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KMID : 0043320120350050905
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Archives of Pharmacal Research
2012 Volume.35 No. 5 p.905 ~ p.910
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Competitive inhibition of cytosolic Ca2+-dependent phospholipase A2 by acteoside in RBL-2H3 cells
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Song Ho-Sun
Choi Mi-Young
Ko Myoung-Soo
Jeong Jae-Min
Kim Yong-Ho
Jang Beom-Hyeon
Sung Ji-Hoon
Kim Min-Gyu
Whang Wan Kyunn
Sim Sang-Soo
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Abstract
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The aim of this study was to investigate whether acteoside isolated from Clerodendron trichotomum Thunberg may act as a selective inhibitor of phospholipase A2 in RBL-2H3 cells. Acteoside dose-dependently inhibited 0.5 μM melittin-induced release of [3H]arachidonic acid, which was due to the inhibition of cytosolic Ca2+-dependent phospholipase A2 (cPLA2) rather than secretory PLA2 (sPLA2). In Dixon plots, the apparent Ki value of acteoside on cPLA2 was 5.9 μM and the inhibitory pattern appeared to be a competitive inhibitor. The above data, suggests that acteoside acts as a competitive inhibitor of cPLA2 in RBL-2H3 cells.
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KEYWORD
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Acteoside, Clerodendron trichotomum Thunberg, Phospholipase A2, Arachidonic acid, RBL-2H3
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