RESUMO
Gnaphalium affine D. Don, a medicinal and edible plant, has been used to treat gout in traditional Chinese medicine and popularly consumed in China for a long time. A detailed phytochemical investigation on the aerial part of G. affine led to the isolation of two new esters of caffeoylquinic acid named (-) ethyl 1, 4-di-O-caffeoylquinate (1) and (-) methyl 1, 4-di-O-caffeoylquinate (2), together with 35 known compounds (3-37). Their structures were elucidated by spectroscopic data and first-order multiplet analysis. All the isolated compounds were tested for their xanthine oxidase inhibitory activity with an in vitro enzyme inhibitory screening assay. Among the tested compounds, 1 (IC 11.94 μmol·L) and 2 (IC 15.04 μmol·L) showed a good inhibitory activity. The current results supported the medical use of the plant.
Assuntos
Adenina , Química , Medicamentos de Ervas Chinesas , Química , Farmacologia , Ativação Enzimática , Flavonoides , Química , Gnaphalium , Química , Supressores da Gota , Química , Farmacologia , Hidroxibenzoatos , Química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Compostos Fitoquímicos , Química , Farmacologia , Componentes Aéreos da Planta , Química , Extratos Vegetais , Química , Farmacologia , Ácido Quínico , Química , Xantina OxidaseRESUMO
Gnaphalium affine D. Don, a medicinal and edible plant, has been used to treat gout in traditional Chinese medicine and popularly consumed in China for a long time. A detailed phytochemical investigation on the aerial part of G. affine led to the isolation of two new esters of caffeoylquinic acid named (-) ethyl 1, 4-di-O-caffeoylquinate (1) and (-) methyl 1, 4-di-O-caffeoylquinate (2), together with 35 known compounds (3-37). Their structures were elucidated by spectroscopic data and first-order multiplet analysis. All the isolated compounds were tested for their xanthine oxidase inhibitory activity with an in vitro enzyme inhibitory screening assay. Among the tested compounds, 1 (IC 11.94 μmol·L) and 2 (IC 15.04 μmol·L) showed a good inhibitory activity. The current results supported the medical use of the plant.
Assuntos
Adenina , Química , Medicamentos de Ervas Chinesas , Química , Farmacologia , Ativação Enzimática , Flavonoides , Química , Gnaphalium , Química , Supressores da Gota , Química , Farmacologia , Hidroxibenzoatos , Química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Compostos Fitoquímicos , Química , Farmacologia , Componentes Aéreos da Planta , Química , Extratos Vegetais , Química , Farmacologia , Ácido Quínico , Química , Xantina OxidaseRESUMO
The aim of the study was to investigate the anti-proliferation and apoptosis-inducing effects of S1, a novel tetrandrine derivative, in human gastric cancer BGC-823 cells and explore the possible mechanism of action. The anti-proliferative activity was determined by MTT assay; the induction of cell cycle arrest and apoptosis were detected by flow cytometry. Quantitative real time RT-PCR and Western blotting were used to evaluate the mRNA and protein expression levels in mitochondrial pathway. S1 significantly reduced cell viability and induced a G2/M phase arrest and apoptosis in dose- and time-dependent manner. Further studies showed that S1 increased mRNA and protein expression of Bax and the Bax/Bcl-2 ratio. Moreover, S1 decreased the protein expression of procaspase-9 and procaspase-3, suggesting that the induction of apoptosis may be related to the alteration of the ratio of Bax/Bcl-2 and the activation of caspases. These findings suggested that S1 merits further investigation as a novel therapeutic agent for the treatment of human gastric cancer.
