Euphzycopins A − D, macrocyclic diterpenoids with potential anti-inflammatory activity from Euphorbia Helioscopia.

Four new diterpenoids (1–4) and four known diterpenoids (5–8) were purified from the whole plant of Euphorbia helioscopia L. Compounds 1 and 2 were jathophanes diterpenoids with a 5/12 polycyclic systems, compound 3 was rhamofolane diterpenoid with a 5/10 bicyclic skeleton and compound 4 was a rare class of euphorbia diterpenes featuring an unusual 5/10 fused ring system. Anti-inflammatory activity tests were conducted on the separated compounds, indicating that compound 4 had significant inhibitory effect on NLRP3 inflammasome with an IC 50 value of 7.75 μM. Further, the inhibitory effect of 4 was determined using immunofluorescence assays. [Display omitted] • Four new diterpenoids (1–4) and four known diterpenoids (5 - 8) were purified from the whole plant of Euphorbia helioscopia L. • Compound 3 was rhamofolane diterpenoid with a 5/10 bicyclic skeleton and 4 was a rare class of euphorbia diterpenes featuring an unusual 5/10 fused ring system • Compound 4 showed strong activity with IC 50 values of 7.75 μM. Frther, the inhibitory effects of 4 on protein levels were determined using immunofluorescence assays. [ABSTRACT FROM AUTHOR]