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  1 / 1928 MEDLINE  
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[PMID]:28633536
[Au] Autor:Ahmed A; Li W; Zhang JS; Sam PH; Zou YH; Tang GH; Yin S
[Ad] Endereço:a School of Pharmaceutical Sciences , Sun Yat-sen University , Guangzhou , China.
[Ti] Título:A new bisabolane sesquiterpenoid and a new abietane diterpenoid from Cephalotaxus sinensis.
[So] Source:Nat Prod Res;32(2):175-181, 2018 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Phytochemical investigation of Cephalotaxus sinensis has led to the isolation of a new bisabolane sesquiterpenoid (1), a new abietane diterpenoid (2), and 13 known compounds (3-15). Their structures were elucidated by extensive spectroscopic analysis (MS, UV, IR, and NMR).
[Mh] Termos MeSH primário: Cephalotaxus/química
Diterpenos Abietanos/isolamento & purificação
Sesquiterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Diterpenos Abietanos/química
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Compostos Fitoquímicos/química
Compostos Fitoquímicos/isolamento & purificação
Sesquiterpenos/química
Análise Espectral
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes, Abietane); 0 (Phytochemicals); 0 (Sesquiterpenes)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180228
[Lr] Data última revisão:
180228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170622
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2017.1343323


  2 / 1928 MEDLINE  
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[PMID]:28470116
[Au] Autor:Hu CL; Xiong J; Xiao CX; Tang Y; Ma GL; Wan J; Hu JF
[Ad] Endereço:a Department of Natural Products Chemistry , School of Pharmacy, Fudan University , Shanghai 201203 , China.
[Ti] Título:Anti-neuroinflammatory diterpenoids from the endangered conifer Podocarpus imbricatus.
[So] Source:J Asian Nat Prod Res;20(2):101-108, 2018 Feb.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Ten diterpenoids including three new abietanes (1-3) were isolated from the twigs and needles of Podocarpus imbricatus, an endangered conifer growing in a Cantonese garden. The new structures were established by means of spectroscopic methods. Among the isolates, 3ß-hydroxy-abieta-8,11,13-trien-7-one (5), decandrin G (6), and 7,15-pimaradien-18-oic acid (8) showed significant anti-neuroinflammatory activities by inhibiting the overproduction of nitric oxide (NO) in lipopolysaccharide (LPS)-stimulated murine BV-2 microglial cells, with IC values of 3.7, 11.1, and 4.5 µM, respectively.
[Mh] Termos MeSH primário: Coniferophyta/química
Diterpenos Abietanos/isolamento & purificação
Diterpenos Abietanos/farmacologia
[Mh] Termos MeSH secundário: Animais
Lipopolissacarídeos/farmacologia
Camundongos
Microglia/efeitos dos fármacos
Estrutura Molecular
Óxido Nítrico/biossíntese
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes, Abietane); 0 (Lipopolysaccharides); 31C4KY9ESH (Nitric Oxide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180202
[Lr] Data última revisão:
180202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2017.1319821


  3 / 1928 MEDLINE  
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[PMID]:29196256
[Au] Autor:Yang D; Fang Y; Xia P; Zhang X; Liang Z
[Ad] Endereço:Key Laboratory of Plant Secondary Metabolism and Regulation of Zhejiang Province, College of Life Sciences, Zhejiang Sci-Tech University, Hangzhou, China.
[Ti] Título:Diverse responses of tanshinone biosynthesis to biotic and abiotic elicitors in hairy root cultures of Salvia miltiorrhiza and Salvia castanea Diels f. tomentosa.
[So] Source:Gene;643:61-67, 2018 Feb 15.
[Is] ISSN:1879-0038
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Salvia miltiorrhiza (S. miltiorrhiza) and Salvia castanea Diels f. tomentosa (S. castanea) are both used for treatment of cardiovascular diseases. They have the same bioactive compound tanshinones, but whose contents are hugely different. This study illustrated diverse responses of tanshinone biosynthesis to yeast extract (YE) and Ag in hairy roots of the two species. YE enhanced both the growth and tanshinone biosynthesis of two hairy roots, and contributed more to tanshinone accumulation in S. castanea than that in S. miltiorrhiza. Genes encoding 1-deoxy-d-xylulose 5-phosphate synthase (DXS2), geranylgeranyl diphosphatesynthase (GGPPS1), copalyl diphosphate synthase (CPS1), and two cytochromes P450 (CYP76AH1 and CYP76AH3) were also more responsive to YE in S. castanea than those in S. miltiorrhiza. Accumulations of dihydrotanshinone I and tanshinone I, and most biosynthetic genes in S. miltiorrhiza were more responsive to Ag than those in S. castanea. Accumulations of dihydrotanshinone I and cryptotanshinone were more responsive to YE, while tanshinone IIA accumulation was more responsive to Ag in S. miltiorrhiza. However, accumulations of other four tanshinones and related genes in S. castanea were more responsive to YE than Ag . This study provides foundations for studying diverse specialized metabolism between the related species.
[Mh] Termos MeSH primário: Diterpenos Abietanos/biossíntese
Salvia miltiorrhiza/genética
Salvia miltiorrhiza/metabolismo
[Mh] Termos MeSH secundário: Alquil e Aril Transferases/genética
Alquil e Aril Transferases/metabolismo
Sistema Enzimático do Citocromo P-450/genética
Sistema Enzimático do Citocromo P-450/metabolismo
Farnesiltranstransferase/genética
Farnesiltranstransferase/metabolismo
Regulação da Expressão Gênica de Plantas/genética
Medicina Tradicional Chinesa
Proteínas de Plantas/genética
Proteínas de Plantas/metabolismo
Raízes de Plantas/metabolismo
Salvia/genética
Prata/metabolismo
Transferases/genética
Transferases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes, Abietane); 0 (Plant Proteins); 03UUH3J385 (tanshinone); 3M4G523W1G (Silver); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 2.- (Transferases); EC 2.2.1.- (deoxyxylulose-5-phosphate synthase); EC 2.5.- (Alkyl and Aryl Transferases); EC 2.5.1.- (ent-kaurene synthetase A); EC 2.5.1.29 (Farnesyltranstransferase)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180123
[Lr] Data última revisão:
180123
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171203
[St] Status:MEDLINE


  4 / 1928 MEDLINE  
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[PMID]:28985481
[Au] Autor:Gao H; Huang H; Zheng A; Yu N; Li N
[Ad] Endereço:School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110013, China.
[Ti] Título:Determination of quantitative retention-activity relationships between pharmacokinetic parameters and biological effectiveness fingerprints of Salvia miltiorrhiza constituents using biopartitioning and microemulsion high-performance liquid chromatography.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1067:10-17, 2017 Nov 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this study, we analyzed danshen (Salvia miltiorrhiza) constituents using biopartitioning and microemulsion high-performance liquid chromatography (MELC). The quantitative retention-activity relationships (QRARs) of the constituents were established to model their pharmacokinetic (PK) parameters and chromatographic retention data, and generate their biological effectiveness fingerprints. A high-performance liquid chromatography (HPLC) method was established to determine the abundance of the extracted danshen constituents, such as sodium danshensu, rosmarinic acid, salvianolic acid B, protocatechuic aldehyde, cryptotanshinone, and tanshinone IIA. And another HPLC protocol was established to determine the abundance of those constituents in rat plasma samples. An experimental model was built in Sprague Dawley (SD) rats, and calculated the corresponding PK parameterst with 3P97 software package. Thirty-five model drugs were selected to test the PK parameter prediction capacities of the various MELC systems and to optimize the chromatographic protocols. QRARs and generated PK fingerprints were established. The test included water/oil-soluble danshen constituents and the prediction capacity of the regression model was validated. The results showed that the model had good predictability.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Medicamentos de Ervas Chinesas/química
Medicamentos de Ervas Chinesas/farmacocinética
Salvia miltiorrhiza/química
[Mh] Termos MeSH secundário: Animais
Área Sob a Curva
Benzofuranos/sangue
Benzofuranos/química
Benzofuranos/farmacocinética
Cinamatos/sangue
Cinamatos/química
Cinamatos/farmacocinética
Depsídeos/sangue
Depsídeos/química
Depsídeos/farmacocinética
Diterpenos Abietanos/sangue
Diterpenos Abietanos/química
Diterpenos Abietanos/farmacocinética
Emulsões/química
Masculino
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Tensoativos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzofurans); 0 (Cinnamates); 0 (Depsides); 0 (Diterpenes, Abietane); 0 (Drugs, Chinese Herbal); 0 (Emulsions); 0 (Surface-Active Agents); 03UUH3J385 (tanshinone); 79483-68-4 (dan-shen root extract); C1GQ844199 (salvianolic acid B); MQE6XG29YI (rosmarinic acid)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171007
[St] Status:MEDLINE


  5 / 1928 MEDLINE  
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[PMID]:28953930
[Au] Autor:Bai Z; Xia P; Wang R; Jiao J; Ru M; Liu J; Liang Z
[Ad] Endereço:College of Life Science, Northwest A&F University, Yangling, China.
[Ti] Título:Molecular cloning and characterization of five SmGRAS genes associated with tanshinone biosynthesis in Salvia miltiorrhiza hairy roots.
[So] Source:PLoS One;12(9):e0185322, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The gibberellin-responsive element binding factor (GRAS) family of proteins plays an important role in the transcriptional regulation of plant development and hormone signaling. To date, there are no reports on GRAS family proteins expressed in Salvia miltiorrhiza. In this study, 28 ESTs that contained the GRAS domain were identified from a S. miltiorrhiza cDNA library. Of these, full-length sequences of five genes were cloned and sequence analysis indicated that all five proteins contain only one GRAS domain and therefore, belong to the GRAS family. The five genes were designated S. miltiorrhiza GRAS1-5 (SmGRAS1-5), which belong to groups I (SmGRAS2 and SmGRAS4), II (SmGRAS3), III (SmGRAS1), and VIII (SmGRAS5) respectively. Additionally, SmGRAS1-5 have different expression patterns in the reed head, stems, leaves, flowers, and roots of S. miltiorrhiza. In this study, the expression of SmGRAS1-5 was sensitive to Gibberellin (GA) stress and that of SmGRAS1, SmGRAS4 and SmGRAS5 was sensitive to Ethephon (Eth) stress respectively. Moreover, S. miltiorrhiza copalyl diphosphate synthases 1 (SmCPS1) and S. miltiorrhiza kaurene synthase like 1 (SmKSL1), which are two key enzymes gene in the diterpenoid biosynthesis pathway, were also response to GA and Eth stress. In addition, Dihydrotanshinone (DT-I) and Tanshinone I (T-I) content were enhanced by GA and Eth stress, Tanshinone IIA (T-IIA) content was increased by GA stress, and the accumulation of Cryptotanshinone (CT) was insensitive to both GA and Eth stress. Together, these results provide insights into functional conservation and diversification of SmGRASs and are useful information for further elucidating SmGRAS functions.
[Mh] Termos MeSH primário: Vias Biossintéticas/genética
Diterpenos Abietanos/biossíntese
Genes de Plantas
Proteínas de Plantas/genética
Raízes de Plantas/genética
Salvia miltiorrhiza/genética
[Mh] Termos MeSH secundário: Motivos de Aminoácidos
Sequência de Aminoácidos
Sequência de Bases
Vias Biossintéticas/efeitos dos fármacos
Clonagem Molecular
Sequência Conservada/genética
Perfilação da Expressão Gênica
Regulação da Expressão Gênica de Plantas/efeitos dos fármacos
Giberelinas/farmacologia
Especificidade de Órgãos/efeitos dos fármacos
Especificidade de Órgãos/genética
Compostos Organofosforados/farmacologia
Fenantrenos/metabolismo
Filogenia
Proteínas de Plantas/química
Proteínas de Plantas/metabolismo
Raízes de Plantas/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes, Abietane); 0 (Gibberellins); 0 (Organophosphorus Compounds); 0 (Phenanthrenes); 0 (Plant Proteins); 03UUH3J385 (tanshinone); XU5R5VQ87S (ethephon)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170928
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0185322


  6 / 1928 MEDLINE  
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[PMID]:28918123
[Au] Autor:Zhang X; Chen Y; Cai G; Li X; Wang D
[Ad] Endereço:School of Life Sciences, Jilin University, Jilin, 130012, China. Electronic address: xrzhang15@mails.jlu.edu.cn.
[Ti] Título:Carnosic acid induces apoptosis of hepatocellular carcinoma cells via ROS-mediated mitochondrial pathway.
[So] Source:Chem Biol Interact;277:91-100, 2017 Nov 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Carnosic acid (CA), an important bioactive phenolic diterpene mainly found in labiate plants, exerts various biological functions, including antioxidant, anti-inflammatory, antitumor, and neuroprotective activities. In the present study, we proved the deleterious effects of CA against hepatocellular carcinoma (HCC) in both in vitro and in vivo models. In vitro, CA significantly decreased cell viability, inhibited cell proliferation and migration, enhanced apoptosis, and increased caspase-3, -8, and -9 activities in HepG2 and SMMC-7721 cells. Specifically, CA led to a decreased mitochondrial membrane potential (MMP) and increases in intracellular reactive oxygen species (ROS) levels and apoptosis-related protein expression. Pre-incubation of HCC cells with N-Acetyl-l-cysteine (NAC), a ROS inhibitor, strongly suppressed CA-induced apoptotic phenomena, including reduced cell viability, excessive ROS levels, MMP decreases, and abnormal protein expression, suggesting an association of CA-induced apoptosis with oxidative stress-mediated mitochondrial pathways. In HepG2-and SMMC-7721-xenograft tumor mouse models, treatment with CA inhibited tumor growth and modulated apoptosis-related protein expression, confirming the anti-HCC effects of this chemical. Moreover, the CA-mediated anti-HCC effects associated with oxidative stress provide experimental evidence to support the potential use of CA as a drug therapy for HCC.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Carcinoma Hepatocelular/tratamento farmacológico
Diterpenos Abietanos/farmacologia
Neoplasias Hepáticas/tratamento farmacológico
Espécies Reativas de Oxigênio/metabolismo
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/uso terapêutico
Carcinoma Hepatocelular/metabolismo
Carcinoma Hepatocelular/patologia
Diterpenos Abietanos/uso terapêutico
Células Hep G2
Seres Humanos
Neoplasias Hepáticas/metabolismo
Neoplasias Hepáticas/patologia
Masculino
Camundongos Endogâmicos BALB C
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Diterpenes, Abietane); 0 (Reactive Oxygen Species); LI791SXT24 (salvin)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170918
[St] Status:MEDLINE


  7 / 1928 MEDLINE  
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[PMID]:28877257
[Au] Autor:Bahri S; Mies F; Ben Ali R; Mlika M; Jameleddine S; Mc Entee K; Shlyonsky V
[Ad] Endereço:Department of physiology, University of Tunis El Manar, La Rabta, Tunis, Tunisia.
[Ti] Título:Rosmarinic acid potentiates carnosic acid induced apoptosis in lung fibroblasts.
[So] Source:PLoS One;12(9):e0184368, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pulmonary fibrosis is characterized by over-population and excessive activation of fibroblasts and myofibroblasts disrupting normal lung structure and functioning. Rosemary extract rich in carnosic acid (CA) and rosmarinic acid (RA) was reported to cure bleomycin-(BLM)-induced pulmonary fibrosis. We demonstrate that CA decreased human lung fibroblast (HLF) viability with IC50 value of 17.13±1.06 µM, while RA had no cytotoxic effect. In the presence of 50 µM of RA, dose-response for CA shifted to IC50 value of 11.70±1.46 µM, indicating synergic action. TGFß-transformed HLF, rat lung fibroblasts and L929 cells presented similar sensitivity to CA and CA+RA (20µM+100µM, respectively) treatment. Rat alveolar epithelial cells died only under CA+RA treatment, while A549 cells were not affected. Annexin V staining and DNA quantification suggested that HLF are arrested in G0/G1 cell cycle phase and undergo apoptosis. CA caused sustained activation of phospho-Akt and phospho-p38 expression and inhibition of p21 protein.Addition of RA potentiated these effects, while RA added alone had no action.Only triple combination of inhibitors (MAPK-p38, pan-caspase, PI3K/Akt/autophagy) partially attenuated apoptosis; this suggests that cytotoxicity of CA+RA treatment has a complex mechanism involving several parallel signaling pathways. The in vivo antifibrotic effect of CA and RA was compared with that of Vitamine-E in BLM-induced fibrosis model in rats. We found comparable reduction in fibrosis score by CA, RA and CA+RA, attenuation of collagen deposition and normalization of oxidative stress markers. In conclusion, antifibrotic effect of CA+RA is due to synergistic pro-apoptotic action on lung fibroblasts and myofibroblasts.
[Mh] Termos MeSH primário: Apoptose
Cinamatos/farmacologia
Depsídeos/farmacologia
Diterpenos Abietanos/farmacologia
Fibroblastos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Bleomicina
Catalase/metabolismo
Ciclo Celular
Linhagem Celular
Movimento Celular
Proliferação Celular/efeitos dos fármacos
Colágeno/metabolismo
Seres Humanos
Hidroxiprolina/metabolismo
Concentração Inibidora 50
Peroxidação de Lipídeos
Pulmão/citologia
Masculino
Camundongos
Estresse Oxidativo
Extratos Vegetais/farmacologia
Alvéolos Pulmonares/metabolismo
Fibrose Pulmonar/tratamento farmacológico
Ratos
Ratos Wistar
Transdução de Sinais
Superóxido Dismutase/metabolismo
Vitamina E/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cinnamates); 0 (Depsides); 0 (Diterpenes, Abietane); 0 (Plant Extracts); 11056-06-7 (Bleomycin); 1406-18-4 (Vitamin E); 9007-34-5 (Collagen); EC 1.11.1.6 (Catalase); EC 1.15.1.1 (Superoxide Dismutase); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); LI791SXT24 (salvin); MQE6XG29YI (rosmarinic acid); RMB44WO89X (Hydroxyproline)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0184368


  8 / 1928 MEDLINE  
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[PMID]:28875214
[Au] Autor:Hanson JR
[Ad] Endereço:Department of Chemistry, University of Sussex, UK.
[Ti] Título:Diterpenoids of terrestrial origin.
[So] Source:Nat Prod Rep;34(10):1233-1243, 2017 Oct 18.
[Is] ISSN:1460-4752
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Covering: January to December, 2016 previous review Nat. Prod. Rep., 2016, 33, 1227-1238This review covers the isolation and chemistry of diterpenoids from terrestrial as opposed to marine sources and includes labdanes, clerodanes, abietanes, pimaranes, kauranes, cembrenes and their cyclization products. There are 205 references.
[Mh] Termos MeSH primário: Diterpenos
[Mh] Termos MeSH secundário: Ciclização
Diterpenos Abietanos
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Plantas Medicinais/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Diterpenes); 0 (Diterpenes, Abietane)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE
[do] DOI:10.1039/c7np00040e


  9 / 1928 MEDLINE  
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[PMID]:28864041
[Au] Autor:Tóth B; Kúsz N; Forgo P; Bózsity N; Zupkó I; Pinke G; Hohmann J; Vasas A
[Ad] Endereço:Department of Pharmacognosy, University of Szeged, 6720 Szeged, Hungary.
[Ti] Título:Abietane diterpenoids from Sideritis montana L. and their antiproliferative activity.
[So] Source:Fitoterapia;122:90-94, 2017 Oct.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The present study aimed at the phytochemical and pharmacological investigation of Sideritis montana L. (Lamiaceae). Two new abietane diterpenes [sideritins A (1) and B (2)] were isolated from the methanol extract of the plant. Six known compounds [pomiferin E (3), 9α,13α-epi-dioxyabiet-8(14)-en-18-ol (4), paulownin (5), 6-methoxysakuranetin (6), 3-oxo-α-ionol (7) and 4-allyl-2,6-dimethoxyphenol glucoside (8)] were also obtained from the plant. The structures were determined by means of HREIMS and NMR experiments. The antiproliferative effect of the isolated compounds was investigated on human cancer cell lines (HeLa, SiHa and C33A) at 10 and 30µM concentrations, using the MTT assay. The results demonstrated that pomiferin E (3) and 6-methoxysakuranetin (6) displayed considerable activity [inhibition (%)±SEM: 46.93±2.35 on HeLa (pomiferin E), and 51.52±2.45 on C33A (6-methoxysakuranetin)] at 30µM concentration.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia
Diterpenos Abietanos/farmacologia
Sideritis/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/isolamento & purificação
Linhagem Celular Tumoral
Diterpenos Abietanos/isolamento & purificação
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Diterpenes, Abietane)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171103
[Lr] Data última revisão:
171103
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170903
[St] Status:MEDLINE


  10 / 1928 MEDLINE  
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[PMID]:28797788
[Au] Autor:Wiemann J; Loesche A; Csuk R
[Ad] Endereço:Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
[Ti] Título:Novel dehydroabietylamine derivatives as potent inhibitors of acetylcholinesterase.
[So] Source:Bioorg Chem;74:145-157, 2017 Oct.
[Is] ISSN:1090-2120
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Nowadays, the inhibition of acetylcholinesterase is one of the main pharmacological strategies for the treatment of Alzheimer's disease. Therefore, a set of thirty-four derivatives of the diterpenoid dehydroabietylamine has been synthesized and screened in colorimetric Ellman's assays to determine their ability to inhibit the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). A systematic variation of the substitution of dehydroabietylamides enabled an approach to analogs showing a remarkable inhibition potency for AChE. Particularly N-benzoyldehydroabietylamines 11, 12 and 13 were excellent inhibitors for AChE, showing inhibition rates comparable to standard galantamine hydrobromide.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Inibidores da Colinesterase/farmacologia
Diterpenos Abietanos/farmacologia
[Mh] Termos MeSH secundário: Animais
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Diterpenos Abietanos/síntese química
Diterpenos Abietanos/química
Relação Dose-Resposta a Droga
Electrophorus
Conformação Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Diterpenes, Abietane); 0 (dehydroabietylamine); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170812
[St] Status:MEDLINE



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