In vitro biological activity of cobalt(II) complexes with salicylaldimine ligands in microbial and cancer cells.

Background: More studies using cobalt complexes as drugs are needed. Results: The drug action of two cobalt salicylaldimines was determined. The complexes and amphotericin B (20 mg/ml) inhibited Candida albicans at 9-15 and 21 mm. This concentration of both ligands inhibited Staphylococcus aureus at 10 mm and one ligand inhibited Escherichia coli at 9 mm, but the complexes and ampicillin inhibited four bacteria at 9-20 and 21-26 mm. The ligands were inactive against cancer and normal cells, but the complexes and doxorubicin provided IC50 values of 28.18-54.19 and 9.66 µM against MCF-7 cells and 15.76-20.49 and 36.42 µM against BHK cells. Conclusion: The ligands' activity was much improved by complexation, although they remained substandard.

Synthesis, Solid State Structure, and Cytotoxic Activity of a Complex Dimer of Yttrium with Anthranilic Acid against Cancer Cells.

This paper presents the synthesis and isolation of a new binuclear complex of yttrium with anthranilic acid (HA). The complex [Y2(HA)6(H2O)4] Cl6.2C2H5OH (C1) was obtained as single crystals that its X-ray analysis revealed its triclinic P-1 space group in addition to anti-prismatic geometry around each of the yttrium ions. In the complex, the anthranilic acid ligands are bidentate, zwitter ionic and neutral, and the yttrium ions' charge is only compensated by six chloride ions. The cytotoxicity of this complex against human breast cancer MDA-MB-231 cells, prostate cancer PC-3 cells, and bladder cancer T-24 cells was evaluated. This yttrium complex displayed more cytotoxic activity against the bladder cancer cells with an IC50 value of 307.7 µg/ml (223 µM). On the other hand, the activities of complex C1 against the MDA-MB-231 and PC-3 cells were less significant respectively with IC50 values of 1097 µg/ml (796 µM) and 921 µg/ml (669 µM).

New iron(III) complexes with 2-formylpyridine thiosemicarbazones: Synthetic aspects, structural and spectral analyses and cytotoxicity screening against MCF-7 human cancer cells.

2-Formylpyridine thiosemicarbazone - iron (III) chelates [ F e L 2 ] C l • 2 H 2 O {L = L1 (C1) [HL 1  = 4-(4-Nitrophenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide] and L = L2 (C2) [HL 2  = 4-(2,5-Dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide]} were prepared. The two ligand anions in each complex resulted in saturation of the iron coordination number and consequently the existence of these complexes as 1:1 electrolytes. As well, the iron in these complexes exhibits low-spin electronic configuration. X-ray crystallography of complex C1 indicated its triclinic crystal system and P 1 ‾ space group. In addition, it proved the ligation through a thiol sulfur atom and two nitrogen atoms of pyridine and azomethine groups. This is while the presence of two water molecules of crystallization in the complex structure was also indicated. The ligand HL 1 was selected for cytotoxicity screening against human MCF-7, A-549, HEPG-2 and HCT-116 cancer cells and the most enhanced activities were detected against the breast cells. Against these cells, the compounds HL 1 , HL 2 , C1 and C2 induced cytotoxicity, respectively, with IC50 values of 52.4, 145.4, 34.3 and 62.0 µM. However, against the healthy BHK cells, HL 1 and HL 2 caused cytotoxicity, respectively, with IC50 values of 54.8 and 110.6 µM and cytotoxicity with percent viabilities of 56.7 and 55.4% of the BHK cells by the complexes (137.4 µM of C1 and 131.9 µM of C2) was determined. These activities against MCF-7 cells are less significant compared with the measured value for doxorubicin. But this standard is more toxic to normal cells than the thiosemicarbazones (IC50 (doxorubicin) = 9.66 µM against MCF-7 cells and 36.42 µM against BHK cells).

Synthesis, X-ray structure and anticancer activity evaluation of a binuclear La(III) complex with anthranilic acid.

A binuclear La(III) complex {[La2(HA)4(H2O)4(C2H5OH)2Cl2]Cl4 (C1)} with 2-aminobenzoic acid (HA) was prepared from the ligand and heptahydrated lanthanum chloride. The complex was characterised by X-ray crystallography that revealed anti-prismatic geometry around both of the lanthanum. In the complex, the four 2-aminobenzoic acid ligands are zwitter ionic and the two lanthanum(III) ions net charge is only counterbalanced by chloride ions. The complex cytotoxicity was determined against human breast (MDA-MB-231), prostate (PC-3) and bladder (T-24) cancer cells. This complex afforded cytotoxicity towards the T-24 bladder cancer cells with an IC50 value of 383.5 µg/mL (319 µM). In contrary, activities by the lanthanum complex with IC50 values of 1124 µg/mL (934 µM) and 739 µg/mL (614 µM) were, respectively, shown against the MDA-MB-231 and PC-3 cancer cells. This means the complex is more cytotoxic against the T-24 cells, despite that its activity is less compared with activities shown by classical drugs.

Zn(II) and Cd(II) thiosemicarbazones for stimulation/inhibition of kojic acid biosynthesis from Aspergillus flavus and the fungal defense behavior against the metal complexes' excesses.

The complexes {[ZnL1Cl] C1, [ZnL2Cl].0.5H2O C2, [CdL1Cl] C3, and [CdL2Cl] C4} were prepared from tridentate thiosemicarbazones {HL1 = 4-(3-nitrophenyl)-1-((pyridin-2-yl)methylene) thiosemicarbazide and HL2 = 4-(2,4-dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide} and identified by elemental CHNS, spectroscopic {IR and UV-Vis.}, thermal and DMF solution electrical conductivity data. On another hand, kojic acid (KA) which represents important secondary metabolite with numerous hot spot applications was successfully biosynthesized from Aspergillus flavus and structurally analyzed by single crystal analysis. The Zn(II) complexes C1&C2 (0.3 mM) enhanced the KA biosynthesis by 70.87% and 42.26%, while 76.09% of C1 and 72.78% of C2 were absorbed by the fungal cells. The Cd(II) complexes C3&C4 at 0.3 mM inhibited KA production by 87.95% and 97.03% with Cd(II) consumption reaching to 40.09% & 37.3%, while 0.4 mM of C3&C4 resulted in 100% inhibition of kojic acid biosynthesis. Light microscopic analysis showed the fungal structural abnormalities and the cell antioxidant behavior was detected. These complexes could be highly applicable as new stimulators and inhibitors of kojic acid production.