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Fundamental & Clinical Pharmacology

Stefânia E Santos, Fernanda P R A Ribeiro, Pedro M N Menezes, Luiz A M Duarte-Filho, Jullyana S S Quintans, Lucindo J Quintans-Junior, Fabricio S Silva, Luciano A A Ribeiro
The monoterpene alcohol (-)-borneol has many biological effects such as sedative, anti-inflammatory, analgesic, anti-nociceptive, antithrombotic and vasorelaxant effects. Our objective in this study was to investigate the mechanism of action of (-)-borneol and determine its vasorelaxant effect. (-)-Borneol was tested on isolated aortic rings contracted with PE (10-6 M). This study was performed in the absence or in the presence of endothelium, L-NAME (100 μM), indomethacin (10 μM), TEA (1 and 10 mM), 4-AP (1 mM), or glibenclamide (1 mM) to assess the participation of EDRF, nitric oxide, prostanoids and potassium channels on the relaxing effect of (-)-borneol...
September 21, 2018: Fundamental & Clinical Pharmacology
Cícero Francisco Bezerra Felipe, Alyne Mirely Sousa Albuquerque, João Luis Xavier de Pontes, José Ítalo Vieira de Melo, Teresa Carolliny Moreira Lustoza Rodrigues, Ada Mirtes Pereira de Sousa, Álefe Brito Monteiro, Ana Elisa da Silva Ribeiro, Janice Pereira Lopes, Irwin Rose Alencar de Menezes, Reinaldo Nóbrega de Almeida
Convulsions occur in response to a loss of balance between excitatory and inhibitory neurotransmitters, and the treatment for this condition consists in restore such lost balance. Many anticonvulsant drugs present side effects which may limit their use. This fact has stimulated the search for new sources of treatment from aromatic plants. Many monoterpenes commonly present in essential oils are known because of their anticonvulsant properties. The anticonvulsant effect of α- and β-pinene, two structural isomers, is still little studied...
September 19, 2018: Fundamental & Clinical Pharmacology
Mete Ozcan, Sinan Canpolat, Ozgur Bulmus, Nazife Ulker, Ahmet Tektemur, Suat Tekin, Sibel Ozcan, Ihsan Serhatlioglu, Emine Kacar, Ahmet Ayar, Haluk Kelestimur
The main objective of this study was to investigate potential effectiveness of agomelatine pre-treatment in prevention of diabetes itself and encephalopathy, with a focus on brain tissue oxidative stress and inflammatory processes in streptozotocin (STZ)-induced diabetic mice. Interleukine-1β (IL-1β) and TACR1 (NK1), which is a tachykinine receptor, were used for the investigation of inflammation in the brain regions including raphe nuclues, periaqueduqtal gyrus (PAG), amygdala and nucleus accumbens. The effects of agomelatine on total antioxidant capacity were also evaluated...
September 14, 2018: Fundamental & Clinical Pharmacology
Zhike Zhou, Jun Hou, Juanjuan Xiong, Min Li
Sulfuretin is a major flavonoid found in Rhus verniciflua and carries anti-oxidative and anti-inflammatory properties, but its potential use in the control of skin pigmentation is unknown. The purpose of the present study was to elucidate sulfuretin as a new active compound inhibiting melanogenesis and the underlying mechanism. The effects of sulfuretin on melanin production, tyrosinase activity, cAMP level and MITF expression were examined in murine melanoma B16 cells challenged with forskolin or α-MSH. The inhibitory effect of sulfuretin on melanogenesis was further validated on neonatal human melanocytes...
September 14, 2018: Fundamental & Clinical Pharmacology
Nataša Ristić, Nataša Nestorović, Milica Manojlović-Stojanoski, Svetlana Trifunović, Vladimir Ajdžanović, Branko Filipović, Lazo Pendovski, Verica Milošević
Dexamethasone (Dx) is often used in obstetric practice to promote fetal lung maturation and to prevent respiratory distress syndrome when the risk of preterm delivery persists. This therapy enables survival of the newborn, but also is associated with deleterious effects on the offspring, such as reproductive disorders. The aim of this study was to determine specifically whether prenatal exposure to Dx disturbs the physiological balance between proliferation and apoptosis of germinative cells (GC) in the ovary of 19 and 21 day old fetuses and thus induces developmental programing of the female reproductive system...
September 14, 2018: Fundamental & Clinical Pharmacology
Camille Tron, Marie Allard, Antoine Petitcollin, Marie-José Ferrand-Sorre, Marie-Clémence Verdier, Julie Querzerho-Raguideau, Benoit Blanchet, Jérôme Le Priol, Mickael Roussel, Yves Deugnier, Eric Bellissant, Florian Lemaitre
Measuring tacrolimus (TAC) concentration in peripheral blood mononuclear cells (PBMC) could better reflect the drug effect on its target (calcineurin (CaN) in lymphocytes) than whole blood concentrations. Mechanisms influencing TAC diffusion into PBMC are not well characterized. This work aimed at describing, ex-vivo, TAC diffusion kinetics into PBMC and investigating the contribution of membrane transporters to regulate TAC intracellular concentration as well as the impact on CaN activity. PBMC were incubated with TAC for 5 min to 4h and under several experimental conditions: 37°C (physiological conditions) 4°C (inhibition of influx and efflux active transport), 37°C + transporter inhibitors (verapamil, carvedilol, probenecid, bromosulphophtalein respectively inhibitors of P-gp, OAT, OATP)...
September 11, 2018: Fundamental & Clinical Pharmacology
Ayat Kaeidi, Zahra Hajializadeh, Farank Jahandari, Iman Fatemi
One of the main pathological mechanisms of neurotoxicity in diabetic situation is oxidative stress promoted by hyperglycemia. It has been shown that leptin has neuroprotective effects and may provide neuronal survival signals. This study was designed to reveal the possible neuroprotective effects of leptin in hyperglycemic conditions. Pheochromocytoma (PC12) cell viability was assessed via the MTT test. Cellular reactive oxygen species (ROS) generation was determined by DCFH-DA analysis. The malondialdehyde (MDA) and glutathione (GSH) levels were measured in high glucose-treated PC12 cells with and without leptin co-treatment...
September 11, 2018: Fundamental & Clinical Pharmacology
Adriane F Brito, Lorrane K S Moreira, Ricardo Menegatti, Elson A Costa
Medicinal chemistry is a science applied to the search and discovery of new therapeutic agents for the treatment of various diseases. Therefore, promising structures have been identified; one of these structures is the piperazine moiety, a cyclic molecule containing two nitrogen atoms in positions 1 and 4 as well as four carbon atoms. Many piperazine derivatives have central pharmacological activity that mainly involves the activation of the monoamine pathway. Thus, piperazine derivatives have been the subject of research for many central therapeutic applications, including antipsychotic, antidepressant, and anxiolytic applications...
August 27, 2018: Fundamental & Clinical Pharmacology
Alecsander F Bressan, Gisele A Fonseca, Rita C Tostes, R Clinton Webb, Victor Vitorino Lima, Fernanda Regina Giachini
The activation of extracellular signal-regulated kinase 1 and 2 (ERK 1/2) pathway promotes increased vascular contractility in angiotensin II (Ang II)-induced hypertensive mice. Interleukin-10 (IL-10) is an immune-regulatory cytokine with the ability to prevent vascular hypercontractility during hypertension. We hypothesized that IL-10 would downregulate vascular ERK 1/2 activation during Ang II-induced hypertension. Wild-type (WT) or IL-10 knockout (IL-10-/- ) mice received Ang II infusion (90 ηg.min) or vehicle (saline), via osmotic mini-pumps (0...
August 24, 2018: Fundamental & Clinical Pharmacology
François Montastruc, Justine Benevent, Vanessa Rousseau, Geneviève Durrieu, Agnès Sommet, Jean-Louis Montastruc
In contrast to statins, the risk of diabetes with fibrates was not clearly studied. This study investigates a putative signal of diabetes associated with the use of fibrates using the World Health Organization (WHO) global individual case safety reports database, VigiBase® . We included all reports registered until the 31st December 2017 in VigiBase® to measure the risk of reporting 'hyperglycemia or new onset of diabetes' (SMQ term) compared with all other reports [as a reporting odds ratio (ROR 95% CI)] for fibrates, statins, and the combination fibrates + statins...
August 11, 2018: Fundamental & Clinical Pharmacology
Nils Bögeholz, Paul Pauls, Bastian K Bauer, Jan S Schulte, Gerrit Frommeyer, Dirk G Dechering, Peter Boknik, Uwe Kirchhefer, Frank U Müller, Christian Pott, Lars Eckardt
Administration of digitalis in heart failure (HF) increases quality of life but does not carry a prognostic benefit. Digitalis is an indirect inhibitor of the Na+ /Ca2+ exchanger (NCX), which is overexpressed in HF. We therefore used the cardiac glycoside ouabain in Ca2+ imaging experiments and patch-clamp experiments in isolated ventricular myocytes from nonfailing transgenic NCX overexpressor mice (OE). In field-stimulated myocytes, ouabain (1-100 μm) increased the amplitude of the Ca2+ transient in OE and wild-type (WT) similarly...
August 9, 2018: Fundamental & Clinical Pharmacology
El-Hadi Zerdazi, Florence Vorspan, Andries T Marees, François Naccache, Jean-Pierre Lepine, Jean-Louis Laplanche, Nathalie Prince, Cynthia Marie-Claire, Frank Bellivier, Stéphane Mouly, Vanessa Bloch
Methadone is known to be a risk factor for sudden death by enlarging ECG QT corrected (QTc) interval. For other medical conditions, QTc lengthening has been described as the result of interactions between pharmacological treatments and genetic factors. Former heroin dependent subjects under methadone maintenance treatment in remission for at last 3 months were recruited. We studied the association between QTc length (Bazett formula) and 126 SNPs located on 5 genes (KCNE1, KCNQ1, KCNH2, NOS1AP and SCN5A) previously associated with drug-induced QT prolongation...
August 7, 2018: Fundamental & Clinical Pharmacology
Hugo F Miranda, Fernando Sierralta, Nicolas Aranda, Paula Poblete, Viviana Noriega, Juan C Prieto
Neuropathic pain is associated with several conditions such as surgery, cancer, and diabetes and can be induced experimentally. Among the drugs used as monotherapy are gabapentin and tramadol. The purpose of this study was to evaluate the coadministration of gabapentin and tramadol, by isobolographic analysis, in three different algesiometric assays in experimental diabetic neuropathic pain induced by streptozocin in mice. In all the behavioral tests, gabapentin or tramadol produced a dose-dependent antinociception and their coadministration resulted in a positive interaction...
August 1, 2018: Fundamental & Clinical Pharmacology
Marie-Laure Laroche, Marianne Teste, Julien Vanoost, Hélène Geniaux
An inappropriate immunologic response has been suggested to play a role in the pathogenesis of hidradenitis suppurativa (HS). Adalimumab was the first TNF-α inhibitor approved for moderate to severe HS. We report on a case of HS (Hurley stage 2) in a 39-year-old man, who had received fusidic acid and isotretinoin treatments without evident benefit during the last 8 years. The patient noticed a reduction in the number of lesions and quality of life (DLQI from 27 to 6) in the 2 months following verapamil initiation for cluster headache...
July 19, 2018: Fundamental & Clinical Pharmacology
Amaurilio O Nogueira, Yasmin Ingrid S Oliveira, Beatriz L Adjafre, Maria E Amaral de Moraes, Gislei F Aragão
Protium heptaphyllum Aubl. belongs to the Burseraceae family. It is commonly called 'almecegueira' and is known to produce an amorphous resin which has constituents such as α- and β-amyrin, taraxastan-3-oxo-20-ol and sitostenonein. The α- and β-amyrin from P. heptaphyllum have pharmacological activities in several systems, such as central and peripheral nervous system, gastrointestinal tract and immunological system. In this study, our objective was to review pharmacological activities and to gather more information on the mixture of α- and β-amyrin obtained from P...
July 13, 2018: Fundamental & Clinical Pharmacology
Gaétan Gentile, Maeva Jego, Michel Spadari, Karolina Griffiths, Emilie Jouanjus, Joëlle Micallef
Addictovigilance is a health vigilance dedicated to the survey of medicinal or illicit psychoactive substance use disorders (SUDs). France is the only European country to have a vigilance system specifically dedicated to substances with an abuse/addiction potential. The French Addictovigilance system is organized in a network of regional tertiary centres (called Abuse and Dependence Monitoring Centres, CEIP-Addictovigilance) and works in close collaboration with Regional and National health authorities. Because of the essential and unavoidable nature of their practice in the French Healthcare system, general practitioners (GPs) are key actors to identify and track Addictovigilance signals...
July 12, 2018: Fundamental & Clinical Pharmacology
Tien-Yao Tsai, Iat-Lon Leong, Ka-Shun Cheng, Lian-Ru Shiao, Tzu-Hui Su, Kar-Lok Wong, Paul Chan, Yuk-Man Leung
A pathological feature in atherosclerosis is the dysfunction and death of vascular endothelial cells (EC). Oxidized low-density lipoprotein (LDL), known to accumulate in the atherosclerotic arterial walls, impairs endothelium-dependent relaxation and causes EC apoptosis. A major bioactive ingredient of the oxidized LDL is lysophosphatidylcholine (LPC), which at higher concentrations causes apoptosis and necrosis in various EC. There is hitherto no report on LPC-induced cytotoxicity in brain EC. In this work, we found that LPC caused cytosolic Ca2+ overload, mitochondrial membrane potential decrease, p38 activation, caspase 3 activation and eventually apoptotic death in mouse cerebral bEND...
July 5, 2018: Fundamental & Clinical Pharmacology
Behnaz Karimi, Mahboobeh Ashrafi, Tahoora Shomali, Azadeh Yektaseresht
Preclinical studies have shown positive effects of statins against specific cancers. This study aimed to determine the therapeutic effect of simvastatin in 12-dimethylbenz(a)anthracene (DMBA)-induced breast cancer. Female albino mice were divided into two groups, with or without DMBA administration. After tumor appearance, DMBA-treated group was further divided into four groups (D1-D4) as control (D1), treated with simvastatin at 80 and 40 mg/kg/day, orally (D2 and D3) and tamoxifen (50 mg/kg/day, orally) treated group (D4)...
July 1, 2018: Fundamental & Clinical Pharmacology
Suchi Raghunathan, Corey L Reynolds, Robert J Schwartz, M David Stewart, Bradley K McConnell
Inbred mouse strains are the most widely used mammalian model organism in biomedical research owing to ease of genetic manipulation and short lifespan; however, each inbred strain possesses a unique repertoire of deleterious homozygous alleles that can make a specific strain more susceptible to a particular disease. In the current study, we report dystrophic cardiac calcinosis (DCC) in C.B-17 SCID male mice at 10 weeks of age with no significant change in cardiac function. Acquisition of DCC was characterized by myocardial injury, fibrosis, calcification, and necrosis of the tissue...
June 30, 2018: Fundamental & Clinical Pharmacology
Bruno Ribeiro Baptista, Nadine Petitpain, Emmanuel Gomez, Melissa Yelehé-Okouma, Simon Valentin, Anne Guillaumot, François Chabot, Ari Chaouat
4-Aminopyridine (4-AP) is a recent treatment indicated to improve walking in patient with multiple sclerosis. We report the first case of pulmonary arterial hypertension (PAH) that we attribute to the use of 4-AP. A 64-year-old woman with multiple sclerosis presented with dyspnea. After excluding other secondary causes of pulmonary hypertension, a diagnosis of severe PAH due to 4-AP was made based on right heart catheterization. History revealed that the dyspnea began with the initiation of 4-AP. After discontinuation of 4-AP therapy and initiation of ambrisentan and tadalafil, dyspnea and pulmonary arterial pressure have improved significantly and one specific PAH treatment was stopped...
June 29, 2018: Fundamental & Clinical Pharmacology
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