作者: L. Pendyala , Y. Kidani , R. Perez , J. Wilkes , R.J. Bernacki
DOI: 10.1016/0304-3835(95)03974-2
关键词: DNA 、 Cytotoxicity 、 Cell culture 、 Biology 、 Adduct 、 Molecular biology 、 Oxaliplatin 、 Biochemistry 、 Metabolism 、 Biological activity 、 In vitro
摘要: Abstract Oxaliplatin (trans-l-1,2-diaminocyclohexane oxalato Pt(II); 1R,2R-dach, l-OHP), its trans-d isomer (1S,2S-dach) and cis-dach (1R,2S-dach) isomers were compared in vitro testing against human ovarian carcinoma cell lines A2780, A2780/CP (cisplatin resistant), A2780/l-OHP (oxaliplatin colon line HT-29, murine leukemia L1210, L1210/CP L1210/dach (tetraplatin resistant). The relative molar potency of the three complexes all except are trans-l > cis-dach; they = cis-dach. selected for resistance is 3.6-fold resistant to oxaliplatin, showed no 6-fold However, which carboxyphthalato 1,2-dach (trans-dl) platinum(II) 140-fold 73-fold trans-d, 41-fold cis-OHP. accumulation DNA binding platinum following a 2-h treatment A2780 cells with each (60 μM) order corresponded cytotoxicity trans-l, but not others. data suggest that other processes, such as differential formation specific adducts and/or repair may be involved. Of l-OHP superior consistent cytotoxicity.