Ali Aydın

Synthesis and characterization of two novel dicyanidoargentate(I) complexes containing N-(2-hydroxyethyl)ethylenediamine exhibiting significant biological activity

Two novel cyanido-bridged bimetallic polymeric complexes, [Ni(hydeten)2Ag(CN)2] [Ag(CN)2]·H2O (C1) and [Cd2(hydeten)2Ag4(CN)8]·H2O (C2) (hydeten: N-(2-hydroxyethyl)ethylenediamine) were synthesized and characterized by elemental, FT-IR, X-ray (C2), thermal and variable temperature magnetic measurement (C1) techniques. Their anticancer, antibacterial and antifungal effects were also investigated. The crystallographic analyses showed that C2 crystallizes in the monoclinic space group P21/c and shows a 3D 6,4 ladder-type polymeric chain in which the CdII centers are linked by [Ag(CN)2]− units. The Ag⋯Ag distance exhibits a short value of 3.1365(9) A. It features a rare linear pentameric unit of [Ag(CN)2]− ions assembled via d10–d10 interaction as building blocks. Both complexes exhibited outstanding antibacterial, antifungal and anticancer activities against ten different bacterial strains, two plant pathogenic fungi (Alternaria solani and Rhizoctonia solani) and four tumor cell lines (HT-29, HeLa, C6 and Vero), respectively.

Bioassay-guided isolation, identification of compounds from Origanum rotundifolium and investigation of their antiproliferative and antioxidant activities

Abstract Context: Origanum (Lamiaceae) has been used in food and pharmaceutical industries. Objective: Isolation and identification of bioactive compounds from Origanum rotundifolium Boiss. and investigation of their antiproliferative and antioxidant activities. Materials and methods: The aerial part of O. rotundifolium was dried and powdered (1.0 kg ±2.0 g) then extracted with hexane, ethyl acetate, methanol and water. Solvent (3 × 1 L) was used for each extraction for a week at room temperature. The aqueous extract was partitioned with ethyl acetate (3 × 1 L) to yield the water/EtOAc extract subjected to chromatography to isolate the active compounds. The structures of isolated compounds were elucidated by 1 D, 2 D NMR and LC-TOF/MS. Results: Apigenin (1), ferulic acid (2), vitexin (3), caprolactam (4), rosmarinic acid (5), and globoidnan A (6) were isolated and identified. Globoidnan A (6), vitexin (3), and rosmarinic acid (5) revealed the excellent DPPH• scavenging effect with IC50 values of 22.4, 31.4, 47.2 μM, respectively. Vitexin (3) (IC50 3.6), globoidnan A (6) (IC50 4.6), apigenin (1) (IC50 8.9) and ferulic acid (2) exhibited more ABTS•+ activity than standard Trolox (IC50 13.8 μg/mL). Vitexin (3) revealed the most antiproliferative activity against HeLa, HT29, C6 and Vero cells lines with IC50 values of 35.6, 32.5, 41.6, 46.7 (μM), respectively. Discussion and conclusion: Globoidnan A (6) has the most antioxidant effects on all assays. This has to do with the chemical structure of the compound bearing the acidic protons. Vitexin (3) could be a promising anticancer agent.

Five novel dicyanidoaurate(I)-based complexes exhibiting significant biological activities: synthesis, characterization and three crystal structures

Five new cyanido-bridged coordination polymers having closed formulae [Ni(hydeten)Au2(CN)4] (C1), [Ni(hydeten)2Au2(CN)4]·H2O (C2), [Cu(hydeten)2Au2(CN)4]·CH3OH (C3), [Zn(hydeten)2 Au2(CN)4]·H2O (C4), and [Cd(hydeten)2Au2(CN)4]·H2O (C5) (hydeten: N-(2-hydroxyethyl)-ethylenediamine) have been prepared and characterized by elemental, thermal, FT-IR and XRD (C3, C4 and C5) measurement techniques. The anticancer, antibacterial and antifungal activities of the complexes are also investigated. The C3, C4 and C5 units according to XRD analyses are linked to each other via –CN–M(hydeten)–NC–Au(1)–CN–M(hydeten)–CN– chains (MII = Cu, Zn and Cd) and aurophilic interacted –Au(1)(CN)2–Au(2)(CN)2–Au(1)(CN)2–Au(2)(CN)2– zig-zag shaped chains along the a axis. C1, C2 and C4 show significant antifungal effects against several plant pathogenic fungi, while surprisingly C3 exhibits a considerable antibacterial effect against Gram negative E. coli. The studies of the antiproliferative activity on Hela, HT29 and C6 tumor cell lines indicated the anticancer potential of these complexes even at low doses.

Biological Property of Fritillaria imperialis L. Extract

A preliminary in vitro screening revealed the therapeutic status of extracts of Fritillaria imperialis L. that belongs to the Liliaceae family. Its tendrilled bulbs are consumed fresh or prepared in a powdered form and used as a home remedy for cough and phlegm, high fever, hemorrhage, lack of milk, treatment of abscesses, asthma, rheumatism, and eye disease. Herein, we investigated the antiproliferative, cytotoxic effects and antibacterial activities of Fritillaria imperialis L. extracts on three cancer cell lines (HeLa, HT29, and C6), and a non-cancer cells (Vero). The potential antiproliferative and cytotoxic impact of Fritillaria imperialis L. extracts were investigated in vitro through MTT and LDH measurement techniques, and its antimicrobial effects were studied with MIC and disc-zone test. The extracts of Fritillaria imperialis L. have been shown to exhibit poor antiproliferative effects and antibacterial activities on some cancer cell lines and bacteria, respectively, at even high concentration. These data suggest that Fritillaria imperialis L. extracts are low cytotoxic to cancer cell lines and Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922). Our results indicate that clinic consideration of Fritillaria imperialis extracts for the treatment of malignant and bacterial disease needs to be re-evaluated due to its different extraction and isolation methods.

Determination of the effective anticandidal concentration of denture cleanser tablets on some denture base resins

Abstract Objective Although the effectiveness of chemical cleansing against Candida albicans biofilm has been shown, the effective concentration of denture cleanser tablets has not been studied. The aim of this study was to assess the effect of three denture materials against Candida albicans biofilm and to determine effective concentrations of denture cleanser tablets. Material and methods The surface-roughness of Acron-hi™, QC-20™ and Deflex™ (n=45 per resin) resins was standardized by using a profilometer and their contact angle or surface free energy was calculated. C. albicans biofilm was formed on all three resins and were treated with Polident 3 min™, Corega™ and Fittydent™ cleanser solutions at various concentrations and both resin-biofilm and cleanser-biofilm interest were determined by using a MTT protocol according to the European Committee on Antimicrobial Susceptibility Testings antifungal susceptibility testing (AFST-EUCAST). Scanning electron microscopy was used to compare the efficacy of different resin materials against C. albicans biofilm. Anticandidal activity and surface free energy statistical parameters were calculated by using 3-way and 1-way ANOVA, respectively (p<0.05). Results Polident 3 min™ and Corega™ tablets significantly inhibited (p<0.05) the proliferation of C. albicans against all denture resins at 27-37 mg/mL. Scanning electron microscopy results indicated that there was no significant difference among resin specimens regarding biofilm formation on dentures. We failed to find a significant relationship between surface free energy and the anticandidal effect of resin types. However, the polarity value of the resins was statistically associated with their anticandidal activity. Conclusions The polarity of the resins, the concentrations of tablets and the chemical content of the cleanser may directly affect C. albicans biofilm formations. Polident 3 min™ and Corega™ tablets should be suggested for patients who use any denture resin types, whereas the Fittydent™ tablet should only be proposed for those who use Deflex™, when two tablets are dropped into 150 mL water.

Cellular toxicity and biological activities of honey bee (Apis mellifera L.) venom

Bee venom (BV) has been suggested as an apitherapy tool to be considered for various diseases including cancer. However, the mechanisms action of BV and its toxicity on tumorigenic and non-tumorigenic cells are poorly understood. Here, we investigated the antiproliferative, cytotoxic and antibacterial activities of honey bee ( Apis mellifera L.) venom on nontumorigenic, several tumor cell lines and multidrug resistant human pathogens (MDRP) such as Extended Spectrum Beta-Lactamases producing Escherichia coli and Vancomycin-resistant Enterococcus Enterococcus faecium. BV treatment showed significant antiproliferative, cytotoxic and antibacterial activities. Our results suggest that BV is highly toxic not only to cancer cell lines but also to nontumorigenic cell line as well. We also investigate the mechanism action of BV, which caused a cleavage of genomic DNA and inhibition of cell migration, indicating induction of apoptosis. Immunohistochemistry studies demonstrated that BV decreased the expression of Bcl-2 and P16. BV showed antimicrobial activity against several MDRP tested. Our results indicate that clinic consideration of BV for the treatment of malignancy needs to be re-evaluated due to its cytotoxicity against normal cells.

Anticancer and Cytotoxic Activities of [Cu(C6H16N2O2)2][Ni(CN)4] and [Cu(C6H16N2O2)Pd(CN)4] Cyanidometallate Compounds on HT29, HeLa, C6 and Vero Cell Lines

BACKGROUND In cancer, apoptosis relevant proteins-such as CaM kinase, Bcl-2 or P53, topoisomerase I, cell migration feature and DNA/BSA-macromolecules represent significant targets for current chemotherapeutics. OBJECTIVE We recently reported two coordination compounds-[Cu(C6H16N2O2)2][Ni(CN)4] (1) and [Cu(C6H16 N2O2)Pd(CN)4] (2)-together with their IR spectra, magnetic properties, thermal analyses and crystal structures. Herein, we describe the ability of these complexes to induce apoptosis in relevant proteins and stimulate topoisomerase I activity, cell migration velocity and DNA/BSA binding properties. METHOD The in vitro antiproliferative effects and cell toxicity of both compounds were investigated through pharmacological measurement techniques, and interactions between both compounds and CT-DNA/BSA were studied with UV-Vis spectroscopy and fluorescence spectroscopy. Results & Conclusion: Studies on cells revealed that 2 (i) demonstrated a high antiproliferative effect, which was higher toward HeLa and C6 cancer cells than toward healthy Vero cells; (ii) impaired the migration of HeLa cells; (iii) altered the P53-Bcl-2 ratio in favor of apoptosis; (iv) strongly bound to DNA/BSA macromolecules; and (v) inhibited human topoisomerase I and KpnI or BamHI restriction endonucleases. In conclusion, this preliminary information demonstrates that 2 may represent a promising antiproliferative agent and a potential candidate for a therapeutic approach against HeLa.