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Pesquisa : B01.650.940.800.575.912.250.859.500.750.199 [Categoria DeCS]
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[PMID]:28666142
[Au] Autor:Callies O; Núñez MJ; Perestelo NR; Reyes CP; Torres-Romero D; Jiménez IA; Bazzocchi IL
[Ad] Endereço:Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain.
[Ti] Título:Distinct sesquiterpene pyridine alkaloids from in Salvadoran and Peruvian Celastraceae species.
[So] Source:Phytochemistry;142:21-29, 2017 Oct.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:As part of a bioprospecting program aimed at the discovery of undescribed natural products from Salvadoran and Peruvian flora, the phytochemical investigations of four Celastraceae species, Celastrus vulcanicola, Maytenus segoviarum, Maytenus jeslkii, and Maytenus cuzcoina, were performed. The current study reports the isolation and structural characterization of five previously undescribed macrolide sesquiterpene pyridine alkaloids, named vulcanicoline-A, cuzcoinine, vulcanicoline-B, jelskiine, and vulcanicoline-C, along with sixteen known alkaloids. The structures of the alkaloids were established by spectrometric and extensive 1D and 2D NMR spectroscopic analysis, including COSY, HSQC, HMBC, and ROESY experiments. The absolute configurations of alkaloids were proposed based on optical rotation sign, and biogenetic considerations. This study represents the first phytochemical analysis of Maytenus segoviarum.
[Mh] Termos MeSH primário: Alcaloides/isolamento & purificação
Celastraceae/química
Piridinas/isolamento & purificação
Sesquiterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Alcaloides/química
Celastrus
El Salvador
Maytenus/química
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Peru
Piridinas/química
Sesquiterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Pyridines); 0 (Sesquiterpenes)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170701
[St] Status:MEDLINE


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[PMID]:28548851
[Au] Autor:Wibowo M; Wang Q; Holst J; White JM; Hofmann A; Davis RA
[Ad] Endereço:Griffith Institute for Drug Discovery, Griffith University , Brisbane, QLD 4111, Australia.
[Ti] Título:Celastrofurans A-G: Dihydro-ß-agarofurans from the Australian Rainforest Vine Celastrus subspicata and Their Inhibitory Effect on Leucine Transport in Prostate Cancer Cells.
[So] Source:J Nat Prod;80(6):1918-1925, 2017 Jun 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Seven new dihydro-ß-agarofurans, celastrofurans A-G (1-7), along with two known secondary metabolites, 9ß-benzoyloxy-1α-furoyloxydihydro-ß-agarofuran (8) and (1R,2R,4R,5S,7R,9S,10R)-2-acetoxy-9-benzoyloxy-1-furoyloxydihydro-ß-agarofuran (9), were obtained from the leaves of the Australian rainforest vine, Celastrus subspicata. The structures of the new compounds were determined by detailed spectroscopic (1D/2D NMR) and MS data analysis. The absolute configurations of compounds 1-4 were defined by ECD and single-crystal X-ray diffraction studies. All compounds were found to exhibit inhibitory activity on leucine transport in the human prostate cancer cell line LNCaP with IC values ranging from 7.0 to 98.9 µM. Dihydro-ß-agarofurans 1-9 showed better potency than the L-type amino acid transporter (LAT) family inhibitor, 2-aminobicyclo[2.2.1]-heptane-2-carboxylic acid (BCH).
[Mh] Termos MeSH primário: Celastrus/química
Leucina/efeitos dos fármacos
Leucina/metabolismo
Neoplasias da Próstata/tratamento farmacológico
Sesquiterpenos/isolamento & purificação
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Sistemas de Transporte de Aminoácidos/farmacologia
Austrália
Cristalografia por Raios X
Seres Humanos
Masculino
Estrutura Molecular
Folhas de Planta/química
Floresta Úmida
Sesquiterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acid Transport Systems); 0 (Sesquiterpenes); 20053-66-1 (dihydroagarofuran); GMW67QNF9C (Leucine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170527
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00220


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[PMID]:28164735
[Au] Autor:Malik J; Karan M; Dogra R
[Ad] Endereço:a University Institute of Pharmaceutical Sciences - Centre of Advanced Study, Panjab University , Chandigarh , India.
[Ti] Título:Ameliorating effect of Celastrus paniculatus standardized extract and its fractions on 3-nitropropionic acid induced neuronal damage in rats: possible antioxidant mechanism.
[So] Source:Pharm Biol;55(1):980-990, 2017 Dec.
[Is] ISSN:1744-5116
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Celastrus paniculatus Wild. (Celasteraceae) (CP) is a well-known Ayurvedic 'Medhya Rasayana' (nervine tonic), used extensively as a neuro-protective and memory enhancer, and in different central nervous system disorders. OBJECTIVE: To evaluate the effect of CP against 3-nitropropionic acid (3-NP) induced Huntington's disease (HD) like symptoms in Wistar male rats. MATERIALS AND METHODS: The ethanol extract of CP seeds (CPEE), prepared by maceration, was standardized on the basis of linoleic acid content (6.42%) using thin layer chromatography densitometric analysis. Protective effect of CPEE (100 and 200 mg/kg) and its various fractions, viz., petroleum ether (40 mg/kg), ethyl acetate (2.5 mg/kg), n-butanol (7 mg/kg) and aqueous (18 mg/kg), administered orally for 20 days, against 3-NP (10 mg/kg, i.p. for 14 days) was assessed by their effect on body weight, locomotor activity, grip strength, gait pattern and cognitive dysfunction and biochemical parameters for oxidative damage in the striatum and cortex regions of the brain. RESULTS: CPEE (100 and 200 mg/kg) treated animals exhibited a significant (p < 0.05) improvement in behavioural and oxidative stress parameters in comparison to only 3-NP treated animals. Amongst various tested fractions of CPEE, aqueous fraction (AF) at 18 mg/kg exhibited maximum reversal of 3-NP induced behavioural and biochemical alterations, and was therefore also tested at 9 and 36 mg/kg. CPEE (100 mg/kg) and AF (36 mg/kg) exhibited maximum and significant (p < 0.05) attenuation of 3-NP induced alterations in comparison to 3-NP treated rats. CONCLUSIONS: CPEE has a protective action against 3-NP induced HD like symptoms due to its strong antioxidant effect.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Encéfalo/efeitos dos fármacos
Celastrus/química
Doença de Huntington/prevenção & controle
Degeneração Neural
Neurônios/efeitos dos fármacos
Fármacos Neuroprotetores/farmacologia
Nitrocompostos
Estresse Oxidativo/efeitos dos fármacos
Extratos Vegetais/farmacologia
Propionatos
[Mh] Termos MeSH secundário: Animais
Antioxidantes/isolamento & purificação
Comportamento Animal/efeitos dos fármacos
Biomarcadores/metabolismo
Encéfalo/metabolismo
Encéfalo/patologia
Encéfalo/fisiopatologia
Cromatografia em Camada Delgada
Cognição/efeitos dos fármacos
Citoproteção
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Etanol/química
Marcha/efeitos dos fármacos
Doença de Huntington/metabolismo
Doença de Huntington/fisiopatologia
Doença de Huntington/psicologia
Masculino
Memória/efeitos dos fármacos
Atividade Motora/efeitos dos fármacos
Força Muscular/efeitos dos fármacos
Neurônios/metabolismo
Neurônios/patologia
Fármacos Neuroprotetores/isolamento & purificação
Fitoterapia
Extratos Vegetais/isolamento & purificação
Plantas Medicinais
Ratos Wistar
Sementes
Solventes/química
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Biomarkers); 0 (Neuroprotective Agents); 0 (Nitro Compounds); 0 (Plant Extracts); 0 (Propionates); 0 (Solvents); 3K9958V90M (Ethanol); QY4L0FOX0D (3-nitropropionic acid)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170309
[Lr] Data última revisão:
170309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170207
[St] Status:MEDLINE
[do] DOI:10.1080/13880209.2017.1285945


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[PMID]:28081198
[Au] Autor:Mu XY; Zhao LC; Zhang ZX
[Ad] Endereço:Laboratory of Systematic Evolution and Biogeography of Woody Plants, College of Nature Conservation, Beijing Forestry University, Beijing, PR China.
[Ti] Título:Molecular Analysis of Chinese Celastrus and Tripterygium and Implications in Medicinal and Pharmacological Studies.
[So] Source:PLoS One;12(1):e0169973, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Celastrus and Tripterygium species, which are used in traditional Chinese medicine, have attracted much attention due to their anti-tumor promoting and neuroprotective activities, in addition to their applications in autoimmune disorders. However, systematic relationships between them and among species are unclear, and it may disturb their further medicinal utilization. In the present study, the molecular analysis of combined chloroplast and nuclear markers of all Chinese Celastrus and Tripterygium was performed, and clear inter- and intra-genus relationships were presented. The result suggests that Tripterygium constitute a natural monophyletic clade within Celastrus with strong support value. Fruit and seed type are better than inflorescence in subgeneric classification. Chinese Celastrus are classified for three sections: Sect. Sempervirentes (Maxim.) CY Cheng & TC Kao, Sect. Lunatus XY Mu & ZX Zhang, sect. nov., and Sect. Ellipticus XY Mu & ZX Zhang, sect. nov. The phylogenetic data was consistent with their chemical components reported previously. Owing to the close relationship, several evergreen Celastrus species are recommended for chemical and pharmacological studies. Our results also provide reference for molecular identification of Chinese Celastrus and Tripterygium.
[Mh] Termos MeSH primário: Celastrus/classificação
Celastrus/genética
Filogenia
Tripterygium/classificação
Tripterygium/genética
[Mh] Termos MeSH secundário: Celastrus/química
Celastrus/metabolismo
Cloroplastos/química
Cloroplastos/metabolismo
DNA de Plantas/genética
Frutas/química
Medicina Tradicional Chinesa
Fenômenos Farmacológicos
Sementes/química
Análise de Sequência de DNA
Tripterygium/química
Tripterygium/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (DNA, Plant)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170824
[Lr] Data última revisão:
170824
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170113
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0169973


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[PMID]:28066108
[Au] Autor:Bhagya V; Christofer T; Shankaranarayana Rao BS
[Ad] Endereço:Department of Neurophysiology, National Institute of Mental Health and Neurosciences, Bengaluru, Karnataka, India.
[Ti] Título:Neuroprotective effect of on chronic stress-induced cognitive impairment.
[So] Source:Indian J Pharmacol;48(6):687-693, 2016 Nov-Dec.
[Is] ISSN:1998-3751
[Cp] País de publicação:India
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Several studies report that chronic stress results in impaired spatial learning and working memory and enhanced anxiety-like behavior. However, not many studies have looked into the possible ways of reversing stress-induced deficits. (CP), a traditional ayurvedic herbal medicine, was used to treat cognitive deficits in mentally retarded children. CP oil has been reported to have neuroprotective and antioxidant activities. However, the effects of CP oil on chronic stress-induced cognitive deficits are unclear. In the present study, we intended to analyze the neuroprotective effects of CP oil on stress-associated cognitive dysfunctions. MATERIALS AND METHODS: Chronic stress was induced by subjecting rats to restrainers for 6 h a day for 21 days. CP oil (400, 600 mg/kg) or vehicle was administered intraperitoneally (i.p.) after stress protocol once a day over the next 14 days. Groups used in the present study: normal control, stress, stress + vehicle, stress + CP oil at 2 different doses (400 and 600 mg/kg, i.p.). After the drug treatment, open field and elevated plus maze (EPM) were used to analyze anxiety-like behavior, and partially baited radial arm maze (RAM) and T-maze were used to evaluate spatial learning and memory capabilities. Analysis has been done using two-way ANOVA followed by Bonferroni's test and one-way ANOVA followed by Tukey's test. RESULTS: Stressed rats showed enhanced anxiety-like behavior in EPM ( < 0.001) and impaired performance in RAM ( < 0.001) and T-maze tasks ( < 0.001) compared to normal animals. In contrast, CP oil treatment to these rats improved their performance in both RAM ( < 0.001) and T-maze ( < 0.001). In addition, CP oil significantly reduced stress-induced anxiety behavior ( < 0.001). CONCLUSION: Chronic treatment with CP oil is to improve cognitive abilities in chronically stressed rats. The current study provides a novel perspective on beneficial effect of herbal therapy on stress-induced cognitive dysfunctions.
[Mh] Termos MeSH primário: Celastrus
Disfunção Cognitiva/tratamento farmacológico
Fármacos Neuroprotetores/uso terapêutico
Óleos Vegetais/uso terapêutico
Estresse Psicológico/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Doença Crônica
Disfunção Cognitiva/psicologia
Comportamento Exploratório/efeitos dos fármacos
Comportamento Exploratório/fisiologia
Masculino
Fármacos Neuroprotetores/isolamento & purificação
Fármacos Neuroprotetores/farmacologia
Extratos Vegetais/isolamento & purificação
Extratos Vegetais/farmacologia
Extratos Vegetais/uso terapêutico
Óleos Vegetais/farmacologia
Ratos
Ratos Wistar
Estresse Psicológico/psicologia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Neuroprotective Agents); 0 (Plant Extracts); 0 (Plant Oils); 93333-86-9 (Celastrus oil)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170110
[St] Status:MEDLINE
[do] DOI:10.4103/0253-7613.194853


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[PMID]:28006915
[Au] Autor:Gao L; Zhang R; Lan J; Ning R; Wu D; Chen D; Zhao W
[Ad] Endereço:Department of Natural Product Chemistry and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, People's Republic of China.
[Ti] Título:ß-Dihydroagarofuran-Type Sesquiterpenes from the Seeds of Celastrus monospermus and Their Lifespan-Extending Effects on the Nematode Caenorhabditis elegans.
[So] Source:J Nat Prod;79(12):3039-3046, 2016 Dec 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Seventeen ß-dihydroagarofuran-type sesquiterpenes were isolated from the seeds of Celastrus monospermus, and, among them, 15 (1-15) were identified as new natural products. Nine isolates were evaluated for their lifespan-extending effect using the standard model animal nematode Caenorhabditis elegans. As a result, all of the tested compounds prolonged the lifespan of C. elegans when compared to the blank control group (p < 0.0001). Among them, celaspermin E (5) extended the average lifespan and maximum lifespan of C. elegans, with effects similar to those of rapamycin, a positive control that has been found experimentally to delay the aging process of yeasts, worms, fruit flies, and mice.
[Mh] Termos MeSH primário: Caenorhabditis elegans/efeitos dos fármacos
Celastrus/química
Sementes/química
Sesquiterpenos/isolamento & purificação
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Longevidade/efeitos dos fármacos
Estrutura Molecular
Sesquiterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sesquiterpenes); 20053-66-1 (dihydroagarofuran)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170503
[Lr] Data última revisão:
170503
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161224
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b00648


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[PMID]:27791375
[Au] Autor:Li JL; Wu L; Wu J; Feng HX; Wang HM; Fu Y; Zhang RJ; Zhang HY; Zhao WM
[Ad] Endereço:State Key Laboratory of Drug Research and ‡CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, People's Republic of China.
[Ti] Título:Caffeoyl Triterpenoid Esters as Potential Anti-ischemic Stroke Agents from Celastrus orbiculatus.
[So] Source:J Nat Prod;79(11):2774-2779, 2016 Nov 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Three new triterpenoids, celastrusins A-C (1-3), together with 3-O-caffeoyl-α-amyrin (4) were isolated from the root bark of Celastrus orbiculatus. Their structures were identified by spectroscopic analysis, X-ray crystallography using Cu Kα radiation, and the comparison of both observed and reported spectroscopic data. An in vitro bioassay revealed that the caffeoyl triterpenoid esters 1, 3, and 4 possess neuroprotective effects against oxygen-glucose deprivation (OGD) induced SH-SY5Y cell damage. Further animal studies indicated that compound 1 significantly reduced brain infarction after transient middle cerebral artery occlusion (MCAO) in rats using a 10 mg/kg (i.v.) dose.
[Mh] Termos MeSH primário: Ácidos Cafeicos/isolamento & purificação
Ácidos Cafeicos/farmacologia
Celastrus/química
Medicamentos de Ervas Chinesas/isolamento & purificação
Medicamentos de Ervas Chinesas/farmacologia
Isquemia/tratamento farmacológico
Fármacos Neuroprotetores/química
Fármacos Neuroprotetores/isolamento & purificação
Fármacos Neuroprotetores/farmacologia
Triterpenos/isolamento & purificação
Triterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Ácidos Cafeicos/química
Doenças Arteriais Cerebrais/tratamento farmacológico
Cristalografia por Raios X
Relação Dose-Resposta a Droga
Medicamentos de Ervas Chinesas/química
Ésteres
Seres Humanos
Masculino
Conformação Molecular
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Ácido Oleanólico/análogos & derivados
Casca de Planta/química
Raízes de Plantas/química
Ratos
Triterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caffeic Acids); 0 (Drugs, Chinese Herbal); 0 (Esters); 0 (Neuroprotective Agents); 0 (Triterpenes); 0 (celastrusin A); 0 (celastrusin B); 0 (celastrusin C); 6SMK8R7TGJ (Oleanolic Acid); KM8353IPSO (amyrin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170609
[Lr] Data última revisão:
170609
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161030
[St] Status:MEDLINE


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[PMID]:27716341
[Au] Autor:Gu H; Feng J; Wang H; Qian Y; Yang L; Chen J; Jin F; Shi Y; Lu S; Liu Y
[Ad] Endereço:Yangzhou University-Yangzhou Cancer Research Institute, Yangzhou, 225009, China.
[Ti] Título:Celastrus orbiculatus extract inhibits the migration and invasion of human glioblastoma cells in vitro.
[So] Source:BMC Complement Altern Med;16(1):387, 2016 Oct 06.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Gliomas are highly aggressive tumors of the nervous system, and current treatments fail to improve patient survival. To identify substances that can be used as treatments for gliomas, we examined the effect of Celastrus orbiculatus extract (COE) on the invasion and migration of human glioblastoma U87 and U251 cells in vitro. METHODS: The effects of COE on cell viability and adhesion were tested using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay and cell adhesion assay, respectively. The effects of COE on cell migration and invasion were assessed by a wound-healing assay and transwell migration and invasion assays. The effects of COE on the expression of epithelial-mesenchymal transition (EMT)-related proteins and matrix metalloproteinases (MMPs) were evaluated using western blot and gelatin zymography, respectively. Finally, the effect of COE on actin assembly was observed using phalloidin-tetramethylrhodamine isothiocyanate labeling and confocal laser scanning microscopy. RESULTS: We found that COE inhibited the adhesion, migration, and invasion of U87 and U251 cells in a dose-dependent manner. COE reduced N-cadherin and vimentin expression, increased E-cadherin expression, and reduced MMP-2 and MMP-9 expression in U87 and U251 cells. Furthermore, COE inhibited actin assembly in U87 and U251 cells. CONCLUSIONS: COE attenuates EMT, MMP expression, and actin assembly in human glioblastoma cells, thereby inhibiting their adhesion, migration, and invasion in vitro.
[Mh] Termos MeSH primário: Celastrus/química
Movimento Celular/efeitos dos fármacos
Transição Epitelial-Mesenquimal/efeitos dos fármacos
Glioblastoma
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Citoesqueleto/efeitos dos fármacos
Seres Humanos
Invasividade Neoplásica
Extratos Vegetais/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Plant Extracts)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161008
[St] Status:MEDLINE


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[PMID]:27324586
[Au] Autor:Cheng D; Feng M; Ji Y; Wu W; Hu Z
[Ad] Endereço:College of Plant Protection, Institute of Pesticide Science, Northwest A&F University, Yangling, Shaanxi 712100, China (chendannwsuaf@126.com; fengmx2010@126.com; jyf_1991@126.com; wuwenjun@nwsuaf.edu.cn; huzhaonong@nwsuaf.edu.cn) Key Laboratory of Botanical Pesticide R & D in Shaanxi Provin
[Ti] Título:Effects of Celangulin IV and V From Celastrus angulatus Maxim on Na+/K+-ATPase Activities of the Oriental Armyworm (Lepidoptera: Noctuidae).
[So] Source:J Insect Sci;16(1), 2016.
[Is] ISSN:1536-2442
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Na(+)/K(+)-ATPase (sodium pump) is an important target for the development of botanical pesticide as it is responsible for transforming chemical energy in ATP to osmotic work and maintaining electrochemical Na(+ )and K(+ )gradients across the cell membrane of most animal cells. Celangulin IV (C-IV) and V (C-V), which are isolated from the root bark of Celastrus angulatus, are the major active ingredients of this insecticidal plant. The activities of C-IV and C-V on Na(+)/K(+)-ATPase were investigated by ultramicro measuring method to evaluate the effects of C-IV and C-V on Na(+)/K(+)-ATPase activities of the brain from the fifth Mythimna separata larvae and to discuss the insecticidal mechanism of C-IV and C-V. Results indicate that inhibitory activities of Na(+)/K(+)-ATPase by C-IV and C-V possess an obvious concentration-dependent in vitro. Compared with C-IV, the inhibition of C-V on Na(+)/K(+)-ATPase was not striking. In vivo, at a concentration of 25 mg/liter, the inhibition ratio of C-IV on Na(+)/K(+)-ATPase activity from the brain in narcosis and recovery period was more remarkable than that of C-V. Furthermore, the insects were fed with different mixture ratios of C-IV and C-V. The inhibition extent of Na(+)/K(+)-ATPase activity was corresponded with the dose of C-IV. However, C-V had no notable effects. This finding may mean that the mechanism of action of C-IV and C-V on Na(+)/K(+)-ATPase were different. Na(+)/K -ATPase may be an action target of C-IV and C-V.
[Mh] Termos MeSH primário: Celastrus/química
Haptenos/farmacologia
Proteínas de Insetos/antagonistas & inibidores
Mariposas/efeitos dos fármacos
ATPase Trocadora de Sódio-Potássio/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Encéfalo/efeitos dos fármacos
Encéfalo/enzimologia
Ativação Enzimática/efeitos dos fármacos
Inibidores Enzimáticos/farmacologia
Inseticidas/farmacologia
Larva/efeitos dos fármacos
Larva/enzimologia
Mariposas/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Haptens); 0 (Insect Proteins); 0 (Insecticides); 0 (celangulin V); EC 3.6.3.9 (Sodium-Potassium-Exchanging ATPase)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160622
[St] Status:MEDLINE


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[PMID]:27159672
[Au] Autor:Li H; Li J; Liu L; Zhang Y; Luo Y; Zhang X; Yang P; Zhang M; Yu W; Qu S
[Ad] Endereço:Department of Endocrinology, Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai, China.
[Ti] Título:Elucidation of the Intestinal Absorption Mechanism of Celastrol Using the Caco-2 Cell Transwell Model.
[So] Source:Planta Med;82(13):1202-7, 2016 Aug.
[Is] ISSN:1439-0221
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Celastrol, a triterpenoid isolated from stem (caulis) of Celastrus orbiculatus Thunb. (Celastraceae), has been known to have various pharmacological effects, including anti-inflammatory, anticancer, and antioxidant activities. However, the mechanism of the intestinal absorption of celastrol is unknown. The aim of this study was to investigate the intestinal absorption of celastrol using the Caco-2 cell transwell model. First, the bidirectional transport of celastrol in Caco-2 cell monolayers was observed. Then, the effects of time, concentration, temperature, paracellular pathway, and efflux transport inhibition on the transport of celastrol across the Caco-2 cell monolayers were investigated. The P-glycoprotein inhibitor verapamil and cyclosporin A, the multidrug resistance protein 2 inhibitor MK571, and the breast cancer resistance protein inhibitor reserpine were used. Additionally, the effects of celastrol on the activity of P-glycoprotein were evaluated using the rhodamine 123 uptake assay. In this study, we found that the intestinal transport of celastrol was a time- and concentration-dependent active transport. The paracellular pathway was not involved in the transport of celastrol, and the efflux of celastrol was energy dependent. The results indicated that celastrol is a substrate of P-glycoprotein but not multidrug resistance protein 2 or the breast cancer resistance protein. In addition, celastrol could not affect the uptake of rhodamine 123 in Caco-2 cells, which indicated that celastrol could not inhibit or induce the activity of P-glycoprotein.
[Mh] Termos MeSH primário: Absorção Intestinal
Triterpenos/farmacocinética
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/farmacocinética
Antineoplásicos Fitogênicos/farmacocinética
Transporte Biológico
Células CACO-2
Proteínas de Transporte/metabolismo
Celastrus/química
Seres Humanos
Mucosa Intestinal/metabolismo
Rodamina 123/metabolismo
Temperatura Ambiente
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents, Phytogenic); 0 (Carrier Proteins); 0 (Triterpenes); 1N3CZ14C5O (Rhodamine 123); L8GG98663L (tripterine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170405
[Lr] Data última revisão:
170405
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160510
[St] Status:MEDLINE
[do] DOI:10.1055/s-0035-1568597



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