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Pharmacological Reports: PR

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https://www.readbyqxmd.com/read/28511054/synthesis-and-in-vitro-anticancer-activity-of-new-2-thioxo-oxazolidin-4-one-derivatives
#1
Júlia Furtado Campos, Michelly Cristiny Pereira, Wanessa Layssa Batista de Sena, Caio Gomes de Barros Martins, Jamerson Ferreira de Oliveira, Cezar Augusto da Cruz Amorim, Moacyr Jesus Barreto de Melo Rêgo, Marina Galdino da Rocha Pitta, Maria do Carmo Alves de Lima, Maira Galdino da Rocha Pitta, Ivan da Rocha Pitta
BACKGROUND: Oxazolidinones derivatives exhibit different biological properties, including anticancer activity. This work aimed to investigate the anticancer potential of five novel 2-Thioxo-oxazolidin-4-one derivatives. METHODS: Cytotoxicity assays were performed in human peripheral blood mononuclear cells (PBMCs) from healthy individuals and seven tumor cell lines. Apoptosis detection and cell cycle were evaluated by flow cytometry and the expression of genes involved in cell death processes by Real-Time PCR...
March 18, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28521173/thymoquinone-ameliorates-renal-damage-in-unilateral-ureteral-obstruction-in-rats
#2
Sara Hosseinian, Abolfazl Khajavi Rad, Alireza Ebrahimzadeh Bideskan, Mohammad Soukhtanloo, Hamidreza Sadeghnia, Mohammad Naser Shafei, Fatemeh Motejadded, Reza Mohebbati, Samira Shahraki, Farimah Beheshti
BACKGROUND: It is well established that renin-angiotensin system (RAS) play a central role in pathophysiology of renal damage following unilateral ureteral obstruction (UUO). The present study investigated the effects of thymoquinone and RAS blockade on renal tissue damage and renal expression of angiotensin II after UUO in rats. METHODS: Forty male rats were divided to five groups: Sham-operated group, UUO group and rats with UUO treated with losartan, captopril and thymoquinone...
March 14, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28505604/nrf2-and-nf-%C3%AE%C2%BAb-modulation-by-plumbagin-attenuates-functional-behavioural-and-biochemical-deficits-in-rat-model-of-neuropathic-pain
#3
Vijay Arruri, Prashanth Komirishetty, Aparna Areti, Siva Kumar Naik Dungavath, Ashutosh Kumar
BACKGROUND: Plumbagin is known to exhibit a broad range of biological activities including anti-cancer, antimicrobial and has been widely used traditionally. Nuclear factor kappa-light-chain-enhancer of activated B-cells (NF-κB) inhibitory and Nuclear factor (erythroid derived-2) like-2 (Nrf2) modulatory activities of Plumbagin have been reported already. In nerve injury model of neuropathy in rats, the role of NF-κB upregulation and declined antioxidant defence has been well recognized...
February 27, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28505603/icariin-protects-against-thioacetamide-induced-liver-fibrosis-in-rats-implication-of-anti-angiogenic-and-anti-autophagic-properties
#4
Mardi M Algandaby, Randa M Breikaa, Basma G Eid, Thikrayat A Neamatallah, Ashraf B Abdel-Naim, Osama M Ashour
BACKGROUND: Liver fibrosis is a major health problem. The current study evaluated the potential of icariin (ICA) to guard against thioacetamide (TAA)-induced liver fibrosis in rats. METHODS: Four groups of male rats were treated as follows: group 1 was the control group, group 2 was given TAA (200mg/kg), group 3 was administered ICA (50mg/kg) and TAA (200mg/kg), and group 4 was given ICA (50mg/kg) alone. Animal treatment was continued for four weeks. RESULTS: Co-administration of ICA guarded against TAA hepatotoxicity as indicated by significant inhibition in the rise of serum ALT and AST activities and albumin concentrations...
February 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28501682/the-role-of-arachidonic-acid-cyclooxygenase-cascade-phosphodiesterase-iv-and-rho-kinase-in-h2s-induced-relaxation-in-the-mouse-corpus-cavernosum
#5
Fatma Aydinoglu, Nuran Ogulener
BACKGROUND: Penile corpus cavernosum is an extremely vascularized tissue and cavernosal smooth muscle tone is regulated by the balance between contractile and relaxant factor. We investigated the possible role of arachidonic acid/cyclooxygenase cascade, phosphodiesterase IV (PDEIV) and Rho-kinase in exogenous hydrogen sulfide (H2S)-induced relaxation in mouse corpus cavernosum. METHODS: The relaxant response to H2S (NaHS as exogenous H2S; 1-1000μM) were obtained in isolated mouse corpus cavernosum tissues which pre-contracted by phenylephrine (5μM)...
February 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28400086/corrigendum-to-epicutaneous-immunization-with-protein-antigen-tnp-ig-alleviates-tnbs-induced-colitis-in-mice-pharmacol-rep-64-2012-1497-1504
#6
Monika Majewska-Szczepanik, Marta Góralska, Katarzyna Marcińska, Magdalena Zemelka-Wiącek, Anna Strzępa, Iwona Dorożyńska, Marian Szczepanik
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28373019/corrigendum-to-inhibition-of-2-4-dinitrofluorobenzene-induced-contact-hypersensitivity-reaction-by-antidepressant-drugs-pharmacol-rep-65-2013-1237-1246
#7
Katarzyna Curzytek, Marta Kubera, Monika Majewska-Szczepanik, Marian Szczepanik, Katarzyna Marcińska, Włodzimierz Ptak, Weronika Duda, Monika Leśkiewicz, Agnieszka Basta-Kaim, Bogusława Budziszewska, Władysław Lasoń, Michael Maes
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28373018/corrigendum-to-metformin-has-adenosine-monophosphate-activated-protein-kinase-ampk-independent-effects-on-lps-stimulated-rat-primary-microglial-cultures-pharmacol-rep-62-2010-827-848
#8
Krzysztof Łabuzek, Sebastian Liber, Bożena Gabryel, Bogusław Okopień
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28365259/corrigendum-to-comparison-of-chosen-activation-markers-of-human-monocytes-macrophages-isolated-from-the-peripheral-blood-of-young-and-elderly-volunteers-pharmacol-rep-66-2014-759-765
#9
Dariusz Suchy, Krzysztof Łabuzek, Łukasz Bułdak, Dawid Szkudłapski, Bogusław Okopień
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28365258/corrigendum-to-eplerenone-promotes-alternative-activation-in-human-monocyte-derived-macrophages-pharmacol-rep-65-2013-226-234
#10
Krzysztof Łabuzek, Sebastian Liber, Łukasz Bułdak, Grzegorz Machnik, Justyna Liber, Bogusław Okopień
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28365257/corrigendum-to-epicutaneous-immunization-with-phosphorylcholine-conjugated-to-bovine-serum-albumin-pc-bsa-and-tlr9-ligand-cpg-alleviates-pneumococcal-pneumonia-in-mice-pharmacol-rep-66-2014-570-575
#11
Monika Majewska-Szczepanik, Natsuo Yamamoto, Philip W Askenase, Marian Szczepanik
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28365256/corrigendum-to-epicutaneous-immunization-with-protein-antigen-tnp-ig-and-nod2-ligand-muramyl-dipeptide-mdp-reverses-skin-induced-suppression-of-contact-hypersensitivity-pharmacol-rep-66-2014-137-142
#12
Monika Majewska-Szczepanik, Iwona Dorożyńska, Anna Strzępa, Marian Szczepanik
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28365255/corrigendum-to-oral-treatment-with-enrofloxacin-early-in-life-promotes-th2-mediated-immune-response-in-mice-pharmacol-rep-68-2016-44-50
#13
Anna Strzępa, Monika Majewska-Szczepanik, Paulina Kowalczyk, Dorota Woźniak, Sylwia Motyl, Marian Szczepanik
No abstract text is available yet for this article.
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364698/n-heterocyclic-choline-analogues-based-on-1-2-3-4-tetrahydro-iso-quinoline-scaffold-with-anticancer-and-anti-infective-dual-action
#14
Alla Zablotskaya, Izolda Segal, Athina Geronikaki, Irina Shestakova, Vizma Nikolajeva, Galina Makarenkova
BACKGROUND: Pharmacological effects of biologically active "small molecules" can be improved by their targeted modification, which affects drug delivery and interaction with tumor cells and microorganisms. We aimed to evaluate anticancer and antimicrobial activity of lipid-like choline derivatives modified via simultaneous introduction of tetrahydro(iso)quinoline based pharmacophore system at nitrogen atom and long chain alkyl substituent at oxygen atom. METHODS: Target compounds were synthesized under phase-transfer catalysis conditions followed by quaternization, and evaluated for cytotoxicity and NO-generation ability on HT-1080 and MG-22A tumor cell lines and NIH 3T3 normal mouse fibroblasts, and screened for antimicrobial activity against gram-positive (Staphylococcus aureus and Bacillus cereus) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa and Proteus mirabilis) and fungi (Candida albicans and Aspergillus niger)...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364697/antidepressant-like-effect-of-1-2-3-4-tetrahydroisoquinoline-and-its-methyl-derivative-in-animal-models-of-depression
#15
Edyta Możdżeń, Agnieszka Wąsik, Irena Romańska, Jerzy Michaluk, Lucyna Antkiewicz-Michaluk
BACKGROUND: Most of the currently used antidepressant drugs are monoamine-based compounds, acting by the inhibition of re-uptake or metabolism of noradrenaline (NA) and/or serotonin (5-HT), because these neurotransmitters play a key role in the pathophysiology of depression. The aim of this study was to investigate the potential antidepressant-like activity of an endogenous amine, 1,2,3,4-tetrahydroisoquinoline (TIQ) and its close derivative, 1-methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ)...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364696/differential-effects-of-liver-steatosis-on-pharmacokinetic-profile-of-two-closely-related-hepatoselective-no-donors-v-pyrro-no-and-v-proli-no
#16
Kamil Kus, Edyta Kus, Agnieszka Zakrzewska, Wojciech Jawien, Barbara Sitek, Maria Walczak, Stefan Chlopicki
PURPOSE: To analyze the effect of liver steatosis and obesity on pharmacokinetic profile of two structurally-related liver-selective NO-donors - V-PYRRO/NO and V-PROLI/NO. METHODS: C57BL/6 mice were fed control or high-fat diet for 15 weeks to induced liver steatosis and obesity (HFD mice). Pharmacokinetics and renal elimination studies were conducted in vivo following iv dosing of V-PYRRO/NO and V-PROLI/NO (0.03mmol/kg). Hepatic clearance was evaluated ex vivo in the isolated perfused mice liver and in vitro with the use of liver microsomes...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364695/the-influence-of-a-single-and-chronic-administration-of-venlafaxine-on-tramadol-pharmacokinetics-in-a-rabbit-model
#17
Danuta Szkutnik-Fiedler, Tomasz Grabowski, Monika Balcerkiewicz, Michał Michalak, Irina Pilipczuk, Łukasz Wyrowski, Hanna Urjasz, Edmund Grześkowiak
BACKGROUND: The combined use of tramadol with selective serotonin and norepinephrine reuptake inhibitors e.g. venlafaxine may be associated with serotonin syndrome. No previous studies exist examining the influence of a weak CYP2D6 inhibitor venlafaxine on the pharmacokinetics of tramadol. Therefore, the aim of this study was to determine the effect of a single and chronic administration of venlafaxine on the pharmacokinetics of tramadol using a rabbit model. METHODS: Adult New Zealand white rabbits of both sexes (n=21) were used...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364694/the-role-of-melatonin-neurokinin-neurotrophic-tyrosine-kinase-and-glucocorticoid-receptors-in-antidepressant-like-effect
#18
REVIEW
Karolina Pytka, Katarzyna Młyniec, Karolina Podkowa, Adrian Podkowa, Magdalena Jakubczyk, Elżbieta Żmudzka, Klaudia Lustyk, Jacek Sapa, Barbara Filipek
Over the last few decades, depression has become one of the major public health problems in our society. This problem is connected not only with morbidity, but also with treatment, specifically with the effectiveness of the therapy as well as the concomitant side effects of available antidepressants. Major depressive disorder is a complex clinical entity, including different molecular mechanisms and neurological processes. This complexity is a challenge for scientists seeking to discover an innovatory antidepressant drug with multiple and complementary mechanisms of action...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364693/the-%C3%AF-1-receptor-agonist-pentazocine-increases-store-operated-ca-2-entry-in-mcf7%C3%AF-1-and-sk-n-sh-cell-lines
#19
Giuseppe Gasparre, Carmen Abate, Roberto Carlucci, Francesco Berardi, Giuseppe Cassano
BACKGROUND: The intracellular [Ca(2+)] is modulated by σ receptors. An important component of the cellular machinery governing the intracellular [Ca(2+)] is Store-Operated Calcium Entry (SOCE). Here we want to investigate whether ligands of σ receptors affect SOCE. METHODS: The intracellular [Ca(2+)] was monitored, with the fluorescent Ca(2+)-sensitive probe Fura-2, in four cell lines with a different expression of σ receptors, namely MCF7 (expressing σ1 receptors with a low density and overexpressing σ2 receptors), MCF7σ1 (overexpressing σ1 receptors), SK-N-SH, and HT-29...
June 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28364692/the-effect-of-three-angiotensin-converting-enzyme-inhibitors-on-kynurenic-acid-production-in-rat-kidney-in-vitro
#20
Izabela Zakrocka, Tomasz Kocki, Waldemar A Turski
BACKGROUND: The renin-angiotensin system (RAS) is commonly known to regulate blood pressure, water and electrolyte homeostasis, however it also exerts paracrine and autocrine actions on the kidney. Angiotensin-converting enzyme inhibitors (ACE-Is), alongside their hypotensive properties, have been shown to decrease kidney function decline in animal models of nephropathy. Glutamate (GLU) is the main stimulatory neurotransmitter in the central nervous system, however its importance in the periphery should also be considered...
June 2017: Pharmacological Reports: PR
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