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[PMID]:29378653
[Au] Autor:Kalyana Sundaram I; Sarangi DD; Sundararajan V; George S; Sheik Mohideen S
[Ad] Endereço:Department of Biotechnology, Dayanandasagar College of Engineering, Kumaraswamy Layout, Bangalore, 560078, Karnataka, India.
[Ti] Título:Poly herbal formulation with anti-elastase and anti-oxidant properties for skin anti-aging.
[So] Source:BMC Complement Altern Med;18(1):33, 2018 Jan 29.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Skin forms an important part of human innate immune system. Wrinkles, thinning and roughening of skin are some of the symptoms that affect the skin as it ages. Reactive oxygen species induced oxidative stress plays a major role in skin aging by modulating the elastase enzyme level in the skin. Extrinsic factors that affect skin aging such as UV radiation can also cause malignant melanoma. Here we selected four medicinal plant materials, namely, leaves of Nyctanthes arbor-tristis, unripe and ripe Aegle marmelos fruit pulp and the terminal meristem of Musa paradisiaca flower and investigated their anti-aging properties and cytotoxicity in vitro individually as well as in a poly herbal formulation containing the four plant extracts in different ratios. METHODS: The phytochemical contents of the plant extracts were investigated for radical scavenging activity and total reducing power. Based upon its anti-oxidant properties, a poly herbal formulation containing leaves of Nyctanthes arbor-tristis, unripe and ripe fruit pulp of Aegle marmelos, and the terminal meristem of Musa paradisiaca flower in the ratio 6:2:1:1 (Poly Herbal Formulation 1) and 1:1:1:1 (Poly Herbal Formulation 2), respectively were formulated. RESULT: It has been observed that the Poly Herbal Formulation 1 was more potent than Poly Herbal Formulation 2 due to better anti-oxidant and anti-elastase activities in NIH3T3 fibroblast cells. In addition Poly Herbal formulation 1 also had better anti-cancer activity in human malignant melanoma cells. CONCLUSION: Based on these results these beneficial plant extracts were identified for its potential application as an anti-aging agent in skin creams as well as an anti-proliferation compound against cancer cells.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Estresse Oxidativo/efeitos dos fármacos
Elastase Pancreática/antagonistas & inibidores
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Aegle/química
Animais
Antineoplásicos/farmacologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Seres Humanos
Camundongos
Células NIH 3T3
Óxido Nítrico/metabolismo
Oleaceae/química
Plantas Medicinais/química
Espécies Reativas de Oxigênio/metabolismo
Envelhecimento da Pele
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Plant Extracts); 0 (Reactive Oxygen Species); 31C4KY9ESH (Nitric Oxide); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180131
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-018-2097-9


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[PMID]:29366749
[Au] Autor:Gonzalez EA; Martins GR; Tavares AMV; Viegas M; Poletto E; Giugliani R; Matte U; Baldo G
[Ad] Endereço:Gene Therapy Center, Hospital de Clínicas de Porto Alegre, Porto Alegre, Brazil; Post-Graduation Program in Genetics and Molecular Biology, UFRGS, Porto Alegre, Brazil.
[Ti] Título:Cathepsin B inhibition attenuates cardiovascular pathology in mucopolysaccharidosis I mice.
[So] Source:Life Sci;196:102-109, 2018 Mar 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Mucopolysaccharidosis type I (MPS I) is a lysosomal storage disorder with multisystemic features, including heart enlargement, heart valve dysfunction, and aortic stiffness and dilatation. Previous studies have shown that MPS I mice overexpress cathepsin B (CtsB) in multiple tissues, including those from the cardiovascular system. Here, we hypothesized that inhibition of CtsB could ameliorate cardiac function parameters, as well as aorta and valve abnormalities found in MPS I. First, we found that total elastase activity in an MPS I aorta is elevated. Following that, we demonstrated that CtsB leaks from the lysosome in MPS I human fibroblasts, possibly acting as a degradative agent of extracellular matrix components from the aorta, cardiac muscle, and heart valves. We then used a CtsB inhibitor in vivo in the MPS I mouse model. After 4 months of treatment, partial inhibition of CtsB activity in treated mice reduced aortic dilatation, as well as heart valve thickening, and led to improvements in cardiac function parameters, although none of these were completely normalized. Based on these results, we conclude that lysosomal alterations in this disease promote leakage of CtsB to outside the organelle, where this protein can have multiple pathological roles. CtsB inhibition improved cardiovascular parameters in MPS I mice and can have a potential benefit in this disease.
[Mh] Termos MeSH primário: Sistema Cardiovascular/patologia
Catepsina B/antagonistas & inibidores
Inibidores de Cisteína Proteinase/uso terapêutico
Dipeptídeos/uso terapêutico
Mucopolissacaridose I/diagnóstico por imagem
Mucopolissacaridose I/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Aorta/patologia
Aorta/fisiopatologia
Sistema Cardiovascular/diagnóstico por imagem
Catepsina B/metabolismo
Colagenases/metabolismo
Feminino
Fibroblastos/metabolismo
Testes de Função Cardíaca
Doenças das Valvas Cardíacas/diagnóstico por imagem
Doenças das Valvas Cardíacas/tratamento farmacológico
Doenças das Valvas Cardíacas/patologia
Seres Humanos
Lisossomos/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Mucopolissacaridose I/patologia
Elastase Pancreática/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cysteine Proteinase Inhibitors); 0 (Dipeptides); 134448-10-5 (N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline); EC 3.4.21.36 (Pancreatic Elastase); EC 3.4.22.1 (Cathepsin B); EC 3.4.24.- (Collagenases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180126
[St] Status:MEDLINE


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[PMID]:28466019
[Au] Autor:Almeida-Reis R; Theodoro-Junior OA; Oliveira BTM; Oliva LV; Toledo-Arruda AC; Bonturi CR; Brito MV; Lopes FDTQS; Prado CM; Florencio AC; Martins MA; Owen CA; Leick EA; Oliva MLV; Tibério IFLC
[Ad] Endereço:Department of Medicine, School of Medicine, University of São Paulo, São Paulo, SP, Brazil.
[Ti] Título:Plant Proteinase Inhibitor BbCI Modulates Lung Inflammatory Responses and Mechanic and Remodeling Alterations Induced by Elastase in Mice.
[So] Source:Biomed Res Int;2017:8287125, 2017.
[Is] ISSN:2314-6141
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Proteinases play a key role in emphysema. inhibitor (BbCI) is a serine-cysteine proteinase inhibitor. We evaluated BbCI treatment in elastase-induced pulmonary alterations. / mice received intratracheal elastase (ELA group) or saline (SAL group). One group of mice was treated with BbCI (days 1, 15, and 21 after elastase instillation, ELABC group). Controls received saline and BbCI (SALBC group). After 28 days, we evaluated respiratory mechanics, exhaled nitric oxide, and bronchoalveolar lavage fluid. In lung tissue we measured airspace enlargement, quantified neutrophils, TNF -, MMP-9-, MMP-12-, TIMP-1-, iNOS-, and eNOS-positive cells, 8-iso-PGF2 , collagen, and elastic fibers in alveolar septa and airways. MUC-5-positive cells were quantified only in airways. BbCI reduced elastase-induced changes in pulmonary mechanics, airspace enlargement and elastase-induced increases in total cells, and neutrophils in BALF. BbCI reduced macrophages and neutrophils positive cells in alveolar septa and neutrophils and TNF -positive cells in airways. BbCI attenuated elastic and collagen fibers, MMP-9- and MMP-12-positive cells, and isoprostane and iNOS-positive cells in alveolar septa and airways. BbCI reduced MUC5ac-positive cells in airways. BbCI improved lung mechanics and reduced lung inflammation and airspace enlargement and increased oxidative stress levels induced by elastase. BbCI may have therapeutic potential in chronic obstructive pulmonary disease.
[Mh] Termos MeSH primário: Cisteína Endopeptidases/administração & dosagem
Proteínas de Plantas/administração & dosagem
Pneumonia/tratamento farmacológico
Enfisema Pulmonar/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Líquido da Lavagem Broncoalveolar
Seres Humanos
Pulmão/efeitos dos fármacos
Pulmão/metabolismo
Pulmão/patologia
Camundongos
Estresse Oxidativo/efeitos dos fármacos
Elastase Pancreática/toxicidade
Pneumonia/induzido quimicamente
Pneumonia/patologia
Enfisema Pulmonar/induzido quimicamente
Enfisema Pulmonar/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (BbCI protein, Bauhinia bauhinoides); 0 (Plant Proteins); EC 3.4.21.36 (Pancreatic Elastase); EC 3.4.22.- (Cysteine Endopeptidases); EC 3.4.22.- (cruzipain)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE
[do] DOI:10.1155/2017/8287125


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[PMID]:28982723
[Au] Autor:Fernandez-García CE; Tarin C; Roldan-Montero R; Martinez-Lopez D; Torres-Fonseca M; Lindhot JS; Vega de Ceniga M; Egido J; Lopez-Andres N; Blanco-Colio LM; Martín-Ventura JL
[Ad] Endereço:Vascular Research Lab, FIIS-Fundación Jiménez Díaz-Autonoma University, Madrid, Spain.
[Ti] Título:Increased galectin-3 levels are associated with abdominal aortic aneurysm progression and inhibition of galectin-3 decreases elastase-induced AAA development.
[So] Source:Clin Sci (Lond);131(22):2707-2719, 2017 Nov 15.
[Is] ISSN:1470-8736
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Abdominal aortic aneurysm (AAA) evolution is unpredictable and no specific treatment exists for AAA, except surgery to prevent aortic rupture. Galectin-3 has been previously associated with CVD, but its potential role in AAA has not been addressed. Galectin-3 levels were increased in the plasma of AAA patients ( =225) compared with the control group ( =100). In addition, galectin-3 concentrations were associated with the need for surgical repair, independently of potential confounding factors. Galectin-3 mRNA and protein expression were increased in human AAA samples compared with healthy aortas. Experimental AAA in mice was induced via aortic elastase perfusion. Mice were treated intravenously with the galectin-3 inhibitor modified citrus pectin (MCP, 10 mg/kg, every other day) or saline. Similar to humans, galectin-3 serum and aortic mRNA levels were also increased in elastase-induced AAA mice compared with control mice. Mice treated with MCP showed decreased aortic dilation, as well as elastin degradation, vascular smooth muscle cell (VSMC) loss, and macrophage content at day 14 postelastase perfusion compared with control mice. The underlying mechanism(s) of the protective effect of MCP was associated with a decrease in galectin-3 and cytokine (mainly CCL5) mRNA and protein expression. Interestingly, galectin-3 induced CCL5 expression by a mechanism involving STAT3 activation in VSMC. Accordingly, MCP treatment decreased STAT3 phosphorylation in elastase-induced AAA. In conclusion, increased galectin-3 levels are associated with AAA progression, while galectin-3 inhibition decreased experimental AAA development. Our data suggest the potential role of galectin-3 as a therapeutic target in AAA.
[Mh] Termos MeSH primário: Aorta Abdominal/efeitos dos fármacos
Aneurisma da Aorta Abdominal/prevenção & controle
Galectina 3/antagonistas & inibidores
Galectina 3/sangue
Elastase Pancreática
Pectinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Aorta Abdominal/enzimologia
Aorta Abdominal/patologia
Aneurisma da Aorta Abdominal/sangue
Aneurisma da Aorta Abdominal/enzimologia
Aneurisma da Aorta Abdominal/patologia
Estudos de Casos e Controles
Células Cultivadas
Quimiocina CCL5/genética
Quimiocina CCL5/metabolismo
Dilatação Patológica
Modelos Animais de Doenças
Progressão da Doença
Galectina 3/genética
Galectina 3/metabolismo
Seres Humanos
Camundongos Endogâmicos C57BL
Músculo Liso Vascular/efeitos dos fármacos
Músculo Liso Vascular/metabolismo
Miócitos de Músculo Liso/efeitos dos fármacos
Miócitos de Músculo Liso/metabolismo
Fosforilação
RNA Mensageiro/sangue
RNA Mensageiro/genética
Fator de Transcrição STAT3/metabolismo
Transdução de Sinais/efeitos dos fármacos
Fatores de Tempo
Regulação para Cima
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ccl5 protein, mouse); 0 (Chemokine CCL5); 0 (Galectin 3); 0 (Lgals3 protein, mouse); 0 (Pectins); 0 (RNA, Messenger); 0 (STAT3 Transcription Factor); 0 (Stat3 protein, mouse); 0 (citrus pectin); 0 (galectin-3, human); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171007
[St] Status:MEDLINE
[do] DOI:10.1042/CS20171142


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[PMID]:28912363
[Au] Autor:Lareyre F; Clément M; Raffort J; Pohlod S; Patel M; Esposito B; Master L; Finigan A; Vandestienne M; Stergiopulos N; Taleb S; Trachet B; Mallat Z
[Ad] Endereço:From the Division of Cardiovascular Medicine, University of Cambridge, UK (F.L., M.C., J.R., M.P., L.M., A.F., Z.M.); Université Côte d'Azur, Centre National de la Recherche Scientifique, Institut National de la Sante et de la Recherche Medicale, Institute for Research on Cancer and Aging in Nice, F
[Ti] Título:TGFß (Transforming Growth Factor-ß) Blockade Induces a Human-Like Disease in a Nondissecting Mouse Model of Abdominal Aortic Aneurysm.
[So] Source:Arterioscler Thromb Vasc Biol;37(11):2171-2181, 2017 Nov.
[Is] ISSN:1524-4636
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Current experimental models of abdominal aortic aneurysm (AAA) do not accurately reproduce the major features of human AAA. We hypothesized that blockade of TGFß (transforming growth factor-ß) activity-a guardian of vascular integrity and immune homeostasis-would impair vascular healing in models of nondissecting AAA and would lead to sustained aneurysmal growth until rupture. APPROACH AND RESULTS: Here, we test this hypothesis in the elastase-induced AAA model in mice. We analyze AAA development and progression using ultrasound in vivo, synchrotron-based ultrahigh resolution imaging ex vivo, and a combination of biological, histological, and flow cytometry-based cellular and molecular approaches in vitro. Systemic blockade of TGFß using a monoclonal antibody induces a transition from a self-contained aortic dilatation to a model of sustained aneurysmal growth, associated with the formation of an intraluminal thrombus. AAA growth is associated with wall disruption but no medial dissection and culminates in fatal transmural aortic wall rupture. TGFß blockade enhances leukocyte infiltration both in the aortic wall and the intraluminal thrombus and aggravates extracellular matrix degradation. Early blockade of IL-1ß or monocyte-dependent responses substantially limits AAA severity. However, blockade of IL-1ß after disease initiation has no effect on AAA progression to rupture. CONCLUSIONS: Endogenous TGFß activity is required for the healing of AAA. TGFß blockade may be harnessed to generate new models of AAA with better relevance to the human disease. We expect that the new models will improve our understanding of the pathophysiology of AAA and will be useful in the identification of new therapeutic targets.
[Mh] Termos MeSH primário: Anticorpos Monoclonais/toxicidade
Aorta Abdominal/efeitos dos fármacos
Aneurisma da Aorta Abdominal/induzido quimicamente
Ruptura Aórtica/induzido quimicamente
Elastase Pancreática
Fator de Crescimento Transformador beta/antagonistas & inibidores
Remodelação Vascular/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Aorta Abdominal/imunologia
Aorta Abdominal/metabolismo
Aorta Abdominal/patologia
Aneurisma da Aorta Abdominal/imunologia
Aneurisma da Aorta Abdominal/metabolismo
Aneurisma da Aorta Abdominal/patologia
Ruptura Aórtica/imunologia
Ruptura Aórtica/metabolismo
Ruptura Aórtica/patologia
Apolipoproteínas E/genética
Apolipoproteínas E/metabolismo
Quimiotaxia de Leucócito/efeitos dos fármacos
Dilatação Patológica
Modelos Animais de Doenças
Progressão da Doença
Matriz Extracelular/efeitos dos fármacos
Matriz Extracelular/metabolismo
Matriz Extracelular/patologia
Interleucina-1beta/metabolismo
Cinética
Masculino
Camundongos Endogâmicos C57BL
Camundongos Knockout
Síncrotrons
Trombose/induzido quimicamente
Trombose/metabolismo
Trombose/patologia
Fator de Crescimento Transformador beta/imunologia
Fator de Crescimento Transformador beta/metabolismo
Ultrassonografia
Cicatrização/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Monoclonal); 0 (Apolipoproteins E); 0 (IL1B protein, mouse); 0 (Interleukin-1beta); 0 (Transforming Growth Factor beta); EC 3.4.21.36 (Pancreatic Elastase)
[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:170916
[St] Status:MEDLINE
[do] DOI:10.1161/ATVBAHA.117.309999


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[PMID]:28841794
[Au] Autor:Lee H; Park Y; Kim S
[Ad] Endereço:Department of Chemistry, Seoul National University , Seoul 08826, Republic of Korea.
[Ti] Título:Enzymatic Cross-Linking of Side Chains Generates a Modified Peptide with Four Hairpin-like Bicyclic Repeats.
[So] Source:Biochemistry;56(37):4927-4930, 2017 Sep 19.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Macrocyclization of peptides is often employed to generate novel structures and biological activities in the biosynthesis of natural products and drug discovery. The enzymatic cross-linking of two side chains in a peptide via an ester or amide has a high potential for making topologically diverse cyclic peptides but is found with only a single consensus sequence in the microviridin class of natural products. Here, we report that a peptide with a new sequence pattern can be enzymatically cross-linked to make a novel microviridin-like peptide, plesiocin, which contains four repeats of a distinct hairpin-like bicyclic structure and shows strong inhibition of proteases. A single ATP-grasp enzyme binds to a leader peptide, of which only 13 residues are required for binding, and performs eight esterification reactions on the core peptide. We also demonstrate that the combination of tandem mass spectrometry and an ester-specific reaction greatly facilitates the determination of connectivity. We suggest that the enzymatic cross-linking of peptide side chains can generate more diverse structures in nature or by engineering.
[Mh] Termos MeSH primário: Organismos Aquáticos/metabolismo
Desenho de Drogas
Myxococcales/metabolismo
Peptídeos Cíclicos/metabolismo
Peptídeos/metabolismo
Inibidores de Proteases/metabolismo
Processamento de Proteína Pós-Traducional
[Mh] Termos MeSH secundário: Organismos Aquáticos/enzimologia
Proteínas de Bactérias/química
Proteínas de Bactérias/metabolismo
Proteínas de Bactérias/farmacologia
Cromatografia Líquida de Alta Pressão
Quimotripsina/antagonistas & inibidores
Quimotripsina/metabolismo
Esterificação
Interações Hidrofóbicas e Hidrofílicas
Sequências Repetidas Invertidas
Cinética
Estrutura Molecular
Família Multigênica
Myxococcales/enzimologia
Elastase Pancreática/antagonistas & inibidores
Elastase Pancreática/metabolismo
Peptídeos/química
Peptídeos/farmacologia
Peptídeos Cíclicos/química
Peptídeos Cíclicos/farmacologia
Inibidores de Proteases/química
Inibidores de Proteases/farmacologia
Conformação Proteica
Proteólise/efeitos dos fármacos
Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Peptides); 0 (Peptides, Cyclic); 0 (Protease Inhibitors); 0 (plesiocin); EC 3.4.21.1 (Chymotrypsin); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170827
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00808


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[PMID]:28825980
[Au] Autor:Chen CH; Hwang TL; Chen LC; Chang TH; Wei CS; Chen JJ
[Ad] Endereço:Faculty of Pharmacy, School of Pharmaceutical Sciences, National Yang-Ming University, Taipei, 112, Taiwan; Department of Pharmacy, Tajen University, Pingtung, 907, Taiwan.
[Ti] Título:Isoflavones and anti-inflammatory constituents from the fruits of Psoralea corylifolia.
[So] Source:Phytochemistry;143:186-193, 2017 Nov.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The fruits of Psoralea corylifolia, known as Psoraleae Fructus (Buguzhi in Chinese), are traditionally used for the treatment of spermatorrhea, nephritis, asthma, pollakiuria, and various inflammatory diseases. Three previously undescribed isoflavone derivatives, 7-O-methylcorylifol A, 7-O-isoprenylcorylifol A, and 7-O-isoprenylneobavaisoflavone, have been isolated from the fruits of P. corylifolia, together with 9 known compounds. The structures of these compounds were determined through spectroscopic and MS analyses. Among the isolated compounds, 7-O-methylcorylifol A and psoralen exhibited potent inhibition (IC values ≤ 10.89 µM) of superoxide anion generation by human neutrophils in response to N-formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B (fMLP/CB). 7-O-Isoprenylcorylifol A, 7-O-isoprenylneobavaisoflavone, and 12,13-dihydro-12,13-epoxybakuchiol inhibited fMLP/CB-induced elastase release with IC values ≤ 14.30 µM. In addition, 7-O-isoprenylcorylifol A, bakuchiol, 12,13-dihydro-12,13-epoxybakuchiol, and psoralidin showed potent inhibition with IC values ≤ 36.65 µM, against lipopolysaccharide (LPS)-induced nitric oxide (NO) generation.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/isolamento & purificação
Anti-Inflamatórios não Esteroides/farmacologia
Isoflavonas/isolamento & purificação
Isoflavonas/farmacologia
Psoralea/química
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/química
Benzofuranos
Cumarínicos
Frutas
Seres Humanos
Isoflavonas/química
Lipopolissacarídeos/farmacologia
Camundongos
N-Formilmetionina Leucil-Fenilalanina
Neutrófilos/efeitos dos fármacos
Óxido Nítrico/biossíntese
Ressonância Magnética Nuclear Biomolecular
Elastase Pancreática/antagonistas & inibidores
Fenóis
Fenilalanina
Superóxidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Benzofurans); 0 (Coumarins); 0 (Isoflavones); 0 (Lipopolysaccharides); 0 (Phenols); 11062-77-4 (Superoxides); 31C4KY9ESH (Nitric Oxide); 47E5O17Y3R (Phenylalanine); 59880-97-6 (N-Formylmethionine Leucyl-Phenylalanine); EC 3.4.21.36 (Pancreatic Elastase); G16ZUQ069L (psoralidin); OT12HJU3AR (bakuchiol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170822
[St] Status:MEDLINE


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[PMID]:28784293
[Au] Autor:Saikiran M; Sato D; Pandey SS; Hayase S; Kato T
[Ad] Endereço:Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, 2-4 Hibikino, Wakamatsu, Kitakyushu 808-0196, Japan. Electronic address: msaikiran87@gmail.com.
[Ti] Título:Efficient near infrared fluorescence detection of elastase enzyme using peptide-bound unsymmetrical squaraine dye.
[So] Source:Bioorg Med Chem Lett;27(17):4024-4029, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Extended wavelength analyte-responsive fluorescent probes are highly desired for the imaging applications owing to their deep tissue penetration, and minimum interference from autofluorescence by biomolecules. Near infra-red (NIR) sensitive and self-quenching fluorescent probe based on the dye-peptide conjugate (SQ 1 PC) was designed and synthesized by facile and efficient one-pot synthetic route for the detection of Elastase activity. In the phosphate buffer solution, there was an efficient quenching of fluorescence of SQ 1 PC (86%) assisted by pronounced dye-dye interaction due to H-aggregate formation. Efficient and fast recovery of this quenched fluorescence of SQ 1 PC (> 50% in 30s) was observed on hydrolysis of this peptide-dye conjugate by elastase enzyme. Presently designed NIR sensitive self-quenching substrate offers the potential application for the detection of diseases related to proteases by efficient and fast detection of their activities.
[Mh] Termos MeSH primário: Fluorescência
Corantes Fluorescentes/química
Elastase Pancreática/análise
Peptídeos/química
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Corantes Fluorescentes/metabolismo
Seres Humanos
Raios Infravermelhos
Estrutura Molecular
Elastase Pancreática/metabolismo
Peptídeos/metabolismo
Espectrometria de Fluorescência
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fluorescent Dyes); 0 (Peptides); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170809
[St] Status:MEDLINE


  9 / 8234 MEDLINE  
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[PMID]:28750062
[Au] Autor:Ochocka R; Hering A; Stefanowicz-Hajduk J; Cal K; Baranska H
[Ad] Endereço:Department of Biology and Pharmaceutical Botany, Medical University of Gdansk, Gdansk, Poland.
[Ti] Título:The effect of mangiferin on skin: Penetration, permeation and inhibition of ECM enzymes.
[So] Source:PLoS One;12(7):e0181542, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Mangiferin (2-C-ß-D-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone) is a polyphenol with strong antioxidant properties. Mangiferin is obtained from the mango tree (Mangifera indica L., Anacardiaceae). It has been proven that mangiferin exhibits many pharmacological activities. The aim of this study was to analyze the penetration of mangiferin into the human skin and through the skin. According to our knowledge, skin penetration and permeation studies of mangiferin have not been analyzed so far. Additionally, the influence of mangiferin on two Extracellular Matrix Enzymes (ECM): collagenase and elastase, was evaluated for the first time. It has been indicated that mangiferin is able to permeate the stratum corneum and penetrate into the epidermis and dermis in comparable amounts. For confirmation of the obtained results, fluorescence microscopy was successfully utilized. The analysis revealed the capability of mangiferin to reversibly inhibit elastase and collagenase activity. The mechanism of mangiferin interaction with both enzymes was estimated as a noncompetitive inhibition.
[Mh] Termos MeSH primário: Colagenases/metabolismo
Matriz Extracelular/enzimologia
Elastase Pancreática/metabolismo
Absorção Cutânea/efeitos dos fármacos
Pele/efeitos dos fármacos
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Adulto
Inibidores Enzimáticos/farmacologia
Matriz Extracelular/efeitos dos fármacos
Seres Humanos
Cinética
Meia-Idade
Soluções
Xantonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Solutions); 0 (Xanthones); 1M84LD0UMD (mangiferin); EC 3.4.21.36 (Pancreatic Elastase); EC 3.4.24.- (Collagenases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0181542


  10 / 8234 MEDLINE  
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[PMID]:28648460
[Au] Autor:Huang CY; Ahmed AF; Su JH; Sung PJ; Hwang TL; Chiang PL; Dai CF; Liaw CC; Sheu JH
[Ad] Endereço:Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung 804, Taiwan.
[Ti] Título:Bioactive new withanolides from the cultured soft coral Sinularia brassica.
[So] Source:Bioorg Med Chem Lett;27(15):3267-3271, 2017 08 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Continuing study of the ethyl acetate (EtOAc) extract of the cultured soft coral Sinularia brassica afforded five new withanolides, sinubrasolides H-L (1-5). The structures of the new compounds were elucidated on the basis of spectroscopic analysis. The cytotoxicities of new compounds 1-5 and a known compound sinubrasolide A (6) against the proliferation of a limited panel of cancer cell lines were assayed. The anti-inflammatory activities of compounds 1-6 were evaluated by measuring their ability to suppress N-formyl-methionyl-leucyl-phenyl-alanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release in human neutrophils.
[Mh] Termos MeSH primário: Antozoários/química
Anti-Inflamatórios/química
Anti-Inflamatórios/farmacologia
Antineoplásicos/química
Antineoplásicos/farmacologia
Vitanolídeos/química
Vitanolídeos/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios/isolamento & purificação
Antineoplásicos/isolamento & purificação
Linhagem Celular Tumoral
Citocalasina B/imunologia
Seres Humanos
Modelos Moleculares
Neoplasias/tratamento farmacológico
Neutrófilos/efeitos dos fármacos
Elastase Pancreática/imunologia
Superóxidos/imunologia
Vitanolídeos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Antineoplastic Agents); 0 (Withanolides); 11062-77-4 (Superoxides); 3CHI920QS7 (Cytochalasin B); EC 3.4.21.36 (Pancreatic Elastase)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170627
[St] Status:MEDLINE



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