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Pesquisa : D04.210.500.247.515 [Categoria DeCS]
Referências encontradas : 460 [refinar]
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[PMID]:28587983
[Au] Autor:Huang X; Wang Y; Zhang Z; Wang Y; Chen X; Wang Y; Gao Y
[Ad] Endereço:Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
[Ti] Título:Ophiopogonin D and EETs ameliorate Ang II-induced inflammatory responses via activating PPARα in HUVECs.
[So] Source:Biochem Biophys Res Commun;490(2):123-133, 2017 Aug 19.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:CYP2J2 is highly expressed in cardiovascular tissue including the heart and vascular endothelial cells. CYP2J2 and the EETs have been shown owning diverse biological effects. Our previous study found that ophiopogonin D (OP-D) suppressed drug-induced endoplasmic reticulum (ER) stress by upregulating the levels of CYP2J3/EETs in cardiomyocytes. The aim of this research was to investigate whether CYP2J2/EETs-PPARα pathway involved in endothelium protective effects of OP-D in human umbilical vein endothelial cells (HUVECs). The results showed that OP-D significantly inhibited Ang II induced NF-κB nuclear translocation, IκBα down-regulation and activation of pro-inflammatory cytokines (TNF-α, IL-6 and VCAM-1) by increasing the expression of CYP2J2/EETs and PPARα in HUVECs. Furthermore, treatment with exogenous 11,12-EET attenuated endothelial inflammation induced by Ang II as evidenced by inhibited NF-κB nuclear translocation, increased IκBα expression and decreased inflammation factor level. Finally, the activation of NF-κB nuclear translocation induced by Ang II was also markedly suppressed by fenofibrate. Co-incubation with 6-(2-proparglyloxyphenyl) hexanoic acid (PPOH) and PPARα inhibitor GW6471 before drug treatment abolished the endothelium protective effects of OP-D. Taken together, these data suggest that OP-D has the endothelial protective effect through activation of CYP2J and increasing EETs, and PPARα involves in this process.
[Mh] Termos MeSH primário: Ácido 8,11,14-Eicosatrienoico/farmacologia
Angiotensina II/farmacologia
Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos
Inflamação/tratamento farmacológico
PPAR alfa/metabolismo
Saponinas/farmacologia
Espirostanos/farmacologia
[Mh] Termos MeSH secundário: Ácido 8,11,14-Eicosatrienoico/análogos & derivados
Células Cultivadas
Células Endoteliais da Veia Umbilical Humana/metabolismo
Seres Humanos
Inflamação/induzido quimicamente
Inflamação/metabolismo
NF-kappa B/metabolismo
Transporte Proteico/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (NF-kappa B); 0 (PPAR alpha); 0 (Saponins); 0 (Spirostans); 11128-99-7 (Angiotensin II); 41753-55-3 (ophiopogonin D); 7324-41-6 (8,11,14-Eicosatrienoic Acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170608
[St] Status:MEDLINE


  2 / 460 MEDLINE  
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[PMID]:28038327
[Au] Autor:Wang W; Wang D; Wang Z; Yao G; Li X; Gao P; Li L; Zhang Y; Wang S; Song S
[Ad] Endereço:Department of Natural Products Chemistry, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery (Ministry of Education), Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
[Ti] Título:Synthesis of new sarsasapogenin derivatives with cytotoxicity and apoptosis-inducing activities in human breast cancer MCF-7 cells.
[So] Source:Eur J Med Chem;127:62-71, 2017 Feb 15.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Based on the fact that Timosaponin A-III, a saponin isolated from the rhizome of Anemarrhena asphodeloides, is a promising bioactive lead compound in the treatment of cancer, structural modification at the C3 and C26 positions of sarsasapogenin has always been the focus of our structure-activity investigations. In this paper, we describe the synthesis of a range of new derivatives 5a-5o and the evaluation of their antitumor activities in a panel of six human cancer cell lines using the MTT assay in vitro. The results obtained showed that compounds 5h, 5i, and 5n exhibited significant cytotoxic activities against the six cell lines, being more potent than their parent compound sarsasapogenin. Furthermore, the p-fluorobenzyloxy series of compounds generally exhibited stronger cytotoxicities against all the tested cancer cells compared with the benzyloxy and p-methoxybenzyloxy series, and the substitution of pyrrolidinyl and piperazinyl groups at the C26 position was the preferred option for these compounds to display antitumor activities. Compound 5n exhibited excellent cytotoxic activity against MCF-7 cell line (IC = 2.95 µM), and was 16.7-fold more potent than sarsasapogenin. Further studies of the cellular mechanism of 5n showed that it arrested MCF-7 cells at the G2/M phase and induced apoptosis and necrosis. All these results show that it is important to carry out structural modification of sarsasapogenin to obtain some promising derivatives with marked antitumor activities, and the representative compound 5n is a lead compound for further research.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Neoplasias da Mama/patologia
Desenho de Drogas
Espirostanos/síntese química
Espirostanos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/química
Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Técnicas de Química Sintética
Ensaios de Seleção de Medicamentos Antitumorais
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Células MCF-7
Espirostanos/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Spirostans); CFS802C28F (sarsasapogenin)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170221
[Lr] Data última revisão:
170221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161231
[St] Status:MEDLINE


  3 / 460 MEDLINE  
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[PMID]:27919659
[Au] Autor:Pan H; Van Khang P; Dong D; Wang R; Ma L
[Ad] Endereço:Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China.
[Ti] Título:Synthesis and SAR study of novel sarsasapogenin derivatives as potent neuroprotective agents and NO production inhibitors.
[So] Source:Bioorg Med Chem Lett;27(3):662-665, 2017 02 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Sarsasapogenin, isolated from rhizomes of Anemarrhena asphodeloides, was found to be able to enhance memory. On the basis of the structure of Sarsasapogenin, a series of derivatives were synthesized and evaluated for their neuroprotective activity in PC12 cells and NO production inhibitory activity in RAW264.7 cell lines. The preliminary structure-activity relationship of them indicated that introduction of carbamate groups at the 3-hydroxyl position of sarsasapogenin might improve neuroprotective activity. Some synthesized derivatives such as AA3, AA4, AA9 and AA13 exhibited both notably neuroprotective activity and NO production inhibitory activity.
[Mh] Termos MeSH primário: Fármacos Neuroprotetores/química
Espirostanos/química
[Mh] Termos MeSH secundário: Anemarrhena/química
Anemarrhena/metabolismo
Animais
Macrófagos/citologia
Macrófagos/efeitos dos fármacos
Macrófagos/metabolismo
Camundongos
Fármacos Neuroprotetores/isolamento & purificação
Fármacos Neuroprotetores/farmacologia
Óxido Nítrico/metabolismo
Células PC12
Células RAW 264.7
Ratos
Rizoma/metabolismo
Espirostanos/isolamento & purificação
Espirostanos/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Neuroprotective Agents); 0 (Spirostans); 31C4KY9ESH (Nitric Oxide); CFS802C28F (sarsasapogenin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161207
[St] Status:MEDLINE


  4 / 460 MEDLINE  
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[PMID]:27834098
[Au] Autor:Zhang H; Su YF; Yang FY; Gao XM
[Ad] Endereço:a Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology , Tianjin University , Tianjin , P.R. China.
[Ti] Título:New minor spirostanol glycosides from Helleborus thibetanus.
[So] Source:Nat Prod Res;31(8):925-931, 2017 Apr.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Phytochemical reinvestigation of the dried roots and rhizomes of Helleborus thibetanus afforded four new minor spirostanol glycosides (1-4) and four known spirostanol glycosides (5-8). Their structures were determined on the basis of spectroscopic analyses, including 1D and 2D NMR experiments, together with HR-ESI-MS and IR measurements and the results of acid hydrolysis.
[Mh] Termos MeSH primário: Glicosídeos/química
Helleborus/química
Espirostanos/química
[Mh] Termos MeSH secundário: Hidrólise
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Raízes de Plantas/química
Plantas Medicinais/química
Rizoma/química
Espectrometria de Massas por Ionização por Electrospray
Espirostanos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycosides); 0 (Spirostans); 0 (thibetanoside A); 0 (thibetanoside B); 0 (thibetanoside C)
[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:161112
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2016.1255888


  5 / 460 MEDLINE  
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[PMID]:27658357
[Au] Autor:Khang PV; Phuong DM; Ma L
[Ad] Endereço:a Faculty of Chemistry , Thai Nguyen University of Education , Thai Nguyen City 250000 , Viet Nam.
[Ti] Título:New steroids from Anemarrhena asphodeloides rhizome and their α-glucosidase inhibitory activity.
[So] Source:J Asian Nat Prod Res;19(5):468-473, 2017 May.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Two new steroids were isolated from acid hydrolysis residue of the rhizomes of Anemarrhena asphodeloides. Their structures were identified on the basis of several spectroscopic analysis approaches including 1D, 2D-NMR techniques, and MS data, and by the comparison of spectral data of the known compounds. The biological activities of these two isolated compounds were explored on α-glucosidase. Compound 1 displayed 4.7 folds inhibitory activity against α-glucosidase compared with the positive control acarbose.
[Mh] Termos MeSH primário: Anemarrhena/química
Medicamentos de Ervas Chinesas/isolamento & purificação
Medicamentos de Ervas Chinesas/farmacologia
Inibidores de Glicosídeo Hidrolases/isolamento & purificação
Inibidores de Glicosídeo Hidrolases/farmacologia
Plantas Medicinais/química
Rizoma/química
Saponinas/isolamento & purificação
Saponinas/farmacologia
Espirostanos/isolamento & purificação
Espirostanos/farmacologia
Esteroides/isolamento & purificação
Esteroides/farmacologia
alfa-Glucosidases/efeitos dos fármacos
[Mh] Termos MeSH secundário: Medicamentos de Ervas Chinesas/química
Inibidores de Glicosídeo Hidrolases/química
Estrutura Molecular
Saponinas/química
Espirostanos/química
Esteroides/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (21-formyl sarsasapogenin); 0 (21-hydroxysarsasapogenin); 0 (Drugs, Chinese Herbal); 0 (Glycoside Hydrolase Inhibitors); 0 (Saponins); 0 (Spirostans); 0 (Steroids); EC 3.2.1.20 (alpha-Glucosidases)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160924
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2016.1234459


  6 / 460 MEDLINE  
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[PMID]:27665149
[Au] Autor:Chen Y; Ni W; Yan H; Qin XJ; Khan A; Liu H; Shu T; Jin LY; Liu HY
[Ad] Endereço:State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China; University of Chinese Academy of Sciences, Beijing 100039, China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming, 650201, China.
[Ti] Título:Spirostanol glycosides with hemostatic and antimicrobial activities from Trillium kamtschaticum.
[So] Source:Phytochemistry;131:165-173, 2016 Nov.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ten spirostanol glycosides, trillikamtosides A-J, together with eleven known analogues, were isolated from the hemostatic fraction of the 75% aqueous EtOH extract of the whole herbs of Trillium kamtschaticum. Their structures were established by extensive spectroscopic data analysis and chemical methods. The aglycones of three of these compounds had unique 3ß,17α-dihydroxy-spirostanes featuring a double bond between C-4 and C-5, while two others represent a rare class of spirostanol glycosides which possess a 5(6 â†’ 7) abeo-steroidal aglycone. All the compounds were evaluated for their hemostatic and antimicrobial activities. Three of the spirostanol glycosides exhibited induced-platelet aggregation at a concentration of 300 µg/mL with maximal induced-platelet aggregation rates of 72%, 71%, and 62% in rabbits, respectively, and their EC values were 492.7, 203.3, and 109.8 µM. Five of the spirostanol glycosides showed an anti-Candida albicans effect with MIC values of 21.1, 10.6, 8.8, 21.6, and 11.0 µM, respectively.
[Mh] Termos MeSH primário: Anti-Infecciosos/isolamento & purificação
Glicosídeos/isolamento & purificação
Glicosídeos/farmacologia
Hemostáticos/isolamento & purificação
Hemostáticos/farmacologia
Espirostanos/isolamento & purificação
Espirostanos/farmacologia
Trillium/química
[Mh] Termos MeSH secundário: Anti-Infecciosos/química
Anti-Infecciosos/farmacologia
Candida albicans/efeitos dos fármacos
Relação Dose-Resposta a Droga
Glicosídeos/química
Hemostáticos/química
Agregação Plaquetária/efeitos dos fármacos
Espirostanos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Glycosides); 0 (Hemostatics); 0 (Spirostans)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170310
[Lr] Data última revisão:
170310
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160926
[St] Status:MEDLINE


  7 / 460 MEDLINE  
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[PMID]:27589720
[Au] Autor:Cao G; Jiang N; Hu Y; Zhang Y; Wang G; Yin M; Ma X; Zhou K; Qi J; Yu B; Kou J
[Ad] Endereço:Jiangsu Key Laboratory of Traditional Chinese Medicine Evaluation and Translational Research, Department of Complex Prescription of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing 211198, China. caoguosheng2006@163.com.
[Ti] Título:Ruscogenin Attenuates Cerebral Ischemia-Induced Blood-Brain Barrier Dysfunction by Suppressing TXNIP/NLRP3 Inflammasome Activation and the MAPK Pathway.
[So] Source:Int J Mol Sci;17(9), 2016 Aug 29.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, has been shown to inhibit cerebral ischemic injury. However, its potential molecular action on blood-brain barrier (BBB) dysfunction after stroke remains unclear. This study aimed to investigate the effects of ruscogenin on BBB dysfunction and the underlying mechanisms in middle cerebral artery occlusion/reperfusion (MCAO/R)-injured mice and oxygen-glucose deprivation/reoxygenation (OGD/R)-injured mouse brain microvascular endothelial cells (bEnd.3). The results demonstrated that administration of ruscogenin (10 mg/kg) decreased the brain infarction and edema, improved neurological deficits, increased cerebral brain flow (CBF), ameliorated histopathological damage, reduced evans blue (EB) leakage and upregulated the expression of tight junctions (TJs) in MCAO/R-injured mice. Meanwhile, ruscogenin (0.1-10 µM) treatment increased cell viability and trans-endothelial electrical resistance (TEER) value, decreased sodium fluorescein leakage, and modulated the TJs expression in OGD/R-induced bEnd.3 cells. Moreover, ruscogenin also inhibited the expression of interleukin-1ß (IL-1ß) and caspase-1, and markedly suppressed the expression of Nucleotide-binding domain (NOD)-like receptor family, pyrin domain containing 3 (NLRP3) and thiredoxin-interactive protein (TXNIP) in vivo and in vitro. Furthermore, ruscogenin decreased reactive oxygen species (ROS) generation and inhibited the mitogen-activated protein kinase (MAPK) pathway in OGD/R-induced bEnd.3 cells. Our findings provide some new insights into its potential application for the prevention and treatment of ischemic stroke.
[Mh] Termos MeSH primário: Anti-Inflamatórios/farmacologia
Antioxidantes/farmacologia
Barreira Hematoencefálica/efeitos dos fármacos
Infarto da Artéria Cerebral Média/tratamento farmacológico
Inflamassomos/metabolismo
Sistema de Sinalização das MAP Quinases
Espirostanos/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/uso terapêutico
Antioxidantes/uso terapêutico
Barreira Hematoencefálica/metabolismo
Proteínas de Transporte/metabolismo
Caspase 1/genética
Caspase 1/metabolismo
Hipóxia Celular
Linhagem Celular
Infarto da Artéria Cerebral Média/metabolismo
Inflamassomos/efeitos dos fármacos
Interleucina-1beta/genética
Interleucina-1beta/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo
Ophiopogon/química
Espécies Reativas de Oxigênio/metabolismo
Espirostanos/uso terapêutico
Tiorredoxinas/metabolismo
Junções Íntimas/efeitos dos fármacos
Junções Íntimas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antioxidants); 0 (Carrier Proteins); 0 (Inflammasomes); 0 (Interleukin-1beta); 0 (NLR Family, Pyrin Domain-Containing 3 Protein); 0 (Nlrp3 protein, mouse); 0 (Reactive Oxygen Species); 0 (Spirostans); 0 (Txnip protein, mouse); 52500-60-4 (Thioredoxins); BXI92R2VUJ (ruscogenin); EC 3.4.22.36 (Caspase 1)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170323
[Lr] Data última revisão:
170323
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160903
[St] Status:MEDLINE


  8 / 460 MEDLINE  
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[PMID]:27561715
[Au] Autor:Panda S; Kar A
[Ad] Endereço:School of Life Sciences, Devi Ahilya University, Indore 452017, India. Electronic address: spanda4@rediffmail.com.
[Ti] Título:Role of a gitogenin-type steroidal saponin (3-O-ß-d-glucopyranosyl (1→2)-ß-d-glucopyranosyl (1→4)-ß-d-galactopyranoside-25R,5α-spirostane-2α,3ß-diol), isolated from the leaves of Malvastrum coromandelianum in regulating thyrotoxicosis in rats.
[So] Source:Bioorg Med Chem Lett;26(19):4804-4807, 2016 10 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The hitherto unknown role of saponin in the regulation of thyrotoxicosis has been revealed in chemically-induced thyrotoxic rats. l-T4 (l-thyroxine) administration at pre-standardized dose of 500-µg/kg body weight for 12days increased the levels of thyroid hormones, enhanced the activity of hepatic 5'-monodeiodinase I (5'DI) and glucose-6-phosphatase (G-6Pase) as well as lipid peroxidation (LPO) with a parallel decrease in the levels of antioxidative enzymes. However, administration of the isolated saponin for 15days ameliorated the T4-induced alterations in serum thyroid hormones, hepatic LPO, G-6-Pase and 5'DI activity, and improved the cellular antioxidant status, indicating its antithyroidal and antioxidative potential. These effects of the test compound were comparable to a reference antithyroid drug, Propylthiouracil (PTU), suggesting that the test saponin may act as a potent anti-thyroid agent.
[Mh] Termos MeSH primário: Antitireóideos/uso terapêutico
Malvaceae/química
Folhas de Planta/química
Espirostanos/uso terapêutico
Tireotoxicose/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antitireóideos/química
Antitireóideos/isolamento & purificação
Feminino
Ratos
Espirostanos/química
Espirostanos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antithyroid Agents); 0 (Spirostans); 60ZMY8IH51 (gitogenin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160827
[St] Status:MEDLINE


  9 / 460 MEDLINE  
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[PMID]:27455578
[Au] Autor:Islamova ZhI; Khushbaktova ZA; Abdullaev ND; Syrov VN
[Ti] Título:[STEROIDAL GENINS AND GLYCOSIDES OF SPIROSTAN AND FUROSTAN SERIES AS ANTHELMINTHIC AGENTS].
[So] Source:Eksp Klin Farmakol;79(3):41-4, 2016.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:It was established that steroidal genins and their glycosides of the spirostan series and (especially) furostan series show anticestodal activity against Hymeiolepis nana species. Search for anthelminthic agents in the indicated series of compounds is a promising direction of research.
[Mh] Termos MeSH primário: Anticestoides/farmacologia
Glicosídeos/farmacologia
Himenolepíase/tratamento farmacológico
Hymenolepis nana/efeitos dos fármacos
Espirostanos/farmacologia
Esteróis/farmacologia
[Mh] Termos MeSH secundário: Allium/química
Animais
Anticestoides/isolamento & purificação
Glicosídeos/isolamento & purificação
Himenolepíase/parasitologia
Hymenolepis nana/fisiologia
Lycopersicon esculentum/química
Masculino
Camundongos
Contagem de Ovos de Parasitas
Testes de Sensibilidade Parasitária
Praziquantel/farmacologia
Espirostanos/isolamento & purificação
Esteróis/isolamento & purificação
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anticestodal Agents); 0 (Glycosides); 0 (Spirostans); 0 (Sterols); 0 (furostanol glycoside); 6490C9U457 (Praziquantel)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:160726
[Lr] Data última revisão:
160726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160727
[St] Status:MEDLINE


  10 / 460 MEDLINE  
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[PMID]:27394958
[Au] Autor:Zhang X; Xue X; Zhao J; Guo Z; Ito Y; Sun W
[Ad] Endereço:College of Pharmacy, Xi'an Jiaotong Univeristy, Xi'an 710061, China.
[Ti] Título:Quantitative determination of gracillin by HPLC-MS/MS after oral administration and its application to a pharmacokinetic study.
[So] Source:Steroids;113:78-86, 2016 Sep.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A sensitive and credible high performance liquid chromatography hyphenated to mass spectrometry (HPLC-MS/MS) was established to quantify the concentration of gracillin in rat plasma. The plasma samples were subjected to a direct protein precipitation process with acetonitrile as a precipitant in a single-step. Ginsenoside Rb1 was selected as an internal standard (IS). The chromatographic separation of analyte and IS were carried out on an Inersil ODS-3 C18 column (250×4.6mm, 5µm) with a binary solvent system containing acetonitrile and 0.1% formic acid in water at a flow rate of 1mLmin(-1) under a gradient elution mode. Mass spectrometric detection was performed on a triple quadrupole tandem mass spectrometer by the multiple reaction monitoring (MRM) mode to examine the precursor-to-daughter ion transitions of 1110.3→948.2 for IS and 886.1→739.9 for gracillin, respectively, in a positive electrospray ionization mode. The calibration curve showed a promising linearity over a concentration range of 0.065-800ngmL(-1) with a better regression coefficient of r(2)=0.9960. The intra- and inter-day precisions (as relative standard deviation) of the assay at three quality control levels were all less than 3.48%, while the intra- and inter-day accuracies (as relative error) ranged from -8.43% to 9.74%, whose data were within the acceptable limits. The mean extraction recoveries of analyte from rat plasma were all more than 74.11%, and no notable matrix effect was observed. Stability experiments revealed that gracillin remained stable throughout the analytical procedure under various stored conditions. The above validated method was successfully used to investigate the pharmacokinetic behaviors of gracillin orally administrated to rats at three proportion doses. The pharmacokinetic analysis would pave the way for understanding the pharmacological actions and provide a meaningful foundation for further development and application in preclinical and clinical use of gracillin in the near future.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Espirostanos/análise
Espirostanos/farmacocinética
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Administração Oral
Animais
Masculino
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Espirostanos/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Spirostans); 19083-00-2 (gracillin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170705
[Lr] Data última revisão:
170705
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160711
[St] Status:MEDLINE



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