RESUMEN
Six new sesquiterpenoids, named as ainslides A-F (1-6), including one carotene-type sesquiterpene (1), one eudesmane (2), four guaianolides (3-6), together with eight known sesquiterpenoids (7-14), were purified from the whole plants of Ainsliaea pertyoides. The structures of these sesquiterpenoids were characterized based on spectroscopic methods including 1D and 2D NMR, HR-ESI-MS, UV, and IR spectra, together with ECD calculations and X-ray diffraction experiments. The anti-inflammatory activity of all the isolated compounds was screened and compounds 3 and 7-13 exhibited NLRP3-inflammasome inhibitory activity with IC50 values of 1.80-4.33â µM.
Asunto(s)
Asteraceae , Sesquiterpenos , Asteraceae/química , Inflamasomas , Estructura Molecular , Proteína con Dominio Pirina 3 de la Familia NLR , Sesquiterpenos/química , Sesquiterpenos/farmacologíaRESUMEN
A phytochemical investigation was conducted on Euphorbia helioscopia, resulting in the isolation of thirteen compounds, including nine undescribed diterpenoids, Euphzycopias A - I (1-9), of which the skeletons of compounds 1-4 were found in E. helioscopia L. Compounds 1-3 had 5/7/6 cyclic systems, while compound 4 had a 4/11 polycyclic system with a 4,7-cyclic ether between C-4 and C-7. The anti-inflammasome test using the isolated compounds (1-6, 8-13) showed that the diterpenes from E. helioscopia L. had a strong inhibitory effect on NLRP3 inflammasomes with IC50 values of 3.34-14.92 µM.
Asunto(s)
Diterpenos/farmacología , Euphorbia/química , Inflamasomas/farmacología , Diterpenos/química , Diterpenos/aislamiento & purificación , Humanos , Inflamasomas/química , Inflamasomas/aislamiento & purificación , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética , Estructura Molecular , Proteína con Dominio Pirina 3 de la Familia NLR/antagonistas & inhibidores , Rotación Óptica , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Espectrofotometría InfrarrojaRESUMEN
Nine new diterpenoids, Rubellacrns A - I (1-9), including five isopimaranes (1-4, 9), four pimaranes (5-8), together with five known isopimarane analogues (10-14), were isolated from Callicarpa rubella. The structures of these compounds were unambiguously established by HR-ESIMS and NMR spectroscopic data, the absolute configurations of compounds 5 and 9 were determined by ECD. All the isolated compounds were tested for their anti-inflammatory effects and compounds 2 and 11-14 showed NLRP3-inflammasome inhibitory activity with IC50 values ranging from 7.02 to 14.38 µM.
