Alkylphosphate Esters as Inhibitors of Phospholipase D

Abstract

Alkylphosphate esters were shown to be potent inhibitors of phospholipase D. Using phosphatidyl choline/sodium dodecylsulfate (2:1) as substrate, IC₅₀ values were determined for alkylphosphocholines of different chain length (C₁₀ - C₁₈) and for various octadecylphosphate esters with different polar head groups. The inhibitory potency strongly increased with increasing chain length of the akyl chain. The substitution of cboline for heterocyclic nitrogen compounds or for 2-himethylarsonio-ethanol also affected the inhibition of phospholipase D. Cktadecylphosphocholine proved to be the most efficient inhibitor (IC₅₀ = 6.4 μM).

Key Words: :

• Phospholipase D
• Alkylphosphocholine
• octadecylphosphate esters
• inhibition
• substrate