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https://www.readbyqxmd.com/read/29786944/design-synthesis-and-evaluation-of-a-novel-series-of-inhibitors-reversing-p-glycoprotein-mediated-multidrug-resistance
#1
Hesham Ghaleb, Huilan Li, Mutta Kairuki, Qianqian Qiu, Xinzhou Bi, Chunxia Liu, Chen Liao, Jieming Li, Kamal Hezam, Wenlong Huang, Hai Qian
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR-reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells...
May 22, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29785610/evaluation-of-strategies-for-the-assessment-of-drug-drug-interactions-involving-cytochrome-p450-enzymes
#2
Jelle Reinen, Martijn Smit, Mira Wenker
BACKGROUND AND OBJECTIVES: Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study, the use of various human liver microsomes (HLM)-based methods to determine occurrence of CYP-mediated metabolism-dependent inhibition (MDI) and possible follow-up studies were evaluated...
May 21, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29784011/extremely-low-frequency-electromagnetic-fields-promote-mesenchymal-stem-cell-migration-by-increasing-intracellular-ca-2-and-activating-the-fak-rho-gtpases-signaling-pathways-in-vitro
#3
Yingchi Zhang, Jiyuan Yan, Haoran Xu, Yong Yang, Wenkai Li, Hua Wu, Chaoxu Liu
BACKGROUND: The ability of mesenchymal stem cells (MSCs) to migrate to the desired tissues or lesions is crucial for stem cell-based regenerative medicine and tissue engineering. Optimal therapeutics for promoting MSC migration are expected to become an effective means for tissue regeneration. Electromagnetic fields (EMF), as a noninvasive therapy, can cause a lot of biological changes in MSCs. However, whether EMF can promote MSC migration has not yet been reported. METHODS: We evaluated the effects of EMF on cell migration in human bone marrow-derived MSCs...
May 21, 2018: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/29779481/absorptive-and-secretory-transport-of-selected-artemisinin-derivatives-across-caco-2-cell-monolayers
#4
Jaco Heyns, Clarissa Willers, Richard K Haynes, Ho N Wong, Josias H Hamman, Chrisna Gouws
Malaria continues to be a major health concern and affects more than 200 million people a year. Drugs currently used for treatment of malaria are increasingly rendered ineffectual by the ongoing emergence of parasite resistance. For any new drugs, however, knowledge of their membrane permeability is an essential pre-requisite for eventual use. Treatment failure and emergence of resistance can occur as a result of reduced availability of the drug at the desired site of action. Cell-based permeability assays such as Caco-2 cell monolayers serve as a model for predicting drug absorption and efflux, and provide an estimate of drug bioavailability...
May 18, 2018: Current Drug Delivery
https://www.readbyqxmd.com/read/29779467/calcium-sodium-and-trp-channel-expression-in-human-fetal-midbrain-derived-neural-progenitor-cells
#5
Nancy Stanslowsky, Salini Tharmarasa, Selma Staege, Norman Kalmbach, Martin Klietz, Sigrid Schwarz, Andreas Leffler, Florian Wegner
Voltage-gated sodium and calcium channels as well as transient receptor potential (TRP) channels are expressed during the differentiation of human neural progenitor cells (hNPCs) and are likely to be involved in regulating neurogenesis. However, the molecular composition of these ion channels in proliferating and differentiating hNPCs is largely unknown. Here, we investigated fetal mesencephalic hNPCs in respect to their sodium, calcium, and TRP channel subunit expression and function. Quantitative real-time PCR indicated a significant upregulation of voltage-gated sodium and calcium channel subunits in hNPCs after differentiation for 3 weeks in vitro...
May 19, 2018: Stem Cells and Development
https://www.readbyqxmd.com/read/29779093/pharmacokinetics-of-the-novel-selective-non-steroidal-mineralocorticoid-receptor-antagonist-finerenone-in-healthy-volunteers-results-from-an-absolute-bioavailability-study-and-drug-drug-interaction-studies-in-vitro-and-in-vivo
#6
Roland Heinig, Michael Gerisch, Anna Engelen, Johannes Nagelschmitz, Stephanie Loewen
BACKGROUND AND OBJECTIVES: Finerenone is a selective, non-steroidal mineralocorticoid receptor antagonist. In vivo and in vitro studies were performed to assess absolute bioavailability of finerenone, the effect of metabolic enzyme inhibitors on the pharmacokinetics of finerenone and its metabolites, the quantitative contribution of the involved enzymes cytochrome P450 (CYP) 3A4 and CYP2C8 and the relevance of gut wall versus liver metabolism. METHODS: The pharmacokinetics, safety and tolerability of finerenone (1...
May 19, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29777297/optical-coherence-tomography-in-stemi-with-bioresorbable-scaffold-possible-cause-of-coronary-flow-impairment-a-sub-study-from-the-prague-19-trial
#7
Marco Loffi, Petr Tousek, Tomas Budesinsky, Libor Lisa, Andrea Santangelo, Petr Widimsky, Viktor Kocka
This study assessed the Optical Coherence Tomography (OCT) impact on the coronary flow in ST-elevation myocardial infarction (STEMI) after bioresorbable scaffold implantation. Only few data about OCT use in STEMI are available and coronary flow before and after OCT is not well studied yet. 54 patients with OCT performed at the end of procedure from the Prague 19 trial were selected and coronary flow was evaluated as TIMI frame count (TFC) before and just after OCT. Significant increase in TIMI frame count after OCT [from 9...
May 18, 2018: Heart and Vessels
https://www.readbyqxmd.com/read/29767558/molecular-basis-of-the-counteraction-by-calcium-channel-blockers-of-cyclosporine-nephrotoxicity
#8
Safaa Hicham Hammoud, Sahar Alkhansa, Neamah Mahjoub, Amal Galal Omar, Mahmoud M El-Mas, Assaad A Eid
Nephrotoxicity is a serious side effect for the immunosuppressant drug cyclosporine (CSA). In this study, we tested the hypothesis that administration of calcium channel blockers such as verapamil or nifedipine ameliorate renal CSA-induced renal dysfunction. Furthermore, our study investigates the roles of inflammatory, oxidative, and fibrotic pathways in CSA-induced renal dysfunction. Six groups of male rats (n=6/group) were used and received one of the following treatments for 7 consecutive days: vehicle (cremophor EL, i...
May 16, 2018: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29761339/-syncope-in-hypertrophic-obstructive-cardiomyopathy
#9
REVIEW
Hubert Seggewiß, Angelika Koljaja-Batzner, Kornelia Seggewiß, Malte Meesmann
Hypertrophic cardiomyopathy is the most common genetic cardiac disease. The most important pathophysiological finding is dynamic (outflow tract) obstruction of the left ventricle in about 70% of affected patients. Especially in younger patients, an increased risk of sudden cardiac death has been observed. Syncope and presyncope-in addition to extremely variable cardiac symptoms (dyspnea and angina)-are common. The etiology of syncope is complex. The most important aspect for diagnosis is a detailed history regarding the accompanying circumstances of the syncope...
May 14, 2018: Herzschrittmachertherapie & Elektrophysiologie
https://www.readbyqxmd.com/read/29751188/reversible-cerebral-vasoconstriction-syndrome-as-an-unusual-complication-of-a-dural-arteriovenous-fistula-treated-with-onyx-embolization
#10
Douglas Gonsales, Fabiano das Gracas, Roberta Santos, Pedro Aguilar-Salinas, Ricardo A Hanel
BACKGROUND: Reversible cerebral vasoconstriction syndrome (RCVS) is a rare entity with an unknown pathophysiology. RCVS has been reported to occur more frequently in women aged 20 to 50 years. Several mechanisms have been postulated involving transient deregulation of cerebral arterial tone, small vessel endothelial dysfunction, biochemical factors, hormonal deregulation, oxidative stress, and genetic predisposition. All these mechanisms and triggers are related with sympathetic over-activation which eventually produce vasoconstriction...
May 8, 2018: World Neurosurgery
https://www.readbyqxmd.com/read/29751140/nanoparticle-based-delivery-of-carbamazepine-a-promising-approach-for-the-treatment-of-refractory-epilepsy
#11
Anna Zybina, Anastasiya Anshakova, Julia Malinovskaya, Pavel Melnikov, Vladimir Baklaushev, Vladimir Chekhonin, Olga Maksimenko, Sergey Titov, Vadim Balabanyan, Jörg Kreuter, Svetlana Gelperina, Kenul Abbasova
Resistance to antiepileptic drugs (AEDs) is a major clinical problem. The overexpression of P-glycoprotein (Pgp), one of the main transporters limiting the entry of xenobiotics into the brain, is among the factors contributing to the AED resistance. Presently, there is no consensus on the interaction of carbamazepine (CBZ) with the Pgp. This study investigates the effect of the Pgp inhibitor verapamil on the anticonvulsant effect of CBZ and its nanoparticulate formulation in the rat model of isoniazid-induced epilepsy...
May 8, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29748816/epicatechin-s-cardiovascular-protective-effects-are-mediated-via-opioid-receptors-and-nitric-oxide
#12
Kirsty MacRae, Kylie Connolly, Rebecca Vella, Andrew Fenning
PURPOSE: Cardiovascular disease is the leading cause of mortality globally. Epicatechin has previously been shown to improve vascular responses and possess cardioprotective properties. However, the mechanisms underpinning these cardiotropic outcomes remain unknown. The aim of this study was to further identify epicatechin's mechanism of action in the cardiovasculature. METHODS: The effects of epicatechin on isolated rat conduit arteries, resistance vessels and cardiac electrophysiology were investigated on resting tension and precontracted vessels and cardiac action potential parameters, both in the presence and in the absence of various antagonists...
May 10, 2018: European Journal of Nutrition
https://www.readbyqxmd.com/read/29743411/effects-of-verapamil-and-pinacidil-on-extracellular-k-ph-and-the-incidence-of-ventricular-fibrillation-during-60-minutes-of-ischemia
#13
Ichiro Watanabe, Leonard S Gettes
Ca++ -channel antagonist verapamil and ATP-sensitive K+ -channel opener pinacidil are known to decrease the rise in extracellular K+ ([K+ ]e ) level and pH (pHe ) that occurs during reversible acute myocardial ischemia and to lessen the accompanying activation delay. Verapamil is also known to decrease the incidence of ventricular tachycardia (VT)/fibrillation (VF) during acute myocardial ischemia; however, the effects of ATP-sensitive K+ -channel opener on the incidence of VT/VF are controversial. We studied, in an in vivo pig model, the effects of verapamil and pinacidil on the changes in [K+ ]e level and pHe , local activation, and the incidence of VT/VF during 60 minutes of ischemia...
May 9, 2018: International Heart Journal
https://www.readbyqxmd.com/read/29738260/hypoxia-protective-azaphilone-adducts-from-peyronellaea-glomerata
#14
Tian-Xiao Li, Rui-Huan Liu, Xiao-Bing Wang, Jun Luo, Jian-Guang Luo, Ling-Yi Kong, Ming-Hua Yang
Peyronellones A and B (1 and 2), a pair of rare tetracyclic caged adducts of azaphilone with pyruvic acid, along with four new analogues (3-6), were isolated from solid cultures of the endophytic fungus Peyronellaea glomerata. Their structures were elucidated through spectroscopic analysis, and their absolute configurations were unambiguously determined by a combination of single-crystal X-ray crystallography, Rh2 (OCOCF3 )4 -induced ECD experiments, ECD calculations, and modified Mosher methods. Compound 2 (5 μM) was found to have a significant hypoxia-protective effect that improved the survival rate of hypoxia/reoxygenation-treated human umbilical vein endothelial cells from 35% to 70%, which was equal to the potency of the positive control, verapamil...
May 8, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29725664/successful-use-of-continuous-vasodilator-infusion-to-treat-critical-vasospasm-threatening-a-distal-bypass
#15
Gregory A Magee, Anastasia Plotkin, Jeniann A Yi, Kathryn E Bowser, David P Kuwayama
Vasospasm immediately after lower extremity arterial bypass may represent an uncommon cause of early graft failure. We report a successful case of catheter-directed, intra-arterial continuous vasodilator infusion to salvage a bypass graft threatened by severe, refractory vasospasm after incomplete response to nicardipine, verapamil, and nitroglycerin boluses. A continuous nitroglycerin infusion was administered for 24 hours, by which time the vasospasm resolved. At 12 months postoperatively, the graft remained patent with normal results of vascular laboratory studies...
March 2018: Journal of Vascular Surgery Cases and Innovative Techniques
https://www.readbyqxmd.com/read/29724724/prevention-of-severe-hypoglycemia-induced-brain-damage-and-cognitive-impairment-with-verapamil
#16
David A Jackson, Trevin Michael, Adriana Vieira de Abreu, Rahul Agrawal, Marco Bortolato, Simon J Fisher
People with insulin-treated diabetes are uniquely at risk for severe hypoglycemia-induced brain damage. Since calcium influx may mediate brain damage, we tested the hypothesis that the calcium channel blocker, verapamil, would significantly reduce brain damage and cognitive impairment caused by severe hypoglycemia. Ten-week-old Sprague-Dawley rats were randomly assigned to one of three treatments; 1) control hyperinsulinemic (200 mU.kg-1 min-1 ) euglycemic (80-100mg/dl) clamps (n=14), 2) hyperinsulinemic hypoglycemic (10-15mg/dl) clamps (n=16), or 3) hyperinsulinemic hypoglycemic clamps followed by a single treatment with verapamil (20mg/kg) (n=11)...
May 3, 2018: Diabetes
https://www.readbyqxmd.com/read/29719553/47-consecutive-cases-of-pipeline-flex-flow-diversion-utilizing-a-novel-large-bore-intracranial-intermediate-catheter-nuances-and-institutional-experience-with-the-syphontrak
#17
Li-Mei Lin, Bowen Jiang, Matthew T Bender, Erick M Westbroek, Jessica K Campos, Rafael J Tamargo, Judy Huang, Alexander L Coon, Geoffrey P Colby
Background: The increasing complexity of modern neurointerventions has necessitated a shift in intracranial access techniques towards more robust distal support platforms. Here we present our experience with the Syphontrak Support Catheter (Codman Neuro, Raynham, MA, USA) in the triaxial platform for the implantation of the second-generation Pipeline Flex embolization device (PED Flex; Medtronic Neurovascular, Irvine, CA, USA). Methods: We retrospectively identified patients who underwent PED Flex treatment utilizing the Syphontrak at a single institution...
April 2018: Interventional Neurology
https://www.readbyqxmd.com/read/29719326/prospective-study-to-evaluate-the-clinical-outcome-of-intralesional-interferon-%C3%AE-2b-in-the-management-of-peyronie-s-disease
#18
Ashok Kumar Sokhal, Nilesh Kumar Jain, Ankur Jhanwar, Kawaljit Singh, Durgesh Kumar Saini
Context: Interferon (IFN)-α2b in Peyronie's disease (PD). Aims: This study aims to evaluate clinical efficacy of the IFN-α2b in both subjective and objective manner for the treatment of PD and compared with previously used intralesional verapamil in terms of cost-benefit analysis. Settings and Design: Prospective study. Materials and Methods: A prospective study conducted from January 2013 to July 2016 in the Department of Urology, Government Medical College, Kota, Rajasthan, India...
April 2018: Urology Annals
https://www.readbyqxmd.com/read/29713575/an-evaluation-of-complications-in-femoral-arterial-sheaths-maintained-post-neuroangiographic-procedures
#19
Zalan Khan, Premkumar Nattanamai, Premkumar Keerthivaas, Christopher R Newey
BACKGROUND: Digital subtraction angiography (DSA) is a frequently used technique in the neuro-diagnosis and treatment of cerebrovascular diseases. The routine use of femoral arterial sheaths (FAS) peri-procedurally has become standard. The maintenance of a FAS post-procedure may be warranted while awaiting the normalization of coagulopathy or to reaccess emergently. We retrospectively reviewed our stroke dataset to evaluate for complications associated with the prolonged use of FAS post-procedure...
February 26, 2018: Curēus
https://www.readbyqxmd.com/read/29709270/selectivity-of-ca-2-channel-blockers-for-dilator-actions-on-the-isolated-lower-esophageal-sphincter-and-aorta-from-rats
#20
Akira Takahara, Shuhei Nozaki, Akane Ishiguro, Kaori Okamura, Xin Cao, Megumi Aimoto, Yoshinobu Nagasawa
We compared dilator actions of representative four Ca2+ channel blockers on the isolated lower esophagus sphincter (LES) and thoracic aorta from rats. Verapamil, diltiazem, nifedipine and cilnidipine suppressed KCl-induced contractions of LES and thoracic aorta in a concentration-dependent manner. The order of selectivity for LES, which was calculated as ratio of IC50 value for thoracic aorta divided by that for LES, was diltiazem > verapamil > nifedipine > cilnidipine. These results suggest that diltiazem more preferentially dilates the LES whereas cilnidipine is expected to have lower potential risk of gastroesophageal dysfunction during the antihypertensive therapy...
April 19, 2018: Journal of Pharmacological Sciences
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