Platinum(II)-thiosemicarbazone drugs override the cell resistance due to glutathione; assessment of their activity against human adenocarcinoma cells

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dc.contributor.authorPoyraz, Mehmet
dc.contributor.authorDemirayak, Şeref
dc.contributor.authorBanti, Christina N.
dc.contributor.authorManos, Manolis J.
dc.contributor.authorKourkoumelis, Nikolaos
dc.contributor.authorHadjikakou, Sotiris K.
dc.date.accessioned10.07.201910:49:13
dc.date.accessioned2019-07-10T19:57:47Z
dc.date.available10.07.201910:49:13
dc.date.available2019-07-10T19:57:47Z
dc.date.issued2016
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasotik Kimya Anabilim Dalı
dc.descriptionWOS: 000387785800010
dc.description.abstractNew platinum(II) compounds of the thiosemicarbazone 1-(1H-Benzimidazol-2-yl)ethan-1-one thiosemicarbazone (BzimetTSCH), [Pt(BzimetTSCH)Cl]center dot 2H(2)O (1) and [Pt(BzimetTSCH)(tpp)]Cl center dot H2O center dot MeCN (2) were synthesized. The complexes were characterized by FT-IR spectroscopy and H-1 NMR spectroscopy. The crystal structures of 1 and 2 were determined with single-crystal X-ray diffraction analysis. The coordination around platinum is square planar in both complexes. Compounds 1 and 2 were evaluated for their in vitro cytotoxic activity against human adenocarcinoma breast (MCF-7) and cervix (HeLa) cells. The apoptotic pathway of cell death was confirmed by cell cycle arrest test. Since deactivation of cisplatin caused by glutathione (GSH) seems to be an important determinant of its cytotoxic effects, the reactions of 1 and 2 with GSH were investigated by UV-absorption spectroscopy. The genotoxicities on normal human fetal lung fibroblast cells (MRC-5) caused by 1 and 2 were evaluated by fluorescence microscopy. The absence of micronucleus in MRC-5 cells confirms the in vitro non toxic behavior of the compounds. Moreover, the in vivo genotoxicities of 1 and 2 were evaluated by the Allium cepa test. Due to negligible genototoxic effect and high antitumor activity which is similar to that of cisplatin, 2 could be a candidate for further study as potential drug since the mitotic index is unchanged. [GRAPHICS] .
dc.description.sponsorshipJosef and Esther Gani Foundation [81455]; State Scholarships Foundation of Greece (IKY) IKY-Siemens [22957]en_US
dc.description.sponsorshipCNB and SKH would like to thank (i) the Unit of bioactivity testing of xenobiotics, the University of Ioannina, for providing access to the facilities, (ii) the Atherothrombosis Research Centre of the University of Ioannina for providing access to the flow cytometer, (iii) the Josef and Esther Gani Foundation for the financial support (project number 81455), and (iv) the State Scholarships Foundation of Greece (IKY) for the post doctoral research fellowship of excellence program IKY-Siemens (project number 22957).en_US
dc.identifier.citationPoyraz, M., Demirayak, Ş., Banti, C. N., Manos, M. J., Kourkoumelis, N. ve Hadjikakou, S. K. (2016). Platinum(II)-thiosemicarbazone drugs override the cell resistance due to glutathione; assessment of their activity against human adenocarcinoma cells. Journal Of Coordination Chemistry, 69(23), 3560-3579. https://dx.doi.org/10.1080/00958972.2016.1241394
dc.identifier.doi10.1080/00958972.2016.1241394
dc.identifier.endpage3579
dc.identifier.issn0095-8972
dc.identifier.issn1029-0389
dc.identifier.issue23
dc.identifier.scopusqualityQ2
dc.identifier.startpage3560
dc.identifier.urihttps://dx.doi.org/10.1080/00958972.2016.1241394
dc.identifier.urihttps://hdl.handle.net/20.500.12511/3048
dc.identifier.volume69
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofJournal Of Coordination Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectBiological Inorganic Chemistry
dc.subjectDrugs Design and Development
dc.subjectPlatinum(II) Metallodrugs
dc.subjectCytotoxicity
dc.subjectGlutathione
dc.subjectGenotoxicity
dc.titlePlatinum(II)-thiosemicarbazone drugs override the cell resistance due to glutathione; assessment of their activity against human adenocarcinoma cells
dc.typeArticle

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