6,153,679 results match your criteria Pharmacology & Pharmacy [Journal]

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Ghrelin signalling within the rat nucleus accumbens and skilled reach foraging.

Psychoneuroendocrinology 2019 Apr 8;106:183-194. Epub 2019 Apr 8.

Department of Pharmacology, Institute of Neuroscience and Physiology, The Sahlgrenska Academy at the University of Gothenburg, Gothenburg, Sweden. Electronic address:

Motivation alters behaviour in a complex manner and nucleus accumbens (NAc) shell has been implied as a key structure regulating such behaviour. Recent studies show that acute ghrelin signalling enhances motivation when assessed in a simple motor task. The aim of the present study was to define the role of ghrelin signalling on motivation in a more complex motor behaviour. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03064530193012
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http://dx.doi.org/10.1016/j.psyneuen.2019.04.008DOI Listing
April 2019
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Impacts of rare earth elements on animal health and production: Highlights of cerium and lanthanum.

Sci Total Environ 2019 Mar 13;672:1021-1032. Epub 2019 Mar 13.

Pharmacology Department, Faculty of Veterinary Medicine, Suez Canal University, Ismailia 41522, Egypt. Electronic address:

Because the use of antibiotics as growth promoters was banned due to global health concerns, researchers are focusing on exploring alternative safe and effective feed additives. Rare earth elements (REEs) are located in group III of the periodic table, which includes cerium (Ce), lanthanum (La), and other elements. Recently, REEs have been involved in many medical, industrial, zootechnical, and agricultural applications. Read More

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http://dx.doi.org/10.1016/j.scitotenv.2019.02.270DOI Listing

Baicalein attenuates pancreatic inflammatory injury through regulating MAPK, STAT 3 and NF-κB activation.

Int Immunopharmacol 2019 Apr 15;72:204-210. Epub 2019 Apr 15.

Tianjin Key Laboratory of Chinese Medicine Pharmacology, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China; School of Integrative Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China. Electronic address:

Acute pancreatitis (AP) is a common acute abdominal disease with local or systemic inflammatory response, caused by abnormal activation of digestive enzymes. Baicalein has been shown to exert anti-inflammatory effects and to attenuate the pathological changes of AP. The aim of the research was to investigate the effects of baicalein on caerulein induced pancreatitis, and to elucidate the putative underlying mechanism. Read More

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http://dx.doi.org/10.1016/j.intimp.2019.04.018DOI Listing

Adverse and hormetic effects in rats exposed for 12 months to low dose mixture of 13 chemicals: RLRS part III.

Toxicol Lett 2019 Apr 15. Epub 2019 Apr 15.

Center of Toxicology Science & Research, Medical School, University of Crete, Heraklion, Crete, Greece; Department of Analytical and Forensic Medical Toxicology, Sechenov University, Moscow 119991, Russian Federation. Electronic address:

The aim of the current study was to evaluate the effects of a mixture of thirteen common chemicals on rats, after a one-year exposure to doses around the acceptable daily intake (ADIs), using blood and urinary tests. The influence of low doses of the mixture on weight gain, water consumption, feed consumption and feed efficiency, biochemistry parameters, haematological parameters, blood lymphocytes subsets, serum inflammation profile and urine parameters was evaluated. Our mixture caused a moderate monotonic increase of the males' appetite and a non-monotonic increase of anabolism and a monotonic increase of appetite for the females. Read More

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http://dx.doi.org/10.1016/j.toxlet.2019.04.005DOI Listing

Pathophysiological Role of TRPM2 in Age-Related Cognitive Impairment in Mice.

Neuroscience 2019 Apr 15. Epub 2019 Apr 15.

Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.

Aging causes various functional changes, including cognitive impairment and inflammatory responses in the brain. Transient receptor potential melastatin 2 (TRPM2), a Ca-permeable channel expressed abundantly in immune cells, exacerbates inflammatory responses. Previously, we reported that TRPM2 on resident microglia plays a critical role in exacerbating inflammation, white matter injury, and cognitive impairment during chronic cerebral hypoperfusion; however, the physiological or pathophysiological role of TRPM2 during age-associated inflammatory responses remains unclear. Read More

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http://dx.doi.org/10.1016/j.neuroscience.2019.04.012DOI Listing

Calcium Influx through Muscle nAChR-Channels: One Route, Multiple Roles.

Neuroscience 2019 Apr 15. Epub 2019 Apr 15.

Department of Physiology and Pharmacology, Sapienza University, piazzale Aldo Moro 5, 00185, Rome, Italy; IRCCS Neuromed, Viale dell'Elettronica, 86077, Pozzilli, Italy.

Although Ca influx through muscle nAChR-channels has been described over the past 40 years, its functions remain still poorly understood. In this review we suggest possible roles of Ca entry at all stages of muscle development, summarizing the evidence present in literature. nAChRs are expressed in myoblasts prior to fusion, and can be activated in the absence of an ACh-releasing nerve terminal, with Ca influx likely contributing to regulate cell fusion. Read More

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http://dx.doi.org/10.1016/j.neuroscience.2019.04.011DOI Listing

Retinal oximetry: Metabolic imaging for diseases of the retina and brain.

Prog Retin Eye Res 2019 Apr 15. Epub 2019 Apr 15.

University of Iceland, Reykjavik, Iceland.

Retinal oximetry imaging of retinal blood vessels measures oxygen saturation of hemoglobin. The imaging technology is non-invasive and reproducible with remarkably low variability on test-retest studies and in healthy cohorts. Pathophysiological principles and novel biomarkers in several retinal diseases have been discovered, as well as possible applications for systemic and brain disease. Read More

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http://dx.doi.org/10.1016/j.preteyeres.2019.04.001DOI Listing

Leaves and stems of Capparis erythrocarpos, more sustainable than roots, show antiarthritic effects.

J Ethnopharmacol 2019 Apr 15:111890. Epub 2019 Apr 15.

Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.

Ethnopharmacological Relevance: Capparis erythrocarpos is a medicinal plant used widely in many parts of Africa for the management of pain and inflammatory conditions such as rheumatoid arthritis. Its wide range of use, popularity and high value, make C. erythrocarpos containing products a target for economically driven adulteration. Read More

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http://dx.doi.org/10.1016/j.jep.2019.111890DOI Listing

Anti-obesity effect of argel (Solenostemma argel) on obese rats fed a high fat diet.

J Ethnopharmacol 2019 Apr 15:111893. Epub 2019 Apr 15.

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Egypt. Electronic address:

Ethnopharmacological Relevance: Solenostemma argel (Argel) is a desert plant commonly used in Egyptian and Sudanese traditional medicine to suppress appetite, for treatment of diabetes, and as antispasmodic and anti-inflammatory agents. Previously the anti-diabetic, hypolipidemic and lipase inhibitory activities of Argel were reported in animal studies and in-vitro assays. However, its specific mechanism of action as an anti-obesity agent has not been studied before. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03788741183492
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http://dx.doi.org/10.1016/j.jep.2019.111893DOI Listing
April 2019
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Differential Expression of HMGA1 and HMGA2 in pituitary neuroendocrine tumors.

Mol Cell Endocrinol 2019 Apr 15. Epub 2019 Apr 15.

Laboratory of Experimental Endocrinology - LEEx, Institute of Biomedical Sciences, Federal University of Rio de Janeiro, Brazil; Graduate Program in Endocrinology, Faculty of Medicine, Federal University of Rio de Janeiro, Brazil; Graduate Program in Pharmacology and Medicinal Chemistry, Institute of Biomedical Sciences, Federal University of Rio de Janeiro, Brazil. Electronic address:

Defining biomarkers for invasive pituitary neuroendocrine tumors (PitNETs) is highly desirable. The high mobility group A (HMGA) proteins are among the most widely expressed cancer-associated proteins. Indeed, their overexpression is a frequent feature of human malignancies, including PitNETs. Read More

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http://dx.doi.org/10.1016/j.mce.2019.04.010DOI Listing

Fatty acid binding protein 4 (FABP4) as a potential biomarker reflecting myocardial lipid storage in type 2 diabetes.

Metabolism 2019 Apr 15. Epub 2019 Apr 15.

Vascular Medicine and Metabolism Unit, Research Unit on Lipids and Atherosclerosis, "Sant Joan" University Hospital, Universitat Rovira i Virgili, Institut de Investigació Sanitaria Pere Virgili (IISPV), Reus, Spain; Spanish Biomedical Research Centre in Diabetes and Associated Metabolic Disorders (CIBERDEM), Institute of Health Carlos III, Madrid, Spain. Electronic address:

Objective: Fatty acid binding protein 4 (FABP4) is an intracellular lipid chaperone involved in the crosstalk between adipose and peripheral tissues, and it contributes to widespread insulin resistance in cells, including cardiac cells. However, the role of this adipokine in regulating cardiac metabolism and myocardial neutral lipid content in patients with type 2 diabetes has not been elucidated.

Methods: The impact of circulating FABP4 on the cardiac neutral lipid content were measured by proton magnetic resonance spectroscopy (H-MRS) in patients with type 2 diabetes. Read More

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http://dx.doi.org/10.1016/j.metabol.2019.04.007DOI Listing

Anhedonia following mild traumatic brain injury in rats: A behavioral economic analysis of positive and negative reinforcement.

Behav Brain Res 2019 Apr 15:111913. Epub 2019 Apr 15.

NeuroBehavioral Research Lab, Department of Veteran Affairs Medical Center, New Jersey Health Care System, East Orange, New Jersey, USA; Department of Pharmacology, Physiology and Neurosciences, New Jersey Medical School - Rutgers Biomedical and Health Sciences, Newark, New Jersey, USA; Graduate School of Biomedical Sciences, New Jersey Medical School-Rutgers Biomedical and Health Sciences, Newark, New Jersey, USA. Electronic address:

Psychiatric disorders affect nearly 50% of individuals who have experienced a traumatic brain injury (TBI). Anhedonia is a major symptom of numerous psychiatric disorders and is a diagnostic criterion for depression. It has recently been appreciated that reinforcement may be separated into consummatory (hedonic), motivational and decisional components, all of which may be affected differently in disease. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S01664328193034
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http://dx.doi.org/10.1016/j.bbr.2019.111913DOI Listing
April 2019
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Glyphaea brevis - In vitro antioxidant and in silico biological activity of major constituents and molecular docking analyses.

Toxicol In Vitro 2019 Apr 15. Epub 2019 Apr 15.

Phytomedicine, Biochemical Pharmacology and Toxicology Laboratories, Department of Biochemistry, School of Sciences, PMB 704, The Federal University of Technology, Akure, Nigeria.

Previous studies have revealed that leaf extracts of Glyphaea brevis possess antioxidant activity but the bioactivity and mechanisms of action of its major constituents remain unknown. This study evaluated in vitro antioxidant and free radical scavenging activities of Glyphaea brevis twigs and leaves, and probable toxicity profile, pharmacological activities and mechanisms of action of major phytoconstituents in silico. Phytochemical screening detected saponins, tannins, steroids, anthraquinones, flavonoids, terpenoids and phenolics in the extracts. Read More

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http://dx.doi.org/10.1016/j.tiv.2019.04.013DOI Listing

Variability in the validity and reliability of outcome measures identified in a systematic review to assess treatment efficacy of cognitive enhancers for Alzheimer's Dementia.

PLoS One 2019 18;14(4):e0215225. Epub 2019 Apr 18.

Institute for Health Policy, Management & Evaluation, University of Toronto, Toronto, Ontario Canada.

Introduction: Selection of optimal outcome measures is a critical step in a systematic review; inclusion of uncommon or non-validated outcome measures can impact the uptake of systematic review findings. Our goals were to identify the validity and reliability of outcome measures used in primary studies to assess cognition, function, behaviour and global status; and, to use these data to select outcomes for a systematic review (SR) on treatment efficacy of cognitive enhancers for Alzheimer's Dementia (AD).

Methods: Articles fulfilling the eligibility criteria of the SR were included in a charting exercise to catalogue outcome measures reported. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0215225PLOS
April 2019
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Neurally mediated syncope diagnosis based on adenylate cyclase activity in Japanese patients.

PLoS One 2019 18;14(4):e0214733. Epub 2019 Apr 18.

Department of Clinical Pharmacology, Tokai University School of Medicine, 143 Shimokasuya, Isehara, Kanagawa, Japan.

The study aims to clarify the mechanism in patients with neurally mediated syncope (NMS), focusing on the adenylate cyclase (AC) activity level in lymphocytes. This study included 40 subjects: 22 healthy volunteers and 18 NMS patients. We investigated the changes in AC activity that occur during of syncope at rest and during the head-up tilt (HUT) test. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0214733PLOS

Radiation induces changes in toll-like receptors of the uterine cervix of the rat.

PLoS One 2019 18;14(4):e0215250. Epub 2019 Apr 18.

Department of Pharmacology, Institute of Neuroscience and Physiology, Sahlgrenska Academy at the University of Gothenburg, Gothenburg, Sweden.

Radiotherapy is an important therapeutic approach against cervical cancer but associated with adverse effects including vaginal fibrosis and dyspareunia. We here assessed the immunological and oxidative responses to cervical irradiation in an animal model for radiation-induced cervicitis. Rats were sedated and either exposed to 20 Gy of ionising radiation given by a linear accelerator or only sedated (controls) and euthanized 1-14 days later. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0215250PLOS

Sumatriptan increase skin flap survival through activation of 5HT 1b/1d receptors in rats: the mediating role of nitric oxide pathway.

Plast Reconstr Surg 2019 Apr 11. Epub 2019 Apr 11.

School of Public Health, Tehran University of Medical Sciences, Tehran, Iran.

Background: Random pattern skin flaps are applicable to reconstruct any defects in plastic surgery. However, they are limited to apply due to necrosis. Sumatriptan, a selective 5HT 1b/1d agonist, routinely use to subset acute migraine attack. Read More

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http://dx.doi.org/10.1097/PRS.0000000000005740DOI Listing

Antipsychotics in the general population and the driver population: comparisons from a population-based registry study.

Int Clin Psychopharmacol 2019 Apr 15. Epub 2019 Apr 15.

Pharmacology and Therapeutics, Faculty of Medicine, University of Valladolid, Valladolid.

Antipsychotics are considered driving-impairing medicines. A population-based registry study design was conceived to assess the year-2016 antipsychotic dispensation in Castile and León, Spain. Weighting was performed to obtain the adjusted antipsychotic consumption for licensed drivers according to age and gender using the Spanish national drivers' license census data. Read More

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http://dx.doi.org/10.1097/YIC.0000000000000263DOI Listing

Clopidogrel Pharmacogenetics.

Circ Cardiovasc Interv 2019 Apr;12(4):e007811

Peter Munk Cardiac Centre, Heart and Stroke Richard Lewar Centre, University of Toronto, Canada (M.E.F.).

Common genetic variation in CYP2C19 (cytochrome P450, family 2, subfamily C, polypeptide 19) *2 and *3 alleles leads to a loss of functional protein, and carriers of these loss-of-function alleles when treated with clopidogrel have significantly reduced clopidogrel active metabolite levels and high on-treatment platelet reactivity resulting in increased risk of major adverse cardiovascular events, especially after percutaneous coronary intervention. The Food and Drug Administration has issued a black box warning advising practitioners to consider alternative treatment in CYP2C19 poor metabolizers who might receive clopidogrel and to identify such patients by genotyping. However, routine clinical use of genotyping for CYP2C19 loss-of-function alleles in patients undergoing percutaneous coronary intervention is not recommended by clinical guidelines because of lack of prospective evidence. Read More

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https://www.ahajournals.org/doi/10.1161/CIRCINTERVENTIONS.11
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http://dx.doi.org/10.1161/CIRCINTERVENTIONS.119.007811DOI Listing
April 2019
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Sacubitril/Valsartan Decreases Cardiac Fibrosis in Left Ventricle Pressure Overload by Restoring PKG Signaling in Cardiac Fibroblasts.

Circ Heart Fail 2019 Apr;12(4):e005565

Department of Medicine, Aab Cardiovascular Research Institute (R.M.B., J.K.L., D.M.M., E.M.S.), University of Rochester, NY.

Background Heart failure (HF) is invariably accompanied by development of cardiac fibrosis, a form of scarring that increases muscular tissue rigidity and decreases cardiac contractility. Cardiac fibrosis arises from a pathological attempt to repair tissue damaged during maladaptive remodeling. Treatment options to block or reverse fibrosis have proven elusive. Read More

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http://dx.doi.org/10.1161/CIRCHEARTFAILURE.118.005565DOI Listing

Nickel-Catalyzed Intramolecular Direct Arylation of Imines toward Diverse Indoles.

Org Lett 2019 Apr 18. Epub 2019 Apr 18.

Institut für Organische und Biomolekulare Chemie , Georg-August-Universität , Tammannstraße 2 , 37077 Göttingen , Germany.

An efficient nickel-catalyzed intramolecular direct arylation of imines with challenging aryl chlorides has been developed. The versatile nickel catalysis made use of easily accessible imines and delivered diversely decorated 2-arylindoles of considerable importance to biological and medicinal chemistry. Read More

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http://dx.doi.org/10.1021/acs.orglett.9b00600DOI Listing

Ferulic Acid Esters and Withanolides: In Search of Withania somnifera GABA Receptor Modulators.

J Nat Prod 2019 Apr 18. Epub 2019 Apr 18.

National Research Council (CNR) , Institute of Neuroscience , 09042 Monserrato , Italy.

Nine compounds, including two undescribed withanolides, withasomniferolides A and B (1 and 2), three known withanolides (3-5), a ferulic acid dimeric ester (6), and an inseparable mixture of three long alkyl chain ferulic acid esters (7-9), were isolated from a GABA receptor positive activator methanol extract of the roots of Withania somnifera. The structures of the isolated compounds were elucidated based on NMR, MS, and ECD data analysis. In order to bioassay the single ferulic acid derivatives, compounds 6-9 were also synthesized. Read More

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http://pubs.acs.org/doi/10.1021/acs.jnatprod.8b01023
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http://dx.doi.org/10.1021/acs.jnatprod.8b01023DOI Listing
April 2019
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Pedagogical training profile of basic health sciences faculty in biomedical and related fields at Brazilian public and private higher education institutions.

Adv Physiol Educ 2019 Jun;43(2):180-190

Graduate Program in Biological Sciences: Physiology, Federal University of Rio Grande do Sul , Porto Alegre, Rio Grande do Sul , Brazil.

Historically, Brazilian higher education teachers' pedagogical training has not been a concern. Even today, a graduate degree is the main requirement to be a faculty member. However, a set of competencies is necessary to teach: pedagogical competency, political competency, and knowledge of specific content. Read More

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http://dx.doi.org/10.1152/advan.00211.2018DOI Listing

The complex pharmacology of natural products.

Future Med Chem 2019 Apr 18. Epub 2019 Apr 18.

Department of Biological Chemistry, Regional University of Cariri, Crato, CE, Brazil.

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http://dx.doi.org/10.4155/fmc-2018-0327DOI Listing

Rationale in diagnosis and management: role of screening and history taking.

Trop Doct 2019 Apr 18:49475519841749. Epub 2019 Apr 18.

2 Assistant Professor, Department of Pharmacology, All India Institute of Medical Sciences, Raipur, Chhattisgarh, India.

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http://dx.doi.org/10.1177/0049475519841749DOI Listing

Perspectives on gender parity in bioanalysis: an interview with Atreyee Sims.

Authors:
Atreyee Sims

Bioanalysis 2019 Apr 18. Epub 2019 Apr 18.

PRA Health Sciences, 11070 Strang Line Road, Lenexa, KS 66215, USA.

Biography Atreyee Sims is an accomplished and committed GCP/GLP trained Project Manager overseeing Phase I-III clinical trials with a strong scientific acumen in pharmacology, microbiology and molecular biology. Project delivery emboldened by 10 years' experience as a Clinical Laboratory Scientist and Microbiologist with more than ten published peer-reviewed manuscripts. Spearheads project leadership role in GCP/GLP and protocol-compliant tracking of project results, implements data collection procedures and verifies project data to ensure timely delivery with the highest priority of both subject safety and data integrity. Read More

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https://www.future-science.com/doi/10.4155/bio-2019-0054
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http://dx.doi.org/10.4155/bio-2019-0054DOI Listing
April 2019
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Development and validation of indirect and generic immunoassays to quantify free and total evolocumab in rat serum.

Bioanalysis 2019 Apr 18. Epub 2019 Apr 18.

Key Laboratory of Molecular Pharmacology & Drug Evaluation, School of Pharmacy, Yantai University, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System & Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, PR China.

Evolocumab is a human monoclonal antibody used in the treatment of cardiovascular diseases, which targeted proprotein convertase subtilisin kexin type 9. To accurately quantify free (including partially bound) and total evolocumab concentrations in serum, indirect and generic ELISA methods were developed and validated in rat serum. Indirect ELISA was accurate and precise over the concentration range of 23. Read More

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http://dx.doi.org/10.4155/bio-2019-0003DOI Listing

Interactions between Clotrimazole and selected essential oils against Malassezia pachydermatis clinical isolates.

Pol J Vet Sci 2019 Mar;22(1):173-175

Department of Pharmacology and Toxicology, University of Veterinary Medicine and Pharmacy in Kosice, Komenskeho 73, 041 81 Kosice, Slovak Republic.

The aim of this study was to investigate interactions between conventional antifungal drug and essential oils against isolates of Malassezia pachydermatis. Antifungal activity of Cinnamomum cassia, Melaleuca alternifolia, Mentha piperita, Origanum vulgare and Syzygium aromaticum essential oils were tested against 19 strains of M. pachydermatis isolated from healthy dogs and reference strain M. Read More

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http://dx.doi.org/10.24425/pjvs.2019.127082DOI Listing

Asprosin attenuates insulin signaling pathway through PKCδ-activated ER stress and inflammation in skeletal muscle.

J Cell Physiol 2019 Apr 17. Epub 2019 Apr 17.

Department of Pharmacology, College of Medicine, Chung-Ang University, Seoul, Republic of Korea.

It has been reported that asprosin is a novel adipokine which is augmented in mice and humans with type 2 diabetes (T2DM). Asprosin stimulates hepatic gluconeogenesis under fasting conditions. However, the roles of asprosin in inflammation, endoplasmic reticulum (ER) stress, and insulin resistance in skeletal muscle has not been studied. Read More

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http://dx.doi.org/10.1002/jcp.28694DOI Listing

Optimal Sampling Strategies for Therapeutic Drug Monitoring of First-Line Tuberculosis Drugs in Patients with Tuberculosis.

Clin Pharmacokinet 2019 Apr 17. Epub 2019 Apr 17.

Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, PO Box 30.001, 9700 RB, Groningen, The Netherlands.

Background: The 24-h area under the concentration-time curve (AUC)/minimal inhibitory concentration ratio is the best predictive pharmacokinetic/pharmacodynamic (PK/PD) parameter of the efficacy of first-line anti-tuberculosis (TB) drugs. An optimal sampling strategy (OSS) is useful for accurately estimating AUC; however, OSS has not been developed in the fed state or in the early phase of treatment for first-line anti-TB drugs.

Methods: An OSS for the prediction of AUC of isoniazid, rifampicin, ethambutol and pyrazinamide was developed for TB patients starting treatment. Read More

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http://dx.doi.org/10.1007/s40262-019-00763-3DOI Listing

Unavailable prescriptions at Danish community pharmacies: A descriptive study.

Int J Clin Pharm 2019 Apr 17. Epub 2019 Apr 17.

Hospital Pharmacy Funen, Odense University Hospital, Solfaldsvej 38, Entrance 208, 5000, Odense C, Denmark.

Background Handling of unavailable prescriptions, i.e. prescriptions missing on the online server, is considered troublesome and time-consuming by community pharmacy staff and may result in both patient dissatisfaction and non-compliance. Read More

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http://dx.doi.org/10.1007/s11096-019-00831-5DOI Listing

Paediatric reference intervals are heterogeneous and differ considerably in the classification of healthy paediatric blood samples.

Eur J Pediatr 2019 Apr 17. Epub 2019 Apr 17.

Department of Clinical Biochemistry and Pharmacology, Odense University Hospital, 5000, Odense, Denmark.

The aim was to elude differences in published paediatric reference intervals (RIs) and the implementations hereof in terms of classification of samples. Predicaments associated with transferring RIs published elsewhere are addressed. A local paediatric (aged 0 days to < 18 years) population of platelet count, haemoglobin level and white blood cell count, based on first draw samples from general practitioners was established. Read More

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http://dx.doi.org/10.1007/s00431-019-03377-wDOI Listing

Systemic pharmacokinetic/pharmacodynamic analysis of intravitreal aflibercept injection in patients with retinal diseases.

BMJ Open Ophthalmol 2019 20;4(1):e000185. Epub 2019 Mar 20.

Bayer Pharma, Berlin, Germany.

Objective: Explore relationships between systemic exposure to intravitreal aflibercept injection (IAI) and systemic pharmacodynamic effects via post hoc analyses of clinical trials of IAI for neovascular age-related macular degeneration (nAMD) or diabetic macular oedema (DME).

Methods And Analysis: Adults from VGFT-OD-0702.PK (n=6), VGFT-OD-0512 (n= 5), VIEW 2 (n=1204) and VIVID-DME (n=404) studies were included. Read More

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http://dx.doi.org/10.1136/bmjophth-2018-000185DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6440611PMC

Pediatric melanoma-The whole (conflicts of interest) story.

Int J Womens Dermatol 2019 Jun 19;5(2):110-115. Epub 2018 Nov 19.

University of Connecticut Health Center, Farmington, Connecticut.

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http://dx.doi.org/10.1016/j.ijwd.2018.10.020DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451736PMC

Tunicates as a biocontrol tool for larvicides acute toxicity of Zika virus vector .

3 Biotech 2019 May 9;9(5):172. Epub 2019 Apr 9.

4Department of Zoology, Ryan Institute, School of Natural Science, National University of Ireland, Galway, Ireland.

In this present study, we conducted untargeted metabolic profiling using gas chromatography-mass spectrometry (GC-MS) analysis of ascidian to assess the chemical constituents by searching in NIST library with promising biological properties against anti-bacterial and Zika virus vector mosquitocidal properties. Metabolites, steroids and fatty acids are abundant in crude compounds of ascidian and showed potential zone growth inhibition against bacterial strains (10 mm). The active crude compounds of exhibited prominent larvicidal activity against the Zika vector mosquitoes of (LC values of 0. Read More

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http://dx.doi.org/10.1007/s13205-019-1699-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6456632PMC

Bisphenol-A induced oxidative stress, inflammatory gene expression, and metabolic and histopathological changes in male Wistar albino rats: protective role of boron.

Toxicol Res (Camb) 2019 Mar 23;8(2):262-269. Epub 2019 Jan 23.

China Agricultural University , College of Veterinary Medicine , Beijing, National Center for Veterinary Drug Safety Evaluation , 100193 , China.

Bisphenol A (BPA) is one of the most produced chemicals in the world and has been widely employed in the food industry. Continuous and widespread exposure to BPA through drinking water and food leads to health concerns for humans. This study evaluated the effects of boron (B) on BPA-mediated oxidative stress in male Wistar albino rats. Read More

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http://dx.doi.org/10.1039/c8tx00312bDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6425992PMC

Protective effects of resveratrol on biomarkers of oxidative stress, biochemical and histopathological changes induced by sub-chronic oral glyphosate-based herbicide in rats.

Toxicol Res (Camb) 2019 Mar 7;8(2):238-245. Epub 2019 Jan 7.

Department of Pharmacology and Toxicology , Faculty of Veterinary Medicine , University of Afyon Kocatepe , Afyonkarahisar , Turkey . Email: ; Email: ; ; Tel: +90272281312-2798.

The aim of this sub-chronic toxicity study is to determine the protective effects of Resveratrol (Res) on oxidative stress, biochemical and histopathological changes induced by glyphosate-based herbicide (GBH) in the blood, brain, heart, liver and renal tissues. A total of 28 male Wistar rats were equally divided into 4 groups so that each group included 7 rats. In the study, Group I (control group) was given normal rodent feed and tap water . Read More

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http://xlink.rsc.org/?DOI=C8TX00287H
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http://dx.doi.org/10.1039/c8tx00287hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6417488PMC
March 2019
1 Read

Chronic low-level cadmium exposure in rats affects cytokine production by activated T cells.

Toxicol Res (Camb) 2019 Mar 4;8(2):227-237. Epub 2019 Jan 4.

Department of Pharmacology & Toxicology , Michigan State University , East Lansing , MI 48824 , USA . Email: ; Tel: +517-884-6692.

Cadmium is a toxic metal and common environmental contaminant. Chronic cadmium exposure results in kidney, bone, reproductive, and immune toxicity as well as cancer. Cadmium induces splenomegaly and affects the adaptive immune system, but specific effects vary depending on the dose, model, and endpoint. Read More

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http://dx.doi.org/10.1039/c8tx00194dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6425995PMC

Lipid-independent control of endothelial and neuronal TRPC3 channels by light.

Chem Sci 2019 Mar 15;10(9):2837-2842. Epub 2019 Jan 15.

Gottfried Schatz Research Center - Biophysics , Medical University of Graz , Neue Stiftingtalstraße 6/D/04 , 8010 Graz , Austria . Email:

Lipid-gated TRPC channels are highly expressed in cardiovascular and neuronal tissues. Exerting precise pharmacological control over their activity in native cells is expected to serve as a basis for the development of novel therapies. Here we report on a new photopharmacological tool that enables manipulation of TRPC3 channels by light, in a manner independent of lipid metabolism and with higher temporal precision than lipid photopharmacology. Read More

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http://dx.doi.org/10.1039/c8sc05536jDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427946PMC

Photolysis of cell-permeant caged inositol pyrophosphates controls oscillations of cytosolic calcium in a β-cell line.

Chem Sci 2019 Mar 10;10(9):2687-2692. Epub 2019 Jan 10.

University of Freiburg , Institute of Organic Chemistry , 79104 Freiburg , Germany . Email:

Among many cellular functions, inositol pyrophosphates (PP-InsPs) are metabolic messengers involved in the regulation of glucose uptake, insulin sensitivity, and weight gain. However, their mechanisms of action are still poorly understood. So far, the influence of PP-InsPs on cellular metabolism has been studied by overexpression or knockout/inhibition of relevant metabolizing kinases (IP6Ks, PPIP5Ks). Read More

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http://dx.doi.org/10.1039/c8sc03479fDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6419925PMC

Light emission enhancement by supramolecular complexation of chemiluminescence probes designed for bioimaging.

Chem Sci 2019 Mar 16;10(10):2945-2955. Epub 2019 Jan 16.

School of Chemistry , Raymond and Beverly Sackler Faculty of Exact Sciences , Israel . Email:

Chemiluminescence offers advantages over fluorescence for bioimaging, since an external light source is unnecessary with chemiluminescent agents. This report demonstrates the first encapsulation of chemiluminescence phenoxy-adamantyl-1,2-dioxetane probes with trimethyl β-cyclodextrin. Clear proof for the formation of a 1 : 1 host-guest complex between the adamantyl-1,2-dioxetane probe and trimethyl β-cyclodextrin was provided by mass spectroscopy and NMR experiments. Read More

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http://dx.doi.org/10.1039/c8sc05174gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427943PMC

Rationally synthesized coumarin based pyrazolines ameliorate carrageenan induced inflammation through COX-2/pro-inflammatory cytokine inhibition.

Medchemcomm 2019 Mar 23;10(3):421-430. Epub 2019 Jan 23.

Department of Pharmaceutical Chemistry , ISF College of Pharmacy , Moga-142001 , Punjab , India . Email: ; ; Tel: +91 1636 324200.

In the present work, coumarin based pyrazolines () have been synthesized and investigated for their and anti-inflammatory potential. Amongst the synthesized compounds, compounds , and exhibited significant anti-inflammatory activity as compared to the standard etoricoxib. Keeping this in mind, investigations were carried out carrageenan induced inflammation and acetic acid induced writhing models in male Wistar rats and compound was found to possess appreciable anti-inflammatory and analgesic potential. Read More

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http://dx.doi.org/10.1039/c8md00457aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6430084PMC

Stereoselective Synthesis of C-2 Alkylated Trihydroxypiperidines: Novel Pharmacological Chaperones for Gaucher Disease.

ACS Med Chem Lett 2019 Apr 8;10(4):621-626. Epub 2019 Feb 8.

Department of Chemistry "Ugo Schiff", University of Firenze, via della Lastruccia n. 3-13, 50019 Sesto Fiorentino (FI), Italy.

Pharmacological chaperones (PCs) are small molecules that bind and stabilize enzymes. They can rescue the enzymatic activity of misfolded or deficient enzymes when they are used at subinhibitory concentration, thus with minimal side effects. Pharmacological Chaperone Therapy (PCT) is an emerging treatment for many lysosomal storage disorders (LSDs) including Gaucher disease, the most common, which is characterized by a deficiency in the GCase enzyme. Read More

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http://dx.doi.org/10.1021/acsmedchemlett.8b00602DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6467014PMC

EC18 as a Tool To Understand the Role of HCN4 Channels in Mediating Hyperpolarization-Activated Current in Tissues.

ACS Med Chem Lett 2019 Apr 6;10(4):584-589. Epub 2019 Feb 6.

Department of Neurosciences, Psychology, Drug Research and Child Health (NeuroFarBa), University of Florence, Florence 50139, Italy.

Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are membrane proteins encoded by four genes (HCN1-4) and widely distributed in the central and peripheral nervous system and in the heart. HCN channels are involved in several physiological functions, including the generation of rhythmic activity, and are considered important drug targets if compounds with isoform selectivity are developed. At present, however, few compounds are known, which are able to discriminate among HCN channel isoforms. Read More

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00587
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http://dx.doi.org/10.1021/acsmedchemlett.8b00587DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466822PMC
April 2019
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Proof-of-Concept Multistage Biomimetic Liposomal DNA Origami Nanosystem for the Remote Loading of Doxorubicin.

ACS Med Chem Lett 2019 Apr 31;10(4):517-521. Epub 2019 Jan 31.

Clinical and Experimental Pharmacology Unit, IRCCS CRO Aviano-National Cancer Institute, 33081 Aviano, Italy.

One of the most promising applications of DNA origami is its use as an excellent evolution of nanostructured intelligent systems for drug delivery, but short lifetime and immune-activation are still major challenges to overcome. On the contrary, stealth liposomes have long-circulation time and are well tolerated by the immune system. To overcome DNA origami limitations, we have designed and synthesized a compact short tube DNA origami (STDO) of approximately 30 nm in length and 10 nm in width. Read More

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http://dx.doi.org/10.1021/acsmedchemlett.8b00557DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466551PMC

Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: and Biological Profile.

ACS Med Chem Lett 2019 Apr 8;10(4):450-456. Epub 2019 Mar 8.

Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.

In this work we report the application of the ring-closing metathesis (RCM) to the preparation of two cyclic olefin-bridged analogues of biphalin (Tyr-d-Ala-Gly-Phe-NH-NH ← Phe ← Gly ← d-Ala ← Tyr), using the second generation Grubbs' catalyst. The resulting - and -cyclic isomers were identified, fully characterized, and tested at μ (ΜΟR), δ (DOR), and κ (KOR) opioid receptors and for antinociceptive activity. Both were shown to be full agonists at MOR and potential partial antagonists at DOR, with low potency KOR agonism. Read More

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http://dx.doi.org/10.1021/acsmedchemlett.8b00495DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466526PMC

Angina and left ventricular dysfunction: can we 'reduce' it?

Eur Heart J Suppl 2019 Apr 10;21(Suppl C):C28-C31. Epub 2019 Apr 10.

Department of Medical Sciences Ferrara University, Ferrara, Italy.

Despite the evolution in pharmacology and devices, recurrent and persistent angina still represent a frequent issue in clinical practice. A 69-year-old Caucasian female patient has history of surgical aortic valve replacement with a bioprosthesis for severe aortic stenosis with subsequent transcatheter valve-in-valve implantation for bioprosthesis degeneration and single coronary artery bypass graft with left internal mammary artery on left anterior descending (LAD). After transcatheter aortic valve implantation, she started to complain angina [Canadian Cardiovascular Society (CCS) Class III], effectively treated with bisoprolol uptitration and ivabradine 5 b. Read More

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http://dx.doi.org/10.1093/eurheartj/suz045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6456877PMC

Population-based study of early-onset neonatal sepsis in Canada.

Paediatr Child Health 2019 May 24;24(2):e66-e73. Epub 2018 Apr 24.

Keenan Research Centre of the Li Ka Shing Knowledge Institute, St Michael's Hospital, Toronto, Ontario.

Objective: To determine the incidence, types of organisms and resistance patterns involved in early-onset neonatal sepsis in Canada.

Study Design: Early-onset neonatal sepsis cases were identified through the Canadian Paediatric Surveillance Program. Neonates were excluded if they were asymptomatic or if intracranial procedures preceded a positive cerebrospinal fluid culture. Read More

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http://dx.doi.org/10.1093/pch/pxy018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6462127PMC

[Chronic phosphoproteomic in temporal lobe epilepsy mouse models induced by kainic acid].

Beijing Da Xue Xue Bao Yi Xue Ban 2019 Apr;51(2):197-205

Institute of Systems Biomedicine, State Key Laboratory of Natural and Biomimetic Drugs, Department of Molecular and Cellular Pharmacology, Peking University School of Pharmaceutical Science, Beijing 100191, China.

Objective: To investigate functions of proteins and signaling pathways involved in epileptogenesis during the chronic stage of temporal lobe epilepsy in mouse models.

Methods: Kainic acid-induced temporal lobe epilepsy models were conducted, when reaching stage 4 using racine scale, the mice of experimental group were supposed to be successfully established. Pentobarbital sodium was injected to stop epileptic seizure in case of death. Read More

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