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[PMID]: 29345156 [Au] Autor: Svetel M; Tomic A; Kresojevic N; Kostic V [Ad] Endereço: a Clinic of Neurology, Clinical Center of Serbia, Faculty of Medicine , University of Belgrade , Belgrade , Serbia. [Ti] Título: Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease. [So] Source: Expert Opin Drug Metab Toxicol;14(3):353-360, 2018 Mar. [Is] ISSN: 1744-7607 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: INTRODUCTION: Opicapone (OPC) is a novel, potent, reversible, and purely peripheral third-generation COMT inhibitor, which provides an enhancement in levodopa (L-Dopa) availability. It represents adjunctive therapy for L-Dopa treated patients with PD and motor fluctuations. Areas covered: The purpose of this study was to evaluate pharmacokinetic of OPC for the treatment of PD. Expert commentary: Oral OPC exhibits linear, dose-dependent absorption. However, following concomitant ingestion of a high-fat, high-calorie meal, the maximum plasma concentration will be decreased. A once-daily bedtime administration of OPC 1 h after the last daily L-Dopa/AADCi, are considered to avoid any interaction during the L-Dopa absorption phase. There are no clinically relevant effects of age (in adults), renal impairment or race on the pharmacokinetics of OPC. OPC dose adjustment is not needed in patients with mild to moderate chronic hepatic impairment. Opicapone exhibits the lowest potential for cytotoxicity in comparison with other COMT inhibitors. It significantly decreases COMT activity, with half-life of COMT inhibition in human erythrocytes of 61.6 h and increases systemic exposure to L-Dopa. This provides an enhancement in L-Dopa availability that translates into clinical benefit for PD patients in terms of significant decrease of OFF periods and increase in ON-time without troublesome dyskinesia. [Mh] Termos MeSH primário: Antiparkinsonianos/administração & dosagem Oxidiazóis/administração & dosagem Doença de Parkinson/tratamento farmacológico [Mh] Termos MeSH secundário: Adulto Animais Antiparkinsonianos/efeitos adversos Antiparkinsonianos/farmacocinética Inibidores de Catecol O-Metiltransferase/administração & dosagem Inibidores de Catecol O-Metiltransferase/farmacocinética Relação Dose-Resposta a Droga Quimioterapia Combinada Interações Alimento-Droga Meia-Vida Seres Humanos Levodopa/administração & dosagem Levodopa/farmacocinética Oxidiazóis/efeitos adversos Oxidiazóis/farmacocinética Doença de Parkinson/fisiopatologia [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Antiparkinson Agents); 0 (Catechol O-Methyltransferase Inhibitors); 0 (Oxadiazoles); 46627O600J (Levodopa); Y5929UIJ5N (opicapone) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180309 [Lr] Data última revisão: 180309 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180119 [St] Status: MEDLINE [do] DOI: 10.1080/17425255.2018.1430138

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[PMID]: 29274492 [Au] Autor: Çavusoglu BK; Yurttas L; Cantürk Z [Ad] Endereço: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey. Electronic address: betulkaya@anadolu.edu.tr. [Ti] Título: The synthesis, antifungal and apoptotic effects of triazole-oxadiazoles against Candida species. [So] Source: Eur J Med Chem;144:255-261, 2018 Jan 20. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: In search of potent and safe antifungal agents, herein, we report the synthesis, characterization and biological activities of triazole-oxadiazole compounds. The structural verification of the molecules was carried out by H NMR, C NMR and mass spectral data. The in vitro antifungal and apoptotic activity were investigated against C. albicans, C. parapsilosis, C. krusei and C. glabrata. The compounds namely N-(4-nitrophenyl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4e) and N-(6-fluorobenzothiazol-2-yl)-2-[(5-(2-((4-methyl-4H-1,2,4-triazol-3-yl)thio)ethyl)-1,3,4-oxadiazol-2-yl)thio]acetamide (4i) were detected as the most potent compounds against C. albicans and C. glabrata (MIC = 62.5 µg/mL). According to studies on their mechanism of action, it was confirmed that compound 4i has apoptotic effect on four Candida via Annexin V-PI with flow cytometry. The MTT assay revealed that all compounds were determined to be non-toxic against healthy cells in the tested concentrations. [Mh] Termos MeSH primário: Antifúngicos/química Antifúngicos/farmacologia Candida/efeitos dos fármacos Oxidiazóis/química Oxidiazóis/farmacologia Triazóis/química Triazóis/farmacologia [Mh] Termos MeSH secundário: Antifúngicos/síntese química Candidíase/tratamento farmacológico Seres Humanos Testes de Sensibilidade Microbiana Oxidiazóis/síntese química Relação Estrutura-Atividade Triazóis/síntese química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antifungal Agents); 0 (Oxadiazoles); 0 (Triazoles) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180309 [Lr] Data última revisão: 180309 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171224 [St] Status: MEDLINE

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[PMID]: 29318321 [Au] Autor: Ziaie M; Dilmaghani KA; Tukmechi A [Ti] Título: Synthesis and Biological Evaluation of 1,2,4-Triazoles and 1,3,4-Oxadiazoles Derivatives Linked to 1,4-Dihydropyridines Scaffold. [So] Source: Acta Chim Slov;64(4):895-901, 2017 Dec. [Is] ISSN: 1318-0207 [Cp] País de publicação: Slovenia [La] Idioma: eng [Ab] Resumo: A series of diethyl-2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate derivative coupled to 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones moieties at C2,C6 positions of 1,4-dihydropyridine ring system was prepared. This linkage was carried out by the reaction of 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones with 2,6-dibromomethyl-3,5-diethoxycarbonyl-4-phenyl-1,4-dihydropyridine in the presence of potassium carbonate as a weak base and dry acetone as the solvent. The newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR spectral data, elemental analysis and FAB-MS. The synthesized compounds were tested for their antimicrobial and antifungal activity against Escherichia coli and Aspergillus fumigatus in vitro in comparison with Enrofloxacin and Amphotericin as the reference drugs which are normally used for treating such infections. The synthetic compounds showed different inhibition zones against tested bacteria and fungi. Compound 8d showed more antagonistic activity against E. coli and A. fumigatus. [Mh] Termos MeSH primário: Anti-Infecciosos/síntese química Di-Hidropiridinas/química Oxidiazóis/química Triazóis/química [Mh] Termos MeSH secundário: Anti-Infecciosos/farmacologia Di-Hidropiridinas/farmacologia Espectroscopia de Ressonância Magnética Testes de Sensibilidade Microbiana Oxidiazóis/farmacologia Espectroscopia de Infravermelho com Transformada de Fourier Triazóis/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Infective Agents); 0 (Dihydropyridines); 0 (Oxadiazoles); 0 (Triazoles) [Em] Mês de entrada: 1803 [Cu] Atualização por classe: 180306 [Lr] Data última revisão: 180306 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180111 [St] Status: MEDLINE

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[PMID]: 27779493 [Au] Autor: Sales AJ; Hiroaki-Sato VA; Joca SR [Ad] Endereço: aDepartment of Pharmacology, School of Medicine of Ribeirão Preto bDepartment of Physics and Chemistry, School of Pharmaceutical Sciences of Ribeirão Preto cCenter for Interdisciplinary Research on Applied Neurosciences (NAPNA), University of São Paulo, Ribeirão Preto, São Paulo, Brazil. [Ti] Título: Participation of hippocampal nitric oxide synthase and soluble guanylate cyclase in the modulation of behavioral responses elicited by the rat forced swimming test. [So] Source: Behav Pharmacol;28(1):19-29, 2017 02. [Is] ISSN: 1473-5849 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Systemic or hippocampal administration of nitric oxide (NO) synthase inhibitors induces antidepressant-like effects in animals, implicating increased hippocampal levels of NO in the neurobiology of depression. However, the role played by different NO synthase in this process has not been clearly defined. As stress is able to induce neuroinflammatory mechanisms and trigger the expression of inducible nitric oxide synthase (iNOS) in the brain, as well as upregulate neuronal nitric oxide synthase (nNOS) activity, the aim of the present study was to investigate the possible differential contribution of hippocampal iNOS and nNOS in the modulation of the consequences of stress elicited by the forced swimming test. Male Wistar rats received intrahippocampal injections, immediately after the pretest or 1 h before the forced swimming test, of selective inhibitors of nNOS (N-propyl-L-arginine), iNOS (1400W), or sGC (ODQ), the main pharmacological target for NO. Stress exposure increased nNOS and phospho-nNOS levels at all time points, whereas iNOS expression was increased only 24 h after the pretest. All drugs induced an antidepressant-like effect. However, whereas the nNOS inhibitor was equally effective when injected at different times, the iNOS inhibitor was more effective 24 h after the pretest. These results suggest that hippocampal nNOS and iNOS contribute to increase in NO levels in response to stress, although with a differential time course after stress exposure. [Mh] Termos MeSH primário: Óxido Nítrico Sintase Tipo II/metabolismo Óxido Nítrico Sintase Tipo I/metabolismo Guanilil Ciclase Solúvel/metabolismo Estresse Psicológico/metabolismo [Mh] Termos MeSH secundário: Amidinas/farmacologia Animais Arginina/análogos & derivados Arginina/farmacologia Benzilaminas/farmacologia Modelos Animais de Doenças Hipocampo/metabolismo Masculino Óxido Nítrico/metabolismo Oxidiazóis/farmacologia Ratos Ratos Wistar Natação Fatores de Tempo [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (1H-(1,2,4)oxadiazolo(4,3-a)-quiloxalin-1-one); 0 (Amidines); 0 (Benzylamines); 0 (N(omega)-propylarginine); 0 (N-(3-(aminomethyl)benzyl)acetamidine); 0 (Oxadiazoles); 31C4KY9ESH (Nitric Oxide); 94ZLA3W45F (Arginine); EC 1.14.13.39 (Nitric Oxide Synthase Type I); EC 1.14.13.39 (Nitric Oxide Synthase Type II); EC 4.6.1.2 (Soluble Guanylyl Cyclase) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180228 [Lr] Data última revisão: 180228 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161026 [St] Status: MEDLINE [do] DOI: 10.1097/FBP.0000000000000263

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[PMID]: 29310025 [Au] Autor: Madhu Sekhar M; Nagarjuna U; Padmavathi V; Padmaja A; Reddy NV; Vijaya T [Ad] Endereço: Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India. [Ti] Título: Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles. [So] Source: Eur J Med Chem;145:1-10, 2018 Feb 10. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: A new class of methylthio linked pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles were prepared under conventional and ultrasound irradiation methods. All the compounds were obtained in higher yields and in shorter reaction times in ultrasound irradiation method when compared with the conventional method. The title compounds were tested for antimicrobial activity. The compounds 12c and 12f exhibited promising antibacterial activity against P. aeruginosa whereas the compounds 13c and 13f showed pronounced antifungal activity against A. niger. [Mh] Termos MeSH primário: Antibacterianos/farmacologia Antifúngicos/farmacologia Aspergillus niger/efeitos dos fármacos Oxidiazóis/farmacologia Pseudomonas aeruginosa/efeitos dos fármacos Pirimidinas/farmacologia Tiadiazóis/farmacologia Triazóis/farmacologia [Mh] Termos MeSH secundário: Antibacterianos/síntese química Antibacterianos/química Antifúngicos/síntese química Antifúngicos/química Relação Dose-Resposta a Droga Testes de Sensibilidade Microbiana Estrutura Molecular Oxidiazóis/síntese química Oxidiazóis/química Pirimidinas/síntese química Pirimidinas/química Relação Estrutura-Atividade Tiadiazóis/síntese química Tiadiazóis/química Triazóis/síntese química Triazóis/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Oxadiazoles); 0 (Pyrimidines); 0 (Thiadiazoles); 0 (Triazoles); 14IAC3GH7G (1,3,4-thiadiazole) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180227 [Lr] Data última revisão: 180227 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180109 [St] Status: MEDLINE

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[PMID]: 29415596 [Au] Autor: Castro Caldas A; Teodoro T; Ferreira JJ [Ad] Endereço: a Neurology Service, Department of Neurosciences , Hospital de Santa Maria , Lisbon , Portugal. [Ti] Título: The launch of opicapone for Parkinson's disease: negatives versus positives. [So] Source: Expert Opin Drug Saf;17(3):331-337, 2018 Mar. [Is] ISSN: 1744-764X [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: INTRODUCTION: Opicapone is a novel, third generation COMT inhibitor approved for the treatment of Parkinson's disease. Safety and tolerability data is critical to determine the benefit-harm balance and anticipate therapeutic adherence. Areas covered: This review evaluates the tolerability and safety profile of opicapone. These data were extracted from all published clinical trials, including preclinical, phase I, phase II and phase III studies as well as postmarketing data. Opicapone was safe and well tolerated, with frequencies of treatment-emergent adverse events similar to placebo. Expert opinion: Opicapone have shown a good safety and tolerability profile. This adds to its proven efficacy and convenient once-daily administration, supporting a role of opicapone as a first-line therapy for motor complications in Parkinson's disease patients. [Mh] Termos MeSH primário: Inibidores de Catecol O-Metiltransferase/administração & dosagem Oxidiazóis/administração & dosagem Doença de Parkinson/tratamento farmacológico [Mh] Termos MeSH secundário: Animais Antiparkinsonianos/administração & dosagem Antiparkinsonianos/efeitos adversos Antiparkinsonianos/farmacologia Inibidores de Catecol O-Metiltransferase/efeitos adversos Inibidores de Catecol O-Metiltransferase/farmacologia Esquema de Medicação Seres Humanos Oxidiazóis/efeitos adversos Oxidiazóis/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Antiparkinson Agents); 0 (Catechol O-Methyltransferase Inhibitors); 0 (Oxadiazoles); Y5929UIJ5N (opicapone) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180215 [Lr] Data última revisão: 180215 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 180209 [St] Status: MEDLINE [do] DOI: 10.1080/14740338.2018.1433659

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[PMID]: 29030082 [Au] Autor: Marszalek-Grabska M; Gibula-Bruzda E; Bodzon-Kulakowska A; Suder P; Gawel K; Talarek S; Listos J; Kedzierska E; Danysz W; Kotlinska JH [Ad] Endereço: Department of Pharmacology and Pharmacodynamics, Medical University, Lublin, Poland. [Ti] Título: ADX-47273, a mGlu5 receptor positive allosteric modulator, attenuates deficits in cognitive flexibility induced by withdrawal from 'binge-like' ethanol exposure in rats. [So] Source: Behav Brain Res;338:9-16, 2018 Feb 15. [Is] ISSN: 1872-7549 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Repeated exposure to and withdrawal from ethanol induces deficits in spatial reversal learning. Data indicate that metabotropic glutamate 5 (mGlu5) receptors are implicated in synaptic plasticity and learning and memory. These receptors functionally interact with N-methyl-d-aspartate (NMDA) receptors, and activation of one type results in the activation of the other. We examined whether (S)-(4-fluorophenyl)(3-(3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl)-piperidin-1-yl (ADX-47273), a positive allosteric modulator (PAM) of mGlu5 receptor, attenuates deficits in reversal learning induced by withdrawal (11-13days) from 'binge-like' ethanol input (5.0g/kg, i.g. for 5days) in the Barnes maze (a spatial learning) task in rats. We additionally examined the effects of ADX-47273 on the expression of the NMDA receptors subunit, GluN2B, in the hippocampus and prefrontal cortex, on the 13th day of ethanol withdrawal. Herein, withdrawal from repeated ethanol administration impaired reversal learning, but not the probe trial. Moreover, ADX-47273 (30mg/kg, i.p.) given prior to the first reversal learning trial for 3days in the Barnes maze, significantly enhanced performance in the ethanol-treated group. The 13th day of ethanol abstinence decreased the expression of the GluN2B subunit in the selected brain regions, but ADX-47273 administration increased it. In conclusion, positive allosteric modulation of mGlu5 receptors recovered spatial reversal learning impairment induced by withdrawal from 'binge-like' ethanol exposure. Such effect seems to be correlated with the mGlu5 receptors mediated potentiation of GluN2B-NMDA receptor mediated responses in the hippocampus and prefrontal cortex. Thus, our results emphasize the role of mGlu5 receptor PAM in the adaptive learning impaired by ethanol exposure. [Mh] Termos MeSH primário: Cognição/efeitos dos fármacos Etanol/administração & dosagem Oxidiazóis/farmacologia Piperidinas/farmacologia Receptor de Glutamato Metabotrópico 5/metabolismo Reversão de Aprendizagem/efeitos dos fármacos Aprendizagem Espacial/efeitos dos fármacos Síndrome de Abstinência a Substâncias/psicologia [Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos Animais Masculino Atividade Motora/efeitos dos fármacos Ratos Ratos Wistar Síndrome de Abstinência a Substâncias/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Oxadiazoles); 0 (Piperidines); 0 (Receptor, Metabotropic Glutamate 5); 0 (S-(4-fluorophenyl)-(3-(3-(4-fluorophenyl)-(1,2,4)-oxadiazol-5-yl)piperidin-1-yl)methanone); 3K9958V90M (Ethanol) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180207 [Lr] Data última revisão: 180207 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171015 [St] Status: MEDLINE

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[PMID]: 28448438 [Au] Autor: Khamrang T; Hung KC; Hsia CH; Hsieh CY; Velusamy M; Jayakumar T; Sheu JR [Ad] Endereço: Department of Chemistry, North Eastern Hill University, Shillong 793022, India. themmilakhamrang@gmail.com. [Ti] Título: Antiplatelet Activity of a Newly Synthesized Novel Ruthenium (II): A Potential Role for Akt/JNK Signaling. [So] Source: Int J Mol Sci;18(5), 2017 Apr 27. [Is] ISSN: 1422-0067 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: In oncotherapy, ruthenium complexes are considered as potential alternatives for platinum compounds, and have been proved as promising anticancer drugs with high efficacy and lesser side effects. Platelet activation plays a major role in cancer metastasis and progression. Hence, this study explored the effect of a newly synthesized ruthenium complex, [Ru(η6-cymene)(L)Cl]BF4(TQ5), where L = 4-phenyl-2-pyridin-2-yl-quinazoline), on human platelet activation. TQ5 (3-5 µM) inhibited concentration-dependent collagen-induced platelet aggregation in washed human platelets. However, this compound only inhibited platelet aggregation at a maximum concentration of 500 and 100 µM against thrombin and 9,11-dideoxy-11α, 9α-epoxymethanoprostaglandin (U46619)-induced stimulation, respectively. TQ5 inhibited collagen-induced ATP release and calcium mobilization ([Ca ] ), without inducing cell cytotoxicity. In addition, neither SQ22536, an adenylate cyclase inhibitor, nor 1H-[1,2,4] oxadiazolo [4,3-a]quinoxalin-1-one (ODQ), a guanylate cyclase inhibitor, significantly reversed the TQ5-mediated inhibition of platelet aggregation. TQ5 inhibited the collagen-induced phosphorylation of protein kinase B (Akt) and c-Jun N-terminal kinase (JNK), but did not effectively inhibit extracellular signal-regulated kinase 1/2 (ERK1/2) and p38-mitogen-activated protein kinase (p38-MAPK) in human platelets. Additionally, TQ5 significantly prolonged the closure time in whole blood and increased the occlusion time of thrombotic platelet plug formation in mice. This study demonstrates, for the first time, that a newly synthesized ruthenium complex, TQ5, exhibits potent antiplatelet activity by hindering ATP release and [Ca ] , and by decreasing the activation of Akt/JNK signals. Together, these results suggest that TQ5 could be developed as a therapeutic agent that helps prevent or treat thromboembolic disorders, since it is found to be potently more effective than a well-established antithrombotic aspirin. [Mh] Termos MeSH primário: Plaquetas/efeitos dos fármacos Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo Agregação Plaquetária/efeitos dos fármacos Proteínas Proto-Oncogênicas c-akt/metabolismo Rutênio/química Rutênio/farmacologia Transdução de Sinais/efeitos dos fármacos [Mh] Termos MeSH secundário: Ácido 15-Hidroxi-11 alfa,9 alfa-(epoximetano)prosta-5,13-dienoico/farmacologia Trifosfato de Adenosina/metabolismo Plaquetas/citologia Plaquetas/metabolismo Cálcio/metabolismo Colágeno/farmacologia Complexos de Coordenação/síntese química Complexos de Coordenação/farmacologia AMP Cíclico/metabolismo Seres Humanos Oxidiazóis/farmacologia Fosforilação/efeitos dos fármacos Ativação Plaquetária/efeitos dos fármacos Inibidores da Agregação de Plaquetas/síntese química Inibidores da Agregação de Plaquetas/farmacologia Quinoxalinas/farmacologia Trombina/farmacologia Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one); 0 (Coordination Complexes); 0 (Oxadiazoles); 0 (Platelet Aggregation Inhibitors); 0 (Quinoxalines); 76898-47-0 (15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid); 7UI0TKC3U5 (Ruthenium); 8L70Q75FXE (Adenosine Triphosphate); 9007-34-5 (Collagen); E0399OZS9N (Cyclic AMP); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EC 2.7.11.24 (JNK Mitogen-Activated Protein Kinases); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); EC 3.4.21.5 (Thrombin); SY7Q814VUP (Calcium) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180122 [Lr] Data última revisão: 180122 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170428 [St] Status: MEDLINE

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[PMID]: 29212068 [Au] Autor: Kitay AM; Link A; Geibel JP [Ad] Endereço: Department of Surgery, Yale University, School of Medicine, New Haven, Connecticut, USA. [Ti] Título: Activation of Secretagogue Independent Gastric Acid Secretion via Endothelial Nitric Oxide Synthase Stimulation in Rats. [So] Source: Cell Physiol Biochem;44(4):1606-1615, 2017. [Is] ISSN: 1421-9778 [Cp] País de publicação: Switzerland [La] Idioma: eng [Ab] Resumo: BACKGROUND/AIMS: L-arginine is an important mediator of cell division, wound healing, and immune function. It can be transformed by the nitric oxide synthase (NOS) to nitric oxide (NO), an important cell signaling molecule. Recent studies from our laboratory demonstrate specific effects of L-arginine (10mM) exposure on gastric acid secretion in rat parietal cells. METHODS: Studies were performed with isolated gastric glands and the pH sensitive dye BCECF-AM +/- L-arginine to examine its effects on acid secretion. The direct NO-donor diethylamine NONOate sodium salt hydrate, was also used while monitoring intracellular pH. The specific inhibitor of the intracellular NO signal cascade ODQ was also used. RESULTS: We found that gastric proton extrusion was activated with application of L-arginine (10mM), in a separate series when L-arginine (10mM) + L-NAME (30µM) were added there was no acid secretion. Addition of the NO-donor diethylamine NONOate sodium salt hydrate (10µM) also induced acid secretion. When the selective sGC-inhibitor ODQ was added with NONOate we did not observe acid secretion. CONCLUSION: We conclude that L-arginine is a novel secretagogue, which can mediate gastric acid secretion. Furthermore, the intake of L-arginine causes direct activation of the H+, K+ ATPase and increased proton extrusion from parietal cells resulting in the increased risk for acid-related diseases. The NO/sGC/cGMP pathway has never been described as a possible intracellular mechanism for H+, K+ ATPase activation before and presents a completely new scientific finding. Moreover, our studies demonstrate a novel role for L-NAME to effectively eliminate NOS induced acid secretion and thereby reducing the risk for L-arginine inducible ulcer disease. [Mh] Termos MeSH primário: Ácido Gástrico/secreção Óxido Nítrico Sintase Tipo III/metabolismo [Mh] Termos MeSH secundário: Animais Arginina/farmacologia ATPase Trocadora de Hidrogênio-Potássio/metabolismo Concentração de Íons de Hidrogênio Masculino NG-Nitroarginina Metil Éster/farmacologia Oxidiazóis/farmacologia Células Parietais Gástricas/citologia Células Parietais Gástricas/efeitos dos fármacos Células Parietais Gástricas/metabolismo Quinoxalinas/farmacologia Ratos Ratos Sprague-Dawley [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one); 0 (Oxadiazoles); 0 (Quinoxalines); 94ZLA3W45F (Arginine); EC 1.14.13.39 (Nitric Oxide Synthase Type III); EC 3.6.3.10 (H(+)-K(+)-Exchanging ATPase); V55S2QJN2X (NG-Nitroarginine Methyl Ester) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180118 [Lr] Data última revisão: 180118 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171207 [St] Status: MEDLINE [do] DOI: 10.1159/000485755

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[PMID]: 28456302 [Au] Autor: Gao M; Yu L; Li P; Song X; Chen Z; He M; Song B [Ad] Endereço: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, PR China. [Ti] Título: Label-free quantitative proteomic analysis of inhibition of Xanthomonas axonopodis pv. citri by the novel bactericide Fubianezuofeng. [So] Source: Pestic Biochem Physiol;138:37-42, 2017 May. [Is] ISSN: 1095-9939 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: To understand the antibacterial mechanism of the new bactericide 2-(methylsulfonyl)-5- (4-fluorobenzyl)-1, 3, 4-oxadiazole (Generic name: Fubianezuofeng), we performed label-free quantitative proteomics analysis of the response of Xanthomonas axonopodis pv. citri (Xac) strain 29-1 to Fubianezuofeng. A total of 1133 proteins were identified in the treatment and control groups. Upon treatment with the 1/2 minimum inhibitory concentration (MIC), 339 proteins were found to be differentially expressed (fold changes>1.5, p<0.05) with 99 upregulated and 240 down-regulated. In comparison, 314 proteins were differentially expressed (125 up-regulated, 189 down-regulated) at MIC. The differentially expressed proteins were enriched for those involved in the pyrimidine metabolic pathway. The results offer a complete view of the proteome changes in bacteria in response to Fubianezuofeng. [Mh] Termos MeSH primário: Antibacterianos/farmacologia Oxidiazóis/farmacologia Proteômica Sulfonas/farmacologia Xanthomonas axonopodis/classificação Xanthomonas axonopodis/efeitos dos fármacos [Mh] Termos MeSH secundário: Antibacterianos/química Proteínas de Bactérias/genética Proteínas de Bactérias/metabolismo Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos Estrutura Molecular Oxidiazóis/química Mapas de Interação de Proteínas Sulfonas/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Bacterial Agents); 0 (Bacterial Proteins); 0 (Oxadiazoles); 0 (Sulfones); 0 (fubianezuofeng) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171128 [Lr] Data última revisão: 171128 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170501 [St] Status: MEDLINE

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