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https://www.readbyqxmd.com/read/28545157/the-aminoestrogen-prolame-increases-recognition-memory-and-hippocampal-neuronal-spine-density-in-aged-mice
#1
Alfonso Diaz, Samuel Treviño, Rubén Vázquez-Roque, Berenice Venegas, Blanca Espinosa, Gonzalo Flores, Juan Manuel Fernández-G, Luis F Montaño, Jorge Guevara
The aging brain shows biochemical and morphological changes in the dendrites of pyramidal neurons from the limbic system associated with memory loss. Prolame (N-(3-hydroxy-1,3,5 (10) -estratrien-17β-yl) -3-hydroxypropylamine) is a non-feminizing aminoestrogen with antithrombotic activity that prevents neuronal deterioration, oxidative stress and neuroinflammation. Our aim was to evaluate the effect of prolame on motor and cognitive processes, as well as its influence on the dendritic morphology of neurons at the CA1, CA3 and granule cells of the dentate gyrus (DG) regions of hippocampus (HP), and medium spiny neurons of the nucleus accumbens (NAcc) of aged mice...
May 25, 2017: Synapse
https://www.readbyqxmd.com/read/28544960/anti-biofilm-effect-of-dihydromyricetin-loaded-nanocapsules-on-urinary-catheter-infected-by-pseudomonas-aeruginosa
#2
A J F Dalcin, C G Santos, S S Gündel, I Roggia, R P Raffin, A F Ourique, R C V Santos, P Gomes
Nosocomial infections associated with biofilm formation on urinary catheters are among the leading causes of complications due to biofilm characteristics and high antimicrobial resistance. An interesting alternative are natural products, such as Dihydromyricetin (DMY), a flavonoid which presents several pharmacological properties, including strong antimicrobial activity against various microorganisms. However, DMY, has low aqueous solubility and consequently low bioavailability. Nanoencapsulation can contribute to the improvement of characteristics of some drugs, by increasing the apparent solubility and sustained release has been reported among other advantages...
May 15, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28544938/sex-steroids-and-metabolic-responses-in-mussels-mytilus-galloprovincialis-exposed-to-drospirenone
#3
Tiziana Cappello, Denise Fernandes, Maria Maisano, Andrea Casano, Marta Bonastre, Maria João Bebianno, Angela Mauceri, Salvatore Fasulo, Cinta Porte
Drospirenone (DRO) is a synthetic progestin derived from 17α-spironolactone with a pharmacological mechanism of action similar to progesterone. Despite its wide use as pharmaceutical and consequent continuous release into the aquatic environment, DRO effects have been poorly investigated on aquatic biota. In order to unravel the toxicity mechanisms of DRO, mussels Mytilus galloprovincialis were exposed for 7 days to different concentrations of DRO, namely 20ng/L (Low; L), 200ng/L (Medium; M), 2000ng/L (High; H) and 10μg/L (Super High; SH) nominal doses...
May 22, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28544935/liquiritin-lt-exhibits-suppressive-effects-against-the-growth-of-human-cervical-cancer-cells-through-activating-caspase-3-in-vitro-and-xenograft-mice-in-vivo
#4
She-Hong He, Hong-Gai Liu, Yu-Fei Zhou, Qing-Fen Yue
Cervical cancer is one of the most common female malignancies worldwide. Liquiritin (LT), a major constituent of Glycyrrhiza Radix, possesses a variety of pharmacological activities, including anti-cancer, anti-oxidative, anti-inflammatory and neuro-protective effects. However, its role in human cervical cancer remains to be elusive. In our study, we found that LT suppressed cervical cancer cell migration, invasion and cloning ability with little cytotoxicity to human normal cells. In addition, apoptosis was induced by LT in cervical cancer cells through activation of Caspase-3 and poly ADP-ribose polymerase (PARP) cleavage...
May 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28544774/safety-pharmacokinetics-and-pharmacodynamics-of-hetrombopag-olamine-a-novel-tpo-r-agonist-in-healthy-subjects
#5
Li Zheng, Mao-Zhi Liang, Xiao-Ling Zeng, Cai-Zheng Li, Yi-Fan Zhang, Xiao-Yan Chen, Xi Zhu, An-Bo Xiang
Hetrombopag olamine (hetrombopag) is a novel small-molecule, orally bioavailable, non-peptide thrombopoietin (TPO) receptor agonist that is being developed as the treatment for thrombocytopenia. Two randomized, placebo-controlled phase I studies were conducted in 72 healthy subjects to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of hetrombopag. Hetrombopag was orally administered with a single dose in 5 dose cohorts (5 mg, 10 mg, 20 mg, 30 mg or 40 mg) in the first study, and given once daily for 10 days in 3 dose cohorts (2...
May 24, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28544619/design-and-synthesis-of-some-acridine-piperazine-hybrids-for-the-improvement-of-cognitive-dysfunction
#6
Anuradha Sharma, Poonam Piplani
A novel series of hybrid molecules (5a-5m) was designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against cognitive dysfunction. Heterocyclic moieties acridine and piperazine were conjugated with suitable linkers in a single scaffold and the structures of the target compounds were confirmed by IR, (1) H NMR, (13) C NMR and LC-MS analysis. The pharmacological activity of synthesized compounds was evaluated using behavioral models of amnesia viz. step down passive avoidance and elevated plus maze at a dose 0...
May 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28544541/identification-and-analysis-of-chemical-constituents-and-rat-serum-metabolites-in-suan-zao-ren-granule-using-ultra-high-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry-combined-with-multiple-data-processing-approaches
#7
Yiyang Du, Bosai He, Qing Li, Jiao He, Di Wang, Kaishun Bi
Suan-Zao-Ren granule is widely used to treat insomnia in China. However, because of the complexity and diversity of the chemical compositions in traditional Chinese medicine formula, the comprehensive analysis of constituents in vitro and in vivo are rather difficult. In our study, an ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry and the PeakView® software, which uses multiple data processing approaches including product ion filter, neutral loss filter and mass defect filter, method was developed to characterize the ingredients and rat serum metabolites in Suan-Zao-Ren granule...
May 24, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28544499/preventing-progression-from-gestational-diabetes-mellitus-to-diabetes-a-thought-filled-review
#8
REVIEW
Michal Kasher-Meron, Martin M Grajower
Women with a history of gestational diabetes (GDM) are at high risk for developing type 2 diabetes mellitus (T2DM). In studies with long periods of follow up, diabetes incidence of up to 70% has been reported. The appropriate follow up of women following a pregnancy complicated by GDM has not been studied. Published guidelines recommend that obstetrician/gynecologists, who are often the de facto primary care physicians for these otherwise healthy young women, make glucose monitoring in the post-partum period part of their annual examinations...
May 19, 2017: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/28544467/a-survey-on-the-beliefs-and-knowledge-of-gout-management-in-new-medical-graduates-new-south-wales-australia
#9
Matthew Terrill, John Riordan
AIM: To assess the beliefs and knowledge of gout management in new medical graduates. METHOD: A survey on gout management was sent to new medical graduates during their orientation week, New South Wales, Australia. RESULTS: Of 15 hospital networks, 11 agreed to participate. From these, 168 graduates responded (23.7% response rate). Most (81.1%) felt that gout was a serious disease, 51.2% answered that they had been taught adequately to manage acute gout, only 37...
May 25, 2017: International Journal of Rheumatic Diseases
https://www.readbyqxmd.com/read/28544245/ghrelin-receptor-inverse-agonists-as-a-novel-therapeutic-approach-against-obesity-related-metabolic-disease
#10
Kathrin Abegg, Lara Bernasconi, Melanie Hutter, Lynda Whiting, Claudio Pietra, Claudio Giuliano, Thomas A Lutz, Thomas Riediger
AIMS: Ghrelin is implicated in the control of energy balance and glucose homeostasis. The ghrelin receptor exhibits ligand independent constitutive activity, which can be pharmacologically exploited to induce inverse ghrelin actions. Since ghrelin receptor inverse agonists (GHSR-IA) might be effective for the treatment of obesity-related metabolic disease, we tested two novel synthetic compounds GHSR-IA1 and GHSR-IA2. MATERIALS AND METHODS: In functional cell assays, electrophysiogical and immunohistochemical experiments, we demonstrated inverse agonist activity for GHSR-IA1 and GHSR-IA2...
May 24, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28544082/a-resource-of-potential-drug-targets-and-strategic-decision-making-for-obstructive-sleep-apnoea-pharmacotherapy
#11
REVIEW
Richard L Horner, Kevin P Grace, Andrew Wellman
There is currently no pharmacotherapy for obstructive sleep apnoea (OSA) but there is no principled a priori reason why there should not be one. This review identifies a rational decision-making strategy with the necessary logical underpinnings that any reasonable approach would be expected to navigate to develop a viable pharmacotherapy for OSA. The process first involves phenotyping an individual to quantify and characterize the critical predisposing factor(s) to their OSA pathogenesis and identify, a priori, if the patient is likely to benefit from a pharmacotherapy that targets those factors...
May 25, 2017: Respirology: Official Journal of the Asian Pacific Society of Respirology
https://www.readbyqxmd.com/read/28544049/tone-identification-behavior-in-rattus-norvergicus-muscarinic-receptor-blockage-lowers-responsiveness-in-non-target-selective-neurons-while-nicotinic-receptor-blockage-selectively-lowers-target-responses
#12
Ezekiel P Carpenter-Hyland, Jackson Griffeth, Kristopher Bunting, Alvin Terry, Almira Vazdarjanova, David T Blake
Learning to associate a stimulus with reinforcement causes plasticity in primary sensory cortex. Neural activity caused by the associated stimulus is paired with reinforcement, but population analyses have not found a selective increase in response to that stimulus. Responses to other stimuli increase as much as, or more than, responses to the associated stimulus. Here, we applied population analysis at a new time point, and additionally evaluated whether cholinergic receptor blockers interacted with the plastic changes in cortex...
May 24, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28543813/inhaled-pulmonary-vasodilator-therapy-for-management-of-right-ventricular-dysfunction-after-left-ventricular-assist-device-placement-and-cardiac-transplantation
#13
Leah A Sabato, David M Salerno, Jeremy D Moretz, Douglas L Jennings
Right ventricular failure (RVF) after cardiac transplant (CTX) or implantation of a continuous-flow left ventricular assist device (CF-LVAD) is associated with significant post-operative morbidity and mortality. A variety of modalities have been used to treat post-operative RVF, including management of volume status, intravenous inotropes and vasodilators, and right-sided mechanical support. Inhaled vasodilator agents are a unique treatment option aimed at minimizing systemic absorption by delivering therapy directly to the pulmonary vasculature...
May 24, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28543679/the-missing-the-short-and-the-long-l-dopa-responses-and-dopamine-actions
#14
Roger L Albin, Daniel K Leventhal
We attempt to correlate the clinical pharmacology of dopamine replacement therapy (DRT) in Parkinson Disease with known features of striatal dopamine actions. Despite its obvious impact, DRT does not normalize motor function, likely due to disrupted phasic dopaminergic signaling. The DRT Short Duration Response is likely a permissive-paracrine effect, possibly resulting from dopaminergic support of corticostriate synaptic plasticity. The DRT Long Duration Response may result from mimicry of tonic dopamine signaling regulation of movement vigor...
May 22, 2017: Annals of Neurology
https://www.readbyqxmd.com/read/28543360/relationship-between-the-uplc-q-tof-ms-fingerprinted-constituents-from-daphne-genkwa-and-their-anti-inflammatory-anti-oxidant-activities
#15
Wen-Juan Du, Jun Ji, Ling Wang, Xin-Yi Lan, Jia Li, Jun-Qiu Lei, Xin He, Chun-Feng Zhang, Wen-Ze Huang, Zhen-Zhong Wang, Wei Xiao, Chong-Zhi Wang, Chun-Su Yuan
Daphne genkwa Sieb.et Zucc. is a well-known medicinal plant. This study was designed to apply the ultra-high performance liquid chromatography (UPLC) system to establish a quality control method of Daphne genkwa. Data revealed that there were fifteen common peaks in ten batches of D. genkwa Sieb. Et Zucc.(Thymelaeaceae) from different provinces of China. On this basis, the fingerprint chromatogram was established to provide references for quality control. Afterwards, the chemical constitutions of these common peaks were analyzed using the UPLC-Q-TOF-MS system and nine of them were identified primarily...
May 22, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28543193/patterns-of-anaphylaxis-after-diagnostic-work-up-a-follow-up-study-of-226-patients-with-suspected-anaphylaxis
#16
Athamaica Ruiz Oropeza, Carsten Bindslev-Jensen, Sigurd Broesby-Olsen, Thomas Kristensen, Michael Boe Møller, Hanne Vestergaard, Henrik Fomsgaard Kjaer, Susanne Halken, Annmarie Lassen, Charlotte G Mortz
BACKGROUND: Most published studies on anaphylaxis are retrospective or register based. Data on subsequent diagnostic work-up are sparse. We aimed to characterize patients seen with suspected anaphylaxis at the emergency care setting (ECS), after subsequent diagnostic work-up at our Allergy Center (AC). METHODS: Prospective study including patients from the ECS, Odense University Hospital, during May 2013-April 2014. Possible anaphylaxis cases were daily identified based on a broad search profile including history and symptoms in patient records, diagnostic codes and pharmacological treatments...
May 19, 2017: Allergy
https://www.readbyqxmd.com/read/28542844/the-inward-rectifier-current-inhibitor-pa-6-terminates-atrial-fibrillation-and-does-not-cause-ventricular-arrhythmias-in-dedicated-goat-and-dog-models
#17
Yuan Ji, Rosanne Varkevisser, Dragan Opacic, Alexandre Bossu, Marion Kuiper, Jet D M Beekman, Sihyung Yang, Azinwi Phina Khan, Dobromir Dobrev, Niels Voigt, Michael Zhuo Wang, Sander Verheule, Marc A Vos, Marcel A G Van der Heyden
BACKGROUND AND PURPOSE: Inward rectifier current (IK1 ) density increases in atrial fibrillation (AF), shortening effective refractory period and thus promotes atrial reentry. Pentamidine-Analogue 6 (PA-6) is a selective and potent IK1 inhibitor. We tested PA-6 for anti-AF efficacy and potential proarrhythmia, in established large animal models. EXPERIMENTAL APPROACH: PA-6 was applied i.v. in anaesthetized goats with rapid pacing induced AF and anaesthetized chronic AV block dogs...
May 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28542801/serum-protein-binding-of-25-antiepileptic-drugs-in-a-routine-clinical-setting-a-comparison-of-free-non-protein-bound-concentrations
#18
Philip N Patsalos, Miguel Zugman, Charlotte Lake, Anthony James, Neville Ratnaraj, Josemir W Sander
OBJECTIVE: Given that only the free non-protein-bound concentration of an antiepileptic drug (AED) crosses the blood-brain barrier, entering the brain and producing an antiepileptic effect, knowledge and measurement of the free drug fraction is important. Such data are sparse, particularly for newer AEDs, and have arisen from the use of disparate methodologies and settings over the past six decades. We report on the protein binding of 25 AEDs that are available for clinical use, along with two pharmacologically active metabolites (carbamazepine-epoxide and N-desmethyl clobazam), using standardized methodology and under set conditions...
May 24, 2017: Epilepsia
https://www.readbyqxmd.com/read/28542663/-periorbital-pallor-post-application-of-mydriatic-in-infants-with-hydrocephalus-associated-to-systemic-effects
#19
Jorge Luis Alvarado Socarras, Sandra Consuelo Rodríguez
Adequate pupil dilation is needed to evaluate some neonates at risk of developing illness during this stage. However, this procedure is not free of adverse effects, either local or systemic. One of these complications is the local vasoconstriction of the preterm baby’s skin following the application of mydriatic eye drops. OBJECTIVE: To describe secondary local and systemic complications of pharmacological pupil dilation in 2 newborns. Clinical case 1: Full term baby with diagnosis of low-birth weight and hydrocephalia...
April 2017: Revista Chilena de Pediatría
https://www.readbyqxmd.com/read/28542523/impact-of-maintenance-immunosuppressive-therapy-on-the-fecal-microbiome-of-renal-transplant-recipients-comparison-between-an-everolimus-and-a-standard-tacrolimus-based-regimen
#20
Gianluigi Zaza, Alessandra Dalla Gassa, Giovanna Felis, Simona Granata, Sandra Torriani, Antonio Lupo
BACKGROUND: The gut microbiome is the full set of microbes living in the gastrointestinal tract and is emerging as an important dynamic/fluid system that, if altered by environmental, dietetic or pharmacological factors, could considerably influence drug response. However, the immunosuppressive drug-induced modifications of this system are still poorly defined. METHODS: We employed an innovative bioinformatics approach to assess differences in the whole-gut microbial metagenomic profile of 20 renal transplant recipients undergoing maintenance treatment with two different immunosuppressive protocols...
2017: PloS One
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