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Haoshi Gao, Yue Wei, Long Xi, Yuanyuan Sun, Tianhong Zhang
Bergenin (BN) is a Biopharmaceutics Classification System class IV (BCS IV) drug with poor hydrophilicity and lipophilicity and is potentially eliminated by the efflux function of P-glycoprotein (P-gp). These factors may explain its low oral bioavailability. In the present study, a BN-phospholipid complex solid dispersion (BNPC-SD) was prepared by solvent evaporation and characterized based on differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, infrared diffraction, solubility, octanol-water partition coefficient, and in vitro dissolution...
March 19, 2018: AAPS PharmSciTech
Hironori Sagawa, Shinsuke Hoshino, Kengo Yoshioka, Wei-Guang Ding, Mariko Omatsu-Kanbe, Masao Nakagawa, Yoshihiro Maruo, Hiroshi Matsuura
BACKGROUND: In the clinical setting, verapamil is contraindicated in neonates and infants because of the perceived risk of hypotension or bradyarrhythmia. However, it remains unclear whether there is an age-dependent difference in the sensitivity of cardiac L-type Ca2+ channel current (ICa,L ) to inhibition by verapamil. METHODS: Ventricular myocytes were enzymatically dissociated from the hearts of 6 different age groups (0, 7, 14, 21, 28 days and 10-15 weeks) of mice using a similar Langendorff-perfusion method...
March 19, 2018: Pediatric Research
Jacob B Williams, Clara G Buchanan, William G Pitt
Background - Patients undergoing chemotherapy can develop resistance not only to the administered drug, but also to many other unrelated types of drugs, a phenomenon known as multidrug resistance. One of the most common mechanisms of multidrug resistance is an elevated expression of drug efflux pumps. Co-delivery of an efflux pump inhibitor with a chemotherapeutic can increase the killing of multidrug resistant cancer cells. Objective - Our hypothesis was that delivering doxorubicin directly to the cytosol of multidrug resistant cancer cells via a folate-targeted liposome loaded with a perfluoropentane emulsion droplet and doxorubicin (folated eLipoDox), along with the delivery of verapamil to block the efflux pumps will prove to be more effective at killing multidrug resistant cancer cells compared to conventional drug delivery...
March 16, 2018: Pharmaceutical Nanotechnology
Yoshiyuki Kubo, Ayumi Nakazawa, Shin-Ichi Akanuma, Ken-Ichi Hosoya
PURPOSE: To investigate the blood-to-retina verapamil transport at the blood-retinal barrier (BRB). METHODS: EverFluor FL Verapamil (EFV) was adopted as the fluorescent probe of verapamil, and its transport across the BRB was investigated with common carotid artery infusion in rats. EFV transport at the inner and outer BRB was investigated with TR-iBRB2 cells and RPE-J cells, respectively. RESULTS: The signal of EFV was detected in the retinal tissue during the weak signal of cell impermeable compound...
March 12, 2018: Pharmaceutical Research
Jasmine L Gowarty, Jon D Herrington
A promising drug, palbociclib, received accelerated approval as a first line treatment when used with the aromatase inhibitor, letrozole, for postmenopausal women with hormone receptor positive advanced or metastatic breast cancer. We report a case of a patient who presented with febrile neutropenia, grade 3 stomatitis with lip swelling, periorbital edema, and transaminitis while on palbociclib and verapamil. Labs normalized upon discontinuation of verapamil and our patient was able to continue treatment with palbociclib and letrozole...
January 1, 2018: Journal of Oncology Pharmacy Practice
Rao Mukkavilli, Gajanan Jadhav, Subrahmanyam Vangala
BACKGROUND: Drug transporters function as gatekeepers and modulate drug access into the body and various tissues. Thus a thorough and precise understanding of transporter liability for compound uptake and efflux is critical during drug development. METHODS: In the present study, we assessed the apparent permeability (Papp) and compared the efflux ratio of various compounds in stably transfected Madin-Darby Canine Kidney (MDCKII) cells overexpressing human P-gp (MDCKII-P-gp), human BCRP (MDCKII-BCRP), wild type (MDCKII-WT), and Caco-2 cell monolayers...
March 7, 2018: Current Pharmaceutical Biotechnology
Chia-Ping Huang Yang, Changwei Wang, Iwao Ojima, Susan Band Horwitz
Several next-generation taxanes have been reported to possess high potency against Taxol-resistant cancer cell lines overexpressing βIII-tubulin and/or P-glycoprotein (P-gp), both of which are involved in drug resistance. Using a photoaffinity Taxol analogue, 2-( m-azidobenzoyl)taxol, two potent next-generation taxanes, SB-T-1214 and SB-CST-10202, exhibited distinct inhibitory effects on photolabeling of β-tubulin from different eukaryotic sources that differ in β-tubulin isotype composition. They also specifically inhibited photolabeling of P-gp, and the inhibitory effect correlated well with the steady-state accumulation of [3 H]vinblastine in a multidrug resistant (MDR) cell line, SKVLB1...
March 8, 2018: Journal of Natural Products
Qi Jin, Liqun Wu, Derek J Dosdall, Li Li, Jack M Rogers, Raymond E Ideker, Jian Huang
INTRODUCTION: Sotalol and verapamil alone reduce reentry incidence during ventricular fibrillation (VF). We tested whether the combination of these two drugs had a synergistic effect on initiation, maintenance and termination of VF. METHODS: Six open-chest pigs received intravenous sotalol (1.5 mg/kg) followed by verapamil (0.136 mg/kg). VF threshold (VFT) was determined by a burst pacing protocol. Two 20 s episodes of VF were recorded from a 21x24 unipolar electrode plaque on the lateral posterior left ventricular epicardium before and after each drug...
February 27, 2018: Cardiovascular Therapeutics
Rojesh Khangembam, Harkirat Singh, Jyoti, Shitanshu Shekar Rath, Nirbhay Kumar Singh
The status of ivermectin resistance in Rhipicephalus (Boophilus) microplus collected from various districts of the Punjab state, India was determined using larval immersion test (LIT). Regression graphs of probit mortality of larval ticks of various field isolates were plotted against log values of increasing concentrations of technical grade ivermectin for determination of slopes of mortality, lethal concentrations for 50% (LC50 ) and resistance factors (RF). Values for the coefficient of determination (R2 ) in LIT assay ranged from 0...
February 17, 2018: Ticks and Tick-borne Diseases
Yan Zhang, Changyuan Wang, Zhihao Liu, Qiang Meng, Xiaokui Huo, Qi Liu, Pengyuan Sun, Xiaobo Yang, Huijun Sun, Xiaodong Ma, Kexin Liu
BACKGROUND: Afatinib is an irreversible multi-targeted TKI, used in the treatment with EGFR mutated non-small cell lung cancer (NSCLC). The purpose of this study is to explore the molecular pharmacokinetic mechanism underlying the effect of P-gp inhibitors on the intestinal absorption and biliary excretion and to understand how P-gp inhibitors affect afatinib pharmacokinetics. METHODS: Pharmacokinetics in vivo, in situ intestinal perfusion, perfused rat liver in situ, Caco-2 cells, P-gp ATPase activity, sandwich-cultured rat hepatocytes (SCRH) and transfected-cell transport were used in the evaluation...
November 4, 2017: Pharmacological Reports: PR
Cecilia Villa Etchegoyen, Guillermo Alberto Keller, Sebastian Mrad, Sixuan Cheng, Guillermo DiGirolamo
Drug-induced QT interval prolongation is the most frequent cause of Long QT syndrome (LQTS) in the clinical practice. This electrophysiological entity, produced by an extended duration of the myocardial repolarization and reflected as a prolonged QT interval in the superficial electrocardiogram (EKG), increases the risk of polymorphic ventricular tachycardia (Torsades de Pointes) appearance and sudden death. Certain antiarrhythmic drugs such as amiodarone, sotalol, quinidine, procainamide, verapamil and diltiazem are known as drugs that, due to their mechanism of action, prolong the QT interval, demanding constant monitorization...
February 23, 2018: Current Clinical Pharmacology
Chao Chen, Susana Gardete, Robert Sander Jansen, Annanya Shetty, Thomas Dick, Kyu Y Rhee, Véronique Dartois
Mycobacterium tuberculosis (Mtb) kills more people than any other bacterial pathogen and is becoming increasingly untreatable due to the emergence of resistance. Verapamil, an FDA-approved calcium channel blocker, potentiates the effect of several anti-tuberculosis (TB) drugs in vitro and in vivo. This potentiation is widely attributed to inhibition of Mtb's efflux pumps, resulting in intrabacterial drug accumulation. Here, we confirm and quantify verapamil's synergy with several anti-TB drugs, including bedaquiline and clofazimine, but find that this effect is not due to increased intrabacterial drug accumulation...
February 20, 2018: Antimicrobial Agents and Chemotherapy
Jaqueline Pazinato, Otávio M Cruz, Karine P Naidek, Amanda R A Pires, Eduard Westphal, Hugo Gallardo, Hélène Baubichon-Cortay, Maria E M Rocha, Glaucia R Martinez, Sheila M B Winnischofer, Attilio Di Pietro, Herbert Winnischofer
A new series of amphiphilic η6 -areneruthenium(II) compounds containing phenylazo ligands (group I: compounds 1a, 1b, 2a and 2b) and phenyloxadiazole ligands (group II: compounds 3a, 3b, 4a and 4b) were synthesized and characterized for their anti-glioblastoma activity. The effects of the amphiphilic η6 -areneruthenium(II) complexes on the viability of three human glioblastoma cell lines, U251, U87MG and T98G, were evaluated. The azo-derivative ruthenium complexes (group I) showed high cytotoxicity to all cell lines, whilst most oxadiazole-derivative complexes (group II) were less cytotoxic, except for compound 4a...
February 12, 2018: European Journal of Medicinal Chemistry
M T Crockett, M Di Loreto, T J Philips
No abstract text is available yet for this article.
December 2017: Journal of Vascular and Interventional Neurology
Yajing Fang, Fuqiang Liang, Kunyuan Liu, Shakeel Qaiser, Siyi Pan, Xiaoyun Xu
Flavonoids are a large group of polyphenols and widely distributed in plant foods. Flavonoids exhibit various biological activities, such as anti-cancer, antioxidant and anti-inflammatory while poor oral bioavailability has been considered as a major hurdle in their use as functional foods. Cellular uptake and efflux of flavonoid implicates their bioavailability. To investigate the cellular uptake and efflux of flavonoids, 27 flavonoids were measured for their cellular uptake in Caco-2 cells with (CUV) and without (CU) the inhibitor of P-glycoprotein (P-gp) verapamil...
March 2018: Food Research International
Joana Bicker, Gilberto Alves, Ana Fortuna, Patrício Soares-da-Silva, Amílcar Falcão
Inhibition of the biosynthesis of noradrenaline is a currently explored strategy for the treatment of hypertension, congestive heart failure and pulmonary arterial hypertension. While some dopamine β-hydroxylase (DBH) inhibitors cross the blood-brain barrier (BBB) and cause central as well as peripheral effects (nepicastat), others have limited access to the brain (etamicastat, zamicastat). In this context, peripheral selectivity is clinically advantageous, in order to prevent alterations of noradrenaline levels in the CNS and the occurrence of adverse central effects...
February 8, 2018: European Journal of Pharmaceutical Sciences
Omkara Swami Muddineti, Asmitha Vanaparthi, Sri Vishnu Kiran Rompicharla, Preeti Kumari, Balaram Ghosh, Swati Biswas
A newly synthesized PEGylated cholesterol/α-tocopheryl succinate (α-TOS) linked polymer (CV) was self-assembled and loaded with curcumin to form a micellar system (C-CVM). The tri-functionalized amphiphilic polymer was constituted of hydrophobic cholesterol and α-TOS connected to hydrophilic PEG via a lysine linker. The synthesized polymer and the micelles were characterized by 1 H NMR, DLS, zeta potentiometer, TEM, CMC determination and hemolysis studies. CVM displayed low CMC value of 15 µM with extent of hemolysis as less than 4%...
February 9, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Rui Hu, Jie Gao, Rushangul Rozimamat, Haji Akber Aisa
Five new (1-5) and ten known (6-15) jatrophane diterpenoids were isolated from the fructus of Euphorbia sororia and their structures were elucidated by extensive spectroscopic analysis. The absolute configurations of compounds 1 and 4 were confirmed by X-ray crystallographic analysis. Cytotoxicity and anti-multidrug resistance effects of these jatrophane diterpenoids were evaluated in multidrug-resistant MCF-7/ADR breast cancer cells with an overexpression of P-glycoprotein (P-gp). Eight compounds (1, 2, 4, 6, 8, 10, 11, and 15) showed promising chemoreversal abilities compared to verapamil (VRP)...
January 11, 2018: European Journal of Medicinal Chemistry
Mariarosa Anna Beatrice Melone, Clemente Dato, Simona Paladino, Cinzia Coppola, Claudia Trebini, Maria Teresa Giordana, Lorena Perrone
PURPOSE: Oxidative stress is a hallmark of Alzheimer's Disease (AD) and promotes tau phosphorylation. Since Thioredoxin Interacting protein (TXNIP), the inhibitor of the anti-oxidant system of Thioredoxin, is up regulated in the hippocampus of AD patients, we investigated whether TXNIP plays a role in promoting tau phosphorylation and whether Verapamil, an inhibitor of TXNIP expression, prevents TXNIP downstream effects. METHODS: We analyzed TXNIP expression and tau phosphorylation in the hippocampus of the 5xFAD mice in the absence and presence of a pharmacological treatment with Verapamil...
February 5, 2018: Pharmaceutical Research
Tahereh Eteraf-Oskouei, Sevda Mikaily Mirak, Moslem Najafi
Purpose: In the present study, the effects of verapamil on inflammation and angiogenesis in air pouch model were studied. Methods: To create a model of inflammation in the rats, on days 1 and 3 sterile air, and on the sixth day, carrageenan was injected into the pouch subcutaneously. Normal saline as control, diclofenac sodium and dexamethasone as standards and verapamil (0.05, 0.1 and 0.2mg/rat) was injected into the pouch simultaneously with carrageenan and as well as 24 and 48 hours later. After 72 hours, volume of exudate, the leukocytes count, concentration of VEGF and IL-1ß, granulomatous tissue weight, histopathological changes and angiogenesis were considered...
December 2017: Advanced Pharmaceutical Bulletin
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