Toxicology 133 (1999) 139 – 145 Inhibition of human erythrocyte Ca 2 + -ATPase by Zn 2 + Christer Hogstrand a, *, Pieter M. Verbost b , Sjoerd E. Wendelaar Bonga b a T.H. Morgan School of Biological Sciences, 101 Morgan Building, Uniersity of Kentucky, Lexington, KY 40506 -0225, USA b Department of Animal Physiology, Uniersity of Nijmegen, Toernooield 1, 6525 ED Nijmegen, The Netherlands Received 23 September 1998; accepted 4 February 1999 Abstract Recent investigations suggest that Ca 2 + -ATPase from fish gills is very sensitive to Zn 2 + (Hogstrand et al., 1996. Am. J. Physiol. 270, R1141–R1147). The effect of free Zn 2 + ion on the human erythrocyte plasma membrane Ca 2 + -ATPase was investigated to explore the possible extension of this finding to humans. Membrane vesicles were prepared and the Ca 2 + -ATPase activity was measured as Ca 2 + -stimulated ATP hydrolysis and as ATP-dependent Ca 2 + transport. The Zn 2 + ion inhibited the erythrocyte Ca 2 + -ATPase by reducing V max and increasing the K 0.5 . While in the Ca 2 + transport assay only the V max was affected at lower Zn 2 + concentrations (50 – 100 pM), reduction of V max was always accompanied by an affinity decrease in the ATP hydrolysis assay. The Ca 2 + -ATPase was found to be inhibited by Zn 2 + at extremely low concentrations. The IC 10 and IC 50 for Zn 2 + , at a Ca 2 + concentration of 1.0 M, were estimated at 4 and 80 pM, respectively. Although the Ca 2 + -ATPase might be more sensitive in vitro than in vivo conditions, the results suggest that physiological concentrations of Zn 2 + may reduce the activity of the erythrocyte Ca 2 + -ATPase. Furthermore, disturbance of Ca homeostasis may be a mechanism causing Zn toxicity during exposure. © 1999 Elsevier Science Ireland Ltd. All rights reserved. Keywords: Zinc; Calcium; Transport; Red blood cells; Inhibition; Membrane 1. Introduction In a recent study, ATP-dependent Ca 2 + trans- port in plasma membranes of rainbow trout gills was found to be sensitive to Zn 2 + (Hogstrand et al., 1996). Concentrations down to 100 pM of free Zn 2 + significantly reduced the activity of the ba- solateral high-affinity Ca 2 + -ATPase by mixed in- hibition and there was possible, but non- significant, inhibition even at 50 pM of Zn 2+ . It was earlier shown that interference with transep- ithelial Ca 2 + transport is a likely mechanism of Zn toxicity to fish (Spry and Wood, 1985; Hogstrand et al., 1994). Thus, this effect can now be explained at the enzymatic level. From some * Corresponding author. E-mail address: hogstra@pop.uky.edu (C. Hogstrand) 0300-483X/99/$ - see front matter © 1999 Elsevier Science Ireland Ltd. All rights reserved. PII:S0300-483X(99)00020-7