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1

Vlok, Nevil, Sarel F. Malan, Neal Castagnoli, Jacobus J. Bergh, and Jacobus P. Petzer. "Inhibition of monoamine oxidase B by analogues of the adenosine A2A receptor antagonist (E)-8-(3-chlorostyryl)caffeine (CSC)." Bioorganic & Medicinal Chemistry 14, no. 10 (2006): 3512–21. http://dx.doi.org/10.1016/j.bmc.2006.01.011.

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2

Rivara, Silvia, Giovanni Piersanti, Francesca Bartoccini, et al. "Synthesis of (E)-8-(3-Chlorostyryl)caffeine Analogues Leading to 9-Deazaxanthine Derivatives as Dual A2A Antagonists/MAO-B Inhibitors." Journal of Medicinal Chemistry 56, no. 3 (2013): 1247–61. http://dx.doi.org/10.1021/jm301686s.

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3

Jacobson, Kenneth A., Olga Nikodijević, William L. Padgett, Carola Gallo-Rodriguez, Michel Maillard, and John W. Daly. "8-(3-Chlorostyryl)caffeine (CSC) is a selective A2 -adenosine antagonist in vitro and in vivo." FEBS Letters 323, no. 1-2 (1993): 141–44. http://dx.doi.org/10.1016/0014-5793(93)81466-d.

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4

Chen, Jiang-Fan, Salome Steyn, Roland Staal, et al. "8-(3-Chlorostyryl)caffeine May Attenuate MPTP Neurotoxicity through Dual Actions of Monoamine Oxidase Inhibition and A2AReceptor Antagonism." Journal of Biological Chemistry 277, no. 39 (2002): 36040–44. http://dx.doi.org/10.1074/jbc.m206830200.

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5

Gołembiowska, Krystyna, and Anna Dziubina. "Effect of the adenosine A2A receptor antagonist 8-(3-chlorostyryl)caffeine on l-DOPA biotransformation in rat striatum." Brain Research 998, no. 2 (2004): 208–17. http://dx.doi.org/10.1016/j.brainres.2003.11.028.

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6

Frédérick, Raphaël, Frederic Ooms, Neal Castagnoli Jr, et al. "(E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting both as antagonist of adenosine A2A receptors and as inhibitor of MAO-B." Acta Crystallographica Section C Crystal Structure Communications 61, no. 9 (2005): o531—o532. http://dx.doi.org/10.1107/s0108270105023140.

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7

Thümmler, Susanne, and Thomas V. Dunwiddie. "Adenosine Receptor Antagonists Induce Persistent Bursting in the Rat Hippocampal CA3 Region Via an NMDA Receptor-Dependent Mechanism." Journal of Neurophysiology 83, no. 4 (2000): 1787–95. http://dx.doi.org/10.1152/jn.2000.83.4.1787.

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Adenosine receptor antagonists initiate repetitive bursting activity in the CA3 region of hippocampal slices. Although some studies have suggested that this effect is irreversible, this has been difficult to establish because many adenosine antagonists wash out of brain slices extremely slowly. Furthermore the cellular mechanism that underlies persistent bursting is unknown. To resolve these issues, we studied the effects of nonselective (8-p-sulfophenyltheophylline, 8SPT, 50–100 μM), Al-selective (8-cyclopentyl-1,3-dipropylxanthine, 100 nM; xanthine carboxylic acid congener, 200 nM), and A2A-
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8

Xu, H., B. Stein, and B. Liang. "Characterization of a stimulatory adenosine A2a receptor in adult rat ventricular myocyte." American Journal of Physiology-Heart and Circulatory Physiology 270, no. 5 (1996): H1655—H1661. http://dx.doi.org/10.1152/ajpheart.1996.270.5.h1655.

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The expression and function of stimulatory adenosine A2 receptor on the cardiac myocyte is not well defined. The objective of the present study is to characterize the A2a receptor in adult rat cardiac ventricular myocytes. After selection of an optimal lot of collagenase for myocyte isolation and for consistent measurement of adenosine-mediated responses, the A1-receptor pathway was inactivated by pertussis toxin and by the A1-selective antagonist 1,3-dipropyl-8-cyclopentylxanthine. Effects of the adenosine agonist and antagonist or cardiac myocyte contractile amplitude and on adenosine 3',5'-
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9

Macala, Lawrence J., and John P. Hayslett. "Basolateral and apical A1 adenosine receptors mediate sodium transport in cultured renal epithelial (A6) cells." American Journal of Physiology-Renal Physiology 283, no. 6 (2002): F1216—F1225. http://dx.doi.org/10.1152/ajprenal.00085.2002.

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There are conflicting reports in the literature regarding the adenosine receptor that mediates the increase in sodium transport in the A6 cell. In this study we used specific A1 and A2 adenosine receptor agonists and antagonists, as well as two different subclones of the A6 cell, to determine which adenosine receptor mediates the increase in sodium transport. In the A6S2 subclone, basolateral and apical N 6-cyclohexyladenosine (CHA), a selective A1 receptor agonist, stimulated sodium transport at a threshold concentration <10−7 M, whereas CGS-21680, a selective A2 receptor agonist, had a th
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10

Merkus, Daphne, David W. Stepp, Deron W. Jones, Yasuhiro Nishikawa, and William M. Chilian. "Adenosine preconditions against endothelin-induced constriction of coronary arterioles." American Journal of Physiology-Heart and Circulatory Physiology 279, no. 6 (2000): H2593—H2597. http://dx.doi.org/10.1152/ajpheart.2000.279.6.h2593.

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Myocardial hypoperfusion is accompanied by concomitant increases in adenosine and endothelin-1 (ET-1) production, but the vasodilatory effect of adenosine prevails over that of ET-1. Therefore, we hypothesized that adenosine-induced or ischemic preconditioning reduces the vasoconstrictive effect of ET-1. Coronary arteriolar diameter in vivo was measured using fluorescence microangiography in anesthetized open-thorax dogs. ET-1 (5 ng · kg−1 · min−1administered intracoronary, n = 10) induced progressive constriction over 45 min [25 ± 6% (SE)]. The constriction was blocked by preconditioning with
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11

Xu, Zhelong, Michael V. Cohen, James M. Downey, Terry L. Vanden Hoek, and Zhenhai Yao. "Attenuation of oxidant stress during reoxygenation by AMP 579 in cardiomyocytes." American Journal of Physiology-Heart and Circulatory Physiology 281, no. 6 (2001): H2585—H2589. http://dx.doi.org/10.1152/ajpheart.2001.281.6.h2585.

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AMP 579, an adenosine A1/A2 receptor agonist, has a strong anti-infarct effect when administered just before reperfusion. Because oxidative stress has been proposed to contribute to myocardial reperfusion injury, we tested whether AMP 579 can reduce the production of reactive oxidant species (ROS) during reoxygenation in cultured chick embryonic cardiomyocytes. The intracellular fluorescent probe 2′,7′-dichlorofluorescin diacetate (DCFH) was used to detect ROS. The cells were subjected to 60 min of simulated ischemia, followed by either 15 min or 3 h of reoxygenation. AMP 579 (0.5 and 1 μM), w
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12

Gu, Ruimin, Jing Wang, Yunhong Zhang, et al. "Adenosine stimulates the basolateral 50 pS K channels in the thick ascending limb of the rat kidney." American Journal of Physiology-Renal Physiology 293, no. 1 (2007): F299—F305. http://dx.doi.org/10.1152/ajprenal.00008.2007.

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We used the patch-clamp technique to examine the effect of adenosine on the basolateral K channels in the thick ascending limb (TAL) of the rat kidney. A 50-pS inwardly rectifying K channel was detected in the basolateral membrane, and the channel activity was decreased by hyperpolarization. Application of adenosine (10 μM) increased the activity of basolateral 50 pS K channels, defined by NPo, from 0.21 to 0.41. The effect of adenosine on the 50 pS K channels was mimicked by cyclohexyladenosine (CHA), which increased channel activity by a dose-dependent manner. However, inhibition of the A1 a
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13

Solenkova, Nataliya V., Viktoriya Solodushko, Michael V. Cohen, and James M. Downey. "Endogenous adenosine protects preconditioned heart during early minutes of reperfusion by activating Akt." American Journal of Physiology-Heart and Circulatory Physiology 290, no. 1 (2006): H441—H449. http://dx.doi.org/10.1152/ajpheart.00589.2005.

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Ischemic preconditioning (IPC) is thought to protect by activating survival kinases during reperfusion. We tested whether binding of adenosine receptors is also required during reperfusion and, if so, how long these receptors must be populated. Isolated rabbit hearts were subjected to 30 min of regional ischemia and 2 h of reperfusion. IPC reduced infarct size from 32.1 ± 4.6% of the risk zone in control hearts to 7.3 ± 3.6%. IPC protection was blocked by a 20-min pulse of the nonselective adenosine receptor blocker 8-( p-sulfophenyl)-theophylline when started either 5 min before or 10 min aft
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14

Krump, Eric, Serge Picard, Joseph Mancini, and Pierre Borgeat. "Suppression of Leukotriene B4 Biosynthesis by Endogenous Adenosine in Ligand-activated Human Neutrophils." Journal of Experimental Medicine 186, no. 8 (1997): 1401–6. http://dx.doi.org/10.1084/jem.186.8.1401.

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Adenosine (Ado) has been shown to suppress several functional responses of human polymorphonuclear leukocytes (PMNs). The current study investigated whether endogenous Ado regulates the biosynthesis of leukotriene (LT)B4 in ligand-stimulated PMNs. Measurements of Ado in PMN resuspended in Hanks' buffered salt solution (HBSS) or plasma showed a cell concentration– and time–dependent accumulation of the nucleoside. The removal of endogenous Ado with either Ado deaminase or the blockade of its action by the Ado A2a receptor antagonist, 8-(3-chlorostyryl) caffeine, markedly increased LTB4 biosynth
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15

Norton, Gavin R., Angela J. Woodiwiss, Robert J. McGinn, et al. "Adenosine A1receptor-mediated antiadrenergic effects are modulated by A2a receptor activation in rat heart." American Journal of Physiology-Heart and Circulatory Physiology 276, no. 2 (1999): H341—H349. http://dx.doi.org/10.1152/ajpheart.1999.276.2.h341.

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Presently, the physiological significance of myocardial adenosine A2a receptor stimulation is unclear. In this study, the influence of adenosine A2a receptor activation on A1 receptor-mediated antiadrenergic actions was studied using constant-flow perfused rat hearts and isolated rat ventricular myocytes. In isolated perfused hearts, the selective A2a receptor antagonists 8-(3-chlorostyryl)caffeine (CSC) and 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol (ZM-241385) potentiated adenosine-mediated decreases in isoproterenol (Iso; 10−8 M)-elicited contractil
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16

Das, Samarjit, Gerald A. Cordis, Nilanjana Maulik, and Dipak K. Das. "Pharmacological preconditioning with resveratrol: role of CREB-dependent Bcl-2 signaling via adenosine A3 receptor activation." American Journal of Physiology-Heart and Circulatory Physiology 288, no. 1 (2005): H328—H335. http://dx.doi.org/10.1152/ajpheart.00453.2004.

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Recent studies demonstrated that resveratrol, a grape-derived polyphenolic phytoalexin, provides pharmacological preconditioning (PC) of the heart through a NO-dependent mechanism. Because adenosine receptors play a role in PC, we examined whether they play any role in resveratrol PC. Rats were randomly assigned to groups perfused for 15 min with 1) Krebs-Henseleit bicarbonate buffer (KHB) only; 2) KHB containing 10 μM resveratrol; 3) 10 μM resveratrol + 1 μM 8-cyclopentyl-1,3-dimethylxanthine (CPT; adenosine A1 receptor blocker); 4) 10 μM resveratrol + 1 μM 8-(3-chlorostyryl)caffeine (CSC; ad
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17

Thibault, Nathalie, Danielle Harbour, Pierre Borgeat, Paul H. Naccache, and Sylvain G. Bourgoin. "Adenosine receptor occupancy suppresses chemoattractant-induced phospholipase D activity by diminishing membrane recruitment of small GTPases." Blood 95, no. 2 (2000): 519–27. http://dx.doi.org/10.1182/blood.v95.2.519.

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Adenosine (Ado) is an important autocrine modulator of neutrophil functions. In this study, we determined the effects of endogenous Ado on fMet-Leu-Phe (fMLP)–induced phospholipase D (PLD) activity in neutrophils. The removal of extracellular Ado by Ado deaminase (ADA) or the blockade of its action by the A2a receptor antagonists 8-(3-chlorostyryl) caffeine (CSC) or CGS15943 markedly increased fMLP-induced PLD activation. The concentration-dependent stimulatory effects of CSC and CGS15943 were abolished by a pretreatment of neutrophil suspensionswith ADA. In contrast, the selective A2a recepto
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18

Gu, Jian-Wei, Ann L. Brady, Vivek Anand, Michael C. Moore, Whitney C. Kelly, and Thomas H. Adair. "Adenosine upregulates VEGF expression in cultured myocardial vascular smooth muscle cells." American Journal of Physiology-Heart and Circulatory Physiology 277, no. 2 (1999): H595—H602. http://dx.doi.org/10.1152/ajpheart.1999.277.2.h595.

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We tested whether adenosine has differential effects on vascular endothelial growth factor (VEGF) expression under normoxic and hypoxic conditions, and whether A1 or A2 receptors (A1R; A2R) mediate these effects. Myocardial vascular smooth muscle cells (MVSMCs) from dog coronary artery were exposed to hypoxia (1% O2) or normoxia (20% O2) in the absence and presence of adenosine agonists or antagonists for 18 h. VEGF protein levels were measured in media with ELISA. VEGF mRNA expression was determined with Northern blot analysis. Under normoxic conditions, the adenosine A1R agonists, N 6-cyclop
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19

Hubálek, Frantisek, Claudia Binda, Ashraf Khalil, et al. "Demonstration of Isoleucine 199 as a Structural Determinant for the Selective Inhibition of Human Monoamine Oxidase B by Specific Reversible Inhibitors." Journal of Biological Chemistry 280, no. 16 (2005): 15761–66. http://dx.doi.org/10.1074/jbc.m500949200.

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Several reversible inhibitors selective for human monoamine oxidase B (MAO B) that do not inhibit MAO A have been described in the literature. The following compounds: 8-(3-chlorostyryl)caffeine, 1,4-diphenyl-2-butene, andtrans,trans-farnesol are shown to inhibit competitively human, horse, rat, and mouse MAO B withKivalues in the low micromolar range but are without effect on either bovine or sheep MAO B or human MAO A. In contrast, the reversible competitive inhibitor isatin binds to all known MAO B and MAO A with similar affinities. Sequence alignments and the crystal structures of human MA
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20

Orefice, V., F. Ceccarelli, C. Barbati, et al. "THU0227 CAFFEINE INTAKE MODULATES DISEASE ACTIVITY AND CYTOKINES LEVELS IN SYSTEMIC LUPUS ERYTHEMATOSUS PATIENTS." Annals of the Rheumatic Diseases 79, Suppl 1 (2020): 340.2–341. http://dx.doi.org/10.1136/annrheumdis-2020-eular.2100.

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Background:Systemic lupus erythematosus (SLE) is an autoimmune disease mainly affecting women of childbearing age. The interplay between genetic and environmental factors may contribute to disease pathogenesis1. At today, no robust data are available about the possible contribute of diet in SLE. Caffeine, one of the most widely consumed products in the world, seems to interact with multiple components of the immune system by acting as a non-specific phosphodiesterase inhibitor2.In vitrodose-dependent treatment with caffeine seems to down-regulate mRNA levels of key inflammation-related genes a
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21

Burdan, F., Z. Siezieniewska, and Z. Urbanowicz. "Combined effects of acetaminophen, isopropylantipyrine and caffeine on pregnant and nonpregnant liver." Human & Experimental Toxicology 20, no. 11 (2001): 569–75. http://dx.doi.org/10.1191/096032701718620873.

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The common effects of acetaminophen (APA), isopropylantipyrine (IPA) and caffeine on liver were examined in rats. The preparations were given in Tween-80 solution once daily, in a constant proportion of 5:3:1, during days 8 to14 of gestation (S1, S2, S3 groups) or between days 8 and 14 of the experiment in nonpregnant female Wistar rats (S1-NP, S2-NP, S3-NP groups). The administration was in three different doses: doses S1, S1-NP — 3.5 mg/kg APA, 2.14 mg/ kg IPA, 0.7 mg/kg caffeine; doses S2, S2-NP were 10 times higher; and doses S3, S3-NP 100 times higher than doses S1, S1-NP. There were two
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22

Shirane, Daniel Cesar, Fernanda Pereira Maiolini, and Dalmo Antônio Ribeiro Moreira. "Variabilidade da Frequência Cardíaca em Universitários Saudáveis Após Ingesta de Bebida Energética / Heart Rate Variability in Healthy College Students After Energy Drink Intake." REVISTA CIÊNCIAS EM SAÚDE 6, no. 4 (2016): 28–41. http://dx.doi.org/10.21876/rcsfmit.v6i4.609.

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Objetivo: O objetivo é analisar a variabilidade da frequência cardíaca em universitários saudáveis, após ingestão de bebida energética. Materiais e Métodos: Estudo prospectivo, uni-cego que incluiu indivíduos de coração normal. Todos submeteram-se à monitorização eletrocardiográfica por 5 minutos, antes da ingestão de 250 ml do energético Red Bull® (grupo A – GA) ou de placebo (grupo B – GB), numa relação 3:1, num período de 10 minutos. Após 45 minutos, um outro ECG foi realizado. Os indivíduos dos GA e GB permaneceram em repouso, sentados. Foi obtida a VFC antes e após a administração das sub
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23

Slawinski, Miroslaw Aleksander, Ewelina Wawryk-Gawda, Michal Konrad Zarobkiewicz, Pawel Halczuk, and Barbara Jodlowska-Jedrych. "Apoptosis of rats’ cardiomyocytes after chronic energy drinks consumption." Current Issues in Pharmacy and Medical Sciences 31, no. 1 (2018): 25–28. http://dx.doi.org/10.1515/cipms-2018-0006.

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AbstractEnergy drinks (ED) are beverages containing caffeine, taurine, vitamins, herbal extracts, and sugar or sweeteners. They are marketed as capable of improving stamina, athletic performance and concentration, moreover, as serving as a source of energy. Still, there are very few papers describing the impact of ED on cell biology – including cell apoptosis within tissues. Therefore, in our study, we assessed the symptoms of rat cardiomyocytes apoptosis after 8 weeks consumption of ED.For the research, we used male Wistar rats divided into 2 groups (experimental and control). The experimenta
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24

Upadhyay, Viral, and Salman Khan. "075 A case of spontaneous CSF rhinorrhea in a patient with marfan syndrome." Journal of Neurology, Neurosurgery & Psychiatry 90, e7 (2019): A23.3—A24. http://dx.doi.org/10.1136/jnnp-2019-anzan.63.

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IntroductionSpontaneous cerebrospinal fluid leak is uncommon condition and frequently associated with hereditary disorders of connective tissues. Nasal CSF leakage is extremely rare.1Methods and resultsWe present the case of a 40-year-old woman presented to hospital for few days history of postural headache associated with clear intermittent discharge from right nostril without any signs of meningism. There was no history of trauma. She has a background history of Marfan syndrome with associated complications of ASD repair at age 2, mechanical Aortic and Mitral valve replacement, aortic root r
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25

Dutta, J., S. Gupta, D. Thakur, and P. J. Handique. "First Report of Nigrospora Leaf Blight on Tea Caused by Nigrospora sphaerica in India." Plant Disease 99, no. 3 (2015): 417. http://dx.doi.org/10.1094/pdis-05-14-0545-pdn.

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Tea [Camellia sinensis (L.) O. Kuntze] is an economically important non-alcoholic caffeine-containing beverage crop widely cultivated for leaves in India, especially in the Darjeeling district of West Bengal. In May 2012, distinct blight symptoms were observed on leaves of popular tea cultivars AV-2, Tukdah 78, Rungli Rungliot 17/144, and Bannockburn 157 in commercial tea estates of the Darjeeling district. This disease reduces yield and quality of the leaves. The initial symptoms were frequently observed on the young leaf margins and apices. Foliar symptoms are characterized by grayish to bro
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26

Sirous, Zohreh N., Kathy L. Cockrell, Barbara T. Alexander, Joey P. Grnager та Raouf A. Khalil. "Tnfα-Induced Hypertension in Pregnant Rats Is Associated with Increased [Ca 2+ ] I Signaling in Renal Arterial Smooth Muscle". Hypertension 36, suppl_1 (2000): 688. http://dx.doi.org/10.1161/hyp.36.suppl_1.688-e.

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61 Placental ischemia during late pregnancy triggers the release of tumor necrosis factor α (TNFα), which may contribute to the increased vascular resistance associated with pregnancy-induced hypertension (PIH). We have reported that elevation of plasma TNFα 2-fold increases blood pressure and renal vascular resistance in pregnant rats; however, the cellular mechanisms involved are unclear. In this study, we investigated whether TNFα infusion in pregnant rats (10 ng/kg/day for 7 days) is associated with increases in [Ca 2+ ] i and contractility of renal arterial smooth muscle. Pregnant (MAP =
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27

Frederick, Raphael, Frederic Ooms, Neal Jr Castagnoli, et al. "(E)-8-(3-Chlorostyryl)-1,3-7-trimethylxanthine, a Caffeine Derivative Acting Both as Antagonist of Adenosine A2A Receptors and as Inhibitor of MAO-B." ChemInform 37, no. 3 (2006). http://dx.doi.org/10.1002/chin.200603164.

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28

Trong Bien, Tra, and Bui Thi Lan Phuong. "Development and Validation of a HPLC Method of Quantification of Caffeine and EGCG in Green Tea (Camellia sinensis L.) Extract." VNU Journal of Science: Medical and Pharmaceutical Sciences 36, no. 3 (2020). http://dx.doi.org/10.25073/2588-1132/vnumps.4212.

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This study investigates a simple high performance liquid chromatography (HPLC) in an isocratic eluent manner for quantification of caffeine and EGCG in green tea extract. The study separation system contained a C18-RP column (250 × 4.6 mm, 5 µm), a mobile phase of methanol/phosphoric acid/water (20/0.1/79.9, v/v) and a DAD detector at 280 nm. This system proves convenient for rapid routine analysis of caffeine and EGCG in green tea extract with good repeatability and accuracy.
 Keywords
 HPLC, caffeine, EGCG, green tea, extract.
 References
 [1] A. Chowdhury, J. Sarkar, T.
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29

Ibraheam, Israa Adnan, Imad Hadi Hameed S., and Haider Mashkoor Hussein. "Cyclamen persicum: Methanolic Extract Using Gas Chromatography-Mass Spectrometry (GC-MS) Technique." International Journal of Pharmaceutical Quality Assurance 8, no. 04 (2017). http://dx.doi.org/10.25258/ijpqa.v8i04.10546.

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Cyclamen was traditionally classified in the family Primulaceae, was reclassified in the subfamily Myrsinoideae within the family Primulaceae. The objective of this study was analysis of the secondary metabolite products. Bioactives are chemical compounds often referred to as secondary metabolites. Thirty eight bioactive compounds were identified in the methanolic extract of Cyclamen persicum. The identification of bioactive chemical compounds is based on the peak area, retention time molecular weight and molecular formula. GC-MS analysis of Cyclamen persicum revealed the existence of the3-Oxo
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