RESUMEN
Five novel iridoid glycosides, avellanedaesides A-E (1 - 5) were isolated from the H2 O extract of Tabebuia avellanedae. Their structures were determined on the basis of NMR and MS analysis. Isolated compounds suppressed inflammatory cytokine, tumor-necrosis factor-α and interleukin-1ß production in cultured human myeloma THP-1 cells co-stimulated with lipopolysaccharide (LPS). In addition, the study revealed iridoid glycosides inhibited the activity of cytochrome CYP3A4 enzyme.
Asunto(s)
Inhibidores del Citocromo P-450 CYP3A/farmacología , Citocromo P-450 CYP3A/metabolismo , Glicósidos Iridoides/farmacología , Tabebuia/química , Línea Celular Tumoral , Inhibidores del Citocromo P-450 CYP3A/química , Inhibidores del Citocromo P-450 CYP3A/aislamiento & purificación , Citocinas/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Humanos , Glicósidos Iridoides/química , Glicósidos Iridoides/aislamiento & purificación , Lipopolisacáridos/farmacología , Conformación Molecular , Relación Estructura-ActividadRESUMEN
To search for bioactive compounds from the flower disc of Helianthus annuus L., chromatography was used to isolate and purify the chemical constituents, their structures were identified by spectral analysis, MTT method was applied to investigate their cytotoxic activities, some compounds showed moderate cytotoxic activities on SF-268, MCF-7 and HepG2 cell lines. Eleven compounds were obtained from the flower disc of H. annuus, and identified as ent-kaurane-2alpha, 16alpha-diol (1) and entkaurane-15alpha,16alpha-epoxy-17-al-19-oic acid (2), and nine known diterpenes, ent-kaurane-16P-ol (3), phyllocladan-16beta-ol (4) , ent-atisan-16a-ol (5) , grandifloric acid (6) , angeloylgrandifloric acid (7), ent-kaurane-16-en-19-oic acid (8), ent-kaurane-17-hydroxy-15-en-19-oic acid (9), ent-kaurane-16beta, 17-dihydroxy-19-oic acid (10), and ciliaric acid (11). Compounds 1 and 2 are new compounds, some compounds showed cytotoxic activities on SF-268, MCF-7 and HepG2 cell lines.
Asunto(s)
Diterpenos de Tipo Kaurano/aislamiento & purificación , Diterpenos/farmacología , Helianthus/química , Plantas Medicinales/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cristalización , Diterpenos/química , Diterpenos/aislamiento & purificación , Diterpenos de Tipo Kaurano/química , Flores/química , Humanos , Concentración 50 Inhibidora , Conformación Molecular , Estructura Molecular , Temperatura de TransiciónRESUMEN
Three new lignan oligosaccharide esters, rupestrin A (1), rupestrin B (2), and rupestrin C (3), were isolated from the ethanol extract of Eritrichium rupestre. Their structures were elucidated on the basis of spectroscopic and chemical evidence.