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[PMID]:28741868
[Au] Autor:Tanaka T; Ueno M; Nakashima Y; Chinen S; Sato E; Masaki M; Mogi A; Sasaki H; Tamura K; Takamatsu Y
[Ad] Endereço:Division of Oncology, Hematology, and Infectious Diseases, Department of Internal Medicine, Fukuoka University Hospital, Fukuoka, Japan.
[Ti] Título:Retrospective analysis of the efficacy and safety of eribulin therapy for metastatic breast cancer in daily practice.
[So] Source:Thorac Cancer;8(5):523-529, 2017 Sep.
[Is] ISSN:1759-7714
[Cp] País de publicação:Singapore
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Evidence of eribulin therapy for metastatic breast cancer (MBC) in clinical practice is not well documented. METHODS: We retrospectively analyzed the safety and efficacy of eribulin in 29 MBC patients from 2011 to 2016 at Fukuoka University Hospital. RESULTS: The median patient age, number of courses, total dose, and relative dose intensity were as follows: 65 years, five courses, 8.6 mg/m , and 75%, respectively. One patient achieved a complete response, (CR) six a partial response (PR), eight stable disease (SD) and 14 patients exhibited progressive disease. The objective response rate (ORR: CR + PR) was 24.1%, and the clinical benefit rate (CBR: CR + PR + SD) was 51.7%. The median progression-free survival was 90 days (95% confidence interval [CI] 67-126) and median overall survival was 264 days (95% CI 198-357). In patients who previously received 2-4 regimens, the ORR was 28.5% and the CBR was 57.1%. In patients who received 5-12 regimens, the ORR was 20% and the CBR was 45%. Chemotherapy was administered to 20 patients (69%) after eribulin administration, and the median overall survival rate of cases that achieved greater than a PR was 1088 days. The most frequent treatment-related grade 3/4 adverse events were neutropenia (55.2%), and febrile neutropenia (20.1%). Grade 3 peripheral neuropathy occurred in 13.8% of patients, but was not exacerbated even if present before treatment. CONCLUSION: Eribulin is effective for MBC patients who have received multiple chemotherapies. Neutropenia and febrile neutropenia may develop after heavy prior therapy.
[Mh] Termos MeSH primário: Antineoplásicos/administração & dosagem
Neoplasias da Mama/tratamento farmacológico
Furanos/administração & dosagem
Cetonas/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Antineoplásicos/efeitos adversos
Intervalo Livre de Doença
Esquema de Medicação
Feminino
Furanos/efeitos adversos
Seres Humanos
Cetonas/efeitos adversos
Meia-Idade
Metástase Neoplásica
Estudos Retrospectivos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Furans); 0 (Ketones); LR24G6354G (eribulin)
[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:170726
[St] Status:MEDLINE
[do] DOI:10.1111/1759-7714.12482


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[PMID]:28826029
[Au] Autor:Masondo NA; Kulkarni MG; Finnie JF; Van Staden J
[Ad] Endereço:Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal, Pietermaritzburg Campus, Private Bag X01, Scottsville 3209, South Africa.
[Ti] Título:Influence of biostimulants-seed-priming on Ceratotheca triloba germination and seedling growth under low temperatures, low osmotic potential and salinity stress.
[So] Source:Ecotoxicol Environ Saf;147:43-48, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Extreme temperatures, drought and salinity stress adversely affect seed germination and seedling growth in crop species. Seed priming has been recognized as an indispensable technique in the production of stress-tolerant plants. Seed priming increases seed water content, improves protein synthesis using mRNA and DNA and repair mitochondria in seeds prior to germination. The current study aimed to determine the role of biostimulants-seed-priming during germination and seedling growth of Ceratotheca triloba (Bernh.) Hook.f. (an indigenous African leafy vegetable) under low temperature, low osmotic potential and salinity stress conditions. Ceratotheca triloba seeds were primed with biostimulants [smoke-water (SW), synthesized smoke-compound karrikinolide (KAR ), Kelpak (commercial seaweed extract), phloroglucinol (PG) and distilled water (control)] for 48h at 25°C. Thereafter, primed seeds were germinated at low temperatures, low osmotic potential and high NaCl concentrations. Low temperature (10°C) completely inhibited seed germination. However, temperature shift to 15°C improved germination. Smoke-water and KAR enhanced seed germination with SW improving seedling growth under different stress conditions. Furthermore, priming seeds with Kelpak stimulated percentage germination, while PG and the control treatment improved seedling growth at different PEG and NaCl concentrations. Generally, high concentrations of PEG and NaCl brought about detrimental effects on seed germination and seedling growth. Findings from this study show the potential role of seed priming with biostimulants in the alleviation of abiotic stress conditions during seed germination and seedling growth in C. triloba plants.
[Mh] Termos MeSH primário: Furanos/farmacologia
Germinação/efeitos dos fármacos
Pedaliaceae/efeitos dos fármacos
Piranos/farmacologia
Plântulas/efeitos dos fármacos
Sementes/efeitos dos fármacos
Estresse Fisiológico/efeitos dos fármacos
[Mh] Termos MeSH secundário: Temperatura Baixa
Secas
Osmose
Pedaliaceae/crescimento & desenvolvimento
Salinidade
Plântulas/crescimento & desenvolvimento
África do Sul
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Furans); 0 (Pyrans); 0 (karrikinolide)
[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:170822
[St] Status:MEDLINE


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[PMID]:29355908
[Au] Autor:Xiao Y; Luo M; Wang J; Luo H
[Ad] Endereço:Department of Neurology, The First Affiliated Hospital, Guangxi Medical University, No. 22, Shuang Yong Lu, Nanning, Guangxi, China, 530021.
[Ti] Título:Losigamone add-on therapy for focal epilepsy.
[So] Source:Cochrane Database Syst Rev;1:CD009324, 2018 01 22.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Epilepsy is a common neurologic disorder, affecting approximately 50 million people worldwide; nearly a third of these people have epilepsy that is not well controlled by a single antiepileptic drug (AED) and they usually require treatment with a combination of two or more AEDs. In recent years, many newer AEDs have been investigated as add-on therapy for focal epilepsy; losigamone is one of these drugs and is the focus of this systematic review. This is an update of a Cochrane review first published in 2012 (Cochrane Database of Systematic Reviews 2012, Issue 6) and updated in 2015. OBJECTIVES: To investigate the efficacy and safety of losigamone when used as an add-on therapy for focal epilepsy. SEARCH METHODS: For the latest update on 9 February 2017, we searched the Cochrane Epilepsy Specialized Register, CENTRAL and MEDLINE . We searched trials registers and contacted the manufacturer of losigamone and authors of included studies for additional information. We did not impose any language restrictions. SELECTION CRITERIA: Randomized controlled, add-on trials comparing losigamone with placebo for focal epilepsy. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trial quality and extracted data. The primary outcomes were 50% or greater reduction in seizure frequency and seizure freedom; the secondary outcomes were treatment withdrawal and adverse events. Results are presented as risk ratios (RRs) with 95% confidence intervals (CIs) or 99% CIs (for the individual listed adverse events to make an allowance for multiple testing). MAIN RESULTS: Two trials involving a total of 467 participants, aged over 18 years, were eligible for inclusion. Both trials assessed losigamone 1200 mg/day or 1500 mg/day as an add-on therapy for focal epilepsy. We assessed one trial as being of good methodological quality while the other was of uncertain quality. For the efficacy outcomes, results did show that participants taking losigamone were significantly more likely to achieve a 50% or greater reduction in seizure frequency (RR 1.76, 95% CI 1.14 to 2.72), but associated with a significant increase of treatment withdrawal when compared with those taking placebo (RR 2.16, 95% CI 1.28 to 3.67). For the safety outcomes, results indicated that the proportion of participants who experienced adverse events in the losigamone group was higher than in the placebo group (RR 1.34, 95% CI 1.00 to 1.80), dizziness was the only adverse event significantly reported in relation to losigamone (RR 3.82, 99% CI 1.69 to 8.64). The proportion of participants achieving seizure freedom was not reported in either trial report. A subgroup analysis according to different doses of losigamone showed that a higher dose of losigamone (1500 mg/day) was associated with a greater reduction in seizure frequency than lower doses, but was also associated with more dropouts due to adverse events. AUTHORS' CONCLUSIONS: The results of this review showed that losigamone did reduce seizure frequency but was associated with more treatment withdrawals when used as an add-on therapy for people with focal epilepsy. However, the included trials were of short-term duration and uncertain quality. Future well-designed randomized, double-blind, placebo-controlled trials with a longer-term duration are needed. No new studies have been found since the last version of this review. We judged the overall quality of the evidence for the outcomes assessed as moderate.
[Mh] Termos MeSH primário: Anticonvulsivantes/uso terapêutico
Epilepsias Parciais/tratamento farmacológico
Furanos/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Anticonvulsivantes/efeitos adversos
Quimioterapia Combinada/métodos
Seres Humanos
Meia-Idade
Pacientes Desistentes do Tratamento/estatística & dados numéricos
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Anticonvulsants); 0 (Furans); 84R8O3QM2G (losigame)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180123
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD009324.pub4


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[PMID]:28456568
[Au] Autor:Yin J; Zhu F; Hao W; Xu Q; Chang J; Wang H; Guo B
[Ad] Endereço:Key Laboratory of Environmental Biotechnology, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing 100085, China; University of Chinese Academy of Sciences, Beijing 100049, China.
[Ti] Título:Acylamino acid chiral fungicides on toxiciepigenetics in lambda DNA methylation.
[So] Source:Food Chem Toxicol;109(Pt 1):735-745, 2017 Nov.
[Is] ISSN:1873-6351
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Acylamino acid chiral fungicides (AACFs) are low-toxicity pesticides and considered as non-carcinogenic chemicals to laboratory animals. Though AACFs have potential toxicological effects on mammals by non-genotoxic mechanisms, the toxicoepigenomics of AACFs has not been documented. In this article, we explored toxiciepigenetics of metalaxyl, benalaxyl and furalaxyl through epigenetics research on lambda DNA under different concentration exposure. The toxicoepigenomic difference of stereoisomers was examined also. Our results showed that AACFs would affect methyltransferase activity resulting in modulating DNA methylation levels and pattern. The LOAEL of R-metalaxyl and S-metalaxyl were 30 mM and 0.3 mM, respectively. The LOAEL of (R, S)-benalaxyl and (R, S)-furalaxyl were 0.3 Mm and 30 mM, respectively. A significant dose-response effect between (R, S)-benalaxyl and global methylation level was observed. Global methylation level was more susceptible to S-enantiomer compared to R-enantiomer, which indicated enantiomers of AACFs have the enantioselectivity in toxiciepigenetics. Moreover, the dependence of the methylation inhibition on the chiral center of metalaxyl may suggest a considerable specificity of the compound of AACFs for DNA methyltransferases. The inhibition effect between R-enantiomer and S-enantiomer of AACFs on DNA methylation levels generated in this study is important for low-toxicity pesticides toxicoepigenomics evaluation.
[Mh] Termos MeSH primário: Bacteriófago lambda/efeitos dos fármacos
Fungicidas Industriais/toxicidade
[Mh] Termos MeSH secundário: Alanina/análogos & derivados
Alanina/toxicidade
Bacteriófago lambda/genética
Bacteriófago lambda/metabolismo
Metilação de DNA/efeitos dos fármacos
DNA Viral/genética
DNA Viral/metabolismo
Epigenômica
Furanos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (DNA, Viral); 0 (Fungicides, Industrial); 0 (Furans); 0 (furalaxyl); 16K4M187IF (metalaxyl); 18TH6NY90J (benalaxyl); OF5P57N2ZX (Alanine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170501
[St] Status:MEDLINE


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[PMID]:29317250
[Au] Autor:Park SH; Cho JY; Oh SW; Kang M; Lee SE; Yoo JA; Jung K; Lee J; Lee SY; Lee J
[Ad] Endereço:Department of Bio and Chemical Engineering, Hongik University, 300-16 Sejong City, Republic of Korea.
[Ti] Título:Arctigenin protects against ultraviolet-A-induced damage to stemness through inhibition of the NF-κB/MAPK pathway.
[So] Source:Chem Biol Interact;282:63-68, 2018 Feb 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:The stemness of stem cells is negatively affected by ultraviolet A (UVA) irradiation. This study was performed to examine the effects of arctigenin on UVA-irradiation-induced damage to the stemness of human mesenchymal stem cells (hMSCs) derived from adipose tissue. The mechanisms of action of arctigenin were also investigated. A BrdU-incorporation assay demonstrated that arctigenin attenuated the UVA-induced reduction of the cellular proliferative potential. Arctigenin also increased the UVA-induced reduction in stemness of hMSCs by upregulating stemness-related genes such as SOX2, OCT4, and NANOG. In addition, the UVA-induced reduction in the mRNA expression level of hypoxia-inducible factor (HIF)-1α was significantly recovered by arctigenin. The antagonizing effect of arctigenin on UVA irradiation was mediated by reduced PGE production through the inhibition of MAPKs (p42/44 MAPK, p38 MAPK, and JNK) and NF-κB. Overall, these findings suggest that arctigenin can ameliorate the reduced stemness of hMSCs induced by UVA irradiation. The effects of arctigenin are mediated by PGE -cAMP signaling-dependent upregulation of HIF-1α. Therefore, arctigenin could be used as an antagonist to attenuate the effects of UVA irradiation.
[Mh] Termos MeSH primário: Furanos/farmacologia
Lignanas/farmacologia
Células Mesenquimais Estromais/efeitos dos fármacos
Proteínas Quinases Ativadas por Mitógeno/metabolismo
NF-kappa B/metabolismo
Substâncias Protetoras/farmacologia
Transdução de Sinais/efeitos dos fármacos
Raios Ultravioleta/efeitos adversos
[Mh] Termos MeSH secundário: Proliferação Celular/efeitos dos fármacos
Células Cultivadas
AMP Cíclico/metabolismo
Dinoprostona/metabolismo
Seres Humanos
Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo
Células Mesenquimais Estromais/metabolismo
Proteína Homeobox Nanog/metabolismo
Fator 3 de Transcrição de Octâmero/metabolismo
RNA Mensageiro/metabolismo
Fatores de Transcrição SOXB1/metabolismo
Regulação para Cima/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Furans); 0 (Hypoxia-Inducible Factor 1, alpha Subunit); 0 (Lignans); 0 (NF-kappa B); 0 (Nanog Homeobox Protein); 0 (Octamer Transcription Factor-3); 0 (Protective Agents); 0 (RNA, Messenger); 0 (SOXB1 Transcription Factors); E0399OZS9N (Cyclic AMP); EC 2.7.11.24 (Mitogen-Activated Protein Kinases); K7Q1JQR04M (Dinoprostone); U76MR9VS6M (arctigenin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180209
[Lr] Data última revisão:
180209
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE


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[PMID]:29201297
[Au] Autor:Lee M; Yoo J; Kim JG; Kyung HS; Bin SI; Kang SB; Choi CH; Moon YW; Kim YM; Han SB; In Y; Choi CH; Kim J; Lee BK; Cho S
[Ad] Endereço:Department of Orthopedic Surgery, Seoul National University Hospital, Seoul, Korea.
[Ti] Título:A Randomized, Multicenter, Phase III Trial to Evaluate the Efficacy and Safety of Polmacoxib Compared with Celecoxib and Placebo for Patients with Osteoarthritis.
[So] Source:Clin Orthop Surg;9(4):439-457, 2017 Dec.
[Is] ISSN:2005-4408
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:Background: The aim of this study was to evaluate the safety and analgesic efficacy of polmacoxib 2 mg versus placebo in a superiority comparison or versus celecoxib 200 mg in a noninferiority comparison in patients with osteoarthritis (OA). Methods: This study was a 6-week, phase III, randomized, double-blind, and parallel-group trial followed by an 18-week, single arm, open-label extension. Of the 441 patients with knee or hip OA screened, 362 were randomized; 324 completed 6 weeks of treatment and 220 completed the extension. Patients were randomized to receive oral polmacoxib 2 mg (n = 146), celecoxib 200 mg (n = 145), or placebo (n = 71) once daily for 6 weeks. During the extension, all participants received open-label polmacoxib 2 mg. The primary endpoint was the change in Western Ontario and McMaster Universities (WOMAC)-pain subscale score from baseline to week 6. Secondary endpoints included WOMAC-OA Index, OA subscales (pain, stiffness, and physical function) and Physician's and Subject's Global Assessments at weeks 3 and 6. Other outcome measures included adverse events (AEs), laboratory tests, vital signs, electrocardiograms, and physical examinations. Results: After 6 weeks, the polmacoxib-placebo treatment difference was -2.5 (95% confidence interval [CI], -4.4 to -0.6; = 0.011) and the polmacoxib-celecoxib treatment difference was 0.6 (CI, -0.9 to 2.2; = 0.425). According to Physician's Global Assessments, more subjects were "much improved" at week 3 with polmacoxib than with celecoxib or placebo. Gastrointestinal and general disorder AEs occurred with a greater frequency with polmacoxib or celecoxib than with placebo. Conclusions: Polmacoxib 2 mg was relatively well tolerated and demonstrated efficacy superior to placebo and noninferior to celecoxib after 6 weeks of treatment in patients with OA. The results obtained during the 18-week trial extension with polmacoxib 2 mg were consistent with those observed during the 6-week treatment period, indicating that polmacoxib can be considered safe for long-term use based on this relatively small scale of study in a Korean population. More importantly, the results of this study showed that polmacoxib has the potential to be used as a pain relief drug with reduced gastrointestinal side effects compared to traditional nonsteroidal anti-inflammatory drugs for OA.
[Mh] Termos MeSH primário: Celecoxib/uso terapêutico
Inibidores de Ciclo-Oxigenase 2/uso terapêutico
Furanos/uso terapêutico
Dor Musculoesquelética/tratamento farmacológico
Osteoartrite do Quadril/tratamento farmacológico
Osteoartrite do Joelho/tratamento farmacológico
Sulfonamidas/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Celecoxib/efeitos adversos
Inibidores de Ciclo-Oxigenase 2/efeitos adversos
Método Duplo-Cego
Feminino
Furanos/efeitos adversos
Gastroenteropatias/induzido quimicamente
Seres Humanos
Masculino
Meia-Idade
Dor Musculoesquelética/etiologia
Osteoartrite do Quadril/complicações
Osteoartrite do Quadril/fisiopatologia
Osteoartrite do Joelho/complicações
Osteoartrite do Joelho/fisiopatologia
Amplitude de Movimento Articular
Sulfonamidas/efeitos adversos
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE III; COMPARATIVE STUDY; EQUIVALENCE TRIAL; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (CG100649); 0 (Cyclooxygenase 2 Inhibitors); 0 (Furans); 0 (Sulfonamides); JCX84Q7J1L (Celecoxib)
[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:171205
[St] Status:MEDLINE
[do] DOI:10.4055/cios.2017.9.4.439


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[PMID]:28468305
[Au] Autor:Kim JH; Kwon SS; Jeong HU; Lee HS
[Ad] Endereço:Drug Metabolism and Bioanalysis Laboratory, College of Pharmacy, The Catholic University of Korea, Bucheon 420-743, Korea. jhyunkim@catholic.ac.kr.
[Ti] Título:Inhibitory Effects of Dimethyllirioresinol, Epimagnolin A, Eudesmin, Fargesin, and Magnolin on Cytochrome P450 Enzyme Activities in Human Liver Microsomes.
[So] Source:Int J Mol Sci;18(5), 2017 May 01.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Magnolin, epimagnolin A, dimethyllirioresinol, eudesmin, and fargesin are pharmacologically active tetrahydrofurofuranoid lignans found in Flos Magnoliae. The inhibitory potentials of dimethyllirioresinol, epimagnolin A, eudesmin, fargesin, and magnolin on eight major human cytochrome P450 (CYP) enzyme activities in human liver microsomes were evaluated using liquid chromatography-tandem mass spectrometry to determine the inhibition mechanisms and inhibition potency. Fargesin inhibited CYP2C9-catalyzed diclofenac 4'-hydroxylation with a Ki value of 16.3 µM, and it exhibited mechanism-based inhibition of CYP2C19-catalyzed [S]-mephenytoin 4'-hydroxylation (Ki, 3.7 µM; kinact, 0.102 min-1), CYP2C8-catalyzed amodiaquine N-deethylation (Ki, 10.7 µM; kinact, 0.082 min-1), and CYP3A4-catalyzed midazolam 1'-hydroxylation (Ki, 23.0 µM; kinact, 0.050 min-1) in human liver microsomes. Fargesin negligibly inhibited CYP1A2-catalyzed phenacetin O-deethylation, CYP2A6-catalyzed coumarin 7-hydroxylation, CYP2B6-catalyzed bupropion hydroxylation, and CYP2D6-catalyzed bufuralol 1'-hydroxylation at 100 µM in human liver microsomes. Dimethyllirioresinol weakly inhibited CYP2C19 and CYP2C8 with IC50 values of 55.1 and 85.0 µM, respectively, without inhibition of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, and CYP3A4 activities at 100 µM. Epimagnolin A, eudesmin, and magnolin showed no the reversible and time-dependent inhibition of eight major CYP activities at 100 µM in human liver microsomes. These in vitro results suggest that it is necessary to investigate the potentials of in vivo fargesin-drug interaction with CYP2C8, CYP2C9, CYP2C19, and CYP3A4 substrates.
[Mh] Termos MeSH primário: Benzodioxóis/farmacologia
Inibidores das Enzimas do Citocromo P-450/farmacocinética
Furanos/farmacologia
Lignanas/farmacocinética
Microssomos Hepáticos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Sistema Enzimático do Citocromo P-450/metabolismo
Seres Humanos
Lignanas/química
Lignanas/farmacologia
Microssomos Hepáticos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzodioxoles); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Furans); 0 (Lignans); 31008-18-1 (magnolin); 526-06-7 (eudesmin); 9035-51-2 (Cytochrome P-450 Enzyme System); GR9853GI71 (fargesin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180202
[Lr] Data última revisão:
180202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE


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[PMID]:29247642
[Au] Autor:Paul D; Gopal J; Kumar M; Manikandan M
[Ad] Endereço:Environmental Microbiology, Department of Environmental Engineering, Konkuk University, Seoul 143-701, South Korea. Electronic address: dibypaul@konkuk.ac.kr.
[Ti] Título:Nature to the natural rescue: Silencing microbial chats.
[So] Source:Chem Biol Interact;280:86-98, 2018 Jan 25.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Communication is the sole means by which effective networking and co-existence is accomplished amongst living beings. Microbes have their own chit-chats. Science has overheard these microbial gossips and have concluded that these aren't just informal communications, but carefully coordinated signals that plan their effective strategies. Tracking one such signal molecule, N-acyl homoserine lactone (AHL), led to a fundamental understanding to microbial quorum sensing (QS). Furtherance of research sought for ways to cut off communication between these virulent forms, so as to hinder their combinatorial attacks through quorum sensing inhibitors (QSIs). A clear understanding of the inhibitors of these microbial communication systems is vital to destroy their networking and co-working. The current review, consolidates the solutions for QSIs offered from natural sources against these micro components, that are capable of slaughtering even nature's most fit entity-man. The applications of effective out sourcing of this QSI technologies and the need for development are discussed. The importance of silencing this microbial chatter to various aspects of human life and their implications are discussed and elaborated.
[Mh] Termos MeSH primário: 4-Butirolactona/análogos & derivados
Bactérias/metabolismo
[Mh] Termos MeSH secundário: 4-Butirolactona/metabolismo
Produtos Biológicos/farmacologia
Furanos/química
Furanos/farmacologia
Bactérias Gram-Negativas/metabolismo
Bactérias Gram-Positivas/metabolismo
Plantas/química
Plantas/metabolismo
Percepção de Quorum/efeitos dos fármacos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Biological Products); 0 (Furans); 1192-20-7 (homoserine lactone); OL659KIY4X (4-Butyrolactone)
[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:171217
[St] Status:MEDLINE


  9 / 11459 MEDLINE  
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[PMID]:29277801
[Au] Autor:Kashiwagi S; Asano Y; Goto W; Takada K; Takahashi K; Hatano T; Tanaka S; Takashima T; Tomita S; Motomura H; Ohsawa M; Hirakawa K; Ohira M
[Ad] Endereço:Department of Surgical Oncology, Osaka City University Graduate School of Medicine, Osaka, Japan spqv9ke9@view.ocn.ne.jp.
[Ti] Título:Mesenchymal-epithelial Transition and Tumor Vascular Remodeling in Eribulin Chemotherapy for Breast Cancer.
[So] Source:Anticancer Res;38(1):401-410, 2018 01.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: Eribulin mesylate (eribulin) is currently used for the treatment of locally advanced or metastatic breast cancer (MBC). It is a cytotoxic agent with unique mechanisms that suppress the epithelial-mesenchymal transition (EMT) of cancer cells and promote tumor vascular remodeling. In this study, we investigated the expression of markers for EMT and hypoxia in sets of clinical specimens collected before and after eribulin treatment to verify its unique mechanisms. PATIENTS AND METHODS: The expression of markers for EMT and cellular hypoxia [E-cadherin, N-cadherin, vimentin, and carbonic anhydrase 9 (CA9)] was examined immunohistochemically in MBC tissues collected from 20 patients before and after chemotherapy with either eribulin (n=10) or paclitaxel (n=10). RESULTS: An increase of E-cadherin and decrease of CA9 expression were observed in MBC tissues from patients with objective clinical responses to eribulin treatment. Patients with E-cadherin-positive conversion and CA9-negative conversion had significantly higher response rates (p=0.004 and p=0.024, respectively) and prolonged time to treatment failure (p=0.018 and p=0.038, respectively) than patients without changes in marker expression. CONCLUSION: Expression of EMT and hypoxia markers in clinical samples from patients with MBC was suppressed by eribulin treatment. The results provide additional clinical data on improved survival of patients treated with eribulin and the mechanism of response.
[Mh] Termos MeSH primário: Antineoplásicos/uso terapêutico
Transição Epitelial-Mesenquimal/efeitos dos fármacos
Furanos/uso terapêutico
Cetonas/uso terapêutico
Paclitaxel/uso terapêutico
Neoplasias de Mama Triplo Negativas/tratamento farmacológico
Remodelação Vascular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/metabolismo
Biomarcadores Tumorais/metabolismo
Caderinas/metabolismo
Anidrase Carbônica IX/metabolismo
Hipóxia Celular/efeitos dos fármacos
Feminino
Seres Humanos
Meia-Idade
Estudos Retrospectivos
Neoplasias de Mama Triplo Negativas/patologia
Vimentina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Antineoplastic Agents); 0 (Biomarkers, Tumor); 0 (Cadherins); 0 (Furans); 0 (Ketones); 0 (Vimentin); EC 4.2.1.1 (CA9 protein, human); EC 4.2.1.1 (Carbonic Anhydrase IX); LR24G6354G (eribulin); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180104
[Lr] Data última revisão:
180104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171227
[St] Status:MEDLINE


  10 / 11459 MEDLINE  
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[PMID]:29223099
[Au] Autor:Horký P; Vorácová M; Konecná K; Sedlák D; Bartunek P; Vacek J; Kunes J; Pour M
[Ad] Endereço:Department of Bioorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
[Ti] Título:Nontoxic combretafuranone analogues with high in vitro antibacterial activity.
[So] Source:Eur J Med Chem;143:843-853, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A library of thirty two 3,4-diphenylfuranones related to both combretastatin A-4 and antifungal 5-(acyloxymethyl)-3-(halophenyl)-2,5-dihydrofuran-2-ones was prepared. Cytotoxic effects on a panel of cancer and normal cell lines and antiinfective activity were evaluated, and the data were complemented with tests for the activation of caspase 3 and 7. High cytotoxicity was observed in some of the halogenated analogues, eg. 3-(3,4-dichlorophenyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one with IC 0.12-0.23 µM, but the compounds were also highly toxic against non-malignant control cells. More importantly, notable antibacterial activity indicating G selectivity has been found in the 3,4-diarylfuranone class of compounds for the first time. Hydroxymethylation of furanone C5 knocked out cytotoxic effects (up to 40 µM) while maintaining significant activity against Staphylococcus strains in some derivatives. MIC of the most promising compound, 3-(4-bromophenyl)-5,5-bis(hydroxymethyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one against S. aureus strain ATCC 6538 was 0.98 µM (0.38 µg/mL) and 3.9 µM (1.52 µg/mL) after 24 and 48 h, respectively.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antifúngicos/farmacologia
Bactérias/efeitos dos fármacos
Fungos/efeitos dos fármacos
Furanos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Antifúngicos/síntese química
Antifúngicos/química
Apoptose/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Células Cultivadas
Relação Dose-Resposta a Droga
Furanos/síntese química
Furanos/química
Seres Humanos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antifungal Agents); 0 (Furans)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171210
[St] Status:MEDLINE



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