Human erythrocyte acetylcholinesterase inhibition by cis-diamminediaquaplatinum (II): a novel kinetic approach

Cancer Lett. 1999 Apr 26;138(1-2):115-9. doi: 10.1016/s0304-3835(98)00385-1.

Abstract

The present work addresses the analyses of some novel kinetic parameters (k(t), K(v), t50, K(ir), t(c), m(c), IC50, IC99 and Ki) of human erythrocyte membrane-bound acetylcholinesterase (AChE, EC 3.1.1.7) inhibition by cis-diamminediaquaplatinum II (PDC). PDC is under a clinical trial for use as an antineoplastic drug. The authors recently reported that PDC and cisplatin have the ability to inhibit AChE activity in vitro. Therefore this study was designed to determine the estimation of time constant (k(t)), velocity constant (K(v)), 50% inhibition time (t50), inhibition rate constant (K(ir)), transition concentration (t(c)), meeting concentration (m(c)), 50% inhibition (IC50), 99% inhibition (IC99) and inhibition constant (Ki) by novel methods. The details are described in the text.

MeSH terms

  • Antineoplastic Agents / adverse effects*
  • Cholinesterase Inhibitors / adverse effects*
  • Cisplatin / adverse effects*
  • Erythrocytes / enzymology*
  • Humans
  • Kinetics

Substances

  • Antineoplastic Agents
  • Cholinesterase Inhibitors
  • Cisplatin