Pd(II) and Pt(II) saccharinate complexes with two phosphine derivatives: Synthesis, anticancer and antiangiogenic activities

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dc.authorid0000-0002-3127-742Xen_US
dc.authorscopusid57126208900en_US
dc.authorwosidAAM-1001-2020en_US
dc.contributor.authorİçsel, Ceyda
dc.contributor.authorYılmaz, Veysel Turan
dc.contributor.authorAygun, Muhittin
dc.contributor.authorErkısa Genel, Merve
dc.contributor.authorUlukaya, Engin
dc.contributor.authorAkar, Remzi Okan
dc.date.accessioned2024-03-11T07:56:35Z
dc.date.available2024-03-11T07:56:35Z
dc.date.issued2024en_US
dc.departmentFakülteler, Tıp Fakültesi, Temel Tıp Bilimleri Bölümü, Tıbbi Biyokimya Ana Bilim Dalıen_US
dc.description.abstractAs clinically used anticancer Pt(II) drugs have severe side effects, there is a growing interest for new metal complexes with great potential for cancer therapy. The current work aimed to prepare and characterize new Pd(II) and Pt(II) saccharinate (sac) complexes bearing pyridyl- and benzyldiphenylphosphines (PPh2Py and PPh2Bz, respectively), cis-[Pd(sac)2(PPh2Py)2] (1), cis-[PtCl(sac)(PPh2Py)2]·0.5DMF (2), cis-[Pd(sac)2(PPh2Bz)2]·DMF (3) and trans-[PtCl(sac)(PPh2Bz)2] (4) as promising anticancer and antiangiogenic drugs. The anticancer activity of the complexes was screened against seven cancer cell lines including HCT116 (colon), HepG2 (liver), MDA-MB-231 (breast), PANC-1 (pancreatic), A549 (lung), C6 (glioma), DU145 (prostate) and normal human lung epithelial cells (BEAS-2B). 1 and 2 did not show biological activity below 20 μM at 48 h, whereas 3 and 4 displayed significant cytotoxic effect on the cancer cells. 4 was the most potent complex (IC50 = 2.2–12.1 μM) and displayed much greater cytotoxicity than cisplatin in all the cancer cell lines. 4 caused apoptosis in HCT116 cells as evidenced by annexin V positivity and caspase 3/7 activity assays. Furthermore, the inhibition of antiapoptotic Bcl-2 proteins by the complex suggested the intrinsic apoptosis. In addition, 4 greatly enhanced generation of intracellular reactive oxygen species (ROS) and consequently caused remarkable DNA double-strand breaks in HCT116 cells. Moreover, the chick chorioallantoic membrane (CAM) assay was used to evaluate antiangiogenic potential of 4. The complex effectively inhibited angiogenesis at a dose of 50 ng, suggesting it as a promising multi-targeted agent for antiangiogenic cancer treatment.en_US
dc.identifier.citationİçsel, C., Yılmaz, V. T., Aygun, M., Erkısa Genel, M., Ulukaya, E., & Akar, R. O. (2024). Pd(II) and Pt(II) saccharinate complexes with two phosphine derivatives: Synthesis, anticancer and antiangiogenic activities. Applied Organometallic Chemistry, 38(5), pp. 1-13. https://doi.org/10.1002/aoc.7433en_US
dc.identifier.endpage13en_US
dc.identifier.issn1099-0739
dc.identifier.issn0268-2605
dc.identifier.issue5en_US
dc.identifier.scopus2-s2.0-85186854479en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1en_US
dc.identifier.urihttps://doi.org/10.1002/aoc.7433
dc.identifier.urihttps://hdl.handle.net/20.500.13055/668
dc.identifier.volume38en_US
dc.identifier.wosWOS:001178627600001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynak.otherSCI-E - Science Citation Index Expandeden_US
dc.institutionauthorErkısa Genel, Merve
dc.language.isoenen_US
dc.publisherWiley Online Libraryen_US
dc.relation.ispartofApplied Organometallic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAntiangiogenicsen_US
dc.subjectAnticancer Activityen_US
dc.subjectCell Apoptosisen_US
dc.subjectPalladium(II) and Platinum(II) Complexesen_US
dc.subjectX-Ray Structuresen_US
dc.titlePd(II) and Pt(II) saccharinate complexes with two phosphine derivatives: Synthesis, anticancer and antiangiogenic activitiesen_US
dc.typeArticleen_US
dspace.entity.typePublication

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