In vitro reversal of chloroquine resistance in Plasmodium falciparum with dihydroethanoanthracene derivatives.

Bruno Pradines Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Sandrine Alibert-Franco Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Carole Houdoin Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Joel Mosnier Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Christiane Santelli-Rouvier Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Vincent Papa Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Christophe Rogier Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Thierry Fusai Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Jacques Barbe Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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Daniel Parzy Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées, Marseille, France.

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DOI:
https://doi.org/10.4269/ajtmh.2002.66.661
Volume/Issue:
Volume 66: Issue 6
Page(s):
661–666
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The effects of combining four dihydroethanoanthracenic (DEA) derivatives and chloroquine were assessed in vitro against Plasmodium falciparum chloroquine resistant parasites W2, Palo Alto, FCR3, and Bres1. Like verapamil or promethazine, the four dihydroethanoanthracenic derivatives tested can be added to the growing list of agents that show capability in enhancing the activity of chloroquine against resistant parasites. The structurally related tricyclic antihistaminic compounds examined in this study exerted different intrinsic antimalarial activity, but the same chloroquine-potentiating activity as verapamil or promethazine. They may act both on the rate of chloroquine accumulation and on its access to ferriprotoporphyrin IX. The reversal mechanism would be assumed to result from competition between DEA derivatives and chloroquine for efflux translocation sites, thus causing an increase in steady-state accumulation of chloroquine and a return to susceptibility. Restoration of therapeutic efficacy of chloroquine against resistant parasites by the administration of an additional drug available at relatively low cost may be a more effective strategy than the introduction of another antimalarial drug at the national level.

Author Notes

Published Online:
Jun 2002
Cover The American Journal of Tropical Medicine and Hygiene
The American Journal of Tropical Medicine and Hygiene
Print ISSN:
0002-9637
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