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1.
Policy Polit Nurs Pract ; 25(1): 6-13, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38116640

RESUMO

Due to a growing physician shortage, patients have difficulty accessing primary care. In an effort to expand access and support patient health, many states are reducing barriers for advanced practice registered nurses to provide primary care without physician collaboration. Maryland provides an interesting case study. We leverage Maryland's policy change to explore the effects of full practice authority (FPA), focusing on the number of professionals and health outcomes for patients. Employing a border county comparison between Maryland and Pennsylvania, we estimate the effect of FPA. Our analysis of health outcomes focuses on three county-level health outcomes: poor or fair health, poor mental health days, and preventable hospital stays. We find that FPA is associated with increases in the number of certified nurse midwives by 0.6 per 100,000 residents and nurse practitioners by 22.4 per 100,000 residents. We also find evidence of an association of FPA with reductions in the share of residents who report being in poor or fair health by 2.8 percentage points and poor mental health days per month by 0.354 days per person. Combined, our results provide suggestive evidence that moving to FPA improves access to care and leads to improved health outcomes for Maryland residents. Removing regulatory barriers that prevent certified nurse midwives and nurse practitioners from working to the full extent of their training may increase access to primary care and improve patient outcomes.


Assuntos
Profissionais de Enfermagem , Médicos , Humanos , Estados Unidos
2.
Health Syst (Basingstoke) ; 8(1): 1-16, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31214351

RESUMO

The need for Long-Term Care (LTC) arises in the elderly population, especially those reaching age 65 each year. This elderly population will grow tremendously in the United States over the next decade, resulting in short- and long-term challenges of matching resource capacity with uncertain demand for hospitals and other healthcare providers. This paper describes research involving the development of a simulation model of patient flow in order to understand the relationship between capacity and demand, and to investigate the impacts on performance measures such as average wait times for LTC patients. We propose an aggregate capacity model to consider patient flow among various types of care providers by integrating hospitals, nursing homes, assisted living facilities, and home health care. Using the data including patient demographics and service provider information, we forecast patient demand for LTC. The computational results demonstrate the efficacy of a simulation-based optimisation solution approach for capacity planning.

3.
Consult Pharm ; 32(9): 535-546, 2017 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-28855012

RESUMO

OBJECTIVE: To survey the status of current tamoxifen pharmacovigilance documentation reflecting tamoxifen use in an academic outpatient multispecialty practice in older adults. This data will help provide information to develop improved pharmacovigilance for a growing cohort of older adult users. The data will be utilized by an interdisciplinary team developing new methods of identifying factors for individualized pharmacovigilance in older adults. DESIGN: Retrospective chart review to gather descriptive and quantitative data on tamoxifen pharmacovigilance. SETTING: Multi-specialty clinic. PATIENTS: Ninety-three patients 60 years of age and older. MAIN OUTCOME MEASURES: Quantitative report of tamoxifen monitoring as well as descriptive analysis of individual cases. RESULTS: We found 19 cases of serious adverse events possibly related to tamoxifen (thrombi, uterine malignancies). There were 15 cases with no documentation of pharmacovigilance. All cases had incomplete pharmacovigilance documented. There were two cases of hypercalcemia. There was one case of tamoxifen discontinuation resulting from muscle pain and with chronic muscle pain complaints while receiving tamoxifen. We observed a correlation in older age or high comorbidity burden patients and adverse events patients. CONCLUSION: Some studies direct the important pharmacovigilance toward prevention of thrombi, uterine malignancies, and hypercalcemia; however, it is not easy to identify recommendations for frequency or focus of monitoring to prevent adverse events for individual older adults based on existing recommendations. The data collected and presented in this study serve to heighten awareness of tamoxifen pharmacovigilance and as a starting point for the application of machine learning techniques and modeling to identify high-risk patients and individualized pharmacovigilance recommendations.


Assuntos
Farmacovigilância , Tamoxifeno/efeitos adversos , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Hipercalcemia/induzido quimicamente , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Trombose/induzido quimicamente , Neoplasias Uterinas/induzido quimicamente
4.
Phytother Res ; 28(2): 308-11, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23595773

RESUMO

Paeonia suffruticosa has been traditionally employed for vitalizing blood circulation and alleviating liver and inflammatory diseases. The pathways by which palbinone (PB) isolated from P. suffruticosa mediates heme oxygenase-1 (HO-1) induction were investigated using the specific inhibitors for PI3K and mitogen activated protein kinases pathways. The effect of PB-treatment on Nrf2 translocalization and HO-1-antioxidant response element (ARE) regulation was examined employing Western blot and luciferase assays. PB induced HO-1 expression via the activation of Nrf2 in the hepatic cells, and ARE-dependent genes were stimulated via the PB-mediated Nrf2 activation. PB-mediated HO-1 expression could be involved with PI3K/Akt and ERK1/2 pathways. Our study suggests the mechanism by which PB induces HO-1 expression in the hepatic cells. This might substantiate the traditional applications of P. suffruticosa for the treatment of oxidative stress-related diseases including oxidant and inflammatory-mediated vascular and liver diseases.


Assuntos
Heme Oxigenase-1/metabolismo , Hepatócitos/efeitos dos fármacos , Paeonia/química , Transdução de Sinais/efeitos dos fármacos , Terpenos/farmacologia , Elementos de Resposta Antioxidante , Linhagem Celular , Heme Oxigenase-1/genética , Hepatócitos/metabolismo , Humanos , Proteínas Quinases Ativadas por Mitógeno/antagonistas & inibidores , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo , Inibidores de Fosfoinositídeo-3 Quinase , Raízes de Plantas/química , Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores , Ativação Transcricional , Regulação para Cima
5.
J Cancer Prev ; 19(4): 273-8, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25574462

RESUMO

BACKGROUND: Physcion is an anthraquinone from rhubarb (rhizomes of Rheum tanguticum) and has been reported to have anti-inflammatory, hepatoprotective, antifungal, and anti-cancer activities. However, the growth inhibitory activity against human cancer cells and the underlying molecular mechanisms have been poorly determined. This study was designed to investigate the anti-proliferative activity of physcion by induction of cell cycle arrest and apoptosis in human MDA-MB-231 triple negative breast cancer cell line. METHODS: MDA-MB-231 cells were treated with physcion, and the anti-proliferative activity was evaluated by the sulforhodamine B assay. The mechanisms of action for the growth inhibitory activity of physcion were evaluated by flow cytometry for cell cycle distribution, and by Western blot for the assessment of potential target proteins. RESULTS: Physcion showed a significant anti-proliferative activity against MDA-MB-231 human breast cancer cells. Flow cytometric analysis indicated that physcion markedly induced the accumulation of cells in the G0/G1 phase and the increase of cell population in the sub-G1 phase. The G0/G1 cell cycle arrest by physcion was associated with the down-regulation of Cyclin D1, Cyclin A, CDK4, CDK2, c-Myc and phosphorylated Rb protein expressions. The increase of sub-G1 peak by physcion was closely correlated with the induction of apoptosis, which was confirmed by the induction of cleaved poly-(adenosine diphosphate ribose) polymerase, activation of Caspases, and suppression of Bid and Bcl-2 expression. CONCLUSIONS: The induction of G0/G1 cell cycle arrest and apoptosis might be one of the plausible mechanisms of actions for the anti-proliferative activity of physcion in human breast cancer cells.

6.
Int J Oncol ; 43(2): 600-10, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23708970

RESUMO

Magnolol, a neolignan from the traditional medicinal plant Magnolia obovata, has been shown to possess neuroprotective, anti-inflammatory, anticancer and anti-angiogenic activities. However, the precise mechanism of the anti-angiogenic activity of magnolol remains to be elucidated. In the present study, the anti-angiogenic effect of magnolol was evaluated in mouse embryonic stem (mES)/embryoid body (EB)-derived endothelial-like cells. The endothelial-like cells were obtained by differentiation from mES/EB cells. Magnolol (20 µM) significantly suppressed the transcriptional and translational expression of platelet endothelial cell adhesion molecule (PECAM), an endothelial biomarker, in mES/EB-derived endothelial-like cells. To further understand the molecular mechanism of the suppression of PECAM expression, signaling pathways were analyzed in the mES/EB-derived endothelial-like cells. Magnolol induced the generation of reactive oxygen species (ROS) by mitochondria, a process that was associated with the induction of apoptosis as determined by positive Annexin V staining and the activation of cleaved caspase-3. The involvement of ROS generation by magnolol was confirmed by treatment with an antioxidant, N-acetyl-cysteine (NAC). NAC inhibited the magnolol-mediated induction of ROS generation and suppression of PECAM expression. In addition, magnolol suppressed the activation of MAPKs (ERK, JNK and p38) and the PI3K/AKT/mTOR signaling pathway in mES/EB-derived endothelial-like cells. Taken together, these findings demonstrate for the first time that the anti-angiogenic activity of magnolol may be associated with ROS-mediated apoptosis and the suppression of the PI3K/AKT/mTOR signaling pathway in mES/EB-derived endothelial-like cells.


Assuntos
Inibidores da Angiogênese/farmacologia , Apoptose/efeitos dos fármacos , Compostos de Bifenilo/farmacologia , Lignanas/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Neovascularização Patológica/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Acetilcisteína/metabolismo , Animais , Caspase 3/biossíntese , Caspase 3/efeitos dos fármacos , Caspase 3/metabolismo , Diferenciação Celular , Linhagem Celular , Células-Tronco Embrionárias/citologia , Células-Tronco Embrionárias/efeitos dos fármacos , Células-Tronco Embrionárias/metabolismo , Células Endoteliais/efeitos dos fármacos , Células Endoteliais/metabolismo , Ativação Enzimática/efeitos dos fármacos , MAP Quinases Reguladas por Sinal Extracelular/efeitos dos fármacos , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Proteínas Quinases JNK Ativadas por Mitógeno/efeitos dos fármacos , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Óxido Nítrico Sintase/antagonistas & inibidores , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Molécula-1 de Adesão Celular Endotelial a Plaquetas/biossíntese , Molécula-1 de Adesão Celular Endotelial a Plaquetas/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Serina-Treonina Quinases TOR/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo , Proteínas Quinases p38 Ativadas por Mitógeno/efeitos dos fármacos , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
7.
Eur J Pharm Sci ; 48(1-2): 272-81, 2013 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-23174748

RESUMO

There is a growing interest in natural products that potentially have anti-inflammatory properties and inhibit P-glycoprotein (P-gp) function. In this report, we assessed the effects of anthraquinone derivatives from rhubarb on LPS-induced RAW 264.7 macrophages to determine their anti-inflammatory potential. The derivatives were also tested in Caco-2 cell lines to evaluate the inhibition of the drug efflux function of P-gp. The transport abilities were examined and the cellular accumulation of rhodamine-123 (R-123) was also measured. Electorphoretic mobility shift assay (EMSA) was performed to check the activator protein-1 (AP-1) DNA binding affinity. Five anthraquinones were tested to determine their inhibitory activities on NO production and the protein and mRNA expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Furthermore, the level of prostaglandin E(2) (PGE(2)) was determined in LPS-induced RAW264.7 macrophages. Emodin was found to be the most potent inhibitor, and it also reduced paw swelling in the mouse model of carrageenan-induced paw edema. In Caco-2 cells, emodin elevated the accumulation of R-123 and decreased the efflux ratio of R-123, which indicates the inhibition of P-gp function. The inhibition of COX-2 protein by emodin paralleled the decrease in P-gp expression. In addition, mitogen-activated protein kinase (MAPK) expression was decreased through the prevention of AP-1 DNA binding, which leads to downregulation in the expression of P-gp. Our data indicate that the decrease of P-gp expression is caused by the decreased expression of COX-2 through the MAPK/AP-1 pathway. Based on our results, we suggest that anti-inflammatory drugs with COX-2 inhibitory activity might be used to modulate P-gp function and expression.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Antraquinonas/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Inibidores de Ciclo-Oxigenase 2/uso terapêutico , Extratos Vegetais/uso terapêutico , Rheum , Animais , Antraquinonas/farmacologia , Anti-Inflamatórios/farmacologia , Células CACO-2 , Carragenina , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/genética , Inibidores de Ciclo-Oxigenase 2/farmacologia , Dinoprostona/metabolismo , Edema/induzido quimicamente , Edema/tratamento farmacológico , Edema/patologia , Humanos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Fitoterapia , Extratos Vegetais/farmacologia , RNA Mensageiro/metabolismo , Rizoma
9.
Cell Physiol Biochem ; 30(3): 758-70, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22890153

RESUMO

Embryonic stem cells, which are characterized by pluripotency and self-renewal, have recently been highlighted in drug discovery. In particular, the potential of ES cells to differentiate into specific-cell types make them an extremely useful tool in the evaluation of the biological activity of test compounds. Honokiol, a major neolignan derived from the bark of Magnolia obovata, has been shown an anti-tumor activity. However, the precise mechanism of action in the anti-tumor activity of honokiol is still poorly understood. Here, we evaluated the antiangiogenic activity of honokiol using mouse ES cell-derived embryoid bodies. mES-derived EBs were formed using hanging drop cultures and vascular formation was induced on gelatincoated plates in EGM-2 medium. The growth inhibition of honokiol was found to be more sensitive in the differentiated EB-derived endothelial cells compared to the undifferentiated EB-derived cells. Honokiol also inhibited the vascular formation of mES cells on 3-D collagen gel and decreased the expression of endothelial biomarkers VEGFR2 and PECAM in the differentiated EB-derived endothelial cells. In addition, honokiol suppressed the MAPK and mTOR signaling pathways in the EB-derived endothelial cells. Therefore, the anti-angiogenic activity of honokiol is associated in part with the suppression of PECAM and MAPK/mTOR pathways in EB-derived endothelial cells.


Assuntos
Inibidores da Angiogênese/farmacologia , Compostos de Bifenilo/farmacologia , Lignanas/farmacologia , Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo , Molécula-1 de Adesão Celular Endotelial a Plaquetas/metabolismo , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo , Inibidores da Angiogênese/química , Animais , Compostos de Bifenilo/química , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular , Corpos Embrioides/efeitos dos fármacos , Corpos Embrioides/fisiologia , Células-Tronco Embrionárias/citologia , Células-Tronco Embrionárias/metabolismo , Células Endoteliais/citologia , Células Endoteliais/metabolismo , Lignanas/química , Camundongos , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/metabolismo
10.
Food Chem Toxicol ; 50(10): 3625-34, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22842120

RESUMO

Acquired resistance to tamoxifen (TAM) is a serious therapeutic problem among estrogen-receptor-positive breast cancer patients. We have previously reported that TAM-resistant MCF-7 (TAMR-MCF-7) cells have elevated angiogenic potential via Pin1-dependent vascular endothelial growth factor (VEGF) production. Vitis amurensis grape consumed as wine and fruit contains several resveratrol-like stilbenes or oligostilbenes. In this study, we screened for the most active compound to inhibit VEGF production from V. amurensis. Among the tested compounds, amurensin G most potently suppressed VEGF production in TAMR-MCF-7 cells. The enhanced VEGF gene transcription in TAMR-MCF-7 cells was suppressed by amurensin G. Molecular analyses using reporter genes with hypoxia response elements and activator protein-1 (AP-1) elements, and western blots revealed that the activities and the nuclear levels of hypoxia inducible factor-1 (HIF-1)α and AP-1 in TAMR-MCF-7 cells were decreased by amurensin G. Moreover, amurensin G concentration-dependently inhibited protein expression and gene transcription of Pin1 in TAMR-MCF-7 cells, which was dependent on E2F1 inhibition. Chick chorioallantoic membrane assays confirmed that amurensin G had significant antiangiogenic and antitumor growth effects in TMAR-MCF-7 cells. These results demonstrate for the first time that amurensin G may have therapeutic potential for TAM-resistant breast cancer through blocking of Pin1-mediated VEGF gene transcription.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Dibenzocicloeptenos/farmacologia , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Peptidilprolil Isomerase/metabolismo , Resorcinóis/farmacologia , Tamoxifeno/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Dibenzocicloeptenos/química , Resistencia a Medicamentos Antineoplásicos , Fator de Transcrição E2F1/genética , Fator de Transcrição E2F1/metabolismo , Feminino , Humanos , Fator 1 Induzível por Hipóxia/genética , Fator 1 Induzível por Hipóxia/metabolismo , Proteínas Quinases JNK Ativadas por Mitógeno/genética , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Estrutura Molecular , Peptidilprolil Isomerase de Interação com NIMA , Neovascularização Patológica , Peptidilprolil Isomerase/genética , Resorcinóis/química , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo
11.
Bioorg Med Chem Lett ; 22(14): 4625-8, 2012 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-22677314

RESUMO

A methanol extract of the twigs of Cinnamomum cassia was found to inhibit xanthine oxidase. Purification of the methanol extract afforded three new phenolic glycosides, cinnacasolide A-C (11-13), together with 10 known compounds (1-10). The structures of the three new compounds were determined by interpretation of spectroscopic data. Cinnamaldehyde derivatives 1-5 and 7 were significant inhibitors of xanthine oxidase, with IC(50) values ranging from 7.8 to 36.3 µg/mL. The results indicate that the acyl group of these cinnamaldehyde derivatives plays an important role in the inhibition of xanthine oxidase.


Assuntos
Cinnamomum aromaticum/química , Inibidores Enzimáticos/química , Xantina Oxidase/antagonistas & inibidores , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Estrutura Molecular , Relação Estrutura-Atividade
12.
Phytomedicine ; 19(2): 150-9, 2012 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-21778042

RESUMO

Vitis amurensis (Vitaceae) has been reported to have anti-oxidant and anti-inflammatory activities. The present study investigated a methanol extract from the leaf and stem of V. amurensis for neuroprotective effects on cerebral ischemic damage in rats and on excitotoxicity induced by glutamate in cultured rat cortical neurons. Transient focal cerebral ischemia was induced by 2h middle cerebral artery occlusion followed by 24h reperfusion (MCAO/reperfusion) in rats. Orally administered V. amurensis (25-100 mg/kg) reduced MCAO/reperfusion-induced infarct and edema formation, neurological deficits, and neuronal death. Depletion of glutathione (GSH) level and lipid peroxidation induced by MCAO/reperfusion was inhibited by administration of V. amurensis. The increase of phosphorylated mitogen-activated protein kinases (MAPKs), cyclooxygenase-2 (COX-2), and pro-apoptotic proteins and the decrease of anti-apoptotic protein in MCAO/reperfusion rats were significantly inhibited by treatment with V. amurensis. Exposure of cultured cortical neurons to 500 µM glutamate for 12h induced neuronal cell death. V. amurensis (1-50 µg/ml) and (+)-ampelopsin A, γ-2-viniferin, and trans-ε-viniferin isolated from the leaf and stem of V. amurensis inhibited glutamate-induced neuronal death, the elevation of intracellular calcium ([Ca(2+)](i)), the generation of reactive oxygen species (ROS), and changes of apoptosis-related proteins in cultured cortical neurons, suggesting that the neuroprotective effect of V. amurensis may be partially attributed to these compounds. These results suggest that the neuroprotective effect of V. amurensis against focal cerebral ischemic injury might be due to its anti-apoptotic effect, resulting from anti-excitotoxic, anti-oxidative, and anti-inflammatory effects and that the leaf and stem of V. amurensis have possible therapeutic roles for preventing neurodegeneration in stroke.


Assuntos
Lesões Encefálicas/tratamento farmacológico , Isquemia Encefálica/tratamento farmacológico , Neurônios/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Vitis/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Apoptose , Edema Encefálico/tratamento farmacológico , Edema Encefálico/patologia , Isquemia Encefálica/patologia , Ciclo-Oxigenase 2/química , Feminino , Ácido Glutâmico/toxicidade , Glutationa/química , Peroxidação de Lipídeos , Masculino , Metanol/química , Estrutura Molecular , Fármacos Neuroprotetores/química , Síndromes Neurotóxicas/patologia , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Caules de Planta/química , Gravidez , Cultura Primária de Células , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/química , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/patologia
13.
J Asian Nat Prod Res ; 13(11): 1061-8, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21985227

RESUMO

A new flavan-3-ol, (+)-afzelechin 5-O-ß-d-glucopyranoside (2), together with 13 known flavonoids (1, 3-14), was isolated from the fruit peels of Wisteria floribunda. Their structures were assigned by detailed interpretation of NMR, MS, and CD spectroscopic data, as well as by comparing with published reports. The in vitro anti-inflammatory activity of the isolated compounds (1-14) was examined. Among them, compounds 3, 6, and 9 produced highest inhibitory effects on tumor necrosis factor alpha (TNF-α)-induced nuclear factor kappa-B activation in HepG2 cells with IC(50) values of 14.1, 16.5, and 11.9 µM, respectively. With the exception of compound 6, the compounds significantly inhibited the accumulation of pro-inflammatory inducible nitric oxide synthase and cyclooxygenase-2 proteins in TNF-α-stimulated HepG2 cells at a concentration as low as 0.1 µM.


Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Ciclo-Oxigenase 2/metabolismo , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Wisteria/química , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/imunologia , Sequência de Bases , Relação Dose-Resposta a Droga , Flavonoides/química , Flavonoides/imunologia , Frutas/química , Glucosídeos/química , Glucosídeos/imunologia , Células Hep G2 , Humanos , Concentração Inibidora 50 , Coreia (Geográfico) , NF-kappa B/imunologia , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/metabolismo , Ressonância Magnética Nuclear Biomolecular , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Fator de Necrose Tumoral alfa/antagonistas & inibidores
14.
Bioorg Med Chem Lett ; 21(21): 6603-7, 2011 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-21924611

RESUMO

Two new lanostane triterpenes, named methyl ganoderate A acetonide (1) and n-butyl ganoderate H (2), were isolated from the fruiting bodies of Ganoderma lucidum together with 16 known compounds (3-18). Extensive spectroscopic and chemical studies established the structures of these compounds as methyl 7ß,15α-isopropylidenedioxy-3,11,23-trioxo-5α-lanost-8-en-26-oate (1) and n-butyl 12ß-acetoxy-3ß-hydroxy-7,11,15,23-tetraoxo-5α-lanost-8-en-26-oate (2). Because new compounds exhibiting specific anti-acetylcholinesterase activity are being sought as possible drug candidates for the treatment of Alzheimer's and related neurodegenerative diseases, compounds 1-18 were examined for their inhibitory activities against acetylcholinesterase and butyrylcholinesterase. All of the compounds exhibited moderate acetylcholinesterase-inhibitory activity, with IC(50) values ranging from 9.40 to 31.03µM. In contrast, none of the compounds except lucidadiol (13) and lucidenic acid N (14) exhibited butyrylcholinesterase-inhibitory activity at concentrations up to 200µM. These results indicate that these lanostane triterpenes are preferential inhibitors of acetylcholinesterase and may be suitable drug candidates.


Assuntos
Inibidores da Colinesterase/farmacologia , Reishi/química , Triterpenos/farmacologia , Inibidores da Colinesterase/isolamento & purificação , Concentração Inibidora 50 , Espectrometria de Massas por Ionização por Electrospray , Triterpenos/isolamento & purificação
15.
Planta Med ; 77(18): 2037-41, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21796576

RESUMO

Four new biphenyl and biphenyl ether quinolizidine N-oxide alkaloids, 5- EPI-dihydrolyfoline N-oxide (1), decamine N-oxide (2), lagerstroemine N-oxide (3), and lagerine N-oxide (4), were isolated from the aerial parts of Lagerstroemia indica, and their structures were established by extensive spectroscopic studies. In addition, the inhibitory effects of isolated compounds on rat lens aldose reductase (RLAR) were examined.


Assuntos
Alcaloides/química , Compostos de Bifenilo/química , Óxidos N-Cíclicos/química , Lagerstroemia/química , Quinolizidinas/química , Aldeído Redutase/efeitos dos fármacos , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Compostos de Bifenilo/isolamento & purificação , Compostos de Bifenilo/farmacologia , Fracionamento Químico , Óxidos N-Cíclicos/isolamento & purificação , Óxidos N-Cíclicos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Éteres/química , Espectroscopia de Ressonância Magnética , Componentes Aéreos da Planta/química , Quinolizidinas/isolamento & purificação , Quinolizidinas/farmacologia , Ratos , Ratos Sprague-Dawley
16.
Bioorg Med Chem Lett ; 21(11): 3483-7, 2011 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-21530248

RESUMO

Rosmarinic acid, its analogues, and a phenolic compound were obtained from G. hederacea var. longituba. There were two new compounds, methyl isoferuloyl-7-(3,4-dihydroxyphenyl) lactate (1) and benzyl-4'-hydroxy-benzoyl-3'-O-ß-D-glucopyranoside (4), and four known compounds (2, 3, 5 and 6). The structures of these compounds were determined on the basis of spectroscopic methods. Each compound was tested by NF-κB luciferase assay and three rosmarinic acid analogues inhibited NF-κB production and the induction of COX-2 and iNOS mRNA in HepG2 cells.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Lamiaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Anti-Inflamatórios/isolamento & purificação , Células Hep G2 , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , NF-kappa B/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
17.
Phytother Res ; 25(5): 755-9, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21442678

RESUMO

The antiallergic activity of rhubarb and its constituents, anthraquinones, has been reported previously. For further evaluation of the antiallergic activity, a 70% ethanol extract of the rhizomes of Rheum tanguticum (RTE) was prepared and its inhibitory activity on an animal model of atopic dermatitis (AD) was examined for the first time. Oral administration of RTE (30-300 mg/kg/day) for 5 weeks significantly inhibited hapten-induced dermatitis in NC/Nga mice based on the skin severity score. In addition, treatment with RTE at 100 mg/kg/day also reduced the numbers of white blood cells, neutrophils and eosinophils in the blood, and led to a significant reduction in the IgE concentration in the serum. In rat basophilic leukemia (RBL)-1 cells, RTE inhibited 5-lipoxygenase (5-LOX)-catalysed leukotriene production (IC(50) = 43.6 µg/mL). Among the anthraquinone derivatives isolated, emodin strongly inhibited this parameter (IC(50) = 4.3 µM). Taken together, these findings suggest that rhubarb exerts inhibitory activity against AD, and that the 5-LOX inhibitory activity of its major constituent, emodin, may contribute to this inhibitory action.


Assuntos
Antialérgicos/farmacologia , Dermatite Atópica/tratamento farmacológico , Emodina/farmacologia , Inibidores de Lipoxigenase/farmacologia , Extratos Vegetais/farmacologia , Rheum/química , Administração Oral , Animais , Antraquinonas/química , Antraquinonas/farmacologia , Antraquinonas/uso terapêutico , Antialérgicos/uso terapêutico , Contagem de Células Sanguíneas , Células Sanguíneas/efeitos dos fármacos , Dermatite Atópica/induzido quimicamente , Emodina/isolamento & purificação , Emodina/uso terapêutico , Haptenos/efeitos adversos , Imunoglobulina E/sangue , Imunoglobulina E/efeitos dos fármacos , Inibidores de Lipoxigenase/isolamento & purificação , Inibidores de Lipoxigenase/uso terapêutico , Masculino , Camundongos , Modelos Animais , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos , Rizoma/química , Pele/efeitos dos fármacos , Pele/patologia
18.
Phytother Res ; 25(11): 1579-85, 2011 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21394807

RESUMO

Ganoderma lucidum is known as a medicinal mushroom used in traditional medicine. In our study, the cytotoxic activities of 17 compounds (1-17) isolated from the fruiting bodies of G. lucidum were investigated. Among them, ergosta-7,22-diene-2ß,3α,9α-triol (EGDT) induced apoptosis in HL-60 human premyelocytic leukemia cells. EGDT activated the apoptotic process, including DNA fragmentation and caspase-3 activity. In immunoblotting analysis, treatment with EGDT resulted in the cleavage of procaspase-3 and poly(ADP-ribose) polymerase (PARP) into active forms. In the in vivo study, the administration (i.p.) of EGDT to Lewis lung carcinoma (LLC)-inoculated mice evidenced a significant inhibition of tumor growth. These results indicate that EGDT was one of the apoptotic constituents of G. lucidum, and might be an antitumor agent.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Fitosteróis/farmacologia , Reishi/química , Animais , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Caspase 3/metabolismo , Fragmentação do DNA , Feminino , Células HL-60/efeitos dos fármacos , Humanos , Camundongos
19.
Planta Med ; 77(9): 955-7, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21243589

RESUMO

Three new sesquiterpene lactones, 1 α,10 ß-epoxy-4-hydroxy-glechoma-5-en-olide (1), 1 ß,10 α-epoxy-4,8-dihydroxy-glechoma-5-en-olide (2), and 1 ß,10 α;4 α,5 ß-diepoxy-8-methoxy-glechoman-8 α,12-olide (3), were isolated from the whole plant of Glechoma hederacea, together with four known sesquiterpene lactones. The structures of the three new sesquiterpene lactones were determined by spectroscopic evidence. Cytotoxic effects of the isolated compounds were examined against MDA-MB-231 (breast), HCT116 (colon), SW620 (colon), and DU145 (prostate) human cancer cell lines.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lactonas/farmacologia , Lamiaceae/química , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Lactonas/química , Lactonas/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação
20.
Planta Med ; 77(1): 66-9, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20645248

RESUMO

Two new lignans, (2 R,3 R)-2 ß-(4''-hydroxy-3''-methoxybenzyl)-3 α-(4'-hydroxy-3'-methoxybenzyl)-γ-butyrolactone 2-O-( ß-D-glucopyranoside) (1) and (1 S,2 R,3 S)-dimethyl-1,2,3,4-tetrahydro-3,6,7-trihydroxy-1-(3',4'-dihydroxyphenyl)naphthalene-2,3-dicarboxylate (2) together with nine known compounds (3-11) were isolated from the ethyl acetate fraction of the roots of Pulsatilla koreana. Their chemical structures were established based on physicochemical and spectroscopic data analyses. All isolates were investigated for their inhibition effects against the classical pathway of the complement system. Among them, compound 6 showed significant inhibitory activity with an IC (50) value of 75.9 µM, compounds 8 and 9 had moderate effects with IC (50) values of 182.2 and 166.5 µM, respectively.


Assuntos
Lignanas/farmacologia , Pulsatilla/química , Fracionamento Químico , Proteínas do Sistema Complemento/química , Lignanas/química , Lignanas/isolamento & purificação , Extratos Vegetais/química , Raízes de Plantas/química
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