Base de dados : MEDLINE
Pesquisa : D03.132.052 [Categoria DeCS]
Referências encontradas : 428 [refinar]
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[PMID]:28898076
[Au] Autor:Zhan G; Zhou J; Liu J; Huang J; Zhang H; Liu R; Yao G
[Ad] Endereço:Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology , Wuhan 430030, People's Republic of China.
[Ti] Título:Acetylcholinesterase Inhibitory Alkaloids from the Whole Plants of Zephyranthes carinata.
[So] Source:J Nat Prod;80(9):2462-2471, 2017 Sep 22.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Eleven new alkaloids (1-11), classified as the 12-acetylplicamine (1), N-deformyl-seco-plicamine (2), plicamine (3-6), 4a-epi-plicamine (7), seco-plicamine (8), and lycorine (9-11) framework types, along with 15 known alkaloids (12-26) were isolated from the whole plants of Zephyranthes carinata. The structures of the new alkaloids 1-11 were established by extensive spectroscopic data interpretation. The absolute configurations of 9 and 10 were defined by single-crystal X-ray diffraction analysis. Zephycarinatines A (1), B (2), and G (7) represent the first examples of 12-acetylplicamine, N-deformyl-seco-plicamine, and 4a-epi-plicamine alkaloids, respectively. Alkaloids 6, 11, 17, and 20-23 exhibited AChE inhibitory activities with IC values ranging from 1.21 to 184.05 µM, and a preliminary structure-activity relationship is discussed.
[Mh] Termos MeSH primário: Acetilcolinesterase/isolamento & purificação
Acetilcolinesterase/metabolismo
Alcaloides/isolamento & purificação
Alcaloides/farmacologia
Alcaloides de Amaryllidaceae/isolamento & purificação
Alcaloides de Amaryllidaceae/farmacologia
Amaryllidaceae/química
Inibidores da Colinesterase/isolamento & purificação
Inibidores da Colinesterase/farmacologia
Compostos Heterocíclicos de 4 ou mais Anéis/isolamento & purificação
Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia
Liliaceae/química
Fenantridinas/isolamento & purificação
Fenantridinas/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Alcaloides/química
Alcaloides de Amaryllidaceae/química
Inibidores da Colinesterase/química
Compostos Heterocíclicos de 4 ou mais Anéis/química
Concentração Inibidora 50
Estrutura Molecular
Fenantridinas/química
Relação Estrutura-Atividade
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Amaryllidaceae Alkaloids); 0 (Cholinesterase Inhibitors); 0 (Heterocyclic Compounds, 4 or More Rings); 0 (Phenanthridines); 0 (Zephycarinatine G); 0 (plicamine); 0 (zephycarinatine A); 0 (zephycarinatine B); EC 3.1.1.7 (Acetylcholinesterase); I9Q105R5BU (lycorine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170913
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00301


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[PMID]:28820699
[Au] Autor:Saidin S; Othman N; Noordin R
[Ad] Endereço:Institute for Research in Molecular Medicine, Universiti Sains Malaysia, USM, Penang, Malaysia.
[Ti] Título:In Vitro Testing of Potential Pyruvate Phosphate Dikinase Inhibitors.
[So] Source:Am J Trop Med Hyg;97(4):1204-1213, 2017 Oct.
[Is] ISSN:1476-1645
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Adverse effects and resistance to metronidazole have motivated the search for new antiamoebic agents against . Control of amoeba growth may be achieved by inhibiting the function of the glycolytic enzyme and pyruvate phosphate dikinase (PPDK). In this study, we screened 10 compounds using an in vitro PPDK enzyme assay. These compounds were selected from a virtual screening of compounds in the National Cancer Institute database. The antiamoebic activity of the selected compounds was also evaluated by determining minimal inhibitory concentrations (MICs) and IC values using the nitro-blue tetrazolium reduction assay. Seven of the 10 compounds showed inhibitory activities against the adenosine triphosphate (ATP)/inorganic phosphate binding site of the ATP-grasp domain. Two compounds, NSC349156 (pancratistatin) and NSC228137 (7-ethoxy-4-[4-methylphenyl] sulfonyl-3-oxido-2, 1, 3-benzoxadiazol-3-ium), exhibited inhibitory effects on the growth of trophozoites with MIC values of 25 and 50 µM, and IC values of 14 and 20.7 µM, respectively.
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/farmacologia
Entamoeba histolytica/efeitos dos fármacos
Entamoeba histolytica/enzimologia
Inibidores Enzimáticos/farmacologia
Isoquinolinas/farmacologia
Oxidiazóis/farmacologia
Piruvato Ortofosfato Diquinase/antagonistas & inibidores
Sulfonas/farmacologia
[Mh] Termos MeSH secundário: Alcaloides de Amaryllidaceae/química
Concentração Inibidora 50
Isoquinolinas/química
Testes de Sensibilidade Microbiana
Estrutura Molecular
Oxidiazóis/química
Piruvato Ortofosfato Diquinase/genética
Piruvato Ortofosfato Diquinase/metabolismo
Sulfonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Enzyme Inhibitors); 0 (Isoquinolines); 0 (NSC228137); 0 (Oxadiazoles); 0 (Sulfones); 96281-31-1 (pancratistatin); EC 2.7.9.1 (Pyruvate, Orthophosphate Dikinase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170819
[St] Status:MEDLINE
[do] DOI:10.4269/ajtmh.17-0132


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[PMID]:28581297
[Au] Autor:Varró G; Hegedus L; Simon A; Balogh A; Grün A; Leveles I; Vértessy BG; Kádas I
[Ad] Endereço:Department of Organic Chemistry and Technology, Budapest University of Technology and Economics , Budafoki út 8, H-1111 Budapest, Hungary.
[Ti] Título:The First Enantioselective Total Synthesis of (-)-trans-Dihydronarciclasine.
[So] Source:J Nat Prod;80(6):1909-1917, 2017 Jun 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A feasible and enantioselective total synthesis of (-)-trans-dihydronarciclasine [(-)-1], a highly biologically active alkaloid, was devised starting from vanillin (8). The key step of this new synthesis was an asymmetric, organocatalytic Michael addition, in which an optically active nitropentanone [(-)-13] was obtained from a butenone derivative (12). Excellent enantioselectivity (>99% ee) was achieved using the (8S,9S)-9-amino(9-deoxy)epiquinine (16) organocatalyst. The target molecule can be prepared in 13 steps from compound (-)-13. The total synthesis has provided a facile and first access to the ent-form of naturally occurring (+)-trans-dihydronarciclasine, a highly potent cytostatic alkaloid.
[Mh] Termos MeSH primário: Alcaloides/síntese química
Alcaloides de Amaryllidaceae/síntese química
[Mh] Termos MeSH secundário: Alcaloides/química
Alcaloides de Amaryllidaceae/química
Catálise
Cristalografia por Raios X
Estrutura Molecular
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Amaryllidaceae Alkaloids); 40042-08-8 (dihydronarciclasine)
[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:170606
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.7b00208


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[PMID]:28441543
[Au] Autor:Sun S; Wei Y; Cao Y; Deng B
[Ad] Endereço:Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China.
[Ti] Título:Simultaneous electrochemiluminescence determination of galanthamine, homolycorine, lycorenine, and tazettine in Lycoris radiata by capillary electrophoresis with ultrasonic-assisted extraction.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1055-1056:15-19, 2017 Jun 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:After ultrasonic-assisted extraction, four lycoris radiata alkaloids: galanthamine, homolycorine, lycorenine, and tazettine were determined by capillary electrophoresis electrochemiluminescence. Polyvinylpyrrolidone was added to the running buffer (RB) to obtain better resolution. Experimental conditions influencing the determination were examined, including the additives, detection potential, separation voltage, injection voltage and time, and RB pH and concentration. Under optimal experimental conditions, the baseline separation of the four alkaloids occurred within 16min. The proposed method displayed the following linear ranges (in ng/mL): galanthamine [60-5000], homolycorine [40-5000], lycorenine [5.0-1500], and tazettine [8.0-2500]. The detection limits in ng/mL, (S/N=3), were galanthamine [14], homolycorine [11], lycorenine [1.8], and tazettine [3.1]. Intra-day and inter-day RSDs for the four alkaloids of the six replicates were less than 2.7% and 3.1%, respectively. The recoveries in% were: tazettine [102.5], lycorenine [98.20], galanthamine [97.30], and homolycorine [98.33].
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/análise
Eletroforese Capilar/métodos
Galantamina/análise
Medições Luminescentes/métodos
Lycoris/química
[Mh] Termos MeSH secundário: Alcaloides de Amaryllidaceae/isolamento & purificação
Tampões (Química)
Eletroforese Capilar/economia
Galantamina/isolamento & purificação
Limite de Detecção
Medições Luminescentes/economia
Extratos Vegetais/química
Povidona/química
Sonicação/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Buffers); 0 (Plant Extracts); 0D3Q044KCA (Galantamine); 477-19-0 (lycorenine); 477-20-3 (homolycorine); 76WEU12CSO (tazettine); FZ989GH94E (Povidone)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170426
[St] Status:MEDLINE


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[PMID]:28416753
[Au] Autor:Li X; Xu P; Wang C; Xu N; Xu A; Xu Y; Sadahira T; Araki M; Wada K; Matsuura E; Watanabe M; Zheng J; Sun P; Huang P; Nasu Y; Liu C
[Ad] Endereço:Department of Urology, Zhujiang Hospital, Southern Medical University, Guangzhou, China.
[Ti] Título:Synergistic effects of the immune checkpoint inhibitor CTLA-4 combined with the growth inhibitor lycorine in a mouse model of renal cell carcinoma.
[So] Source:Oncotarget;8(13):21177-21186, 2017 Mar 28.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Renal cell carcinoma (RCC) management has undergone a major transformation over the past decade; immune checkpoint inhibitors are currently undergoing clinical trials and show promising results. However, the effectiveness of immune checkpoint inhibitors in patients with metastatic RCC (mRCC) is still limited. Lycorine, an alkaloid extracted from plants of the Amaryllidaceae family, is touted as a potential anti-cancer drug because of its demonstrative growth inhibition capacity (induction of cell cycle arrest and inhibition of vasculogenic mimicry formation). Moreover, T cell checkpoint blockade therapy with antibodies targeting cytotoxic T-lymphocyte associated protein 4 (CTLA-4) has improved outcomes in cancer patients. However, the anti-tumor efficacy of combined lycorine and anti-CTLA-4 therapy remains unknown. Thus, we investigated a combination therapy of lycorine hydrochloride and anti-CTLA-4 using a murine RCC model. As a means of in vitro confirmation, we found that lycorine hydrochloride inhibited the viability of various RCC cell lines. Furthermore, luciferase-expressing Renca cells were implanted in the left kidney and the lung of BALB/c mice to develop a RCC metastatic mouse model. Lycorine hydrochloride and anti-CTLA-4 synergistically decreased tumor weight, lung metastasis, and luciferin-staining in tumor images. Importantly, the observed anti-tumor effects of this combination were dependent on significantly suppressing regulatory T cells while upregulating effector T cells; a decrease in regulatory T cells by 31.43% but an increase in effector T cells by 31.59% were observed in the combination group compared with those in the control group). We suggest that a combination of lycorine hydrochloride and anti-CTLA-4 is a viable therapeutic option for RCC patients.
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/farmacologia
Anticorpos Monoclonais/farmacologia
Antineoplásicos/farmacologia
Antígeno CTLA-4/antagonistas & inibidores
Carcinoma de Células Renais/terapia
Inibidores do Crescimento/farmacologia
Fenantridinas/farmacologia
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Alcaloides de Amaryllidaceae/uso terapêutico
Animais
Anticorpos Monoclonais/uso terapêutico
Antineoplásicos/uso terapêutico
Carcinoma de Células Renais/tratamento farmacológico
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Terapia Combinada
Sinergismo Farmacológico
Feminino
Inibidores do Crescimento/uso terapêutico
Seres Humanos
Fatores Imunológicos/farmacologia
Fatores Imunológicos/uso terapêutico
Imunoterapia/métodos
Camundongos
Camundongos Endogâmicos BALB C
Neoplasias Experimentais
Fenantridinas/uso terapêutico
Extratos Vegetais/uso terapêutico
Subpopulações de Linfócitos T/efeitos dos fármacos
Subpopulações de Linfócitos T/imunologia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Antibodies, Monoclonal); 0 (Antineoplastic Agents); 0 (CTLA-4 Antigen); 0 (Ctla4 protein, mouse); 0 (Growth Inhibitors); 0 (Immunologic Factors); 0 (Phenanthridines); 0 (Plant Extracts); I9Q105R5BU (lycorine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170524
[Lr] Data última revisão:
170524
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170419
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.15505


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[PMID]:28207742
[Au] Autor:Julien SG; Kim SY; Brunmeir R; Sinnakannu JR; Ge X; Li H; Ma W; Yaligar J; Kn BP; Velan SS; Röder PV; Zhang Q; Sim CK; Wu J; Garcia-Miralles M; Pouladi MA; Xie W; McFarlane C; Han W; Xu F
[Ad] Endereço:Singapore Institute for Clinical Sciences, Agency for Science, Technology and Research (A*STAR), Singapore, Republic of Singapore.
[Ti] Título:Narciclasine attenuates diet-induced obesity by promoting oxidative metabolism in skeletal muscle.
[So] Source:PLoS Biol;15(2):e1002597, 2017 Feb.
[Is] ISSN:1545-7885
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Obesity develops when caloric intake exceeds metabolic needs. Promoting energy expenditure represents an attractive approach in the prevention of this fast-spreading epidemic. Here, we report a novel pharmacological strategy in which a natural compound, narciclasine (ncls), attenuates diet-induced obesity (DIO) in mice by promoting energy expenditure. Moreover, ncls promotes fat clearance from peripheral metabolic tissues, improves blood metabolic parameters in DIO mice, and protects these mice from the loss of voluntary physical activity. Further investigation suggested that ncls achieves these beneficial effects by promoting a shift from glycolytic to oxidative muscle fibers in the DIO mice thereby enhancing mitochondrial respiration and fatty acid oxidation (FAO) in the skeletal muscle. Moreover, ncls strongly activates AMPK signaling specifically in the skeletal muscle. The beneficial effects of ncls treatment in fat clearance and AMPK activation were faithfully reproduced in vitro in cultured murine and human primary myotubes. Mechanistically, ncls increases cellular cAMP concentration and ADP/ATP ratio, which further lead to the activation of AMPK signaling. Blocking AMPK signaling through a specific inhibitor significantly reduces FAO in myotubes. Finally, ncls also enhances mitochondrial membrane potential and reduces the formation of reactive oxygen species in cultured myotubes.
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/farmacologia
Alcaloides de Amaryllidaceae/uso terapêutico
Dieta/efeitos adversos
Músculo Esquelético/metabolismo
Obesidade/tratamento farmacológico
Obesidade/metabolismo
Fenantridinas/farmacologia
Fenantridinas/uso terapêutico
[Mh] Termos MeSH secundário: Proteínas Quinases Ativadas por AMP/metabolismo
Difosfato de Adenosina/metabolismo
Trifosfato de Adenosina/metabolismo
Animais
Biomarcadores/metabolismo
Respiração Celular/efeitos dos fármacos
Células Cultivadas
AMP Cíclico/metabolismo
Dieta Hiperlipídica
Metabolismo Energético/efeitos dos fármacos
Ativação Enzimática/efeitos dos fármacos
Ácidos Graxos/metabolismo
Seres Humanos
Masculino
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos C57BL
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/metabolismo
Fibras Musculares Esqueléticas/efeitos dos fármacos
Fibras Musculares Esqueléticas/metabolismo
Fibras Musculares de Contração Lenta/efeitos dos fármacos
Fibras Musculares de Contração Lenta/metabolismo
Músculo Esquelético/efeitos dos fármacos
Oxirredução/efeitos dos fármacos
Condicionamento Físico Animal
Substâncias Protetoras/farmacologia
Substâncias Protetoras/uso terapêutico
Espécies Reativas de Oxigênio/metabolismo
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Biomarkers); 0 (Fatty Acids); 0 (Phenanthridines); 0 (Protective Agents); 0 (Reactive Oxygen Species); 29477-83-6 (narciclasine); 61D2G4IYVH (Adenosine Diphosphate); 8L70Q75FXE (Adenosine Triphosphate); E0399OZS9N (Cyclic AMP); EC 2.7.11.31 (AMP-Activated Protein Kinases)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170217
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pbio.1002597


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[PMID]:28042037
[Au] Autor:Wang C; Wang Q; Li X; Jin Z; Xu P; Xu N; Xu A; Xu Y; Zheng S; Zheng J; Liu C; Huang P
[Ad] Endereço:Department of Urology, Zhujiang Hospital, Southern Medical University, Guangzhou, China.
[Ti] Título:Lycorine induces apoptosis of bladder cancer T24 cells by inhibiting phospho-Akt and activating the intrinsic apoptotic cascade.
[So] Source:Biochem Biophys Res Commun;483(1):197-202, 2017 Jan 29.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Lycorine, an alkaloid extracted from Amaryllidaceae genera, exhibits antitumor activities against several human solid-tumor and leukemia cells with extensive influence on various cell signaling molecules. However, the effect of lycorine on bladder cancer has not yet been investigated. In this study, we demonstrated that lycorine induced apoptosis in human bladder cancer T24 cells, an effect that is mediated via inhibition of phospho-Akt expression and the consequent activation of caspase-3 and Bax in vitro. In an in vivo experiment, T24 cells were subcutaneously implanted in the right rear flank of nu/nu mice. Lycorine treatment for 14 days significantly inhibited tumor growth compared with that in controls. Collectively, our findings suggest that lycorine suppressed the Akt pathway and activated the intrinsic apoptotic cascade, leading to the apoptosis of bladder cancer cells. We suggest that lycorine can be a viable therapeutic option for bladder cancer patients.
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/farmacologia
Apoptose/efeitos dos fármacos
Fenantridinas/farmacologia
Proteínas Proto-Oncogênicas c-akt/metabolismo
Neoplasias da Bexiga Urinária/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/farmacologia
Caspase 3/metabolismo
Linhagem Celular
Linhagem Celular Tumoral
Feminino
Seres Humanos
Camundongos Nus
PTEN Fosfo-Hidrolase/metabolismo
Proteínas Proto-Oncogênicas c-akt/genética
Bexiga Urinária/citologia
Neoplasias da Bexiga Urinária/metabolismo
Neoplasias da Bexiga Urinária/patologia
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Antineoplastic Agents, Phytogenic); 0 (Phenanthridines); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EC 3.1.3.67 (PTEN Phosphohydrolase); EC 3.1.3.67 (PTEN protein, human); EC 3.4.22.- (Caspase 3); I9Q105R5BU (lycorine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170601
[Lr] Data última revisão:
170601
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170103
[St] Status:MEDLINE


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[PMID]:27903551
[Au] Autor:Chen T; Li W; Gong T; Fu Y; Ding R; Gong T; Zhang Z
[Ad] Endereço:Key laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China.
[Ti] Título:Analysis of Lycobetaine in Rat Plasma by LC-ESI-MS/MS.
[So] Source:J Chromatogr Sci;55(3):301-308, 2017 03 01.
[Is] ISSN:1945-239X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In this study, a selective and sensitive liquid chromatography-electrospray ionization-tandem mass spectrometric method was developed and validated for the determination of lycobetaine in rat plasma. Berberine was selected as the internal standard, and rat plasma samples were pretreated via protein precipitation and further separated on a diamonsil octadecyl-silylated silica column using 0.2% (v/v) aqueous formic acid and methanol as the mobile phase. Selected reaction monitoring was performed using the transitions m/z 266.1 → 208.1 and m/z 336.1 → 320.0 to determine the concentrations of lycobetaine and internal standard, respectively. The injection volume was 1 µL, and the calibration curve was linear (R2 = 0.9998), while the validated lower limit of quantification was 25 ng/mL. Precision varied from 3.4% to 9.9%, and accuracy varied from -2.6% to 8.7%. Lycobetaine remained stable under all relevant analytical conditions tested in the study. The method was successfully applied to determine the plasma concentration of lycobetaine in a pharmacokinetic study. After intravenous administration of 10 mg/kg and oral administration of 200 mg/kg lycobetaine in rats, the pharmacokinetic parameters were calculated and the oral bioavailability of lycobetaine was determined as 7.30% ± 1.44%.
[Mh] Termos MeSH primário: Alcaloides de Amaryllidaceae/sangue
Cromatografia Líquida/métodos
Indolizinas/sangue
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Administração Intravenosa
Administração Oral
Alcaloides de Amaryllidaceae/química
Alcaloides de Amaryllidaceae/farmacocinética
Animais
Berberina/análise
Disponibilidade Biológica
Estabilidade de Medicamentos
Indolizinas/química
Indolizinas/farmacocinética
Modelos Lineares
Masculino
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
Espectrometria de Massas por Ionização por Electrospray/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Indolizines); 0I8Y3P32UF (Berberine); 2121-12-2 (ungeremine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161202
[St] Status:MEDLINE
[do] DOI:10.1093/chromsci/bmw185


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[PMID]:27864138
[Au] Autor:Masi M; van der Westhuyzen AE; Tabanca N; Evidente M; Cimmino A; Green IR; Bernier UR; Becnel JJ; Bloomquist JR; van Otterlo WA; Evidente A
[Ad] Endereço:Department of Chemical Sciences, University of Naples "Federico II", Complesso Universitario Monte S. Angelo, Via Cintia 4, 80126 Napoli, Italy.
[Ti] Título:Sarniensine, a mesembrine-type alkaloid isolated from Nerine sarniensis, an indigenous South African Amaryllidaceae, with larvicidal and adulticidal activities against Aedes aegypti.
[So] Source:Fitoterapia;116:34-38, 2017 Jan.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A new mesembrine-type alkaloid, named sarniensine, was isolated together with tazettine, lycorine, the main alkaloid, and 3-epimacronine from Nerine sarniensis, with the last two produced for the first time by this plant. This Amaryllidaceae, which is indigenous of South Africa, was investigated for its alkaloid content, because the organic extract of its bulbs showed strong larvicidal activity with an LC value of 0.008µgµL against first instar Aedes aegypti larvae and with an LD value 4.6µg/mosquito against adult female Ae. aegypti, which is the major vector for dengue, yellow fever and the Zika virus. The extract did not show repellency at MED value of 0.375mgcm against adult Ae. aegypti. Sarniensine was characterized using spectroscopic and chiroptical methods as (3aR,4Z,6S,7aS)-6-methoxy-3a-(2'-methoxymethyl-benzo [1,3]dioxol-1'-yl)-1-methyl-2,3,3a,6,7,7a-hexahydro-1H-indole. It was less effective against larva at the lowest concentration of 0.1µgµL , however it showed strong adulticidal activity with an LD value of 1.38±0.056µgmosquito .
[Mh] Termos MeSH primário: Aedes
Amaryllidaceae/química
Alcaloides de Indol/química
Inseticidas/química
Extratos Vegetais/química
[Mh] Termos MeSH secundário: Alcaloides de Amaryllidaceae/química
Alcaloides de Amaryllidaceae/isolamento & purificação
Animais
Alcaloides de Indol/isolamento & purificação
Inseticidas/isolamento & purificação
Larva
Estrutura Molecular
Fenantridinas/química
Fenantridinas/isolamento & purificação
Raízes de Plantas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-epimacronine); 0 (Amaryllidaceae Alkaloids); 0 (Indole Alkaloids); 0 (Insecticides); 0 (Phenanthridines); 0 (Plant Extracts); 0 (sarniensine); 76WEU12CSO (tazettine); 86E2ZU4ETY (mesembrine); I9Q105R5BU (lycorine)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170118
[Lr] Data última revisão:
170118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161120
[St] Status:MEDLINE


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[PMID]:27823880
[Au] Autor:Zhan G; Liu J; Zhou J; Sun B; Aisa HA; Yao G
[Ad] Endereço:Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People's Republic of China.
[Ti] Título:Amaryllidaceae alkaloids with new framework types from Zephyranthes candida as potent acetylcholinesterase inhibitors.
[So] Source:Eur J Med Chem;127:771-780, 2017 Feb 15.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Three new Amaryllidaceae alkaloids, named zephycandidines I-III (1-3), were isolated from Zephyranthes candida. The structures of 1-3 were elucidated by spectroscopic analyses including HRESIMS, H NMR, C NMR, DEPT, HSQC, H- H COSY, HMBC, ROESY, and electronic circular dichroism (ECD), as well as ECD calculation. The absolute configuration of 1 was finally established by single crystal X-ray diffraction using Cu Kα radiation. Zephycandidines I (1) and III (3) with new framework types represent the first example of 7-phenyl-hexahydroindole and 5,2'-dimethyl-biphenyl-2-ylamine alkaloids, respectively, and their plausible biosynthetic pathway are proposed. Zephycandidine II (2) is the first C3a-phenyl-hexahydroindole type alkaloid isolated from the genus of Zephyranthes. These new alkaloids 1-3 were evaluated for their acetylcholinesterase (AChE) inhibitory activities, and 3 showed potent AChE inhibitory activity with an IC value of 8.82 µM, suggesting that the framework of 5,2'-dimethyl-biphenyl-2-ylamine in 3 may be a potential group for the AChE inhibitory activity. The docking studies of 1-3 and galanthamine with AChE revealed that interactions with W286 and Y337 are necessary for the AChE inhibitory activity.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Alcaloides de Amaryllidaceae/farmacologia
Amaryllidaceae/química
Inibidores da Colinesterase/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Alcaloides de Amaryllidaceae/química
Alcaloides de Amaryllidaceae/metabolismo
Animais
Inibidores da Colinesterase/química
Inibidores da Colinesterase/metabolismo
Electrophorus
Simulação de Acoplamento Molecular
Conformação Proteica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amaryllidaceae Alkaloids); 0 (Cholinesterase Inhibitors); EC 3.1.1.7 (Acetylcholinesterase)
[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:161109
[St] Status:MEDLINE



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