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    Pd(II) and Pt(II) saccharinate complexes with two phosphine derivatives: Synthesis, anticancer and antiangiogenic activities
    (Wiley, 2024) Icsel, Ceyda; Yilmaz, Veysel T.; Aygun, Muhittin; Erkisa, Merve; Ulukaya, Engin; Akar, R. Okan
    As 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]center dot 0.5DMF (2), cis-[Pd(sac)2(PPh2Bz)2]center dot 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 mu M 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 mu M) 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. A trans-configured Pt(II) saccharinate complex bearing benzyldiphenylphosphine inhibits both growth of human colorectal carcinoma cells (HCT116) and angiogenesis, acting as a multifunctional anticancer and antiangiogenic agent. image
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    Water-soluble copper(II) 5-fluorouracil complexes bearing polypyridyl co-ligands: synthesis, structures and anticancer activity
    (Royal Soc Chemistry, 2023) Icsel, Ceyda; Yilmaz, Veysel T.; Aygun, Muhittin; Erkisa, Merve; Ulukaya, Engin
    Five newly synthesized copper(II) 5-fluorouracil (5-FU) complexes of polypyridyl co-ligands with good solubility in water, namely [CuCl(5-FU)(bpy)(DMSO)] (1), [Cu(5-FU)(phen)(2)](5-FU)center dot 4H(2)O (2), [Cu(5-FU)(dpya)(2)](NO3)center dot 2.5H(2)O (3), [Cu(5-FU)(NO3)(bpyma)]center dot H2O (4) and [CuCl(5-FU)(terpy)] (5) (bpy = 2,2 '-bipyridine, phen = 1,10-phenanthroline, dpya = 2,2 '-dipyridylamine, bpyma = bis(2-pyridylmethyl)amine and terpy = 2,2 ';6 ',2 ''-terpyridine), were characterized by elemental analysis and a number of spectrometric methods. The structures of complexes 1-5 were determined by X-ray crystallography and the copper(II) ions were five coordinate. Cytotoxic activity of the complexes in four human cancer cell lines, A549 (lung carcinoma), MDA-MB-231 (breast carcinoma), HCT116 (colon carcinoma) and DU145 (prostate carcinoma), and a normal cell line, BEAS-2B (human lung epithelial), was determined by SRB assay and compared with that of 5-FU and cisplatin. The complexation of 5-FU together with polypyridyl ligands resulted in a significant increase in the cytotoxicity of the complexes, with complex 2 exhibiting the highest anticancer potency against all the cell lines, with HCT116 being the most sensitive. The mode of action of cell death for 2 was investigated using morphological imaging and cytometric analyses, including the capacity for induction of apoptosis, generation of reactive oxygen species, mitochondrial dysfunction and DNA damage.