Structures and anticancer activity of chlorido platinum(II) saccharinate complexes with mono- and dialkylphenylphosphines

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dc.authoridEngin Ulukaya / 0000-0003-4875-5472en_US
dc.authorscopusidEngin Ulukaya / 6602927353
dc.authorwosidEngin Ulukaya / K-5792-2018
dc.contributor.authorİçsel, Ceyda
dc.contributor.authorYılmaz, Veysel T.
dc.contributor.authorCevatemre, Buse
dc.contributor.authorAygün, Muhittin
dc.contributor.authorUlukaya, Engin
dc.date.accessioned2020-08-30T20:06:48Z
dc.date.available2020-08-30T20:06:48Z
dc.date.issued2019
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Temel Tıp Bilimleri Bölümüen_US
dc.description.abstractcis-[PtCl(sac)(PPh2Me)(2)] (1), cis-[PtCl(sac)(PPhMe2)(2)] (2), trans-[PtCl(sac)(PPh2Et)(2)] (3) and trans- [PtCl(sac) (PPhEt2)(2)] (4) complexes (sac = saccharinate) were synthesized and characterized by elemental analysis and spectroscopic methods. The structures of 2-4 were determined by X-ray single-crystal diffraction. The interaction of the complexes with DNA was studied various biochemical, biophysical and molecular docking methods. Only the cis-configured complexes (1 and 2) showed nuclease activity and their binding affinity towards DNA was considerably higher than those of their trans-congeners (3 and 4). The chlorido ligand in the cis-configured complexes underwent aquation, making them more reactive towards DNA. Furthermore, 1 and 2 exhibited anticancer potency on breast (MCF-7) and colon (HCT116) cancer cells similar to cisplatin, whereas 3 and 4 were biologicallly inactive. Mechanistic studies on MCF-7 cells showed that higher nuclear uptake, cell cycle arrest at the S phase, dramatically increased DNA double-strand breaks, apoptosis induction, elevated levels of reactive oxygen species (ROS) and high mitochondrial membrane depolarization greatly contribute to the anticancer potency of 1 and 2.en_US
dc.description.sponsorshipTUBITAKTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [215Z230]en_US
dc.description.sponsorshipThe financial support for the research project (215Z230) from TUBITAK is gratefully acknowledged. The authors thank Prof. Dr. Ismail Ozdemir (Inonu University) for collecting NMR spectroscopic data.en_US
dc.identifier.citationIcsel, C., Yilmaz, V. T., Cevatemre, B., Aygun, M., & Ulukaya, E. (2019). Structures and anticancer activity of chlorido platinum(II) saccharinate complexes with mono- and dialkylphenylphosphines. Journal of Inorganic Biochemistry, 195, 39–50. https://doi.org/10.1016/j.jinorgbio.2019.03.008en_US
dc.identifier.doi10.1016/j.jinorgbio.2019.03.008en_US
dc.identifier.endpage50en_US
dc.identifier.issn0162-0134en_US
dc.identifier.issn1873-3344en_US
dc.identifier.pmid30889415en_US
dc.identifier.scopus2-s2.0-85062936854en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage39en_US
dc.identifier.urihttps://doi.org/10.1016/j.jinorgbio.2019.03.008
dc.identifier.urihttps://hdl.handle.net/20.500.12713/623
dc.identifier.volume195en_US
dc.identifier.wosWOS:000469408500005en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorUlukaya, Enginen_US
dc.language.isoenen_US
dc.publisherElsevier Science Incen_US
dc.relation.ispartofJournal of Inorganic Biochemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectPt(Ii) Complexen_US
dc.subjectSaccharinateen_US
dc.subjectPhosphineen_US
dc.subjectDna Bindingen_US
dc.subjectCytotoxicityen_US
dc.subjectAnticancer Mechanismen_US
dc.titleStructures and anticancer activity of chlorido platinum(II) saccharinate complexes with mono- and dialkylphenylphosphinesen_US
dc.typeArticleen_US

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