Table of Contents
Metal-Based Drugs
Volume 2, Issue 2, Pages 73-80
http://dx.doi.org/10.1155/MBD.1995.73

Effects of Cisplatin and its Analogues on the Permeability of Human Erythrocyte Membrane

1The National Laboratory of Natural and Biomimetic Drugs, Beijing Medical University, Beijing 100083, China
2National Biomedical ESR Center, Medical College of Wisconsin, Milwaukee 53226, Wl, USA

Received 6 July 1994; Accepted 27 July 1994

Copyright © 1995 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The biomembrane is postulated as the initial target when Platinum(II) complexes attack cells. In this work, a spin-labeling ESR technique has been used to study the effects of cis-DCDP, cis-DBDP, cis-DIDP, trans-DCDP, and cis-DADP on the permeability of human erythrocyte membrane. We monitored the reduction processes of the ESR signal of a nitroxide spin label, (TEMPO), which leaks out through the membrane and is reduced by the external ascorbate. Our results indicate that cisplatin and its analogues can enhance the permeability of membranes to small moieties such as TEMPO and ascorbate, and the differences between these compounds are related to features of the leaving group. In addition, changes in the order parameter of 5DS spin label in membrane indicate that hydrolysis of these Pt(II) complexes result in membrane damage.