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  1 / 806 MEDLINE  
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[PMID]:28830911
[Au] Autor:Park JW; Byrd A; Lee CM; Morgan ET
[Ad] Endereço:Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322, U.S.A.
[Ti] Título:Nitric oxide stimulates cellular degradation of human CYP51A1, the highly conserved lanosterol 14α-demethylase.
[So] Source:Biochem J;474(19):3241-3252, 2017 Sep 14.
[Is] ISSN:1470-8728
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nitric oxide (NO) is known to down-regulate drug-metabolizing cytochrome P450 enzymes in an enzyme-selective manner. Ubiquitin-proteasome-dependent and -independent pathways have been reported. Here, we studied the regulation of expression of human CYP51A1, the lanosterol 14α-demethylase required for synthesis of cholesterol and other sterols in mammals, which is found in every kingdom of life. In Huh7 human hepatoma cells, treatment with NO donors caused rapid post-translational down-regulation of CYP51A1 protein. Human NO synthase (NOS)-dependent down-regulation was also observed in cultured human hepatocytes treated with a cytokine mixture and in Huh7 cells expressing human NOS2 under control of a doxycycline-regulated promoter. This down-regulation was partially attenuated by proteasome inhibitors, but only trace levels of ubiquitination could be found. Further studies with inhibitors of other proteolytic pathways suggest a possible role for calpains, especially when the proteasome is inhibited. NO donors also down-regulated CYP51A1 mRNA in Huh7 cells, but to a lesser degree, than the down-regulation of the protein.
[Mh] Termos MeSH primário: Sequência Conservada
Lanosterol/metabolismo
Óxido Nítrico/farmacologia
Proteólise/efeitos dos fármacos
Esterol 14-Desmetilase/metabolismo
[Mh] Termos MeSH secundário: Calpaína/metabolismo
Linhagem Celular Tumoral
Regulação para Baixo/efeitos dos fármacos
Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos
Seres Humanos
Doadores de Óxido Nítrico/farmacologia
Inibidores de Proteassoma/farmacologia
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Esterol 14-Desmetilase/genética
Ubiquitinação/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Nitric Oxide Donors); 0 (Proteasome Inhibitors); 0 (RNA, Messenger); 1J05Z83K3M (Lanosterol); 31C4KY9ESH (Nitric Oxide); EC 1.14.13.70 (CYP51A1 protein, human); EC 1.14.13.70 (Sterol 14-Demethylase); EC 3.4.22.- (Calpain)
[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:170824
[St] Status:MEDLINE
[do] DOI:10.1042/BCJ20170459


  2 / 806 MEDLINE  
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[PMID]:28800421
[Au] Autor:Huang SZ; Ma QY; Kong FD; Guo ZK; Cai CH; Hu LL; Zhou LM; Wang Q; Dai HF; Mei WL; Zhao YX
[Ad] Endereço:Key Laboratory of Biology and Genetic Resources of Tropical Crops, Ministry of Agriculture, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agriculture Sciences, Haikou, 571101, People's Republic of China.
[Ti] Título:Lanostane-type triterpenoids from the fruiting body of Ganoderma calidophilum.
[So] Source:Phytochemistry;143:104-110, 2017 Nov.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To search for active anti-cancer constituents in the fruiting body of Ganoderma calidophilum, we have successfully isolated four previously undescribed spiro-lactone lanostane triterpenoids (spiroganocalitones A-D), two previously undescribed lanostanoids (ganodecalones A and B) together with twenty-three known ones. The structures of the six previously undescribed compounds were elucidated based on 1D, 2D-NMR, and HRMS analyses. Ganoderone A showed moderate cytotoxic activity against K562, BEL7402, and SGC790 cell lines with IC values of 7.62, 6.28, and 3.55 µM, respectively.
[Mh] Termos MeSH primário: Carpóforos/química
Ganoderma/química
Lanosterol/análogos & derivados
Triterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Seres Humanos
Concentração Inibidora 50
Lanosterol/química
Lanosterol/isolamento & purificação
Lanosterol/farmacologia
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Triterpenos/química
Triterpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Triterpenes); 0 (lanostanoid); 1J05Z83K3M (Lanosterol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE


  3 / 806 MEDLINE  
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[PMID]:28504879
[Au] Autor:Isaka M; Chinthanom P; Sappan M; Supothina S; Vichai V; Danwisetkanjana K; Boonpratuang T; Hyde KD; Choeyklin R
[Ad] Endereço:National Center for Genetic Engineering and Biotechnology (BIOTEC) , 113 Thailand Science Park, Phaholyothin Road, Klong Luang, Pathumthani 12120, Thailand.
[Ti] Título:Antitubercular Activity of Mycelium-Associated Ganoderma Lanostanoids.
[So] Source:J Nat Prod;80(5):1361-1369, 2017 May 26.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In a continuation of our research into antitubercular lanostane triterpenoids from submerged cultures of Ganoderma species, three strains, Ganoderma orbiforme BCC 22325, Ganoderma sp. BCC 60695, and Ganoderma australe BCC 22314, have been investigated. Fourteen new lanostane triterpenoids, together with 35 known compounds, were isolated. Antitubercular activities of these mycelium-associated Ganoderma lanostanoids against Mycobacterium tuberculosis H37Ra were evaluated. Taken together with the assay data of previously isolated compounds, structure-activity relationships of the antitubercular activity are proposed. Most importantly, 3ß- and 15α-acetoxy groups were shown to be critical for antimycobacterial activity. The most potent compound was (24E)-3ß,15α-diacetoxylanosta-7,9(11),24-trien-26-oic acid (35).
[Mh] Termos MeSH primário: Antituberculosos/isolamento & purificação
Antituberculosos/farmacologia
Carpóforos/química
Ganoderma/isolamento & purificação
Lanosterol/análogos & derivados
Micélio/química
Mycobacterium tuberculosis/química
[Mh] Termos MeSH secundário: Antituberculosos/química
Ganoderma/química
Lanosterol/química
Lanosterol/isolamento & purificação
Lanosterol/farmacologia
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (lanostanoid); 1J05Z83K3M (Lanosterol)
[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:170516
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b00973


  4 / 806 MEDLINE  
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[PMID]:28346885
[Au] Autor:Cao FR; Xiao BX; Wang LS; Tao X; Yan MZ; Pan RL; Liao YH; Liu XM; Chang Q
[Ad] Endereço:Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, PR China.
[Ti] Título:Plasma and brain pharmacokinetics of ganoderic acid A in rats determined by a developed UFLC-MS/MS method.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1052:19-26, 2017 May 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Ganoderic acid A (GAA), an active triterpenoid of the traditional Chinese herbal medicine Lingzhi, has been reported to exhibit antinociceptive, antioxidative, and anti-cancer activities. The present study aims to establish a sensitive and rapid UPLC-MS/MS method for studying the plasma and brain pharmacokinetics of GAA in rats. The analytes were separated on a C18 column eluted with a gradient mobile phase consisting of acetonitrile and 0.1% aqueous formic acid at 0.3mL/min. The eluate was monitored by a mass detector using an MRM (m/z, 515.3-285.1) model in negative electrospray ionization. The calibration curve showed good linearity (r >0.99), with limits of detection and quantification of 0.25 and 2.00 nmol/L, respectively. The intra- and inter-day precision and accuracy were less than 9.99% and ranged from 97.45% to 114.62%, respectively. The extraction recovery from plasma was between 92.89% and 98.87%. GAA was found to be stable in treated samples at room temperature (22°C) for 12h and in plasma at -20°C for 7d. The developed method was successfully applied to a pharmacokinetic study of GAA in rats. GAA could be rapidly absorbed into the circulation (T , 0.15h) and eliminated relatively slowly (t , 2.46h) after orally dosing, and could also be detected in the brain lateral ventricle (T , 0.25h and t , 1.40h) after intravenously dosing. The absolute oral bioavailability and brain permeability of GAA were estimated to be 8.68% and 2.96%, respectively.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Cromatografia Líquida de Alta Pressão/métodos
Medicamentos de Ervas Chinesas/farmacocinética
Ácidos Heptanoicos/sangue
Ácidos Heptanoicos/líquido cefalorraquidiano
Lanosterol/análogos & derivados
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Analgésicos/sangue
Analgésicos/líquido cefalorraquidiano
Animais
Antineoplásicos Fitogênicos/sangue
Antineoplásicos Fitogênicos/líquido cefalorraquidiano
Antioxidantes/farmacocinética
Lanosterol/sangue
Lanosterol/líquido cefalorraquidiano
Limite de Detecção
Masculino
Microdiálise/métodos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Analgesics); 0 (Antineoplastic Agents, Phytogenic); 0 (Antioxidants); 0 (Drugs, Chinese Herbal); 0 (Heptanoic Acids); 1J05Z83K3M (Lanosterol); 548G37DF65 (ganoderic acid A)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170328
[St] Status:MEDLINE


  5 / 806 MEDLINE  
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[PMID]:28099150
[Au] Autor:Dai J; Miller MA; Everetts NJ; Wang X; Li P; Li Y; Xu JH; Yao G
[Ad] Endereço:Department of Molecular and Cellular Biology, University of Arizona, Tucson, AZ, USA.
[Ti] Título:Elimination of quiescent slow-cycling cells via reducing quiescence depth by natural compounds purified from Ganoderma lucidum.
[So] Source:Oncotarget;8(8):13770-13781, 2017 Feb 21.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The medical mushroom Ganoderma lucidum has long been used in traditional Chinese medicine and shown effective in the treatment of many diseases including cancer. Here we studied the cytotoxic effects of two natural compounds purified from Ganoderma lucidum, ergosterol peroxide and ganodermanondiol. We found that these two compounds exhibited cytotoxicity not only against fast proliferating cells, but on quiescent, slow-cycling cells. Using a fibroblast cell-quiescence model, we found that the cytotoxicity on quiescent cells was due to induced apoptosis, and was associated with a shallower quiescent state in compound-treated cells, resultant from the increased basal activity of an Rb-E2F bistable switch that controls quiescence exit. Accordingly, we showed that quiescent breast cancer cells (MCF7), compared to its non-transformed counterpart (MCF10A), were preferentially killed by ergosterol peroxide and ganodermanondiol treatment presumably due to their already less stable quiescent state. The cytotoxic effect of natural Ganoderma lucidum compounds against quiescent cells, preferentially on quiescent cancer cells vs. non-cancer cells, may help future antitumor development against the slow-cycling cancer cell subpopulations including cancer stem and progenitor cells.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Medicamentos de Ervas Chinesas/farmacologia
Ergosterol/análogos & derivados
Lanosterol/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/farmacologia
Ciclo Celular/efeitos dos fármacos
Linhagem Celular
Linhagem Celular Tumoral
Ergosterol/farmacologia
Citometria de Fluxo
Seres Humanos
Lanosterol/farmacologia
Ratos
Reishi
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Drugs, Chinese Herbal); 104700-96-1 (ganodermadiol); 1J05Z83K3M (Lanosterol); UG9TN81TGH (ergosterol-5,8-peroxide); Z30RAY509F (Ergosterol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170119
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.14634


  6 / 806 MEDLINE  
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[PMID]:27894599
[Au] Autor:Zhang DH; Li N; Yu X; Zhao P; Li T; Xu JW
[Ad] Endereço:Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, 650500, China.
[Ti] Título:Overexpression of the homologous lanosterol synthase gene in ganoderic acid biosynthesis in Ganoderma lingzhi.
[So] Source:Phytochemistry;134:46-53, 2017 Feb.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ganoderic acids (GAs) in Ganoderma lingzhi exhibit anticancer and antimetastatic activities. GA yields can be potentially improved by manipulating G. lingzhi through genetic engineering. In this study, a putative lanosterol synthase (LS) gene was cloned and overexpressed in G. lingzhi. Results showed that its overexpression (OE) increased the ganoderic acid (GA) content and the accumulation of lanosterol and ergosterol in a submerged G. lingzhi culture. The maximum contents of GA-O, GA-Mk, GA-T, GA-S, GA-Mf, and GA-Me in transgenic strains were 46.6 ± 4.8, 24.3 ± 3.5, 69.8 ± 8.2, 28.9 ± 1.4, 15.4 ± 1.2, and 26.7 ± 3.1 µg/100 mg dry weight, respectively, these values being 6.1-, 2.2-, 3.2-, 4.8-, 2.0-, and 1.9-times higher than those in wild-type strains. In addition, accumulated amounts of lanosterol and ergosterol in transgenic strains were 2.3 and 1.4-fold higher than those in the control strains, respectively. The transcription level of LS was also increased by more than five times in the presence of the G. lingzhi glyceraldehyde-3-phosphate dehydrogenase gene promoter, whereas transcription levels of 3-hydroxy-3-methylglutaryl coenzyme A enzyme and squalene synthase did not change significantly in transgenic strains. This study demonstrated that OE of the homologous LS gene can enhance lanosterol accumulation. A large precursor supply promotes GA biosynthesis.
[Mh] Termos MeSH primário: Ganoderma
Transferases Intramoleculares/metabolismo
Triterpenos
[Mh] Termos MeSH secundário: Ergosterol/análise
Ganoderma/química
Ganoderma/enzimologia
Ganoderma/genética
Gliceraldeído-3-Fosfato Desidrogenase (Fosforiladora)/metabolismo
Transferases Intramoleculares/genética
Lanosterol/análise
Plantas Geneticamente Modificadas
Reishi/química
Triterpenos/química
Triterpenos/metabolismo
Triterpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Triterpenes); 0 (ganoderic acid); 0 (ganoderic acid Mf); 1J05Z83K3M (Lanosterol); EC 1.2.1.12 (Glyceraldehyde-3-Phosphate Dehydrogenase (Phosphorylating)); EC 5.4.- (Intramolecular Transferases); EC 5.4.99.7 (lanosterol synthase); Z30RAY509F (Ergosterol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170306
[Lr] Data última revisão:
170306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161130
[St] Status:MEDLINE


  7 / 806 MEDLINE  
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[PMID]:27329305
[Au] Autor:Katja DG; Farabi K; Nurlelasari; Harneti D; Mayanti T; Supratman U; Awang K; Hayashi H
[Ad] Endereço:a Faculty of Mathematics and Natural Sciences, Department of Chemistry , Universitas Padjadjaran , Jatinangor 45363 , Indonesia.
[Ti] Título:Cytototoxic constituents from the bark of Chisocheton cumingianus (Meliaceae).
[So] Source:J Asian Nat Prod Res;19(2):194-200, 2017 Feb.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new lanostane-type triterpenoid, 3ß-hydroxy-25-ethyl-lanost-9(11),24(24')-diene (1), along with 3ß-hydroxy-lanost-7-ene (2) and ß-sitosterol-3-O-acetate (3) was isolated from the stem bark of C. cumingianus. The chemical structure of the new compound was elucidated on the basis of spectroscopic data. All of the compounds were evaluated for their cytotoxic effects against P-388 murine leukemia cells. Compounds 1-3 showed cytotoxicity against P-388 murine leukemia cells with IC values of 28.8 ± 0.10, 4.29 ± 0.03, and 100.18 ± 0.16 µg/ml, respectively.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/farmacologia
Meliaceae/química
Casca de Planta/química
Sitosteroides/isolamento & purificação
Triterpenos/isolamento & purificação
Triterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/química
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Concentração Inibidora 50
Lanosterol/análogos & derivados
Leucemia P388
Camundongos
Estrutura Molecular
Sitosteroides/química
Sitosteroides/farmacologia
Triterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3beta-hydroxy-25-ethyl-lanost-9(11),24(24')-diene); 0 (3beta-hydroxy-lanost-7-ene); 0 (Antineoplastic Agents, Phytogenic); 0 (Sitosterols); 0 (Triterpenes); 0 (beta-sitosterol-3-O-acetate); 1J05Z83K3M (Lanosterol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170324
[Lr] Data última revisão:
170324
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160623
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2016.1196671


  8 / 806 MEDLINE  
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[PMID]:28314390
[Au] Autor:Schrack S; Hohl C; Schwack W
[Ad] Endereço:State Laboratory of the Canton Basel-City, CH-4056 Basel, Switzerland. Electronic address: sonja.schrack@bs.ch.
[Ti] Título:Oxysterols in cosmetics-Determination by planar solid phase extraction and gas chromatography-mass spectrometry.
[So] Source:J Chromatogr A;1473:10-18, 2016 Nov 18.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Sterol oxidation products (SOPs) are linked to several toxicological effects. Therefore, investigation of potential dietary uptake sources particularly food of animal origin has been a key issue for these compounds. For the simultaneous determination of oxysterols from cholesterol, phytosterols, dihydrolanosterol and lanosterol in complex cosmetic matrices, planar solid phase extraction (pSPE) was applied as clean-up tool. SOPs were first separated from more non-polar and polar matrix constituents by normal phase thin-layer chromatography and then focussed into one target zone. Zone extraction was performed with the TLC-MS interface, followed by gas chromatography-mass spectrometry analysis. pSPE showed to be effective for cleaning up cosmetic samples as sample extracts were free of interferences, and gas chromatographic columns did not show any signs of overloading. Recoveries were between 86 and 113% with relative standard deviations of below 10% (n=6). Results of our market survey in 2016 showed that some cosmetics with ingredients of plant origin contained phytosterol oxidation products (POPs) in the low ppm range and therefore in line with levels reported for food. In lanolin containing products, total SOPs levels (cholesterol oxidation products (COPs), lanosterol oxidation products (LOPs), dihydrolanosterol oxidation products (DOPs)) being in the low percent range exceeded reported levels for food by several orders of magnitudes.
[Mh] Termos MeSH primário: Cosméticos/química
Cromatografia Gasosa-Espectrometria de Massas/métodos
Oxisteróis/análise
Extração em Fase Sólida/métodos
[Mh] Termos MeSH secundário: Animais
Colesterol/análise
Colesterol/metabolismo
Cromatografia em Camada Delgada
Lanolina/análise
Lanolina/metabolismo
Lanosterol/análogos & derivados
Lanosterol/análise
Lanosterol/metabolismo
Oxirredução
Oxisteróis/metabolismo
Fitosteróis/análise
Fitosteróis/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cosmetics); 0 (Oxysterols); 0 (Phytosterols); 1J05Z83K3M (Lanosterol); 8006-54-0 (Lanolin); 97C5T2UQ7J (Cholesterol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170404
[Lr] Data última revisão:
170404
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170319
[St] Status:MEDLINE


  9 / 806 MEDLINE  
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[PMID]:28008815
[Au] Autor:Suarez-Medellin J; Meza-Menchaca T; Carranza JA; Trigos A; Vidal-Limon AM
[Ad] Endereço:Centro de Investigaciones Cerebrales (CICE), Universidad Veracruzana. Av. Dr. Luis Castelazo Ayala s/n, Colonia Industrial Animas, 9119, Xalapa, Veracruz, Mexico.
[Ti] Título:In Silico Analysis of Lanostanoids Characterized in Ganoderma Mushrooms (Agaricomycetes) as Potential Ligands of the Vitamin D Receptor.
[So] Source:Int J Med Mushrooms;18(11):1037-1047, 2016.
[Is] ISSN:1940-4344
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The metabolism of vitamin D is a very important pathway involved in the regulation of sterols and maintenance of cell health. The physiological activity of the human hormone 1α,25-dihydroxyvitamin D3, or calcitriol, is mediated by the vitamin D receptor (VDR), an endocrine member of the nuclear receptor superfamily that inhibits cell growth and stimulates cell differentiation, suggesting a potential application in cancer chemoprevention. Since nonpolar extracts obtained from Ganoderma mushrooms have also been shown to exert an antiproliferative effect on several cancer cell lines, it was suggested that at least part of its activity might be mediated by VDR. The aim of this work was to identify possible VDR ligands from an extensive library of lanostanoids isolated from several Ganoderma mushrooms. Using an in silico approach, 30 lanostanoids were found to interact with the VDR ligand-binding pocket in the same way as calcitriol. The possible implications of using these compounds are discussed here.
[Mh] Termos MeSH primário: Lanosterol/análogos & derivados
Receptores de Calcitriol/metabolismo
[Mh] Termos MeSH secundário: Simulação por Computador
Ganoderma/metabolismo
Lanosterol/química
Lanosterol/isolamento & purificação
Lanosterol/metabolismo
Ligantes
Ligação Proteica
Receptores de Calcitriol/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ligands); 0 (Receptors, Calcitriol); 0 (lanostanoid); 1J05Z83K3M (Lanosterol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170308
[Lr] Data última revisão:
170308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161224
[St] Status:MEDLINE
[do] DOI:10.1615/IntJMedMushrooms.v18.i11.80


  10 / 806 MEDLINE  
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[PMID]:27808511
[Au] Autor:Lai KH; Lu MC; Du YC; El-Shazly M; Wu TY; Hsu YM; Henz A; Yang JC; Backlund A; Chang FR; Wu YC
[Ad] Endereço:Graduate Institute of Natural Products, College of Pharmacy, Kaohsiung Medical University , Kaohsiung 807, Taiwan.
[Ti] Título:Cytotoxic Lanostanoids from Poria cocos.
[So] Source:J Nat Prod;79(11):2805-2813, 2016 Nov 23.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Six new and 16 known lanostanoids were isolated from the sclerotia of Poria cocos. The structures of the new isolates were elucidated to be 16α-hydroxy-3-oxo-24-methyllanosta-5,7,9(11),24(31)-tetraen-21-oic acid (1), 3ß,16α,29-trihydroxy-24-methyllanosta-7,9(11),24(31)-trien-21-oic acid (2), 3ß,16α,30-trihydroxy-24-methyllanosta-7,9(11),24(31)-trien-21-oic acid (3), 3ß-acetoxy-16α,24ß-dihydroxylanosta-7,9(11),25-trien-21-oic acid (4), 3ß,16α-dihydroxy-7-oxo-24-methyllanosta-8,24(31)-dien-21-oic acid (5), and 3α,16α-dihydroxy-7-oxo-24-methyllanosta-8,24(31)-dien-21-oic acid (6), based on extensive spectroscopic analyses. The absolute configuration of 4 was determined using Mosher's method. The antiproliferative activity of the isolated compounds (except 3 and 4) was evaluated against four leukemic cell lines (Molt 4, CCRF-CEM, HL 60, and K562). Dehydropachymic acid (9), dehydroeburicoic acid (12), pachymic acid (14), and lanosta-7,9(11),24-trien-21-oic acid (20) exhibited an antiproliferative effect on the CCRF-CEM cancer cell line with IC values of 2.7, 6.3, 4.9, and 13.1 µM, respectively. Both dehydropachymic acid (9) and dehydroeburicoic acid (12) showed antiproliferative effects against Molt 4 (IC 13.8 and 14.3 µM) and HL 60 (IC 7.3 and 6.0 µM) leukemic cell lines. Primary computational analysis using a chemical global positioning system for natural products (ChemGPS-NP) on the active lanostanoids from P. cocos suggested that targets other than topoisomerases may be involved in the antiproliferative activity.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos
Produtos Biológicos
Lanosterol/análogos & derivados
Wolfiporia/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química
Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/farmacologia
Produtos Biológicos/química
Produtos Biológicos/isolamento & purificação
Produtos Biológicos/farmacologia
DNA Topoisomerases/metabolismo
Ensaios de Seleção de Medicamentos Antitumorais
Células HL-60
Seres Humanos
Concentração Inibidora 50
Lanosterol/química
Lanosterol/isolamento & purificação
Lanosterol/farmacologia
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Triterpenos/química
Triterpenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Biological Products); 0 (Triterpenes); 0 (dehydroeburicoic acid); 0 (lanostanoid); 1J05Z83K3M (Lanosterol); EC 5.99.1.- (DNA Topoisomerases); X2FCK16QAH (pachymic acid)
[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:161104
[St] Status:MEDLINE



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