In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border
Abstract Background On the borders of Thailand, Plasmodium falciparum has become resistant to nearly all available drugs, and there is an urgent need to find new antimalarial drugs or drug combinations. Ferroquine (SSR97193) is a new 4-aminoquinoline antimalarial active against chloroquine resistant...
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ftdoajarticles:oai:doaj.org/article:a7cb268ae01d4b7f82303c942c1d7eee 2023-05-15T15:15:33+02:00 In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border Khaohirun Nopparat Jaidee Anchalee Barends Marion Singhasivanon Pratap Nosten François 2007-06-01T00:00:00Z https://doi.org/10.1186/1475-2875-6-81 https://doaj.org/article/a7cb268ae01d4b7f82303c942c1d7eee EN eng BMC http://www.malariajournal.com/content/6/1/81 https://doaj.org/toc/1475-2875 doi:10.1186/1475-2875-6-81 1475-2875 https://doaj.org/article/a7cb268ae01d4b7f82303c942c1d7eee Malaria Journal, Vol 6, Iss 1, p 81 (2007) Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 article 2007 ftdoajarticles https://doi.org/10.1186/1475-2875-6-81 2022-12-31T13:59:16Z Abstract Background On the borders of Thailand, Plasmodium falciparum has become resistant to nearly all available drugs, and there is an urgent need to find new antimalarial drugs or drug combinations. Ferroquine (SSR97193) is a new 4-aminoquinoline antimalarial active against chloroquine resistant and sensitive P. falciparum strains in vivo and in vitro . This antimalarial organic iron complex (a ferrocenyl group has been associated with chloroquine) is meant to use the affinity of Plasmodium for iron to increase the probability for encountering the anti-malarial molecule. The aim of the present study was to investigate the activity of ferroquine against P. falciparum isolates from an area with a known high multi-drug resistance rate. Methods Parasite isolates were obtained from patients with acute falciparum malaria attending the clinics of SMRU. In vitro cultures of these isolates were set-up in the SMRU-laboratory on pre-dosed drug plates, and grown in culture for 42 hours. Parasite growth was assessed by the double-site enzyme-linked pLDH immunodetection (DELI) assay. Results Sixty-five P. falciparum isolates were successfully grown in culture. The ferroquine mean IC 50 (95% CI) was 9.3 nM (95% C.I.: 8.7 – 10.0). The mean IC50 value for the principal metabolite of ferroquin, SR97213A, was 37.0 nM (95% C.I.: 34.3 – 39.9), which is four times less active than ferroquine. The isolates in this study were highly multi-drug resistant but ferroquine was more active than chloroquine, quinine, mefloquine and piperaquine. Only artesunate was more active than ferroquine. Weak but significant correlations were found between ferroquine and its principal metabolite (r 2 = 0.4288), chloroquine (r 2 = 0.1107) and lumefantrine (r 2 = 0.2364). Conclusion The results presented in this study demonstrate that the new ferroquine compound SSR97193 has high anti-malarial activity in vitro against multi-drug resistant P. falciparum . Article in Journal/Newspaper Arctic Directory of Open Access Journals: DOAJ Articles Arctic Malaria Journal 6 1 81 |
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Directory of Open Access Journals: DOAJ Articles |
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Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 |
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Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 Khaohirun Nopparat Jaidee Anchalee Barends Marion Singhasivanon Pratap Nosten François In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
topic_facet |
Arctic medicine. Tropical medicine RC955-962 Infectious and parasitic diseases RC109-216 |
description |
Abstract Background On the borders of Thailand, Plasmodium falciparum has become resistant to nearly all available drugs, and there is an urgent need to find new antimalarial drugs or drug combinations. Ferroquine (SSR97193) is a new 4-aminoquinoline antimalarial active against chloroquine resistant and sensitive P. falciparum strains in vivo and in vitro . This antimalarial organic iron complex (a ferrocenyl group has been associated with chloroquine) is meant to use the affinity of Plasmodium for iron to increase the probability for encountering the anti-malarial molecule. The aim of the present study was to investigate the activity of ferroquine against P. falciparum isolates from an area with a known high multi-drug resistance rate. Methods Parasite isolates were obtained from patients with acute falciparum malaria attending the clinics of SMRU. In vitro cultures of these isolates were set-up in the SMRU-laboratory on pre-dosed drug plates, and grown in culture for 42 hours. Parasite growth was assessed by the double-site enzyme-linked pLDH immunodetection (DELI) assay. Results Sixty-five P. falciparum isolates were successfully grown in culture. The ferroquine mean IC 50 (95% CI) was 9.3 nM (95% C.I.: 8.7 – 10.0). The mean IC50 value for the principal metabolite of ferroquin, SR97213A, was 37.0 nM (95% C.I.: 34.3 – 39.9), which is four times less active than ferroquine. The isolates in this study were highly multi-drug resistant but ferroquine was more active than chloroquine, quinine, mefloquine and piperaquine. Only artesunate was more active than ferroquine. Weak but significant correlations were found between ferroquine and its principal metabolite (r 2 = 0.4288), chloroquine (r 2 = 0.1107) and lumefantrine (r 2 = 0.2364). Conclusion The results presented in this study demonstrate that the new ferroquine compound SSR97193 has high anti-malarial activity in vitro against multi-drug resistant P. falciparum . |
format |
Article in Journal/Newspaper |
author |
Khaohirun Nopparat Jaidee Anchalee Barends Marion Singhasivanon Pratap Nosten François |
author_facet |
Khaohirun Nopparat Jaidee Anchalee Barends Marion Singhasivanon Pratap Nosten François |
author_sort |
Khaohirun Nopparat |
title |
In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
title_short |
In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
title_full |
In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
title_fullStr |
In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
title_full_unstemmed |
In vitro activity of ferroquine (SSR 97193) against Plasmodium falciparum isolates from the Thai-Burmese border |
title_sort |
in vitro activity of ferroquine (ssr 97193) against plasmodium falciparum isolates from the thai-burmese border |
publisher |
BMC |
publishDate |
2007 |
url |
https://doi.org/10.1186/1475-2875-6-81 https://doaj.org/article/a7cb268ae01d4b7f82303c942c1d7eee |
geographic |
Arctic |
geographic_facet |
Arctic |
genre |
Arctic |
genre_facet |
Arctic |
op_source |
Malaria Journal, Vol 6, Iss 1, p 81 (2007) |
op_relation |
http://www.malariajournal.com/content/6/1/81 https://doaj.org/toc/1475-2875 doi:10.1186/1475-2875-6-81 1475-2875 https://doaj.org/article/a7cb268ae01d4b7f82303c942c1d7eee |
op_doi |
https://doi.org/10.1186/1475-2875-6-81 |
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Malaria Journal |
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6 |
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81 |
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1766345924588601344 |