RESUMO
Withaminimas A-F (1-6), six new withaphysalin-type withanolides were isolated from the aerial parts of Physalis minima L.. The structures of these compounds were elucidated through a variety of spectroscopic techniques including HR-MS, NMR, and ECD. Compound 1 belongs to rare 18-norwithanolides, and 2-3 were 13/14-secowithanolides. According to the traditional usage of P. minima, inhibitory effects on nitric oxide (NO) production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated, and compounds 1-4 exhibited significant inhibitory effects with IC values among 3.91-18.46 μmol·L.
Assuntos
Animais , Camundongos , Anti-Inflamatórios , Química , Farmacologia , Medicamentos de Ervas Chinesas , Química , Farmacologia , Lipopolissacarídeos , Farmacologia , Macrófagos , Alergia e Imunologia , Estrutura Molecular , Physalis , Química , Relação Estrutura-Atividade , Vitanolídeos , Química , FarmacologiaRESUMO
<p><b>OBJECTIVE</b>To evaluate the growth-inhibiting and pro-apoptotic effect of kaempferol in human esophageal squamous carcinoma Eca-109 cells and explore the mechanism.</p><p><b>METHODS</b>The effect of kaempferol on Eca-109 cell proliferation in vitro was measured by MTT assay. TUNEL staining was used to detect the cell apoptosis following kaempferol treatment. The changes in Bax and Bcl-2 mRNA expressions in response to kaempferol treatment were determined by RT-PCR, and the caspase-3 and caspase-9 activities were evaluated using colorimetric assay.</p><p><b>RESULTS</b>Kaempferol significantly inhibited Eca-109 cell proliferation (P<0.05) in a concentration-dependent manner and induced obvious cell apoptosis. RT-PCR showed that after kaempferol treatment caused up-regulated Bax and down-regulated Bcl-2 mRNA expression. The colorimetric assay revealed significantly increased caspase-3 and caspase-9 activities in Eca-109 cells following kaempferol treatment (P<0.01).</p><p><b>CONCLUSION</b>Kaempferol can induce apoptosis of Eca-109 cells via a mitochondria-dependent pathway.</p>