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Vinpocetine

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https://www.readbyqxmd.com/read/29206914/simultaneous-determination-of-vinpocetine-and-its-major-active-metabolite-apovincaminic-acid-in-rats-by-uplc-ms-ms-and-its-application-to-the-brain-tissue-distribution-study
#1
Manman Wang, Lijuan Wang, Jinghan Sun, Lili Zhang, Longshan Zhao, Zhili Xiong
A specific, rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS) method was developed for simultaneous determination of vinpocetine (VP) and its active metabolite, apovincaminic acid (AVA) in rat brain regions, such as hypothalamus, striatum, cortex, cerebellum and hippocampus. Phenacetin was used as internal standard (IS). Brain tissue samples were precipitated protein by using 500 μL methanol. The separation was achieved on a Waters ACQUITY UPLC BEH C18 column (100 mm × 2...
December 1, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29183836/an-update-on-vinpocetine-new-discoveries-and-clinical-implications
#2
REVIEW
Yi-Shuai Zhang, Jian-Dong Li, Chen Yan
Vinpocetine, a derivative of the alkaloid vincamine, has been clinically used in many countries for treatment of cerebrovascular disorders such as stroke and dementia for more than 30 years. Currently, vinpocetine is also available in the market as a dietary supplement to enhance cognition and memory. Due to its excellent safety profile, increasing efforts have been put into exploring the novel therapeutic effects and mechanism of actions of vinpocetine in various cell types and disease models. Recent studies have revealed a number of novel functions of vinpocetine, including anti-inflammation, antagonizing injury-induced vascular remodeling and high-fat-diet-induced atherosclerosis, as well as attenuating pathological cardiac remodeling...
November 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29178152/identification-characterization-and-distribution-of-terpene-indole-alkaloids-in-ethanolic-extracts-of-catharanthus-roseus-using-hplc-esi-qtof-ms-ms-and-the-study-of-their-geographical-variation
#3
Sunil Kumar, Vikas Bajpai, Awantika Singh, Brijesh Kumar
RATIONALE: Catharanthus roseus is a well-known dicotyledonous medicinal plant containing diverse classes of bioactive terpene indole alkaloids (TIAs), in particular the anticancer agents, vinblastine and vincristine. In view of the commercial importance of these compounds there is an urgent need to develop an accurate and reliable method for the screening of TIAs from C. roseus. METHODS: A method for the separation and characterization of these compounds was developed using high performance liquid chromatography coupled with positive electrospray ionization quadrupole time of flight tandem mass spectrometry (HPLC/ESI-QTOF-MS/MS)...
November 26, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29155086/systemic-exposure-of-vinpocetine-in-pregnant-sprague-dawley-rats-following-repeated-oral-exposure-an-investigation-of-fetal-transfer
#4
Suramya Waidyanatha, Heather Toy, Natalie South, Seth Gibbs, Esra Mutlu, Brian Burback, Barry S McIntyre, Natasha Catlin
Vinpocetine is being used worldwide by people of all ages, including pregnant women, for its purported multiple health benefits. However, limited data is available addressing the safety/toxicity of vinpocetine. The National Toxicology Program conducted studies to examine potential effects of vinpocetine on the developing rat. Disposition data is helpful to put the fetal findings into context and provide information on the potential risk for humans. The current study reports the systemic exposure and toxicokinetic (TK) parameters of vinpocetine and metabolite, apovincaminic acid (AVA), in pregnant Harlan Sprague Dawley rats, fetuses and amniotic fluid following oral gavage exposure of dams to 5 and 20mg/kg vinpocetine from gestational day 6 to 18...
November 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29129665/intravasation-of-sw620-colon-cancer-cell-spheroids-through-the-blood-endothelial-barrier-is-inhibited-by-clinical-drugs-and-flavonoids-in-vitro
#5
Silvio Holzner, Stefan Brenner, Atanas Georgiev Atanasov, Daniel Senfter, Serena Stadler, Chi Huu Nguyen, Adryan Fristiohady, Daniela Milovanovic, Nicole Huttary, Sigurd Krieger, Zsuzsanna Bago-Horvath, Oliver de Wever, Ioannis Tentes, Ali Özmen, Walter Jäger, Helmut Dolznig, Verena Maria Dirsch, Robert Michael Mader, Liselotte Krenn, Georg Krupitza
Mechanisms how colorectal cancer (CRC) cells penetrate blood micro-vessel endothelia and metastasise is poorly understood. To study blood endothelial cell (BEC) barrier breaching by CRC emboli, an in vitro assay measuring BEC-free areas underneath SW620 cell spheroids, so called "circular chemorepellent induced defects" (CCIDs, appearing in consequence of endothelial retraction), was adapted and supported by Western blotting, EIA-, EROD- and luciferase reporter assays. Inhibition of ALOX12 or NF-κB in SW620 cells or BECs, respectively, caused attenuation of CCIDs...
November 10, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29113305/vinpocetine-alleviate-cerebral-ischemia-reperfusion-injury-by-down-regulating-tlr4-myd88-nf-%C3%AE%C2%BAb-signaling
#6
Li-Rong Wu, Liang Liu, Xiao-Yi Xiong, Qin Zhang, Fa-Xiang Wang, Chang-Xiong Gong, Qi Zhong, Yuan-Rui Yang, Zhao-You Meng, Qing-Wu Yang
Inflammatory responses play crucial roles in cerebral ischemia/reperfusion injury. Toll-like receptor 4 (TLR4) is an important mediator of the neuroinflammatory response to cerebral ischemia/reperfusion injury. Vinpocetine is a derivative of the alkaloid vincamine and exerts an anti-inflammatory effect by inhibiting NF-κB activation. However, the effects of vinpocetine on pathways upstream of NF-κB signaling, such as TLR4, have not been fully elucidated. Here, we used mouse middle cerebral artery occlusion (MCAO) and cell-based oxygen-glucose deprivation (OGD) models to evaluate the therapeutic effects and mechanisms of vinpocetine treatment...
October 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/29106899/vinpocetine-protects-inner-retinal-neurons-with-functional-nmda-glutamate-receptors-against-retinal-ischemia
#7
Lisa Nivison-Smith, Pauline Khoo, Monica L Acosta, Michael Kalloniatis
Retinal ischemia is involved in the pathogenesis of many major vision threatening diseases. Vinpocetine is a natural drug, which has a range of neuroprotective actions against retinal ischemia including modulating cation flow, improving metabolic activity and preventing apoptosis. The exact mechanism behind these actions remains unknown but may involve glutamate receptors, major components of the ischemic cascade. This study examined the effects of vinpocetine in association with specific ionotropic glutamate receptor agonists: N-methyl-D-aspartate (NMDA) and kainate...
November 4, 2017: Experimental Eye Research
https://www.readbyqxmd.com/read/29043863/preparation-and-evaluation-of-vinpocetine-self-emulsifying-ph-gradient-release-pellets
#8
Mengqi Liu, Shiming Zhang, Shuxia Cui, Fen Chen, Lianqun Jia, Shu Wang, Xiumei Gai, Pingfei Li, Feifei Yang, Weisan Pan, Xinggang Yang
The main objective of this study was to develop a pH gradient release pellet with self-emulsifying drug delivery system (SEDDS), which could not only improve the oral bioavailability of Vinpocetine (VIN), a poor soluble drug, but reduce the fluctuation of plasma concentration. First, the liquid VIN SEDDS formulation was prepared. Then the self-emulsifying pH gradient release pellets were prepared by extrusion spheronization technique, and formulation consisted by the liquid SEDDS, absorbent (colloidal silicon dioxide), penetration enhancer (sodium chloride), microcrystalline cellulose, ethyl alcohol, and three coating materials (HPMC, Eudragit L30D55, Eudragit FS30D) were eventually selected...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28931329/cramps-and-vinpocetine-in-als
#9
Mamede de Carvalho
No abstract text is available yet for this article.
September 21, 2017: Amyotrophic Lateral Sclerosis and Frontotemporal Degeneration
https://www.readbyqxmd.com/read/28843828/vinpocetine-mitigates-proteinuria-and-podocytes-injury-in-a-rat-model-of-diabetic-nephropathy
#10
Walaa Wadie, Dalia M El-Tanbouly
Podocyte injury and glomerular basement membrane thickening have been considered as essential pathophysiological events in diabetic nephropathy. The aim of this study was to investigate the possible beneficial effects of vinpocetine on diabetes-associated renal damage. Male Wistar rats were made diabetic by injection of streptozotocin (STZ). Diabetic rats were treated with vinpocetine in a dose of 20mg/kg/day for 6 weeks. Treatment with vinpocetine resulted in a marked decrease in the levels of blood glucose, glycosylated haemoglobin, creatinine, blood urea nitrogen, urinary albumin and albumin/creatinine ratio along with an elevation in creatinine clearance rate...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28799255/synergy-between-5-ht4-receptor-stimulation-and-phosphodiesterase-4-inhibition-in-facilitating-acetylcholine-release-in-human-large-intestinal-circular-muscle
#11
V Pauwelyn, W Ceelen, R A Lefebvre
BACKGROUND: Gastroprokinetic properties of 5-HT4 receptor agonists, such as prucalopride, are attributed to activation of 5-HT4 receptors on cholinergic nerves innervating smooth muscle in the gastrointestinal smooth muscle layer, increasing acetylcholine release and muscle contraction. In porcine stomach and colon, phosphodiesterase (PDE) 4 has been shown to control the signaling pathway of these 5-HT4 receptors. The aim of this study was to investigate the PDE-mediated control of these 5-HT4 receptors in human large intestine...
August 10, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28757393/a-comparative-study-on-the-anti-schistosomal-and-hepatoprotective-effects-of-vinpocetine-and-isosorbide-5-mononitrate-on-schistosoma-mansoni-infected-mice
#12
Samar M Alhusseiny, Samar N El-Beshbishi, Maha M Abu Hashim, Hosam El-Dein E El-Nemr, Aya E Handoussa
Schistosomiasis is a remarkable public health problem in developing countries. Presently, praziquantel is the optional drug for all human schistosomiasis. Owing to the increased praziquantel resistance, there is an urgent need to develop new alternatives. This study aims at determining the anti-schistosomal and/or the hepatoprotective effects of the anti-inflammatory drug; vinpocetine, and the vasodilator and the nitric oxide donor; isosorbide-5-mononitrate, in comparison to praziquantel. In the present research, the therapeutic efficacies of these drugs were assessed in Swiss albino female mice (CD-I strain) experimentally infected with an Egyptian strain of Schistosoma mansoni, using some general, parasitological, and histopathological parameters...
December 2017: Acta Tropica
https://www.readbyqxmd.com/read/28691141/vinpocetine-inhibits-nf-%C3%AE%C2%BAb-dependent-inflammation-in-acute-ischemic-stroke-patients
#13
Fang Zhang, Chen Yan, Changjuan Wei, Yang Yao, Xiaofeng Ma, Zhongying Gong, Shoufeng Liu, Dawei Zang, Jieli Chen, Fu-Dong Shi, Junwei Hao
Immunity and inflammation play critical roles in the pathogenesis of acute ischemic stroke. Therefore, immune intervention, as a new therapeutic strategy, is worthy of exploration. Here, we tested the inflammation modulator, vinpocetine, for its effect on the outcomes of stroke. For this multi-center study, we recruited 60 patients with anterior cerebral circulation occlusion and onset of stroke that had exceeded 4.5 h but lasted less than 48 h. These patients, after random division into two groups, received either standard management alone (controls) or standard management plus vinpocetine (30 mg per day intravenously for 14 consecutive days, Gedeon Richter Plc...
July 9, 2017: Translational Stroke Research
https://www.readbyqxmd.com/read/28638040/-complex-application-2-ethyl-6-methyl-3-hydroxypyridine-succinate-and-vinpocetine-in-cerebrovascular-disorder
#14
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
#15
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...
June 8, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28321644/vinpocetine-attenuates-pathological-cardiac-remodeling-by-inhibiting-cardiac-hypertrophy-and-fibrosis
#16
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)...
April 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
#17
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
#18
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
#19
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...
April 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
#20
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
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