artemisinin

Chalcones (1, 3-diaryl-2-propen-1-ones) and their derivatives are widely explored from the past decade for its antimalarial activity. To elucidate their mechanism of action on the malaria parasite, the ultrastructural changes with the action of these derivatives in different organelles of the parasite were studied in vitro. Infected RBCs [CQ sensitive (MRC-2) and CQ resistant (RKL-9) Plasmodium strain] were treated with three chalcone derivatives 1, 2 and 3 and standard drugs, i.e., CQ and artemisinin at twice their respective IC50 values for 24 h and then harvested, washed, fixed, embedded and stained to visualize ultra-structure changes before and after intervention of treatment under in vitro condition through transmission electron microscope.

Artemisinins are sesquiterpene lactones with a peroxide moiety that are isolated from the herb Artemisia annua. It has been used for centuries for the treatment of fever and chills, and has been recently approved for the treatment of malaria due to its endoperoxidase properties. Progressively, research has found that artemisinins displayed multiple pharmacological actions against inflammation, viral infections, and cell and tumour proliferation, making them effective against diseases. Moreover, it has displayed a relatively safe toxicity profile.

Artemisinin-based drugs are the most effective medicine for the malaria treatment. To date, the main method of artemisinin production is its extraction from wormwood plants Artemisia annua L. Due to the limitation of this source, considerable efforts are now directed to the development of methods for artemisinin production using heterologous expression systems. Artemisinin is a sesquiterpene lactone, synthesized through the cyclization of farnesyl diphosphate involved in other sesquiterpene biosynthetic systems.

Artemisia annua L. and artemisinin, have been used for millennia to treat malaria. We used human liver microsomes (HLM) and rats to compare hepatic metabolism, tissue distribution, and inflammation attenuation by dried leaves of A. annua (DLA) and pure artemisinin. For HLM assays, extracts, teas, and phytochemicals from DLA were tested and IC50 values for CYP2B6 and CYP3A4 were measured.