YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Inhibition of 100 kDa Cytosolic Phospholipase $A_2$ by Hydrolysable Tannin, 1-desgalloylrugosin-F

가수분해형 탄닌 1-desgalloylrugosin-F에 의한 100 kDa 세포질 포스포리파아제 $A_2$ 활성의 억제효과

  • Published : 2000.02.01
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Abstract

To examine whether DGRF inhibits $cPLA_2$ activity in vitro, we purified a 100 kDa $cPLA_2$enzyme from porcine spleen and performed an inhibition study at two concentrations of 5.0 and 50.0 $\mu$M 1-stearoyl-2-[1-$^{l4C}$ ]arachidonoyl-sn -glycero-3-phosphocholine as a substrate to rule out an apparent inhibition due to "substrate depletion". Here we reported that DGRF inhibited $cPLA_2$activity with $ID_{50}$ of 3.2 $\mu$M and virtually complete inactivation of the enzyme occurred at 60 $\mu$M. Interaction experiment between enzyme protein and inhibitor by ultrafiltration method indicated that 1-desgalloylrugosin-F inactivates $cPLA_2$enzyme by an irreversible mechanism.

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References

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