Oleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC50 value of 6.2 μM for porcine pancreatic PLA2.
(Z)-Oleyloxyethyl phosphorylcholine ((Z)-OPC) is an isomer of Oleyloxyethyl phosphorylcholine (OPC). Oleyloxyethyl phosphorylcholine is an inhibitor of secreted Phospholipase A2 (sPLA2), which is involved in the biosynthesis of proinflammatory lipid media. Oleyloxyethyl phosphorylcholine can be used to study inflammatory diseases. Oleyloxyethyl phosphorylcholine also modified the red blood membrane and was used to bind the oxygen-carrying liquid perfluorocarbons as an antivenom agent to reduce toxin-induced hemolysis[1][2].
to examine the phospholipids including oleyloxyethyl phosphorylcholine as pla2 inhibitors, the enzyme assay was employed. determinations were performed below critical micelle concentration. porcine pancreatic pla2 and phospholipid inhibitor were preincubated for 2 min at 37°c in buffer at ph 8.5. introduction of [l4c]arachidonate phosphatidylcholine initiated the enzymatic reaction, which is quenched after 5 min at 37°c. in this manner 50% inhibitor concentrations were determined for mepacrine and alkylphosphorylcholines, indicating oleyloxyethyl phosphorylcholine was an inhibitor of pla2 with an ic50 of 6.2 μm for porcine pancreatic pla2 [1].
6.2 μm for porcine pancreatic pla2
[1] magolda, r. l.,ripka, w.c.,galbraith, w., et al. novel synthesis of potent site-specific phospholipase a2 inhibitors. book: prostaglandins, leukotrienes and lipoxins 669-676 (1985).