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Fundamental & Clinical Pharmacology

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https://www.readbyqxmd.com/read/28636803/atorvastatin-attenuates-testosterone-induced-benign-prostatic-hyperplasia-in-rats-role-of-peroxisome-proliferator-activated-receptor-%C3%AE-and-cyclo-oxygenase-2
#1
Ismail O Ishola, Habeeb K Tijani, Olufunke O Dosumu, Charles C Anunobi, Tolulope O Oshodi
Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, an attempt was made to investigate the protective effect of atorvastatin (ATR) in combination with celecoxib (CEL) or pioglitazone (PIO) on testosterone-induced BPH in rats. Male Wistar rats (200-250 g) were randomly divided into 9 groups (n=8) and orally treated as follows for 28 consecutive days; Group 1: vehicle (10 ml/kg), group 2: vehicle (10 ml/kg), groups 3 - 5: ATR (0.5, 2.5 and 5 mg/kg, respectively); group 6: CEL (20 mg/kg); Group 7: PIO (20 mg/kg); Groups 8-9: ATR 0...
June 21, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28622415/is-bisphenol-a-an-environmental-obesogen
#2
REVIEW
Samuel Legeay, Sébastien Faure
Bisphenol a (BPA) is an endocrine disruptor with an estrogenic activity that is widely produced for the manufacture of polycarbonate plastic, epoxy resin and thermal paper. Its ubiquitous presence in the environment contributes to broad and continuous human exposure which has been associated with deleterious health effects. Despite numerous controversial discussions and a lack of consensus about BPA's safety, growing evidence indicates that BPA exposure positively correlates with an increased risk of developing obesity...
June 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28575541/trends-in-the-incidence-of-use-of-non-insulin-glucose-lowering-drugs-between-2006-and-2013-in-france
#3
Mickael Arnaud, Julien Bezin, Bernard Bégaud, Antoine Pariente, Francesco Salvo
This study aimed at describing trends in the incidence of use of non-insulin glucose-lowering drugs (NIGLDs) between 2006 and 2013 in France. Repeated cross-sectional studies on NIGLD new users were performed annually from 2006 to 2013 within the Echantillon Généraliste des Bénéficiaires (EGB) database, a 1/97(th) representative sample of the population covered by the French healthcare insurance system. NIGLD included metformin, sulfonylureas, α-glucosidase inhibitors, thiazolidinediones, dipeptidylpeptidase-4 (DPP-4) inhibitors, glinides and glucagon-like peptide-1 analogues...
June 2, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28544244/branched-chain-amino-acids-supplementation-modulates-tgf-%C3%AE-1-smad-signaling-pathway-and-interleukins-in-ccl4-induced-liver-fibrosis
#4
Naglaa F Khedr, Eman G Khedr
The alterations and low levels of circulating branched chain amino acids (BCAAs), leucine, isoleucine and valine, are associated with liver diseases. The study was designed to evaluate hepatoprotective effect of BCAAs on CCl4 -induced liver fibrosis and to investigate the molecular mechanisms underlying these effects in rats. Thirty male rats were divided into three groups. Control group (n=10), CCl4 group (n=10); rats were injected with CCl4 (1 mL/kg of 0.5:1 v/v injected i.p. twice weekly for 12 weeks). CCl4 +BCAAs group (n=10); rats were injected with similar doses of CCl4 and supplemented with a mixture of 600 mg/kg BCAAs (2: 1: 1...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28543930/further-analysis-of-acute-antinociceptive-and-anti-inflammatory-actions-of-4-phenylselenyl-7-chloroquinoline-in-mice
#5
Vanessa D G Silva, Angélica S Reis, Mikaela Pinz, Caren A R da Fonseca, Luis Fernando B Duarte, Juliano A Roehrs, Diego Alves, Cristiane Luchese, Ethel A Wilhelm
A new quinoline containing selenium, 4-phenylselenyl-7-chloroquinoline (4-PSQ), was described and synthetized by our research group. Recently, we demonstrated the potential antinociceptive and anti-inflammatory of 4-PSQ. For this reason, the first objective of this study was to expand our previous findings by investigating the contribution of glutamatergic, serotonergic and nitrergic systems to the acute antinociceptive action of this compound. Pretreatment with 4-PSQ (0.01-25 mg/kg, p.o.) reduced the nociception induced by glutamate...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28543864/modulation-of-heme-oxygenase-1-expression-and-activity-affects-streptozotocin-induced-diabetic-nephropathy-in-rats
#6
Marwa A M Ali, Gehan H Heeba, Azza A K El-Sheikh
Heme oxygenase (HO)-1 has exhibited nephro-protective actions in different animal models; however, its full mechanistic potential in diabetic nephropathy (DN) has not yet been elucidated. Hence, the present study has been undertaken by inducing DN in rats using streptozotocin (50mg/kg i.p.), with or without either HO-1 inducer; hemin (HM; 40 μmol/kg, s.c.), or HO-1 blocker; zinc protoporphyrin-IX (ZnPP; 50 μmol/kg, i.p.), for one month. Compared to control, rats with DN suffered from hyperglycemia and hyperlipidemia, with signs of renal damage, as assessed by distortion in renal histopathological architecture and kidney function...
May 23, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28477356/epigallocatechin-3-gallate-ameliorates-intrahepatic-cholestasis-of-pregnancy-by-inhibiting-matrix-metalloproteinase-2-and-matrix-metalloproteinase-9
#7
Mei Zhang, Meimei Xu
Matrix metalloproteinase (MMP)-2 and matrix metalloproteinase-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
#8
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
#9
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
#10
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
#11
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
#12
Babar Murtaza, Meryem Berrichi, Chahid Bennamar, Thierry Tordjmann, Fatima Z 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+) channels...
April 2, 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
#13
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
#14
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
#15
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
#16
(no author information available yet)
No abstract text is available yet for this article.
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27885718/purinergic-receptors-new-targets-for-the-treatment-of-gout-and-fibrosis
#17
REVIEW
Thomas Gicquel, Brendan Le Daré, Elisabeth Boichot, Vincent Lagente
Adenosine triphosphate is involved in many metabolic reactions, but it has also a role as a cellular danger signal transmitted through purinergic receptors (PRs). Indeed, adenosine 5'-triphosphate (ATP) can bind to PRs which are found in the membrane of many cell types, although the relative proportions of the receptor subtypes differ. PRs are classified according to genetic and pharmacological criteria and especially their affinities for agonists and their transduction mechanism (i.e. as metabotropic P2YRs or ionotropic P2XRs)...
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27873354/gastroprotective-effect-of-esculin-on-ethanol-induced-gastric-lesion-in-mice
#18
Weifeng Li, Yu Wang, Xiumei Wang, Hailin Zhang, Zehong He, Wenbing Zhi, Fang Liu, Xiaofeng Niu
The gastroprotective effect of esculin was investigated in a mouse model of ethanol-induced gastric lesion. Administration of esculin at doses of 5, 10, and 20 mg/kg body weight prior to ethanol ingestion led to significant gastroprotection compared with untreated mice. Gastric mucosal lesions were evaluated by macroscopic and histopathological alterations, lesion index, and myeloperoxidase (MPO) activity. Pretreatment with esculin significantly reduced macroscopic and histopathological damage, gastric lesion index, and MPO activity in a dose-dependent manner...
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27862262/different-effects-of-selective-%C3%AE-1-adrenoceptor-antagonists-nebivolol-or-atenolol-in-acetaminophen-induced-hepatotoxicity-of-rats
#19
COMPARATIVE STUDY
Remon R Rofaeil, Maha Y Kamel, Walaa Y Abdelzaher
Acetaminophen (APAP) overdose is a common cause of acute liver failure, and beta-blockers are commonly used drugs in clinical practice. This study aimed to evaluate the effect of two different beta-blocker agents as nebivolol and atenolol against APAP-induced hepatotoxicity. Male Wistar rats were treated with APAP (2 g/kg/day, p.o.) to induce hepatotoxicity. Our results showed that nebivolol and atenolol reduced heart rate and blood pressure. Nebivolol (5 mg/kg/day, p.o.) for 14 days has a hepatoprotective effect shown by significant decrease in hepatic injury parameters (serum AST and ALT) with significant suppression of hepatic malondialdehyde (MDA) and nitric oxide (NO) which were elevated with APAP administration...
April 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27862243/antidepressant-adherence-patterns-in-older-patients-use-of-a-clustering-method-on-a-prescription-database
#20
David Braunstein, Amélie Hardy, Quentin Boucherie, Elisabeth Frauger, Olivier Blin, Gaétan Gentile, Joëlle Micallef
According to the World Health Organization, depression will become the second most important cause of disability worldwide by 2020. Our objective was to identify patterns of adherence to antidepressant treatments in older patients using several indicators of adherence and to characterize these patterns in terms of medication exposure. We conducted a retrospective cohort study using the French National Health Insurance reimbursement database. Incident antidepressant users aged more than 65 were included from July 1, 2010, to June 30, 2011, and followed up for 18 months...
April 2017: Fundamental & Clinical Pharmacology
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