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Full-Text Articles in Social and Behavioral Sciences
C-Amp Dependent Protein Kinase A Inhibitory Activity Of Six Algal Extracts From South Eastern Australia And Their Fatty Acid Composition, Ana Zivanovic, Danielle Skropeta
C-Amp Dependent Protein Kinase A Inhibitory Activity Of Six Algal Extracts From South Eastern Australia And Their Fatty Acid Composition, Ana Zivanovic, Danielle Skropeta
Danielle Skropeta
c-AMP dependent protein kinase (protein kinase A, PKA) is an important enzyme involved in the regulation of an increasing number of physiological processes including immune function, cardiovascular disease, memory disorders and cancer. The objective of this study was to evaluate the PKA inhibitory activity of a range of algal extracts, along with their fatty acid composition. Six algal species were investigated including two Chlorophyta (Codium dimorphum and Ulva lactuca), two Phaeophyta (Phyllospora comosa and Sargassum sp.) and two Rhodophyta (Prionitis linearis and Corallina vancouveriensis), with the order of PKA inhibitory activity of their extracts identified as follows: brown seaweeds > red …
Removal Of Trace Organic Contaminants By Nitrifying Activated Sludge And Whole-Cell And Crude Enzyme Extract Of Trametes Versicolor, Shufan Yang, Faisal I. Hai, Long D. Nghiem, Felicity Roddick, William E. Price
Removal Of Trace Organic Contaminants By Nitrifying Activated Sludge And Whole-Cell And Crude Enzyme Extract Of Trametes Versicolor, Shufan Yang, Faisal I. Hai, Long D. Nghiem, Felicity Roddick, William E. Price
William E. Price
The resistance of certain anthropogenic trace organic contaminants (TrOCs) to conventional wastewater treatment and their potential adverse effects on human and ecological health raise significant concerns and have prompted research on their bioremediation by white-rot fungi. This study compared the removal efficiencies of four widespread TrOCs: carbamazepine (CBZ), sulfamethoxazole (SMX), bisphenol A (BPA) and diclofenac (DCF), by nitrifying activated sludge as well as whole-cell and extracellular enzyme (laccase) extract of the white-rot fungus Trametes versicolor. Fungal whole-cell culture removed only BPA and DCF but with high efficiencies (>90%) while the mixed nitrifying culture removed all compounds, although by levels …
An Assessment Of The Bhutanese Traditional Medicine For Its Ethnopharmacology, Ethnobotany And Ethnoquality: Textual Understanding And The Current Practices, Phurpa Wangchuk, Stephen G. Pyne, Paul A. Keller
An Assessment Of The Bhutanese Traditional Medicine For Its Ethnopharmacology, Ethnobotany And Ethnoquality: Textual Understanding And The Current Practices, Phurpa Wangchuk, Stephen G. Pyne, Paul A. Keller
Paul Keller
Ethnopharmacological relevance : This study involves the assessment of the Bhutanese traditional medicine (BTM) which was integrated with the mainstream biomedicine in 1967 to provide primary health care services in the country. It caters to 20-30% of the daily out-patients within 49 traditional medicine units attached to 20 district modern hospitals and 29 Basic Health Units in the country. Aim of the study : This study presents the ethnopharmacological, ethnobotanical and the ethnoquality concepts in relation to mainstream Tibetan medicine and describes the current practices of BTM. Materials and methods : Experienced BTM practitioners (Drung-tshos and Smen-pas) were selected using …
Bacterial Filtration Using Carbon Nanotube/Antibiotic Buckypaper Membranes, Luke J. Sweetman, Leighton J. Alcock, Jason D. Mcarthur, Elise M. Stewart, Gerry Triani, Marc In Het Panhuis, Stephen F. Ralph
Bacterial Filtration Using Carbon Nanotube/Antibiotic Buckypaper Membranes, Luke J. Sweetman, Leighton J. Alcock, Jason D. Mcarthur, Elise M. Stewart, Gerry Triani, Marc In Het Panhuis, Stephen F. Ralph
Luke Sweetman
The preparation of free-standing carbon nanotube “buckypaper” (BP) membranes consisting of either single-walled carbon nanotubes (SWNTs) or multi-walled carbon nanotubes (MWNTs), and the antibiotic ciprofloxacin (cipro), is reported. The electrical, mechanical and morphological properties of these membranes have been characterised and are compared to those of the corresponding buckypaper membranes containing the surfactant Triton X-100 (Trix). Analysis of scanning electron microscopic images of the surfaces of SWNT/cipro and SWNT/Trix (Trix = Triton X-100) buckypapers revealed that the diameter of their surface pores was significantly smaller than that of the corresponding materials prepared using MWNTs. Similarly, the average internal pore diameter …
Rapid Differentiation Of Isomeric Lipids By Photodissociation Mass Spectrometry Of Fatty Acid Derivatives, Huong T. Pham, Adam J. Trevitt, Todd W. Mitchell, Stephen J. Blanksby
Rapid Differentiation Of Isomeric Lipids By Photodissociation Mass Spectrometry Of Fatty Acid Derivatives, Huong T. Pham, Adam J. Trevitt, Todd W. Mitchell, Stephen J. Blanksby
Adam Trevitt
RATIONALE Both traditional electron ionization and electrospray ionization tandem mass spectrometry have demonstrated limitations in the unambiguous identification of fatty acids. In the former case, high electron energies lead to extensive dissociation of the radical cations from which little specific structural information can be obtained. In the latter, conventional collision-induced dissociation (CID) of even-electron ions provides little intra-chain fragmentation and thus few structural diagnostics. New approaches that harness the desirable features of both methods, namely radical-driven dissociation with discrete energy deposition, are thus required. METHODS Herein we describe the derivatization of a structurally diverse suite of fatty acids as 4-iodobenzyl …
Escherichia Coli Single-Stranded Dna-Binding Protein: Nanoesi-Ms Studies Of Salt-Modulated Subunit Exchange And Dna Binding Transactions, Claire E. Mason, Slobodan Jergic, Allen Lo, Yao Wang, Nicholas E. Dixon, Jennifer L. Beck
Escherichia Coli Single-Stranded Dna-Binding Protein: Nanoesi-Ms Studies Of Salt-Modulated Subunit Exchange And Dna Binding Transactions, Claire E. Mason, Slobodan Jergic, Allen Lo, Yao Wang, Nicholas E. Dixon, Jennifer L. Beck
Professor Nick E Dixon
Single-stranded DNA-binding proteins (SSBs) are ubiquitous oligomeric proteins that bind with very high affinity to single-stranded DNA and have a variety of essential roles in DNA metabolism. Nanoelectrospray ionization mass spectrometry (nanoESI-MS) was used to monitor subunit exchange in full-length and truncated forms of the homotetrameric SSB from Escherichia coli. Subunit exchange in the native protein was found to occur slowly over a period of hours, but was significantly more rapid in a truncated variant of SSB from which the eight C-terminal residues were deleted. This effect is proposed to result from C-terminus mediated stabilization of the SSB tetramer, in …
Characterization Of Cleavage Events In The Multifunctional Cilium Adhesin Mhp684 (P146) Reveals A Mechanism By Which Mycoplasma Hyopneumoniae Regulates Surface Topography, Daniel Bogema, Ania T. Deutscher, Lauren K. Woolley, Lisa M. Seymour, Benjamin B. A Raymond, Jessica L. Tacchi, Matthew P. Padula, Nicholas E. Dixon, F Chris Minion, Cheryl Jenkins, Mark J. Walker, Steven P. Djordjevic
Characterization Of Cleavage Events In The Multifunctional Cilium Adhesin Mhp684 (P146) Reveals A Mechanism By Which Mycoplasma Hyopneumoniae Regulates Surface Topography, Daniel Bogema, Ania T. Deutscher, Lauren K. Woolley, Lisa M. Seymour, Benjamin B. A Raymond, Jessica L. Tacchi, Matthew P. Padula, Nicholas E. Dixon, F Chris Minion, Cheryl Jenkins, Mark J. Walker, Steven P. Djordjevic
Professor Nick E Dixon
Mycoplasma hyopneumoniae causes enormous economic losses to swine production worldwide by colonizing the ciliated epithelium in the porcine respiratory tract, resulting in widespread damage to the mucociliary escalator, prolonged inflammation, reduced weight gain, and secondary infections. Protein Mhp684 (P146) comprises 1,317 amino acids, and while the N-terminal 400 residues display significant sequence identity to the archetype cilium adhesin P97, the remainder of the molecule is novel and displays unusual motifs. Proteome analysis shows that P146 preprotein is endogenously cleaved into three major fragments identified here as P50P146, P40P146, and P85P146 that reside on the cell surface. Liquid chromatography with tandem …
Structure Of The Theta Subunit Of Escherichia Coli Dna Polymerase Iii In Complex With The Epsilon Subunit, Max A Keniry, Ah-Young Park, Elisabeth A. Owen, Samir M. Hamdan, Guido Pintacuda, Gottfried Otting, Nicholas E. Dixon
Structure Of The Theta Subunit Of Escherichia Coli Dna Polymerase Iii In Complex With The Epsilon Subunit, Max A Keniry, Ah-Young Park, Elisabeth A. Owen, Samir M. Hamdan, Guido Pintacuda, Gottfried Otting, Nicholas E. Dixon
Professor Nick E Dixon
The catalytic core of Escherichia coli DNA polymerase III contains three tightly associated subunits, the α, ε, and θ subunits. The θ subunit is the smallest and least understood subunit. The three-dimensional structure of θ in a complex with the unlabeled N-terminal domain of the ε subunit, ε186, was determined by multidimensional nuclear magnetic resonance spectroscopy. The structure was refined using pseudocontact shifts that resulted from inserting a lanthanide ion (Dy3+, Er3+, or Ho3+) at the active site of ε186. The structure determination revealed a three-helix bundle fold that is similar to the solution structures of θ in a methanol-water …
Replication Termination In Escherichia Coli: Structure And Anti-Helicase Activity Of The Tus-Ter Complex, Cameron Neylon, Andrew V. Kralicek, Thomas M. Hill, Nicholas E. Dixon
Replication Termination In Escherichia Coli: Structure And Anti-Helicase Activity Of The Tus-Ter Complex, Cameron Neylon, Andrew V. Kralicek, Thomas M. Hill, Nicholas E. Dixon
Professor Nick E Dixon
The arrest of DNA replication in Escherichia coli is triggered by the encounter of a replisome with a Tus protein-Ter DNA complex. A replication fork can pass through a Tus-Ter complex when traveling in one direction but not the other, and the chromosomal Ter sites are oriented so replication forks can enter, but not exit, the terminus region. The Tus-Ter complex acts by blocking the action of the replicative DnaB helicase, but details of the mechanism are uncertain. One proposed mechanism involves a specific interaction between Tus-Ter and the helicase that prevents further DNA unwinding, while another is that the …
Proofreading Exonuclease On A Tether: The Complex Between The E. Coli Dna Polymerase Iii Subunits Α, Ε, Θ And Β Reveals A Highly Flexible Arrangement Of The Proofreading Domain, Kiyoshi Ozawa, Nicholas P. Horan, Andrew Robinson, Hiromasa Yagi, Flynn R. Hill, Slobodan Jergic, Zhi-Qiang Xu, Karin V. Loscha, Nan Li, Moeava Tehei, Aaron J. Oakley, Gottfried Otting, Thomas Huber, Nicholas E. Dixon
Proofreading Exonuclease On A Tether: The Complex Between The E. Coli Dna Polymerase Iii Subunits Α, Ε, Θ And Β Reveals A Highly Flexible Arrangement Of The Proofreading Domain, Kiyoshi Ozawa, Nicholas P. Horan, Andrew Robinson, Hiromasa Yagi, Flynn R. Hill, Slobodan Jergic, Zhi-Qiang Xu, Karin V. Loscha, Nan Li, Moeava Tehei, Aaron J. Oakley, Gottfried Otting, Thomas Huber, Nicholas E. Dixon
Professor Nick E Dixon
A complex of the three (αεθ) core subunits and the β2 sliding clamp is responsible for DNA synthesis by Pol III, the Escherichia coli chromosomal DNA replicase. The 1.7 Å crystal structure of a complex between the PHP domain of α (polymerase) and the C-terminal segment of ε (proofreading exonuclease) subunits shows that ε is attached to α at a site far from the polymerase active site. Both α and ε contain clamp-binding motifs (CBMs) that interact simultaneously with β2 in the polymerization mode of DNA replication by Pol III. Strengthening of both CBMs enables isolation of stable αεθ:β2 complexes. …
Flexibility Revealed By The 1.85 Å Crystal Structure Of The Β Sliding-Clamp Subunit Of Escherichia Coli Dna Polymerase Iii, Aaron J. Oakley, Pavel Prosselkov, Gene Wijffels, Jennifer L. Beck, Matthew Cj Wilce, Nicholas E. Dixon
Flexibility Revealed By The 1.85 Å Crystal Structure Of The Β Sliding-Clamp Subunit Of Escherichia Coli Dna Polymerase Iii, Aaron J. Oakley, Pavel Prosselkov, Gene Wijffels, Jennifer L. Beck, Matthew Cj Wilce, Nicholas E. Dixon
Professor Nick E Dixon
The subunit of the Escherichia coli replicative DNA polymerase III holoenzyme is the sliding clamp that interacts with the (polymerase) subunit to maintain the high processivity of the enzyme. The protein is a ring-shaped dimer of 40.6 kDa subunits whose structure has previously been determined at a resolution of 2.5 Å [Kong et al. (1992), Cell, 69, 425-437]. Here, the construction of a new plasmid that directs overproduction of to very high levels and a simple procedure for large-scale purification of the protein are described. Crystals grown under slightly modified conditions diffracted to beyond 1.9 Å at 100 K at …
Rapid Cascade Synthesis Of Poly-Heterocyclic Architectures From Indigo, Alireza Shakoori Ghasabi, John Bremner, Anthony C. Willis, Rachada Haritakun, Paul A. Keller
Rapid Cascade Synthesis Of Poly-Heterocyclic Architectures From Indigo, Alireza Shakoori Ghasabi, John Bremner, Anthony C. Willis, Rachada Haritakun, Paul A. Keller
Faculty of Science, Medicine and Health - Papers: part A
The base-induced propargylation of the dye indigo results in the rapid and unprecedented one-pot synthesis of highly functionalized representatives of the pyrazino[1,2-a:4,3-a′]diindole, pyrido[1,2-a:3,4-b′]diindole and benzo[b]indolo[1,2-h]naphthyridine heterocyclic systems, with the last two reflecting the core skeleton of the anticancer/antiplasmodial marine natural products fascaplysin and homofascaplysins and a ring B-homologue, respectively. The polycyclic compounds 6–8, whose structures were confirmed through single-crystal X-ray crystallographic analysis, arise from sequential inter/intramolecular substitution–addition reactions, and in some cases, ring rearrangement reactions. Preliminary studies on controlling the reaction path selectivity, and the potential reaction mechanisms, are also described. Initial biological activity studies with these new heterocyclic derivatives …
Extracellular Chaperones, Rebecca A. Dabbs, Amy R. Wyatt, Justin J. Yerbury, Heath Ecroyd, Mark R. Wilson
Extracellular Chaperones, Rebecca A. Dabbs, Amy R. Wyatt, Justin J. Yerbury, Heath Ecroyd, Mark R. Wilson
Mark R Wilson
The maintenance of the levels and correct folding state of proteins (proteostasis) is a fundamental prerequisite for life. Life has evolved complex mechanisms to maintain proteostasis and many of these that operate inside cells are now well understood. The same cannot yet be said of corresponding processes in extracellular fluids of the human body, where inappropriate protein aggregation is known to underpin many serious diseases such as Alzheimer's disease, type II diabetes and prion diseases. Recent research has uncovered a growing family of abundant extracellular chaperones in body fluids which appear to selectively bind to exposed regions of hydrophobicity on …
Single Molecule Characterization Of The Interactions Between Amyloid-Β Peptides And The Membranes Of Hippocampal Cells, Priyanka Narayan, Kristina A. Ganzinger, James Mccoll, Laura Weimann, Sarah Meehan, Seema Qamar, John A. Carver, Mark R. Wilson, Peter St George-Hyslop, Christopher M. Dobson, David Klenerman
Single Molecule Characterization Of The Interactions Between Amyloid-Β Peptides And The Membranes Of Hippocampal Cells, Priyanka Narayan, Kristina A. Ganzinger, James Mccoll, Laura Weimann, Sarah Meehan, Seema Qamar, John A. Carver, Mark R. Wilson, Peter St George-Hyslop, Christopher M. Dobson, David Klenerman
Mark R Wilson
Oligomers of the 40 and 42 residue amyloid-β peptides (Aβ40 and Aβ42) have been implicated in the neuronal damage and impaired cognitive function associated with Alzheimer’s disease. However, little is known about the specific mechanisms by which these misfolded species induce such detrimental effects on cells. In this work, we use single-molecule imaging techniques to examine the initial interactions between Aβ monomers and oligomers and the membranes of live cells. This highly sensitive method enables the visualization of individual Aβ species on the cell surface and characterization of their oligomerization state, all at biologically relevant, nanomolar concentrations. The results indicate …
Concise Synthesis Of (-)-Steviamine And Analogues And Their Glycosidase Inhibitory Activities, Nadechanok Jiangseubchatveera, Marc E. Bouillon, Boonsom Liawruangrath, Saisunee Liawruangrath, Robert J. Nash, Stephen G. Pyne
Concise Synthesis Of (-)-Steviamine And Analogues And Their Glycosidase Inhibitory Activities, Nadechanok Jiangseubchatveera, Marc E. Bouillon, Boonsom Liawruangrath, Saisunee Liawruangrath, Robert J. Nash, Stephen G. Pyne
Faculty of Science, Medicine and Health - Papers: part A
A concise synthesis of (−)-steviamine is reported along with the synthesis of its analogues 10-nor-steviamine, 10-nor-ent-steviamine and 5-epi-ent-steviamine. These compounds were tested against twelve glycosidases (at 143 μg mL−1 concentrations) and were found to have in general poor inhibitory activity against most enzymes. The 10-nor analogues however, showed 50–54% inhibition of α-L-rhamnosidase from Penicillium decumbens while one of these, 10-nor-steviamine, showed 51% inhibition of N-acetyl-β-D-glucosaminidase (from Jack bean) at the same concentration (760 μM).
Novel Olanzapine Analogues Presenting A Reduced H1 Receptor Affinity And Retained 5ht2a/D2 Binding Affinity Ratio, Somayeh Jafari, Marc E. Bouillon, Xu-Feng Huang, Stephen G. Pyne, Francesca Fernandez-Enright
Novel Olanzapine Analogues Presenting A Reduced H1 Receptor Affinity And Retained 5ht2a/D2 Binding Affinity Ratio, Somayeh Jafari, Marc E. Bouillon, Xu-Feng Huang, Stephen G. Pyne, Francesca Fernandez-Enright
Xu-Feng Huang
Background Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H1) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT2A/D2) receptor binding affinity ratios. Results We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT2A, D2, and H1 receptors. Conclusions …
Neuregulin-1 Signalling And Antipsychotic Treatment: Potential Therapeutic Targets In A Schizophrenia Candidate Signalling Pathway, Chao Deng, Bo Pan, Martin Engel, Xu-Feng Huang
Neuregulin-1 Signalling And Antipsychotic Treatment: Potential Therapeutic Targets In A Schizophrenia Candidate Signalling Pathway, Chao Deng, Bo Pan, Martin Engel, Xu-Feng Huang
Xu-Feng Huang
Identifying the signalling pathways underlying the pathophysiology of schizophrenia is an essential step in the rational development of new antipsychotic drugs for this devastating disease. Evidence from genetic, transgenic and post-mortem studies have strongly supported neuregulin-1 (NRG1)-ErbB4 signalling as a schizophrenia susceptibility pathway. NRG1-ErbB4 signalling plays crucial roles in regulating neurodevelopment and neurotransmission, with implications for the pathophysiology of schizophrenia. Post-mortem studies have demonstrated altered NRG1-ErbB4 signalling in the brain of schizophrenia patients. Antipsychotic drugs have different effects on NRG1-ErbB4 signalling depending on treatment duration. Abnormal behaviours relevant to certain features of schizophrenia are displayed in NRG1/ErbB4 knockout mice or …
Increases In Peptide Y-Y Levels Following Oat Β-Glucan Ingestion Are Dose-Dependent In Overweight Adults, Eleanor J. Beck, Linda C. Tapsell, Marijka J. Batterham, Susan M. Tosh, Xu-Feng Huang
Increases In Peptide Y-Y Levels Following Oat Β-Glucan Ingestion Are Dose-Dependent In Overweight Adults, Eleanor J. Beck, Linda C. Tapsell, Marijka J. Batterham, Susan M. Tosh, Xu-Feng Huang
Xu-Feng Huang
Peptide Y-Y (PYY) is an anorexigenic hormone implicated in appetite control, and β-glucan is a fiber known to affect appetite. We hypothesized that plasma PYY levels would increase in overweight human adults consuming increasing doses of β-glucan. The objective was to test whether the effect could be seen with β-glucan delivered through extruded cereals containing a high β-glucan oat bran with demonstrated high molecular weight and solubility. Fourteen subjects consumed a control meal and 3 cereals of varying β-glucan concentration (between 2.2 and 5.5 g), and blood samples were collected over 4 hours. Analysis of raw PYY data showed a …
Oat Β-Glucan Supplementation Does Not Enhance The Effectiveness Of An Energy-Restricted Diet In Overweight Women, Eleanor J. Beck, Linda C. Tapsell, Marijka J. Batterham, Susan M. Tosh, Xu-Feng Huang
Oat Β-Glucan Supplementation Does Not Enhance The Effectiveness Of An Energy-Restricted Diet In Overweight Women, Eleanor J. Beck, Linda C. Tapsell, Marijka J. Batterham, Susan M. Tosh, Xu-Feng Huang
Xu-Feng Huang
Epidemiological evidence shows an inverse relationship between dietary fibre intake and body weight gain. Oat β-glucan, a soluble fibre alters appetite hormones and subjective satiety in acute meal test studies, but its effects have not been demonstrated with chronic consumption. The present study aimed to test the effects in women of two different doses of oat β-glucan on weight loss and hormones associated with appetite regulation. In a 3-month parallel trial, sixty-six overweight females were randomised into one of three 2 MJ energy-deficit diets: a control and two interventions including 5–6 g or 8–9 g β-glucan. Anthropometric and metabolic variables …
Single Molecule Characterization Of The Interactions Between Amyloid-Β Peptides And The Membranes Of Hippocampal Cells, Priyanka Narayan, Kristina A. Ganzinger, James Mccoll, Laura Weimann, Sarah Meehan, Seema Qamar, John A. Carver, Mark R. Wilson, Peter St George-Hyslop, Christopher M. Dobson, David Klenerman
Single Molecule Characterization Of The Interactions Between Amyloid-Β Peptides And The Membranes Of Hippocampal Cells, Priyanka Narayan, Kristina A. Ganzinger, James Mccoll, Laura Weimann, Sarah Meehan, Seema Qamar, John A. Carver, Mark R. Wilson, Peter St George-Hyslop, Christopher M. Dobson, David Klenerman
Faculty of Science, Medicine and Health - Papers: part A
Oligomers of the 40 and 42 residue amyloid-β peptides (Aβ40 and Aβ42) have been implicated in the neuronal damage and impaired cognitive function associated with Alzheimer’s disease. However, little is known about the specific mechanisms by which these misfolded species induce such detrimental effects on cells. In this work, we use single-molecule imaging techniques to examine the initial interactions between Aβ monomers and oligomers and the membranes of live cells. This highly sensitive method enables the visualization of individual Aβ species on the cell surface and characterization of their oligomerization state, all at biologically relevant, nanomolar concentrations. The results indicate …
Concise Synthesis Of Α-Substituted 2-Benzofuranmethamines And Other 2-Subsituted Benzofurans Via Α-Substituted 2-Benzofuranmethyl Carbocation Intermediates, Nikhom Wongsa, Ubonta Sommart, Thunwadee Ritthiwigrom, Arife Yazici, Somdej Kanokmedhakul, Kwanjai Kanokmedhakul, Anthony C. Willis, Stephen G. Pyne
Concise Synthesis Of Α-Substituted 2-Benzofuranmethamines And Other 2-Subsituted Benzofurans Via Α-Substituted 2-Benzofuranmethyl Carbocation Intermediates, Nikhom Wongsa, Ubonta Sommart, Thunwadee Ritthiwigrom, Arife Yazici, Somdej Kanokmedhakul, Kwanjai Kanokmedhakul, Anthony C. Willis, Stephen G. Pyne
Faculty of Science, Medicine and Health - Papers: part A
Propargyl amines 4, where R3 is aryl, undergo 5-exo-dig cyclization reactions under relatively mild conditions (AgNO3, DMF, 60 °C, 1 h) to give 3-amino-2,3-dihydro-2-arylmethylidenebenzofurans 5 (R3 = aryl). In contrast, substrates where R3 is alkyl undergo competing 6-endo-dig and 5-exo-dig cyclization processes. The hydroxymethyl substrate 4 (R3 = CH2OH), however, was smoothly converted to its corresponding 5-exo-dig cyclization product 5, likely due to the assistance of the primary hydroxyl group in the 5-exo-dig cyclization process by silver cation coordination. Under more enforcing conditions (AgNO3, DMF, 100 °C, 18 h), the initially formed products 5 undergo a 1,3-allylic rearrangement to their …
Daedalic Dna Vaccination Against Self Antigens As A Treatment For Chronic Kidney Disease, Yuan Min Wang, Jimmy Jianheng Zhou, Ya Wang, Debbie Watson, Geoff Yu Zhang, Min Hu, Huiling Wu, Guoping Zheng, Yiping Wang, Anne M. Durkan, David Ch Harris, Stephen I. Alexander
Daedalic Dna Vaccination Against Self Antigens As A Treatment For Chronic Kidney Disease, Yuan Min Wang, Jimmy Jianheng Zhou, Ya Wang, Debbie Watson, Geoff Yu Zhang, Min Hu, Huiling Wu, Guoping Zheng, Yiping Wang, Anne M. Durkan, David Ch Harris, Stephen I. Alexander
Faculty of Science, Medicine and Health - Papers: part A
Chronic kidney disease (CKD) is a major cause of death and morbidity in Australia and worldwide. DNA vaccination has been used for targeting foreign antigens to induce immune responses and prevent autoimmune disease, viral infection and cancer. However, the use of DNA vaccination has been restricted by a limited ability to induce strong immune responses, especially against self-antigens which are limited by mechanisms of self-tolerance. Furthermore, there have been few studies on the potential of DNA vaccination in chronic inflammatory diseases, including CKD. We have established strategies of DNA vaccination targeting specific self-antigens in the immune system including co-stimulatory pathways, …
Slow Avoidance Response To Contaminated Sediments Elicits Sublethal Toxicity To Benthic Invertebrates, Daniel J. Ward, Stuart L. Simpson, Dianne F. Jolley
Slow Avoidance Response To Contaminated Sediments Elicits Sublethal Toxicity To Benthic Invertebrates, Daniel J. Ward, Stuart L. Simpson, Dianne F. Jolley
Faculty of Science, Medicine and Health - Papers: part A
Advanced analytical techniques have identified the heterogeneity of sediments in aquatic environments which may impact the exposure of benthic organisms to contaminants. Acute and chronic toxicity associated with short, intermittent exposure to four field-collected contaminated sediments were assessed for the epi-benthic amphipod Melita plumulosa and the harpacticoid copepod Nitocra spinipes. Increasing the duration of exposure caused a decrease in survival of M. plumulosa and N. spinipes during 10-d bioassays. Increasing the frequency of exposure to a total exposure time >96-h resulted in a significant toxicity to M. plumulosa. Reproduction decreased for both species from exposure to contaminated sediment. For M. …
An Assessment Of The Bhutanese Traditional Medicine For Its Ethnopharmacology, Ethnobotany And Ethnoquality: Textual Understanding And The Current Practices, Phurpa Wangchuk, Stephen G. Pyne, Paul A. Keller
An Assessment Of The Bhutanese Traditional Medicine For Its Ethnopharmacology, Ethnobotany And Ethnoquality: Textual Understanding And The Current Practices, Phurpa Wangchuk, Stephen G. Pyne, Paul A. Keller
Faculty of Science, Medicine and Health - Papers: part A
Ethnopharmacological relevance : This study involves the assessment of the Bhutanese traditional medicine (BTM) which was integrated with the mainstream biomedicine in 1967 to provide primary health care services in the country. It caters to 20-30% of the daily out-patients within 49 traditional medicine units attached to 20 district modern hospitals and 29 Basic Health Units in the country. Aim of the study : This study presents the ethnopharmacological, ethnobotanical and the ethnoquality concepts in relation to mainstream Tibetan medicine and describes the current practices of BTM. Materials and methods : Experienced BTM practitioners (Drung-tshos and Smen-pas) were selected using …
The Role Of Hypothalamic H1 Receptor Antagonism In Antipsychotic-Induced Weight Gain, Meng He, Chao Deng, Xu-Feng Huang
The Role Of Hypothalamic H1 Receptor Antagonism In Antipsychotic-Induced Weight Gain, Meng He, Chao Deng, Xu-Feng Huang
Faculty of Science, Medicine and Health - Papers: part A
Treatment with second generation antipsychotics (SGAs), notably olanzapine and clozapine, causes severe obesity side effects. Antagonism of histamine H1 receptors has been identified as a main cause of SGA-induced obesity, but the molecular mechanisms associated with this antagonism in different stages of SGA-induced weight gain remain unclear. This review aims to explore the potential role of hypothalamic histamine H1 receptors in different stages of SGA-induced weight gain/obesity and the molecular pathways related to SGA-induced antagonism of these receptors. Initial data have demonstrated the importance of hypothalamic H1 receptors in both short- and long-term SGA-induced obesity. Blocking hypothalamic H1 receptors by …
Extracellular Chaperones And Proteostasis, Amy R. Wyatt, Justin J. Yerbury, Heath Ecroyd, Mark R. Wilson
Extracellular Chaperones And Proteostasis, Amy R. Wyatt, Justin J. Yerbury, Heath Ecroyd, Mark R. Wilson
Faculty of Science, Medicine and Health - Papers: part A
There is a family of currently untreatable serious human diseases that arise from the inappropriate misfolding and aggregation of extracellular proteins. At present our understanding of mechanisms that operate to maintain proteostasis in extracellular body fluids is limited but has significantly advanced with the discovery of a small but growing family of constitutively secreted extracellular chaperones (ECs). The available evidence strongly suggests that these chaperones act as both sensors and disposal-mediators of misfolded proteins in extracellular fluids, thereby normally protecting us from disease pathologies. It is critically important to further increase our understanding of the mechanisms that operate to effect …
Generation Of Hydrogen Peroxide-Resistant Murine Neuroblastoma Cells: A Target Discovery Platform For Novel Neuroprotective Genes, Annette E. Maczurek, Rebekka Wild, Daunia Laurenti, Megan L. Steele, Lezanne Ooi, Gerald Munch
Generation Of Hydrogen Peroxide-Resistant Murine Neuroblastoma Cells: A Target Discovery Platform For Novel Neuroprotective Genes, Annette E. Maczurek, Rebekka Wild, Daunia Laurenti, Megan L. Steele, Lezanne Ooi, Gerald Munch
Faculty of Science, Medicine and Health - Papers: part A
Oxidative stress has been suggested to play an important role in the pathogenesis of various neurodegenerative diseases including Alzheimer’s disease (AD). Hydrogen peroxide (H2O2), one of the main reactive oxygen species, is converted into the highly toxic ·OH radical in the presence of redox-active transition metals, which then oxidises nucleic acids, lipids and proteins, leading to neurodegeneration and cell death. There is an urgent need to gain more knowledge about relevant therapeutic targets to combat oxidative stress and it neurotoxic effects, and how this knowledge can be utilized to develop novel neuroprotective therapies for AD. One way to identify new …
Mechanism For The Synergistic Effect Of Rapamycin And Resveratrol On Hyperinsulinemia May Involve The Activation Of Protein Kinase B, J Chen, Xu-Feng Huang
Mechanism For The Synergistic Effect Of Rapamycin And Resveratrol On Hyperinsulinemia May Involve The Activation Of Protein Kinase B, J Chen, Xu-Feng Huang
Faculty of Science, Medicine and Health - Papers: part A
Dear Editor, We read with great interest Leontiev et al.'s paper entitled 'Resveratrol potentiates rapamycin to prevent hyperinsulinemia and obesity in male mice on high-fat diet' recently published in Cell Death & Disease.1 Their finding that rapamycin and resveratrol have a synergistic effect is important for treating insulin resistance. They showed that rapamycin inhibited mammalian target of rapamycin (mTOR) activity, while resveratrol inhibited S6 kinase (S6K). We think that these compounds may exert their effects through activating protein kinase B (Akt), a key regulator of insulin sensitivity. Both the inhibition of mTOR by rapamycin and of S6K by resveratrol could …
Allosteric Activation Transitions In Enzymes And Biomolecular Motors: Insights From Atomistic And Coarse-Grained Simulations, Michael D. Daily, Haibo Yu, George N. Phillips, Qiang Cui
Allosteric Activation Transitions In Enzymes And Biomolecular Motors: Insights From Atomistic And Coarse-Grained Simulations, Michael D. Daily, Haibo Yu, George N. Phillips, Qiang Cui
Faculty of Science, Medicine and Health - Papers: part A
The chemical step in enzymes is usually preceded by a kinetically distinct activation step that involves large-scale conformational transitions. In "simple" enzymes this step corresponds to the closure of the active site; in more complex enzymes, such as biomolecular motors, the activation step is more complex and may involve interactions with other biomolecules. These activation transitions are essential to the function of enzymes and perturbations in the scale and/or rate of these transitions are implicated in various serious human diseases; incorporating key flexibilities into engineered enzymes is also considered a major remaining challenge in rational enzyme design. Therefore it is …
Sequential 1,4- And 1,2-Addition Reactions To Α,Β-Unsaturated N-Acyliminium Ions: A New Strategy For The Synthesis Of Spiro And Bridged Heterocycles, Arife Yazici, Stephen G. Pyne
Sequential 1,4- And 1,2-Addition Reactions To Α,Β-Unsaturated N-Acyliminium Ions: A New Strategy For The Synthesis Of Spiro And Bridged Heterocycles, Arife Yazici, Stephen G. Pyne
Faculty of Science, Medicine and Health - Papers: part A
Novel bicyclic and tetracyclic spirocycles and tricyclic bridged heterocyclic systems can be readily prepared from sequential 1,4- and 1,2-addition reactions of latent bis-nucleophiles to α,β-unsaturated N-acyliminium ions.