RESUMO
Three new isobenzofurans (1-3), together with four known phenylpropanoids (4-7) were isolated from the roots of Nicotiana tabacum. Their structures were determined by means of HRESIMS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1-6 were tested for their anti-tobacco mosaic virus (anti-TMV) activities and cytotoxicity activities. The results showed that compounds 5 and 6 exhibited high anti-TMV activities with inhibition rates of 35.1 and 33.4%, respectively. The cytotoxicities of compounds 1-7 against five human tumor cell lines (NB4, A549, SHSY5Y, PC3 were also tested. Compounds 1-7 showed weak inhibitory activities against some tested human tumor cell lines with IC50 values in the range of 3.8-9.6 µM.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Antivirais/farmacologia , Benzofuranos/química , Nicotiana/química , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antineoplásicos Fitogênicos/química , Antivirais/química , Benzofuranos/farmacologia , Linhagem Celular Tumoral , Avaliação Pré-Clínica de Medicamentos/métodos , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Raízes de Plantas/químicaRESUMO
Three new benzolactones (1-3), together with four known ones (4-7), were isolated from the whole herb of Lavandula angustifolia. Their structures were established on the basis of detailed spectroscopic analysis (1D- and 2D-NMR, HRESIMS, UV, and IR) and comparison with data reported in the literature. New compounds were evaluated for their anti-tobacco mosaic virus (TMV) activities and cytotoxic activities. The results revealed that compounds 1-3 showed obvious anti-TMV activities with inhibition rates of 26.9, 30.2, and 28.4%, which were at the same grade as positive control. Compounds 1-3 also showed weak inhibitory activities against some tested human tumor cell lines with IC50 values in the range of 32.1-7.6 µM.
Assuntos
Antivirais/isolamento & purificação , Antivirais/farmacologia , Benzofuranos/isolamento & purificação , Benzofuranos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Furocumarinas/isolamento & purificação , Furocumarinas/farmacologia , Lactonas/isolamento & purificação , Lactonas/farmacologia , Lavandula/química , Antivirais/química , Benzofuranos/química , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Furocumarinas/química , Humanos , Concentração Inibidora 50 , Lactonas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Vírus do Mosaico do Tabaco/efeitos dos fármacosRESUMO
Four new flavones, tobaflavones E-H (1-4), together with two known flavones (5 and 6), were isolated from the leaves of Dali Tiandeng tobacco (a variety of Yunnan local air cured tobacco). Their structures were elucidated by spectroscopic methods, including extensive 1D- and 2D NMR techniques. Compound 2 is the first naturally occurring flavone bearing a (4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)methyl moiety. These compounds were also evaluated for their anti-tobacco mosaic virus (anti-TMV) activity. The results revealed that compounds 1 and 2 exhibited high anti-TMV activity with inhibition rate of 35.3% and 39.6%, respectively. The rates are higher than those of positive control. The other compounds also showed potential anti-TMV activity with inhibition rates in the range of 18.7-28.4%, respectively.
Assuntos
Antivirais/farmacologia , Flavonas/farmacologia , Nicotiana/química , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antivirais/isolamento & purificação , China , Flavonas/isolamento & purificação , Estrutura Molecular , Folhas de Planta/químicaRESUMO
A sensitive fluorescence turn-on biosensing platform for protein kinase activity assay has been developed based on fluorescence resonance energy transfer (FRET) between a fluorophore labeled peptide and a water soluble cationic conjugated polymer (CCP). The CCP-based assay is based on the electrostatic interaction between the peptide and the CCP. The FRET efficiency will change with the changing charges around the peptide after phosphorylation. The feasibility of this method has been demonstrated by sensitive measurement of the activity of cAMP-dependent protein kinase (PKA) with a low detection limit (0.3 mU µL(-1)). Based on its simple mechanism, this assay is also sensitive and robust enough to be applied to the evaluation of PKA inhibitor H-89. The IC50 value, the half maximal inhibitory concentration, was 40 nM. Furthermore, our method has excellent selectivity. CCP-based assay is sensitive, versatile, cost-effective and easy to operate, so, this method is a promising candidate for kinase activity assay and inhibitor screening.