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Full-Text Articles in Medicinal and Pharmaceutical Chemistry

Responsiveness Of Higher Education Programs To Policy And Recommendations In The Biopharmaceutical Sector, Maeve Scott Mar 2023

Responsiveness Of Higher Education Programs To Policy And Recommendations In The Biopharmaceutical Sector, Maeve Scott

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This essay will review the business and government policies relevant to the biopharmaceutical sector which influence higher education programs. The mechanisms which enable higher education to adapt to policy will be summarised and the pace of the response estimated.

Higher education (HE) programs need to respond in a timely manner to dynamic industries to maximise opportunities for graduates and support the Irish economy. The author manages internships and teaches on pharmaceutical science programs and aims to ensure the program is current to maximise student success. This review intends to identify the most relevant policy sources that can inform the Pharmaceutical …


Formulation, Characterisation And Evaluation Of The Antihypertensive Peptides, Isoleucine-Proline-Proline And Leucine-Lysine-Proline In Chitosan Nanoparticles Coated With Zein For Oral Drug Delivery, Minna Khalid Danish, John P. Gleeson, David J. Brayden, Hugh Byrne, Jesus Maria Frias, Sinead Ryan Jan 2022

Formulation, Characterisation And Evaluation Of The Antihypertensive Peptides, Isoleucine-Proline-Proline And Leucine-Lysine-Proline In Chitosan Nanoparticles Coated With Zein For Oral Drug Delivery, Minna Khalid Danish, John P. Gleeson, David J. Brayden, Hugh Byrne, Jesus Maria Frias, Sinead Ryan

Articles

Isoleucine-Proline-Proline (IPP) and Leucine-Lysine-Proline (LKP) are food-derived tripeptides whose antihypertensive functions have been demonstrated in hypertensive rat models. However, peptides display low oral bioavailability due to poor intestinal epithelial permeability and instability. IPP and LKP were formulated into nanoparticles (NP) using chitosan (CL113) via ionotropic gelation and then coated with zein. Following addition of zein, a high encapsulation efficiency (EE) (>80%) was obtained for the NP. In simulated gastric fluid (SGF), 20% cumulative release of the peptides was achieved after 2 h, whereas in simulated intestinal fluid (SIF), ~90% cumulative release was observed after 6 h. Higher colloidal stability …


Design, Synthesis, And Biological Evaluation Of Aryl Piperazines With Potential As Antidiabetic Agents Via The Stimulation Of Glucose Uptake And Inhibition Of Nadh:Ubiquinone Oxidoreductase, R. Devine, M. Kelada, S. Leonard, D.S.D. Martin, J.M.D. Walsh, C.J. Breen, R.B. Driver, Gemma K. Kinsella, J.B.C Findlay, J.C. Stephens Jan 2020

Design, Synthesis, And Biological Evaluation Of Aryl Piperazines With Potential As Antidiabetic Agents Via The Stimulation Of Glucose Uptake And Inhibition Of Nadh:Ubiquinone Oxidoreductase, R. Devine, M. Kelada, S. Leonard, D.S.D. Martin, J.M.D. Walsh, C.J. Breen, R.B. Driver, Gemma K. Kinsella, J.B.C Findlay, J.C. Stephens

Articles

The management of blood glucose levels and the avoidance of diabetic hyperglycemia are common objectives of many therapies in the treatment of diabetes. An aryl piperazine compound 3a (RTC1) has been described as a promoter of glucose uptake, in part through a cellular mechanism that involves inhibition of NADH:ubiquinone oxidoreductase. We report herein the synthesis of 41 derivatives of 3a (RTC1) and a systematic structure-activity-relationship study where a number of compounds were shown to effectively stimulate glucose uptake in vitro and inhibit NADH:ubiquinone oxidoreductase. The hit compound 3a (RTC1) remained the most efficacious with a 2.57 fold increase in glucose …


Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle Jan 2016

Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle

Articles

Piperlongumine (piplartine, 1) is a small molecule alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and Western blotting, we demonstrated that 1 is a tubulin-destabilising agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerised when treated with 1. We synthesised a number of analogues of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, …


The Synthesis And Applications Of [2.2]Paracyclophane Derivatives, Craig Hicks Jan 2016

The Synthesis And Applications Of [2.2]Paracyclophane Derivatives, Craig Hicks

Doctoral

This work concerns the preparation of novel [2.2]paracyclophane derivatives intended for use as asymmetric ligands and investigations into surface coatings prepared from [2.2]paracylophanes. This begins with a general introduction to enantioselective synthesis, followed by a review of relevant reported ligands based on the [2.2]paracyclophane framework and their applications. Next is described the preparation of novel ligands based on the [2.2]paracyclophane structure. Starting with the preparation of a range of mono and disubstituted [2.2]paracyclophanes, including several novel analogues, this moves on to investigating resolution procedures where a novel method for the preparation of enantiopure 4-bromo[2.2]paracyclophane is described. The coupling of prepared …


Anode Catalysts For The Direct Ethanol Fuel Cell, Daryl Fox Jan 2016

Anode Catalysts For The Direct Ethanol Fuel Cell, Daryl Fox

Doctoral

The anodic reaction of the Direct Ethanol Fuel Cell has been studied with various catalysts such as electrodeposited platinum, palladium, nickel and gold electrodes. The mechanism of bimetallic catalysts was used to reduce the platinum content needed for ethanol oxidation. The effects of increased temperature, ethanol concentration, electrolyte pH and scan rate have been examined. The impact of different carbon surfaces such as carbon ink, carbon paper and commonly used Vulcan XC72 have also been analysed in order to determine the optimum conditions for the EOR in a fuel cell.

Electrochemical methods were used to analyse catalyst performance such as …


Isolation And Partial Characterization Of Bioactive Fucoxanthin From Himanthalia Elongata Brown Seaweed: A Tlc-Based Approach, Gaurav Rajauria, Nissreen Abu-Ghannam May 2013

Isolation And Partial Characterization Of Bioactive Fucoxanthin From Himanthalia Elongata Brown Seaweed: A Tlc-Based Approach, Gaurav Rajauria, Nissreen Abu-Ghannam

Articles

Seaweeds are important sources of carotenoids, and numerous studies have shown the beneficial effects of these pigments on human health. In the present study, Himanthalia elongata brown seaweed was extracted with a mixture of low polarity solvents, and the crude extract was separated using analytical thin-layer chromatography (TLC).The separated compounds were tested for their potential antioxidant capacity and antimicrobial activity against Listeria monocytogenes bacteria using TLC bioautography approach. For bio-autography, the coloured band on TLC chromatogram was visualized after spraying with DPPH and triphenyltetrazolium chloride reagents which screen antioxidant and antimicrobial compounds, respectively, and only one active compound was screened …


The Mechanism Of Silver Dissolution For Biomedical Devices And Hygienic Coating Applications., Yanmei Ma Jan 2008

The Mechanism Of Silver Dissolution For Biomedical Devices And Hygienic Coating Applications., Yanmei Ma

Doctoral

This work focuses on the mechanism of silver dissolution for biomedical and hygienic coating applications. The research work began from the investigation of silver dissolution behaviour from pure silver and silver-platinum alloys in solutions with or without chloride using the technique of cyclic volammetry (CV). A zero resistance amperometry (ZRA) measurement was carried out to study the effect of platinum on the silver dissolution behaviour in 0.89%wt. NaCI solution. The mechanism of silver dissolution from pure silver and silver-platinum alloys in 0.89%wt. NaCI solution was proposed by an equivalent circuit model under the investigation of electrochemical impedance spectroscopy (EIS). It …