期刊
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
卷 32, 期 1, 页码 -出版社
WILEY
DOI: 10.1002/jbt.22010
关键词
avermectin; carbonic anhydrase; enzyme inhibition; enzyme purification; goat liver
Avermectins are used worldwide as antiparasitic drugs in the field of veterinary medicine and as agricultural pesticides and insecticides. Carbonic anhydrase (CA, E.C. 4.2.1.1) is a zinc-containing metalloenzyme that catalyzes the reversible hydration of carbon dioxide (CO2) to yield protons (H+) and bicarbonate (HCO3-). In this study, some avermectins, including abamectin, doramectin, eprinomectin, and moxidectin, were investigated for in vitro inhibitory effects on the CA enzyme purified from goat liver, which was purified (125.00-fold) using sepharose 4B-l-tyrosine-sulfanilamide affinity chromatography, with a yield of 68.27% and a specific activity of 21765.31 EU/mg proteins. The inhibition results obtained from this study showed K-i values of 0.283, 0.153, 0.232, and 0.317 nM for abamectin, doramectin, eprinomectin, and moxidectin, respectively. On the other hand, acetazolamide, well-known clinically established CA inhibitor, possessed a K-i value of 0.707 nM against goat liver CA.
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