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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...
November 26, 2016: Experimental Eye Research
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
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
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...
September 10, 2016: Journal of Neuroscience Research
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
S A Trofimova, E E Dubinina, O A Balunov, N V Leonova
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
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
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
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
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
Saylav Bora, Mumin Alper Erdogan, Güliz Armagan, Elvin Sevgili, Taner Dagcı
No abstract text is available yet for this article.
June 14, 2016: Biological Trace Element Research
Weiwei Zhang, Yining Huang, Ying Li, Liming Tan, Jianfei Nao, Hongtao Hu, Jingyu Zhang, Chen Li, Yuenan Kong, Yulin Song
OBJECTIVE: The objective of this study was to evaluate the efficacy and safety of intravenous vinpocetine administration as part of a comprehensive treatment for acute cerebral infarction in a Chinese population. METHODS: 610 acute cerebral infarction patients were randomized into two groups: the vinpocetine group (469 patients) received cytidine disphosphate choline 0.4-0.5 g in combination with aspirin 75-100 mg or clopidogrel 75 mg once daily, plus vinpocetine 30 mg intravenously once daily for 7 days, while the control group (141 patients) received cytidine disphosphate choline 0...
September 2016: Clinical Drug Investigation
E A Antipenko, A V Deryugina, A V Gustov
OBJECTIVE: To clarify the mechanisms of the action of anti-stress antioxidant agent (mexidol) in patients with chronic cerebral ischemia. MATERIAL AND METHODS: Sixty-seven patients with chronic cerebral ischemia (TE stage II),48 women and 19 men, mean age 48.2 years, were examined. To assess the stateof multilevel stress system, the level of anxiety and depression, degree of autonomic imbalance, adaptive reactions of the blood and functional properties of erythrocyte membranes, level of average weight molecules in the blood plasma were studied...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Ejder Saylav Bora, Alper Mümin Erdoğan, Güliz Armagan, Elvin Sevgili, Taner Dagcı
Increased concentration of manganese (Mn) in the brain is known to be associated with excitotoxicity and neuroinflammation. Vinpocetine, an alkaloid derived from the plant Vinca minor L., basically shows its effect via phosphodiesterase inhibition and voltage-dependent Na(+) channels. Vasoactive intestinal peptide (VIP) has gastrointestinal, vasomotor, muscular, and neuroprotective effects. The aim of this study was to examine the potential protective effects of vinpocetine and VIP against Mn toxicity in NE-4C neural stem cells (NSCs)...
May 20, 2016: Biological Trace Element Research
Lingti Kong, Chunli Song, Linhu Ye, Daohua Guo, Meiling Yu, Rong Xing
Vinpocetine is a derivative of the alkaloid vincamine, which had been prescribed for chronic cerebral vascular ischemia and acute ischemic stroke or used as a dietary supplement for its several different mechanisms of biological activities. However, information on the cytochrome P450 (CYP) enzyme-mediated drug metabolism has not been previously studied. The present study was performed to investigate the effects of vinpocetine on CYPs activity, and cocktail method was used, respectively. To evaluate the effects of vinpocetine on the activity of human CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP2E1, human liver microsomes were utilized to incubate with the mixed CYPs probe substrates and the target components...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
Run Wang, Yong Xu
The aim of present study was to develop VIN-loaded mPEG-PLA nanoparticle systems. The VIN mPEG-PLA nanoparticles were prepared using an emulsion solvent evaporation method, and studied their particle size, morphology, encapsulation efficiency and drug-loading coefficient. Moreover, the nanoparticles were evaluated on the drug release behaviors in vitro and bioavailability in vivo. The results show that the spherical nanoparticles obtained were negatively charged with a zeta potential of about -23.4 mV and characterized ∼110 nm with a narrow size distribution...
February 2, 2016: Artificial Cells, Nanomedicine, and Biotechnology
Maria Sitges, Blanca Irene Aldana, Ronald Charles Reed
Seizures are accompanied by an exacerbated activation of cerebral ion channels. 4-aminopyridine (4-AP) is a pro-convulsive agent which mechanism of action involves activation of Na(+) and Ca(2+) channels, and several antiepileptic drugs control seizures by reducing these channels permeability. The antidepressant, sertraline, and the anti-seizure drug vinpocetine are effective inhibitors of cerebral presynaptic Na(+) channels. Here the effectiveness of these compounds to prevent the epileptiform EEG activity induced by 4-AP was compared with the effectiveness of seven conventional antiepileptic drugs...
June 2016: Neurochemical Research
María Sitges, Luz María Chiu, Ronald C Reed
Ion channels are targets of various antiepileptic drugs. In cerebral presynaptic nerve endings Na(+) and Ca(2+) channels are particularly abundant, as they control neurotransmitter release, including the release of glutamate (Glu), the most concentrated excitatory amino acid neurotransmitter in the brain. Several pre-synaptic channels are implicated in the mechanism of action of the pro-convulsive agent, 4-aminopyridine (4-AP). In the present study the effects of levetiracetam and other established and newer (vinpocetine) anti-epileptic drugs, as well as of the anti-depressant, sertraline on the increase in Ca(2+) induced by 4-AP in hippocampal isolated nerve endings were investigated...
April 2016: Neurochemical Research
F Ghayomi, M Navaei-Nigjeh, M Baeeri, M A Rezvanfar, M Abdollahi
BACKGROUND: Chlorpyrifos (CP) is an organophosphorus pesticide that induces oxidative stress through the production of free radicals and depletes intracellular antioxidant reserves. In this study, the efficacy of three antioxidants (melatonin, coenzyme Q10 (CoQ10), and vinpocetine) on alleviation of toxic effects of CP was evaluated. MATERIALS AND METHODS: Cytotoxicity of CP, in the presence or absence of effective doses of melatonin, CoQ10, and vinpocetine, was determined in human peripheral blood lymphocytes after 72-h exposure...
August 2016: Human & Experimental Toxicology
Patrizzia Mastromatteo-Alberga, Fabiola Placeres-Uray, Marcelo A Alfonzo-González, Ramona Gonzalez de Alfonzo, Itala Lippo de Becemberg, Marcelo J Alfonzo
Muscarinic antagonists, via muscarinic receptors increase the cAMP/cGMP levels at bovine tracheal smooth muscle (BTSM) through the inhibition of phosphodiesterases (PDEs), displaying a similar behavior of vinpocetine (a specific-PDE1 inhibitor). The presence of PDE1 hydrolyzing both cyclic nucleotides in BTSM strips was revealed. Moreover, a vinpocetine and muscarinic antagonists inhibited PDE1 located at plasma membranes (PM) fractions from BTSM showing such inhibition, an M(2)AChR pharmacological profile...
2016: Journal of Receptor and Signal Transduction Research
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