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Pesquisa : D03.383.663.283.266.450.284 [Categoria DeCS]
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  1 / 1991 MEDLINE  
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[PMID]:29225170
[Au] Autor:He MH; Zhang Q; Shu G; Lin JC; Zhao L; Liang XX; Yin L; Shi F; Fu HL; Yuan ZX
[Ad] Endereço:Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, 611130, China.
[Ti] Título:Dihydromyricetin sensitizes human acute myeloid leukemia cells to retinoic acid-induced myeloid differentiation by activating STAT1.
[So] Source:Biochem Biophys Res Commun;495(2):1702-1707, 2018 01 08.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The success of all-trans retinoic acid (ATRA) in differentiation therapy for patients with acute promyelocytic leukemia (APL) highly encourages researches to apply a new combination therapy based on ATRA. Therefore, research strategies to further sensitize cells to retinoids are urgently needed. In this study, we showed that Dihydromyricetin (DMY), a 2,3-dihydroflavonol compound, exhibited a strong synergy with ATRA to promote APL NB4 cell differentiation. We observed that DMY sensitized the NB4 cells to ATRA-induced cell growth inhibition, CD11b expression, NBT reduction and myeloid regulator expression. PML-RARα might not be essential for DMY-enhanced differentiation when combined with ATRA, while the enhanced differentiation was dependent on the activation of p38-STAT1 signaling pathway. Taken together, our study is the first to evaluate the synergy of DMY and ATRA in NB4 cell differentiation and to assess new opportunities for the combination of DMY and ATRA as a promising approach for future differentiation therapy.
[Mh] Termos MeSH primário: Flavonóis/administração & dosagem
Leucemia Promielocítica Aguda/tratamento farmacológico
Fator de Transcrição STAT1/metabolismo
Tretinoína/administração & dosagem
[Mh] Termos MeSH secundário: Antineoplásicos/administração & dosagem
Diferenciação Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Sinergismo Farmacológico
Seres Humanos
Leucemia Mieloide Aguda/tratamento farmacológico
Leucemia Mieloide Aguda/metabolismo
Leucemia Mieloide Aguda/patologia
Leucemia Promielocítica Aguda/metabolismo
Leucemia Promielocítica Aguda/patologia
Sistema de Sinalização das MAP Quinases/efeitos dos fármacos
Proteínas de Fusão Oncogênicas/metabolismo
Proteólise/efeitos dos fármacos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Flavonols); 0 (Oncogene Proteins, Fusion); 0 (STAT1 Transcription Factor); 0 (STAT1 protein, human); 0 (promyelocytic leukemia-retinoic acid receptor alpha fusion oncoprotein); 5688UTC01R (Tretinoin); KD8QND6427 (dihydromyricetin)
[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:171212
[St] Status:MEDLINE


  2 / 1991 MEDLINE  
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[PMID]:28966277
[Au] Autor:Terazawa S; Uemura Y; Koyama Y; Kawakami S; Sugimoto S; Matsunami K; Otsuka H; Shinzato T; Kawahata M; Yamaguchi K
[Ad] Endereço:Graduate School of Biomedical and Health Sciences, Hiroshima University.
[Ti] Título:Microtropins Q-W, ent-Labdane Glucosides: Microtropiosides G-I, Ursane-Type Triterpene Diglucoside and Flavonol Glycoside from the Leaves of Microtropis japonica.
[So] Source:Chem Pharm Bull (Tokyo);65(10):930-939, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Microtropins Q-W, (2S,3R)-2-ethyl-2,3-dihydroxybutyrate of various glucosides and glucose, as well as three ent-labdane diterpenoid glucosides, named microtropiosides G, H and I, an ursane-type triterpene diglucoside and a flavonoid glycoside were isolated from the MeOH extract of the leaves of Microtropis japonica. The structure of microtropioside A, also isolated from the branches of M. japonica, was elucidated spectroscopically in a previous experiment and was found to possess a rare seven-membered oxyrane ring. Its structure was confirmed by X-ray crystallographic analysis of its pentaacetate.
[Mh] Termos MeSH primário: Celastraceae/química
Flavonóis/química
Glucosídeos/química
Triterpenos/química
[Mh] Termos MeSH secundário: Celastraceae/metabolismo
Cristalografia por Raios X
Diterpenos/química
Flavonóis/isolamento & purificação
Glucosídeos/isolamento & purificação
Espectroscopia de Ressonância Magnética
Conformação Molecular
Extratos Vegetais/química
Folhas de Planta/química
Folhas de Planta/metabolismo
Triterpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes); 0 (Flavonols); 0 (Glucosides); 0 (Plant Extracts); 0 (Triterpenes); 0 (labdane); 0 (ursane)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00459


  3 / 1991 MEDLINE  
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[PMID]:28779689
[Au] Autor:Dutta Gupta S; Karmakar A
[Ad] Endereço:Agricultural and Food Engineering Department, Indian Institute of Technology Kharagpur, Kharagpur 721302, India. Electronic address: sdg@agfe.iitkgp.ernet.in.
[Ti] Título:Machine vision based evaluation of impact of light emitting diodes (LEDs) on shoot regeneration and the effect of spectral quality on phenolic content and antioxidant capacity in Swertia chirata.
[So] Source:J Photochem Photobiol B;174:162-172, 2017 Sep.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The present study demonstrates the influence of LED irradiance of various wavelengths on shoot regeneration, biomass accumulation, photosynthetic pigment contents, and antioxidant potentials of Swertia chirata - a critically endangered medicinal plant. Mixed treatment of blue (BL) and red LEDs (RL) in equal proportion (1:1) significantly improved the shoot regeneration response. A machine vision system was developed to assess the shoot regeneration potential under different lighting treatments. Regenerated shoots exposed under BL:RL (1:1) exhibited higher biomass accumulation and canopy development compared to other lighting treatments. Improved canopy growth was evident from the increase in the area, major axis, minor axis, convex area, equivalent diameter and perimeter of regenerated shoot clusters. A higher correlation of dry weight (DW) was noted with the image feature, weighted density (WD) than the fresh weight (FW) in all the LED treated cultures. The significant correlation between DW and WD implies that the image feature WD can be adopted as a non-invasive approach for measuring biomass accumulation as well as detecting hyperhydricity. The developed machine vision approach provides a new direction in the evaluation of shoot organogenesis that displayed features including both shoot multiplication and canopy development. Chlorophyll and carotenoid contents of the regenerated shoots were found to be higher under BL:RL (1:1) than the other treatments. Supplementation of RL led to a reduction in the pigment contents. Spectral quality of lights also significantly influenced the accumulation of total phenolics, flavonoids and flavonols. Cultures exposed under BL exhibited the maximum accumulation of polyphenols. A similar effect of spectral quality was observed with the antioxidant capacity and reducing power potential of leaf extract. The findings demonstrate the ability of LEDs in inducing shoot regeneration as well as accumulation of phenolic antioxidants and suggest that the proportion of blue and red LEDs is an important factor in achieving the optimum response.
[Mh] Termos MeSH primário: Antioxidantes/metabolismo
Luz
Fenóis/metabolismo
Brotos de Planta/fisiologia
Brotos de Planta/efeitos da radiação
Regeneração/efeitos da radiação
Swertia/efeitos da radiação
[Mh] Termos MeSH secundário: Flavonóis/metabolismo
Imagem Molecular
Fotossíntese/efeitos da radiação
Swertia/metabolismo
Swertia/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Flavonols); 0 (Phenols)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171012
[Lr] Data última revisão:
171012
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170806
[St] Status:MEDLINE


  4 / 1991 MEDLINE  
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[PMID]:28760528
[Au] Autor:Li X; Lee M; Chen G; Zhang Q; Zheng S; Wang G; Chen QH
[Ad] Endereço:Department of Chemistry, California State University, Fresno, 2555 E. San Ramon Avenue, M/S SB70, Fresno, CA 93740, USA.
[Ti] Título:3-O-Substituted-3',4',5'-trimethoxyflavonols: Synthesis and cell-based evaluation as anti-prostate cancer agents.
[So] Source:Bioorg Med Chem;25(17):4768-4777, 2017 Sep 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Twenty-two 3-O-substituted-3',4',5'-trimethoxyflavonols have been designed and synthesized for their anti-proliferative activity towards three human prostate cancer cell lines. Our results indicate that most of them are significantly more potent than the parent 3',4',5'-trimethoxyflavonol in inhibiting the cell proliferation in PC-3 and LNCaP prostate cancer cell models. 3-O-Substituted-3',4',5'-trimethoxyflavonols have generally higher potency towards PC-3 and LNCaP cell lines than the DU145 cell line. Incorporation of an ethyl group to 3-OH of 3',4',5'-trimethoxyflavonol leads to 3-O-ethyl-3',4',5'-trimethoxyflavonol as the optimal derivative with up to 36-fold enhanced potency as compared with the corresponding lead compound 3',4',5'-trimethoxyflavonol, but with reversed PC-3 cell apoptotic response. Introduction of a dipentylaminopropyl group to 3-OH increases not only the antiproliferative potency but also the ability in activating PC-3 cell apoptosis. Our findings imply that modification on 3-OH of trimethoxyflavonol can further enhance its in vitro anti-proliferative potency and PC-3 cell apoptosis induction.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Flavonóis/química
Flavonóis/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Flavonóis/síntese química
Seres Humanos
Masculino
Neoplasias da Próstata/metabolismo
Neoplasias da Próstata/patologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3',4',5'-trimethoxyflavonol); 0 (Antineoplastic Agents); 0 (Flavonols)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170802
[St] Status:MEDLINE


  5 / 1991 MEDLINE  
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[PMID]:28692289
[Au] Autor:De Leo M; Peruzzi L; Granchi C; Tuccinardi T; Minutolo F; De Tommasi N; Braca A
[Ad] Endereço:Dipartimento di Farmacia, Università di Pisa , Via Bonanno 6 and 33, 56126 Pisa, Italy.
[Ti] Título:Constituents of Polygala flavescens ssp. flavescens and Their Activity as Inhibitors of Human Lactate Dehydrogenase.
[So] Source:J Nat Prod;80(7):2077-2087, 2017 Jul 28.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Four new flavonol glycosides (1-4), two oligosaccharides (5, 6), one α-ionone (7), and three triterpenoid saponins (8-10), together with four known secondary metabolites (11-14), were isolated from the aerial parts of Polygala flavescens ssp. flavescens. All structures were elucidated on the basis of their spectroscopic and spectrometric data. The isolates were assayed for their inhibitory activity against isoform 5 of human lactate dehydrogenase, and compound 11 (3,6'-di-O-sinapoylsucrose) showed an IC value of 90.4 µM. Modeling studies were carried out to suggest the putative interaction mode of compound 11 in the enzyme active site.
[Mh] Termos MeSH primário: Flavonóis/isolamento & purificação
Flavonóis/farmacologia
L-Lactato Desidrogenase/antagonistas & inibidores
Norisoprenoides/isolamento & purificação
Norisoprenoides/farmacologia
Polygala/química
Saponinas/isolamento & purificação
Saponinas/farmacologia
Sacarose/análogos & derivados
Sacarose/farmacologia
Triterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Flavonóis/química
Seres Humanos
Concentração Inibidora 50
Itália
Estrutura Molecular
Norisoprenoides/química
Ressonância Magnética Nuclear Biomolecular
Componentes Aéreos da Planta/química
Saponinas/química
Sacarose/química
Sacarose/isolamento & purificação
Triterpenos/química
Triterpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavonols); 0 (Norisoprenoids); 0 (Saponins); 0 (Triterpenes); 57-50-1 (Sucrose); EC 1.1.1.27 (L-Lactate Dehydrogenase); I9V075M61R (alpha-ionone)
[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:170711
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00295


  6 / 1991 MEDLINE  
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[PMID]:28686246
[Au] Autor:Fan M; Zhang G; Pan J; Gong D
[Ad] Endereço:State Key Laboratory of Food Science and Technology, Nanchang University, 235 Nanjing East Road, Nanchang 330047, China. gwzhang@ncu.edu.cn.
[Ti] Título:An inhibition mechanism of dihydromyricetin on tyrosinase and the joint effects of vitamins B , D or E.
[So] Source:Food Funct;8(7):2601-2610, 2017 Jul 19.
[Is] ISSN:2042-650X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Dihydromyricetin (DMY), a natural flavonoid, was found to effectively inhibit tyrosinase activity in a mixed-type manner with an IC value of (3.66 ± 0.14) × 10 mol L . DMY combined with the dietary vitamin D at lower concentrations exhibited a synergistic effect on the inhibition of tyrosinase. The formation of a DMY-tyrosinase complex led to fluorescence quenching and conformational changes of tyrosinase, which was driven mainly by hydrophobic interactions and hydrogen bonds. The molecular simulation further found that DMY inserted into the active pocket of tyrosinase interacted with amino acid residues Tyr78, His85, and Ala323, occupying the catalytic center of tyrosinase to hinder entrance of the substrate, leading to the inhibition of tyrosinase. This study may provide a scientific foundation for screening effective tyrosinase inhibitors.
[Mh] Termos MeSH primário: Colecalciferol/química
Inibidores Enzimáticos/química
Flavonóis/química
Monofenol Mono-Oxigenase/química
Vitamina B 6/química
Vitamina E/química
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Sítios de Ligação
Cinética
Simulação de Acoplamento Molecular
Monofenol Mono-Oxigenase/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Flavonols); 1406-18-4 (Vitamin E); 1C6V77QF41 (Cholecalciferol); 8059-24-3 (Vitamin B 6); EC 1.14.18.1 (Monophenol Monooxygenase); KD8QND6427 (dihydromyricetin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170708
[St] Status:MEDLINE
[do] DOI:10.1039/c7fo00236j


  7 / 1991 MEDLINE  
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[PMID]:28667870
[Au] Autor:Nguyen PD; Sayagh C; Borie N; Lavaud C
[Ad] Endereço:Institut de Chimie Moléculaire de Reims (ICMR), CNRS UMR 7312, BP 1039, 51687 Reims cedex 2, France.
[Ti] Título:Anti-radical flavonol glycosides from the aerial parts of Cleome chelidonii L.f.
[So] Source:Phytochemistry;142:30-37, 2017 Oct.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Eleven previously undescribed flavonoid glycosides, named cleomesides C-M, along with five known compounds, were isolated from the aerial parts of Cleome chelidonii L.f. (Cleomaceae). All flavonol glycosides were esterified derivatives of 3,7-O-diglycosides of quercetin or kaempferol. Their structures were elucidated by analysis of the 1D and 2D NMR spectra, HR-ESI-MS data, UV spectra, optical rotation and by comparison with literature data. The DPPH radical scavenging properties of the flavonoid glycosides were studied in order to appreciate the effect of the glycoside parts and of the ester groups on this activity compared with the quercetin and kaempferol aglycones. An acetate at position 3 of rhamnose linked to C-7 of flavonol, gave compounds with the strongest antiradical activity. An aromatic ester group at position 6 of terminal glucose of diglycoside chain linked to C-3 of flavonol did not seem to influence the antiradical activity.
[Mh] Termos MeSH primário: Cleome/química
Flavonóis/isolamento & purificação
Depuradores de Radicais Livres/isolamento & purificação
Glicosídeos/isolamento & purificação
Componentes Aéreos da Planta/química
[Mh] Termos MeSH secundário: Flavonóis/química
Depuradores de Radicais Livres/química
Glicosídeos/química
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavonols); 0 (Free Radical Scavengers); 0 (Glycosides)
[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:170702
[St] Status:MEDLINE


  8 / 1991 MEDLINE  
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[PMID]:28638883
[Au] Autor:Wu G; Dai X; Li X; Jiang H
[Ad] Endereço:Department of respiratory medicine, Changzhou Jintan District People's Hospital, Changzhou, Jiangsu 213200, China.
[Ti] Título:ANTIOXIDANT AND ANTI-INFLAMMATORY EFFECTS OF RHAMNAZIN ON LIPOPOLYSACCHARIDE-INDUCED ACUTE LUNG INJURY AND INFLAMMATION IN RATS.
[So] Source:Afr J Tradit Complement Altern Med;14(4):201-212, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Acute Lung Injury (ALI) results into severe inflammation and oxidative stress to the pulmonary tissue. Rhamnazin is a natural flavonoid and known for its antioxidant and anti-inflammatory properties. MATERIALS AND METHODS: The antioxidative and anti-inflammatory properties rhamnazin were tested for protection against the acute lung injury. We investigated whether rhamnazin improves the lipopolysaccharide (LPS)-induced ALI in an animal model (rat). We also studied the probable molecular mechanism of action of rhamnazin. Rhamnazin was injected intraperitoneally (i.p.) (5, 10 and 20 mg/kg) two days before intratracheal LPS challenge (5mg/kg). The changes in lung wet-to-dry weight ratio, LDH activity, pulmonary histopathology, BALF protein concentration, MPO activity, oxidative stress, cytokine production were estimated. RESULTS: The results showed a significant attenuation of all the inflammatory parameters and a marked improvement in the pulmonary histopathology in the animal groups pretreated with rhamnazin. The rhamnazin pretreated group also showed activation of Nrf2 pathway and attenuation of ROS such as H O , MDA and hydroxyl ion. These results indicated that rhamnazin could attenuate the symptoms of ALI in rats due to its strong antioxidant and anti-inflammatory properties. CONCLUSION: The results strongly demonstrated that rhamnazin provides protection against LPS-induced ALI. The underlying mechanisms of its anti-inflammatory action may include inhibition of Nrf2 mediated antioxidative pathway.
[Mh] Termos MeSH primário: Lesão Pulmonar Aguda/tratamento farmacológico
Lesão Pulmonar Aguda/imunologia
Anti-Inflamatórios/administração & dosagem
Antioxidantes/administração & dosagem
Flavonóis/administração & dosagem
[Mh] Termos MeSH secundário: Lesão Pulmonar Aguda/metabolismo
Animais
Seres Humanos
Lipopolissacarídeos/efeitos adversos
Pulmão/efeitos dos fármacos
Pulmão/imunologia
Masculino
Estresse Oxidativo/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
Espécies Reativas de Oxigênio/imunologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antioxidants); 0 (Flavonols); 0 (Lipopolysaccharides); 0 (Reactive Oxygen Species); 0 (rhamnazin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170623
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i4.23


  9 / 1991 MEDLINE  
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[PMID]:28624472
[Au] Autor:Gao Y; Li C; Wang Y; Liu Y; Li G; Fan X; Li Y; Tian J; Lee AW
[Ad] Endereço:School of Life Sciences, Yantai University, Yantai, 264005, PR China.
[Ti] Título:Nonclinical safety of astilbin: A 4-week oral toxicity study in rats with genotoxicity, chromosomal aberration, and mammalian micronucleus tests.
[So] Source:Food Chem Toxicol;107(Pt A):1-9, 2017 Sep.
[Is] ISSN:1873-6351
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Astilbin is an active flavonoid compound isolated from Rhizoma Smilacis Glabrae. It has been widely used as an anti-hepatic, anti-arthritic, and anti-renal injury agent. However, its safety has not yet been established. The objective of this study was to evaluate 4-week repeated oral toxicity and genotoxicity of astilbin. We examined oral toxicity in Sprague-Dawley rats after daily oral administration of astilbin at 50, 150, and 500 mg/kg for 4 weeks. Negative control animals received the same volume of the solvent. Astilbin administration did not lead to death, body weight gain, food consumption, or adverse events. There were no significant differences in toxicity between the astilbin and control group; we observed no toxic effects on hematological or urinalysis parameters, biochemical values, organ weight, or histopathological findings. We assessed the genotoxicity of astilbin with the Ames test (TA97a, TA98, TA100, TA102, and TA1535), chromosomal aberration assay (using Chinese hamster ovary cells), and mammalian micronucleus test (in mice). We found no genotoxicity in any tested strains. The no-observed-adverse-effect level (NOAEL) for astilbin in the 4-week repeated oral toxicity study in rats was greater than 500 mg/kg body weight/day, regardless of gender. Results also suggested that astilbin does not have genotoxicity potential.
[Mh] Termos MeSH primário: Aberrações Cromossômicas/efeitos dos fármacos
Medicamentos de Ervas Chinesas/efeitos adversos
Flavonóis/efeitos adversos
Smilacaceae/química
[Mh] Termos MeSH secundário: Animais
Células CHO
Cricetinae
Cricetulus
Dano ao DNA/efeitos dos fármacos
Feminino
Flavonóis/administração & dosagem
Masculino
Camundongos
Testes para Micronúcleos
Testes de Mutagenicidade
Nível de Efeito Adverso não Observado
Extratos Vegetais/administração & dosagem
Extratos Vegetais/química
Ratos
Ratos Sprague-Dawley
Salmonella typhimurium/efeitos dos fármacos
Salmonella typhimurium/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drugs, Chinese Herbal); 0 (Flavonols); 0 (Plant Extracts); 29838-67-3 (astilbin)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170829
[Lr] Data última revisão:
170829
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170619
[St] Status:MEDLINE


  10 / 1991 MEDLINE  
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[PMID]:28622617
[Au] Autor:Ye W; Chen R; Sun W; Huang C; Lin X; Dong Y; Wen C; Wang X
[Ad] Endereço:The Second Affiliated Hospital and Yuying Children' s Hospital of Wenzhou Medical University, Wenzhou 325027, China.
[Ti] Título:Determination and pharmacokinetics of engeletin in rat plasma by ultra-high performance liquid chromatography with tandem mass spectrometry.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1060:144-149, 2017 Aug 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Engeletin, a bioactive flavonoid, has attracted much attention recently by virtue of its multiple biological (anti-diabetic and anti-inflammatory) activities. Despite signifying many therapeutic applications researches indicating quantification or pharmacokinetics of engeletin in biological matrix are still lacking. Here, a simple, sensitive, accurate and reliable ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) approach for the quantification of engeletin in rat plasma was developed and fully validated for the first time. Plasma samples were processed with acetonitrile by a single step protein precipitation and the separation was achieved on a ZORBAX Eclipse Plus C18 Rapid Resolution High Definition column with a gradient acetonitrile-water mobile phase. Quantification of engeletin was carried out by electrospray ionization tandem mass spectrometry in multiple reaction monitoring (MRM) mode with negative ionization. Results revealed that the approach was linearity from 5 to 5000ng/mL (r =0.9937) and proved to be precise (better than 12.3%) and accurate (-3.3%-5.2%). The developed approach was successfully employed to pharmacokinetic study of engeletin following peroral and intravenous administration to rats. The results of pharmacokinetics demonstrated rapid engeletin absorption (T of 15min) after oral administration, extensive distribution after three different dosages and an absolute bioavailability of ∼1.53%. The developed method and pharmacokinetic data can provide a meaningful basis for further studies on engeletin.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Flavonóis/sangue
Flavonóis/farmacocinética
Glicosídeos/sangue
Glicosídeos/farmacocinética
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Animais
Disponibilidade Biológica
Estabilidade de Medicamentos
Feminino
Flavonóis/química
Glicosídeos/química
Limite de Detecção
Modelos Lineares
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavonols); 0 (Glycosides); 0 (engeletin)
[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:170617
[St] Status:MEDLINE



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