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https://www.readbyqxmd.com/read/28549321/studies-on-free-radical-scavenging-cancer-cell-antiproliferation-and-calf-thymus-dna-interaction-of-schiff-bases
#1
Cleiton M da Silva, Marina M Silva, Fabiano S Reis, Ana Lúcia T G Ruiz, João E de Carvalho, Josué C C Santos, Isis M Figueiredo, Rosemeire B Alves, Luzia V Modolo, Ângelo de Fátima
Thirty-nine Schiff bases were synthesized by performing microwave-assisted condensation of the corresponding aldehydes and aromatic amines. Their reactive nitrogen species (RNS) scavenging activity and inhibitory effects against cancer cell growth were then subsequently investigated. Additionally, the interaction between the calf thymus DNA (ctDNA) and selected Schiff bases was evaluated using fluorescence spectroscopy, and their binding parameters were determined. The yields of the various compounds ranged from moderate to excellent (43-99%) after only a 2-min reaction...
May 17, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28549309/switching-between-intravenous-and-subcutaneous-trastuzumab-safety-results-from-the-prefher-trial
#2
Joseph Gligorov, Giuseppe Curigliano, Volkmar Müller, Ann Knoop, Valerie Jenkins, Sunil Verma, Stuart Osborne, Sabine Lauer, Zuzana Machackova, Lesley Fallowfield, Xavier Pivot
AIM: To assess the safety and tolerability of switching between subcutaneous (SC) and intravenous (IV) trastuzumab in the PrefHer study (NCT01401166). PATIENTS AND METHODS: Patients with HER2-positive early breast cancer completed (neo)adjuvant chemotherapy and were randomised to receive four cycles of SC trastuzumab, via single-use injection device (SID; Cohort 1) or hand-held syringe (Cohort 2), followed by four cycles of IV, or vice versa (the crossover period presented here) as part of their 18 standard cycles of adjuvant trastuzumab treatment...
May 23, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/28549301/ecotoxicological-effect-of-ketamine-evidence-of-acute-chronic-and-photolysis-toxicity-to-daphnia-magna
#3
Shih-Wei Li, Yu-Hsiang Wang, Angela Yu-Chen Lin
Ketamine has been increasingly used in medicine and has the potential for abuse or illicit use around the world. Ketamine cannot be removed by conventional wastewater treatment plants. Although ketamine and its metabolite norketamine have been detected to a significant degree in effluents and aquatic environments, their ecotoxicity effects in aquatic organisms remain undefined. In this study, we investigated the acute toxicity of ketamine and its metabolite, along with the chronic reproductive toxicity of ketamine (5-100μg/L) to Daphnia magna...
May 23, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28549219/design-synthesis-and-properties-of-a-potent-inhibitor-of-pseudomonas-aeruginosa-deacetylase-lpxc
#4
Grazia Piizzi, David T Parker, Yunshan Peng, Markus Rolf Dobler, Anup Patnaik, Som Wattanasin, Eugene Liu, Francois Lenoir, Jill Nunez, John Kerrigan, David McKenney, Colin S Osborne, Donghui Yu, Leanne Lanieri, Jade Bojkovic, JoAnne Dzink-Fox, Maria-Dawn Lilly, Elizabeth R Sprague, Yipin Lu, Hongming Wang, Srijan Ranjitkar, Bing Wang, Meir Glick, Lawrence G Hamann, Ruben Tommasi, Xia Yang, Charles R Dean
Over the past several decades the frequency of antibacterial resistance in hospitals, including multi-drug resistance (MDR) and its association with serious infectious diseases, has increased at alarming rates. Pseudomonas aeruginosa is a leading cause of nosocomial infections, and resistance to virtually all approved antibacterial agents is emerging in this pathogen. To address the need for new agents to treat MDR P. aeruginosa, we focused on inhibiting the first committed step in the biosynthesis of lipid A, the deacetylation of uridyldiphospho-3-O-(R-hydroxydecanoyl)-N-acetylglucosamine by the enzyme LpxC...
May 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28549173/incidental-mosquitocidal-effect-of-an-ivermectin-mass-drug-administration-on-anopheles-farauti-conducted-for-scabies-control-in-the-solomon-islands
#5
Christian Kositz, Jeptah Talina, Jason Diau, Rowena Asugeni, Cheryl Whitehorn, David Mabey, Carlos Chaccour, Michael Marks
Background: The Solomon Islands is targeting elimination of malaria by 2030. The dominant vector is the predominantly exophagic, exophilic Anopheles farauti sensu strictu. This biting behaviour limits the efficacy of conventional vector control tools and highlights the need for new strategies. When administered to humans ivermectin has been shown to have a mosquitocidal effect. Mass drug administration (MDA) with ivermectin is an emerging strategy in the control of scabies. In this study we explored any incidental effect of ivermectin MDA conducted for scabies control on mosquitoes...
May 26, 2017: Transactions of the Royal Society of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28548925/immunological-consequences-of-ageing-microvascular-hemodynamic-changes-in-view-of-cancer-development-and-treatment
#6
REVIEW
Jinhyuk Fred Chung, Sang Joon Lee, Anil K Sood
Risk factors of cardiovascular diseases have long been implicated as risk factors for carcinogenesis, but clear explanations for their association have not been presented. In this article, fundamental concepts from carcinogenesis, microvascular hemodynamics, and immunity are collectively reviewed and analyzed in context of the known features of vascular ageing effects, in formulating a theory that suggests reduced microvascular immunity as an important driving factor for carcinogenesis. Furthermore, scientific, preclinical, and clinical evidence that support this new theory are presented in an interdisciplinary manner, offering new explanations to previously unanswered factors that impact cancer risks and its treatment outcome such as chronic drug use, temperature, stress and exercise effects among others...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28548833/structure-activity-relationship-for-small-molecule-inhibitors-of-nicotinamide-n-methyltransferase
#7
Harshini Neelakantan, Hua-Yu Wang, Virginia Vance, Jonathan D Hommel, Stanton F McHardy, Stanley J Watowich
Nicotinamide N-methyltransferase (NNMT) is a fundamental cytosolic biotransforming enzyme that catalyzes the N-methylation of endogenous and exogenous xenobiotics. We have identified small molecule inhibitors of NNMT with >1000-fold range of activity and developed comprehensive structure-activity relationships (SARs) for NNMT inhibitors. Screening of N-methylated quinolinium, isoquinolinium, pyrididium, and benzimidazolium/benzothiazolium analogs resulted in the identification of quinoliniums as a promising scaffold with very low micromolar (IC50 ~1 μM) NNMT inhibition...
May 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28548464/control-of-cell-death-and-mitochondrial-fission-by-erk1-2-map-kinase-signalling
#8
REVIEW
Simon J Cook, Kate Stuart, Rebecca Gilley, Matthew J Sale
The ERK1/2 signalling pathway is best known for its role in connecting activated growth factor receptors to changes in gene expression due to activated ERK1/2 entering the nucleus and phosphorylating transcription factors. However, active ERK1/2 also translocate to a variety of other organelles including the endoplasmic reticulum, endosomes, golgi and mitochondria to access specific substrates and influence cell physiology. In this article we review two aspects of ERK1/2 signalling at the mitochondria that are involved in regulating cell fate decisions...
May 26, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28548387/a-quantitative-systems-physiology-model-of-renal-function-and-blood-pressure-regulation-model-description
#9
K M Hallow, Y Gebremichael
Renal function plays a central role in cardiovascular, kidney, and multiple other diseases, and many existing and novel therapies act through renal mechanisms. Even with decades of accumulated knowledge of renal physiology, pathophysiology, and pharmacology, the dynamics of renal function remain difficult to understand and predict, often resulting in unexpected or counterintuitive therapy responses. Quantitative systems pharmacology modeling of renal function integrates this accumulated knowledge into a quantitative framework, allowing evaluation of competing hypotheses, identification of knowledge gaps, and generation of new experimentally testable hypotheses...
May 26, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28548370/current-state-of-a-dual-behavior-of-antimicrobial-peptides-therapeutic-agents-and-promising-delivery-vectors
#10
REVIEW
Urszula Piotrowska, Marcin Sobczak, Ewa Oledzka
Microorganism resistance is an important challenge in modern medicine due to the global uncontrolled use of antibiotics. Natural and synthetic antimicrobial peptides (AMPs) symbolize a new family of antibiotics, which have stimulated research and clinical interest as new therapeutic options for infections. They represent one of the most promising antimicrobial substances, due to their broad spectrum of biological activity, against bacteria, fungi, protozoa, viruses, yeast and even tumour cells. Besides, being antimicrobial, AMPs have been shown to bind and neutralize bacterial endotoxins, as well as possess immunomodulatory, anti-inflammatory, wound-healing, angiogenic and antitumour properties...
May 26, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28548229/endoplasmic-reticulum-stress-in-the-heart-the-insights-into-mechanisms-and-drug-targets
#11
REVIEW
Shunyao Wang, Pablo Binder, Qiru Fang, Zhenzhong Wang, Wei Xiao, Wei Liu, Xin Wang
The endoplasmic reticulum (ER) serves several essential cellular functions including protein synthesis, protein folding, protein translocation, calcium homoeostasis and lipid biosynthesis. Physiological or pathological stimuli which disrupt ER homoeostasis and disturb its functions lead to an accumulation of misfolded and unfolded proteins, a condition referred to as ER stress. ER stress triggers unfolded protein response (UPR) to restore the homoeostasis of ER through activating transcriptional and translational pathways...
May 26, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28548221/psilocybin-good-trip-or-bad-trip
#12
E M Sellers
Much of the history of pharmacology and therapeutics involves finding new uses for old drugs. The latest rediscovery is that of psychedelic drugs. Since they can cause profound distortions of perception and were once used as part of religious ceremonies, such research may seem unusual at this time.
May 26, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28548108/drugging-the-pain-epigenome
#13
REVIEW
Ellen Niederberger, Eduard Resch, Michael J Parnham, Gerd Geisslinger
More than 20% of adults worldwide experience different types of chronic pain, which are frequently associated with several comorbidities and a decrease in quality of life. Several approved painkillers are available, but current analgesics are often hampered by insufficient efficacy and/or severe adverse effects. Consequently, novel strategies for safe, highly efficacious treatments are highly desirable, particularly for chronic pain. Epigenetic mechanisms such as DNA methylation, histone modifications and microRNAs (miRNAs) strongly affect the regulation of gene expression, potentially for long periods over years or even generations, and have been associated with pathophysiological pain...
May 26, 2017: Nature Reviews. Neurology
https://www.readbyqxmd.com/read/28547936/fragment-based-drug-discovery-as-alternative-strategy-to-the-drug-development-for-neglected-diseases
#14
REVIEW
Juliana da Fonseca Rezende E Mello, Renan Augusto Gomes, Drielli Gomes Vital-Fujii, Glaucio Monteiro Ferreira, Gustavo Henrique Goulart Trossini
Neglected diseases (NDs) affect large populations and almost whole continents, representing 12% of the global health burden. In contrast, the treatment available today is limited and sometimes ineffective. Under this scenery, the Fragment-Based Drug Discovery (FBDD) emerged as one of the most promising alternatives to the traditional methods of drug development. This method allows achieving new lead compounds with smaller size of fragment libraries. Even with the wide Fragment-Based Drug Discovery success resulting in new effective therapeutic agents against different diseases, until this moment few studies have been applied this approach for NDs area...
May 26, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28547729/doctors-and-nurses-perceptions-of-a-ward-based-pharmacist-in-rural-northern-sweden
#15
Maria Sjölander, Maria Gustafsson, Gisselle Gallego
Background This project is part of the prospective quasi experimental proof-of-concept investigation of clinical pharmacist intervention study to reduce drug-related problems among people admitted to a ward in a rural hospital in northern Sweden. Objective To explore doctors' and nurses' perceptions and expectations of having a ward-based pharmacist providing clinical pharmacy services. Setting Medical ward in a rural hospital in northern Sweden. Method Eighteen face-to-face semi-structured interviews were conducted with a purposive sample of doctors and nurses working on the ward where the clinical pharmacy service was due to be implemented...
May 25, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28547521/validation-of-the-cingulate-island-sign-with-optimized-ratios-for-discriminating-dementia-with-lewy-bodies-from-alzheimer-s-disease-using-brain-perfusion-spect
#16
Etsuko Imabayashi, Tsutomu Soma, Daichi Sone, Tadashi Tsukamoto, Yukio Kimura, Noriko Sato, Miho Murata, Hiroshi Matsuda
OBJECTIVE: Dementia with Lewy bodies (DLB) is often cited as the second most common dementia after Alzheimer's disease (AD). It is clinically important to distinguish DLB from AD because specific side effects of antipsychotic drugs are limited to DLB. The relative preservation of cingulate glucose metabolism in the posterior cingulate gyri versus that in the precuni, known as the cingulate island sign (CIS), in patients with DLB compared with AD is supposed to be highly specific for diagnosing DLB...
May 25, 2017: Annals of Nuclear Medicine
https://www.readbyqxmd.com/read/28547246/indications-for-opioid-antagonists
#17
REVIEW
O J Michael Coppes, Christine N Sang
PURPOSE OF REVIEW: As opioids have become more common in clinical practice for the treatment of both acute and chronic pain, so too has the need for a deeper understanding of the clinical applications of opioid antagonists. The purpose of this review is to present both the longstanding and potential new indications for the use of drugs that block the effects of opioid receptors. RECENT FINDINGS: There is a growing body of data demonstrating the modulation of pain by opioid antagonists...
June 2017: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/28546954/pleiotropic-cytotoxicity-of-vaca-toxin-in-host-cells-and-its-impact-on-immunotherapy
#18
REVIEW
Farnaz Fahimi, Mohammad Reza Tohidkia, Mehdi Fouladi, Reza Aghabeygi, Naser Samadi, Yadollah Omidi
Introduction: In the recent decades, a number of studies have highlighted the importance of Helicobacter pylori in the initiation and development of peptic ulcer and gastric cancer. Some potential virulence factors (e.g., urease, CagA, VacA, BabA) are exploited by this microorganism, facilitating its persistence through evading human defense mechanisms. Among these toxins and enzymes, vacuolating toxin A (VacA) is of a great importance in the pathogenesis of H. pylori. VacA toxin shows different pattern of cytotoxicity through binding to different cell surface receptors in various cells...
2017: BioImpacts: BI
https://www.readbyqxmd.com/read/28546948/liquigroud-technique-a-new-concept-for-enhancing-dissolution-rate-of-glibenclamide-by-combination-of-liquisolid-and-co-grinding-technologies
#19
Leila Azharshekoufeh, Javad Shokri, Mohammad Barzegar-Jalali, Yousef Javadzadeh
Introduction: The potential of combining liquisolid and co-grinding technologies (liquiground technique) was investigated to improve the dissolution rate of a water-insoluble agent (glibenclamide) with formulation-dependent bioavailability. Methods: To this end, different formulations of liquisolid tablets with a wide variety of non-volatile solvents contained varied ratios of drug: solvent and dissimilar carriers were prepared, and then their release profiles were evaluated. Furthermore, the effect of size reduction by ball milling on the dissolution behavior of glibenclamide from liquisolid tablets was investigated...
2017: BioImpacts: BI
https://www.readbyqxmd.com/read/28546920/ocular-penetration-of-topically-applied-1-tigecycline-in-a-rabbit-model
#20
Yasar Sakarya, Rabia Sakarya, Muammer Ozcimen, Sertan Goktas, Serap Ozcimen, Ismail Alpfidan, Ismail Senol Ivacık, Erkan Erdogan, Servet Cetinkaya, Abdulkadir Bukus
AIM: To evaluate ocular penetration of topically applied 1% tigecycline. METHODS: Forty-two New Zealand White rabbits were divided into 3 groups. A 50 µL drop of 1% tigecycline was administered in group 1. In groups 2 and 3, the drop was administered every 15min for 60min (keratitis protocol). Aqueous humor samples in groups 1 and 2 were collected under general anesthesia at 15, 30, 45, 60, 120, and 180min after the last drop. All animals in group 3 were euthanatized...
2017: International Journal of Ophthalmology
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