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Articles 61 - 75 of 75
Full-Text Articles in Pharmacology, Toxicology and Environmental Health
Comparison Of Subcellular Responses For The Evaluation And Prediction Of The Chemotherapeutic Response To Cisplatin In Lung Adenocarcinoma Using Raman Spectroscopy, Haq Nawaz, Franck Bonnier, Aidan Meade, Fiona Lyng, Hugh Byrne
Comparison Of Subcellular Responses For The Evaluation And Prediction Of The Chemotherapeutic Response To Cisplatin In Lung Adenocarcinoma Using Raman Spectroscopy, Haq Nawaz, Franck Bonnier, Aidan Meade, Fiona Lyng, Hugh Byrne
Articles
Confocal Raman Micro spectroscopy (CRM) is employed to examine the chemical and physiological effects of anticancer agents, using cisplatin and A549 adenocarcinoma cells as a model compound and test system respectively. Spectral responses of the membrane and cytoplasm of the cell are analysed independently and the results are compared to previously reported spectroscopic studies of the nucleus. Moreover, Raman spectra from the proteins extracted from the control and exposed samples are acquired and analysed to confirm the origin of the molecular changes of the cell membrane and cytoplasm of the A549 cells. Multivariate data analysis techniques including Principal Component Analysis …
Synthesis, Evaluation And Structural Studies Of Antiproliferative Tubulin-Targeting Azetidin-2-Ones, Niamh O'Boyle, Lisa M. Greene, Orla Bergin, Jean-Baptiste Fichet, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Synthesis, Evaluation And Structural Studies Of Antiproliferative Tubulin-Targeting Azetidin-2-Ones, Niamh O'Boyle, Lisa M. Greene, Orla Bergin, Jean-Baptiste Fichet, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Articles
A series of azetidin-2-ones substituted at positions 2, 3 and 4 of the azetidinone ring scaffold were synthesised and evaluated for antiproliferative, cytotoxic and tubulin binding activity. In these compounds, the cis double bond of the vascular targeting agent combretastatin A-4 is replaced with the azetidinone ring in order to enhance the antiproliferative effects displayed by combretastatin A-4 and prevent the cis/trans isomerization that is associated with inactivation of combretastatin A-4. The series of azetidinones was synthetically accessible via the Staudinger and Reformatsky reactions. Of a diverse range of heterocyclic derivatives, 3-(2-thienyl) analogue 28 and 3-(3-thienyl) analogue 29 displayed the …
Lead Identification Of Β-Lactam And Related Imine Inhibitors Of The Molecular Caperone Heat Shock Protein 90, Niamh O'Boyle, Andrew Js Knox, Trevor P. Price, D. Clive Williams, Daniela M. Zisterer, David G. Lloyd, Mary J. Meegan
Lead Identification Of Β-Lactam And Related Imine Inhibitors Of The Molecular Caperone Heat Shock Protein 90, Niamh O'Boyle, Andrew Js Knox, Trevor P. Price, D. Clive Williams, Daniela M. Zisterer, David G. Lloyd, Mary J. Meegan
Articles
Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical trials and represent a new and exciting area in the treatment of cancer. Heat shock protein 90 inhibitors have huge structural diversity, and here we present the identification of inhibitors based on β-lactam and imine templates. β-Lactam 5 and imines 12 and 18 exhibit binding to heat shock protein 90-α with IC50 values of 5.6 μM, 14.5 μM and 22.1 μM respectively. The binding affinity displayed …
Synthesis, Biochemical And Molecular Modelling Studies Of Antiproliferative Azetidinones Causing Microtubule Disruption And Mitotic Catastrophe, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Niall O. Keely, Andrew Js Knox, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Synthesis, Biochemical And Molecular Modelling Studies Of Antiproliferative Azetidinones Causing Microtubule Disruption And Mitotic Catastrophe, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Niall O. Keely, Andrew Js Knox, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Articles
The structure-activity relationships of antiproliferative β-lactams, focusing on modifications at the 4-position of the β-lactam ring, is described. Synthesis of this series of compounds was achieved utilizing the Staudinger and Reformatsky reactions. The antiproliferative activity was assessed in MCF-7 cells, where the 4-(4-ethoxy)phenyl substituted compound 26 displayed the most potent activity with an IC50 value of 0.22 μM. The mechanism of action was demonstrated to be by inhibition of tubulin. Cell exposure to combretastatin A-4 and 26 led to arrest of MCF-7 cells in the G2/M phase of the cell cycle and induction of apoptosis. Additionally, mitotic catastrophe for …
Anticancer And Antifungal Activity Of Copper(Ii) Complexes Of Quinolin-2(1h)-One-Derived Schiff Bases, Bernadette S. Creaven, Brian Duff, Denise A. Egan, Kevin Kavanagh, Georgina Rosair, Venkat Reddy Thangella, Maureen Walsh
Anticancer And Antifungal Activity Of Copper(Ii) Complexes Of Quinolin-2(1h)-One-Derived Schiff Bases, Bernadette S. Creaven, Brian Duff, Denise A. Egan, Kevin Kavanagh, Georgina Rosair, Venkat Reddy Thangella, Maureen Walsh
Articles
The condensation of substituted aromatic aldehydes with 7-amino-4-methyl-quinolin-2(1H)-one (1) has lead to the isolation of quinolin-2(1H)-one derived Schiff bases (2–14). The copper(II) complexes (2a–14a) of the ligands were also prepared, and together with their corresponding free ligands were fully characterised by elemental analyses, spectral methods (IR, 1H and 13C NMR, AAS, UV–Vis), magnetic and conductance measurements. The bidentate ligands coordinated to the copper(II) ion through the deprotonated phenolic oxygen and the azomethine nitrogen of the ligands in almost all cases. X-ray crystal structures of two of the complexes, 5a and 8a, confirmed the bidentate …
Synthesis And Evaluation Of Azetidinone Analogues Of Combretastatin A-4 As Tubulin Targeting Agents, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Orla Bergin, Seema M. Nathwani, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Synthesis And Evaluation Of Azetidinone Analogues Of Combretastatin A-4 As Tubulin Targeting Agents, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Orla Bergin, Seema M. Nathwani, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan
Articles
The synthesis and antiproliferative activity of a new series of rigid analogues of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (β-lactam) ring system in place of the usual ethylene bridge present in the natural combretastatin stilbene products. These novel compounds are also substituted at position 3 of the β-lactam ring with an aryl ring. A number of analogues showed potent nanomolar activity in human MCF-7 and MDA-MB-231 breast cancer cell lines, displayed in vitro inhibition of tubulin polymerization and did not cause significant cytotoxicity in normal murine breast epithelial cells. 4-(4-Methoxyaryl)-substituted compound 32, 4-(3-hydroxy-4-methoxyaryl)-substituted compounds 35 and 41 and …
Copper(Ii) Complexes Of Coumarin-Derived Schiff Bases And Their Anti-Candida Activity, Bernadette S. Creaven, Michael Devereux, Dariusz Karcz, Andrew Kellett, Malachy Mccann, Andy Noble, Maureen Walsh
Copper(Ii) Complexes Of Coumarin-Derived Schiff Bases And Their Anti-Candida Activity, Bernadette S. Creaven, Michael Devereux, Dariusz Karcz, Andrew Kellett, Malachy Mccann, Andy Noble, Maureen Walsh
Articles
The condensation of 7-amino-4-methyl-coumarin (1) with a number of substituted salicylaldehydes yielded a series of Schiff bases (2a–2k) in good yields. Subsequent reaction of these ligands with copper( II) acetate yielded Cu(II) complexes (3a–3k) and some were characterised using X-ray crystallography. All of the free ligands and their metal complexes were tested for their anti-Candida activity.
Preparation, Characterization And Ecotoxicological Evaluation Of Four Environmentally Relevant Species Of N-Isopropylacrylamide And N-Isopropylacrylamide-Co-N-Tert-Butylacrylamide Copolymer Nanoparticles, Pratap Naha, Alan Casey, Tiziana Tenuta, Iseult Lynch, Kenneth Dawson, Hugh Byrne, Maria Davoren
Preparation, Characterization And Ecotoxicological Evaluation Of Four Environmentally Relevant Species Of N-Isopropylacrylamide And N-Isopropylacrylamide-Co-N-Tert-Butylacrylamide Copolymer Nanoparticles, Pratap Naha, Alan Casey, Tiziana Tenuta, Iseult Lynch, Kenneth Dawson, Hugh Byrne, Maria Davoren
Articles
Poly N-isopropylacrylamide and N-isopropylacrylamide / N-tert-butylacrylamide copolymer nanoparticles of 50 to 70 nm were prepared by free radical polymerisation. The particle sizes of the copolymer nanoparticles were measured in the test media Milli-Q water, Algae Media, Daphnia Media and Microtox Diluent as a function of temperature. Whereas in Milli-Q water the particle size was seen to decrease above the lower critical solution temperature of the thermoresponsive polymer, in the test media it was seen to increase significantly, indicative of aggregation. At the temperatures employed for the ecotoxicological studies all particles, with the exception of the 50:50 copolymer existed as nanoparticles, …
An Integrated Approach To The Toxicity Assessment Of Irish Marine Sediments Application Of Porewater Toxicity Identification Evaluation (Tie) To Irish Marine Sediments, Ailbhe Macken, Michelle Giltrap, Barry Foley, Evin Mcgovern, Brendan Mchugh, Maria Davoren
An Integrated Approach To The Toxicity Assessment Of Irish Marine Sediments Application Of Porewater Toxicity Identification Evaluation (Tie) To Irish Marine Sediments, Ailbhe Macken, Michelle Giltrap, Barry Foley, Evin Mcgovern, Brendan Mchugh, Maria Davoren
Articles
An integrated approach to the ecotoxicological assessment of Irish marine sediments was carried out between 2004 and 2007. Phase I Toxicity Identification Evaluation (TIE) of sediment porewaters from two sites on the east coast of Ireland were conducted. Initial Tier I screening of three Irish sites identified the need for TIE after significant toxicity was observed with Tisbe battagliai and the Microtox® assay at two of the assayed sites (Alexandra Basin and Dunmore East). Porewaters classified as toxic were characterised using four manipulations, ethylenediaminetetraacetic acid (EDTA) chelation, sodium thiosulphate addition, C18 Solid Phase Extraction (SPE) and Cation Exchange (CE) SPE. …
Reflection Contributions To The Dispersion Artefact In Ftir Spectra Of Single Biological Cells., Paul Bassan, Hugh Byrne, Joe Lee, Franck Bonnier, Colin Clarke, Paul Dumas, Ehsan Gazi, Michael Brown, Noel Clarke, Peter Gardner
Reflection Contributions To The Dispersion Artefact In Ftir Spectra Of Single Biological Cells., Paul Bassan, Hugh Byrne, Joe Lee, Franck Bonnier, Colin Clarke, Paul Dumas, Ehsan Gazi, Michael Brown, Noel Clarke, Peter Gardner
Articles
Fourier transform infrared spectra of a single cell in transflection geometry are seen to vary significantly with position on the cell, showing a distorted derivative-like lineshape in the region of the optically dense nucleus. A similar behaviour is observable in a model system of the protein albumin doped in a potassium bromide disk. It is demonstrated that the spectrum at any point is a weighted sum of the sample reflection and transmission and that the dominance of the reflection spectrum in optically dense regions can account for some of the spectral distortions previously attributed to dispersion artefacts. Rather than being …
Dispersion Medium Modulates Oxidative Stress Response Of Human Lung Epithelial Cells Upon Exposure To Carbon Nanomaterial Samples, Eva Herzog, Hugh Byrne, Maria Davoren, Alan Casey, Albert Duschl, Gertie Janneke Oostingh
Dispersion Medium Modulates Oxidative Stress Response Of Human Lung Epithelial Cells Upon Exposure To Carbon Nanomaterial Samples, Eva Herzog, Hugh Byrne, Maria Davoren, Alan Casey, Albert Duschl, Gertie Janneke Oostingh
Articles
Due to their large specific surface area, the potential of nanoparticles to be highly reactive and to induce oxidative stress is particularly high. In addition, some types of nanoparticles contain transition metals as trace impurities which are known to generate reactive oxygen species (ROS) in biological systems. This study investigates the potential of two types of single-walled carbon nanotube samples, nanoparticulate carbon black and crocidolite asbestos to induce ROS in lung epithelial cells in vitro. Carbon nanotube and carbon black samples were used as produced, without further purification or processing, in order to best mimic occupational exposure by inhalation of …
Raman Spectroscopy: A Potential Platform For The Rapid Measurement Of Carbon Nanotube-Induced Cytotoxicity, Peter Knief, Colin Clarke, Eva Herzog, Maria Davoren, Fiona Lyng, Aidan Meade, Hugh Byrne
Raman Spectroscopy: A Potential Platform For The Rapid Measurement Of Carbon Nanotube-Induced Cytotoxicity, Peter Knief, Colin Clarke, Eva Herzog, Maria Davoren, Fiona Lyng, Aidan Meade, Hugh Byrne
Articles
In this study the suitability of Raman spectroscopy for the determination of carbon nanotube mediated toxicity on human alveolar carcinoma epithelial cells (A549) is explored. The exposure of this cell line represents the primary pathway of exposure in humans, that of inhalation. Peak ratio analysis demonstrates a dose dependent response which correlates to previous toxicological studies. Principal component analysis is employed to further classify cellular response as a function of dose and to examine differences between spectra as a function of exposed concentration. To further illustrate the potential of Raman spectroscopy in this field, Partial Least Squares (PLS) regression and …
First Approaches To Standard Protocols And Reference Materials For The Assessment Of Potential Hazards Associated With Nanomaterialss, Gordon Chambers, Hugh Byrne, Iseult Lynch, Micheal Riediker, Hans Bouwmeester, Hans Marvin, Alan Casey, Markus Berges, Martin Clift, Teresa Fernandez, Lise Fjellsbo, Lucienne Juillerat, Gert Roebben, Christoph, Klein, Qinglan Wu, Vince Hackley, Jean-Pierre Kaiser, Wolfganag Kreyling, Michael Garner, Peter Hatto,, Kenneth Dawson
First Approaches To Standard Protocols And Reference Materials For The Assessment Of Potential Hazards Associated With Nanomaterialss, Gordon Chambers, Hugh Byrne, Iseult Lynch, Micheal Riediker, Hans Bouwmeester, Hans Marvin, Alan Casey, Markus Berges, Martin Clift, Teresa Fernandez, Lise Fjellsbo, Lucienne Juillerat, Gert Roebben, Christoph, Klein, Qinglan Wu, Vince Hackley, Jean-Pierre Kaiser, Wolfganag Kreyling, Michael Garner, Peter Hatto,, Kenneth Dawson
Articles
All new technologies have an inherent risk, which is typically assessed alongside the development of applications of the technology. This is also the case for nanotechnology: a key concern in the case of engineered nanomaterials (ENMs) is that due to their very small size, NMs can reach areas such as the cell that are inaccessible to other materials, such as implants and drugs. As a result of their large surface area, NMs may be more reactive than other larger materials. The large physical and chemical variability of NMs, and the fact that small changes can have large consequences, mean that …
A Model Compound Study: The Ecotoxicological Evaluation Of Five Organic Contaminants With A Battery Of Marine Bioassays, Ailbhe Macken, Michelle Giltrap, Barry Foley, Evin Mcgovern, Brendan Mchugh, Maria Davoren
A Model Compound Study: The Ecotoxicological Evaluation Of Five Organic Contaminants With A Battery Of Marine Bioassays, Ailbhe Macken, Michelle Giltrap, Barry Foley, Evin Mcgovern, Brendan Mchugh, Maria Davoren
Articles
This paper describes the ecotoxicological evaluation of five organic contaminants frequently detected in marine sediments (tributyltin, triphenyltin, benzo[a]pyrene, fluoranthene, and PCB 153) using three marine species (Vibrio fischeri, Tetraselmis suecica, and Tisbe battagliai). The sensitivity of each species varied for all compounds. The triorganotins were consistently the most toxic to all species. The applicability of each test system to assess the acute toxicity of environmental contaminants and their use in Toxicity Identification Evaluation (TIE) is discussed. Suitability of the Microtox and T. battagliai tests for employment in TIE studies were further assessed through spiking experiments with tributyltin. Results demonstrated that …
The Involvement Of Calcium And Map Kinase Signaling Pathways In The Production Of Radiation-Induced Bystander Effects, Fiona Lyng, Paula Maguire, B. Mcclean, C. Seymour, Carmel Mothersill
The Involvement Of Calcium And Map Kinase Signaling Pathways In The Production Of Radiation-Induced Bystander Effects, Fiona Lyng, Paula Maguire, B. Mcclean, C. Seymour, Carmel Mothersill
Articles
Much evidence now exists regarding radiation-induced bystander effects, but the mechanisms involved in the transduction of the signal are still unclear. The mitogen-activated protein kinase (MAPK) pathways have been linked to growth factor-mediated regulation of cellular events such as proliferation, senescence, differentiation and apoptosis. Activation of multiple MAPK pathways such as the ERK, JNK and p38 pathways have been shown to occur after exposure of cells to radiation and a variety of other toxic stresses. Previous studies have shown oxidative stress and calcium signaling to be important in radiation-induced bystander effects. The aim of the present study was to investigate …