가수분해형 탄닌 1-desgalloylrugosin-F 에 의한 100kDa 세포질 포스포리파아제 A2 활성억제효과

Inhibition of 100kDa Cytosolic Phospholipase A2 by Hydrolysable Tannin, 1-desgalloylrugosin-F

To examine whether DGRF inhibits cPLA2 activity in vitro, we purified a 100kDa cPLA2 enzyme from porcine spleen and performed an inhibition study at two concentrations of 5.0 and 50.0mcM 1-stearoyl-2-[1-14C]arachidonoyl-sn-glycero-3-phosphocholine as a substrate to rule out an apparent inhibition due to "substrate depletion". Here we reported that DGRF inhibited cPLA2 activity with ID50 of 3.2mcM and virtually complete inactivation of the enzyme occurred at 60mcM. Interaction experiment between enzyme protein and inhibitor by ultrafiltration method indicated that 1-desgalloylrugosin-F inactivates cPLA2 enzyme by an irreversible mechanism.