The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance

Eze, A. A., Igoli, J., Gray, A. I., Skellern, G. G. and De Koning, H. P. (2019) The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance. International Journal for Parasitology: Drugs and Drug Resistance, 9, pp. 54-58. (doi:10.1016/j.ijpddr.2019.01.003) (PMID:30685630) (PMCID:PMC6356087)

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Abstract

The four components present in the trypanocidal treatment Samorin, the commercially available formulation of isometamidium, were separated and purified by column chromatography. These compounds as well as the Samorin mixture and the other phenanthridine trypanocide, homidium, were tested on Trypanosoma congolense and wild type, diamidine- and isometamidium-resistant Trypanosoma brucei brucei strains using an Alamar blue drug sensitivity assay. EC50 values obtained suggest that M&B4180A (2) was the most active of the components, followed by M&B38897 (1) in all the strains tested, whereas M&B4596 (4) was inactive. Samorin was found to be significantly more active than any of the individual components alone, against T. congolense and all three T. b, brucei strains. Samorin and all its active constituents displayed reduced activity against the previously characterised isometamidium-resistant strain ISMR1.

Item Type:Articles
Additional Information:A.A.E. was supported by a Commonwealth Scholarship (grant reference NGCS-2009-246).
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:De Koning, Professor Harry
Authors: Eze, A. A., Igoli, J., Gray, A. I., Skellern, G. G., and De Koning, H. P.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:International Journal for Parasitology: Drugs and Drug Resistance
Publisher:Elsevier
ISSN:2211-3207
ISSN (Online):2211-3207
Published Online:21 January 2019
Copyright Holders:Copyright © 2019 Elsevier Ltd on behalf of Australian Society for Parasitology
First Published:First published in International Journal for Parasitology: Drugs and Drug Resistance 9:54-58
Publisher Policy:Reproduced under a Creative Commons License

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