Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 28, Issue 2, Pages 283-288Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2011.643303
Keywords
Carbonic anhydrase; flavonoid; inhibitor; phenol
Funding
- Turkish Republic Prime Ministry State Planning Organization (DPT), [2010K120440]
- EU
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A series of flavonoids, such as quercetin, catechin, apigenin, luteolin, morin, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA). The compounds were tested against four alpha-CA isozymes purified from human and bovine (hCA I, hCA II, bCA III, hCA IV) tissues. The four isozymes showed quite diverse inhibition profiles with these compounds. The flavonoids inhibited hCA I with K-I-s in the range of 2.2-12.8 mu M, hCA II with K-I-s in the range of 0.74-6.2 mu M, bCA III with K-I-s in the range of 2.2-21.3 mu M, and hCA IV with inhibition constants in the range of 4.4-15.7, with an esterase assay using 4-nitrophenyl acetate as substrate. Some simple phenols/sulfonamides were also investigated as standard inhibitors. The flavonoids incorporate phenol moieties which inhibit these CAs through a diverse, not yet determined inhibition mechanism, compared to classic inhibitors such as the sulfonamide/sulfamate ones.
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