Abstract
In an effort to evaluate novel derivatives from artemisinin, possessing potential antimalarial activity, a new derivative artecyclopentyl mether (CPM-1) was derivatized and evaluated for its dose-dependent efficacy in Plasmodium yoelii nigeriensis infected mice. The survivability of mice at 7.5 mg/kg was >28 days with negligible parasitaemia and recovered anemia (66.16-72.62%). Artecyclopentyl mether was also found to modulate the pro- and anti-inflammatory cytokines (IFN-γ, 39.64-56.92%; TNF, 49.10-74.31%; IL-4, 11.53-43.22%; IL-10, 37.60-53.52%) favourably besides optimizing the oxidative stress to the infected subjects as evident by the nitric oxide (88.76-95.43%), lipid peroxidation (59.30-76.05%) and glycaemic data (62.70-76.66%). The results indicate the potentiality of the new derivative as an antimalarial against asexual stages of the parasite.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials / administration & dosage*
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Antimalarials / chemical synthesis
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Antimalarials / therapeutic use
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Artemisinins / administration & dosage*
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Artemisinins / chemical synthesis
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Artemisinins / therapeutic use
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Cytokines / analysis
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Cytokines / immunology
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Drug Resistance, Multiple
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Enzyme-Linked Immunosorbent Assay
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Erythrocytes / drug effects
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Erythrocytes / parasitology
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Female
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Lipid Peroxidation / drug effects
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Malaria / drug therapy*
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Malaria / immunology
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Malaria / metabolism
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Malaria / mortality
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Malaria / pathology
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Mice
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Nitric Oxide / analysis
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Nitric Oxide / biosynthesis
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Oxidative Stress / drug effects
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Parasitemia / drug therapy*
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Plasmodium yoelii / drug effects*
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Plasmodium yoelii / physiology
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Rodent Diseases / drug therapy*
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Rodent Diseases / immunology
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Rodent Diseases / metabolism
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Rodent Diseases / mortality
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Rodent Diseases / pathology
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Survival Rate
Substances
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Antimalarials
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Artemisinins
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Cytokines
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Nitric Oxide