American Journal of Tropical Medicine and Hygiene · 1999 · 37 citations · 33 references
MedicineInfectious DiseasesPharmacologyAntimicrobial PharmacologyBiochemical PharmacologyPharmacodynamicsAntiparasitic PharmacologyEnzyme InhibitionMalariaTropical MedicineAntimalarial AgentsAntimalarial ChemotherapyAntimalarial Drug DevelopmentChemotherapy Of MalariaIsotopic AnalysisPlasmodium FalciparumResistance In Clinical IsolatesTreatment Of Malaria
The in vitro activities of dihydroartemisinin (the biologically active metabolite of artemisinin derivatives), chloroquine, monodesethylamodiaquine (the biologically active metabolite of amodiaquine), quinine, mefloquine, halofantrine, and pyrimethamine were assessed in 65 African isolates of Plasmodium falciparum from Yaounde, Cameroon using an isotopic microtest. The 50% inhibitory concentration (IC50) values for dihydroartemisinin were within a narrow range from 0.25 to 4.56 nM, with a geometric mean of 1.11 nM (95% confidence interval = 0.96-1.28 nM). Dihydroartemisinin was equally active (P > 0.05) against the chloroquine-sensitive isolates (geometric mean IC50 = 1.25 nM, 95% confidence interval = 0.99-1.57 nM) and the chloroquine-resistant isolates (geometric mean IC50 = 0.979 nM, 95% confidence interval = 0.816-1.18 nM). A significant positive correlation was observed between the responses to dihydroartemisinin and mefloquine (r = 0.662) or halofantrine (r = 0.284), suggesting in vitro cross-resistance. There was no correlation between the responses to dihydroartemisinin and other antimalarial drugs.
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Wenmin Wu, Yikang Wu, Yu‐Lin Wu et al. · Journal of the American Chemical Society · 1998 · 175 citations
Pharmacy, Chemistry, Pharmacology +15
Michèle van Vugt, A Brockman, B Gemperli et al. · Antimicrobial Agents and Chemotherapy · 1998 · 170 citations · Full text
Veterinary Medicine, Infectious Diseases, Pharmacotherapy +12