PACOCF3 is a inhibitor of both Ca2+-dependent cytosolic cPLA2 and Ca2+-independent phospholipases A2 iPLA2 with IC50 values of 45 µM and 3.8 µM [1,2], which is an innovate and potential candidate drug for inflammation, atherosclerosis, diabetes mellitus, therapeutic shock, cancer therapyetc [3,4,5,6]. It has been reported that PACOCF3 can inhibit PLA2 and reduce the inflammatory response. PACOCF3 also can stimulate insulin release at basal glucose levels (2 mmol/l). Application of PACOCF3 can inhibit endogenous arachidonic acid generation which significantly decreased the amplitude of the insulin secretory response to 20 mmol/l glucose [7,8]. PACOCF3 have a dual protective role in diabetes which could minimize β-cell dysfunction while maintaining insulin secretory output through enhancing endogenous arachidonic acid levels.
References:
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