Inhibition by Several Standard Antiprotozoal Drugs of Growth and O2 Uptake of Cells and Particulate Preparations of a Leptomonas*

Abstract

SYNOPSISDrug sensitivities of a lower trypanosomatid, Leptomonas sp. from the hemipteran Dysdercus, to antitrypanosomatid agents were estimated by growth inhibition and inhibition of polarographically measured O2 uptake of cells and particulate fractions. Several standard trypanocides, antimalarials, and electron‐transport inhibitors were used. Acriflavine, quinacrine, primaquine, pentamidine, and ethidium, each at ∼1 mM, inhibited cellular O2 uptake by 50% after 3‐hr incubation. Suramin and melarsen were inactive. Crude particulate fractions oxidized L‐α‐glycerophosphate at 80% the rate of succinate oxidation and L‐proline at 55% the succinate rate, leading to choice of succinate as standard respiratory substrate. Concentrations for 50% inhibition of growth were (μg/ml): ethidium bromide 0.009, acriflavine HCl 0.12, Antrycide 0.83, pentamidine diisethionate 1.5, and stilbamidine isethionate 1.1. Possible use of this trypanosomatid as model organism for screening antitrypanosomatid agents, and use of ethidium and acriflavine as initial model compounds are discussed.