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

Abstract

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 IC₅₀ value of 7.75 μM. Further, the inhibitory effect of 4 was determined using immunofluorescence assays.

Keywords: Diterpenoids; Euphorbia helioscopia L.; NLRP3 inflammasome.