Relationship between cellular uptake rate and chemical behavior of diammine/diaminocyclohexane platinum (II) complexes with oxygen-ligating anionic groups.
The uptake kinetics of the platinum (II) complexes of the formula Pt(NH3)2X, Pt(dach)X by human erythrocyte in the plasma isotonic buffer was studied. The results showed that across-membrane transport of all the platinum complexes studied follows a first-order kinetic process. The uptake rate constants decrease with the change of oxygen-ligating anionic group in the sequence: sulfato > selenato > anion of squaric acid > oxalato > anion of demethylcantharic acid > malonato and increase with increasing lipophilicity of carrier group. The relationship between uptake rate and reactivity of these complexes was established. The stereochemistry of dach isomers was shown without effect on the reactivity and the sequence.
Inorganic Chemistry Department, School of Pharmaceutical Sciences, Beijing Medical University, People's Republic of China.
J
J
Zou
X D
XD
Yang
F
F
An
K
K
Wang
D000199:Actins / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism; D003514:Cyclohexylamines / Q000737:chemistry; D004912:Erythrocytes / Q000187:drug effects* / Q000378:metabolism; D005453:Fluorescence; D006801:Humans; D007700:Kinetics; D008301:Maleimides / Q000737:chemistry; D008715:Methionine / Q000737:chemistry / Q000378:metabolism; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000493:pharmacokinetics*; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds
D000199:Actins; D003514:Cyclohexylamines; D008301:Maleimides; D009944:Organoplatinum Compounds; D013438:Sulfhydryl Compounds; C003944:N-(3-pyrene)maleimide; D008715:Methionine; C030435:1,2-cyclohexanediamine