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KMID : 0370219960400020218
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Yakhak Hoeji
1996 Volume.40 No. 2 p.218 ~ p.224
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In Vitro Cytotoxicity of pt(II) Complexes Containing Ethylenediamine in Rabbit Kidney Proximal Tubular and Human Renal Cortical Cells
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노영수/Rho YS
이경태/정지창/장성구/Lee KT/Jung JC/Chang SG
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Abstract
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This laboratory has recently reported the synthesis and in vitro antitumor activity of PT(II) complexes containing ethylenediamine and diphosphine. In view of the reports of others, cisplatin is toxic to the kidney since the kidney’’s vulnerability to PT(II) complexes may originate in its ability to accumulate and retain platinum to a greater degree than other organs. The in vitro cytotoxicity of these synthetic PT(II) complexes on the primary cultured proximal tubular cells of rabbit kidney and renal cortical cells of human kidney was investigated. Three endpoints for cytotoxicity tests were evaluated:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), 3H-thymidine uptake and the glucose consumption tests. The rank order of sensitivity exhibited 3H-thymidine uptake>MTT>glucose consumption test. The agents with diphosphine leaving group were significantly less cytotoxic than cisplatin. Moreover, 1,2-bis(diphenylphosphino)ethane (DPPE) exhibited less cytotoxicity than 1.3-bis (diphenylphosphino)propane (DPPP) against on rabbit and human cultured kidney cells. Based on these results, the decreased nephrotoxicity of these new complexes over cisplatin appeared to be partially attributable to a leaving group of DPPP and DPPE. This novel class of platinum compound represents a valuable lead in the development of a "third-generation" agent.
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