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https://www.readbyqxmd.com/read/28102715/capsaicin-pretreatment-enhanced-the-bioavailability-of-fexofenadine-in-rats-by-p-glycoprotein-modulation-in-vitro-in-situ-and-in-vivo-evaluation
#1
Satish Kumar Bedada, Ramgopal Appani, Praveen Kumar Boga
BACKGROUND AND OBJECTIVE: Capsaicin is the main pungent principle present in chilli peppers has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro, which may have the potential to modulate bioavailability of P-gp substrates. Therefore, purpose of the present study was to evaluate the effect of capsaicin on intestinal absorption and bioavailability of fexofenadine, a P-gp substrate in rats. METHODS: The mechanistic evaluation was determined by non-everted sac and intestinal perfusion studies to explore the intestinal absorption of fexofenadine...
January 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28102360/modification-of-distinct-ion-channels-differentially-modulates-ca-2-dynamics-in-primary-cultured-rat-ventricular-cardiomyocytes
#2
Xichun Li, Liping Shen, Fang Zhao, Xiaohan Zou, Yuwei He, Fan Zhang, Chunlei Zhang, Boyang Yu, Zhengyu Cao
Primary cultured cardiomyocytes show spontaneous Ca(2+) oscillations (SCOs) which not only govern contractile events, but undergo derangements that promote arrhythmogenesis through Ca(2+) -dependent mechanism. We systematically examined influence on SCOs of an array of ion channel modifiers by recording intracellular Ca(2+) dynamics in rat ventricular cardiomyocytes using Ca(2+) specific fluorescence dye, Fluo-8/AM. Voltage-gated sodium channels (VGSCs) activation elongates SCO duration and reduces SCO frequency while inhibition of VGSCs decreases SCO frequency without affecting amplitude and duration...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28100216/antispasmodic-bronchodilator-vasorelaxant-and-cardiosuppressant-effects-of-buxus-papillosa
#3
Arif-Ullah Khan, Shamsher Ali, Anwarul-Hassan Gilani, Manzoor Ahmed, Muhammad Iqbal Choudhary
BACKGROUND: The present research was carried out to investigate pharmacological properties of Buxus papillosa C.K. Schneid. (Buxaceae). METHODS: Buxus papillosa extracts of leaves (BpL), stem (BpS), roots (BpR) and BpL fractions: hexane (BpL-H), aqueous (BpL-A) also plant constituent, cyclomicrobuxine effect were studied in jejunum, atria, aorta and tracheal preparations from rabbit and guine-peg. RESULTS: Ca(++) antagonistic effect of BpS, BpR, BpL-H, BpL-A and cyclomicrobuxine were conclusively suggested, when spontaneous contractions of rabbit jejunal preparation was relaxed along with subsequent relaxation of potassium chloride (80 mM) induced contractions...
January 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28096338/mitochondrial-fusion-dynamics-is-robust-in-the-heart-and-depends-on-calcium-oscillations-and-contractile-activity
#4
Verónica Eisner, Ryan R Cupo, Erhe Gao, György Csordás, William S Slovinsky, Melanie Paillard, Lan Cheng, Jessica Ibetti, S R Wayne Chen, J Kurt Chuprun, Jan B Hoek, Walter J Koch, György Hajnóczky
Mitochondrial fusion is thought to be important for supporting cardiac contractility, but is hardly detectable in cultured cardiomyocytes and is difficult to directly evaluate in the heart. We overcame this obstacle through in vivo adenoviral transduction with matrix-targeted photoactivatable GFP and confocal microscopy. Imaging in whole rat hearts indicated mitochondrial network formation and fusion activity in ventricular cardiomyocytes. Promptly after isolation, cardiomyocytes showed extensive mitochondrial connectivity and fusion, which decayed in culture (at 24-48 h)...
January 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28095559/comparative-results-in-treatment-of-keloids-with-intralesional-5-fu-kenalog-5-fu-verapamil-enalapril-alone-verapamil-alone-and-laser-a-case-report-and-review-of-the-literature
#5
Doru Alexandrescu, Sabrina Fabi, Lindsey C Yeh, Richard E Fitzpatrick, Mitchel P Goldman
BACKGROUND: The pathogenesis of keloids involves a hyperproliferative state due to molecular abnormalities, cellular driving pathways, such as TGF, VEGF, and the inactivation of proapoptotic genes. We reviewed the literature and compared various treatment combina- tions in the treatment of keloids in a one patient observation. METHODS AND MATERIALS: Treatment modalities consisted of: intralesional 5- uorouracil (5-FU)/triamcinolone (TMC), 5-FU/verapamil, enal- april alone, verapamil alone, and fractional carbon dioxide laser...
November 1, 2016: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28070974/stimulus-responsive-short-peptide-nanogels-for-controlled-intracellular-drug-release-and-overcome-tumor-resistance
#6
Bengang Xing, Linna Lyu, Fang Liu, Xiaoyong Wang, Ming Hu, Jing Mu, Haolun Cheong, Gang Liu
Multidrug resistance (MDR) places a major burden against cancer treatment. As one important factor contributing to MDR, over-expression of P-glycoprotein (P-gp), results in the reduced intracellular drug accumulation. Hence, the ability to effectively block the efflux protein and accumulate the therapeutics in cancer cells is of great significance in clinical practice. In this work, we successfully developed a smart stimulus-responsive short peptide assembled system, termed as PD/VER nanogels, which synergistically combined the acid activatable Doxorubicin (Dox) antitumor prodrug with the P-gp inhibitor (Verapamil, VER) for reversing MDR...
January 9, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28070045/-effect-of-calcium-channel-blockers-on-primary-cultured-human-urethra-scar-fibroblasts
#7
Mingqiang Zeng, Junjie Chen, Liang Huang, Ruizhi Xue, Xuyu Xiang, Fanchang Zeng, Guilin Wang, Zhengyan Tang
To investigate effects of verapamil on primary cultured human urethral scar fibroblasts (USFs) and to provide basis for protecting the formation of urethra scar.
 Methods: The cell proliferation was evaluated with the cell counting kit (CCK)-8 method after USFs were incubated various verapamil concentrations (50, 100, 150, 200, or 250 μmol/L) or solvent for 12, 24, or 48 h. The protein level of matrix metalloproteinase (MMP) was evaluated with ELISA after cells were incubated with verapamil (100 μmol/L) or solvent (control cells) for 24 h...
December 28, 2016: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
https://www.readbyqxmd.com/read/28043777/quercetin-glutamic-acid-conjugate-with-a-non-hydrolysable-linker-a-novel-scaffold-for-multidrug-resistance-reversal-agents-through-inhibition-of-p-glycoprotein
#8
Mi Kyoung Kim, Yunyoung Kim, Hyunah Choo, Youhoon Chong
Previously, we have reported remarkable effect of a quercetin-glutamic acid conjugate to reverse multidrug resistance (MDR) of cancer cells to a broad spectrum of anticancer agents through inhibition of P-glycoprotein (Pgp)-mediated drug efflux. Due to the hydrolysable nature, MDR-reversal activity of the quercetin conjugate was attributed to its hydrolysis product, quercetin. However, several lines of evidence demonstrated that the intact quercetin-glutamic acid conjugate has stronger MDR-reversal activity than quercetin...
December 23, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28034363/the-screening-of-novel-inhibitors-against-leishmania-donovani-calcium-ion-channel-to-fight-leishmaniasis
#9
Mohammad Kashif, Partha Pratim Manna, Yusuf Akhter, Mohammed Alaidarous, Abdur Rub
Leishmania is an intracellular protozoan parasite which causes Leishmaniasis, a global health problem affecting millions of people throughout 89 different countries in the world. The current treatment which includes use of amphotericin B, antimonials, and others has major drawbacks due to toxicity, resistance, and extraordinary high cost. So there is an urgent need of development of new drug targets to fight against leishmaniasis. In this regard we have selected Leishmania donovani Ca2+ ion channel (Ld-CC) as potential drug target...
December 30, 2016: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28031098/mechanical-strain-regulates-osteoblast-proliferation-through-ca-2-camk-creb-signal-pathway
#10
Yong Guo, Qi Lv, Xian-Qiong Zou, Zhi-Xiong Yan, Yu-Xian Yan
Objective To investigate the effects of mechanical strain on Ca(2+)-calmodulin dependent kinase (CaMK)-cAMP response element binding protein (CREB) signal pathway and proliferation of osteoblasts.Methods Using a four-point bending device, MC3T3-E1 cells were exposed to mechanical tensile strains of 2500 µs and 5000 µs at 0.5 Hz respectively. The intracellular free Ca(2+) ([Ca(2+)]i) concentration and calmodulin activity were assayed by fluorospectrophotometry, CaMK II β, CREB, and phosphorylated (activated) CREB (p-CREB) were assessed by Western blot, and cells proliferation was assayed with MTT...
June 20, 2016: Chinese Medical Sciences Journal, Chung-kuo i Hsüeh K'o Hsüeh Tsa Chih
https://www.readbyqxmd.com/read/28028729/cardiovascular-ion-channel-inhibitor-drug-drug-interactions-with-p-glycoprotein
#11
Kaitlyn V Ledwitch, Arthur G Roberts
P-glycoprotein (Pgp) is an ATP-binding cassette (ABC) transporter that plays a major role in cardiovascular drug disposition by effluxing a chemically and structurally diverse range of cardiovascular therapeutics. Unfortunately, drug-drug interactions (DDIs) with the transporter have become a major roadblock to effective cardiovascular drug administration because they can cause adverse drug reactions (ADRs) or reduce the efficacy of drugs. Cardiovascular ion channel inhibitors are particularly susceptible to DDIs and ADRs with Pgp because they often have low therapeutic indexes and are commonly coadministered with other drugs that are also Pgp substrates...
December 27, 2016: AAPS Journal
https://www.readbyqxmd.com/read/28012673/characteristics-of-cadmium-uptake-and-membrane-transport-in-roots-of-intact-wheat-triticum-aestivum-l-seedlings
#12
Lian-Zhen Li, Chen Tu, Willie J G M Peijnenburg, Yong-Ming Luo
Wheat is one of several cereals that is capable of accumulating higher amounts of Cd in plant tissues. It is important to understand the Cd(2+) transport processes in roots that result in excess Cd accumulation. Traditional destructive technologies have limited capabilities in analyzing root samples due to methodological limitations, and sometimes may result in false conclusions. The mechanisms of Cd(2+) uptake into the roots of wheat seedlings (Triticum aestivum L.) were investigated by assessing the impact of various inhibitors and channel blockers on Cd accumulation as well as the real-time net Cd(2+) flux at roots with the non-destructive scanning ion-selective electrode technique...
February 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28009689/a-comparison-of-gene-expression-of-decorin-and-mmp13-in-hypertrophic-scars-treated-with-calcium-channel-blocker-steroid-and-interferon-a-human-scar-carrying-animal-model-study
#13
Shih-Yi Yang, Jui-Yung Yang, Yen-Chang Hsiao, Shiow-Shuh Chuang
BACKGROUND: The formation of hypertrophic scaring (HSc) is an abnormal wound-healing response. In a previous study, an animal model with human scar tissue implanted into nude mice (BALB/c) has been successfully established. The effects of verapamil as well as combination therapy with verapamil and kenacort have been studied and compared. OBJECTIVE: To treat persistent hypertrophic scars, local injection of drugs composed of steroids, calcium channel blockers (CCBs), and interferon might be a good method...
January 2017: Dermatologic Surgery: Official Publication for American Society for Dermatologic Surgery [et Al.]
https://www.readbyqxmd.com/read/28000173/in-vitro-evaluation-of-absorption-characteristics-of-peramivir-for-oral-delivery
#14
Ying Li, Zhiyuan Wang, Xin Li, Wei Gong, Xiangyang Xie, Yang Yang, Wu Zhong, Aiping Zheng
BACKGROUND AND OBJECTIVE: Peramivir is a novel antiviral agent approved for the treatment of severe influenza. However, the development of oral formulation of peramivir has been severely hurdled by poor bioavailability (human, ≤3%). The present work aims to evaluate oral permeability characteristics of peramivir. METHODS: In vitro gastrointestinal stability, metabolic stability in human intestinal S9 fraction and Caco-2 permeability were performed. The liquid chromatography with tandem mass spectrometric (LC-MS/MS) was used to quantify peramivir in buffer and biological sample...
December 21, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27998394/the-hypertension-drug-verapamil-activates-nrf2-by-promoting-p62-dependent-autophagic-keap1-degradation-and-prevents-acetaminophen-induced-cytotoxicity
#15
Da Hyun Lee, Jeong Su Park, Yu Seol Lee, Su Haeng Sung, Yong-Ho Lee, Soo Han Bae
Nuclear factor erythroid 2-related factor 2 (Nrf2) provides cellular defense against oxidative stress by inducing the expression of antioxidant and detoxification enzymes. The calcium antagonist verapamil is an FDA-approved drug prescribed for the treatment of hypertension. Here, we show that verapamil acts as a potent Nrf2 activator without causing cytotoxicity through degradation of Kelch-like ECH-associated protein 1 (Keap1), an Nrf2 repressor. Furthermore, verapamil-induced Keap1 degradation is prominently mediated by a p62-dependent autophagic pathway...
December 20, 2016: BMB Reports
https://www.readbyqxmd.com/read/27996361/insight-into-the-molecular-mechanism-of-p-glycoprotein-mediated-drug-toxicity-induced-by-bioflavonoids-an-integrated-computational-approach
#16
Pathomwat Wongrattanakamon, Vannajan Sanghiran Lee, Piyarat Nimmanpipug, Sunee Chansakaow, Supat Jiranusornkul
In this work, molecular docking, pharmacophore modelling, and molecular dynamics (MD) simulation were rendered for the mouse P-gp (code: 4Q9H) and bioflavonoids; amorphigenin, chrysin, epigallocatechin, formononetin, and rotenone including a positive control; verapamil to identify protein-ligand interaction features including binding affinities, interaction characteristics, hot-spot amino acid residues, and complex stabilities. These flavonoids occupied the same binding site with high binding affinities and shared the same key residues for their binding interactions and the binding region of the flavonoids was revealed that overlapped the ATP binding region with hydrophobic and hydrophilic interactions suggesting a competitive inhibition mechanism of the compounds...
December 20, 2016: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/27992072/comparison-of-intestinal-permeability-and-p-glycoprotein-effects-on-the-intestinal-absorption-of-enantiomers-of-2-2-hydroxypropanamido-benzoic-acid-in-rats
#17
Qili Zhang, Meiyan Zhang, Danlin Wang, Yunli Zhao, Zhiguo Yu
The purpose of this study was to compare intestinal permeability between enantiomers of 2-(2-hydroxypropanamido) benzoic acid ((R)-/(S)-HPABA), a marine-derived antiinflammatory drug, using an in situ single-pass intestinal perfusion (SPIP) model in rats. Concentrations, isolated regions of small intestine, and p-glycoprotein (P-gp) inhibitor were performed to investigate their influences on the intestinal absorption of (R)-/(S)-HPABA. In addition, a molecular docking method was performed to illustrate our prediction...
December 19, 2016: Chirality
https://www.readbyqxmd.com/read/27990618/lipid-emulsion-inhibits-apoptosis-induced-by-a-toxic-dose-of-verapamil-via-the-delta-opioid-receptor-in-h9c2-rat-cardiomyoblasts
#18
Seong-Ho Ok, Mun Hwan Choi, Il-Woo Shin, Soo Hee Lee, Sebin Kang, Jiah Oh, Jeong Yeol Han, Ju-Tae Sohn
The goals of this study were to investigate the effects of lipid emulsion (LE) on apoptosis induced by a toxic dose of verapamil in H9c2 cells and to elucidate the associated cellular mechanism. The effects of LE alone and combined with an inhibitor on the decreases in cell counts and viability induced by verapamil and diltiazem were examined using the MTT assay. The effects of verapamil alone, combined LE and verapamil treatment, and combined inhibitor, LE and verapamil treatment on cleaved caspase-3, caspase-8 and Bax expression, were examined using Western blotting...
December 19, 2016: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/27988472/co-delivery-of-docetaxel-and-verapamil-by-reduction-sensitive-peg-plga-ss-dtx-conjugate-micelles-to-reverse-the-multi-drug-resistance-of-breast-cancer
#19
Yuanyuan Guo, Wenxiu He, Shengfeng Yang, Dujuan Zhao, Zhonghao Li, Yuxia Luan
The clinical usage of docetaxel (DTX) has been blocked in the clinic because of its poor solubility and tumour multi-drug resistance (MDR). The dominating mechanism of MDR is the over-expression of p-gp on tumour cells. Traditional nano-medicines, such as nanoparticles and micelles, have been used to physically entrap DTX to improve their solubility, while the drug loading content was very low and the tumour resistance was neglected. In this study, the synthesized reduction-sensitive mPEG-PLGA-SS-DTX conjugate was utilized to load the p-gp inhibitor veraparmil (VRP) to prepare DTX and VRP co-delivered mPEG-PLGA-SS-DTX/VRP (PP-SS-DTX/VRP) multi-functional micelles to reverse MDR and enhance the anti-tumour effect of DTX...
December 11, 2016: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27988399/spasmogenic-and-spasmolytic-activities-of-agastache-mexicana-ssp-mexicana-and-a-mexicana-ssp-xolocotziana-methanolic-extracts-on-the-guinea-pig-ileum
#20
Rosa Ventura-Martínez, Rodolfo Rodríguez, María Eva González-Trujano, Guadalupe E Ángeles-López, Myrna Déciga-Campos, Claudia Gómez
ETHNOPHARMACOLOGICAL RELEVANCE: Agastache mexicana has been used in traditional medicine for relief of abdominal pain and treatment of other diseases. Two subspecies have been identified: A. mexicana ssp. mexicana (AMM) and A. mexicana ssp. xolocotziana (AMX) and both are used traditionally without distinction or in combination. AIM OF THE STUDY: To determine the effect of methanol extracts of A. mexicana ssp. mexicana and A. mexicana ssp. xolocotziana on gut motility and their possible mechanism of action...
January 20, 2017: Journal of Ethnopharmacology
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