title: The effects of some avermectins on bovine carbonic anhydrase enzyme.
abstract: Avermectins are effective agricultural pesticides and antiparasitic agents that are widely employed in the agricultural, veterinary and medical fields. The aim of this study was to investigate the inhibitory effects of selected avermectins including abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin that are used as drugs against a wide variety of internal and external mammalian parasites, on the carbonic anhydrase enzyme (CA, EC 4.2.1.1.) purified from fresh bovine erythrocyte. CA catalyses the rapid interconversion of carbon dioxide (CO2) and water (H2O) to bicarbonate ([Formula: see text]) and protons (H(+)) and regulate the acidity of the local tissues. Bovine erythrocyte CA (bCA) enzyme was purified by Sepharose-4B affinity chromatography with a yield of 21.96% and 262.7-fold purification. The inhibition results obtained from this study showed Ki values of 9.73, 17.39, 20.43, 13.39, 16.44 and 17.73 nM for abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin, respectively. However, acetazolamide, well-known clinically established CA inhibitor, possessed a Ki value of 27.68 nM.
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
authors.forename: Leyla Polat
authors.initials: LP
authors.lastname: Kose
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .|b Zoology Department , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.affiliation: a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
authors.forename: Hasan
authors.initials: H
authors.lastname: Özdemir
authors.affiliation: c Ispir Hamza Polat Vocational Training School, Ataturk University , Erzurum , Turkey , and.
authors.forename: Ali
authors.initials: A
authors.lastname: Atasever
authors.affiliation: b Zoology Department , College of Science, King Saud University , Riyadh , Saudi Arabia .
authors.forename: Saleh H
authors.initials: SH
authors.lastname: Alwasel
authors.affiliation: d Section of Pharmaceutical and Nutriceutical Sciences, Neurofarba Department, Università degli Studi di Firenze , Sesto Fiorentino (Florence) , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000086:Acetazolamide / Q000494:pharmacology; D000818:Animals; D000977:Antiparasitic Agents / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000378:metabolism*; D002417:Cattle; D004187:Disaccharides / Q000494:pharmacology; D004591:Electrophoresis, Polyacrylamide Gel; D004789:Enzyme Activation / Q000187:drug effects; D004912:Erythrocytes / Q000201:enzymology*; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000494:pharmacology; D018942:Macrolides / Q000494:pharmacology; D015394:Molecular Structure
chemical_list: D000977:Antiparasitic Agents; D004187:Disaccharides; D018942:Macrolides; C048324:abamectin; D007559:Ivermectin; C019264:avermectin; C101434:eprinomectin; C443359:emamectin; D002256:Carbonic Anhydrases; C084101:doramectin; C027837:moxidectin; D000086:Acetazolamide
keywords: Avermectin; bovine; carbonic anhydrase; enzyme inhibition; enzyme purification