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가수분해형 탄닌 1-desgalloylrugosin-F 에 의한 100kDa 세포질 포스포리파아제 A2 활성억제효과
진미령(Mi Reyoung Chin),신혜숙(Hye Sook Shin),정광묵(Kwang Mook Jung),강미선(Mi Sun Kang),이민원(Min Won Lee),김대경(Dae Kyong Kim) 대한약학회 2000 약학회지 Vol.44 No.1
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.