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Cytotoxicity

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Alkylaminophenol Induces G1/S Phase Cell Cycle Arrest In Glioblastoma Cells Through P53 And Cyclin-Dependent Kinase Signaling Pathway., Phuong Doan, Aliyu Musa, Nuno R Candeias, Frank Emmert-Streib, Olli Yli-Harja, Meenakshisundaram Kandhavelu Jan 2019

Alkylaminophenol Induces G1/S Phase Cell Cycle Arrest In Glioblastoma Cells Through P53 And Cyclin-Dependent Kinase Signaling Pathway., Phuong Doan, Aliyu Musa, Nuno R Candeias, Frank Emmert-Streib, Olli Yli-Harja, Meenakshisundaram Kandhavelu

Articles, Abstracts, and Reports

Glioblastoma (GBM) is the most common type of malignant brain tumor in adults. We show here that small molecule 2-[(3,4-dihydroquinolin-1(2H)-yl)(p-tolyl)methyl]phenol (THTMP), a potential anticancer agent, increases the human glioblastoma cell death. Its mechanism of action and the interaction of selective signaling pathways remain elusive. Three structurally related phenolic compounds were tested in multiple glioma cell lines in which the potential activity of the compound, THTMP, was further validated and characterized. Upon prolonged exposer to THTMP, all glioma cell lines undergo p53 and cyclin-dependent kinase mediated cell death with the IC

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Novel Hybrid Analogs Of Estrone Origin Exhibits Cytotoxic Effects Against Egfr-Dependent Cancers, Felix Acheampong Jan 2019

Novel Hybrid Analogs Of Estrone Origin Exhibits Cytotoxic Effects Against Egfr-Dependent Cancers, Felix Acheampong

Electronic Theses and Dissertations

Cancer is second only to cardiovascular illnesses as the deadliest human disease globally. Currently, non-small cell lung cancer (NSCLC) and triple negative breast carcinoma (TNBC) are the most frequent types of cancer and have the highest mortalities. Epidermal growth factor receptor (EGFR), a central regulator of tumor progression, is frequently overexpressed in both cancers and is a key clinical target for therapeutic intervention. Natural products and their synthetic analogs have been utilized as EGFR tyrosine kinase inhibitors (TKIs) with potent antitumor effects. However, acquired resistance limits the long-term efficacy of these drugs. Estrone has been used as a scaffold in …

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A Novel 1,4-Naphthoquinone-Derived Compound Induces Apoptotic Cell Deathin Breast Cancer Cells, Di̇dem Karakaş Zeybek, Remzi̇ Okan Akar, Zeli̇ha Gökmen, Nahi̇de Gülşah Deni̇z, Engi̇n Ulukaya Jan 2019

A Novel 1,4-Naphthoquinone-Derived Compound Induces Apoptotic Cell Deathin Breast Cancer Cells, Di̇dem Karakaş Zeybek, Remzi̇ Okan Akar, Zeli̇ha Gökmen, Nahi̇de Gülşah Deni̇z, Engi̇n Ulukaya

Turkish Journal of Biology

Breast cancer is the most-diagnosed cancer type among women. The triple-negative subtype is an especially aggressive type of breast cancer. Although chemotherapy is almost the only option for the treatment of triple-negative breast cancer (TNBC), currently used chemotherapeutics are not effective enough, considering the poor survival rate of patients. Therefore, novel compounds need to be developed to improve survival rates. It has been known that quinonic compounds, which are found in nature, have antibacterial, antifungal, and antitumorigenic properties. Naphthoquinones are members of the quinone family and are widely used in research due to their promising properties. In this study, we …

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Spheroid-3d And Monolayer-2d Intestinal Electrochemical Biosensor For Toxicity/Viability Testing: Applications In Drug Screening, Food Safety, And Environmental Pollutant Analysis, Evangelia Flampouri, Shahzad Imar, Kieran O'Connell, Baljit Singh Jan 2019

Spheroid-3d And Monolayer-2d Intestinal Electrochemical Biosensor For Toxicity/Viability Testing: Applications In Drug Screening, Food Safety, And Environmental Pollutant Analysis, Evangelia Flampouri, Shahzad Imar, Kieran O'Connell, Baljit Singh

Articles

The rise of three-dimensional cell culture systems that provide in vivo-like environments for pharmaco-toxicological models has prompted the need for simple and robust viability assays suitable for complex cell architectural structures. This study addresses that challenge with the development of an in vitro enzyme based electrochemical sensor for viability/cytotoxicity assessment of two-dimensional (2D) monolayer and three-dimensional (3D) spheroid culture formats. The biosensor measures the cell viability/toxicity via electrochemical monitoring of the enzymatic activity of nonspecific esterases of viable cells, through the hydrolysis of 1-naphthyl acetate to 1-naphthol. The proposed sensor demonstrated strong correlation (r = 0.979) with viable …

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Characterizing The Physicochemical Properties Of Tdp-43 Protein And Acetylated Amyloid Β Peptides To Discern Its Role In Neurodegenerative Diseases, Rashmi Adhikari Jan 2019

Characterizing The Physicochemical Properties Of Tdp-43 Protein And Acetylated Amyloid Β Peptides To Discern Its Role In Neurodegenerative Diseases, Rashmi Adhikari

Dissertations, Master's Theses and Master's Reports

Proteins are the biological macromolecules central to most cellular functions. The native structure of protein determines its function and any perturbations such as mutation, changes in pH, macromolecular crowding, oxidative stress, may promote protein misfolding and/or aggregation. Protein misfolding or aggregation can contribute to diseases either through loss of proteins’ critical function or by gain of toxic function. Among the various proteins associated with neurodegeneration, trans-active response (TAR) DNA binding protein 43 (TDP-43) has sparked interest in researchers due to its diverse role in several neurodegenerative diseases like Amyotrophic Lateral Sclerosis (ALS), Frontotemporal Lobar degeneration (FTLD), Alzheimer’s, Parkinson’s and Huntington’s …

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Is Tpmt Testing A Predictor Of Duration Of Use Or Long-Term Benefit Of Thiopurine Agents?, Shatoya R. Wilson Dec 2018

Is Tpmt Testing A Predictor Of Duration Of Use Or Long-Term Benefit Of Thiopurine Agents?, Shatoya R. Wilson

Masters Theses

Background: Inflammatory Bowel Disease (IBD) affects as many as 1.3 million Americans and includes both ulcerative colitis (UC) and Crohn’s disease (CD). Recent practices have moved towards using immunomodulators early in the course of disease to prevent disease progression. Patients have shown improved outcomes on immunomodulators compared to aminosalicylates, and reduced risk for tachyphylaxis compared to corticosteroid treatment. Thiopurine agents such as azathioprine and 6-mercaptopurine are immunomodulators often used to treat IBD. Unfortunately, many patients experience cytotoxicity from thiopurine use. Recent studies have shown that patients deficient in thiopurine-S-methyltransferase (TMPT), produce an overabundance of the therapeutic end product, 6-thioguanine nucleotide …

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Pyronaridine Exerts Potent Cytotoxicity On Human Breast And Hematological Cancer Cells Through Induction Of Apoptosis, Paulina J. Villanueva, Alberto Martinez, Sarah T. Baca, Rebecca E. Dejesus, Manuel Larragoity, Lisett Contreras, Denisse A. Gutierrez, Armando Varela-Ramirez, Renato J. Aguilera Nov 2018

Pyronaridine Exerts Potent Cytotoxicity On Human Breast And Hematological Cancer Cells Through Induction Of Apoptosis, Paulina J. Villanueva, Alberto Martinez, Sarah T. Baca, Rebecca E. Dejesus, Manuel Larragoity, Lisett Contreras, Denisse A. Gutierrez, Armando Varela-Ramirez, Renato J. Aguilera

Publications and Research

The potent antimalarial drug pyronaridine (PND) was tested for its potential as an anticancer drug. After exposing cancerous (17) and non-cancerous (2) cells to PND for 72 hr, PND was found to exhibit consistent and potent cytotoxic activity at low micromolar (μM) concentrations that ranged from 1.6 μM to 9.4 μM. Moreover, PND exerted a significant selective cytotoxicity index (SCI) on five out of seven breast cancer cell lines tested, with favorable values of 2.5 to 4.4, as compared with the non-cancerous breast MCF-10A cell line. By using the same comparison, PND exhibited a significant SCI on three out of …

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Polyestyrene And Low Density Polyethylene Oregano´S Essential Oil Functionalization For Possible Antimicrobial Active Packaging Applications, Edgar Díaz-Acosta, Claudia Rodríguez-González, Laura Valencia-Gómez, Santos Adriana Martel-Estrada, Maria Hernández-González, Hortensia Reyes-Blas, Imelda Olivas Armendáriz 1761524 Sep 2018

Polyestyrene And Low Density Polyethylene Oregano´S Essential Oil Functionalization For Possible Antimicrobial Active Packaging Applications, Edgar Díaz-Acosta, Claudia Rodríguez-González, Laura Valencia-Gómez, Santos Adriana Martel-Estrada, Maria Hernández-González, Hortensia Reyes-Blas, Imelda Olivas Armendáriz 1761524

Journal of Applied Packaging Research

Low density polyethylene (LDPE) and polystyrene (PS) samples were functionalized with oregano´s essential oil (OEO) for possible antimicrobial packing applications. Different concentrations of OEO were used (0.5-1.5 % v/v). Polymers were UV light irradiated during 60 min to improve the OEO adhesion through the polar groups (COOH, OH or COO-) generation on their surface. The effect of OEO different concentration on their antimicrobial activity, mechanical properties and cytotoxicity of the functionalized polymers were analyzed. All functionalized samples showed antimicrobial activity against Gram positive and Gram negative bacteria and this activity increased with OEO concentration. The addition of OEO did not …

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Chemical Strategies For Drug Development Of Fucose-Truncated Ipomoeassin F Analogues, Melissa Hirsch Aug 2018

Chemical Strategies For Drug Development Of Fucose-Truncated Ipomoeassin F Analogues, Melissa Hirsch

Graduate Theses and Dissertations

Natural product synthesis has many applications in the field of chemical biology, due to the protein binding affinity to the complex three-dimensional structure. However, synthetic and structure-activity relationship studies concerning certain drug targets are scarce. For example, members of the ipomoeassin family have exhibited anti-cancer properties, but cost-effective optimization of these compounds has not yet been extensively studied. Ipomoeassin F, a natural glycoresin isolated from the leaves of the Ipomoea squamosa plant in the Suriname rainforest, has shown high cytotoxicity, with IC50 values measured at the low nanomolar range. Two studies by Postema and Fuerstner have outlined synthesis pathways for …

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Bioactivities Of Extracts, Debromolaurinterol And Fucosterol From Macroalgae Species, Sartaz Begum, Stephen S. Nyandoro, Amelia S. Buriyo, John J. Makangara, Joan J. E. Munissi, Sandra Duffy, Vicky M. Avery, Mate Erdelyi Jul 2018

Bioactivities Of Extracts, Debromolaurinterol And Fucosterol From Macroalgae Species, Sartaz Begum, Stephen S. Nyandoro, Amelia S. Buriyo, John J. Makangara, Joan J. E. Munissi, Sandra Duffy, Vicky M. Avery, Mate Erdelyi

Tanzania Journal of Science

Parasitic diseases including malaria, and other numerous microbial infections and physiological diseases are threatening the global population. Tanzanian coast shores are endowed with a variety of macroalgae (seaweeds), hitherto unsystematically explored to establish their biomedical potentials. Thus, antiplasmodial activity using malarial imaging assay, antimicrobial activity using microplate dilution technique, antioxidant activity using DPPH radical scavenging method and cytotoxicity using brine shrimp test were carried out on crude extracts from the selected species of algae (Acanthophora spicifera, Cystoseira myrica, Cystoseira trinodis, Laurencia filiformis, Padina boryana, Sargassum oligocystum, Turbinaria crateriformis, Ulva fasciata and Ulva reticulata) occurring along the coast of Tanzania. The …

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Synthesis And In Vitro Pdt Evaluation Of New Porphyrins Containing Meso-Epoxymethylaryl Cationic Groups, Jaqueline Carneiro, Alan Gonçalves, Zehua Zhou, Kaitlin E. Griffin, Nichole E.M. Kaufman, Maria Da Graça Henriques Vicente Jul 2018

Synthesis And In Vitro Pdt Evaluation Of New Porphyrins Containing Meso-Epoxymethylaryl Cationic Groups, Jaqueline Carneiro, Alan Gonçalves, Zehua Zhou, Kaitlin E. Griffin, Nichole E.M. Kaufman, Maria Da Graça Henriques Vicente

Faculty Publications

© 2018 Wiley Periodicals, Inc. Objectives: Photodynamic therapy (PDT) is an effective cancer treatment that uses photosensitizers, light, and oxygen to destroy malignant cells. Porphyrins, and in particular the cationic derivatives, are the most investigated photosensitizers for PDT. In this context, it is important to study new methodologies to develop efficient cationic photosensitizers for use in PDT. Materials and Methods: New porphyrins bearing cationic epoxymethylaryl groups were synthesized and characterized. Their cellular uptake, intracellular localization, and phototoxicity were evaluated in human HEp2 cells, and compared with their methylated analogs. Results: All cationic porphyrins were efficient generators of singlet oxygen, with …

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Design, Synthesis, And Evaluation Of Homochiral Peptides Containing Arginine And Histidine As Molecular Transporters, Naglaa Salem El-Sayed, Taryn Miyake, Amir Nasrolahi Shirazi, Shang Eun Park, Jimmy Clark, Stephani Buchholz, Keykavous Parang, Rakesh Tiwari Jun 2018

Design, Synthesis, And Evaluation Of Homochiral Peptides Containing Arginine And Histidine As Molecular Transporters, Naglaa Salem El-Sayed, Taryn Miyake, Amir Nasrolahi Shirazi, Shang Eun Park, Jimmy Clark, Stephani Buchholz, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

Linear (HR)n and cyclic [HR]n peptides (n = 4,5) containing alternate arginine and histidine residues were synthesized. The peptides showed 0–15% cytotoxicity at 5–100 μM in human ovarian adenocarcinoma (SK-OV-3) cells while they exhibited 0–12% toxicity in human leukemia cancer cell line (CCRF-CEM). Among all peptides, cyclic [HR]4 peptide was able to improve the delivery of a cell impermeable fluorescence-labeled phosphopeptide by two-fold. Fatty acids of different alkyl chain length were attached at the N-terminal of the linear peptide (HR)4 to improve the molecular transporter property. Addition of fatty acyl chains was expected to help with the permeation of the …

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Human Gucy2c-Targeted Chimeric Antigen Receptor (Car)-Expressing T Cells Eliminate Colorectal Cancer Metastases., Michael S. Magee, Tara S. Abraham, Trevor R. Baybutt, John C. Flickinger, Natalie A. Ridge, Glen P Marszalowicz, Priyanka Prajapati, Adam R. Hersperger, Scott A. Waldman, Adam E. Snook May 2018

Human Gucy2c-Targeted Chimeric Antigen Receptor (Car)-Expressing T Cells Eliminate Colorectal Cancer Metastases., Michael S. Magee, Tara S. Abraham, Trevor R. Baybutt, John C. Flickinger, Natalie A. Ridge, Glen P Marszalowicz, Priyanka Prajapati, Adam R. Hersperger, Scott A. Waldman, Adam E. Snook

Department of Pharmacology and Experimental Therapeutics Faculty Papers

One major hurdle to the success of adoptive T-cell therapy is the identification of antigens that permit effective targeting of tumors in the absence of toxicities to essential organs. Previous work has demonstrated that T cells engineered to express chimeric antigen receptors (CAR-T cells) targeting the murine homolog of the colorectal cancer antigen GUCY2C treat established colorectal cancer metastases, without toxicity to the normal GUCY2C-expressing intestinal epithelium, reflecting structural compartmentalization of endogenous GUCY2C to apical membranes comprising the intestinal lumen. Here, we examined the utility of a human-specific, GUCY2C-directed single-chain variable fragment as the basis for a CAR construct targeting …

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Differential Effects Of Linkers On The Activity Of Amphiphilic Tobramycin Antifungals, Marina Y. Fosso, Sanjib K. Shrestha, Nishad Thamban Chandrika, Emily K. Dennis, Keith D. Green, Sylvie Garneau-Tsodikova Apr 2018

Differential Effects Of Linkers On The Activity Of Amphiphilic Tobramycin Antifungals, Marina Y. Fosso, Sanjib K. Shrestha, Nishad Thamban Chandrika, Emily K. Dennis, Keith D. Green, Sylvie Garneau-Tsodikova

Pharmaceutical Sciences Faculty Publications

As the threat associated with fungal infections continues to rise and the availability of antifungal drugs remains a concern, it becomes obvious that the need to bolster the antifungal armamentarium is urgent. Building from our previous findings of tobramycin (TOB) derivatives with antifungal activity, we further investigate the effects of various linkers on the biological activity of these aminoglycosides. Herein, we analyze how thioether, sulfone, triazole, amide, and ether functionalities affect the antifungal activity of alkylated TOB derivatives against 22 Candida, Cryptococcus, and Aspergillus species. We also evaluate their impact on the hemolysis of murine erythrocytes and the …

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Toxicological Assessment Of Nanomaterials: The Role Of In Vitro Raman Microspectroscopic Analysis, Esen Efeoglu, Marcus Maher, Alan Casey, Hugh Byrne Apr 2018

Toxicological Assessment Of Nanomaterials: The Role Of In Vitro Raman Microspectroscopic Analysis, Esen Efeoglu, Marcus Maher, Alan Casey, Hugh Byrne

Articles

The acceleration of nanomaterials research has brought about increased demands for rapid analysis of their bioactivity, in a multi-parametric fashion, to minimise the gap between potential applications and knowledge of their toxicological properties. The potential of Raman microspectroscopy for the analysis of biological systems with the aid of multivariate analysis techniques has been demonstrated. In this study, an overview of recent efforts towards establishing a ‘label-free high content nanotoxicological assessment technique’ using Raman microspectroscopy is presented. The current state of the art for cellular toxicity assessment and the potential of Raman microspectroscopy are discussed, and the spectral markers of the …

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Comparative Cytotoxicity Study Of Nicotine And Cotinine On Mrc-5 Cell Line, Ana-Maria Vlasceanu, Daniela Luiza Baconi, Bianca Galateanu, Miriana Stan, Cristian Balalau Mar 2018

Comparative Cytotoxicity Study Of Nicotine And Cotinine On Mrc-5 Cell Line, Ana-Maria Vlasceanu, Daniela Luiza Baconi, Bianca Galateanu, Miriana Stan, Cristian Balalau

Journal of Mind and Medical Sciences

Nicotine has several health hazards regarding carcinogenic potential. It also imparts increased risk for respiratory, cardiovascular, and gastrointestinal disorders. Several mechanisms have been proposed for the carcinogenic potential, including effects on cell proliferation, inducing oxidative stress, DNA mutation, or inhibition of apoptosis. The cotinine metabolite is generally thought to have effects similar to nicotine in some experimental systems. The purpose of this study was to assess the nicotine and cotinine cytotoxicity on MRC-5 lung fibroblasts. The pulmonary fibroblasts were treated with various concentrations of nicotine or cotinine (in the range 1 µM – 2 mM) for 24 or 48 h …

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Phaeophleospora Vochysiae Savi & Glienke Sp. Nov. Isolated From Vochysia Divergens Found In The Pantanal, Brazil, Produces Bioactive Secondary Metabolites, Daiani C. Savi, Khaled A. Shaaban, Francielly M. W. Gos, Larissa V. Ponomareva, Jon S. Thorson, Chirlei Glienke, Jürgen Rohr Feb 2018

Phaeophleospora Vochysiae Savi & Glienke Sp. Nov. Isolated From Vochysia Divergens Found In The Pantanal, Brazil, Produces Bioactive Secondary Metabolites, Daiani C. Savi, Khaled A. Shaaban, Francielly M. W. Gos, Larissa V. Ponomareva, Jon S. Thorson, Chirlei Glienke, Jürgen Rohr

Pharmaceutical Sciences Faculty Publications

Microorganisms associated with plants are highly diverse and can produce a large number of secondary metabolites, with antimicrobial, anti-parasitic and cytotoxic activities. We are particularly interested in exploring endophytes from medicinal plants found in the Pantanal, a unique and widely unexplored wetland in Brazil. In a bio-prospecting study, strains LGMF1213 and LGMF1215 were isolated as endophytes from Vochysia divergens, and by morphological and molecular phylogenetic analyses were characterized as Phaeophleospora vochysiae sp. nov. The chemical assessment of this species reveals three major compounds with high biological activity, cercoscosporin (1), isocercosporin (2) and the new compound 3-(sec-butyl)-6-ethyl-4,5-dihydroxy-2-methoxy-6-methylcyclohex-2-enone (3). …

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Synthesis, Characterization, And In Vitro Cytotoxicity Of Fatty Acyl-Cgkrk-Chitosan Oligosaccharides Conjugates For Sirna Delivery, Naglaa Salem El-Sayed, Meenakshi Sharma, Hamidreza Montazeri Aliabadi, Magda Goda El-Meligy, Ahmed Kamed El-Zaity, Zenat Adeeb Nageib, Rakesh Tiwari Feb 2018

Synthesis, Characterization, And In Vitro Cytotoxicity Of Fatty Acyl-Cgkrk-Chitosan Oligosaccharides Conjugates For Sirna Delivery, Naglaa Salem El-Sayed, Meenakshi Sharma, Hamidreza Montazeri Aliabadi, Magda Goda El-Meligy, Ahmed Kamed El-Zaity, Zenat Adeeb Nageib, Rakesh Tiwari

Pharmacy Faculty Articles and Research

In this studies, three fatty acyl derivatives of CGKRK homing peptides were coupled successfully to chitosan oligosaccharides (COS) using sulfosuccinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate sodium salt (sulfo-SMCC). The COS-SMCC was prepared by direct coupling between COS and sulfo-SMCC in PBS (pH 7.5) at RT for 48 h. The structure of COS-SMCC and the three fatty acyl-CGKRK-SMCC-COS conjugates were characterized by FT-IR, 13C NMR, and SEM. The ability of three conjugates to condense siRNA into nanosized polyplexes and their efficacy in protecting siRNA from serum nucleases degradation were investigated. Among the investigated derivatives, S-CGKRK-COS showed higher siRNA binding affinity as compared to …

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Novel Fluconazole Derivatives With Promising Antifungal Activity, Nishad Thamban Chandrika, Sanjib K. Shrestha, Huy X. Ngo, Kaitlind C. Howard, Sylvie Garneau-Tsodikova Feb 2018

Novel Fluconazole Derivatives With Promising Antifungal Activity, Nishad Thamban Chandrika, Sanjib K. Shrestha, Huy X. Ngo, Kaitlind C. Howard, Sylvie Garneau-Tsodikova

Pharmaceutical Sciences Faculty Publications

The fungistatic nature and toxicity concern associated with the azole drugs currently on the market have resulted in an increased demand for new azole antifungal agents for which these problematic characteristics do not exist. The extensive use of azoles has resulted in fungal strains capable of resisting the action of these drugs. Herein, we report the synthesis and antifungal activities of novel fluconazole (FLC) analogues with alkyl-, aryl-, cycloalkyl-, and dialkyl-amino substituents. We evaluated their antifungal activity by MIC determination and time-kill assay as well as their safety profile by hemolytic activity against murine erythrocytes as well as cytotoxicity against …

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Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel Jan 2018

Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel

Turkish Journal of Chemistry

A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16-25 were synthesized by reacting the corresponding $N$-(5-substituted-1,3,4-thiadiazol-2-yl)-2-chloroacetamides with ciprofloxacin or norfloxacin. The purity and identity of the synthesized compounds were determined by the use of chromatographic and spectral techniques (NMR, IR, MS, etc.) besides elemental analysis. Antibacterial, antituberculosis, and anticancer activity of the target compounds were evaluated against selected strains and cancer cell lines. Compound 20 was appreciated as the most active agent representing antibacterial activity against Escherichia coli and Staphylococcus aureus with MIC values of 4 …

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Synthesis And Cytotoxicity Evaluation Of [(2,4-Dichlorophenoxy)Methyl]-5-Aryl-1,3,4-Oxadiazole/4$H$-1,2,4-Triazole Analogues, Mohamed Jawed Ahsan Jan 2018

Synthesis And Cytotoxicity Evaluation Of [(2,4-Dichlorophenoxy)Methyl]-5-Aryl-1,3,4-Oxadiazole/4$H$-1,2,4-Triazole Analogues, Mohamed Jawed Ahsan

Turkish Journal of Chemistry

We report herein the synthesis, characterization, and cytotoxicity evaluations of some newer oxadiazole and triazole analogues (5a-j). The cytotoxicity of all the title compounds were evaluated as per the National Cancer Institute protocol in a one-dose assay (10 $\mu $M) on nine different panels of 59 cancer cell lines. 2-$\{$5-[(2,4-Dichlorophenoxy)methyl]-1,3,4-oxadiazol-2-yl$\}$phenol (5e) showed the maximum cytotoxicity among the series of ten compounds. The cytotoxicity of 5e was comparable to that of the standard anticancer drug, 5-fluorouracil, and better than that of imatinib. The structure activity relationship was also discussed.

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Hydrogen Peroxide And Beyond - The Potential Of High-Voltage Plasma Activated Liquids Against Cancerous Cells, Daniela Boehm, James Curtin, Patrick J. Cullen, Paula Bourke Jan 2018

Hydrogen Peroxide And Beyond - The Potential Of High-Voltage Plasma Activated Liquids Against Cancerous Cells, Daniela Boehm, James Curtin, Patrick J. Cullen, Paula Bourke

Articles

Abstract: The use of plasma-activated liquids such as PBS, medium or simply plasma-activated water (PAW) has been receiving increasing attention for applications in cancer treatments. Amongst the reactive species contained in these solutions, hydrogen peroxide appears to play a pivotal role in causing cytotoxic effects. While H2O2 concentrations can be correlated with reduced cell viability and growth and used as an indicator of the potential efficacy of a plasma-activated water, comparisons to standard H2O2 kill curves demonstrate a potency in PAW which exceeds H2O2 associated toxicity, indicating that other plasma-generated species play an important role. Using a high-voltage dielectric barrier …

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Understanding The Differences Between Antimicrobial And Cytotoxic Properties Of Plasma Activated Liquids, Eva Tsoukou, Paula Bourke, Daniela Boehm Jan 2018

Understanding The Differences Between Antimicrobial And Cytotoxic Properties Of Plasma Activated Liquids, Eva Tsoukou, Paula Bourke, Daniela Boehm

Articles

The aqueous environment plays an important role in the transmission of cold plasma effects to both prokaryotic and eukaryotic cells. The exposure of liquids to cold atmospheric plasma discharges results in the generation of secondary reactive species; specifically, hydrogen peroxide (H2O2) seems to be one of the most important amongst the reactive species contained in plasma activated liquids (PALs) in causing cytotoxicity. Detailed understanding of the effects of PALs on cells is essential to harness this new technology. Liquids acting as models for non-complex solutions were generated using a dielectric barrier discharge atmospheric cold plasma (DBD-ACP) system. The chemical characterization …

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Comparative Evaluation Of Nano And Bulk Tin Dioxide Cytotoxicity On Dermal Fibroblasts By Real-Time Impedance-Based And Conventional Methods, Şükran Şeker Jan 2018

Comparative Evaluation Of Nano And Bulk Tin Dioxide Cytotoxicity On Dermal Fibroblasts By Real-Time Impedance-Based And Conventional Methods, Şükran Şeker

Turkish Journal of Biology

In this study, the possible cellular effects of tin dioxide (SnO2) nanoparticles, together with its bulk form, on mouse dermal fibroblasts (DFs) were revealed using in vitro assays. Particle characterizations were carried out with AFM, Braun-Emmet-Teller, and DLS analyses. The cells were treated with nano and bulk SnO2 at concentrations of 0.1, 1, 10, 50, and 100 μg/mL for 6, 24, and 48 h. At the end of the exposure periods, the morphology, viability, particle uptake, and membrane leakage statuses of the cells were evaluated. Furthermore, real-time monitoring of cell responses was performed by using an impedance-based label-free system. Findings …

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Cytoprotective Effect Of A Functional Antipollutant Blend Through Reducing B[A] P-Induced Intracellular Oxidative Stress And Uva Exposure, Gi̇zem Örs, Sultan Gülçe İz Jan 2018

Cytoprotective Effect Of A Functional Antipollutant Blend Through Reducing B[A] P-Induced Intracellular Oxidative Stress And Uva Exposure, Gi̇zem Örs, Sultan Gülçe İz

Turkish Journal of Biology

Benzo[a]pyrene (B[a]P) is a ubiquitous environmental pollutant that reacts with skin and induces intracellular oxidative stress through reactive oxygen species (ROS) accumulation. The antipollution properties of natural extracts, especially including antioxidants, for inhibiting ROS in cells are gaining importance, in addition to the anticancer effects attributed to them. In this study, a commercial functional antipollutant blend of plant extracts consisting of ellagic acid standardized Punica granatum peel extract, Sambucus nigra fruit extract, Prunus cerasus seed extract, and hydrolyzed wheat protein with high antioxidant properties and UV damage-protective properties attributed to each one was investigated. The cytoprotective effect of this functional …

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Peptidomic Characterization And Bioactivity Of Protoiurus Kraepelini(Scorpiones: Iuridae) Venom, Tuğba Doğan, Naşi̇t İğci̇, Ayşenur Bi̇ber, Seli̇n Gerekci̇, Hepşen Hazal Hüsnügi̇l, Afi̇fe İzbirak, Can Özen Jan 2018

Peptidomic Characterization And Bioactivity Of Protoiurus Kraepelini(Scorpiones: Iuridae) Venom, Tuğba Doğan, Naşi̇t İğci̇, Ayşenur Bi̇ber, Seli̇n Gerekci̇, Hepşen Hazal Hüsnügi̇l, Afi̇fe İzbirak, Can Özen

Turkish Journal of Biology

Protoiurus kraepelini is a scorpion species found in parts of Turkey and Greece. In this study, the peptide profile of its venom was determined for the first time. The electrophoretic profile of the crude venom showed a protein distribution from 2 to 130 kDa. MALDI-TOF MS analysis of the venom peptide fraction yielded 27 peptides between 1059 and 4623 Da in mass. Several ion channelblocking and antimicrobial peptides were identified by peptide mass fingerprinting analysis. Cytotoxic and antimicrobial effects of the venom were also demonstrated on Jurkat cells and Escherichia coli, respectively. As the first peptidomic characterization study on P. …

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Comparative Toxicology Of Nio And Ni(Oh)₂ Nanoparticles, Melissa Hope Cambre Jan 2018

Comparative Toxicology Of Nio And Ni(Oh)₂ Nanoparticles, Melissa Hope Cambre

Masters Theses

“Understanding the potential toxicity of nanoparticles (NPs) is important to ensure that these new products do not impose harmful effects to human and environmental health. Paper I is a literature review in which we discuss characteristics of nanomaterials, with an emphasis on transition metal oxide nanoparticles that influence cytotoxicity. Identification of those properties may lead to the design of more efficient and safer nanosized products for various industrial purposes and provide guidance for assessment of human and environmental health risk. We then investigate biochemical and molecular mechanisms of cytotoxicity that include oxidative stress-induced cellular events and alteration of the pathways …

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The Protective Effects Of Ferrostatin-1 (Fer-1) In Response To Excitotoxicity In Mouse Hippocampal Slices, Mireya Nael Ramirez Jan 2018

The Protective Effects Of Ferrostatin-1 (Fer-1) In Response To Excitotoxicity In Mouse Hippocampal Slices, Mireya Nael Ramirez

Open Access Theses & Dissertations

The development of different neurological disorders has been associated with the accumulation of reactive oxygen species (ROS). Elevated ROS levels can disrupt the neuronal electrical activity. This phenomenon has been seen during epilepsy and neurodegenerative diseases like Parkinson's disease. Furthermore, the excess of ROS and development of such disorders have been linked to neuronal cell death partly due to excessive, non-physiological glutamate release. Ferroptosis is a recently defined iron-dependent cell death mechanism. Inducible by a small molecule called erastin, ferroptosis was first described in cancer cells. Erastin-induced ferroptosis differs from apoptosis, necrosis and autophagy, since it leads to different biochemical …

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Toxicological And Biopharmacological Investigations Of Tiger Milk Mushroom-Lignosus Tigris / Kong Boon Hong, Boon Hong Kong Jan 2018

Toxicological And Biopharmacological Investigations Of Tiger Milk Mushroom-Lignosus Tigris / Kong Boon Hong, Boon Hong Kong

Student Works (2010-2019)

The traditional use for the sclerotium of Tiger Milk mushroom (Lignosus spp.) by local Malaysian natives as a cure for a variety of illnesses has been well documented and scientifically validated. Lignosus tigris C.S. Tan, a species of the Tiger Milk mushroom, has been identified recently and successfully cultivated. In the present study, the potential toxicity of the cultivated L. tigris E sclerotia was evaluated using Sprague Dawley (SD) rats in 14-day acute and 28-day sub-acute toxicity studies. Acute toxicity study showed that the sclerotial powder at a single dose of 2000 mg/kg did not cause adverse effects on growth …

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Cytotoxicity, Antimicrobial And Antioxidant Activities Of Boletus Bicolor, A Basidiomycetes Mushroom Indigenous To Tanzania, Donatha Tibuhwa Dec 2017

Cytotoxicity, Antimicrobial And Antioxidant Activities Of Boletus Bicolor, A Basidiomycetes Mushroom Indigenous To Tanzania, Donatha Tibuhwa

Tanzania Journal of Science

Boletus bicolor commonly known as coloured bolete is a basidiomyctes mushroom species widely used as a delicacy and its extract has been used traditionally to treat several human ailments in Tanzania. This study evaluates its extracts in order to provide a scientific foundation on the possible application in folk medicine system based on the biochemical evaluation. Standard microbes Bacillus subtilis and Candida albicans were used to test, the antifungal and antibacterial activity.  Cytotoxicity test was also done on the extracts using brine shrimp test. Besides, the extracts were also used to investigate for antioxidant activity using DPPH  (1, 1-diphenyl-2-picrylhydrazyl radical). …

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