Citation: Juan ZOU, Xiao Cai YANG, Gang LIU, Rong Chang LI, Kui WANG. THE CHIRAL SELECTIVITY IN ACROSS-MEMBRANE TRANSPORT OF 1,2-DIAMINOCYCLOHEXANE PLATINUM (II) COMPLEXES AND THE CONTRIBUTION OF LEAVING GROUPS[J]. Chinese Chemical Letters, ;1996, 7(7): 657-660. shu

THE CHIRAL SELECTIVITY IN ACROSS-MEMBRANE TRANSPORT OF 1,2-DIAMINOCYCLOHEXANE PLATINUM (II) COMPLEXES AND THE CONTRIBUTION OF LEAVING GROUPS

a State Key Laboratory of Coordination Chemistry, Coordination Chemistry Institute, Nanjing University, Nanjing 210093;
b Inorganic Chemistry DePartment, School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083

Received Date: 26 July 1995

Fund Project: The project is supported by the State Commission of Science and Technology and National Natural Sciences Foundation of China.

The uptake kinetics of platinum (Ⅱ) complexes of 1, 2-diaminocyclohexane (dach) isomers (1R, 2R-dach, 1R, 2S-dach, 1S, 2S-dach) with various leaving groups, chloride (Cl), oxalate (OX), squaric acid (SA), and demethylcantharic acid (DA) was studied in the plasma isotonic buffer. The experimental results show that across-membrane transport of all the platinum complexes studied follows a firstorder kinetic process and a passive diffusion mechanism. The uptake rate constants of these platinum (Ⅱ) complexes decrease in the following sequence with the k value (h^-1) :Cl >SA >OX >DA. It is noteworthy that the k values of the platinum (Ⅱ) complexes with same leaving group reduce as:1R, 2R-dach >1R, 2S-dach >1S, 2S-dach. Based on these results, it is firstly suggested that the erythrocyte membrane recognizes the chirality of these platinum complexes.
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