Cytotoxicity of Platinum(IV) and Platinum(II) Complexes Containing lR,2R-Cyclohexanediamine as a Ligand.
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Several Pt(IV) and Pt(II) complexes containing 1R, 2R-cyclohexanediamine (1R, 2R-dach) as a carrier ligand were synthesized. The cytotoxicities and the uptake of the platinum complexes by leukemia L1210 cells were compared in order to study the correlation between their structures and cytotoxicities.[Pt(II)Cl2(1R, 2R-dach)], [(Pt(II)(oxalato)(1R, 2R, -dach)], and [Pt(II)(malonato)(1R, 2R-dach)], which have excellent anticancer properties, exhibited very high cytotoxicities and were easily taken up by leukemia L1210 cells. [Pt(IV)Cl4(1R, 2R-dach)], trans(Cl)-[Pt(IV)Cl2(oxalato)(1R, 2R-dach)], and trans(Cl)-[Pt(IV)Cl2(malonato)(1R, 2R-dach)] also had high cytotoxicities. After a short incubation time, the uptake of [Pt(II)Cl2(1R, 2R-dach)], [Pt(II)(oxalato)(1R, 2R-dach)], and [Pt(II)(malonato)(1R, 2R-dach)] by leukemia L1210 cells were respectively very similar to those of [Pt(IV)Cl4(1R, 2R-dach)], trans(Cl)-[Pt(IV)Cl2(oxalato)(1R, 2R-dach)], and trans(Cl)-[Pt(IV)Cl2(malonato)(1R, 2R-dach)].In addition, trans(OH)-[Pt(IV)(OH)2Y2(1R, 2R-dach)] (Y2 : oxalato or malonato) did not exhibit cytotoxicity towards leukemia L1210 cells, whereas trans(Cl)-[Pt(IV)Cl2Y2(1R, 2R-dach)] (Y2 : oxalato or malonato) were highly cytotoxic. The accumulation of trans(OH)-[Pt(IV)(OH)2Y2(1R, 2R-dach)] in leukemia L1210 cells was much lower than that of trans(Cl)-[Pt(IV)Cl2Y2(1R, 2R-dach)]. Platinum(IV) complexes, in which leaving groups are replaced by hydroxide groups, have decreased cytotoxic activity, because the hydroxide groups of the platinum(IV) complex reduce the uptake of platinum by the cells. trans(OH), cis(Cl)-[Pt(IV)(OH)2Cl2(1R, 2R-dach)], which has hydroxide and chloride groups, was easily incorporated into the cells and exhibited the high cytotoxic activity. This behavior indicates that the chloride group apparently overcomes the ameliorating effect of the hydroxide group.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 16 (10), 1014-1018, 1993
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204623143936
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- NII論文ID
- 110003640177
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- NII書誌ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- PubMed
- 8287030
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可