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Fundamental & Clinical Pharmacology

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https://www.readbyqxmd.com/read/28477356/epigallocatechin-3-gallate-ameliorates-intrahepatic-cholestasis-of-pregnancy-by-inhibiting-matrix-metalloproteinases-2-and-9
#1
Mei Zhang, Meimei Xu
Matrix metalloproteinase (MMP)-2 and -9 are involved in many illnesses affecting pregnant women, including intrahepatic cholestasis of pregnancy (ICP), a serious liver abnormality during pregnancy. Epigallocatechin 3-gallate (EGCG) has been widely reported to inhibit activities of MMP-2 and MMP-9. We aimed to investigate the role of EGCG in ameliorating ICP symptoms in a rat model. Using 17α-ethinylestradiol to induce ICP in pregnant rats, we investigated the efficacy of EGCG administration on ICP symptoms, including bile flow rate, total bile acids (TBA) and MMP-2 and MMP-9 activities...
May 5, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28429826/effect-of-alpha-lipoic-acid-on-endometrial-implants-in-an-experimental-rat-model
#2
Neslihan Pınar, Oya Soylu Karapınar, Oğuzhan Özcan, Tümay Özgür, Suphi Bayraktar
To investigate the antioxidant and anti-inflammatory effects of alpha-lipoic acid (ALA) in the treatment of endometriosis in an experimental rat model by evaluating biochemical and histopathologic parameters. Experimental endometriosis was induced by the peritoneal implantation of autologous endometrial tissue. The rats were randomly divided into two groups with 8 rats each. Group I was intraperitoneally administered ALA 100 mg/kg/day for 14 days. Group II was intraperitoneally administered saline solution at the same dosage and over the same period...
April 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28407450/finding-the-optimal-dose-of-vitamin-k1-to-treat-vitamin-k-deficiency-and-to-avoid-anaphylactoid-reactions
#3
Yan-Ni Mi, Na-Na Ping, Bo Li, Xue Xiao, Yan-Bing Zhu, Lei Cao, Jian-Kang Ren, Yong-Xiao Cao
Vitamin K1 injection induces severe dose-related anaphylactoid reactions and overdose for the treatment of vitamin K deficiency. We aimed to find an optimal and small dose of vitamin K1 injection to treat vitamin K deficiency and avoid anaphylactoid reactions in animal. Rats were administered a vitamin K-deficient diet and gentamicin to establish vitamin K deficiency model. Behaviour tests were performed in beagle dogs to observe anaphylactoid reactions. The results showed an increased protein induced by vitamin K absence or antagonist II (PIVKA-II) levels, a prolonging of prothrombin time (PT) and activated partial thromboplastin time (APTT), and a decrease in vitamin K-dependent coagulation factor (F) II, VII, IX and X activities in the model group...
April 13, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28407406/phenobarbital-in-intensive-care-unit-pediatric-population-predictive-performances-of-population-pharmacokinetic-model
#4
Amélie Marsot, Fabrice Michel, Estelle Chasseloup, Olivier Paut, Romain Guilhaumou, Olivier Blin
An external evaluation of phenobarbital population pharmacokinetic model described by Marsot et al. was performed in pediatric intensive care unit. Model evaluation is an important issue for dose adjustment. This external evaluation should allow confirming the proposed dosage adaptation and extending these recommendations to the entire intensive care pediatric population. External evaluation of phenobarbital published population pharmacokinetic model of Marsot et al. was realized in a new retrospective dataset of 35 patients hospitalized in a pediatric intensive care unit...
April 13, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28407303/rifampicin-reverses-nicardipine-effect-inducing-uncontrolled-essential-hypertension
#5
Elena-Mihaela Cordeanu, Sébastien Gaertner, Alix Faller, Corina Mirea, Jean-Marc Lessinger, Veronique Kemmel, Dominique Stephan
Dihydropyridine calcium-channel blockers are a known substrate for the cytochrome P450 isoform 3A4. Rifampicin, an antitubercular agent, is one of the most potent inducers of hepatic and intestinal CYP3A4 thus increasing dihydropyridine metabolism. We report a case of a 67-year-old hypertensive female treated with a 4-drug antihypertensive regimen including a dihydropyridine (nicardipine 50mg bid), who was admitted for septic arthritis of the knee requiring antibiotic treatment with teicoplanin 400mg od and rifampicin 600mg bid...
April 13, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28370265/zizyphin-modulates-calcium-signalling-in-human-taste-bud-cells-and-fat-taste-perception-in-the-mouse
#6
Babar Murtaza, Meryem Berrichi, Chahid Bennamar, Thierry Tordjmann, Fatima Zohara Djeziri, Aziz Hichami, Julia Leemput, Meriem Belarbi, Hakan Ozdener, Naim A Khan
Zizyphin, isolated from Zizyphus sps. leaf extracts, has been shown to modulate sugar taste perception, and the palatability of a sweet solution is increased by the addition of fatty acids. We, therefore, studied whether zizyphin also modulates fat taste perception. Zizyphin was purified from edible fruit of Zizyphus lotus L. Zizyphin induced increases in [Ca(2+) ]i in human taste bud cells (hTBC). Zizyphin shared the endoplasmic reticulum Ca(2+) pool and also recruited, in part, Ca(2+) from extracellular environment via the opening of store-operated Ca(2+) (SOC) channels...
April 2, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28370178/curcuma-decreases-serum-hepcidin-levels-in-healthy-volunteers-a-placebo-controlled-randomized-double-blind-cross-over-study
#7
Fabrice Lainé, Bruno Laviolle, Edouard Bardou-Jacquet, Nadia Fatih, Caroline Jezequel, Nicolas Collet, Martine Ropert, Jeff Morcet, Catherine Hamon, Jean-Michel Reymann, Olivier Loréal
Hepcidin, secreted by hepatocytes, controls iron metabolism by limiting iron egress in plasma. Hepcidin is upregulated during inflammation through the activation of the signal transducer and activator of transcription 3 (STAT3) transduction pathway, which decreases iron bioavailability and may explain the anemia of chronic inflammatory disease. In vitro, it has been shown that curcumin can decrease hepcidin synthesis by decreasing STAT3 activity. We conducted a proof-of-concept study to assess the effect of curcuma on hepcidin synthesis in human...
March 30, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28322465/opioid-substitution-therapy-or-hidden-opioids-are-a-minefield-for-nalmefene-an-atypical-case-series-of-11-patients-in-lorraine
#8
Melissa Yéléhé-Okouma, Hervé Martini, Jérémie Lemarié, Pierre Labroca, Nadine Petitpain, Valérie Gibaja, François Paille, Pierre Gillet
Opioid antagonists such as naltrexone and nalmefene are used in drug therapy for alcoholism. Nalmefene, approved in Europe in February 2013 for the reduction of alcohol consumption is used in patients with alcohol dependence. We report 11 cases of opioid withdrawal syndrome after a single dose of nalmefene in patients usually treated with methadone, buprenorphine, but also with fentanyl or loperamide. Nalmefene is both a partial agonist and an antagonist of opioid receptors. Regarding to its opioid antagonist activity, nalmefene is contraindicated in patients with an opioid treatment...
March 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28322460/dapsone-induced-agranulocytosis-possible-involvement-of-low-activity-n-acetyltransferase-2
#9
Ines Potočnjak, Robert Likić, Iveta Šimić, Danica Juričić Nahal, Ivana Čegec, Lana Ganoci, Nada Božina
Dapsone-induced agranulocytosis is a rare but potentially fatal adverse drug reaction (ADR). A 45-year old male Caucasian patient developed agranulocytosis caused by dapsone (diamino-diphenyl sulfone) which he was prescribed for leukocytoclastic vasculitis. Patient's treatment consisted of termination of dapsone, antibiotic therapy, and granulocyte colony stimulating factor leading to prompt improvement of symptoms and normalization of laboratory blood values. Diagnostic evaluation revealed methemoglobinemia and excluded glucose-6-phosphate dehydrogenase (G6PD) deficiency...
March 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28299825/fingolimod-gilenya-%C3%A2-in-multiple-sclerosis-bradycardia-atrioventricular-blocks-and-mild-effect-on-the-qtc-interval-something-to-do-with-the-l-type-calcium-channel
#10
Sylvie Pilote, Chantale Simard, Benoit Drolet
Cardiac arrhythmias and ECG abnormalities including bradycardia, prolongation of the QT interval, and atrioventricular (AV) conduction blocks have been extensively observed with fingolimod, the first marketed oral drug for treating the relapsing-remitting form of multiple sclerosis. This study was aiming to further elucidate the effects of fingolimod on cardiac electrophysiology at three different levels: (i) in vitro, (ii) ex vivo, and (iii) in vivo. (i) Patch-clamp experiments in whole cell configuration were performed on Cav 1...
March 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28299811/the-role-of-interleukin-1b-and-its-antagonist-diacerein-in-estradiol-benzoate-induced-endometrial-hyperplasia-and-atypia-in-female-rats
#11
Marwa M M Refaie, Maram El-Hussieny
Endometrial hyperplasia (EH) is a common gynecological condition and may progress to carcinoma. We investigated the effect of diacerein (DIA) on estradiol benzoate (EB)-induced EH and atypia. DIA (50mg/kg/day) was administered orally to rats for 4 weeks, in the presence or absence of EH induced by intramuscular (im) injection of EB (60μg/100g) 3 times per week for 4 weeks. We measured levels of serum total cholesterol, uterine tissue malondialdehyde (MDA), total nitrites (NOx ), superoxide dismutase (SOD) activity, caspase-3, interleukin-1b (IL-1b) immunoexpressions and histopathology...
March 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28295557/parachlorophenylalanine-induced-5-ht-depletion-alters-behavioral-and-brain-neurotransmitters-levels-in-6-hz-psychomotor-seizure-model-in-mice
#12
Kausar Jahan, Krishna K Pillai, Divya Vohora
The present study was designed to investigate the role of serotonin and other neurotransmitters namely dopamine (DA), histamine, nor-epinephrine (NE), glutamate, and γ-aminobutyric acid (GABA) in the 6-Hz-induced psychomotor seizures in Swiss albino mice. Parachlorophenylalanine (PCPA, 300 mg/kg/day, i.p for 3 days)-treated mice were given 6-Hz stimulation. Sodium valproate (SVP) (200 mg/kg/day, p.o for 3 days) was used as a reference antiepileptic drug. The behavioral changes induced by 6 Hz including increased rearing and grooming, Straub's tail, behavioral arrest, stun position were amplified by PCPA...
March 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28267871/effect-of-bucladesine-pentoxifylline-and-h-89-as-cyclic-adenosine-monophosphate-analog-phosphodiesterase-and-protein-kinase-a-inhibitor-on-acute-pain
#13
Forouz Salehi, Mahshid Sadat Hosseini-Zare, Haleh Aghajani, Yalda Seyedi, Maryam Sadat Hosseini-Zare, Mohammad Sharifzadeh
The aim of the present study was to determine the effects of Cyclic adenosine monophosphate (cAMP) and its dependent pathway on thermal nociception in a mouse model of acute pain. Here we studied the effect of H-89 (protein kinase A inhibitor), Bucladesine (Db-cAMP) (membrane permeable analog of cAMP) and pentoxifylline (PTX) (non-specific phosphodiesterase (PDE) inhibitor) on pain sensation. Different doses of H-89 (0.05, 0.1 and 0.5 mg/100g), PTX (5, 10 and 20 mg/100g), and Db-cAMP (50, 100 and 300 nM/mouse) were administered intraperitoneally (I...
March 7, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28258589/effect-of-dementia-on-receipt-of-influenza-vaccine-a-cohort-study-in-french-older-adults-using-administrative-data-2007-2012
#14
Adeline Gallini, Nicola Coley, Sandrine Andrieu, Maryse Lapeyre-Mestre, Virginie Gardette
Despite guidelines stating the vaccine benefit in this population, older adults with dementia may be less likely to receive influenza vaccine than cognitively intact older adults. But no study has yet reported on vaccine uptake in patients newly diagnosed with dementia or whether years since dementia diagnosis influence vaccine uptake. We conducted a cohort study in the French Health Insurance database (EGB) which contains hospital data and claims for a 1/97(th) random sample of the French population. Diseased subjects were ≥65 years and had a new record of dementia diagnosis between September 1 2007 and August 31 2008...
March 4, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28012206/uptake-and-efflux-kinetics-and-intracellular-activity-of-voriconazole-against-aspergillus-fumigatus-in-human-pulmonary-epithelial-cells-a-new-application-for-the-prophylaxis-and-early-treatment-of-invasive-pulmonary-aspergillosis
#15
Taotao Wang, Qianting Yang, Lu Chen, Ying Li, Ti Meng, Yan Wang, Tao Zhang, Jin'e Lei, Jianfeng Xing, Yalin Dong
Invasive pulmonary aspergillosis (IPA), most caused by Aspergillus fumigatus, is a serious life-threatening infection in immunocompromised patients. Voriconazole is used to prevent and treat IPA. However, little is known about the pharmacological characteristics of voriconazole in pulmonary epithelial cells, which are the target site for the prophylaxis and early treatment of IPA. The aim of the study was to evaluate the kinetics and activity of voriconazole against A. fumigatus in A549 cells. High-performance liquid chromatography/tandem mass spectrometry and time-kill method were used to study the cellular pharmacokinetic and pharmacodynamics of voriconazole...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27891661/synergistic-effects-of-polydatin-and-vitamin-c-in-inhibiting-cardiotoxicity-induced-by-doxorubicin-in-rats
#16
Hui-Lin Wang, Xiao-Hua Cui, Hai-Lun Yu, Rong Wu, Xu Xu, Jian-Ping Gao
The purpose of this study was to assess the synergistic effect of polydatin and vitamin C on attenuating cardiotoxicity induced by doxorubicin (DOX) in rats. Polydatin could significantly increase the activity of superoxide dismutase (SOD) and the heart rate, attenuate myocardial pathological damage, decrease malondialdehyde (MDA) content, slightly increase arterial pressure and glutathione peroxidase (GSH-Px) activity, reduce intervals of QRS, QT, and ST, and lower free fatty acid (FFA) content. The combination of polydatin and vitamin C could significantly increase arterial pressure and heart rate, decrease QRS interval and slightly reduce ST and QT intervals, significantly attenuate myocardial pathological damage, increase the activities of GSH-Px,T-SOD, Na(+) K(+) -ATPase, and Ca(2+) Mg(2+) -ATPase, elevate phosphocreatine (PCr) and adenosine triphosphate (ATP) contents, slightly increase adenosine diphosphate (ADP) and total adenine nucleotide (TAN) contents and PCr/ATP, and significantly decrease the contents of MDA and FFA, when compared with those in the DOX group...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27885727/growth-inhibitory-and-proapoptotic-effects-of-l-asparaginase-from-fusarium-culmorum-asp-87-on-human-leukemia-cells-jurkat
#17
Anil K Meghavarnam, Maryam Salah, Meenakshisundaram Sreepriya, Savitha Janakiraman
The objective of this study was to evaluate the anticancer properties of l-asparaginase purified from fungal isolate Fusarium culmorum ASP-87 against human T-cell leukemia cell line (Jurkat). The growth inhibitory and proapoptotic effects of purified l-asparaginase on Jurkat cell lines were investigated by determining its influence on cell viability, colony formation, DNA fragmentation, and cell cycle progression. The results revealed that purified l-asparaginase showed significant decrease in cell survival with IC50 value of 90 μg/mL (9 IU/mL)...
June 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28370515/abstracts-of-the-annual-meeting-of-french-society-of-pharmacology-and-therapeutics-and-inserm-clinical-research-centers-cic-meeting-19-21-april-2017-rouen-france
#18
(no author information available yet)
No abstract text is available yet for this article.
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28214375/antifatigue-effects-of-troxerutin-on-exercise-endurance-capacity-oxidative-stress-and-matrix-metalloproteinase-9-levels-in-trained-male-rats
#19
Mohammad Zamanian, Mohammad R Hajizadeh, Ali Esmaeili Nadimi, Ali Shamsizadeh, Mohammad Allahtavakoli
The aim of this study was to investigate effects of troxerutin (TRX) on endurance capacity, oxidative stress and matrix metalloproteinase-9 (MMP-9) levels in trained male rats. Forty male Wistar rats were divided into five groups. The control (Vehicle) and exercise training (5 days/week) with vehicle treatment (Exercise), exercise training with TRX treatment at 75 (Ex-TRX75), 150 (Ex-TRX150), and 300 mg/kg (Ex-TRX300). The treated groups received TRX by gavage every day while the other groups received water for 30 days...
February 18, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28199737/inhibition-of-trpv1-confers-neuroprotection-reduces-tnf-%C3%AE-and-increases-il-10-in-a-rat-stroke-model
#20
Elham Hakimizadeh, Ali Shamsizadeh, Ali Roohbakhsh, Mohammad Kazemi Arababadi, Mohammad Reza Hajizadeh, Mehdi Shariati, Mohammad Reza Rahmani, Mohammad Allahtavakoli
Stroke is a major cause of mortality and long-term disability in adults. TRPV1 plays a crucial role in neuroinflammation. In the current study, the effects of TRPV1 agonist (capsaicin) and antagonist (AMG9810) on cerebral ischemia were investigated. Forty male Wistar rats were assigned to the following experimental groups: sham, vehicle) ischemic), AMG9810 (selective TRPV1 antagonist, 0.5 mg/kg; 3 h after stroke), and capsaicin (1 mg/kg; 3 h after stroke). Stroke was induced by permanent middle cerebral artery occlusion and neurological deficits were evaluated 1, 3, and 7 days after stroke...
February 15, 2017: Fundamental & Clinical Pharmacology
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