Spectrofluorometric Determination of the Antibiotic Lasalocid in Blood

Brooks, Marvin A.; D'Arconte, L.; Silva, J.A.F. de; Chen, G.; Crowley, Christopher J.

doi:10.1002/jps.2600641128

Cited by 7 publications

(1 citation statement)

References 17 publications

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“…On the other hand, higher blood levels of lasalocid acid can be achieved by intravenous administration. For instance, intravenous injection of 5 mg of sodium lasalocid per kilogram body weight in a dog resulted in blood levels of the ionophore of > 7.3 μg/ml (> 12 μM) for the following 30 min (Brooks et al 1975 ), a concentration that killed trypanosomes in our in vitro assay (MIC = 10 μM, see above). In addition, at normal dosage, lasalocid acid is of low toxicity and usually causes no adverse side effects in cattle.…”

Section: Resultsmentioning

confidence: 85%

Trypanosoma brucei: trypanocidal and cell swelling activities of lasalocid acid

Steverding

Huczyński

2017

Parasitol Res

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Chemotherapeutic treatment of human and animal trypanosomiasis is unsatisfactory because only a few drugs are available. As these drugs have poor efficacy and cause adverse reactions, more effective and tolerable medications are needed. As the polyether ionophore antibiotic lasalocid acid is used as medicated feed additive in cattle, the compound was tested for its trypanocidal and cytotoxic activity against bloodstream forms of Trypanosoma brucei and human myeloid HL-60 cells. The concentrations required of lasalocid acid to reduce the growth rate of trypanosomes by 50% and to kill the parasites were 1.75 and 10 μM, respectively. The ionophore displayed also cytotoxic activity against HL-60 cells but the human cells were about 10 to 14 times less sensitive indicating moderate selectivity. As the trypanocidal mechanism of action of polyether ionophore antibiotics is due to a sodium influx-induced cell swelling, the effect of lasalocid acid on cell volume change in bloodstream-form trypanosomes was investigated. Interestingly, lasalocid acid induced a much faster cell swelling in trypanosomes than the more trypanocidal related ionophore salinomycin. These results support further investigations of lasalocid acid and derivatives thereof as potential agents against African trypanosomiasis.Electronic supplementary materialThe online version of this article (10.1007/s00436-017-5624-6) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 85%