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Teucrium polium (T. polium), commonly known as golden germander, is a herb that grows in the Mediterranean region and is used by the locals to treat diabetes mellitus. The glucose-lowering effect of T. polium is well established in rodents. This study aims to examine whether the glucose-lowering effect is by inducing the release of insulin from pancreatic beta cells and to identify key measurable biomolecules/sites that are modified in the lead-up to insulin release. Insulin secretion was examined in BRIN-BD11 pancreatic beta cells treated with T. polium extract in vitro and key flavonoids were identified using LCMS. The T. polium extract promoted increased insulin secretion (p<0.05), in a dose-dependent manner, and increased glucose uptake (p<0.05) within 30min. This was accompanied by an increase in GLUT2 (p<0.05) and glucokinase (p<0.01) expression. Also, mitochondrial metabolism and glycolytic rates were enhanced (p<0.05), and ATP production increased (p<0.01), which coincided with increased (p<0.01) calcium influx. Rutin and apigenin were detected, but not quercetin, in this extract. T. polium promotes insulin secretion. T. polium does this by GLUT2 and glucokinase expression, increased glucose transport, metabolism and ATP production, ultimately increasing intracellular calcium.

Prescriptions and use of medications to treat mental health conditions in young autistic populations are inconsistent worldwide. This makes it hard to compare findings from international studies to the Australian autistic population, where there are limited relevant studies. Apart from risperidone, there are no other medications specified for direct use in autistic persons. This study aims to gain initial broad understanding of the use of medications, commonly prescribed for mental health conditions, specifically by autistics under the age of 21 years. We analysed data that were previously collected as part of the Western Australian Autism Biological Registry between 2011 and 2015 which amounted to 239 surveys completed on young persons with diagnosed autism. The questionnaires included information on co-occurring conditions, current or previous use of medications and reasons for use of the medications. Only one-quarter of the participants in this study reported using at least one mental health-related medication in their lifetime. The most reported medications were stimulants, antidepressants and antiepileptics. The reasons for using medication included managing attention deficit hyperactivity disorder, challenging behaviours, seizures, sleep difficulties and symptoms of anxiety and depression. The number of individuals reporting medication use in this study was lower compared to other developed countries. Nevertheless, these medications should be monitored due to limited understanding of their use to manage co-occurring symptoms in young autistic persons. The findings highlight the importance of ongoing research to better understand mental health-related medications and inform best practice.

© 2019 Royal Pharmaceutical Society Objectives: To assess the knowledge and understanding of autism spectrum disorder (ASD) by community pharmacists, across Western Australia (WA) and evaluate the extent to which they incorporate ASD friendly practices in their pharmacy. Methods: A cross-sectional study involved a postal questionnaire sent to a stratified random sample of 250 community pharmacies across WA. A score of ≥10/13 (≥76.9%) appropriate responses to selected questions was considered an indication of ‘good knowledge’ of ASD. Univariate associations between ‘good knowledge’ and variables in the questionnaire were analysed using chi-square statistics, and multivariate analysis was performed using a logistic regression model. Demographic data relating to the pharmacy were used to determine the likelihood it was ASD friendly. Key findings: Overall, 97/250 (38.8%) questionnaires were returned. There were 34/96 (35.4%) respondents classified as having ‘good knowledge’. Stigma surrounding ASD was the single best indicator of ‘good knowledge’ (P < 0.0001). None of the respondents indicated they catered specifically for ASD, and 38/97 (39.2%) reported that no changes were needed to their pharmacy to improve accessibility. There were a number of demographic features that increased the likelihood that pharmacies had the potential to be ASD friendly. Conclusions: Pharmacists overall had a basic understanding of ASD. Pharmacists who identified that stigma surrounding ASD existed in the community were more likely to achieve ‘good knowledge’. There was a reluctance to improve pharmacy accessibility to patients with ASD. Pharmacists did not appear to incorporate ASD beneficial practices into their pharmacy and pharmacy environment.

Short-chain lipid conjugates can increase permeability of a small peptide across human epidermis; however, the emerging lipoaminoacid (LAA) conjugation technique is costly and can deliver mixed synthetic products of varied biological potential. LAA conjugation using a racemic mixture produces a mixture of D- and L-stereoisomers. Individual enantiomers can be produced at an extra cost. We investigated an affordable technique that produces only one synthetic product: short-chain (C7–C8) acyl lipidation. Acyl lipidation of Ala-Ala-Pro-Val, an inhibitor of human neutrophil elastase (HNE; believed to lead to abnormal tissue destruction and disease development), was investigated as an alternative to LAA conjugation. The current study aimed to assess the effects of acyl lipidation (either at the N-terminal or at the C-terminal) on neutrophil elastase activity in vitro and on transdermal delivery ex vivo. The inhibitory capacity of the acyl conjugates was compared to LAA conjugates (conjugated at the N-terminal) of the same peptide. The L-stereoisomer appears to rapidly degrade, but it represents a significantly (P<0.05) better inhibitor of HNE than the parent peptide (Ala-Ala-Pro-Val). Although the D-stereoisomer appears to permeate human epidermal skin sections in a better fashion than the L-stereoisomer, it is not a significantly better inhibitor of HNE than the parent peptide. Acyl lipidation (with a C7 lipid chain) at either end of the peptide substantially enhances the permeability of the peptide across human skin epidermis as well as significantly (P<0.005) increases its elastase inhibitory potential. Therefore, our current study indicates that acyl lipidation of a peptide is a more economical and effective alternative to LAA conjugation.

Daniel Rocco,1,2 James Ross,1,2 Paul E Murray,1 Rima Caccetta1,2 1School of Pharmacy, 2Curtin Health Innovation Research Institute, Curtin University, Perth, WA, Australia Abstract: Short-chain lipid conjugates can increase permeability of a small peptide across human epidermis; however, the emerging lipoaminoacid (LAA) conjugation technique is costly and can deliver mixed synthetic products of varied biological potential. LAA conjugation using a racemic mixture produces a mixture of D- and L-stereoisomers. Individual enantiomers can be produced at an extra cost. We investigated an affordable technique that produces only one synthetic product: short-chain (C7–C8) acyl lipidation. Acyl lipidation of Ala-Ala-Pro-Val, an inhibitor of human neutrophil elastase (HNE; believed to lead to abnormal tissue destruction and disease development), was investigated as an alternative to LAA conjugation. The current study aimed to assess the effects of acyl lipidation (either at the N-terminal or at the C-terminal) on neutrophil elastase activity in vitro and on transdermal delivery ex vivo. The inhibitory capacity of the acyl conjugates was compared to LAA conjugates (conjugated at the N-terminal) of the same peptide. The L-stereoisomer appears to rapidly degrade, but it represents a significantly (P<0.05) better inhibitor of HNE than the parent peptide (Ala-Ala-Pro-Val). Although the D-stereoisomer appears to permeate human epidermal skin sections in a better fashion than the L-stereoisomer, it is not a significantly better inhibitor of HNE than the parent peptide. Acyl lipidation (with a C7 lipid chain) at either end of the peptide substantially enhances the permeability of the peptide across human skin epidermis as well as significantly (P<0.005) increases its elastase inhibitory potential. Therefore, our current study indicates that acyl lipidation of a peptide is a more economical and effective alternative to LAA conjugation. Keywords: topical delivery

Screening extracts and drug entities for antidiabetic bioactivity is essentially limited to animal models as the processes leading to hyperglycemia and the complications of diabetes involve more than one organ. Further, in vitro results seldom translate into meaningful in vivo outcomes especially in a disease such as Diabetes Mellitus. In vivo studies on specialized animal models have allowed great progress in tailoring research questions towards individualized genetic and biochemical contributors and their effect on the pathogenesis of the disease processes. Various disease models have been used either through genetic-manipulation (transgenic models) or through chemical induction (disease-induced models). Although there is a surplus of animal models (spontaneous and induced) to study Type I and Type II diabetes, there is no ideal or standard model for studying the individualized effects of various classes of antidiabetic drugs. Rodents, most commonly rats and mice, have been used by researchers as animal models of the disease and both normoglycemic and diabetic animals are used to assess the antidiabetic activities of drugs or extracts under investigation. Screening for antidiabetic activities can be achieved by measuring a wide range of biomarkers and end points including blood glucose and insulin levels. © 2013 Springer Science+Business Media, LLC.