Abstract

The role of the natural product, artemisinin, is discussed, with a view to elucidating its importance as an antimalarial, essential to sustainable global development, especially in the health and welfare industry. An estimated 243 million cases of malaria led to an estimated 863,000 deaths in 2008. The Roll Back Malaria (RBM) Partnership is a global network for co-ordinated action against malaria, launched in 1998 by the World Health Organization (WHO), United Nations International Children Emergency Fund (UNICEF), United Nations Development Programme (UNDP), and World Bank. It promotes consensus among key actors in malaria control, harmonizes action, and mobilizes resources to fight malaria in endemic countries. Large scale use of antimalarial monotherapies such as quinoline compounds (for example, chloroquine) and antifolate drugs (for example, sulfonamides), have culminated in cross-resistance, especially of Plasmodium falciparum, to these conventional antimalarial drugs. Artemisinin, (a sesquiterpene lactone), isolated from the plant Artemisia annua, is a drug used to treat multi-drug resistant strains of falciparum malaria. Saccharomyces cerevisiae microbes can produce the precursor artemisinic acid, by a technique of synthetic biology. The total synthesis of artemisinin can also be performed using the organic reagents, isopulegol. The iron-porphyrin complex-moiety, produced during plasmodium infection of the red blood cells, reacts with artemisinin, a potent inhibitor of hemozoin formation, to produce reactive oxygen radicals which damage the parasite leading to its death. Artemisinin acts on the electron transport chain, by causing the depolarization of the parasite’s mitochondrial membrane, and kills the asexual forms of plasmodium at the erythrocytic stage. Artemisinin selectively inhibits the production of estrogen receptor-alpha gene and thus, arrests the growth of estrogen responsive breast cancer cells. Artemesinin is not used for malaria prophylaxis because of it’s extremely short activity. Artemisinin is fast-acting and poorly bioavailable. The use of semi-synthetic derivatives and analogues of artemisinin, such as artesunate, and artemether, in the production of Artemisinin-based combination therapies (ACTs), for example, lumefantrine-artesunate, increase the therapeutic efficiency of artemisinin to more than 90%, and prevents recrudescence.

Key words: Artemisinin, monotherapies, plasmodium, artemisinin-based combination therapies.