Extracellular heme enhances the antimalarial activity of artemisinin
Artemisinin exerts the antimalarial activity through activation by heme. The hemolysis in malaria results in the elevated levels of plasma heme which may affect the activity of artemisinin. We hypothesized that the extracellular heme would potentiate the antimalarial activity of artemisinin. Hemin (...
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th-mahidol.151782018-06-11T12:24:26Z Extracellular heme enhances the antimalarial activity of artemisinin Sunanta Tangnitipong Thitiporn Thaptimthong Sirada Srihirun Supeenun Unchern Dusadee Kittikool Rachanee Udomsangpetch Nathawut Sibmooh Mahidol University Pharmacology, Toxicology and Pharmaceutics Artemisinin exerts the antimalarial activity through activation by heme. The hemolysis in malaria results in the elevated levels of plasma heme which may affect the activity of artemisinin. We hypothesized that the extracellular heme would potentiate the antimalarial activity of artemisinin. Hemin (ferric heme) at the pathologic concentrations enhanced the activity of artemisinin against Plasmodium falciparum in vitro and increased the levels of the lipid peroxidation products in the presence of artemisinin. The antimalarial activity of artemisinin and potentiation by hemin was decreased by vitamin E. Hemin had no effect on the activity of quinoline drugs (chloroquine, quinine and mefloquine). Furthermore, the oxidative effect of hemin in the presence of artemisinin or quinoline drugs was studied using low-density lipoprotein (LDL) oxidation as a model. Artemisinin enhanced the effects of hemin on lipid peroxidation and a decrease of tryptophan fluorescence in LDL whereas the quinoline drugs inhibited the oxidation by hemin. In conclusion, the extracellular hemin enhances the antimalarial activity of artemisinin as a result of the increasing oxidative effect of hemin. © 2012 The Pharmaceutical Society of Japan. 2018-06-11T05:24:26Z 2018-06-11T05:24:26Z 2012-01-16 Article Biological and Pharmaceutical Bulletin. Vol.35, No.1 (2012), 29-33 10.1248/bpb.35.29 13475215 09186158 2-s2.0-84855685579 https://repository.li.mahidol.ac.th/handle/123456789/15178 Mahidol University SCOPUS https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84855685579&origin=inward |
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Pharmacology, Toxicology and Pharmaceutics Sunanta Tangnitipong Thitiporn Thaptimthong Sirada Srihirun Supeenun Unchern Dusadee Kittikool Rachanee Udomsangpetch Nathawut Sibmooh Extracellular heme enhances the antimalarial activity of artemisinin |
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Artemisinin exerts the antimalarial activity through activation by heme. The hemolysis in malaria results in the elevated levels of plasma heme which may affect the activity of artemisinin. We hypothesized that the extracellular heme would potentiate the antimalarial activity of artemisinin. Hemin (ferric heme) at the pathologic concentrations enhanced the activity of artemisinin against Plasmodium falciparum in vitro and increased the levels of the lipid peroxidation products in the presence of artemisinin. The antimalarial activity of artemisinin and potentiation by hemin was decreased by vitamin E. Hemin had no effect on the activity of quinoline drugs (chloroquine, quinine and mefloquine). Furthermore, the oxidative effect of hemin in the presence of artemisinin or quinoline drugs was studied using low-density lipoprotein (LDL) oxidation as a model. Artemisinin enhanced the effects of hemin on lipid peroxidation and a decrease of tryptophan fluorescence in LDL whereas the quinoline drugs inhibited the oxidation by hemin. In conclusion, the extracellular hemin enhances the antimalarial activity of artemisinin as a result of the increasing oxidative effect of hemin. © 2012 The Pharmaceutical Society of Japan. |
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Mahidol University |
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Mahidol University Sunanta Tangnitipong Thitiporn Thaptimthong Sirada Srihirun Supeenun Unchern Dusadee Kittikool Rachanee Udomsangpetch Nathawut Sibmooh |
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Article |
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Sunanta Tangnitipong Thitiporn Thaptimthong Sirada Srihirun Supeenun Unchern Dusadee Kittikool Rachanee Udomsangpetch Nathawut Sibmooh |
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Sunanta Tangnitipong |
title |
Extracellular heme enhances the antimalarial activity of artemisinin |
title_short |
Extracellular heme enhances the antimalarial activity of artemisinin |
title_full |
Extracellular heme enhances the antimalarial activity of artemisinin |
title_fullStr |
Extracellular heme enhances the antimalarial activity of artemisinin |
title_full_unstemmed |
Extracellular heme enhances the antimalarial activity of artemisinin |
title_sort |
extracellular heme enhances the antimalarial activity of artemisinin |
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2018 |
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https://repository.li.mahidol.ac.th/handle/123456789/15178 |
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1763496437266513920 |