
mechanism
