Abstract
Acetylcholine is proposed to be involved in nervous transmission in nematodes. Cholinesterase activity has been demonstrated in several species of filarial worms and has been localized in the nervous system. Here we report on the interaction of metrifonate and diethylcarbamazine with cholinesterase from O. volvulus, the patho-geneous agent of river blindness. The cholinesterase activity from adult filarial worms was characterized by its preference for acetylcholine compared to butyryl-choline and its sensitivity for eserine. The Michaelis constant for acetylcholine was found to be 0.11 mM. The inhibition constants for diethylcarbamazine, metrifonate and its metabolite dichlorvos were determined by be 0.3 mM, 6 μM and 0.4 μM, respectively. The microfilaricidal action of these cholinesterase-inhibitors might depend on a paralyzing effect on the neuromuscular system, by which the microfilariae hold themselves in their preferred position in the dermis. (Supported by UNDP/World Bank/WHO Special Programme, Filariasis component.)
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