Toxicological Evaluation of Benzothiazole Derivatives Carrying Piperazine Ring

Charehsaz, Mohammad | Gürdal, Enise Ece | Helvacıoğlu, Sinem | Yarım, Mine

Article | 2017 | Marmara Pharmaceutical Journal21 ( 2 ) , pp.243 - 250

Benzothiazole-piperazine derivatives prepared previously, 1hand 1j are potential anticancer agents. Since the mutagenicand genotoxic properties of anticancer drugs compose anessential issue to be researched, this study is focused onthe analysis of the mutagenicity and genotoxicity of thesemolecules. The mutagenicity of 1h and 1j were determined byAmes test performed on Salmonella TA98 and TA100 strains.Sample 1j was mutagenic on TA98 bacterial strain. However,compound 1h was not mutagenic in bacterial strains TA98and TA100 with and without S9 activation. The genotoxicityof 1h was evaluated by the chromosomal aberration assay onhuman . . . lymphocytes. Compound 1h was also not genotoxicin human lymphocytes in vitro. All results revealed that,1h was not mutagenic in the two Salmonella strains testedand was not genotoxic in chromosomal aberration assay.Therefore, results demonstrate that the described moleculeis promising as a new anticancer drug without mutagenicity.Also, after performing Ames test with other recommendedbacterial strains and in vivo experiments can be used safelyfor the development of new structures exhibiting anticanceractivities Daha fazlası Daha az

Direct to consumer drug advertisments and patient rights: A qualitative research

Şencan, N. | Uyar, M.

Article | 2014 | Marmara Pharmaceutical Journal18 ( 3 ) , pp.164 - 176

AİM: This study aims to understand and manifest the health professionals point of views’ (pharmacists and physicians) on direct to consumer drug advertisements as a part of patient right, who are members of Non Govermental Organisations (NGO). METOD: Focus group discussions and interviewing is used as one of a qualitative research method. In summer and fall of 2012, 3 group discussions were carried out with physicians and pharmacists. Participants’ own opinions on direct to consumer drug advertisements, independent from their memberships of their NGO’s, were talked and recorded via semi structured questions. All the group interviews . . . lasted 1 to 2 hours. The assessments were done after the transcriptions. RESULTS and DISCUSSION: In this priliminary reserach, it is understood that, direct to consumer drug advertismets may harm the patient rights as well as human rights. The participants, phsicians and pharmacists, who are members of pharmaceutical industry and pharmaceutical profession association, declared and mentioned that, a global negotiation of drug industry, manufactırers, exporters,stake holders, pharmacists, community representers and governmental authority is needed on drug advertisements. © 2014, Marmara University. All rights reserved Daha fazlası Daha az

Etanercept protects remote organ damage in a rat model of thermal injury

Şehirli, Ö. | Ünlü, B. | Çetinel, Ş. | Tetik, Ş. | Şener, E. | Şener, G.

Article | 2011 | Marmara Pharmaceutical Journal15 ( 3 ) , pp.118 - 124

Thermal injury may lead to systemic inflammatory response, and multiple organ failure. This study was designed to determine the possible protective effect of etanercept treatment against oxidative damage in the lung tissue induced by burn injury. Under ether anaesthesia, the shaved dorsum of rats was exposed to a 90°C bath for 10 s to induce burn injury. Etanercept (1 mg/kg) or saline was administered intraperitoneally immediately after and at 24th hour burn injury. Rats were decapitated at 6 h and 48 h following burn injury and trunk blood was collected to assay pro-inflammatory cytokines (TNF-? and IL-1ß), lactate dehydrogenase (L . . .DH) activity. In order to evaluate the presence of oxidant injury lung tissue samples were taken for the determination of malondialdehyde (MDA) and glutathione levels, myelopreoxidase (MPO) and Na+-K+ ATPase activities. Tissues were also examined microscopically. Severe skin scald injury (30% of total body surface area) caused a significant decrease in GSH level and Na+-K+ ATPase activity, which was accompanied with significant increases in MDA level, MPO activity. Similarly, serum TNF-?, IL-1ß and LDH were elevated in the burn group as compared to control group. On the other hand, etanercept treatment reversed all these biochemical indices, as well as histopathological alterations, which were induced by thermal trauma. Findings of the present study suggest that etanercept possesses an anti-inflammatory effect on burn-induced pulmonary damage and may be beneficial in thermal trauma Daha fazlası Daha az

Synthesis and antibacterial activity of new hydrazide-hydrazones derived from Benzocaine

Han, Muhammed İhsan | Gürol, Güler | Yıldırım, Temel | Kalaycı, Sadık | Şahin, Fikrettin | Küçükgüzel, Ş. Güniz

Article | 2017 | Marmara Pharmaceutical Journal21 ( 4 ) , pp.961 - 966

A novel series of new eleven benzocaine hydrazide derivatives, N-(4-{[2-(nonsubstituted/ substitutedfuryl/ phenyl/ pyridinyl/ thienyl/ pyrrole)methylidene]hydrazinyl] carbonyl}phenyl) benzamides [3a-k] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR and 1H-NMR) methods and their purity was proven by elemental analysis and thin layer chromatography. These compounds were evaluated for in vitro antibacterial activity by using micro-well dilution method against Escherichia coli ATCC 10536, Escherichia coli ATCC 15442, Staphylococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC . . . 15442, Acinetobacter baumannii , Klebsiella pneumonia ATCC 13883 Daha fazlası Daha az

Influence of honey addition on the bioaccessibility of phenolic contents and antioxidant capacities of different coffee types

Celep, Engin | Yeşilada, Erdem

Article | 2017 | Marmara Pharmaceutical Journal21 ( 4 ) , pp.906 - 914

This study was designed to assess the effect of honey addition to the antioxidant capacity and in vitro bioaccessibility of phenolic content of both brewed and soluble coffee. Floral and pine honey were used in the assay. The antioxidant capacities of the samples were evaluated with three different methods: DPPH radical scavenging activity, cupric reducing capacity and total antioxidant capacity tests. In order to measure the antioxidant metabolites of the samples, total phenolic and flavonoid contents were appraised. In vitro gastrointestinal digestion simulation procedure was conducted to mimic the physiochemical and biochemical f . . .actors of the gastrointestinal tract. During the digestion process, components in the food matrix are exposed to significant structural changes and certain amount of them are effectively absorbed and reach the circulation. To that end, the importance of studies concerning the simulated gastrointestinal digestion increases. The results of this study revealed that honey addition to coffee samples induced increases in antioxidant capacities, total phenolic and flavonoid contents Daha fazlası Daha az

Characterization of Sideritis trojana Bornm. essential oil and its antimicrobial activity

Kırmızıbekmez, Hasan | Karaca, Nursenem | Demirci, Betül | Demirci, Fatih

Article | 2017 | Marmara Pharmaceutical Journal21 ( 4 ) , pp.860 - 865

The components of the essential oil obtained from the dried aerial parts of Sideritis trojana Bornm. by hydrodistillation was analyzed both by GC-FID and GC-MS, simultaneously. Overall 57 compounds were identified representing 83.8% of the oil. The major components of the oil were identified as valeranone (11.3%), ?-bisabolol (10.9%) and ?-caryophyllene (8.8%), respectively. The composition of the oil showed quantitative chemical variation from previously studied material in terms of its major components. Moreover, the essential oil was evaluated for its in vitro antibacterial and anticandidal activities using a broth microdilution . . .method. A selected panel of standard strains of Gram () and Gram (-) human pathogens as well as Candida albicans were used in the assay. As a preliminary result, it was observed that the oil displayed relatively moderate antibacterial activity against Helicobacter pylori with MIC value of 250 µg/mL when compared to standard antimicrobials. As a conclusion, it is worthwhile to evaluate the plant material against a broader spectrum of activities Daha fazlası Daha az

Effect of honey supplementation on total antioxidant capacity of herbal teas

Ş. Özdatli | H. Sipahi | M. Charehsaz | A. Aydin | E. Yeşilada

Article | 2014 | Marmara Pharmaceutical Journal18 ( 3 ) , pp.147 - 152

Scientific researchers have revealed that antioxidant components in herbal teas and honey would be beneficial for the health and may help to reduce the risk of development of acute and chronic diseases. However, possible changes in the antioxidant capacity of herbal teas by the addition of honey as a sweetener have not been investigated in detail yet. The aim of this study was to determine the total antioxidant capacity (TOAC) of 9 different mixed or pure herbal teas marketed in Turkey and then possible changes in the TOAC value of these tea samples after addition of either flower or pine honey. For 100 ml tea which is equivalent to . . . a cup of tea, the highest TOAC value was observed in melissa, black tea and white tea and these were followed by green tea > sage > echinacea > daisy > ginger > linden, respectively. The antioxidant activity of these tea samples increased by the addition of both flowers and pine honeys and 7 g of honey exerted higher activity than 3 g of honey. Higher antioxidant activity was observed in some herbal tea samples (melissa, sage, linden, chamomile, lemon ginger) by the addition of pine honey, whereas in some teas (echinacea, black, white and green teas) flower honey supplementation has been found to be more effective. In conclusion, our study suggests that addition of honey to herbal tea increase its antioxidant activity significantly and drinking herbal tea with honey at least once a day may protect the body against the harmful effects of free radicals. However, further studies are required to understand the protective mechanisms of this combination. © 2014, Marmara University. All rights reserved Daha fazlası Daha az

Determination and safety evaluation of furfural and hydroxymethylfurfural in some honey samples by using a validated hplc-dad method

Türköz Acar, E. | Helvacioğlu, S. | Charehsaz, M. | Aydin, A.

Article | 2018 | Marmara Pharmaceutical Journal22 ( 4 ) , pp.519 - 527

Synthesis and biological evaluation of some new 1,3,4-thiadiazole and 1,2,4-triazole derivatives from L-methionine as antituberculosis and antiviral agents

Tatar, E. | Küçükgüzel, Ş. | Karakuş, S. | de Clercq, E. | Andrei, G. | Snoeck, R. | Küçükgüzel, İ.

Article | 2015 | Marmara Pharmaceutical Journal19 ( 2 ) , pp.88 - 102

Some novel 1,3,4-thiadiazole [5-8] and 1,2,4-triazole [9-12] derivatives carrying amino acid moiety were synthesized starting from L-methionine. 1,3,4-Thiadiazole and 1,2,4-triazole scaffolds were prepared by cyclocondensation of the corresponding thiosemicarbazide and finally converted to their thiourea derivatives. Structures of the synthesized compounds [4-12] were confirmed by IR, 1H-NMR and 13C-NMR spectral data and elemental analysis. Synthesized compounds were evaluated for their antiviral and antibacterial activity. Of the screened compounds, N-{3-(methylsulfanyl)- 1-[5-(phenylamino)-1,3,4-thiadiazole-2-yl]propyl}benzamide [ . . .5] was identified as the most potent inhibitor of Influenza A H3N2 virus with an EC50 value of 31.4 µM, which serves as a lead compound for prospective development. The antituberculosis activity screen of the synthesized compounds revealed 1-[4-(4-chloro-(3-trifluoromethyl)phenyl]-3-[3-(methylsulfanyl)- 1-(4-phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole- 3-yl)propyl]thiourea [12] as the most active compound against M. tuberculosis H37Rv strain (MIC : 30.88 µM) but the compound proved not selective. © 2015, Marmara University. All rights reserved Daha fazlası Daha az

Synthesis and evaluation of antiviral, antitubercular and anticancer activities of some novel thioureas derived from 4-aminobenzohydrazide hydrazones

Çikla, P. | Güniz Küçükgüzel, Ş. | Küçükgüzel, I. | Rollas, S. | De Clercq, E. | Pannecouque, C. | Bayrak, Ö.F.

Article | 2010 | Marmara Pharmaceutical Journal14 ( 1 ) , pp.13 - 20

A series of novel 1-[4-[[2-[(4-substituted phenyl)methylene]hydrazino]carbonyl]p henyl]-3-substituted thiourea derivatives have been synthesized by the addition of substituted aryl isothiocyanates to 4-amino-N'-[(4-substituted phenyl) methylene] benzohydrazide, which was prepared by condensation of 4-aminobenzoic acid hydrazide with 4-fluorobenzaldehyde or 4-(trifluoromethyl)benzaldeyde. All synthesized compounds were evaluated in vitro against HIV-1 (IIIB) and HIV-2 (ROD) strains in MT-4 cells, as well as other selected viruses such as HSV-1, HSV-2, Coxsackie virus B4, Sindbis virus, human cytomegalovirus, and varicella-zoster viru . . .s using HeLa, Vero, or HEL cell cultures. Antimycobacterial activity against Mycobacterium tuberculosis H37 Rv was also evaluated. The anticancer activity and cytotoxicity screening of the synthesized compounds were determined on A 549 and L 929 cell lines Daha fazlası Daha az

The role of patient education in adherence to antibiotic therapy in primary care

N.B. Göktay | S. Telefoncu | S.B. Kadioglu | C. Macit | N. Şencan | P.M. Clark

Article | 2013 | Marmara Pharmaceutical Journal17 ( 2 ) , pp.113 - 119

AIM: Adherence is an important factor in the achievement of therapeutic outcomes, while patient education is thought to positively affect adherence. The aim of this study is to assess patient adherence to prescribed antibacterial agents impact of patient education on adherence with the therapy. MATERIALS AND METHODS: This study was a prospective, controlled trial conducted at a community pharmacy in Istanbul, between January and July 2010, among patients who had been prescribed antibiotics. After filling out an initial questionnaire, patients were educated about their antibiotic therapy either in a simple (control group) or more com . . .prehensive way (study group). A second questionnaire, conducted the day after antibiotic therapy ended, focused on how patients had actually used their antibiotics. and based on patients' self reports Adherence was assessed using both a tablet count and a self-report method to explore whether the timing of the doses was correct. RESULTS AND DISCUSSION: Patients in the study group demonstrated a non-significantly better adherence to therapy than those in the control group. There was no significant difference between the patients informed and uninformed by the physician in terms of the rates of information request from pharmacist. However, patients who were prescribed a once daily dose regimen for a short duration were found more adherent to antibacterial therapy in terms both of dose-taking (self-administration) and dose-timing (p < 0.05). In addition, more mature patients (>30 year-old) were found more adherent than younger people (p < 0.05). The potential role of the pharmacist in providing patient education was underscored Daha fazlası Daha az

Quality of life assessment of patients with metastatic lung cancer receiving platinum-based chemotherapy

Kivrak-Bernardelli, B.G. | Macit, C. | Beril Kadioglu, S. | Salepci, T. | Clark, P.M.

Article | 2013 | Marmara Pharmaceutical Journal17 ( 2 ) , pp.120 - 130

AIM: The aims of the study were to investigate, possible changes in quality of life (QOL) during chemotherapy, which factors might affect QOL and the relationship between QOL and performance status. MATERIAL AND METHODS: The study was conducted at the oncology clinics of Dr. Lutfi Kirdar Kartal Training and Research Hospital, Istanbul, Turkey. Patients diagnosed with advanced small-cell lung cancer or stage IV non-small cell lung cancer were enrolled in the study. They were given platinum-based chemotherapy. The QOL EORTC core questionnaire QLQ-C30 (version 3.0) and the lung cancer module QLQ-LC13 were conducted on four separate occ . . .asions. Data related to the patients' clincal and performance status (Karnofsky Performance Status Scale (KPS) and ECOG) were recorded throughout the study. RESULTS: With treatment, significant increases in chemotherapy related side-effects and in symptom scales related both to adverse drug reactions and disease progression were recorded. A strong, significant, negative correlation (r = -0.71, p< 0.05) between ECOG performance and all domains of EORTC QLQ-C30 was observed, similar to that between KPS and EORTC QLQ-C30 (r = -0.74, p< 0.05). CONCLUSION: This research indicates a lack of benefit in terms of QOL from platinum-based chemotherapy in patients with metastatic lung cancer. Routine QOL assessment in this patient population may encourage the development of treatment programs which minimize chemotherapy side-effects, while maximizing patients' well being Daha fazlası Daha az

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