title: In Vitro inhibition of human carbonic anhydrase I and II isozymes with natural phenolic compounds.
abstract: Inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II with some natural phenolic derivatives was investigated using the esterase assay with 4-nitrophenyl acetate as substrate. Resveratrol, catechin, silymarin, dobutamin, and curcumin showed K(I) values in the range of 4.47-9.47 mm for hCA I and of 2.86-7.44 μm against hCA II, respectively. These natural product phenols were generally competitive inhibitors with 4-nitrophenylacetate as substrate. Some natural phenols investigated here showed effective hCA II inhibitory effects, in the same range as the clinically used sulfonamide acetazolamide, and might be used as leads for generating enzyme inhibitors possibly targeting other CA isoforms that have not been yet assayed for their interactions with such agents.
authors.forename: Murat
authors.initials: M
authors.lastname: Sentürk
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gülçin
authors.forename: Sükrü
authors.initials: S
authors.lastname: Beydemir
authors.forename: O İrfan
authors.initials: Oİ
authors.lastname: Küfrevioğlu
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors* / Q000302:isolation & purification / Q000378:metabolism; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors* / Q000302:isolation & purification / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000302:isolation & purification / Q000378:metabolism; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D001688:Biological Products; D002257:Carbonic Anhydrase Inhibitors; D007527:Isoenzymes; D010636:Phenols; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II