title: Acetylcholinesterase and carbonic anhydrase isoenzymes I and II inhibition profiles of taxifolin.
abstract: Taxifolin, also known as dihydroquercetin, is a flavonoid commonly found in plants. Carbonic anhydrase (CA, EC 4.2.1.1) plays an important role in many critical physiological events including carbon dioxide (CO2)/bicarbonate (HCO3(-)) respiration and pH regulation. There are 16 known CA isoforms in humans, of which human hCA isoenzymes I and II (hCA I and II) are ubiquitous cytosolic isoforms. In this study, the inhibition properties of taxifolin against the slow cytosolic isoenzyme hCA I, and the ubiquitous and dominant rapid cytosolic isoenzyme hCA II were studied. Taxifolin, as a naturally bioactive flavonoid, has a K(i) of 29.2 nM against hCA I, and 24.2 nM against hCA II. For acetylcholinesterase enzyme (AChE) inhibition, K(i) parameter of taxifolin was determined to be 16.7 nM. These results clearly show that taxifolin inhibited both CA isoenzymes and AChE at the nM levels.
authors.affiliation: a Central Researching Laboratory, Agri Ibrahim Cecen University , Agri , Turkey .
authors.forename: Hulya
authors.initials: H
authors.lastname: Gocer
authors.affiliation: b Department of Medical Services and Techniques, Vocational School of Health Services, Gumushane University , Gumushane , Turkey .
authors.forename: Fevzi
authors.initials: F
authors.lastname: Topal
authors.affiliation: b Department of Medical Services and Techniques, Vocational School of Health Services, Gumushane University , Gumushane , Turkey .
authors.forename: Meryem
authors.initials: M
authors.lastname: Topal
authors.affiliation: c Department of Chemistry, Faculty of Sciences, Atatürk University , Erzurum , Turkey .
authors.forename: Murat
authors.initials: M
authors.lastname: Küçük
authors.affiliation: c Department of Chemistry, Faculty of Sciences, Atatürk University , Erzurum , Turkey .
authors.forename: Dilek
authors.initials: D
authors.lastname: Teke
authors.affiliation: c Department of Chemistry, Faculty of Sciences, Atatürk University , Erzurum , Turkey .|d Zoology Department, College of Science, Fetal Programming of Diseases Research Chair, King Saud University , Riyadh , Saudi Arabia .
authors.forename: İlhami
authors.initials: İ
authors.lastname: Gülçin
authors.affiliation: d Zoology Department, College of Science, Fetal Programming of Diseases Research Chair, King Saud University , Riyadh , Saudi Arabia .
authors.forename: Saleh H
authors.initials: SH
authors.lastname: Alwasel
authors.affiliation: e Dipartimento di Chimica Ugo Schiff, Universita degli Studi di Firenze , Sesto Fiorentino , Firenze , Italy , and.|f Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Universita degli Studi di Firenze , Sesto Fiorentino , Florence , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000110:Acetylcholinesterase / Q000302:isolation & purification / Q000378:metabolism*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000302:isolation & purification / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000302:isolation & purification / Q000378:metabolism; D015394:Molecular Structure; D011794:Quercetin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D002800:Cholinesterase Inhibitors; D007527:Isoenzymes; D011794:Quercetin; C003377:taxifolin; D000110:Acetylcholinesterase; D002256:Carbonic Anhydrases
keywords: Acetylcholinesterase; carbonic anhydrase; enzyme inhibition; enzyme purification; taxifolin