ALKYLPHOSPHATE ESTERS AS INHIBITORS OF PHOSPHOLIPASE-D

Alkylphosphate esters were shown to be potent inhibitors of phospholip ase D. Using phosphatidyl choline/sodium dodecylsulfate (2:1) as subst rate, IC50 values were determined for alkylphosphocholines of differen t chain length (C-10 - C-18) and for various octadecylphosphate esters with different polar head groups. The inhibitory potency strongly inc reased with increasing chain length of the alkyl chain. The substituti on of choline for heterocyclic nitrogen compounds or for 2-trimethylar sonio-ethanol also affected the inhibition of phospholipase D. Octadec ylphosphocholine proved to be the most efficient inhibitor (IC50 = 6.4 mu M).