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Antimicrobial Agents and Chemotherapy, July 2002, p. 2061-2068, Vol. 46, No. 7
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.7.2061-2068.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

In Vitro Increase in Chloroquine Accumulation Induced by Dihydroethano- and Ethenoanthracene Derivatives in Plasmodium falciparum-Parasitized Erythrocytes

Unité de Parasitologie, Institut de Médecine Tropicale du Service de Santé des Armées,¹ GERCTOP-UMR 6009, Faculté de Pharmacie,³ Institut Fédératif de la Recherche 48, Marseille, France²

Received 17 October 2001/ Returned for modification 3 December 2001/ Accepted 27 March 2002

The effects of a series of dihydroethano- and ethenoanthracene derivatives on chloroquine (CQ) accumulation in CQ-susceptible strain 3D7 and CQ-resistant clone W2 were assessed. The levels of CQ accumulation increased little or none in CQ-susceptible strain 3D7 and generally increased markedly in CQ-resistant strain W2. At 10 µM, 28 compounds yielded cellular accumulation ratios (CARs) greater than that observed with CQ alone in W2. At 10 µM, in strain W2, 21 of 31 compounds had CQ CARs two or more times higher than that of CQ alone, 15 of 31 compounds had CQ CARs three or more times higher than that of CQ alone, 13 of 31 compounds had CQ CARs four or more times higher than that of CQ alone, and 9 of 31 compounds had CQ CARs five or more times higher than that of CQ alone. At 1 µM, 17 of 31 compounds had CQ CARs two or more times higher than that of CQ alone, 12 of 31 compounds had CQ CARs three or more times higher than that of CQ alone, 6 of 31 compounds had CQ CARs four or more times higher than that of CQ alone, and 3 of 31 compounds had CQ CARs five or more times higher than that of CQ alone. At 1 µM, 17 of 31 compounds were more potent inducers of CQ accumulation than verapamil and 12 of 31 compounds were more potent inducers of CQ accumulation than promethazine. The nature of the basic group seems to be associated with increases in the levels of CQ accumulation. At 1 and 10 µM, 10 of 14 and 13 of 14 compounds with amino group (amines and diamines), respectively, had CARs 3, while at 1 and 10 µM, only 1 of the 13 derivatives with amido groups had CARs 3. Among 12 of the 31 compounds which were more active inducers of CQ accumulation than promethazine at 1 µM, 10 had amino groups and 1 had an amido group.

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