Toxicology 132 (1999) 19 – 32 Pb 2 + promotes lipid oxidation and alterations in membrane physical properties V.N. Adonaylo, P.I. Oteiza * Instituto de Quı ´mica y Fisicoquı ´mica Biolo ´gicas (UBA-CONICET), Uniersidad de Buenos Aires, Facultad de Farmacia y Bioquı ´mica, Junı ´n 956, 1113 Buenos Aires, Argentina Received 22 June 1998; accepted 4 October 1998 Abstract Experimental evidence suggests that cellular damage mediated by oxidants could be involved in the pathology associated with lead (Pb) toxicity. We investigated the effect of Pb 2 + on lipid oxidation in liposomes using different initiators. In the presence of Fe 2 + , Pb 2 + (12.5 – 200 M) stimulated lipid oxidation in phosphatidyl- choline:phosphatidylserine-containing liposomes, measured as 2-thiobarbituric acid-reactive substances (TBARS) and conjugated dienes. This stimulatory effect depended on the presence of membrane negative charges and on bilayer integrity. Pb 2 + did not stimulate TBARS formation in the presence of 25 mM 2,2-azo-bis (2,4 dimethylvaleronitrile (AMVN) and 2,2azobis (2-amidinopropane) (AAPH). Pb 2 + significantly stimulated TBARS production and NADH oxidation in the presence of photoactivated rose Bengal. The use of specific inhibitors indicated that several reactive oxygen species were involved in the pro-oxidant action of Pb 2 + . Pb 2 + (12.5 – 200 M) caused membrane lateral phase separation and this effect was positively correlated with its capacity to stimulate Fe 2 + and rose Bengal-initiated TBARS production. Pb 2 + could bind to the membrane and act to stimulate lipid oxidation by causing changes in membrane physical properties. Through this mechanism Pb 2 + would favor the propagation of lipid oxidation. By causing lateral phase separation and/or by increasing lipid oxidation rates, Pb 2 + could be cytotoxic by altering membrane-related processes. © 1999 Elsevier Science Ireland Ltd. All rights reserved. Keywords: Lead; Lipid oxidation; Iron; Free radicals; Phase separation Abbreiations: AMVN, 2,2-azo-bis (2,4 dimethylvaleronitrile); AAPH, 2,2azobis (2-amidinopropane); PC, phosphatidylcholine; PS, phosphatidylserine; TBARS, 2-thiobarbituric acid-reactive substances; C6-NBD-PC, 2-(6-(7nitrobenz-2-oxa-1,3-diazol-4-yl) amino) dodecanoyl-1-hexadecanoyl-sn -glycero-3-phosphocholine. * Corresponding author. Fax: +54-1-9625457; e-mail: oteiza@qb.ffyb.uba.ar. 0300-483X/99/$ - see front matter © 1999 Elsevier Science Ireland Ltd. All rights reserved. PII:S0300-483X(98)00134-6