DSpace Arşivi :: by Yazar "Acik, Leyla" değerine göre listeleniyor

Yazar "Acik, Leyla" seçeneğine göre listele

Listeleniyor 1 - 20 / 28

Antimicrobial, antioxidant, cytotoxic and apoptotic activities of Satureja khuzestanica
(Gazi Univ, Fac Med, 2018) Soltanzadeh, Hossein; Acik, Leyla; Turk, Mustafa; Houshmand, Massoud; Shahsavari, Gholamreza
Objective: Natural products with antimicrobial effect are currently investigated in order to eliminate the use of synthetic antibiotics that cause the resistance of microorganisms. This study determines the antibacterial, antioxidant activity, and also the cytotoxic and apoptotic effect of Satureja khuzestanica on various cancer cell lines. Materials and methods: The individual constituents were identified by their identical retention indices referring to known compounds from the literature. Methanol and ethanol extracts of S. khuzestanica (25 and 50 mg/(mL)) were screened against four Gram-positive and four Gram-negative bacteria. The plant extracts were tested for their antioxidant activity against 2,2-diphenyl1- picrylhydrazyl (DPPH) radical. The interaction between the extracts and plasmid DNA were analyzed by agarose gel electrophoresis. In addition, the cytotoxic activity of the extracts was evaluated on MCF-7, DLD-1, osteosarcoma, and fibroblast cell line. Finally, gene expression of caspase-3, Bax and Bcl-2 were investigated by real-time PCR. Results: Our result indicated that both extracts showed good inhibitory activity against both Gram-negative (Escherichia coli ATCC 35218) and positive (Bacillus subtilis ATCC 6633) bacteria. In addition, the methanol extract of S. khuzestanica had strong antioxidant activity (IC50= 37.0 +/- 0.3 mu g/mL). The extracts showed a strong effect on plasmid DNA. The methanol extract of S. khuzestanica showed a good concentration-dependent cytotoxicity. Finally, IC50= 47.00a +/- 1.21 mu g/mL, ethanol, and water extract had apoptotic effect in MCF-7 cell line. Discussion: MCF-7 was detected as the most sensitive cell line therefore further studies should be done on this plant extract as a potential anticancer agent against breast cancer.
Characterisation of coagulase positive Staphylococcus species isolated from bovine mastitis using protein and plasmid patterns
(Scientific Technical Research Council Turkey-Tubitak, 2009) Arslan, Emine; Celebi, Ayten; Acik, Leyla; Ucan, Uckun Sait
The objective of this work was to study the protein patterns, plasmid profiles, and antibiotic susceptibility of Staphylococcus intermedius and Staphylococcus aureus isolates originating from mastitic mammary glands of dairy cattle in different parts of Konya province. A total of 114 Staphylococcus species were isolated and identified by conventional bacteriological methods from bovine mastitis. Of the total isolates 77 were identified as S. aureus and 37 as S. intermedius. Intra- and inter-species diversities in the coagulase-positive staphylococci were investigated by analysis of whole-cell protein profiles using sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE). Plasmid profiling also demonstrated that 75 S. aureus isolates and 36 S. intermedius isolates contained plasmid. In addition, 88.3% of S. aureus and 59.4% of S. intermedius isolates were resistant to penicillin. Sixty-six of the 77 S. aureus isolates were also resistant to amoxicillin+clavulanic acid (85.7%). The corresponding number for S. intermedius was 17 (45.9%). Only 1 S. aureus isolate was resistant to danofloxacin. One of each of the Staphylococcus isolates was resistant to methicillin. Results from the study showed that the susceptibility of S. intermedius isolates to antibiotics used widely in mastitis therapy is a matter of concern.
Cytotoxicity and DNA interactions of some platinum(II) complexes with substituted benzimidazole ligands
(Informa Healthcare, 2012) Ozcelik, Azime Berna; Utku, Semra; Gumus, Fatma; Keskin, Ayten Celebi; Acik, Leyla; Yilmaz, Sukran; Ozgungor, Adeviye
In the present study, four Pt(II) complexes with 2-ethyl (1)/or benzyl (2)/or p-chlorobenzyl (3)/or 2-phenoxymethyl (4) benzimidazole carrier ligands were evaluated for their in vitro cytotoxic activities against the human HeLa cervix, oestrogen receptor-positive MCF-7 breast, and oestrogen receptor-negative MDA-MB 231 breast cancer cell lines. The plasmid DNA interactions and inhibition of the BamHI restriction enzyme activities of the complexes were also studied. Complex 3 was found to be more active than carboplatin for all examined cell lines and comparable with cisplatin, except for the HeLa cell line.
Dispiro-4-bromobenzylaminophosphazenes: Synthesis reactions, spectroscopic and chromatographic properties, crystal structures, biological, and cytotoxic activities
(Amer Chemical Soc, 2019) Kuzey, Nur Guven; Ozgur, Mehtap; Asmafiliz, Nuran; Acik, Leyla; Aydin, Betul; Hokelek, Tuncer; Cerci, Aytuna
…
Dispiro-4-bromobenzylaminophosphazenes: Synthesize reactions, spectroscopic properties, crystal structures, biological and cytotoxic activities
(Amer Chemical Soc, 2019) Kuzey, Nur Guven; Ozgur, Mehtap; Asmafiliz, Nuran; Acik, Leyla; Aydin, Betul; Hokelek, Tuncer; Cerci, Nebahat Aytuna
…
Genetic Differentiation of Lactobacillus delbrueckii subsp bulgaricus and Streptococcus thermophilus Strains Isolated from Raw Milk Samples Collected from Different Regions of Turkey
(Taylor & Francis Inc, 2015) Yilmaz, Remziye; Temiz, Ayhan; Acik, Leyla; Keskin, Ayten Celebi
Yogurt is a fermented milk product produced by two homofermentative lactic acid bacteria, Lactobacillus delbrueckii subsp. bulgaricus and Streptococcus thermophilus. It is consumed throughout the world as a healthy, nutritional food. In this study, the strains of Lactobacillus and Streptococcus were isolated from raw milk samples collected from different local geographical regions of Turkey. One hundred and thirty isolates were characterized to genus level by classical morphological, physiological and biochemical tests. Twenty six of all isolates were identified as L. delbrueckii subsp. bulgaricus and 47 isolates were identified as S. thermophilus using API 50 CHL system. RAPD-PCR was used to explain molecular characterization and genetic differentiation of a total of 73 strains. The whole cell protein profiles of these strains were tested by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). In this study, all strains were identified by the RAPD-PCR technique to species or strain level. SDS-PAGE was also shown to be an effective method for molecular differentiation all of the strains. Phenotypic identification, RAPD-PCR and SDS-PAGE proved to be informative methods suitable to explain molecular characterization and genetic differentiation of L. delbrueckii subsp. bulgaricus and S. thermophilus strains isolated from raw milk. In the present study, we described an identification system by using RAPD-PCR and SDS-PAGE techniques and used this system for genetic differentiation of L. delbrueckii subsp. bulgaricus and S. thermophilus strains isolated from raw milk. It is believed that these two molecular techniques allow researchers to fill the significant gaps present in our understanding of these organisms by providing a comprehensive view potentially involved in industrially relevant phenotypes from different geographical origin.
Investigation of potential virulence genes and antibiotic resistance characteristics of Enterococcus faecalis isolates from human milk and colostrum samples
(Tubitak Scientific & Technical Research Council Turkey, 2014) Togay, Sine Ozmen; Temiz, Ayhan; Celebi, Ayten; Acik, Leyla; Yalcin, Siddika Songul
Enterococci may improve the typical taste and flavor of fermented foods through their proteolytic and lipolytic activities. However, some enterococcal strains are recognized as nosocomial pathogens, which have virulence genes and resistance to certain antibiotics. Enteroccocci are also found in human milk microflora. The aim of this study was to investigate the potential virulence genes and antibiotic resistance characteristics of Enterococcus faecalis isolates from human milk and colostrum samples. In total, 23 Enterococcus faecalis strains were identified from human milk and colostrum samples. Antibiotic-resistant E. faecalis isolates were determined using the disk diffusion method. Vancomycin resistance genes (vanA, vanB) and some virulence genes (agg(2), gelE, efaAfm, ccf, cpd, cad, cylM, cylB, etc.) were investigated using polymerase chain reaction (PCR). All strains were sensitive to ampicillin, penicillin G, chloramphenicol, and vancomycin. None of the E. faecalis isolates contained vanA, vanB, or efaAfm genes. The results of this study indicated that there were no harmful enterococci strains in human milk and colostrum samples in terms of tested virulence factors and antibiotic resistance. Therefore, the E. faecalis isolates from human milk may have the potential to be considered as a functional culture for the food industry.
Novel fluorescent coumarin-thiophene-derived Schiff bases: Synthesis, effects of substituents, photophysical properties, DFT calculations, and biological activities
(Elsevier Science Sa, 2019) Yahaya, Issah; Chemchem, Meryem; Aydiner, Burcu; Seferoglu, Nurgul; Tepe, Fulya Erva; Acik, Leyla; Seferoglu, Zeynel
Novel fluorescent coumarin-thiophene appended Schiff bases have been synthesized in good yields (76-89%). The effects of substitution on the fluorescent intensity and solubility of the molecules were examined with experimental techniques. The deprotonation properties of the prepared Schiff bases were examined, in DMSO, by titration of each of the ligands with TBAOH. We also studied the reverse protonation of the fluorophores using TFA. The structural and electronic properties of the neutral and the deprotonated forms of the fluorophores were also examined in the framework of DFT calculations. Also, the cytotoxicity of each of the compounds was tested against L929 fibroblasts and human lung cancer (small cell). Furthermore, the antimicrobial activity of each of the compounds was studied against both Gram-negative and Gram-positive bacterial and fungal species. In the final studies, the plasmid DNA interactions with the compounds were investigated with agarose gel electrophoresis. The thermal properties of all the prepared compounds were determined by thermal gravimetric analysis (TGA) and were found to be thermostable up to at least 335 degrees C.
Phosphorus nitrogen compounds: Part 34. Syntheses, structural investigations, cytotoxic and biological activities of spiro-ansa-spiro and spiro-bino-spiro tetrameric phosphazene derivatives
(Elsevier Science Sa, 2016) Berberoglu, Ipek; Asmafiliz, Nuran; Kilic, Zeynel; Hokelek, Tuncer; Koc, L. Yasemin; Acik, Leyla; Dal, Hakan
The reactions of N4P4Cl8 with the symmetric N2N2 (1-3) and N2O2 (4) bulky ligands gave partly substituted 2,4-sas (5 and 6), 2,6-sas (7-10) and sbs (11-14) tetrameric phosphazene derivatives. The 2,4-sas-5, 2,6-sas-8 and sbs-12 reacted with pyrrolidine to give fully-substituted tetra-(15 and 16) and dode-capyrrolidinocyclotetraphosphazenes (17-19). The structures of all the phosphazenes were verified by FTIR, MS, H-1, C-13{H-1} and P-31{H-1} NMR, and HSQC spectral data. The crystal structures of 7, 9 and 10 were examined by single crystal X-ray diffraction techniques. The compounds 1-3, 5, 8, 9, 12, 13, 16 and 18 were screened for antimicrobial activity against G(+) and G(-) bacteria and fungi. The compound 16 is found to possess excellent activity (MIC values of 39 and 78 mu M) against fungal pathogen Candida krusei and Candida albicans. Meanwhile, interactions between pBR322 plasmid DNA and 1-3, 5, 8, 9, 12, 13, 14, 16 and 18 were investigated by agarose gel electrophoresis. The compounds 5, 8, 9, 12, 13, 16 and 18 were appraised for their cytotoxic activity against L929 Fibroblast and MDA-MB-231 breast cancer cell lines. Compounds 13 and 16 are as effective as cis-platin. (C) 2016 Elsevier B.V. All rights reserved.
Phosphorus-nitrogen compounds part 33: in vitro cytotoxic and antimicrobial activities, DNA interactions, syntheses, and structural investigations of new mono(4-nitrobenzyl)spirocyclotriphosphazenes
(Springer, 2016) Okumus, Aytug; Akbas, Huseyin; Kilic, Zeynel; Koc, L. Yasemin; Acik, Leyla; Aydin, Betul; Dal, Hakan
The condensation reactions of hexachlorocyclotriphosphazene, N3P3Cl6, with N-alkyl-N'-mono(4-nitrobenzyl)diamines (1-3), NO2PhCH2NH(CH2) (n) NHR1 (R-1 = CH3 or C2H5), led to the formation of the mono(4-nitrobenzyl)spirocyclotriphosphazenes (4-6). The tetra-pyrrolidino (4a-6a), piperidino (4b-6b), and 1,4-dioxa-8-azaspiro[4,5]decaphosphazenes (4c-6c) were prepared from(for) the reactions of partly substituted compounds (4, 5, and 6) with excess pyrrolidine, piperidine, and 1,4-dioxa-8-azaspiro[4,5]decane (DASD), respectively. The partly substituted geminal (4d and 5d) and cis-morpholino (6d) phosphazenes were isolated from the reactions of excess morpholine in boiling THF and o-xylene, but the expected fully substituted compounds were not obtained. The structures of all the phosphazene derivatives were determined by elemental analyses, MS, FTIR, H-1, C-13{H-1}, P-31{H-1} NMR, HSQC, and HMBC techniques. The crystal structures of 4, 6, 4a, and 5a were verified by X-ray diffraction analysis. In addition, in vitro cytotoxic activities of fully substituted phosphazenes (4a-6c) against HeLa cervical cancer cell lines (ATCC CCL-2) and the compounds 4a and 4c against breast cancer cell lines (MDA-MB-231) and L929 fibroblast cells were evaluated, respectively. Apoptosis effect was determined by MDA-MB-231 cancer cell lines and fibroblast cells. The MIC values of the compounds were in the ranges of 9.8-19.5 A mu M. The compounds 6, 5a, 6a, 5b, and 6d have greater MIC activity against bacterial and yeast strain. The investigation of DNA binding with the phosphazenes was studied using plasmid DNA. The phosphazene derivatives inhibit the restriction endonuclease cleavage of plasmid DNA by BamHI and HindIII enzymes. BamHI and HindIII digestion results demonstrate that the compounds bind with G/G and A/A nucleotides.
Phosphorus-nitrogen compounds. Part 36. Syntheses, Langmuir-Blodgett thin films and biological activities of spiro-bino-spiro trimeric phosphazenes
(Royal Soc Chemistry, 2016) Asmafiliz, Nuran; Kilic, Zeynel; Civan, Mehmet; Avci, Orhan; Gonder, L. Yasemin; Acik, Leyla; Hokelek, Tuncer
The condensation reactions of hexachlorocyclotriphosphazene (N3P3Cl6, trimer) with the symmetric N2N2 or N2O2 donor type tetradentate bulky ligands (1-4) gave partly substituted spiro-bino-spiro (sbs) (5-8) trimeric phosphazenes. Compounds 5-8 reacted with pyrrolidine, morpholine and 1,4-dioxa-8-azaspiro[4,5]decane (DASD) to give octapyrrolidino-(9-12), morpholino-(13-16) and DASD-substituted cyclotriphosphazenes (17-20). The structures of the phosphazenes have been elucidated using FTIR, MS, H-1, C-13{H-1} and P-31{H-1} NMR, and HSQC spectral data. The molecular and solid-state structures of 5, 6 and 12 were verified by single crystal X-ray diffraction techniques. On the other hand, the ultrathin and highly ordered Langmuir-Blodgett (LB) films of compounds 6, 7, 9 and 12 were also fabricated. The structural characterization of the LB films was made using p-polarized grazing angle (GAIR) and horizontal attenuated total reflectance (HATR) techniques. All the novel phosphazene derivatives were evaluated for antibacterial activities against Gram-positive (G+) and Gram-negative (G-) bacteria and for antifungal activities against yeast strains. In addition, the cytotoxic effects of compounds 9, 13, 15, 16, 19 and 20 were investigated against L929 fibroblast and MDA-MB-231 breast cancer cells. The most active one among these compounds was compound 9 at 6.25 mu g mL(-1) concentration. The interactions between compounds 5-20 and pBR322 plasmid DNA were determined by agarose gel electrophoresis.
Phosphorus-nitrogen compounds. Part 37. Syntheses and structural characterizations, biological activities of mono and bis(4-fluorobenzyl)spirocyclotetraphosphazenes
(Royal Soc Chemistry, 2017) Elmas, Gamze; Okumus, Aytug; Sevinc, Pelin; Kilic, Zeynel; Acik, Leyla; Atalan, Mustafa; Hokelek, Tuncer
The Cl substitution reactions of octachlorocyclotetraphosphazene, N4P4Cl8, with one equimolar amount of (4-fluorobenzyl)diamines (1-3) affords mono(4-fluorobenzyl) spirocyclotetraphosphazenes (4-6) as minor products. However, the reactions of N4P4Cl8 with two equimolar amounts of (4-fluorobenzyl) diamines (1-3) leads to the formation of mono (4-6), 2-trans-6-bis (7-9, as major products) and 2-cis-6-bis (4-fluorobenzyl) spirocyclotetraphosphazenes (10-12). The 2-cis-6-bis compounds (10 and 12) were separated and purified using column chromatography as minor products, whereas compound 11 could not be isolated. The mono-spiro (4-6) and 2-trans-6-bis-spiro (7-9) cyclotetraphosphazenes were reacted with excess pyrrolidine in THF to afford the fully substituted hexapyrrolidino (4a-6a) and tetra-pyrrolidino (7a-9a) products in high yield. Compound 9 was also reacted with piperidine, morpholine and 1,4-dioxa-8-azaspiro[4,5]decane (DASD) to obtain the tetraamino products (9b, 9c and 9d), respectively, due to its very high yield. The elemental analyses, mass spectra (ESI-MS), Fourier transform infrared (FTIR) spectra, and H-1, C-13{H-1}, and P-31{H-1} NMR data of the cyclotetraphosphazenes were in agreement with the suggested structures. The molecular structures of 7, 9 and 12 were established by X-ray crystallography. The antibacterial activities of the compounds against G(+) and G(-) bacteria and their antifungal activities against yeast strains were scrutinized. The results indicated that 4a and 5a were the most active compounds, especially to yeast strains. In addition, it was found that the most active compound toward DNA was 8. The cytotoxic activities of the cyclotetraphosphazenes against L929 fibroblast and MCF-7 breast cancer cell lines were elucidated. Compound 8a exhibited the most toxic effects against both types of cells.
Phosphorus-nitrogen compounds. part 38. Syntheses, characterizations, cytotoxic, antituberculosis and antimicrobial activities and DNA interactions of spirocyclotetraphosphazenes with bis-ferrocenyl pendant arms
(Elsevier Science Sa, 2017) Elmas, Gamze; Okumus, Aytug; Cemaloglu, Resit; Kilic, Zeynel; Celik, Suheyla Pinar; Acik, Leyla; Hokelek, Tuncer
The reactions of N4P4Cl8 (1), with two equimolar amounts of N-(1-ferrocenylmethyl)-N-methyl-propylenediamine gave the monoferrocenyl-spiro (as a byproduct), bisferrocenyl-2-trans-6-dispiro (2) and bisferrocenyl-2-cis-6-dispiro (3) cyclotetraphosphazenes. The 2-trans-6-dispiro (2) was reacted with excess monoamines to produce the tetraamino products (2a-2d). The one equimolar amount of the diamines and dialkoxides with 2 afforded the mono-diamino (2e and 2f) and mono-dialkoxy (2g and 2h) cyclotetraphosphazenes. Whereas, excess diamines and dialkoxides with 2 produced the bis-diamino (2i and 2j) and bis-dialkoxy (2k and 2l) bisferrocenyl-2-trans-6-dispirocyclotetraphosphazenes. The structures of the compounds were verified by elemental analyses, ESI-MS, FTIR, HSQC, HMBC, H-1, C-13, and P-31 NMR techniques. The molecular structures of 2 and 2b were established by X-ray crystallography. Compounds 2e and 2f have two stereogenic P-atoms. Additionally, the structures of 2i-2l containing tetraspiro rings in the skeletons look similar a propeller. The Fc groups of the cyclotetraphosphazenes were found to be redox active with two-reversible electron oxidations. The antimicrobial activity of the compounds was examined against some bacteria and yeast strains. The interactions of the compounds with DNA revealed that the compounds caused conformational changes even strand break on super-coiled DNA helix. Furthermore, the compounds (except 2, 2a and 2d) inhibited DNA restriction indicating compounds binding to A/A and G/G nucleotides of the DNA. The evaluations of the cytotoxic activity against L929 fibroblast and DLD-1 colon cancer cell lines were carried out. Some of the compounds were evaluated for antituberculosis activity against reference strain Mycobacterium tuberculosis H37Rv, and 2i and 2l displayed antituberculosis activity against H37Rv. (C) 2017 Elsevier B.V. All rights reserved.
Phosphorus-nitrogen compounds. Part 42. The comparative syntheses of 2-cis-4-ansa(N/O) and spiro(N/O) cyclotetraphosphazene derivatives: spectroscopic and crystallographic characterization, antituberculosis and cytotoxic activity studies
(Royal Soc Chemistry, 2019) Binici, Arzu; Okumus, Aytug; Elmas, Gamze; Kilic, Zeynel; Ramazanoglu, Nagehan; Acik, Leyla; Hokelek, Tuncer
The reaction of N4P4Cl8 (1) with one equimolar amount of the sodium salt of an N/O donor-type bidentate ligand (2) afforded two kinds of derivatives, namely, mono-ferrocenyl-2-cis-4-dichloro-ansa- (2,4-ansa; 3) and mono-ferrocenyl-spiro- (spiro; 4) hexachlorocyclotetraphosphazenes. The reaction yield (35%) of 4 was significantly larger than that of 3 (14%). The 2,4-ansa compound (3) was reacted with excess secondary amines to produce 2-cis-4-dichloro-ansa-cyclotetraphosphazenes (3a-3d). On the other hand, the spiro compound (4) gave fully substituted mono-ferrocenyl-spiro-cyclotetraphosphazenes (4a-4d) with excess monoamines as well. The tetrameric phosphazene derivatives were characterized by ESI-MS and/or HRMS, FTIR, HSQC, HMBC, H-1, C-13, and P-31 NMR spectroscopy and X-ray crystallography (for 4). It is observed that the 2,4-ansa and spiro-cyclotetraphosphazenes have different thermal stabilities. Additionally, the CVs of the new mono-ferrocenyl pendant-armed cyclotetraphosphazenes revealed electrochemically reversible one-electron oxidation of the Fe-redox centre. The 2,4-ansa phosphazenes (3 and 3a-3d) have two different stereogenic P centers indicating that they are expected to be in racemic mixtures (RR'/SS'). The chiralities of 3a and 3c were investigated by chiral HPLC. The manuscript also deals with the antimicrobial activities against G(+)/G(-) bacteria and fungi, the interactions with plasmid DNA, the in vitro cytotoxic activities against L929 fibroblast and MCF7 breast cells, and the antituberculosis activities against Mycobacterium tuberculosis H37Rv of the cyclotetraphosphazenes.
Phosphorus-nitrogen compounds. Part 44. The syntheses of N,N-spiro bridged cyclotriphosphazene derivatives with (4-fluorobenzyl) pendant arms: Structural and stereogenic properties, DNA interactions, antimicrobial and cytotoxic activities
(Elsevier Science Sa, 2019) Ozturk, Ezel; Okumus, Aytug; Kilic, Zeynel; Kilic, Adem; Kayalak, Hande; Acik, Leyla; Hokelek, Tuncer
Isopropylaminopentachlorocyclotriphosphazene, (N3P3Cl5(NHCHMe2) (1), containing a P-NH group in the alkyl-chain, gives the NN-spirobridged octachlorobiscyclotriphosphazene, [N3P3Cl4(NCHMe2)](2) (2), in the presence of NaH. The reactions of 2 with excess pyrrolidine result in the formation of the fully substituted bridged product 2a. The reactions of 2 with 1:1 and 1:2 equimolar amounts of N-(4-fluorobenzyl)N'methylethane-1,2-diamine and N-(4-fluorobenzyl)-N'methylpropane-1,3-diamine produce the (4-fluorobenzyl) pendant armed monospiro (2b and 2c) and dispiro (2f and 2g) products. These compounds react with excess pyrrolidine to form stable, fully substituted cyclotriphosphazenes (2d, 2e, 2h and 2i). The structures of 2a and 2f are determined by X-ray crystallography. The stereogenic properties of 2a and 2f having four potential stereogenic P-centers are investigated by crystallography. The monospiro (2b-2e) and dispiro (2f-2i) products have one and two equivalent chiral centers, respectively. The dispiro derivatives may have two meso (trans-trans and cis-cis) and two racemate (trans-cis and cis-trans) mixtures. However, the structure of 2f is found to be as trans-trans (meso) isomer. Besides, in vitro antimicrobial and cytotoxic activities of 2d and 2h are evaluated. The compounds exhibit significant growth inhibitory effects on E. coli and B. cereus bacteria. Compound 2d has high anticancer and apoptotic activities.
Phosphorus-nitrogen compounds. Part 48. syntheses of the phosphazenium salts containing 2-pyridyl pendant arm: structural characterizations, thermal analysis, antimicrobial and cytotoxic activity studies
(NATL INST SCIENCE COMMUNICATION-NISCAIR, 2020) Elmas, Gamze; Okumus, Aytug; Kilic, Zeynel; Ozbeden, Pelin; Acik, Leyla; Tunali, Beste Cagdas; Turk, Mustafa
The phosphazenium salts (protic ionic liquids, PILs/protic molten salts, PMOSs) (6a-6d and 7a) of the free phosphazene bases (4a-4d and 5a) have been prepared by the reactions of the corresponding cyclotriphosphazenes with the bulky gentisic acid. The structures of the PMOS have been evaluated using the elemental analyses, FTIR, H-1, C-13{H-1} and P-31{H-1} NmR data. The molecular and crystal structures of 4a and 6c are established by X-ray crystallography. The thermal properties of the PMOS are determined using TG and DTA techniques. On the other hand, the antimicrobial activities of the free phosphazene bases (4a-4d and 5a-5d) and PMOSs (6a-6d and 7a) are screened against the selected bacteria and yeast strains. The antimicrobial activities of the free phosphazene bases and the PMOSs are compared. The interactions of the phosphazenes and their salts with plasmid DNA are elucidated by the agarose gel electrophoresis. The evaluations of the cytotoxic activities of these compounds are also studied against to L929 fibroblast and breast cancer cells (MDA-MB-231).
Phosphorus-nitrogen compounds: Part 46. The reactions of N3P3Cl6 with bidentate and monodentate ligands: The syntheses, structural characterizations, antimicrobial and cytotoxic activities, and DNA interactions of (N/N)spirocyclotriphosphazenes with 4-chlorobenzyl pendant arm
(Elsevier Science Sa, 2019) Asmafiliz, Nuran; Berberoglu, Ipek; Ozgur, Mehtap; Kilic, Zeynel; Kayalak, Hande; Acik, Leyla; Hokelek, Tuncer
In the present study, the partly and fully-substituted monospiro (4-6, 4a-6d), cis-dispiro (7-9), trans-dispiro (10-15) cyclotriphosphazenes were synthesized for the investigations of their chemical, stereogenic and biological properties. The cis/trans phosphazenes (7-12) have two stereogenic P centers. They are expected to be in meso and racemic forms. In addition, the structures of four compounds were evaluated using X-ray crystal-lographic data. Compound 13 was found to be a single enantiomer (RR) in the solid state, as also proved with its CD spectrum. The antibacterial and antifungal activities of the phosphazenes were elucidated for against Gram-positive (G+) and Gram-negative (G-) bacteria, and yeast strains, respectively. Of the compounds, 14 exhibits strong antimicrobial activity against most of the tested organisms, especially B. cereus and E. hirae. MBC and MFC values of compounds on different bacterial and fungal species ranged from < 9.8 mu M to 2500 mu M. Furthermore, the cytotoxic activities of 6, 4c, 10 and 14 were investigated against L929 fibroblast and DLD-1 cells, and 14 was the most cytotoxic compound against DLD-1.
Phosphorus-nitrogen compounds: part 53-synthesis, characterization, cytotoxic and antimicrobial activity, DNA interaction and molecular docking studies of new mono- and dispirocyclotriphosphazenes with pendant arm(s)
(Springer, 2022) Iscan, Ozlem; Cemaloglu, Resit; Asmafiliz, Nuran; Zeyrek, Celal Tugrul; Kilic, Zeynel; Acik, Leyla; Aydin, Betul
Mono-/dispirocyclotriphosphazenes with pendant arm(s) are robust, but they are less investigated inorganic ring systems. In this study, a series of mono (3 and 4)- and dispirocyclotriphosphazenes with 4-chloro-benzyl pendant arm(s) (13-16) was obtained from the Cl exchange reactions of hexachlorocyclotriphosphazene with sodium (N-benzyl)aminopropanoxides (1 and 2). When compound (3) reacted with excess pyrrolidine, morpholine, tetra-1,4-dioxa-8-azaspiro[4,5]decane (DASD) and piperidine, the fully substituted monospirocyclotriphosphazenes (7, 9, 10 and 12) occurred. But, the reactions of 4 with excess piperidine and morpholine produced the gem-piperidino (5)- and morpholino (6)-substituted monospirocyclotriphosphazenes, whereas the reactions of 4 with excess pyrrolidine and DASD gave the fully substituted monospirocyclotriphosphazenes (8) and (11). However, it should be indicated that these derivatives were obtained to be used for the investigation of their spectral, stereogenic and biological properties. The structures of 5, 7 and 14 were determined crystallographically. X-ray data of 5 and 14 displayed that both of compounds were chiral in solid state, and their absolute configurations were assigned as R and RR. Additionally, the antimicrobial activities of phosphazenes were investigated. Minimum inhibitory concentrations, minimal bacterial concentrations and minimum fungicidal concentrations of phosphazenes were determined. The interactions of phosphazenes with plasmid DNA were evaluated by agarose gel electrophoresis. The cytotoxic activities of compounds were studied against L929 fibroblast and DLD-1 colon cancer cells. In addition, density functional theory calculations of 5, 7 and 14 were reported, and their molecular docking studies with DNA, E. coli DNA gyrase and topoisomerase IV were presented.
Phosphorus-nitrogen compounds: part 57-Syntheses of tetrachloro- and tetraaminobenzylspiro(N/N) cyclotriphosphazenes: chemical, structural characterizations, bioactivity and molecular docking studies
(Springer, 2022) Berberoglu, Ipek; Cemaloglu, Resit; Asmafiliz, Nuran; Kilic, Zeynel; Zeyrek, Celal Tugrul; Acik, Leyla; Koyunoglu, Dila
Despite a significant amount of research in the field of cyclotriphosphazene chemistry, bioactivity and molecular docking studies of this class of cyclotriphosphazenes have still not been adequately studied. In this study, for bioactivity studies, tetrachlorobenzylmonospiro(N/N)cyclotriphosphazenes (4, 5 and 6) were synthesized by the reactions of hexachlorocyclotriphosphazene (N3P3Cl6; trimer; HCCP) with diamines (1, 2 and 3), respectively. Reactions of 4, 5 and 6 with excess pyrrolidine, piperidine, morpholine and 1, 4-dioxa-8-azaspiro[4.5]decane (DASD) gave the tetrapyrrolidino (7, 8 and 9), tetrapiperidino (10, 11 and 12), tetramorpholino (13, 14 and 15) and tetraDASD (16, 17 and 18) substituted benzylmonospiro(N/N) cyclotriphosphazenes. Microanalytical, spectral and crystallographic data (for 6 and 15) revealed the structures of the cyclotriphosphazenes. Antibacterial and antifungal activities of all phosphazenes against selected strains of bacteria and yeast, and pBR322 plasmid DNA cleavage activities were discussed. MIC values of 11 and 12 (78.1 and 156.3 mu M, respectively) against C. albicans are higher than the reference antibiotic Ketoconazole. Cytotoxic activities of five phosphazenes against L929 Fibroblast and DLD-1 cells were evaluated. Additionally, Density Functional Theory (DFT) calculations of 6 and 15 were performed. Molecular docking studies of 6 and 15 with DNA, endonuclease BamHI, S. aureus Dihydrofolate Reductase and E. coli DNA gyrase were presented. [GRAPHICS] .
Phosphorus-nitrogen compounds: part 68. Synthesis, characterization, stereogenism, photophysical and bioactivity studies of novel unsymmetrical dispiro(N/N)cyclotriphosphazenes with carbazolyl and 4-chlorobenzyl pendant arms
(Royal Soc Chemistry, 2023) Cemaloglu, Resit; Asmafiliz, Nuran; Kilic, Zeynel; Cosut, Bunyemin; Sabah, Busra Nur; Acik, Leyla; Cerci, Nebahat Aytuna
Organic-inorganic hybrid multi-heterocyclic unsymmetrical cis/trans dispirocyclotriphosphazenes with different pendant arms were obtained and their spectral, stereogenic, photophysical and bioactivity properties were investigated. To prepare these phosphazenes, the starting compounds tetrachloro(4-chlorobenzyl)spiro(N/N)cyclotriphosphazenes, (ClBzSpiro-5)R-1(N3P3)Cl-4 [Bz: Benzyl; R-1: Me (1) and R-1: Et (2)], were prepared regioselectively from the reactions of hexachlorocyclotriphosphazene, N3P3Cl6 (HCCP, trimer) with N-methyl/ethyl-N'-(4-chlorobenzyl)-1,2-diaminoethanes. Reactions of tetrachlorocyclotriphosphazenes (1 and 2) and 9-ethyl-N-methyl-3-carbazolyl-1,2-diaminoethane (3) or 9-ethyl-N-methyl-3-carbazolyl-1,3-diaminopropane (4) produce new cis/trans-dispirocyclotriphosphazenes, [(ClBzSpiro-5)R-1(N3P3)(CzSpiro-n)R-2]Cl-2 (Cz: Carbazolyl; R-1, R-2: Me or Et; n = 5 or 6; (5a-8a and 5b-8b), containing unsymmetrical spiro-architectures. In addition, the structures of trans-7a and cis-7b isomers were clarified by single crystal X-ray crystallography. The chiralities of trans-7a and cis-7b were confirmed using X-ray crystal structures, P-31 NMR spectra recorded upon the addition of chiral solvating agent [(S)-(+)-2,2,2-trifluoro-1-(9 & PRIME;-anthryl)ethanol; CSA], and circular dichroism (CD) spectra. Moreover, the photophysical properties of phosphazenes showed a fluorescence profile with lifetimes of about 4.9-6.6 ns and quantum yields in the range of 0.10-0.14. Additionally, the antibacterial and antifungal activities of the newly synthesized phosphazenes against some bacteria and yeast strains and their interactions with pBR322 plasmid DNA were investigated. The bacterial strain most susceptible (MIC = 156.3 mu M) to compounds 5a and 8a was P. aeruginosa. However, it was found that the yeast strain most susceptible (MIC = 156.3 mu M) to compounds 5b, 7a, 7b and 8b was C.albicans. The cytotoxic activities of 5a, 5b, 7b and 8a against L929 fibroblast and MCF-7 breast cancer cells were determined. However, cis-5b showed reasonable antioxidant activity with a radical scavenging value of 35.20%.

Yazar "Acik, Leyla" seçeneğine göre listele

Sayfa Başına Sonuç

Sıralama seçenekleri