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dc.creatorBondžić, Aleksandra M.
dc.creatorČolović, Mirjana B.
dc.creatorJanjić, Goran
dc.creatorZarić, Božidarka
dc.creatorPetrović, Sandra
dc.creatorKrstic, Danijela Z.
dc.creatorMarzo, Tiziano
dc.creatorMessori, Luigi
dc.creatorVasić, Vesna M.
dc.date.accessioned2019-01-30T17:54:22Z
dc.date.available2019-01-30T17:54:22Z
dc.date.issued2017
dc.identifier.issn0949-8257
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2143
dc.description.abstractThe in vitro effects of oxo-bridged binuclear gold(III) complexes, i.e., [(bipy2Me)(2)Au-2(mu-O)(2)][PF6](2) (Auoxo6), Au-2[(bipydmb-H)(2)(mu-O)][PF6] (Au(2)bipyC) and [Au-2(phen(2Me))(2)(mu-O)(2)](PF6)(2) (Au(2)phen) on Na/K-ATPase, purified from the porcine cerebral cortex, were investigated. All three studied gold complexes inhibited the enzyme activity in a concentration-dependent manner achieving IC50 values in the low micromolar range. Kinetic analysis suggested an uncompetitive mode of inhibition for Auoxo6 and Au(2)bipyC, and a mixed type one for Au(2)phen. Docking studies indicated that the inhibitory actions of all tested complexes are related to E2-P enzyme conformation binding to ion channel and intracellular part between N and P sub-domain. In addition, Au(2)phen was able to inhibit the enzyme by interacting with its extracellular part as well. Toxic effects of the gold(III) complexes were evaluated in vitro by following lactate dehydrogenase activity in rat brain synaptosomes and incidence of micronuclei and cytokinesis-block proliferation index in cultivated human lymphocytes. All investigated complexes turned out to induce cytogenetic damage consisting of a significant decrease in cell proliferation and an increase in micronuclei in a dose-dependent manner. On the other hand, lactate dehydrogenase activity, an indicator of membrane integrity/viability, was not affected by Auoxo6 and Au(2)bipyC, while Au(2)phen slightly modified its activity.en
dc.publisherSpringer, New York
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172023/RS//
dc.relationBeneficentia Stiftung (Vaduz)
dc.relationITT (Istituto Toscano Tumori)
dc.relationFondazione Cassa Risparmio Firenze (CRF)
dc.relationAIRC - IG-16049
dc.relationAIRC-FIRC (Fondazione Italiana per la Ricerca sul Cancro) - 18044
dc.rightsrestrictedAccess
dc.sourceJournal of Biological Inorganic Chemistry
dc.subjectBinuclear gold(III) complexesen
dc.subjectNa/K-ATPaseen
dc.subjectInhibitionen
dc.subjectDocking studiesen
dc.subjectCytotoxicityen
dc.subjectGenotoxicityen
dc.titleThe influence of oxo-bridged binuclear gold(III) complexes on Na/K-ATPase activity: a joint experimental and theoretical approachen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractЈањић, Горан; Крстиц, Данијела З.; Зариц, Бозидарка; Васиц, Весна М.; Петровиц, Сандра; Цоловиц, Мирјана Б.; Бондзиц, Aлександра М.; Мессори, Луиги; Марзо, Тизиано;
dc.citation.volume22
dc.citation.issue6
dc.citation.spage819
dc.citation.epage832
dc.citation.other22(6): 819-832
dc.citation.rankM22
dc.identifier.pmid28432453
dc.identifier.doi10.1007/s00775-017-1460-5
dc.identifier.rcubConv_3755
dc.identifier.scopus2-s2.0-85018825607
dc.identifier.wos000406036700003
dc.type.versionpublishedVersion


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