Inhibition of human sPLA2 and 5-lipoxygenase activities by two neo-clerodane diterpenoids

1999

Abstract The inhibitory effect of two neo -clerodane diterpenoids, E -isolinaridial (EI) and its methylketone derivative (EIM), isolated from Linaria saxatilis var. glutinosa , on PLA2 and other enzyme activities involved in the inflammatory process was studied. Both compounds inhibited human synovial sPLA 2 in a concentration-dependent manner with IC 50 values of 0.20 and 0.49 μM, respectively, similar to scalaradial. Besides, these compounds decreased the cell-free 5-lipoxygenase activity and A23187-induced neutrophil LTB 4 biosynthesis. Another function of human neutrophils, such as receptor-mediated degranulation, was also significantly reduced. In contrast, none of the compounds affect…