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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
agricultural and biological sciences
Effect of folate derivatives on the activity of antifolate drugs used against malaria and cancer
Parasitology Research, Volume 102, No. 6, Year 2008
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Description
The folate derivatives folic acid (FA) and folinic acid (FNA) decrease the in vivo and in vitro activities of antifolate drugs in Plasmodium falciparum. However, the effects of 5-methyl-tetrahydrofolate (5-Me-THF) and tetrahydrofolate (THF), the two dominant circulating folate forms in humans, have not been explored yet. We have investigated the effects of FA, FNA, 5-Me-THF, and THF on the in vitro activity of the antimalarial antifolates pyrimethamine and chlorcycloguanil and the anticancer antifolates methotrexate (MTX), aminopterin, and trimetrexate (TMX), against P. falciparum. The results indicate that these anticancers are potent against P. falciparum, with IC 50<50 nM. 5-Me-THF does not significantly decrease the activity of all tested drugs, and none of the tested folate derivatives significantly decrease the activity of these anticancers. Thus, malaria folate metabolism has features different from those in human, and the exploitation of this difference could lead to the discovery of new drugs to treat malaria. For instance, the combination of 5-Me-THF with a low dose of TMX could be used to treat malaria. In addition, the safety of a low dose of MTX in the treatment of arthritis indicates that this drug could be used alone to treat malaria. © 2008 The Author(s).
Authors & Co-Authors
Nduati, Eunice Wambui
Kenya, Nairobi
Kenya Medical Research Institute
Diriye, Abdi
Kenya, Nairobi
Kenya Medical Research Institute
Ommeh, Sheila Cecily
Kenya, Nairobi
Wellcome Trust Research Laboratories Nairobi
Mwai, Leah
Kenya, Nairobi
Kenya Medical Research Institute
Kiara, Steven M.
Kenya, Nairobi
Kenya Medical Research Institute
Masseno, Victor
Kenya, Nairobi
Kenya Medical Research Institute
K’okwaro, Gilbert O.
Kenya, Nairobi
Wellcome Trust Research Laboratories Nairobi
Nzila, Alexis M.
Kenya, Nairobi
Kenya Medical Research Institute
United Kingdom, Liverpool
Liverpool School of Tropical Medicine
United Kingdom, Liverpool
University of Liverpool
Statistics
Citations: 50
Authors: 8
Affiliations: 4
Identifiers
Doi:
10.1007/s00436-008-0897-4
ISSN:
09320113
Research Areas
Cancer
Infectious Diseases