Effects of Cisplatin and its analogues on the permeability of human erythrocyte membrane.
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.
Lu
J F
JF
The National Laboratory of Natural and Biomimetic Drugs Beijing Medical University Beijing 100083 China.
Wang
K
K
Sun
X Z
XZ
Xing
F
F
An
P D
PD
Yang
Z H
ZH
Yin
J J
JJ