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双核铂(Ⅱ)配合物[{Pt(H2O)2I}-μOOC-COO-{Pt(H2O)2I}]对人体癌细胞的作用

Effect of binuclear platinum(Ⅱ) complex [{Pt(H2O)2I}μ-OOC-COO-{Pt(H2O)2I}] on human cancer cells.

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【作者】 张金超张祥龚钰秋郑小明崔景荣杨梦苏

【Author】 ZHANG Jin-chao~(1,2),ZHANG Xiang~3,GONG Yu-qiu~1,ZHENG Xiao-ming~1, CUI Jing-rong~3,YANG Meng-su~4(1.Department of Chemistry,Zhejiang University,Hangzhou 310028,China;2.College of Chemistry & Enviromental Science,Hebei University,Baoding 071002,China;3.Baoding Sino French Water Supply Co,Ltd,Baoding 071000,China;4.Laboratory of Natural and Biomimetic Drugs,Peking University,Beijing 100083,China)

【机构】 浙江大学化学系保定中法供水有限公司北京大学天然药物及仿生药物国家重点实验室 浙江杭州310028河北大学化学与环境科学学院河北保定071002河北保定071000浙江杭州310028北京100083

【摘要】 采用MTT和SRB法研究了双核铂(Ⅱ)配合物[{Pt(H2O)2I}-μOOC-COO-{Pt(H2O)2I}](BPI)对人体癌细胞的增殖抑制作用,又通过流式细胞法、Giemsa染色法、等离子体质谱法研究了它的抗癌机制.实验结果表明:在10μmol.L-1浓度下,该配合物对HL-60,BGC-823,Bel-7402,KB,Hela,HCT-8,MCF-7和EJ 8种肿瘤细胞都表现出有较高的活性,对HL-60、BGC-823和Bel-7402 3种肿瘤细胞的抑制率都在70%以上,它能阻止HL-60细胞G2+M→G1期的进行;对HL-60细胞的凋亡诱导作用不明显;在相同浓度情况下其与HL-60细胞的DNA键合量大于顺铂.

【Abstract】 The antitumor activity of binuclear platinum(Ⅱ) complex [{Pt(H2O)2I}μ-OOC-COO-{Pt(H2O)2I}] was determined by MTT and SRB methods in vitro.At the same time,the anticancer mechanism was studied by flow cytometry,Giemsa and Icp-Ms.The experimental results indicated that the complex had high activity against HL-60、BGC-823,Bel-7402,KB,Hela,HCT-8,MCF-7 and EJ,and the inhibition rate was greater than 70% against HL-60、BGC-823 and Bel-7402 at concentration of 10 μmol·L-1.The cell cycle was arrested on the G2+M→G1,the effect of the complex on apoptosis was not obvious,and the level of total platinum bound to DNA was higher than that of cisplatin under the same conditions.

【基金】 浙江省自然科学基金资助项目(298068);北京大学医学部天然药物及仿生药物国家重点实验室资助项目
  • 【文献出处】 浙江大学学报(理学版) ,Journal of Zhejiang University(Science Edition) , 编辑部邮箱 ,2006年03期
  • 【分类号】R73-36
  • 【被引频次】1
  • 【下载频次】126
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