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[PMID]:29314204
[Au] Autor:Jin Z; Tan Q; Sun B
[Ad] Endereço:State Key Laboratory of Biomembrane and Membrane Biotechnology, School of Medicine, Tsinghua University, Beijing, China.
[Ti] Título:Telmisartan ameliorates vascular endothelial dysfunction in coronary slow flow phenomenon (CSFP).
[So] Source:Cell Biochem Funct;36(1):18-26, 2018 Jan.
[Is] ISSN:1099-0844
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Coronary slow flow phenomenon (CSFP) is a coronary microvascular disorder with an increasing morbidity, and currently, available therapies are of limited clinical value for its cure. Hence, it is urgent to find a novel approach to CSFP treatment. Several studies show that endothelial dysfunction plays a critical role in the aetiology of CSFP. Telmisartan (TMST) is a clinically available anti-hypertensive medicine and has shown its potential properties for improving vascular endothelial function. Thus, we aimed to investigate the effect of TMST on endothelial dysfunction in CSFP, Endothelial-dependent flow-mediated vasodilation, serum levels of nitric oxide, adiponectin, and endothelin-1 were surveyed before and after 3 months of TMST treatment. And the percentages of vasodilator response to acetylcholine (Ach) were detected after 12 weeks of TMST treatment. Compare with pretreatment, flow-mediated vasodilation, nitric oxide, and adiponectin were substantially improved after TMST treatment; meanwhile, endothelin-1 was decreased in the TMST group (all P < .01). Compared with the model group, the vasodilator response to Ach was enormously increased after TMST intervention. Additionally, administration of SU11274 or GW9662 would partially reverse the protective effects of TMST on accumulative concentration-vasodilator responses to Ach (P < .01). We demonstrated that administration of TMST could remarkably increase the mRNA and/or protein levels of hepatocyte growth factor, mesenchymal-epithelial transition factor, peroxisome proliferation-activated receptor γ, whereas dramatically diminish mRNA and/or protein levels of p-JNK1/2, mitogen-activated protein kinase, and nuclear factor kappa B (P < .05). Our results thus implicate that TMST ameliorates endothelial dysfunction in CSFP. It is suggested that TSMF may play an important role in the medication of CSFP.
[Mh] Termos MeSH primário: Benzimidazóis/farmacologia
Benzimidazóis/uso terapêutico
Benzoatos/farmacologia
Benzoatos/uso terapêutico
Endotélio Vascular/efeitos dos fármacos
Endotélio Vascular/fisiopatologia
Fenômeno de não Refluxo/tratamento farmacológico
[Mh] Termos MeSH secundário: Angiotensina II/farmacologia
Animais
Benzimidazóis/química
Benzoatos/química
Relação Dose-Resposta a Droga
Endotélio Vascular/metabolismo
Feminino
Seres Humanos
Masculino
Meia-Idade
Coelhos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Benzoates); 11128-99-7 (Angiotensin II); U5SYW473RQ (telmisartan)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180110
[St] Status:MEDLINE
[do] DOI:10.1002/cbf.3313


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[PMID]:29194017
[Au] Autor:Abdul Manan FM; Attan N; Widodo N; Aboul-Enein HY; Wahab RA
[Ad] Endereço:a Department of Chemistry, Faculty of Science , Universiti Teknologi Malaysia , Skudai , Malaysia.
[Ti] Título:Rhizomucor miehei lipase immobilized on reinforced chitosan-chitin nanowhiskers support for synthesis of eugenyl benzoate.
[So] Source:Prep Biochem Biotechnol;48(1):92-102, 2018 Jan 02.
[Is] ISSN:1532-2297
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:An alternative environmentally benign support was prepared from chitosan-chitin nanowhiskers (CS/CNWs) for covalent immobilization of Rhizomucor miehei lipase (RML) to increase the operational stability and recyclability of RML in synthesizing eugenyl benzoate. The CS/CNWs support and RML-CS/CNWs were characterized using X-ray diffraction, fluorescent microscopy, and Fourier transform infrared spectroscopy. Efficiency of the RML-CS/CNWs was compared to the free RML to synthesize eugenyl benzoate for parameters: reaction temperature, stirring rate, reusability, and thermal stability. Under optimal experimental conditions (50°C, 250 rpm, catalyst loading 3 mg/mL), a twofold increase in yield of eugenyl benzoate was observed for RML-CS/CNWs as compared to free RML, with the former achieving maximum yield of the ester at 62.1% after 5 hr. Results demonstrated that the strategy adopted to prepare RML-CS/CNWs was useful, producing an improved and prospectively greener biocatalyst that supported a sustainable process to prepare eugenyl benzoate. Moreover, RML-CS/CNWs are biodegradable and perform esterification reactions under ambient conditions as compared to the less eco-friendly conventional acid catalyst. This research provides a facile and promising approach for improving activity of RML in which the resultant RML-CS/CNWs demonstrated good operational stability for up to eight successive esterification cycles to synthesize eugenyl benzoate.
[Mh] Termos MeSH primário: Benzoatos/metabolismo
Quitina/química
Quitosana/química
Enzimas Imobilizadas/metabolismo
Eugenol/análogos & derivados
Lipase/metabolismo
Rhizomucor/enzimologia
[Mh] Termos MeSH secundário: Benzoatos/química
Estabilidade Enzimática
Enzimas Imobilizadas/química
Esterificação
Eugenol/metabolismo
Microbiologia Industrial
Lipase/química
Nanoestruturas/química
Rhizomucor/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Enzymes, Immobilized); 1398-61-4 (Chitin); 3T8H1794QW (Eugenol); 9012-76-4 (Chitosan); EC 3.1.1.3 (Lipase)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[St] Status:MEDLINE
[do] DOI:10.1080/10826068.2017.1405021


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[PMID]:29217191
[Au] Autor:Yoshida K; Nakai A; Kaneshiro K; Hashimoto N; Suzuki K; Uchida K; Hashimoto T; Kawasaki Y; Tateishi K; Nakagawa N; Shibanuma N; Sakai Y; Hashiramoto A
[Ad] Endereço:Department of Biophysics, Kobe University Graduate School of Health Sciences, Kobe 654-0142, Japan.
[Ti] Título:TNF-α induces expression of the circadian clock gene Bmal1 via dual calcium-dependent pathways in rheumatoid synovial cells.
[So] Source:Biochem Biophys Res Commun;495(2):1675-1680, 2018 01 08.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Tumor necrosis factor (TNF)-α is responsible for expressions of several clock genes and affects joint symptoms of rheumatoid arthritis (RA) with diurnal fluctuation. We tried to determine the mechanism involved in over-expression of Bmal1, induced by TNF-α, in primary cultured rheumatoid synovial cells. Cells were incubated with intra-cellular Ca chelator BAPTA-AM, calcineurin inhibitor FK506 and p300/CBP (CREB binding protein) inhibitor C646, respectively, or transfected with p300 and CBP small interfering RNA (siRNA) before stimulation with TNF-α. Oscillation phase and amplitude of Bmal1, transcriptional activator Rorα, transcriptional repressor Rev-erbα, and histone acetyltransferases (p300 and Cbp) were evaluated by quantitative real-time PCR. As results, TNF-α did not influence the oscillation phase of Rev-erbα, while enhanced those of Rorα, resulting in over-expression of Bmal1. When Ca influx was inhibited by BAPTA-AM, TNF-α-mediated up-regulation of Rorα was cancelled, however, that of Bmal1 was still apparent. When we further explored another pathway between TNF-α and Bmal1, TNF-α suppressed the expression of Rev-erbα in the absence of Ca influx, as well as those of p300 and Cbp genes. Finally, actions of TNF-α, in increasing Bmal1/Rorα and decreasing Rev-erbα, were cancelled by C646 treatment or silencing of both p300 and Cbp. In conclusion, we determined a novel role of TNF-α in inducing Bmal1 via dual calcium dependent pathways; Rorα was up-regulated in the presence of Ca influx and Rev-erbα was down-regulated in the absence of that. Results proposed that inhibition of p300/CBP could be new therapeutic targets for RA.
[Mh] Termos MeSH primário: Fatores de Transcrição ARNTL/genética
Artrite Reumatoide/genética
Artrite Reumatoide/metabolismo
Sinalização do Cálcio
Relógios Circadianos/genética
Membrana Sinovial/metabolismo
Fator de Necrose Tumoral alfa/metabolismo
[Mh] Termos MeSH secundário: Artrite Reumatoide/patologia
Benzoatos/farmacologia
Proteína de Ligação a CREB/antagonistas & inibidores
Proteína de Ligação a CREB/genética
Quelantes de Cálcio/farmacologia
Sinalização do Cálcio/efeitos dos fármacos
Células Cultivadas
Proteína p300 Associada a E1A/antagonistas & inibidores
Proteína p300 Associada a E1A/genética
Ácido Egtázico/análogos & derivados
Ácido Egtázico/farmacologia
Expressão Gênica/efeitos dos fármacos
Seres Humanos
Membro 1 do Grupo D da Subfamília 1 de Receptores Nucleares/genética
Membro 1 do Grupo F da Subfamília 1 de Receptores Nucleares/genética
Pirazóis/farmacologia
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
RNA Interferente Pequeno/genética
Membrana Sinovial/efeitos dos fármacos
Membrana Sinovial/patologia
Fator de Necrose Tumoral alfa/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (ARNTL Transcription Factors); 0 (ARNTL protein, human); 0 (Benzoates); 0 (C646 compound); 0 (Calcium Chelating Agents); 0 (NR1D1 protein, human); 0 (Nuclear Receptor Subfamily 1, Group D, Member 1); 0 (Nuclear Receptor Subfamily 1, Group F, Member 1); 0 (Pyrazoles); 0 (RNA, Messenger); 0 (RNA, Small Interfering); 0 (RORA protein, human); 0 (Tumor Necrosis Factor-alpha); 139890-68-9 (1,2-bis(2-aminophenoxy)ethane N,N,N',N'-tetraacetic acid acetoxymethyl ester); 526U7A2651 (Egtazic Acid); EC 2.3.1.48 (CREB-Binding Protein); EC 2.3.1.48 (CREBBP protein, human); EC 2.3.1.48 (E1A-Associated p300 Protein); EC 2.3.1.48 (EP300 protein, human)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180220
[Lr] Data última revisão:
180220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171209
[St] Status:MEDLINE


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[PMID]:29306026
[Au] Autor:So EC; Wu SN; Lo YC; Su K
[Ad] Endereço:Department of Anesthesia, An Nan Hospital, China Medical University, 70965, Tainan City, Taiwan; Department of Anesthesia, China Medical University, 40447 Taichung City, Taiwan. Electronic address: d11320@mail.tmanh.org.tw.
[Ti] Título:Differential regulation of tefluthrin and telmisartan on the gating charges of I activation and inactivation as well as on resurgent and persistent I in a pituitary cell line (GH ).
[So] Source:Toxicol Lett;285:104-112, 2018 Mar 15.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Voltage-gated Na currents (I ), known to contain many components (e.g., transient, resurgent and persistent I ) with unique gating properties, are involved in the generation and propagation of action potentials in excitable cells. In this study, how tefluthrin (Tef), a synthetic pyrethoid, and telmisartan (TEL), blocker of angiotensin II receptors can perturb those components of I was investigated. The presence of either Tef or TEL increased the values of the gating charges of I involved in the activation (z ) and inactivation (z ). Tef also increased the amplitude of resurgent I (I ) or persistent I (I ) in a pituitary cell line (GH ), while TEL produced minimal effects on them. Subsequent addition of either ranolazine (a blocker of late I ) or d-limonene (a monoterpene), could reverse the changes by TEL or Tef on z or z . In SCN5A-expressing HEK293T cells, addition of Tef or TEL also increased the peak amplitude and the inactivation time constant of I which was accompanied by the increased z value of I . Taken together, the results indicated that Tef- or TEL-mediated changes in the gating kinetics of I are linked to their actions on functional activity of neurons, neuroendocrine or endocrine cells.
[Mh] Termos MeSH primário: Benzimidazóis/farmacologia
Benzoatos/farmacologia
Ciclopropanos/farmacologia
Hidrocarbonetos Fluorados/farmacologia
Ativação do Canal Iônico/efeitos dos fármacos
Somatotrofos/efeitos dos fármacos
Canais de Sódio Disparados por Voltagem/metabolismo
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Animais
Linhagem Celular Tumoral
Cicloexenos/farmacologia
Células HEK293
Seres Humanos
Canal de Sódio Disparado por Voltagem NAV1.5/genética
Canal de Sódio Disparado por Voltagem NAV1.5/metabolismo
Ranolazina/farmacologia
Ratos
Somatotrofos/metabolismo
Terpenos/farmacologia
Transfecção
Canais de Sódio Disparados por Voltagem/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzimidazoles); 0 (Benzoates); 0 (Cyclohexenes); 0 (Cyclopropanes); 0 (Hydrocarbons, Fluorinated); 0 (NAV1.5 Voltage-Gated Sodium Channel); 0 (SCN5A protein, human); 0 (Terpenes); 0 (Voltage-Gated Sodium Channels); 2HE8P42H2J (2,3,5,6-tetrafluoro-4-methylbenzyl (Z)-(1RS)-cis-3-(2-chloro-3,3,3-trifluoroprop-1-enyl)-2,2-dimethylcyclopropanecarboxylate); 9MC3I34447 (limonene); A6IEZ5M406 (Ranolazine); U5SYW473RQ (telmisartan)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180219
[Lr] Data última revisão:
180219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180107
[St] Status:MEDLINE


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[PMID]:29287783
[Au] Autor:da Silva Mansano N; Jorge IF; Chies AB; Viani GA; Spadella MA
[Ad] Endereço:Marília Medical School, Marília, São Paulo, Brazil. Electronic address: maspadella@famema.br.
[Ti] Título:Effects of telmisartan and losartan on irradiated testes.
[So] Source:Life Sci;194:157-167, 2018 Feb 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: To analyze the effects of radiation on the reproductive tissue of male Wistar rats and to evaluate whether treatment with the Ang II AT1 receptor antagonists telmisartan and losartan mitigate the dysfunctions resulting from this exposure. MAIN METHODS: Rats were randomly divided into groups: Control, Irradiated, Telmisartan, Losartan, Irradiated+Telmisartan, and Irradiated+Losartan. Single dose of 5Gy was administered directly into the scrotum, followed by treatment with telmisartan (12mg/kg/day) or losartan (34mg/kg/two times/day) for 60days. Testicular function parameters were evaluated from spermatozoa of the vas deferens. Testes were processed for histopathological and morphometric-stereological analysis. Proliferating cell nuclear antigen (PCNA) immunohistochemistry was evaluated. KEY FINDINGS: Radiation significantly reduced sperm motility, concentration, vitality, and increased the number of abnormal spermatozoa. Telmisartan and losartan did not significantly prevent these radiation-induced disorders. Seminiferous tubules were atrophied in both untreated and treated irradiated testes, and exhibited vacuoles, increased interstitial tissue and high number of blood vessels. However, several seminiferous tubules in recuperation were founded among damaged tubules in the testes of treated animals. The PCNA immunohistochemistry confirmed these outcomes. PCNA-positive cells were detected in dividing spermatogonia and spermatocytes from irradiated telmisartan and losartan treated rats whereas in the only-irradiated group, PCNA staining was observed in the nuclei of only the surviving spermatogonia. SIGNIFICANCE: Under these experimental conditions, the testicular function parameters showed that radiation produced marked damage that was not reversed by treatments. However, gonadal restructuring and recovery of spermatogenesis in treated animals may to reflect attenuation of radiation-induced damages and potential start of recovery.
[Mh] Termos MeSH primário: Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacologia
Benzimidazóis/farmacologia
Benzoatos/farmacologia
Losartan/farmacologia
Protetores contra Radiação/farmacologia
Testículo/efeitos dos fármacos
Testículo/efeitos da radiação
[Mh] Termos MeSH secundário: Animais
Masculino
Ratos Wistar
Espermatogênese/efeitos dos fármacos
Espermatogênese/efeitos da radiação
Espermatozoides/efeitos dos fármacos
Espermatozoides/patologia
Espermatozoides/efeitos da radiação
Testículo/patologia
Testículo/fisiopatologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Angiotensin II Type 1 Receptor Blockers); 0 (Benzimidazoles); 0 (Benzoates); 0 (Radiation-Protective Agents); JMS50MPO89 (Losartan); U5SYW473RQ (telmisartan)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


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[PMID]:29172661
[Au] Autor:Kovács G; Kiss C
[Ad] Endereço:II. Gyermekgyógyászati Klinika, Semmelweis Egyetem, Általános Orvostudományi Kar Budapest, Tuzoltó u. 7-9., 1094.
[Ti] Título:[Novelties in the treatment of pediatric immune thrombocytopenia - 2017].
[Ti] Título:Újdonságok a gyermekkori immunthrombocytopenia kezelésében ­ 2017..
[So] Source:Orv Hetil;158(48):1891-1896, 2017 Dec.
[Is] ISSN:0030-6002
[Cp] País de publicação:Hungary
[La] Idioma:hun
[Ab] Resumo:Immune thrombocitopenia in children is a very variable disease. International recommendations give therapeutic possibilities without strong protocols. In 2011, a therapeutic algorithm was published based on Hungarian practice. Recently, new innovative drugs have been available even in Hungary, so there is a need for modification of the therapeutic protocols. In this summary we give an overview about the current up-to-date management. In infancy and in childhood, high-dose immunglobulin treatment is recommended henceforward. In older children an alternative can be steroid therapy (pulses or long-term low-dose treatment). In resistant cases, a new thrombopoetin receptor stimulant, eltrombopag can be administered. This drug is registered in Hungary, and can very effectively influence the prognosis. Splenectomy is very rare nowadays in children. Immune thrombocytopenia is an unpredictable disease. Cure rate is about 70-80% of the cases, but management of the patients needs special care and specialist. Orv Hetil. 2017; 158(48): 1891-1896.
[Mh] Termos MeSH primário: Benzoatos/uso terapêutico
Hidrazinas/uso terapêutico
Imunoglobulinas Intravenosas/uso terapêutico
Conduta do Tratamento Medicamentoso
Púrpura Trombocitopênica Idiopática/tratamento farmacológico
Pirazóis/uso terapêutico
Esteroides/uso terapêutico
[Mh] Termos MeSH secundário: Adolescente
Criança
Pré-Escolar
Resistência a Medicamentos
Seres Humanos
Lactente
Recém-Nascido
Pediatria
Prognóstico
Púrpura Trombocitopênica Idiopática/cirurgia
Esplenectomia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Hydrazines); 0 (Immunoglobulins, Intravenous); 0 (Pyrazoles); 0 (Steroids); S56D65XJ9G (eltrombopag)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1556/650.2017.30934


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[PMID]:29322271
[Au] Autor:Stenert C; de Mello ÍCMF; Pires MM; Knauth DS; Katayama N; Maltchik L
[Ad] Endereço:Laboratory of Ecology and Conservation of Aquatic Ecosystems, UNISINOS, Unisinos Avenue, 950, São Leopoldo, RS, 93.022-750, Brazil. cstenert@unisinos.br.
[Ti] Título:Responses of macroinvertebrate communities to pesticide application in irrigated rice fields.
[So] Source:Environ Monit Assess;190(2):74, 2018 Jan 10.
[Is] ISSN:1573-2959
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The ability to recover to original states after disturbances makes macroinvertebrates useful tools for assessing the impacts of pesticides. Many studies showed that direct exposure to pesticides decreases macroinvertebrate richness and alters their composition. The main objective of this study was to assess recovery patterns in macroinvertebrate communities after pesticide application in irrigated rice fields. We analyzed short-term temporal dynamics of macroinvertebrate communities after application of the herbicides bispyribac-sodium and clomazone and the insecticide chlorantraniliprole, over the rice-growing season in southern Brazil. We selected three conventional rice fields and the recovery of macroinvertebrate communities was also compared with three adjacent natural ponds. The study was developed from November 2011 to February 2012 (rice-growing season). Five macroinvertebrate collections were carried out 3, 7, 14, 38, and 60 days after pesticide application (November 25). Rice fields showed lower richness and abundance than ponds in the period immediately after pesticide application, and recovery rates in the richness of macroinvertebrate communities were more conspicuous as pesticide residuals dissipated from the fields. Macroinvertebrate community structure in rice fields also became more similar to natural ponds as pesticide traces were scarcer. However, macroinvertebrate abundance patterns were not related to pesticide concentrations in the fields. Our results supported the general hypothesis on the negative effects of pesticide application on macroinvertebrate community in irrigated rice fields, although other environmental features (e.g., length of the flooded period) also contributed to explain temporal dynamics in the macroinvertebrate communities from irrigated rice fields.
[Mh] Termos MeSH primário: Irrigação Agrícola
Herbicidas/toxicidade
Inseticidas/toxicidade
Invertebrados/efeitos dos fármacos
Oryza
[Mh] Termos MeSH secundário: Animais
Benzoatos/análise
Benzoatos/toxicidade
Monitoramento Ambiental/métodos
Herbicidas/análise
Inseticidas/análise
Isoxazóis/análise
Isoxazóis/toxicidade
Oxazolidinonas/análise
Oxazolidinonas/toxicidade
Pirimidinas/análise
Pirimidinas/toxicidade
ortoaminobenzoatos/análise
ortoaminobenzoatos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Herbicides); 0 (Insecticides); 0 (Isoxazoles); 0 (Oxazolidinones); 0 (Pyrimidines); 0 (ortho-Aminobenzoates); 570RAC03NF (clomazone); 622AK9DH9G (chlorantranilipole); 9W20BD966G (bispyribac)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180129
[Lr] Data última revisão:
180129
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE
[do] DOI:10.1007/s10661-017-6425-1


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[PMID]:28970022
[Au] Autor:Chang J; Hao W; Xu Y; Xu P; Li W; Li J; Wang H
[Ad] Endereço:Research Center for Eco-Environmental Science, Chinese Academy of Sciences, Shuangqing RD 18, Beijing 100085, China; University of Chinese Academy of Sciences, Yuquan RD 19 a, Beijing 100049, China.
[Ti] Título:Stereoselective degradation and thyroid endocrine disruption of lambda-cyhalothrin in lizards (Eremias argus) following oral exposure.
[So] Source:Environ Pollut;232:300-309, 2018 Jan.
[Is] ISSN:1873-6424
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The disturbance of the thyroid system and elimination of chiral pyrethroid pesticides with respect to enantioselectivity in reptiles have so far received limited attention by research. In this study, bioaccumulation, thyroid gland lesions, thyroid hormone levels, and hypothalamus-pituitary-thyroid axis-related gene expression in male Eremias argus were investigated after three weeks oral administration of lambda-cyhalothrin (LCT) enantiomers. In the lizard liver, the concentration of LCT was negatively correlated with the metabolite-3-phenoxybenzoic acid (PBA) level during 21 days of exposure. (+)-LCT exposure induced a higher thyroid follicular epithelium height than (-)-LCT exposure. The thyroxine levels were increased in both treated groups while only (+)-LCT exposure induced a significant change in the triiodothyronine (T3) level. In addition, the expressions of hypothalamus-pituitary-thyroid axis-related genes including thyroid hormone receptors (trs), deiodinases (dios), uridinediphosphate glucuronosyltransferase (udp), and sulfotransferase (sult) were up-regulated after exposure to the two enantiomers. (+)-LCT treatment resulted in higher expression of trs and (-)-LCT exposure led to greater stimulation of dios in the liver, which indicated PBA-induced antagonism on thyroid hormone receptors and LCT-induced disruption of thyroxine (T4) deiodination. The results suggest the (-)-LCT exposure causes higher residual level in lizard liver while induces less disruption on lizard thyroid activity than (+)-LCT.
[Mh] Termos MeSH primário: Lagartos/fisiologia
Nitrilos/toxicidade
Praguicidas/toxicidade
Piretrinas/toxicidade
Glândula Tireoide/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Benzoatos
Disruptores Endócrinos/metabolismo
Iodeto Peroxidase/metabolismo
Fígado/metabolismo
Lagartos/metabolismo
Masculino
Praguicidas/metabolismo
Receptores dos Hormônios Tireóideos/metabolismo
Estereoisomerismo
Glândula Tireoide/metabolismo
Hormônios Tireóideos/metabolismo
Tiroxina
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzoates); 0 (Endocrine Disruptors); 0 (Nitriles); 0 (Pesticides); 0 (Pyrethrins); 0 (Receptors, Thyroid Hormone); 0 (Thyroid Hormones); 69DC2655VH (3-phenoxybenzoic acid); EC 1.11.1.8 (Iodide Peroxidase); Q51BO43MG4 (Thyroxine); V0V73PEB8M (cyhalothrin)
[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:171004
[St] Status:MEDLINE


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[PMID]:29179179
[Au] Autor:Shi R; Xiao ZT; Zheng YJ; Zhang YL; Xu JW; Huang JH; Zhou WL; Li PB; Su WW
[Ad] Endereço:Guangdong Engineering & Technology Research Center for Quality and Efficacy Re-evaluation of Post-market Traditional Chinese Medicine, School of Life Sciences, Sun Yat-sen University, Guangzhou, China.
[Ti] Título:Naringenin Regulates CFTR Activation and Expression in Airway Epithelial Cells.
[So] Source:Cell Physiol Biochem;44(3):1146-1160, 2017.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: Sputum symptoms are commonly seen in the elderly. This study aimed to identify an efficacious expectorant treatment stratagem through evaluating the secretion-promoting activation and cystic fibrosis transmembrane conductance regulator (CFTR) expression of the bioactive herbal monomer naringenin. METHODS: Vectorial Cl- transport was determined by measuring short-circuit current (ISC) in rat airway epithelium. cAMP content was measured by ELISA in primary cultured epithelial cells and Calu-3 cells. CFTR expression in Calu-3 cells was determined by qPCR. RESULTS: Addition of naringenin to the basolateral side of the rat airway led to a concentration-dependent sustained increase in ISC. The current was suppressed when exposed to Cl--free solution or by bumetanide, BaCl2, and DPC but not by DIDS and IBMX. Forskolin-induced ISC increase and CFTRinh-172/MDL-12330A-induced ISC inhibition were not altered by naringenin. Intracellular cAMP content was significantly increased by naringenin. With lipopolysaccharide stimulation, CFTR expression was significantly reduced, and naringenin dose-dependently enhanced CFTR mRNA expression. CONCLUSION: These results demonstrate that naringenin has the ability to stimulate Cl- secretion, which is mediated by CFTR through a signaling pathway by increasing cAMP content. Moreover, naringenin can increase CFTR expression when organism CFTR expression is seriously hampered. Our data suggest a potentially effective treatment strategy for sputum.
[Mh] Termos MeSH primário: Regulador de Condutância Transmembrana em Fibrose Cística/metabolismo
Células Epiteliais/efeitos dos fármacos
Flavanonas/farmacologia
[Mh] Termos MeSH secundário: Animais
Compostos de Bário/farmacologia
Benzoatos/farmacologia
Células Cultivadas
Canais de Cloreto/antagonistas & inibidores
Canais de Cloreto/metabolismo
Cloretos/farmacologia
Colforsina/farmacologia
AMP Cíclico/análise
Regulador de Condutância Transmembrana em Fibrose Cística/antagonistas & inibidores
Regulador de Condutância Transmembrana em Fibrose Cística/genética
Células Epiteliais/citologia
Células Epiteliais/metabolismo
Feminino
Seres Humanos
Iminas/farmacologia
Transporte de Íons/efeitos dos fármacos
Masculino
Microscopia de Fluorescência
Ratos
Ratos Sprague-Dawley
Reação em Cadeia da Polimerase em Tempo Real
Tiazolidinas/farmacologia
Traqueia/citologia
ortoaminobenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-((3-trifluoromethyl)phenyl)-5-((3-carboxyphenyl)methylene)-2-thioxo-4-thiazolidinone); 0 (Barium Compounds); 0 (Benzoates); 0 (Chloride Channels); 0 (Chlorides); 0 (Flavanones); 0 (Imines); 0 (Thiazolidines); 0 (ortho-Aminobenzoates); 0VK51DA1T2 (barium chloride); 126880-72-6 (Cystic Fibrosis Transmembrane Conductance Regulator); 1F7A44V6OU (Colforsin); 82985-31-7 (RMI 12330A); 952VN06WBB (fenamic acid); E0399OZS9N (Cyclic AMP); HN5425SBF2 (naringenin)
[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:171128
[St] Status:MEDLINE
[do] DOI:10.1159/000485419


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[PMID]:29178132
[Au] Autor:Zhang X; Chuai Y; Nie W; Wang A; Dai G
[Ad] Endereço:Department of Oncology, Chinese PLA General Hospital, Beijing, China.
[Ti] Título:Thrombopoietin receptor agonists for prevention and treatment of chemotherapy-induced thrombocytopenia in patients with solid tumours.
[So] Source:Cochrane Database Syst Rev;11:CD012035, 2017 11 27.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Chemotherapy-induced thrombocytopenia (CIT) is defined as a peripheral platelet count less than 100×10 /L, with or without bleeding in cancer patients receiving myelosuppressive chemotherapy. CIT is a significant medical problem during chemotherapy, and it carries the risk of sub-optimal overall survival and bleeding. Alternative interventions to platelet transfusion are limited. Different stages of preclinical and clinical studies have examined the thrombopoietin receptor agonists (TPO-RAs) for CIT in patients with solid tumours. OBJECTIVES: To assess the effects of TPO-RAs to prevent and treat CIT in patients with solid tumours:(1) to prevent CIT in patients without thrombocytopenia before chemotherapy, (2) to prevent recurrence of CIT, and (3) to treat CIT in patients with thrombocytopenia during chemotherapy. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL, to 28 September 2017), MEDLINE (from 1950 to 28 September 2017), as well as online registers of ongoing trials (Clinical Trials, Chinese Clinical Trial Register, Australian New Zealand Clinical Trial Registry, WHO ICTRP Search Portal, International Standard Randomised Controlled Trial Number registry, GlaxoSmithKline Clinical Study Register, and Amgen Clinical Trials) and conference proceedings (American Society of Hematology, American Society of Clinical Oncology, European Hematology Association, European Society of Medical Oncology, and Conference Proceedings Citation Index-Science, from 2002 up to September 2017) for studies. SELECTION CRITERIA: Randomised controlled trials (RCTs) comparing TPO-RAs alone, or in combination with other drugs, to placebo, no treatment, other drugs, or another TPO-RAs for CIT in patients with solid tumours. DATA COLLECTION AND ANALYSIS: Two review authors independently screened the results of the search strategies, extracted data, assessed risk of bias, and analysed data according to standard methodological methods expected by Cochrane. MAIN RESULTS: We identified six trials eligible for inclusion, of which two are ongoing, and one awaiting classification study. The three included trials were conducted at many different sites in Europe, America, and Asia. All of the three studies recruited adult and elder participants (no children were included) with solid tumours, and compared TPO-RAs with placebo. No studies compared TPO-RAs alone, or in combination with other drugs, to no treatment, or other drugs, or another TPO-RAs.We judged the overall risk of bias as high as we found a high risk for detection bias. We assessed the risk of bias arising from inadequate blinding of outcome assessors as high for number and severity of bleeding episodes (one of the primary outcomes).To prevent CIT: We included two trials (206 participants) comparing TPO-RAs (eltrombopag, multiple-dose oral administration with chemotherapy) with placebo. The use of TPO-RAs may make little or no difference to the all-cause mortality at 33 weeks of follow-up (RR 1.35, 95% CI 0.53 to 3.45; one trial, 26 participants; low quality of evidence). There is not enough evidence to determine whether TPO-RAs reduce the number of patients with at least one bleeding episode of any severity (RR 0.62, 95% CI 0.22 to 1.78; two trials, 206 participants; very low quality of evidence). There is not enough evidence to determine whether TPO-RAs reduce the number of patients with at least one severe/life-threatening bleeding episode (RR 0.36, 95% CI 0.06 to 2.06; two trials, 206 participants; very low quality of evidence). No studies were found that looked at overall survival (one of the primary outcomes), the number of treatment cycles with at least one bleeding episode, the number of days on which bleeding occurred, the amount of bleeding, or quality of life.To prevent recurrence of CIT: We included one trial (62 participants) comparing TPO-RAs (romiplostim, single-dose subcutaneous administration with chemotherapy) with placebo. There is not enough evidence to determine whether TPO-RAs reduce the number of patients with at least one bleeding episode of any severity (RR 2.80, 95% CI 0.17 to 47.53; one trial, 62 participants; very low quality of evidence). There is not enough evidence to determine whether TPO-RAs reduce the number of patients with at least one severe/life-threatening bleeding episode (no severe/life-threatening bleeding episodes; one trial, 62 participants; very low quality of evidence). No studies were found that looked at overall survival (one of the primary outcomes), the number of treatment cycles with at least one bleeding episode, the number of days on which bleeding occurred, the amount of bleeding, or quality of life. We found one ongoing study (expected recruitment 74 participants), it is planned to give TPO-RAs (romiplostim, subcutaneous administration with chemotherapy) to participants, but to date this trial has not reported any outcomes.To treat CIT: We found one ongoing study (expected recruitment 83 participants), which is planned to give TPO-RAs (eltrombopag, seven days orally) to participants when their platelet counts are less than 75×10 /L during chemotherapy. This trial was originally planned to complete in March 2017, however, the completion date has passed and no results are reported.The one awaiting classification study included patients without thrombocytopenia before chemotherapy (to prevent CIT), patients with thrombocytopenia during chemotherapy (to prevent recurrence of CIT), and other patients during chemotherapy (uncertain whether CIT had happened). There was no evidence for a difference in the number of patients with at least one bleeding episode of any severity (RR 0.27, 95% CI 0.07 to 1.02; one trial, 75 participants). There was no evidence for a difference in the number of patients with at least one severe/life-threatening bleeding episode (RR 0.44, 95% CI 0.03 to 6.77; one trial, 75 participants). This study did not address overall survival or quality of life. AUTHORS' CONCLUSIONS: No certain conclusions can be drawn due to the lack of strong evidence in the review. The available weak evidence did not support the use of TPO-RAs for preventing CIT or preventing recurrence of CIT in patients with solid tumours. There was no evidence to support the use of TPO-RAs for treating CIT in patients with solid tumours.
[Mh] Termos MeSH primário: Antineoplásicos/efeitos adversos
Benzoatos/administração & dosagem
Hidrazinas/administração & dosagem
Pirazóis/administração & dosagem
Receptores Fc/administração & dosagem
Receptores de Trombopoetina/agonistas
Proteínas Recombinantes de Fusão/administração & dosagem
Trombocitopenia/tratamento farmacológico
Trombocitopenia/prevenção & controle
Trombopoetina/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Seres Humanos
Meia-Idade
Neoplasias/tratamento farmacológico
Ensaios Clínicos Controlados Aleatórios como Assunto
Trombocitopenia/induzido quimicamente
Trombocitopenia/mortalidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzoates); 0 (Hydrazines); 0 (Pyrazoles); 0 (Receptors, Fc); 0 (Receptors, Thrombopoietin); 0 (Recombinant Fusion Proteins); 9014-42-0 (Thrombopoietin); GN5XU2DXKV (romiplostim); S56D65XJ9G (eltrombopag)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180111
[Lr] Data última revisão:
180111
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD012035.pub2



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