Some phenolic natural compounds as carbonic anhydrase inhibitors: An in vitro and in silico study

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dc.authoridKUZU, Muslum/0000-0002-1375-7673
dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridAGGUL, AHMET GOKHAN/0000-0003-0377-0388
dc.authoridTaslimi, Parham/0000-0002-3171-0633
dc.authoridUZUN, NAIM/0000-0002-9763-7643
dc.contributor.authorAggul, Ahmet Gokhan
dc.contributor.authorUzun, Naim
dc.contributor.authorKuzu, Muslum
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-09-29T15:50:38Z
dc.date.available2024-09-29T15:50:38Z
dc.date.issued2022
dc.departmentKarabük Üniversitesien_US
dc.description.abstractThis paper presents experimental and molecular docking studies on the inhibitory effects of tyrosol, hydroxytyrosol, luteolin, diosmetin, caffeic acid, luteolin 7-O-glycoside, and apigenin 7-O-glycoside from olive (Olea europaea L.) leaf against human carbonic anhydrase (hCA, E.C.4.2.1.1) isozymes I and II. After these isozymes were separately purified, their activities were determined using the esterase activity. IC50 values for hCA I and II were calculated as 2.02-11.38 mu M and 2.23-9.05 mu M, respectively. The compounds were identified as CA inhibitors, with K-i values in the ranges of 1.66-9.17 mu M for the hCA I isozyme and 1.49-14.21 mu M for hCA II. The inhibitory effects of these natural compounds were also compared to acetazolamide, which is a potent inhibitor of both CA isozymes. Our results may contribute to the synthesis of new CA inhibitors and pave the way for new drug design in the treatment of a number of diseases including cancer, obesity, diabetes, and glaucoma.en_US
dc.identifier.doi10.1002/ardp.202100476
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue6en_US
dc.identifier.pmid35306678en_US
dc.identifier.scopus2-s2.0-85126563829en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202100476
dc.identifier.urihttps://hdl.handle.net/20.500.14619/3643
dc.identifier.volume355en_US
dc.identifier.wosWOS:000770784600001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectenzyme inhibitionen_US
dc.subjectmolecular dockingen_US
dc.subjectolive leafen_US
dc.subjectphenolic compounden_US
dc.titleSome phenolic natural compounds as carbonic anhydrase inhibitors: An in vitro and in silico studyen_US
dc.typeArticleen_US

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