title: Capsaicin: a potent inhibitor of carbonic anhydrase isoenzymes.
abstract: Carbonic anhydrase (CA, EC 4.2.1.1) is a zinc containing metalloenzyme that catalyzes the rapid and reversible conversion of carbon dioxide (CO2) and water (H2O) into a proton (H+) and bicarbonate (HCO3-) ion. On the other hand, capsaicin is the main component in hot chili peppers and is used extensively used in spices, food additives and drugs; it is responsible for their spicy flavor and pungent taste. There are sixteen known CA isoforms in humans. Human CA isoenzymes I, and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. In this study, the inhibition properties of capsaicin against the slow cytosolic isoform hCA I, and the ubiquitous and dominant rapid cytosolic isozymes hCA II were studied. Both CA isozymes were inhibited by capsaicin in the micromolar range. This naturally bioactive compound has a Ki of 696.15 µM against hCA I, and of 208.37 µM against hCA II.
authors.affiliation: Atatürk University, Faculty of Sciences, Department of Chemistry, Erzurum 25240, Turkey. btlozer@hotmail.com.tr.
authors.forename: Betul
authors.initials: B
authors.lastname: Arabaci
authors.affiliation: Atatürk University, Faculty of Sciences, Department of Chemistry, Erzurum 25240, Turkey. igulcin@atauni.edu.tr.
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gulcin
authors.affiliation: Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia. salwasel@ksu.edu.sa.
authors.forename: Saleh
authors.initials: S
authors.lastname: Alwasel
mesh_terms: D002211:Capsaicin / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000737:chemistry / Q000378:metabolism; D002384:Catalysis; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes; D007700:Kinetics; D011485:Protein Binding
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D002256:Carbonic Anhydrases; D002211:Capsaicin