title: Treatment with antimalarials adversely affects the oxidative energy metabolism in rat liver mitochondria.
abstract: Effects of in vivo treatment with the three antimalarials chloroquine, primaquine and quinine on rat liver mitochondrial energy transduction functions were examined. Treatment with all the three antimalarials decreased the state 3 and state 4 respiration rates drastically. The extent of inhibition was higher with pyruvate + malate as the substrate than with glutamate. The antimalarials also acted as uncouplers. The uncoupling effect was seen on site II and site III of phosphorylation; site I was unaffected. As a consequence the ADP phosphorylation rates also decreased significantly. Following antimalarials treatment the basal and Mg2+ stimulated ATPase activities increased while the DNP-stimulated ATPase activity was reduced by half. Treatment with chloroquine resulted in decreased contents of cytochromes aa3 and b; primaquine and quinine treatments increased the contents of the two cytochromes in 14 day treatment groups.
authors.affiliation: Department of Biochemistry, Faculty of Science, M. S. University of Baroda, Vadodara 390 002, Gujarat, India.
authors.forename: Subhash D
authors.initials: SD
authors.lastname: Katewa
authors.forename: Surendra S
authors.initials: SS
authors.lastname: Katyare
mesh_terms: D000251:Adenosine Triphosphatases / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D000962:Antimalarials / Q000633:toxicity*; D002738:Chloroquine / Q000633:toxicity; D003580:Cytochromes / Q000145:classification / Q000187:drug effects / Q000378:metabolism; D004734:Energy Metabolism / Q000187:drug effects; D008297:Male; D008930:Mitochondria, Liver / Q000187:drug effects* / Q000201:enzymology; D010085:Oxidative Phosphorylation / Q000187:drug effects; D011319:Primaquine / Q000633:toxicity; D011803:Quinine / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D000962:Antimalarials; D003580:Cytochromes; D002738:Chloroquine; D011803:Quinine; D000251:Adenosine Triphosphatases; D011319:Primaquine