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Inhibition by Several Standard Antiprotozoal Drugs of Growth and O 2 Uptake of Cells and Particulate Preparations of a Leptomonas *
Author(s) -
GOLDBERG BURT,
LAMBROS CHRIS,
BACCHI CYRUS J.,
HUTNER S. H.
Publication year - 1974
Publication title -
the journal of protozoology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.067
H-Index - 77
eISSN - 1550-7408
pISSN - 0022-3921
DOI - 10.1111/j.1550-7408.1974.tb03662.x
Subject(s) - acriflavine , ethidium bromide , phenanthridine , suramin , biochemistry , biology , growth inhibition , chemistry , in vitro , stereochemistry , dna
SYNOPSIS Drug sensitivities of a lower trypanosomatid, Leptomonas sp. from the hemipteran Dysdercus , to antitrypanosomatid agents were estimated by growth inhibition and inhibition of polarographically measured O 2 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 O 2 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.

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