Zerrin Cantürk

Triply phenoxo bridged Eu(III) and Sm(III) complexes with 2,6-diformyl-4-methylphenol-di(benzoylhydrazone): structure, spectra and biological study in human cell lines

Two dinuclear lanthanide(III) complexes, [M2(HL)3] (M = Sm(III) (1), Eu(III) (2); H3L, 2,6-diformyl-4-methylphenol-di(benzoylhydrazone)) were generated with good yield and characterised systematically. The single crystal X-ray structure determination of [Eu2(HL)3] (2) confirmed the tricapped trigonal prismatic geometry of the N3O6 coordination environment around europium. Indeed, Eu(1) and Eu(2) are bridged by phenolato-O belonging to the p-cresol ring, by deprotonated ‘enol’ groups from the benzoyl hydrazide part and by the imine-N centres. A temperature dependent magnetic study suggested that anti-ferromagnetic coupling occurs between the two Eu(III) ions and the magnetic moment was found to vary from 0.48 B.M. at 5 K to 3.03 B.M. at 300 K. Electron paramagnetic resonance spectroscopy confirmed that anti-ferromagnetic coupling occurs between the atoms of Eu(III) and Sm(III). Both the complexes show emission in the visible range. The ligand, H3L and the complexes exhibit anti-mycobacterial activity against M. tuberculosis H37Rv (ATCC 27294) and M. tuberculosis H37Ra (ATCC 25177) strains. The molecular docking of H3L with the enoyl acyl carrier protein reductase of M. tuberculosis H37Rv (PDB ID: 4U0K) was examined and the best docked pose of H3L was shown to have one hydrogen bond with Thr196 (2.03 A).

Investigation of the Apoptotic Effect of Curcumin in Human Leukemia HL-60 Cells by Using Flow Cytometry

Curcumin (diferuloylmethane), the major yellow pigment isolated from the turmeric (Curcuma longa), has received much attention due to several biological properties. Curcumin exhibits a variety of pharmacological effects including antitumor, anti-inflammatory, and anti-infectious activities. In the present study, the effects of curcumin on apoptosis in the acute promyelocytic human leukemia (HL-60) cells was evaluated. Cytotoxic effects of curcumin on HL-60 cells were determined by MTT. HL-60 cells underwent apoptosis on treatment with curcumin, as indicated by increased annexin V-binding capacity and caspase-3 activation with flow cytometric analysis. Concentrations of 15, 20, and 40 μM curcumin significantly reduced cell proliferations. When HL-60 cells were treated with 10, 15, 20, and 40 μM concentration of curcumin, apoptotic rates were determined as 1.2, 81.1, 84.5, and 88.6%, respectively. On the incubations with the concentrations of curcumin, caspase-3 expressions (+) were found to be elevated by 8.5, 18.6, 91.2, and 92.4%, respectively. It was shown that curcumin had significant cytotoxic and apoptotic effects on HL-60 cells. It was suggested that curcumin may have a potential therapeutic role for human leukemia.

A Ni(II) dinuclear complex bridged by end-on azide-N and phenolate-O atoms: spectral interpretation, magnetism and biological study

A potential tetradentate monoanionic N2O2 chelator, HL, derived from the condensation of o-vanillin and N,N-dimethylethylenediammine, has been reacted with nickel perchlorate and sodium azide to yield the dinuclear Ni(II) complex [Ni(L)(μ1,1-N3)Ni(L)(OH2)2]·ClO4 (1), where L = Me2N(CH2)2NCH–C6H3(O−)(OCH3). The complex has been characterized by X-ray diffraction analysis and different spectroscopic techniques. The coordination geometry around the Ni(II) centres is a distorted octahedron, with the azide ligand and the phenolato oxygen atom bridging in μ1,1 and μ2 mode, respectively. The EPR spectra, recorded at liquid nitrogen temperature (77 K) and room temperature (298 K), show g factors of 2.080 and 2.085, in agreement with the structure determined by X-ray diffraction analysis. The VTM study confirms that there are ferromagnetic interactions between the bridging binuclear Ni(II) ions (S = 1). The evaluation of cytotoxic effects on different human cancer cell lines (A-549, MCF-7 and CaCo-2) suggests that both the ligand and complex 1 have potential anticancer properties. Furthermore, they also exhibit anti-mycobacterial activity against M. tuberculosis H37Rv (ATCC 27294) and M. tuberculosis H37Ra (ATCC 25177) strains. Molecular docking of HL with the enoyl acyl carrier protein reductase of M. tuberculosis H37Rv (PDB ID: 4U0K) has been examined, showing that HL forms two hydrogen bonds with Lys165 (1.94 and 2.53 A) in its best docked pose.

Synthesis and antimicrobial activity evaluation of new dithiocarbamate derivatives bearing thiazole/benzothiazole rings

GRAPHICAL ABSTRACT ABSTRACT The synthesis of 2-(substituted phenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A1-A24) derivatives and 2-(4-substituted thiazol-2-ylamino)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (B1-B14) derivatives was undertaken starting from the potassium salt of 4-(2-pyrimidinyl)piperazine dithiocarbamate. The structures of the obtained compounds were elucidated by 1H NMR, 13C NMR, MS spectral data, and elemental analysis. The antimicrobial activity of the thirty eight newly synthesized compounds were tested against 12 microorganism strains using the microdilution technique. Compounds 2-(4-ethoxycarbonylthiazol-2-ylamino)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (B12), 2-(3-fluorophenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A18) and 2-(3,4-difluorophenyl)-2-oxoethyl 4-(pyrimidin-2-yl)piperazin-1-carbodithiodate (A21) were determined to possess high antimicrobial activity.

Cytotoxic and genotoxic effects of [Ru(phi)3]2+ evaluated by Ames/Salmonella and MTT methods.

In this work, we synthesized and evaluated the cytotoxic effect of [Ru(phi)(3)](2+), on rat C6 glioma cell line. Cell viability was determined by assay with 3-(4-5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT). The mutagenicity of [Ru(phi)(3)](2+) was studied in vitro by using two strains of Salmonella typhimurium with frameshift mutation (TA98) and base-pair substitution mutation (TA100) were used in plate incorporation assay in the absence of metabolic activation. According to the results, the Ru compound is not toxic but mutagenic, and it shows cytotoxic effect towards C6 rat glioma cells in 100 microM.

Synthesis, Antituberculotic, and Cytotoxic Properties of New Hydrazone Derivatives Bearing Pyrimidine-Alkylsulfanyl Moiety

GRAPHICAL ABSTRACT Abstract A series of N’-(arylidene)-4-[(pyrimidine-2-yl)thio]butanohydrazide derivatives (3a-3m) has been synthesized and investigated for their antituberculotic and cytotoxic activity. The antitubercular activities of the newly synthesized compounds were tested against Mycobacterium tuberculosis H37Rv strain by MABA (Microplate Alamar Blue Assay) method and cytotoxic properties were tested against NIH/3T3 and A549 cell lines by MTT method. The title compounds have been exhibited moderate antitubercular activity. Compound 3m, titled N’-(4-nitrobenzylidene)-4-[(pyrimidine-2-yl)thio]butanohydrazide showed promising cytotoxic activity when compared with the standard drug.

Synthesis and In Vitro Evaluation of New Thiosemicarbazone Derivatives as Potential Antimicrobial Agents

In an effort to develop potent antimicrobial agents, new thiosemicarbazone derivatives were synthesized via the reaction of 4-[4-(trifluoromethyl)phenyl]thiosemicarbazide with aromatic aldehydes. The compounds were evaluated for their inhibitory effects on pathogenic bacteria and yeasts using the CLSI broth microdilution method. Microplate Alamar Blue Assay was also carried out to determine the antimycobacterial activities of the compounds against Mycobacterium tuberculosis H37Rv. Among these derivatives, compounds 5 and 11 were more effective against Enterococcus faecalis (ATCC 29212) than chloramphenicol, whereas compounds 1, 2, and 12 and chloramphenicol showed the same level of antibacterial activity against E. faecalis. Moreover, compound 2 and chloramphenicol exhibited the same level of antibacterial activity against Staphylococcus aureus. On the other hand, the most potent anticandidal derivatives were found as compounds 2 and 5. These derivatives and ketoconazole exhibited the same level of antifungal activity against Candida glabrata. According to the Microplate Alamar Blue Assay, the tested compounds showed weak to moderate antitubercular activity.

Synthesis and biological evaluation of some new amide moiety bearing quinoxaline derivatives as antimicrobial agents.

In this study, we aimed to synthesize some new quinoxaline derivatives bearing amide moiety and to evaluate their antimicrobial activity. A set of 16 novel compounds of N-[2,3-bis(4-methoxy/methylphenyl)quinoxalin-6-yl]-substituted benzamide derivatives were synthesized by reacting 2,3-bis(4-methoxyphenyl)-6-aminoquinoxaline or 2,3-bis(4-methylphenyl)-6-aminoquinoxaline with benzoyl chloride derivatives in tetrahydrofuran and investigated for their antimicrobial activity. The structures of the obtained final compounds were confirmed by spectral data (IR, (1)H-NMR, (13)C-NMR and MS). The antimicrobial activity of the compounds were determined by using the microbroth dilution method. Antimicrobial activity results revealed that synthesized compounds exhibited remarkable activity against Candida krusei (ATCC 6258) and Candida parapsilosis (ATCC 22019).

Escitalopram oxalate, a selective serotonin reuptake inhibitor, exhibits cytotoxic and apoptotic effects in glioma C6 cells

Dikmen M, Cantürk Z, Öztürk Y. Escitalopram oxalate, a selective serotonin reuptake inhibitor, exhibits cytotoxic and apoptotic effects in glioma C6 cells. Objective: Various antidepressants, mainly tricyclic antidepressants (TCAs) and selective serotonin reuptake inhibitors (SSRIs), have been reported to exhibit potent anticancer properties in different cancer cells. In this study, we evaluated the antiproliferative and apoptotic effects of escitalopram oxalate (25, 50, 100 and 200 µM) on rat C6 glioma cells. Methods: Cell proliferations were measured by [3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide] (MTT) assay, apoptosis was observed by flow cytometric analysis on C6 cells. Results: Significant decreases in the proliferation of C6 glioma cells were detected depending on increases in the escitalopram concentrations and incubation periods. When compared to controls, C6 cell proliferations after 24 h incubation were determined with 97.7, 85.9, 74.5 and 67.9% for 25, 50, 100 and 200 µM escitalopram, respectively, while the cell proliferations after 48 h were established as 96.5, 68.0, 50.7 and 39.9% for 25, 50, 100 and 200 µM concentrations, respectively. IC50 value of escitalopram was able to be calculated as 106.97 µM after 48 h. Based on Annexin V-propidium iodide (PI) binding capacity for 25, 50, 100 and 200 µM escitalopram, apoptotic effects were determined as 17.0, 22.3, 12.5 and 7.8%, respectively. Conclusion: Based on our findings, escitalopram oxalate was observed to induce cytotoxic and apoptotic activities in C6 cells.

Evaluation of antioxidant and antiproliferative metabolites of Penicillium flavigenum isolated from hypersaline environment: Tuz (Salt) Lake by Xcelligence technology

The aim of the study is the determination of antioxidant and antiproliferative activities of fungal isolates’ metabolites belonging to Penicillium flavigenum isolated from Lake Tuz, Turkey. Evaluation of the antioxidant activity, the total phenolic content and antiproliferative effect were evaluated with DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assay, Folin-ciocalteu method, Xcelligence real-time cell analysis. The total phenolic content of these isolates were found 62–82 mg/GAE. Ethyl acetate extracts from identified isolates, P. flavigenum, showed cytotoxic effects on A549, MCF7, Caco-2 cell lines. IC50 values of P. flavigenum ethyl acetate extracts were found 96.7 μg/mL for A549, 33.4 μg/mL for MCF7, 43.4 μg/mL for Caco-2 and 97.3 μg/mL for 3T3. Phenolic acids in the extracts from P. flavigenum were identified with HPLC and GC-MS. Penicillium flavigenum is a new report for Turkey. According to these findings, fungi-related secondary metabolites are very important sources in terms of antioxidant and antiproliferative effects.