Chemico-Biological Interactions 165 (2007) 127–137 Cadmium inhibits -aminolevulinate dehydratase from rat lung in vitro: Interaction with chelating and antioxidant agents Cristiane Luchese a , Gilson Zeni a , Jo˜ ao B.T. Rocha a , Cristina W. Nogueira a , Francielli W. Santos a,b, a Departamento de Qu´ ımica, Centro de Ciˆ encias Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, CEP 97105-900, RS, Brazil b Centro de Ciˆ encias da Sa ´ ude de Uruguaiana (UNIPAMPA), Universidade Federal de Santa Maria, Uruguaiana, CEP 97500-009, RS, Brazil Received 26 September 2006; received in revised form 20 November 2006; accepted 21 November 2006 Available online 24 November 2006 Abstract The effect of cadmium (Cd 2+ ) on -aminolevulinate dehydratase (-ALA-D) activity from rat lung in vitro was investigated. -ALA-D activity, a parameter for metal intoxication, has been reported as a target of Cd 2+ in different tissues. The protective effect of monotherapies with dithiol chelating (meso-2,3-dimercaptosuccinic acid (DMSA) and 2,3-dimercaptopropane-1-sulfonic acid (DMPS)) or antioxidant agents (ascorbic acid, diphenyl diselenide (PhSe) 2 , and N-acetylcysteine (NAC)) was evaluated. The effect of a combined therapy (dithiol chelating × antioxidant agent) was also studied. Zinc chloride (ZnCl 2 ) and dithiothreitol (DTT) were used to investigate the mechanisms involved in cadmium, chelating and antioxidant effects on -ALA-D activity. Cadmium inhibited rat lung -ALA-D activity at low concentrations. DTT (3 mM), but not ZnCl 2 (100 M), protected the inhibition of enzyme activity caused by Cd 2+ . Chelating agents were not effective in restoring the enzyme activity. DMPS and DMSA presented inhibitory effect on enzyme activity. DTT restored the inhibition caused by both chelating agents, but ZnCl 2 restored only the inhibitory effect induced by DMSA. These compounds caused a marked potentiation of -ALA-D inhibition induced by Cd 2+ . ZnCl 2 did not restore inhibition of enzyme activity caused by Cd 2+ plus chelating agents. Conversely, DTT restored the inhibition induced by Cd 2+ /DMSA, but not by Cd 2+ /DMPS. Antioxidants were not effective in ameliorating -ALA-D inhibition induced by Cd 2+ , whereas ascorbic acid potentiated the enzyme inhibition induced by this metal. A combined effect of Cd 2+ × DMPS × (PhSe) 2 and Cd 2+ × DMPS × NAC was observed. There was no combined effect of Cd 2+ × chelator × antioxidants when DMSA was used. This study demonstrated that Cd 2+ inhibited -ALA-D activity and chelating and antioxidant agents, alone or combined, did not restore the enzyme activity. In contrast, these compounds potentiated the inhibition induced by Cd 2+ in rat lung. © 2006 Elsevier Ireland Ltd. All rights reserved. Keywords: Cadmium; -ALA-D; Chelating agents; Antioxidant; Selenium; Lung Corresponding author at: Centro de Ciˆ encias da Sa ´ ude de Urugua- iana (UNIPAMPA), Universidade Federal de Santa Maria, 97500-009 Uruguaiana, RS, Brazil. Tel.: +55 55 3411 5174; fax: +55 55 3220 8978. E-mail address: francielliweber@yahoo.com.br (F.W. Santos). 1. Introduction The exposure of human population to a variety of heavy metals has been a public health concern [1]. Several metals are known to disturb cellular functions by binding to thiol groups of biomolecules. Cadmium (Cd 2+ ) is one of the most abundant non-essential ele- 0009-2797/$ – see front matter © 2006 Elsevier Ireland Ltd. All rights reserved. doi:10.1016/j.cbi.2006.11.007