Artemisinin is a drug used to treat multi-drug resistant strains of falciparum malaria. The compound (a sesquiterpene lactone) is isolated from the shrub Artemisia annua long used in traditional Chinese medicine.
ANALOGUES
INDICATIONS
- Antimalarial
- Antiparasitic: ex. antischistosomal
- Antiviral: ex. HPV
- Antineoplastic
- as antiangiogenetic
- as productor of ROS
- as proapoptotic by p53 -dependent and -independent pathways
- Antiinflammatory: The inducible nitric oxide synthase (iNOS) gene in macrophages catalyzes the generation of NO, which is involved in inflammation and immune response.
- Immunosuppressive
MOLECULAR MECHANISM
The specific mechanism of action of artemisinin is not well understood, and there is ongoing research directed at elucidating it. When the parasite that causes malaria infects a red blood cell, it consumes hemoglobin and liberates free heme, an iron-porphyrin complex. The iron reduces the peroxide bond in artemisinin generating high-valent iron-oxo species, resulting in a cascade of reactions that produce reactive oxygen radicals which damage the parasite leading to its death.
Artemisinin as anticancer drug?
TOXICITY
- Neurotoxicity 1 + 2 = Unanswered
occurs particularly following repeated high-dose intramuscular
injections of the oil-based dihydroartemisinin derivatives artemether and artemotil (arteether).
