Base de dados : MEDLINE
Pesquisa : B01.650.940.800.575.912.250.100.989 [Categoria DeCS]
Referências encontradas : 55 [refinar]
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[PMID]:28480428
[Au] Autor:Venkatesh U; Javarasetty C; Murari SK
[Ad] Endereço:Department of Biochemistry, Bharathiar University, Coimbatore-641 046, Tamilnadu, India.
[Ti] Título:PURIFICATION AND FRACTIONAL ANALYSIS OF METHANOLIC EXTRACT OF POSSESSING APOPTOTIC AND ANTI-LEUKEMIC ACTIVITY.
[So] Source:Afr J Tradit Complement Altern Med;14(3):167-174, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: ( .) (WT), commonly known as yellow dots or creeping daisy, is a shrub possessing potent biological activities, and is traditionally used a medicinal plant in Ayurveda, Siddha and Unani systems of medicines, and it has also been tried against leukemia cell line MEG- 01. In the present study, purification and screening of the plant was done for bioactive compounds in methanolic extract of WT for apoptotic and anti-leukemia activity. MATERIALS AND METHODS: The methanolic extract of WT was initially purified through thin layer chromatography (TLC) and screened for the apoptotic and anti-leukemia activities. The positive band of TLC was subjected to silica gel column chromatography for further purification and the fractions obtained from it were screened again for anti-leukemia activity through thymidine uptake assay and apoptotic activity by DNA fragmentation, nuclear staining and flow cytometry assays. The fraction with positive result was subjected to HPLC for analysis of bioactive components. RESULTS: Out of many combinations of solvents, the methanol and dichloromethane combination in the ratio 6:4 has revealed two bands in TLC, among which the second band showed positive results for apoptotic and anti-leukemic activities. Further purification of second band through silica gel chromatography gave five fractions in which the 3 fraction gave positive results and it shows single peak during compositional analysis through HPLC. CONCLUSION: The single peak revealed through HPLC indicates the presence of pure compound with apoptotic and anti-leukemia activities encouraging for further structural analysis.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação
Apoptose/efeitos dos fármacos
Metanol/isolamento & purificação
Extratos Vegetais/isolamento & purificação
Wedelia/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/química
Antineoplásicos Fitogênicos/farmacologia
Linhagem Celular Tumoral
Cromatografia em Camada Delgada
Seres Humanos
Megacariócitos/efeitos dos fármacos
Metanol/farmacologia
Cloreto de Metileno
Extratos Vegetais/química
Extratos Vegetais/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Plant Extracts); 588X2YUY0A (Methylene Chloride); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170815
[Lr] Data última revisão:
170815
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170509
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i3.18


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[PMID]:28155120
[Au] Autor:Verma A; Ahmed B; Anwar F; Rahman M; Patel DK; Kaithwas G; Rani R; Bhatt PC; Kumar V
[Ad] Endereço:Bio-organic and Medicinal Chemistry Research Laboratory, Department of Pharmaceutical Sciences, Faculty of Health Sciences, Sam Higginbottom University of Agriculture, Technology and Sciences, Allahabad, Uttar Pradesh, 211007, India.
[Ti] Título:Novel glycoside from Wedelia calendulacea inhibits diethyl nitrosamine-induced renal cancer via downregulating the COX-2 and PEG through nuclear factor-κB pathway.
[So] Source:Inflammopharmacology;25(1):159-175, 2017 Feb.
[Is] ISSN:1568-5608
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-ß-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. The histopathological changes were observed in the HEG pre-treated group, which was proof for its safety concern as far as its toxicity is concerned. The isolated compound HEG can impart momentous chemo-protection against experimental RCC by suppressing the cyclooxygenase (COX-2) and prostaglandin E2 (PGE ) expression via nuclear factor-kappa B (NF-κB) pathway.
[Mh] Termos MeSH primário: Ciclo-Oxigenase 2/metabolismo
Dinoprostona/metabolismo
Glicosídeos/uso terapêutico
Neoplasias Renais/metabolismo
NF-kappa B/metabolismo
Wedelia
[Mh] Termos MeSH secundário: Animais
Dietilnitrosamina/toxicidade
Dinoprostona/antagonistas & inibidores
Relação Dose-Resposta a Droga
Regulação para Baixo/efeitos dos fármacos
Regulação para Baixo/fisiologia
Glicosídeos/isolamento & purificação
Glicosídeos/farmacologia
Neoplasias Renais/induzido quimicamente
Neoplasias Renais/prevenção & controle
Masculino
NF-kappa B/antagonistas & inibidores
Extratos Vegetais/isolamento & purificação
Extratos Vegetais/farmacologia
Extratos Vegetais/uso terapêutico
Ratos
Ratos Wistar
Transdução de Sinais/efeitos dos fármacos
Transdução de Sinais/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycosides); 0 (NF-kappa B); 0 (Plant Extracts); 3IQ78TTX1A (Diethylnitrosamine); EC 1.14.99.1 (Cyclooxygenase 2); K7Q1JQR04M (Dinoprostone)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171020
[Lr] Data última revisão:
171020
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170204
[St] Status:MEDLINE
[do] DOI:10.1007/s10787-017-0310-y


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[PMID]:28130826
[Au] Autor:Ma XH; Wang ZB; Zhang L; Li W; Deng CM; Zhong TH; Li GY; Zheng WM; Zhang YH
[Ad] Endereço:Key Laboratory of Natural Drug Pharmacology in Fujian Province, School of Pharmacy, Fujian Medical University, 88 Jiao Tong Road, Fuzhou, 350004, P. R. China.
[Ti] Título:Diterpenoids from Wedelia prostrata and Their Derivatives and Cytotoxic Activities.
[So] Source:Chem Biodivers;14(5), 2017 May.
[Is] ISSN:1612-1880
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:One new ent-kaurane diterpenoid, 11ß,16α-dihydroxy-ent-kauran-19-oic acid (1), together with eight known analogues 2 - 9 were isolated from the aerial parts of Wedelia prostrata. One of the acidic diterpenoids, kaurenoic acid (3), was converted to seven derivatives, 10 - 16. All compounds were evaluated for their cytotoxic activity in vitro against human leukemia (K562), liver (HepG-2), and stomach (SGC-7901) cancer cell lines. Only four kaurenoic acid derivatives, 13 - 16, with 15-keto and substitutions at C(19) position, exhibited notable cytotoxic activities on these tumor cell lines with IC value ranging from 0.05 to 3.71 µm. Compounds 10 - 12, with oxime on C(15) showed moderate inhibitory effects and compounds 1 - 9 showed no cytotoxicities on them. Structure-activity relationships were also discussed based on the experimental data obtained. The known derivative, 15-oxokaurenoic acid 4-piperdin-1-ylbutyl ester (17), induced typical apoptotic cell death in colon SW480 cells upon evaluation of the apoptosis-inducing activity by flow-cytometric analysis.
[Mh] Termos MeSH primário: Diterpenos/isolamento & purificação
Diterpenos/toxicidade
Wedelia/química
[Mh] Termos MeSH secundário: Antineoplásicos Fitogênicos/isolamento & purificação
Antineoplásicos Fitogênicos/farmacologia
Apoptose/efeitos dos fármacos
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Diterpenos Caurânicos/isolamento & purificação
Células Hep G2
Seres Humanos
Concentração Inibidora 50
Células K562
Componentes Aéreos da Planta/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Diterpenes); 0 (Diterpenes, Kaurane); 6730-83-2 (kaurenoic acid)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170731
[Lr] Data última revisão:
170731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170129
[St] Status:MEDLINE
[do] DOI:10.1002/cbdv.201600423


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[PMID]:27604295
[Au] Autor:Wu Z; Zhang Y; Yang L; Chen N; Jiang L; Jiang S; Li G; Li Y; Wang G
[Ad] Endereço:Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, 510632, People's Republic of China.
[Ti] Título:Three new ent-kaurane diterpenes from the herbs of Wedelia prostrata.
[So] Source:J Nat Med;71(1):305-309, 2017 Jan.
[Is] ISSN:1861-0293
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Three new ent-kaurane diterpenes, 3α-angeloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (1), 3α-tigloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (2) and 3α-cinnamoyloxykaur-9(11),16-dien-19-oic acid (3), along with five known compounds (4-8), were isolated from the herbs of Wedelia prostrata (Asteraceae). The structures were determined by extensive analysis of their spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The isolated compounds were evaluated for their cytotoxic activity on human hepatocellular carcinoma HepG2 cells. Among them, all isolates exhibited cytotoxic activities with IC values ranging from 9.55 ± 0.45 to 53.92 ± 1.22 µM.
[Mh] Termos MeSH primário: Diterpenos Caurânicos/química
Wedelia/química
[Mh] Termos MeSH secundário: Células Hep G2
Seres Humanos
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Diterpenes, Kaurane)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171104
[Lr] Data última revisão:
171104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160909
[St] Status:MEDLINE
[do] DOI:10.1007/s11418-016-1037-6


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[PMID]:27070557
[Au] Autor:Li SF; Ding JY; Li YT; Hao XJ; Li SL
[Ad] Endereço:State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China. lisf@sxu.edu.cn.
[Ti] Título:Antimicrobial Diterpenoids of Wedelia trilobata (L.) Hitchc.
[So] Source:Molecules;21(4):457, 2016 Apr 07.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Continued interest in the metabolites of Wedelia trilobata (L.) Hitchc, a notoriously invasive weed in South China, led to the isolation of twenty-six ent-kaurane diterpenoids, including seven new ones 1-7. Their structures and relative configuration were elucidated on the basis of extensive spectroscopic analysis, including 1D- and 2D-NMR experiments. The antimicrobial activities of all isolated diterpenoids were evaluated against a panel of bacteria and fungi.
[Mh] Termos MeSH primário: Anti-Infecciosos/química
Diterpenos Caurânicos/química
Extratos Vegetais/química
Wedelia/química
[Mh] Termos MeSH secundário: Anti-Infecciosos/farmacologia
Bactérias/efeitos dos fármacos
China
Diterpenos Caurânicos/isolamento & purificação
Diterpenos Caurânicos/farmacologia
Fungos/efeitos dos fármacos
Seres Humanos
Extratos Vegetais/farmacologia
Folhas de Planta/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Diterpenes, Kaurane); 0 (Plant Extracts)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160413
[St] Status:MEDLINE


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[PMID]:26969382
[Au] Autor:Huang W; Liang Y; Wang J; Li G; Wang G; Li Y; Chung HY
[Ad] Endereço:Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, P. R. China.
[Ti] Título:Anti-angiogenic activity and mechanism of kaurane diterpenoids from Wedelia chinensis.
[So] Source:Phytomedicine;23(3):283-92, 2016 Mar 15.
[Is] ISSN:1618-095X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Wedelia chinensis is a traditional medicinal herb used in Asia and it has been reported to possess various bioactivities including anti-inflammatory and anticancer effects. However, its anti-angiogenic activity has never been reported. PURPOSE: To determine the most potent anti-angiogenic component in W. chinensis and its molecular mechanism of action. STUDY DESIGN: Initially, the active fraction of the plant was studied. Then, we determined the active components of the fraction and explored the mechanism of the most active compound. METHODS: The ethanol extract of W. chinensis and its four fractions with different polarities were evaluated for their anti-angiogenic activity in the Zebrafish model using quantitative endogenous alkaline phosphatase (EAP) assay. The molecular mechanism of the most active compound from the active fraction was studied using the real-time polymerase chain reaction (PCR) assay on Zebrafish embryos. The inhibitory effect of the most active compound on the proliferation, invasion and tube formation steps of angiogenesis was evaluated using the vascular endothelial growth factor (VEGF)-induced human umbilical vein endothelial cells (HUVECs) model, and the influences of the active compound on tyrosine phosphorylation of VEGF receptor (VEGFR-2) and its downstream signal pathway were evaluated by western blotting assay. Moreover, its anti-angiogenic effect was further evaluated by the VEGF-induced sprouts formation on aortic ring assay and the VEGF-induced vessel formation of mice on matrigel plug assay, respectively. RESULTS: Petroleum ether (PE) fraction of the plant displayed potent anti-angiogenic activity. Twelve kaurane diterpenoids (1-12) isolated from this fraction showed quite different effects. Compounds 9-12 could dose-dependently inhibit vessel formation in the Zebrafish embryos while the others showed little inhibitory effect. Among the active diterpenoids, compound 10, 3α-cinnamoyloxy-9ß-hydroxy-ent-kaura-16-en-19-oic acid (CHKA), possessed the strongest effect, and it affected multiple molecular targets related to angiogenesis including VEGF and angiopoietin in Zerbrafish. Moreover, CHKA significantly inhibited a series of VEGF-induced angiogenesis processes including proliferation, invasion, and tube formation of endothelial cells. Besides, it directly inhibited VEGFR-2 tyrosine kinase activity and its downstream signaling pathways in HUVECs. CHKA also obviously inhibited sprouts formation of aortic ring, and block vessel formation in mice. CONCLUSION: Our findings demonstrate that kaurane diterpenoids is one of anti-angiogenic components in W. chinensis, and CHKA may become a promising candidate for the development of anti-angiogenic agent.
[Mh] Termos MeSH primário: Inibidores da Angiogênese/farmacologia
Diterpenos Caurânicos/farmacologia
Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos
Wedelia/química
[Mh] Termos MeSH secundário: Animais
Aorta/efeitos dos fármacos
Movimento Celular/efeitos dos fármacos
Embrião não Mamífero/efeitos dos fármacos
Seres Humanos
Camundongos
Camundongos Endogâmicos C57BL
Estrutura Molecular
Neovascularização Patológica/tratamento farmacológico
Fosforilação
Extratos Vegetais/farmacologia
Ratos Sprague-Dawley
Transdução de Sinais/efeitos dos fármacos
Fator A de Crescimento do Endotélio Vascular/farmacologia
Receptor 1 de Fatores de Crescimento do Endotélio Vascular/metabolismo
Receptor 2 de Fatores de Crescimento do Endotélio Vascular/metabolismo
Peixe-Zebra
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Angiogenesis Inhibitors); 0 (Diterpenes, Kaurane); 0 (Plant Extracts); 0 (Vascular Endothelial Growth Factor A); EC 2.7.10.1 (FLT1 protein, human); EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-1); EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-2)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160312
[Lr] Data última revisão:
160312
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160313
[St] Status:MEDLINE


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[PMID]:26879680
[Au] Autor:Dai ZC; Fu W; Qi SS; Zhai DL; Chen SC; Wan LY; Huang P; Du DL
[Ad] Endereço:Jingjiang College, Jiangsu University, Zhenjiang, 212013, China.
[Ti] Título:Different Responses of an Invasive Clonal Plant Wedelia trilobata and its Native Congener to Gibberellin: Implications for Biological Invasion.
[So] Source:J Chem Ecol;42(2):85-94, 2016 Feb.
[Is] ISSN:1573-1561
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The invasive clonal plant Wedelia trilobata contains higher levels of ent-kaurane diterpenes, which are precursors of gibberellins (GAs), and higher rates of clonal growth than its native congener W. chinensis in invaded habitats. We hypothesized that the higher levels of endogenous GAs facilitate greater ramet growth in W. trilobata compared with W. chinensis. We quantified endogenous levels of GA1+3 in the two species and compared their growth responses to the changes of endogenous and exogenous GA3 by using short-term and long-term hydroponics experiments. After a period of homogeneous cultivation, levels of endogenous GA1+3 were higher in W. trilobata than in W. chinensis. The reduction of endogenous GAs repressed the emergence of adventitious roots and the growth of W. trilobata in the initial cultivation stage, and inhibited its shoot elongation and biomass. Levels of endogenous GA1+3 were positively correlated with the length of shoots and adventitious roots of W. trilobata. Adventitious roots of W. trilobata also emerged earlier and grew faster when treated with exogenous GA3. In contrast, exogenous GA3 treatment inhibited the length of adventitious roots in W. chinensis, and levels of endogenous GA1+3 did not correlate with shoot or adventitious root length. Our study suggests that GAs accelerate the rapid clonal growth of W. trilobata, more than that of its native congener W. chinensis, illustrating the relationship between plant hormones and the clonal growth of invasive plants. These findings are important for understanding the mechanisms associated with the invasiveness of clonal plants and their potential management.
[Mh] Termos MeSH primário: Giberelinas/fisiologia
Espécies Introduzidas
Wedelia/fisiologia
[Mh] Termos MeSH secundário: Raízes de Plantas/crescimento & desenvolvimento
Wedelia/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Gibberellins)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:171027
[Lr] Data última revisão:
171027
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160217
[St] Status:MEDLINE
[do] DOI:10.1007/s10886-016-0670-6


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[PMID]:26042672
[Au] Autor:Lin WC; Wen CC; Chen YH; Hsiao PW; Liao JW; Peng CI; Yang NS
[Ad] Endereço:Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan; Institute of Plant Biology, National Taiwan University, Taipei, Taiwan.
[Ti] Título:Integrative approach to analyze biodiversity and anti-inflammatory bioactivity of Wedelia medicinal plants.
[So] Source:PLoS One;10(6):e0129067, 2015.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:For the development of "medical foods" and/or botanical drugs as defined USA FDA, clear and systemic characterizations of the taxonomy, index phytochemical components, and the functional or medicinal bioactivities of the reputed or candidate medicinal plant are needed. In this study, we used an integrative approach, including macroscopic and microscopic examination, marker gene analysis, and chemical fingerprinting, to authenticate and validate various species/varieties of Wedelia, a reputed medicinal plant that grows naturally and commonly used in Asian countries. The anti-inflammatory bioactivities of Wedelia extracts were then evaluated in a DSS-induced murine colitis model. Different species/varieties of Wedelia exhibited distinguishable morphology and histological structures. Analysis of the ribosomal DNA internal transcribed spacer (ITS) region revealed significant differences among these plants. Chemical profiling of test Wedelia species demonstrated candidate index compounds and distinguishable secondary metabolites, such as caffeic acid derivatives, which may serve as phytochemical markers or index for quality control and identification of specific Wedelia species. In assessing their effect on treating DSS induced-murine colitis, we observed that only the phytoextract from W. chinensis species exhibited significant anti-inflammatory bioactivity on DSS-induced murine colitis among the various Wedelia species commonly found in Taiwan. Our results provide a translational research approach that may serve as a useful reference platform for biotechnological applications of traditional phytomedicines. Our findings indicate that specific Wedelia species warrant further investigation for potential treatment of human inflammatory bowel disease.
[Mh] Termos MeSH primário: Anti-Inflamatórios/uso terapêutico
Biodiversidade
Plantas Medicinais/química
Wedelia/química
[Mh] Termos MeSH secundário: Doença Aguda
Animais
Anti-Inflamatórios/farmacologia
Sequência de Bases
Cromatografia Líquida de Alta Pressão
Colite/induzido quimicamente
Colite/tratamento farmacológico
Colite/patologia
DNA Intergênico/genética
Sulfato de Dextrana
Genótipo
Masculino
Camundongos Endogâmicos C57BL
Dados de Sequência Molecular
Extratos Vegetais/farmacologia
Extratos Vegetais/uso terapêutico
Folhas de Planta/química
Caules de Planta/química
Análise de Componente Principal
Alinhamento de Sequência
Especificidade da Espécie
Espectrometria de Massas por Ionização por Electrospray
Taiwan
Wedelia/anatomia & histologia
Wedelia/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (DNA, Intergenic); 0 (Plant Extracts); 9042-14-2 (Dextran Sulfate)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150605
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0129067


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[PMID]:25946251
[Au] Autor:Guimarães DS; Fonseca AL; Batista R; Comar Junior M; Oliveira AB; Taranto AG; Varotti Fde P
[Ad] Endereço:Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João del-Rei, Divinópolis, MG, Brasil.
[Ti] Título:Structure-based drug design studies of the interactions of ent-kaurane diterpenes derived from Wedelia paludosa with the Plasmodium falciparum sarco/endoplasmic reticulum Ca²âº-ATPase PfATP6.
[So] Source:Mem Inst Oswaldo Cruz;110(2):255-8, 2015 Apr.
[Is] ISSN:1678-8060
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Malaria is responsible for more deaths around the world than any other parasitic disease. Due to the emergence of strains that are resistant to the current chemotherapeutic antimalarial arsenal, the search for new antimalarial drugs remains urgent though hampered by a lack of knowledge regarding the molecular mechanisms of artemisinin resistance. Semisynthetic compounds derived from diterpenes from the medicinal plant Wedelia paludosa were tested in silico against the Plasmodium falciparum Ca2+-ATPase, PfATP6. This protein was constructed by comparative modelling using the three-dimensional structure of a homologous protein, 1IWO, as a scaffold. Compound 21 showed the best docking scores, indicating a better interaction with PfATP6 than that of thapsigargin, the natural inhibitor. Inhibition of PfATP6 by diterpene compounds could promote a change in calcium homeostasis, leading to parasite death. These data suggest PfATP6 as a potential target for the antimalarial ent-kaurane diterpenes.
[Mh] Termos MeSH primário: ATPases Transportadoras de Cálcio/metabolismo
Diterpenos Caurânicos/uso terapêutico
Desenho de Drogas
Plasmodium falciparum/enzimologia
ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/metabolismo
Wedelia/química
[Mh] Termos MeSH secundário: Antimaláricos/metabolismo
Artemisininas/metabolismo
Cálcio/metabolismo
Diterpenos Caurânicos/síntese química
Diterpenos Caurânicos/farmacologia
Interações Medicamentosas
Inibidores Enzimáticos/farmacologia
Simulação de Acoplamento Molecular
Estrutura Molecular
Plasmodium falciparum/efeitos dos fármacos
Tapsigargina/farmacologia
Wedelia/classificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antimalarials); 0 (Artemisinins); 0 (Diterpenes, Kaurane); 0 (Enzyme Inhibitors); 67526-95-8 (Thapsigargin); 9RMU91N5K2 (artemisinine); EC 3.6.3.8 (ATP6 protein, Plasmodium falciparum); EC 3.6.3.8 (Calcium-Transporting ATPases); EC 3.6.3.8 (Sarcoplasmic Reticulum Calcium-Transporting ATPases); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150507
[St] Status:MEDLINE


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[PMID]:25837279
[Au] Autor:Tsai CH; Tzeng SF; Hsieh SC; Lin CY; Tsai CJ; Chen YR; Yang YC; Chou YW; Lee MT; Hsiao PW
[Ad] Endereço:Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan; Institute of Biochemical Sciences, College of Life Science, National Taiwan University, Taipei, Taiwan. Electronic address: tch@gate.sinica.edu.tw.
[Ti] Título:Development of a standardized and effect-optimized herbal extract of Wedelia chinensis for prostate cancer.
[So] Source:Phytomedicine;22(3):406-14, 2015 Mar 15.
[Is] ISSN:1618-095X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Herbal medicine is a popular complementary or alternative treatment for prostate cancer. Wedelia chinensis has at least three active compounds, wedelolactone, luteolin, and apigenin synergistically inhibiting prostate cancer cell growth in vitro. Here, we report a systematic study to develop a standardized and effect-optimized herbal extract, designated as W. chinensis extract (WCE) to facilitate its future scientific validation and clinical use. Ethanolic extract of dried W. chinensis plant was further condensed, acid hydrolyzed, and enriched with preparative chromatography. The chemical compositions of multiple batches of the standardized preparation WCE were quantified by LC/MS/MS, and biological activities were analyzed by in vitro and in vivo assays. Furthermore, the pharmacokinetics of the holistic WCE were compared with the combination of the equivalent principal active compounds through oral administration. The results indicated that quantitative chemical assay and PSA (prostate-specific antigen)-reporter assay together are suitable to measure the quality and efficacy of a standardized Wedelia extract on a xenograft tumor model. The presence of minor concomitant compounds in WCE prolonged the systemic exposure to the active compounds, thus augmented the anti-tumor efficacy of WCE. In conclusion, a combination of LC/MS/MS and PSA reporter assay is suitable to qualify a standardized preparation of WCE. Furthermore, the pharmacokinetics and oral bioavailability of active compounds demonstrate that holistic WCE exerted additional pharmacological synergy beyond the multi-targeted therapeutic effects caused by more than one active compound. WCE merits a higher priority to be studied for use in prostate cancer treatment.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/normas
Fitoterapia/normas
Extratos Vegetais/normas
Neoplasias da Próstata/tratamento farmacológico
Wedelia/química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos Fitogênicos/farmacocinética
Linhagem Celular Tumoral
Cromatografia Líquida
Seres Humanos
Masculino
Camundongos Endogâmicos BALB C
Camundongos Nus
Extratos Vegetais/farmacocinética
Controle de Qualidade
Espectrometria de Massas em Tandem
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Plant Extracts)
[Em] Mês de entrada:1509
[Cu] Atualização por classe:150403
[Lr] Data última revisão:
150403
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150404
[St] Status:MEDLINE



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