RESUMO
Polyynes, such as facarindiol (FAD) and oplopandiol (OPD), are responsible for anticancer activities of Oplopanax elatus (O. elatus). A novel approach to pharmacokinetics determination of the two natural polyynes in rats was developed and validated using a liquid chromatography-electrospray ionization-mass spectrometry (LC-MS) method. Biosamples were prepared by liquid-liquid extraction using ethyl acetate/n-hexane (V : V = 9 : 1) and the analytes were eluted on an Agilent ZORBAX Eclipse Plus C18 threaded column (4.6 mm × 50 mm, 1.8 μm) with the mobile phase of acetonitrile-0.1% aqueous formic acid at a flow-rate of 0.5 mL·min(-1) within a total run time of 11 min. All analytes were simultaneously monitored in a single-quadrupole mass spectrometer in the selected ion monitoring (SIM) mode using electrospray source in positive mode. The method was demonstrated to be rapid, sensitive, and reliable, and it was successfully applied to the pharmacokinetic studies of the two polyynes in rat plasma after oral administration of polyynes extract of O. elatus.
Assuntos
Animais , Masculino , Ratos , Administração Oral , Cromatografia Líquida de Alta Pressão , Métodos , Di-Inos , Farmacocinética , Medicamentos de Ervas Chinesas , Farmacocinética , Álcoois Graxos , Farmacocinética , Naftóis , Farmacocinética , Oplopanax , Química , Poli-Inos , Farmacocinética , Ratos Sprague-Dawley , Espectrometria de Massas por Ionização por Electrospray , MétodosRESUMO
Rheumatoid arthritis (RA) is the most common inflammatory arthritis and a major cause of disability. Presently, the clinical therapeutic medicines for inflammatory and arthritic diseases are unsatisfactory due to severe adverse effects or ineffectiveness. The Guge Fengtong formula (GGFT), containing the standardized extracts of Dioscoreae Nipponicae Rhizoma, Spatholobi Caulis, and Zingiberis Rhizoma, has long been used for RA treatment by Chinese doctorsin China. However, the detailed anti-inflammatory and anti-arthritic activity of GGFT has not been reported so far. In the present work, we aimed to evaluate the anti-inflammatory and anti-arthritic effects of GGFT using three in vivo animal models, and tried to uncover its preliminarythe underlying mechanism of action mechanism in RAW 264.7 macrophages. The obtained results indicated that GGFT significantly attenuated ear edema, decreased carrageenan-induced paw edema, reduced the arthritis score, and reversed the weight loss of the complete Freund's adjuvant (CFA)CFA-injected rats. Additionally, marked decrease of in synovial inflammatory infiltration and synovial lining hyperplasia in the joints and decline of inflammatory factors (TNF-α and IL-1β) in the serum were observed in the GGFT-treated rats. In lipopolysaccharide-activated RAW264.7 macrophages, GGFT reduced the production of NO, PGE2, and IL-6, and inhibited the expression of iNOS, COX-2, and NF-κB expression. Our results demonstrated that GGFT possessed considerable anti-inflammatory activity and have had potential therapeutic effects on adjuvant induced arthritis in rats, which provided providing experimental evidences for its traditional application in the treatment of RA and other inflammatory diseases.
Assuntos
Animais , Masculino , Camundongos , Anti-Inflamatórios , Farmacologia , Usos Terapêuticos , Antirreumáticos , Farmacologia , Usos Terapêuticos , Artrite , Artrite Reumatoide , Tratamento Farmacológico , Metabolismo , Patologia , Carragenina , Citocinas , Sangue , Dioscorea , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas , Farmacologia , Usos Terapêuticos , Fabaceae , Adjuvante de Freund , Inflamação , Tratamento Farmacológico , Metabolismo , Mediadores da Inflamação , Metabolismo , Macrófagos , Camundongos Endogâmicos ICR , Fitoterapia , Ratos Sprague-Dawley , ZingiberaceaeRESUMO
AIM@#To reveal the profile of astragalosides for better quality evaluation of Radix Astragali, this study was aimed to investigate the transformation of astragalosides under different conditions.@*METHOD@#Seven major astragalosides were selected for evaluation under acidic, neutral and alkaline conditions. The transformation in real plant samples was also examined and the products were characterized by LC-ESI-TOF/MS.@*RESULTS@#In weak acidic solution, all of the astragalosides are stable. In addition, the transformation ratios of the astragalosides under neutral and alkaline conditions were also obtained.@*CONCLUSION@#In neutral solution, malonylastragaloside I was transformed to astragaloside I; and in alkaline solution, substituent group(s) in the xylose moiety of all the astragalosides were eliminated. Since astragalosdie IV is the basic skeleton structure of the astrgalosides, it is a common transformation product of other astragalosides.