The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance
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 Trypanos...
| Main Authors: | , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2019-04-01
|
| Series: | International Journal for Parasitology: Drugs and Drug Resistance |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211320718301830 |
| _version_ | 1818149787508146176 |
|---|---|
| author | Anthonius A. Eze John Igoli Alexander I. Gray Graham G. Skellern Harry P. De Koning |
| author_facet | Anthonius A. Eze John Igoli Alexander I. Gray Graham G. Skellern Harry P. De Koning |
| author_sort | Anthonius A. Eze |
| collection | DOAJ |
| description | 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. Keywords: Isometamidium, Trypanosoma congolense, Trypanosoma brucei brucei, Samorin, Drug resistance |
| first_indexed | 2024-12-11T13:12:35Z |
| format | Article |
| id | doaj.art-0d2e39fcb4c6402a91bba21a31244e4b |
| institution | Directory Open Access Journal |
| issn | 2211-3207 |
| language | English |
| last_indexed | 2024-12-11T13:12:35Z |
| publishDate | 2019-04-01 |
| publisher | Elsevier |
| record_format | Article |
| series | International Journal for Parasitology: Drugs and Drug Resistance |
| spelling | doaj.art-0d2e39fcb4c6402a91bba21a31244e4b2022-12-22T01:06:08ZengElsevierInternational Journal for Parasitology: Drugs and Drug Resistance2211-32072019-04-0195458The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistanceAnthonius A. Eze0John Igoli1Alexander I. Gray2Graham G. Skellern3Harry P. De Koning4Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom; Medical Biochemistry Department, Faculty of Basic Medical Sciences, College of Medicine, University of Nigeria, Enugu Campus, Enugu, NigeriaStrathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK; Department of Chemistry, College of Science, University of Agriculture, Makurdi, NigeriaStrathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UKStrathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UKInstitute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom; Corresponding author.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. Keywords: Isometamidium, Trypanosoma congolense, Trypanosoma brucei brucei, Samorin, Drug resistancehttp://www.sciencedirect.com/science/article/pii/S2211320718301830 |
| spellingShingle | Anthonius A. Eze John Igoli Alexander I. Gray Graham G. Skellern Harry P. De Koning 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 |
| title | The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance |
| title_full | The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance |
| title_fullStr | The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance |
| title_full_unstemmed | The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance |
| title_short | The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance |
| title_sort | individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture nor bypass isometamidium resistance |
| url | http://www.sciencedirect.com/science/article/pii/S2211320718301830 |
| work_keys_str_mv | AT anthoniusaeze theindividualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT johnigoli theindividualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT alexanderigray theindividualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT grahamgskellern theindividualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT harrypdekoning theindividualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT anthoniusaeze individualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT johnigoli individualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT alexanderigray individualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT grahamgskellern individualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance AT harrypdekoning individualcomponentsofcommercialisometamidiumdonotpossessstrongertrypanocidalactivitythanthemixturenorbypassisometamidiumresistance |