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Pesquisa : D03.132.098.057.100 [Categoria DeCS]
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[PMID]:29276980
[Au] Autor:Zhang H; Gao L; Shu M; Liu J; Yu B
[Ad] Endereço:Jiangsu Provincial Key Laboratory for TCM Evaluation and Translational Development, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
[Ti] Título:Development of a highly sensitive and specific ELISA method for the determination of l-corydalmine in SD rats with monoclonal antibody.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1073:163-169, 2018 Jan 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:l-Corydalmine (l-CDL) is a potent analgesic constituent of the traditional Chinese medicine, Rhizoma Corydalis. However, the pharmacokinetic process and tissue distribution of l-CDL in vivo are still unknown. Therefore, it is necessary to establish a simple and sensitive method to detect l-CDL, which will be helpful to study its distribution and pharmacokinetic process. To determine this compound in biological samples, a monoclonal antibody (mAb) against l-CDL was produced and a fast and highly sensitive indirect competitive enzyme-linked immunosorbent assay (icELISA) was developed in this study. The icELISA was applied to determine l-CDL in biological samples. The limit of detection (LOD) of the method was 0.015 ng/mL with a liner range of 1-1000 ng/mL (R = 0.9912). The intra- and inter-day precision were below 15% and the recoveries were within 80-117%. Finally, the developed immunoassay was successfully applied to the analysis of the distribution of l-CDL in SD rats. In conclusion, the icELISA based on the anti-l-CDL mAb could be considered as a highly sensitive and rapid method for the determination of l-CDL in biological samples. The ELISA approach may provide a valuable tool for the analysis of small molecules in biological samples.
[Mh] Termos MeSH primário: Anticorpos Monoclonais/metabolismo
Berberina/análogos & derivados
Ensaio de Imunoadsorção Enzimática/métodos
[Mh] Termos MeSH secundário: Animais
Berberina/análise
Berberina/química
Berberina/farmacocinética
Cromatografia Líquida de Alta Pressão
Limite de Detecção
Modelos Lineares
Fígado/química
Fígado/metabolismo
Miocárdio/química
Miocárdio/metabolismo
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Monoclonal); 0I8Y3P32UF (Berberine); 30413-84-4 (corydalmine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171226
[St] Status:MEDLINE


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[PMID]:29232416
[Au] Autor:More NV; Kharat KR; Kharat AS
[Ad] Endereço:Department of Biotechnology, Dr. Babasaheb Ambedkar Marathwada University, Subcampus, Osmanabad 413501, Maharashtra, India.
[Ti] Título:Berberine from Argemone mexicana L exhibits a broadspectrum antibacterial activity.
[So] Source:Acta Biochim Pol;64(4):653-660, 2017.
[Is] ISSN:1734-154X
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:The Argemone mexicana L, commonly found on desolate land in the Marathwada region of Maharashtra state, India, has been used for treating oral cavity infections. We sought to investigate the antimicrobial potential of A. mexicana L. In this study, cold aqueous and methanolic extracts were prepared from the A. mexicana L leaves. These extracts were tested for their antibacterial activities against selected bacterial isolates. The antibacterial activity and MICs were tested using the agar well diffusion method and broth dilution method, respectively. The cold aqueous and methanolic extracts of A. mexicana L leaves inhibited growth of clinical isolates of Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa.The antibacterial potentiality of A. mexicana L extracts was compared with Streptomycin - the reference antibiotic used in this study. The active ingredient of antibacterial potentiality within the A. mexicana L extract was purified and characterized by TLC, HPLC and NMR analysis. Structural elucidation of Berberine and its bioactivity both, from the A. mexicana L and commercial preparation, is investigated.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Argemone/química
Berberina/farmacologia
Extratos Vegetais/química
[Mh] Termos MeSH secundário: Antibacterianos/química
Berberina/isolamento & purificação
Cromatografia Líquida de Alta Pressão
Cromatografia em Camada Delgada
Escherichia coli/efeitos dos fármacos
Espectroscopia de Ressonância Magnética
Testes de Sensibilidade Microbiana
Extratos Vegetais/análise
Extratos Vegetais/farmacologia
Folhas de Planta/química
Pseudomonas aeruginosa/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Plant Extracts); 0I8Y3P32UF (Berberine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE
[do] DOI:10.18388/abp.2017_1621


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[PMID]:29177319
[Au] Autor:Li ZQ; Liao TC; Dong C; Yang JW; Chen XJ; Liu L; Luo Y; Liang YY; Chen WH; Zhou CQ
[Ad] Endereço:Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, P. R. China. whchen@smu.edu.cn zcqlg@smu.edu.cn.
[Ti] Título:Specifically targeting mixed-type dimeric G-quadruplexes using berberine dimers.
[So] Source:Org Biomol Chem;15(48):10221-10229, 2017 Dec 13.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Three polyether-tethered berberine dimers (1a-c) were studied for their binding affinity, selectivity and thermal stabilization towards human telomeric dimeric quadruplex DNA (G2T1). Compound 1a with the shortest polyether linker showed the highest affinity (K > 10 M ) and 76-508-fold higher selectivity for mixed-type G2T1 over antiparallel G2T1 and three monomeric G-quadruplexes, which are human telomeric monomeric quadruplex G1, c-kit 1 and c-kit 2. Compound 1a induced the formation of quadruplex structures and showed higher thermal stabilization for mixed-type G2T1 than for anti-parallel G2T1, G1 and ds DNA. Spectroscopic studies suggest that compound 1a could bind to mixed-type G2T1 via end-stacking and external binding modes. These results suggest that the polyether linkers in these compounds play an important role in regulating the binding affinity and selectivity towards mixed-type G2T1 and that compound 1a could target mixed-type G2T1 at other genome regions with antiparallel G2T1 and monomeric G-quadruplexes. These results may provide useful guidance for the rational design of selective multimeric G-quadruplex binders and potential anticancer agents.
[Mh] Termos MeSH primário: Berberina/farmacologia
Quadruplex G/efeitos dos fármacos
[Mh] Termos MeSH secundário: Berberina/síntese química
Berberina/química
Dimerização
Seres Humanos
Estrutura Molecular
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0I8Y3P32UF (Berberine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob02326j


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[PMID]:27779107
[Au] Autor:Zhang Q; Wang J; Zhang C; Liao S; Li P; Xu D; Lv Y; Yang M; Kong L
[Ad] Endereço:State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, P.R. China.
[Ti] Título:The components of Huang-Lian-Jie-Du-Decoction act synergistically to exert protective effects in a rat ischemic stroke model.
[So] Source:Oncotarget;7(49):80872-80887, 2016 Dec 06.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Huang-Lian-Jie-Du-Decoction (HLJDD, Oren-gedoku-to in Japanese) is commonly used in traditional Chinese medicine (TCM) to treat ischemic stroke. This study investigated the efficacy of various combinations of the major components of HLJDD, berberine (A), baicalin (B), and jasminoidin (C), on the treatment of ischemic stroke modeled by middle cerebral artery occlusion (MCAO) in rats. The effects of A, B and C individually and their combinations were investigated using proton nuclear magnetic resonance (1H NMR)-based metabolomics complemented with neurologic deficit scoring, infarct volume measurement, biochemistry, histopathology and immunohistochemistry, as well as quantitative real-time polymerase chain reaction (qRT-PCR) and western blotting. Ischemic stroke produces severe oxidative stress, which induces further damage. Our results show that the ABC combination treatment increased levels of cellular antioxidants that scavenged reactive oxygen species during ischemia-reperfusion via the nuclear erythroid 2-related factor 2 (Nrf2) signaling cascade. These protective effects were not observed with the other treatments. These results suggest that a combination of component herbs in HLJDD exhibit stronger effects than the individual herbs alone. Our integrated metabolomics approach also provides a tractable, powerful tool for understanding the science behind TCM formulations.
[Mh] Termos MeSH primário: Encéfalo/efeitos dos fármacos
Medicamentos de Ervas Chinesas/farmacologia
Depuradores de Radicais Livres/farmacologia
Infarto da Artéria Cerebral Média/tratamento farmacológico
Fármacos Neuroprotetores/farmacologia
Traumatismo por Reperfusão/prevenção & controle
[Mh] Termos MeSH secundário: Animais
Berberina/farmacologia
Encéfalo/metabolismo
Encéfalo/patologia
Modelos Animais de Doenças
Sinergismo Farmacológico
Flavonoides/farmacologia
Infarto da Artéria Cerebral Média/metabolismo
Infarto da Artéria Cerebral Média/patologia
Iridoides/farmacologia
Masculino
Metabolômica/métodos
Fator 2 Relacionado a NF-E2/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Fitoterapia
Plantas Medicinais
Espectroscopia de Prótons por Ressonância Magnética
Ratos Sprague-Dawley
Traumatismo por Reperfusão/metabolismo
Traumatismo por Reperfusão/patologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drugs, Chinese Herbal); 0 (Flavonoids); 0 (Free Radical Scavengers); 0 (Iridoids); 0 (NF-E2-Related Factor 2); 0 (Neuroprotective Agents); 0 (Nfe2l2 protein, rat); 0 (huanglian-jie-du decoction); 0I8Y3P32UF (Berberine); 145295QLXY (geniposide); 347Q89U4M5 (baicalin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.12645


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[PMID]:29247651
[Au] Autor:Zhou F; Bai M; Zhang Y; Zhu Q; Zhang L; Zhang Q; Wang S; Zhu K; Liu Y; Wang X; Zhou L
[Ad] Endereço:Shanghai Institute of Endocrine and Metabolic Diseases, Shanghai Clinical Center for Endocrine and Metabolic Diseases, Department of Endocrine and Metabolic Diseases, Ruijin Hospital, Shanghai Jiaotong University School of Medicine, Shanghai 200025, China.
[Ti] Título:Berberine-induced activation of AMPK increases hepatic FGF21 expression via NUR77.
[So] Source:Biochem Biophys Res Commun;495(2):1936-1941, 2018 01 08.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Fibroblast growth factor 21 (FGF21), a hormone-like protein mainly derived from liver, exhibits multiple beneficial effect on energy metabolism. Similar to FGF21, berberine exerts anti-hyperglycemic and anti-dyslipidemic properties. Previous studies revealed that the beneficial metabolic effect of berberine was attributed to the activation of AMP-activated protein kinase (AMPK). Here we investigated the effect of berberine on FGF21 expression in primary mouse hepatocytes. As expected, berberine induced hepatic FGF21 expression in a dose-dependent and time-dependent manner, along with the increased expression of NUR77, a proved transcription factor of FGF21. Berberine stimulated the phosphorylations of AMPK and acetyl-CoA carboxylase in primary mouse hepatocytes. Adenovirus-mediated overexpression of constitutively active AMPK triggered hepatic FGF21 and NUR77 expressions. The inhibition of AMPK by compound C abolished berberine-stimulated FGF21 and NUR77 expressions. These results suggest that berberine-induced activation of AMPK may contribute to hepatic FGF21 expression via NUR77.
[Mh] Termos MeSH primário: Berberina/administração & dosagem
Fatores de Crescimento de Fibroblastos/metabolismo
Hepatócitos/metabolismo
Membro 1 do Grupo A da Subfamília 4 de Receptores Nucleares/metabolismo
Proteínas Quinases/metabolismo
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Relação Dose-Resposta a Droga
Ativação Enzimática/efeitos dos fármacos
Ativação Enzimática/fisiologia
Hepatócitos/efeitos dos fármacos
Hipoglicemiantes/administração & dosagem
Hipolipemiantes/administração & dosagem
Masculino
Redes e Vias Metabólicas/efeitos dos fármacos
Redes e Vias Metabólicas/fisiologia
Camundongos
Camundongos Endogâmicos C57BL
Regulação para Cima/efeitos dos fármacos
Regulação para Cima/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Hypolipidemic Agents); 0 (Nr4a1 protein, mouse); 0 (Nuclear Receptor Subfamily 4, Group A, Member 1); 0 (fibroblast growth factor 21); 0I8Y3P32UF (Berberine); 62031-54-3 (Fibroblast Growth Factors); EC 2.7.- (Protein Kinases); EC 2.7.1.- (AMP-activated protein kinase kinase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180214
[Lr] Data última revisão:
180214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171217
[St] Status:MEDLINE


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[PMID]:29289560
[Au] Autor:Sreeja S; Krishnan Nair CK
[Ad] Endereço:Pushpagiri Institute of Medical Sciences and Research Centre, Thiruvalla 689101, India; Mar Athanasios College for Advanced Studies, Thiruvalla 689101, India.
[Ti] Título:Tumor control by hypoxia-specific chemotargeting of iron-oxide nanoparticle - Berberine complexes in a mouse model.
[So] Source:Life Sci;195:71-80, 2018 Feb 15.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIM: To evaluate the therapeutic efficacy of hypoxic cell-sensitizer Sanazole (SAN) -directed targeting of cytotoxic drug Berberine (BBN) and Iron-oxide nanoparticle (NP) complexes, to solid tumor in Swiss albino mice. MAIN METHODS: NP-BBN-SAN complexes were characterized by FTIR, XRD, TEM and Nano-size analyzer. This complex was orally administered to mice-bearing solid tumor in hind limb. Tumor regression was analysed by measuring tumor volume. Cellular DNA damages were assessed by comet assay. Transcriptional expression of genes related to tumor hypoxia and apoptosis was evaluated by quantitative real-time PCR and morphological changes in tissues were analysed by histopathology. Also levels of antioxidants and tumor markers in tissues and serum biochemical parameters were analysed. KEY FINDINGS: Administration of NP-BBN-SAN complexes reduced tumor volume and studies were focussed on the underlying mechanisms. Extensive damage to cellular-DNA; down-regulated transcription of hif-1α, vegf, akt and bcl2; and up-regulated expression of bax and caspases, were observed in tumor. Results on tumor markers, antioxidant-status and serum parameters corroborated the molecular findings. Histopathology of tumor, liver and kidney revealed the therapeutic specificity of NP-BBN-SAN. SIGNIFICANCE: Thus SAN and NP can be used for specific targeting of drugs, to hypoxic solid tumor, to improve therapeutic efficacy.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/uso terapêutico
Berberina/uso terapêutico
Sistemas de Liberação de Medicamentos/métodos
Compostos Férricos/uso terapêutico
Hipóxia
Nanopartículas
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/administração & dosagem
Antineoplásicos Fitogênicos/química
Antioxidantes/metabolismo
Berberina/administração & dosagem
Berberina/química
Biomarcadores Tumorais
DNA de Neoplasias/biossíntese
DNA de Neoplasias/efeitos dos fármacos
Feminino
Compostos Férricos/administração & dosagem
Compostos Férricos/química
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Camundongos
Neoplasias Experimentais/tratamento farmacológico
Neoplasias Experimentais/patologia
Neoplasias Experimentais/terapia
Tamanho da Partícula
Espectroscopia de Infravermelho com Transformada de Fourier
Análise de Sobrevida
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Antioxidants); 0 (Biomarkers, Tumor); 0 (DNA, Neoplasm); 0 (Ferric Compounds); 0I8Y3P32UF (Berberine); 1K09F3G675 (ferric oxide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180208
[Lr] Data última revisão:
180208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180101
[St] Status:MEDLINE


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[PMID]:29223540
[Au] Autor:Luo C; Chen H; Wang Y; Lin G; Li C; Tan L; Su Z; Lai X; Xie J; Zeng H
[Ad] Endereço:Guangdong Provincial Key Laboratory of New Drug Development and Research of Chinese Medicine, Mathematical Engineering Academy of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China.
[Ti] Título:Protective effect of coptisine free base on indomethacin-induced gastric ulcers in rats: Characterization of potential molecular mechanisms.
[So] Source:Life Sci;193:47-56, 2018 Jan 15.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: The aim of this study was to comparatively investigate the potential gastroprotective effect and underlying mechanisms of coptisine free base (CFB, 8-hydroxy-7, 8-dihydrocoptisine), berberine and lansoprazole against indomethacin-induced gastric ulcer in rats. MATERIALS AND METHODS: CFB (10, 20 and 40mg/kg), berberine (20mg/kg) and lansoprazole (30mg/kg) were orally administrated to rats prior to indometacin ingestion, and gastric lesions were evaluated macroscopically and histologically, and further analyzed by ELISA, qRT-PCR and Western blot. KEY FINDINGS: CFB exerted comparable or superior gastroprotective effect to berberine in protecting against indomethacin-induced gastric injury. CFB pretreatment significantly enhanced the levels of superoxide dismutase (SOD) and glutathione (GSH), and markedly decreased the malonaldehyde (MDA) content. CFB administration effectively suppressed the levels of myeloperoxidase (MPO), interleukin-1ß (IL-1ß), tumor necrosis factor-α (TNF-α) and angiotensin II (Ang II). Besides, CFB substantially up-regulated the mRNA expressions of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), and promoted gastric mucosal prostaglandin E level (PGE ). Furthermore, CFB pretreatment remarkably increased the translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) from cytosol into the nucleus, and the expression of heme oxygenase-1 (HO-1), while significantly decreased the expression of mitogen activated protein Kinase Kinase 6 (MKK6) and translocation of p38 mitogen-activated protein kinase (p38 MAPK). SIGNIFICANCE: This was the first investigation reporting the anti-ulcer effect of protoberberine alkaloid free base on in vivo rodent model. The gastroprotective mechanism of CFB might involve favorable regulation of antioxidant and anti-inflammatory status mediated, at least partially, by the Nrf2 signaling pathway and p38 MAPK translocation.
[Mh] Termos MeSH primário: Berberina/análogos & derivados
Úlcera Gástrica/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/farmacologia
Antioxidantes/farmacologia
Berberina/metabolismo
Berberina/farmacologia
Berberina/uso terapêutico
Ciclo-Oxigenase 1/metabolismo
Ciclo-Oxigenase 2/metabolismo
Modelos Animais de Doenças
Mucosa Gástrica/patologia
Indometacina
Interleucina-1beta/metabolismo
Lansoprazol/farmacologia
Lansoprazol/uso terapêutico
Masculino
Ratos
Úlcera Gástrica/patologia
Superóxido Dismutase/metabolismo
Fator de Necrose Tumoral alfa/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antioxidants); 0 (Interleukin-1beta); 0 (Tumor Necrosis Factor-alpha); 0GCL71VN14 (coptisine); 0I8Y3P32UF (Berberine); 0K5C5T2QPG (Lansoprazole); EC 1.14.99.1 (Cyclooxygenase 1); EC 1.14.99.1 (Cyclooxygenase 2); EC 1.15.1.1 (Superoxide Dismutase); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180108
[Lr] Data última revisão:
180108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171211
[St] Status:MEDLINE


  8 / 2390 MEDLINE  
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[PMID]:28459539
[Au] Autor:Raghav D; Ashraf SM; Mohan L; Rathinasamy K
[Ad] Endereço:School of Biotechnology, National Institute of Technology Calicut , Calicut, Kerala, India.
[Ti] Título:Berberine Induces Toxicity in HeLa Cells through Perturbation of Microtubule Polymerization by Binding to Tubulin at a Unique Site.
[So] Source:Biochemistry;56(20):2594-2611, 2017 05 23.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Berberine has been used traditionally for its diverse pharmacological actions. It exhibits remarkable anticancer activities and is currently under clinical trials. In this study, we report that the anticancer activity of berberine could be partly due to its inhibitory actions on tubulin and microtubule assembly. Berberine inhibited the proliferation of HeLa cells with an IC of 18 µM and induced significant depolymerization of interphase and mitotic microtubules. At its IC , berberine exerted a moderate G2/M arrest and mitotic block as detected by fluorescence-activated cell sorting analysis and fluorescence microscopy, respectively. In a wound closure assay, berberine inhibited the migration of HeLa cells at concentrations lower than its IC , indicating its excellent potential as an anticancer agent. In vitro studies with tubulin isolated from goat brain indicated that berberine binds to tubulin at a single site with a K of 11 µM. Berberine inhibited the assembly of tubulin into microtubules and also disrupted the preformed microtubules polymerized in the presence of glutamate and paclitaxel. Competition experiments indicated that berberine could partially displace colchicine from its binding site. Results from fluorescence resonance energy transfer, computational docking, and molecular dynamics simulations suggest that berberine forms a stable complex with tubulin and binds at a novel site 24 Å from the colchicine site on the ß-tubulin. Data obtained from synchronous fluorescence analysis of the tryptophan residues of tubulin and from the Fourier transform infrared spectroscopy studies revealed that binding of berberine alters the conformation of the tubulin heterodimer, which could be the molecular mechanism behind the depolymerizing effects on tubulin assembly.
[Mh] Termos MeSH primário: Berberina/toxicidade
Microtúbulos/efeitos dos fármacos
Tubulina (Proteína)/metabolismo
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Encéfalo/metabolismo
Proliferação Celular/efeitos dos fármacos
Transferência Ressonante de Energia de Fluorescência
Cabras
Células HeLa
Seres Humanos
Interações Hidrofóbicas e Hidrofílicas
Microtúbulos/metabolismo
Mitose/efeitos dos fármacos
Simulação de Dinâmica Molecular
Polimerização
Triptofano/química
Tubulina (Proteína)/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Tubulin); 0I8Y3P32UF (Berberine); 8DUH1N11BX (Tryptophan)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171205
[Lr] Data última revisão:
171205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00101


  9 / 2390 MEDLINE  
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[PMID]:29061795
[Au] Autor:Du J; Sun Y; Lu YY; Lau E; Zhao M; Zhou QM; Su SB
[Ad] Endereço:Research Center for Traditional Chinese Medicine Complexity System, Shanghai University of Traditional Chinese Medicine, Shanghai, P.R. China.
[Ti] Título:Berberine and Evodiamine Act Synergistically Against Human Breast Cancer MCF-7 Cells by Inducing Cell Cycle Arrest and Apoptosis.
[So] Source:Anticancer Res;37(11):6141-6151, 2017 11.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: The synergistic combinations of natural products have long been the basis of Traditional Chinese herbal Medicine formulas. In this study, we investigated the synergistic effects of a combination of berberine and evodiamine against human breast cancer MCF-7 cells in vitro and in vivo, and explored its mechanism. MATERIALS AND METHODS: Cell survival was measured using the MTT assay. Apoptosis-related proteins were observed using western blot analysis. Apoptosis was detected with flow cytometric analysis and by Hoechst 33258 staining. Tumor xenografts were used in vivo. RESULTS: Compared to berberine or evodiamine treatments alone, the combination treatment of berberine (25 µM) and evodiamine (15 µM) synergistically inhibited the proliferation of MCF-7 cells in a time-dependent manner and resulted in the G /G phase accumulation of cells that exhibited increased expression levels of the CDK inhibitors p21 and p27 with a concomitant reduction in the expression levels of cell-cycle checkpoint proteins cyclin D1, cyclin E, CDK4, and CDK6. Furthermore, the combination treatment induced apoptosis that was accompanied by increased expression levels of p53 and Bax, reduced expression levels of Bcl-2, activation of caspase-7, and caspase-9, and the cleavage of PARP. The combination of berberine and evodiamine synergistically inhibited tumor growth in vivo in MCF-7 human breast cancer xenografts. CONCLUSION: Combination of berberine and evodiamine acts synergistically to suppress the proliferation of MCF-7 cells by inducing cell cycle arrest and apoptosis, illustrating the potential synergistic and combinatorial application of bioactive natural products.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Berberina/farmacologia
Neoplasias da Mama/tratamento farmacológico
Neoplasias da Mama/patologia
Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Quinazolinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Proteínas Reguladoras de Apoptose/metabolismo
Neoplasias da Mama/metabolismo
Sinergismo Farmacológico
Quimioterapia Combinada
Feminino
Seres Humanos
Camundongos
Camundongos Endogâmicos BALB C
Camundongos Nus
Células Tumorais Cultivadas
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Apoptosis Regulatory Proteins); 0 (Quinazolines); 0I8Y3P32UF (Berberine); C01825BVNL (evodiamine)
[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:171025
[St] Status:MEDLINE


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[PMID]:28958846
[Au] Autor:Enkhtaivan G; Muthuraman P; Kim DH; Mistry B
[Ad] Endereço:Department of Bio-resources and Food Science, Konkuk University, Seoul 143-701, South Korea.
[Ti] Título:Discovery of berberine based derivatives as anti-influenza agent through blocking of neuraminidase.
[So] Source:Bioorg Med Chem;25(20):5185-5193, 2017 Oct 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In this study, we investigated the antiviral activity of newly synthesized berberine derivatives (BD) against influenza virus infection using several strains in in vitro and in silico. The CPE reduction, pre-incubation, NA activity inhibition and molecular docking assays were used for antiviral evaluation. The anti-influenza activities of BDs were stronger than plant-derived pure commercial berberine, and some of the BDs were more potent than control drug Oseltamivir. The cytotoxicity level was observed in the range 63.16-1639µg/mL for synthesized BDs. Additionally, BDs were detected as able to block influenza viral particles. We targeted neuraminidase one of the influenza surface protein for further probing. Moreover, BDs registered competitive NA inhibition activity comparing with Oseltamivir. The active site of viral NA subunit was fully blocked by BD as the same location as Oseltamivir. The binding energies between influenza NA subunit and BD-5 were higher than Oseltamivir. More H-bonds and NA residues were occupied by BD for stronger binding ability than Oseltamivir. These results indicated that BD inhibits various strains of influenza virus by blocking of viral NA subunit.
[Mh] Termos MeSH primário: Antivirais/farmacologia
Berberina/farmacologia
Descoberta de Drogas
Inibidores Enzimáticos/farmacologia
Neuraminidase/antagonistas & inibidores
Orthomyxoviridae/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antivirais/síntese química
Antivirais/química
Berberina/síntese química
Berberina/química
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Seres Humanos
Testes de Sensibilidade Microbiana
Estrutura Molecular
Neuraminidase/metabolismo
Orthomyxoviridae/enzimologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Enzyme Inhibitors); 0I8Y3P32UF (Berberine); EC 3.2.1.18 (Neuraminidase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171107
[Lr] Data última revisão:
171107
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170930
[St] Status:MEDLINE



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