In spite of increasing evidence that parasitic worms may protect humans from developing allergic and autoimmune diseases and the continuing identification of defined helminth-derived immunomodulatory molecules, to date no new anti-inflammatory drugs have been developed from these organisms. We have approached this matter in a novel manner by synthesizing a library of drug-like small molecules based upon phosphorylcholine, the active moiety of the anti-inflammatory Acanthocheilonema viteae product, ES-62, which as an immunogenic protein is unsuitable for use as a drug. Following preliminary in vitro screening for inhibitory effects on relevant macrophage cytokine responses, a sulfone-containing phosphorylcholine analogue (11a) was selected for testing in an in vivo model of inflammation, collagen-induced arthritis (CIA). Testing revealed that 11a was as effective as ES-62 in protecting DBA/1 mice from developing CIA and mirrored its mechanism of action in downregulating the TLR/IL-1R transducer, MyD88. 11a is thus a novel prototype for anti-inflammatory drug development.
Dimethyl sulfoxide (DMSO) is currently employed across the biomedical field, from cryopreservation to in vitro assays, despite the fact that it has been shown to have an assortment of biologically relevant effects. The amphiphilic nature of DMSO along with its relatively low toxicity at dilute concentrations make it a challenging solvent to replace. A possible alternative is Cyrene™ (dihydrolevoglucosenone), an aprotic dipolar solvent that is derived from waste biomass. In addition to being a green solvent, Cyrene™ has comparable solvation properties and is reported to have low toxicity. Herein the abilities of the two solvents to solubilize drug compounds and to act as non-participatory vehicles in drug discovery for antibacterials are compared. It was demonstrate that the results of standardised antimicrobial susceptibility testing do not differ between drugs prepared from either Cyrene™ or DMSO stock. Moreover, in contrast to DMSO, Cyrene™ does not offer protection from ROS mediated killing of bacteria and may therefore be an improvement over DMSO as a vehicle in antimicrobial drug discovery.
22 November 2017 in Journal of Further and Higher Education
Recognising the importance of graduates being equipped with appropriate employability skills alongside their subject-specific skills, we have had transferable skills training embedded throughout our degree programmes for 30 years. More recently, a specific employability skills module for final-year honours students has been created. This module consists of a programme of activities supporting employability skills, which was delivered to final-year undergraduate students from 2012 to 2015. A key feature in the development and delivery of these activities was the involvement of external experts. Detailed questionnaires have captured student perceptions and thematic analysis has revealed key themes. The module has been perceived to be highly useful, resulting in significant increases in students’ confidence across key areas of employability skills. Furthermore, students may hold skewed perceptions of the relevance of generic employability skills to their chosen career path. This fact should be considered when delivering employability skills programmes.
3 May 2012 in Chemistry Education Research and Practice
Mathematical ability is a major contributory factor to the success of a student in any science course. This paper aims to determine the source of the difficulty that students often find when performing calculations in chemistry. Through the design and analysis of a set of chemistry questions and analogous mathematics questions, set in a Standard Grade context, it is revealed that a basic grasp of mathematics is missing.
26 May 2021 in Journal of Further and Higher Education
For many years, a key driver for Higher Education Institutions (HEIs) has been ensuring that students are prepared for employment post-graduation. This has often resulted in HEIs providing specific modules of study focussing on employability and soft skills. The existing research literature presents a variety of strategies for embedding employability within curricula, often focusing on frameworks to review the provision of employability opportunities within a degree programme. The authors have previously investigated an employability module within an Undergraduate Chemistry Programme at their UK HEI, particularly focusing on students’ perceptions – these coalesced around the themes of personal progression, relevance of the module and interactions. However, before using these findings to further develop the module, it was deemed necessary to investigate the module in a different context. This study investigates the employability module in an Australian HEI and its delivery to undergraduate and postgraduate students from a range of different disciplines. Free text comments from questionnaires answered by 85 participants were subjected to thematic analysis in order to understand students’ perceptions of the module in this new context. The new thematic map was compared to that from the original study to reveal several key similarities and differences between students’ perceptions. However, the most important finding is thast employability modules should be tailored to a specific cohort to ensure they are aligned with their needs. This suggests that Central University employability module providers should work closely with individual departments to maximise the impact of these for students.
1 June 2016 in European Journal of Medicinal Chemistry
A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.