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Vinpocetine

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https://www.readbyqxmd.com/read/28638040/-complex-application-2-ethyl-6-methyl-3-hydroxypyridine-succinate-and-vinpocetine-in-cerebrovascular-disorder
#1
E Yu Solovyeva, A N Karneev, A V Chekanov, O A Baranova, I V Choi
Developing brain ischemia due to cerebral vascularization leads to disruption of brain metabolism. Chronic cerebral hypoperfusion leads to irreversible brain damage and plays an important role in the development of some types of dementia. Early use of antioxidants such as ethyl ether apovincamine acid (vinpocetine) and 2-ethyl-6-methyl-3-hydroxypyridine-succinate in the treatment of this pathology is seen as a real pathogenetically based method of correction of cerebral metabolism with cerebral vascular disorders, demonstrating the increase in cerebral blood flow and also neuroprotective effects...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28540754/zero-order-release-and-bioavailability-enhancement-of-poorly-water-soluble-vinpocetine-from-self-nanoemulsifying-osmotic-pump-tablet
#2
Sally A El-Zahaby, Mohamed H H AbouGhaly, Ghada A Abdelbary, Omaima N El-Gazayerly
Solid self-nanoemulsifying (S-SNEDDS) asymmetrically coated osmotic tablets of the poorly water-soluble drug Vinpocetine (VNP) were designed. The aim was to control the release of VNP by the osmotic technology taking advantage of the solubility and bioavailability-enhancing capacity of S-SNEDDS. Liquid SNEDDS loaded with 2.5 mg VNP composed of Maisine™ 35-1, Transcutol® HP and Cremophor(®) EL was adsorbed on the solid carrier Aeroperl(®). S-SNEDDS was mixed with the osmotic tablet excipients (Sodium chloride, Avicel(®), HPMC-K4M, PVP-K30 and Lubripharm(®)), then directly compressed to form the core tablet...
May 25, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28321644/vinpocetine-attenuates-pathological-cardiac-remodeling-by-inhibiting-cardiac-hypertrophy-and-fibrosis
#3
Mei-Ping Wu, Yi-Shuai Zhang, Xiangbin Xu, Qian Zhou, Jian-Dong Li, Chen Yan
PURPOSE: Pathological cardiac remodeling, characterized by cardiac hypertrophy and fibrosis, is a pathological feature of many cardiac disorders that leads to heart failure and cardiac arrest. Vinpocetine, a derivative of the alkaloid vincamine, has been used for enhancing cerebral blood flow to treat cognitive impairment. However, its role in pathological cardiac remodeling remains unknown. The aim of this study is to examine the effect of vinpocetine on pathological cardiac remodeling induced by chronic stimulation with angiotensin II (Ang II)...
March 20, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28315429/vinpocetine-reduces-diclofenac-induced-acute-kidney-injury-through-inhibition-of-oxidative-stress-apoptosis-cytokine-production-and-nf-%C3%AE%C2%BAb-activation-in-mice
#4
Victor Fattori, Sergio M Borghi, Carla F S Guazelli, Andressa C Giroldo, Jefferson Crespigio, Allan J C Bussmann, Letícia Coelho-Silva, Natasha G Ludwig, Tânia L Mazzuco, Rubia Casagrande, Waldiceu A Verri
Acute kidney injury (AKI) represents a complex clinical condition associated with significant morbidity and mortality. Approximately, 19-33% AKI episodes in hospitalized patients are related to drug-induced nephrotoxicity. Although, considered safe, non-steroidal anti-inflammatory drugs such as diclofenac have received special attention in the past years due to the potential risk of renal damage. Vinpocetine is a nootropic drug known to have anti-inflammatory properties. In this study, we investigated the effect and mechanisms of vinpocetine in a model of diclofenac-induced AKI...
June 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28296551/the-ameliorative-effects-of-vinpocetine-on-apoptosis-and-hsp-70-expression-in-testicular-torsion-in-rats
#5
M F Sönmez, Ş Ozdemir, M Guzel, E Kaymak
Vinpocetine is a potent antioxidant and free radical scavenger. We investigated the effects of vinpocetine on torsion/detorsion (T/D) induced testicular damage, HSP-70 expression and germ cell apoptosis in rats. Sixty Wistar albino adult male rats were divided into five groups of 12. The groups comprised a control group, a sham treated group, a T/D group, a vinpocetine treated group, and a T/D plus vinpocetine treated group. The left testis of each rat was subjected to unilateral torsion followed by detorsion after 2 h...
2017: Biotechnic & Histochemistry: Official Publication of the Biological Stain Commission
https://www.readbyqxmd.com/read/28188510/medication-use-and-risk-of-falls-among-nursing-home-residents-a-retrospective-cohort-study
#6
Andrea Bor, Mária Matuz, Márta Csatordai, Gábor Szalai, András Bálint, Ria Benkő, Gyöngyvér Soós, Péter Doró
Background Geriatric falls are leading causes of hospital trauma admissions and injury-related deaths. Medication use is a crucial element among extrinsic risk factors for falls. To reduce fall risk and the prevalence of adverse drug reactions, potentially inappropriate medication (PIM) lists are widely used. Objective Our aim was to investigate the possible predictors of geriatric falls annualized over a 5-year-long period, as well as to evaluate the medication use of nursing home residents. Setting Nursing home residents were recruited from the same institution between 2010 and 2015 in Szeged, Hungary...
February 10, 2017: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/28151022/enhanced-blood-brain-barrier-transport-of-vinpocetine-by-oral-delivery-of-mixed-micelles-in-combination-with-a-message-guider
#7
Jiaojiao Ding, Yujiao Sun, Jinfeng Li, Huimin Wang, Shirui Mao
The blood-brain barrier represents an insurmountable obstacle for the therapy of central nervous system related diseases. Polymeric micelles have many desirable properties for brain targeting by oral delivery, but the stability and targeting efficiency needs to be improved. In this study, it was demonstrated that binary micelle system can compensate the drawbacks of mono system by preparing mixed micelles in combination with PEG-based copolymers. Here, we explored a brain targeting drug delivery system via facile approaches using P123 based mixed micelles in combination with a message guider from traditional Chinese medicine, borneol, for oral delivery...
July 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28074742/development-and-validation-of-an-rp-hplc-method-for-the-determination-of-vinpocetine-and-folic-acid-in-the-presence-of-a-vinpocetine-alkaline-degradation-product-in-bulk-and-in-capsule-form
#8
Ehab F Elkady, Marwa H Tammam, Ayman A Mohamed
An alkaline-forced degradation hydrolytic product of vinpocetine was prepared and characterized by 1H-NMR, FTIR spectroscopy, and MS. Subsequently, a simple, selective, and validated reversed-phase HPLC method was developed for the simultaneous estimation of vinpocetine and folic acid in the presence of a vinpocetine alkaline degradation product. Chromatographic separation was achieved using an isocratic mobile phase consisting of acetonitrile-0.02 M KH2PO4 [containing 0.2% (v/v) triethylamine and adjusted to pH 6 with orthophosphoric acid; (80 + 20, v/v)] at a flow rate of 0...
May 1, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28052870/phosphodiesterase-5-inhibition-ameliorates-angiotensin-ii-dependent-hypertension-and-renal-vascular-dysfunction
#9
Manuel Thieme, Sema Hayriye Sivritas, Evanthia Mergia, Sebastian Alexander Potthoff, Guang Yang, Lydia Hering, Katharina Grave, Henning Hoch, Lars Christian Rump, Johannes Stegbauer
Changes in renal hemodynamics have a major impact on blood pressure (BP). Angiotensin (Ang) II has been shown to induce vascular dysfunction by interacting with phosphodiesterases (PDE)1 and PDE5. The predominant PDE isoform responsible for renal vascular dysfunction in hypertension is unknown. Here, we measured effects of PDE5-(sildenafil) or PDE1-(vinpocetine) inhibition on renal blood flow (RBF), BP and renal vascular function in normotensive and hypertensive mice. During acute short-term Ang II infusion, sildenafil decreased BP and increased RBF in C57BL/6 (WT) mice...
January 4, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/27967259/vinpocetine-inhibited-the-cpg-oligodeoxynucleotide-induced-immune-response-in-plasmacytoid-dendritic-cells
#10
Xungang Feng, Yuzhong Wang, Yanlei Hao, Qun Ma, Jun Dai, Zhibo Liang, Yantao Liu, Xiangyuan Li, Yan Song, Chuanping Si
Plasmacytoid dendritic cells (pDCs) exert dual roles in immune responses through inducing inflammation and maintaining immune tolerance. A switch of pDC phenotype from pro-inflammation to tolerance has therapeutic promise in the treatment of autoimmune diseases. Vinpocetine, a vasoactive vinca alkaloid extracted from the periwinkle plant, has recently emerged as an immunomodulatory agent. In this study, we evaluated the effect of vinpocetine on phenotype of pDCs isolated from C57BL/6 mice and explored its possible mechanism...
April 2017: Immunological Investigations
https://www.readbyqxmd.com/read/27899287/pre-treatment-with-vinpocetine-protects-against-retinal-ischemia
#11
Lisa Nivison-Smith, Pauline Khoo, Monica L Acosta, Michael Kalloniatis
Vinpocetine has been shown to have beneficial effects for tissues of the central nervous system subjected to ischemia and other related metabolic insults. We recently showed vinpocetine promotes glucose availability, prevents unregulated cation channel permeability and regulates glial reactivity when present during retinal ischemia. Less is known however about the ability of vinpocetine to protect against future ischemic insults. This study explores the effect of vinpocetine when used as a pre-treatment in an ex vivo model for retinal ischemia using cation channel permeability of agmatine (AGB) combined with immunohistochemistry as a measure for cell functionality...
January 2017: Experimental Eye Research
https://www.readbyqxmd.com/read/27789032/improving-biopharmaceutical-properties-of-vinpocetine-through-cocrystallization
#12
Samuel Golob, Miranda Perry, Matteo Lusi, Michele R Chierotti, Iztok Grabnar, Lucia Lassiani, Dario Voinovich, Michael J Zaworotko
Vinpocetine is a poorly water soluble weakly basic drug (pKa = 7.1) used for the treatment of several cerebrovascular and cognitive disorders. Because existing formulations exhibit poor bioavailability and scarce absorption, a dosage form with improved pharmacokinetic properties is highly desirable. Cocrystallization represents a promising approach to generate diverse novel crystal forms and to improve the aqueous solubility and in turn the oral bioavailability. In this article, a novel ionic cocrystal of vinpocetine is described, using boric acid as a coformer, and fully characterized (by means of differential scanning calorimetry, solid-state nuclear magnetic resonance, powder and single-crystal X-ray diffraction, and powder dissolution test)...
October 24, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27677308/ahr-cyp1a1-interplay-triggers-lymphatic-barrier-breaching-in-breast-cancer-spheroids-by-inducing-12-s-hete-synthesis
#13
Chi Huu Nguyen, Stefan Brenner, Nicole Huttary, Atanas Georgiev Atanasov, Verena Maria Dirsch, Waranya Chatuphonprasert, Sivio Holzner, Serena Stadler, Juliane Riha, Sigurd Krieger, Rainer de Martin, Zsuzsanna Bago-Horvath, Georg Krupitza, Walter Jäger
A causal link between overexpression of aryl hydrocarbon receptor (AHR) and its target cytochrome P450 1A1 (CYP1A1) and metastatic outgrowth of various cancer entities has been established. Nevertheless, the mechanism how AHR/CYP1A1 support metastasis formation is still little understood. In vitro we discovered a potential mechanism facilitating tumour dissemination based on the production of 12(S)-hydroxyeicosatetraenoic acid (12(S)-HETE). Utilising a three-dimensional lymph endothelial cell (LEC) monolayer & MDA-MB231 breast cancer cell spheroid co-culture model in combination with knock-down approach allowed elucidation of the molecular/biochemical basis of AHR/CYP1A1-induced tumour breaching through the LEC barrier...
September 27, 2016: Human Molecular Genetics
https://www.readbyqxmd.com/read/27614144/early-ethanol-exposure-and-vinpocetine-treatment-alter-learning-and-memory-related-proteins-in-the-rat-hippocampus-and-prefrontal-cortex
#14
Patricia C Swart, Christopher B Currin, Vivienne A Russell, Jacqueline J Dimatelis
This study investigates the effects of early exposure to ethanol on cognitive function and neural plasticity-related proteins in the rat brain. Sprague-Dawley rats were administered 12% ethanol solution (4 g/kg/day i.p.) or saline from P4 to P9. Vinpocetine, a phosphodiesterase type 1 inhibitor, was tested to determine whether it could reverse any changes induced by early ethanol exposure. Hence, from P25 to P31, ethanol-exposed male rats were injected with vinpocetine (20 mg/kg/day i.p.) or vehicle (DMSO) prior to undergoing behavioral testing in the open field and Morris water maze (MWM) tests...
May 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/27589055/vinpocetine-attenuates-the-osteoblastic-differentiation-of-vascular-smooth-muscle-cells
#15
Yun-Yun Ma, Lin Sun, Xiu-Juan Chen, Na Wang, Peng-Fei Yi, Min Song, Bo Zhang, Yu-Zhong Wang, Qiu-Hua Liang
Vascular calcification is an active process of osteoblastic differentiation of vascular smooth muscle cells; however, its definite mechanism remains unknown. Vinpocetine, a derivative of the alkaloid vincamine, has been demonstrated to inhibit the high glucose-induced proliferation of vascular smooth muscle cells; however, it remains unknown whether vinpocetine can affect the osteoblastic differentiation of vascular smooth muscle cells. We hereby investigated the effect of vinpocetine on vascular calcification using a beta-glycerophosphate-induced cell model...
2016: PloS One
https://www.readbyqxmd.com/read/27500876/-an-experimental-in-vitro-study-of-antioxidant-and-antiradical-properties-of-cytoflavin-vinpocetine-actovegin-and-ethylmethylhydroxypyridine-succinate
#16
Trofimova S A, Dubinina E E, Balunov O A, Leonova N V
AIM: To investigate experimentally in vitro the antioxidant and anti-radical activity of several drugs. MATERIAL AND METHODS: Antioxidant activity was assessed by induced luminol-dependent chemiluminescence (CL). An impact on the generation of reactive oxygen species (O2-, OH, 1D, H2O2, HClO) and their ability to inhibit the auto-oxidation of quercetin combined with the generation of superoxide radical anion were determined. Anti-radical activity was studied by the method of restoring a stable radical α-α-diphenyl-β-picryl hydrazine (DPPH) molecule of the alleged anti-oxidant...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/27460983/swath-acquisition-mode-for-drug-metabolism-and-metabolomics-investigations
#17
Ron Bonner, Gérard Hopfgartner
AIM: Sequential window acquisition of all theoretical fragment-ion spectra (SWATH) has recently emerged as a powerful high resolution mass spectrometric data independent acquisition technique. In the present work, the potential and challenges of an integrated strategy based on LC-SWATH/MS for simultaneous drug metabolism and metabolomics studies was investigated. METHODOLOGY: The richness of SWATH data allows numerous data analysis approaches, including: detection of metabolites by prediction; metabolite detection by mass defect filtering; quantification from high-resolution MS precursor chromatograms or fragment chromatograms...
August 2016: Bioanalysis
https://www.readbyqxmd.com/read/27428180/nanostructured-drugs-embedded-into-a-polymeric-matrix-vinpocetine-pvp-hybrids-investigated-by-debye-function-analysis
#18
Dritan Hasa, Carlotta Giacobbe, Beatrice Perissutti, Dario Voinovich, Mario Grassi, Antonio Cervellino, Norberto Masciocchi, Antonietta Guagliardi
Microcrystalline vinpocetine, coground with cross-linked polyvinylpyrrolidone, affords hybrids containing nanosized drug nanocrystals, the size and size distributions of which depend on milling times and drug-to-polymer weight ratios. Using an innovative approach to microstructural characterization, we analyzed wide-angle X-ray total scattering data by the Debye function analysis and demonstrated the possibility to characterize pharmaceutical solid dispersions obtaining a reliable quantitative view of the physicochemical status of the drug dispersed in an amorphous carrier...
September 6, 2016: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/27334578/vinpocetine-improves-scopolamine-induced-learning-and-memory-dysfunction-in-c57-bl-6j-mice
#19
Yu Shang, Lei Wang, Yue Li, Pei-Fei Gu
Vinpocetine is an inhibitor of phosphodiesterase type 1 (PDE1), which has been used for treating stroke for over 40 years. However, according to current clinical dosage and treatment period, its direct effect on memory is unclear. In this study, we investigated whether vinpocetine could reverse the scopolamine (SCO)-induced cognitive deficits in animals. Behavioral experiments, including open field, Y-maze, and fear conditioning tests were used to determine the possible role of vinpocetine on scopolamine-induced memory dysfunction...
September 1, 2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27319129/quantitative-determination-of-vinpocetine-in-dietary-supplements
#20
John M T French, Matthew D King, Owen M McDougal
Current United States regulatory policies allow for the addition of pharmacologically active substances in dietary supplements if derived from a botanical source. The inclusion of certain nootropic drugs, such as vinpocetine, in dietary supplements has recently come under scrutiny due to the lack of defined dosage parameters and yet unproven short- and long-term benefits and risks to human health. This study quantified the concentration of vinpocetine in several commercially available dietary supplements and found that a highly variable range of 0...
May 2016: Natural Product Communications
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