Artemisinin, and its semi-synthetic derivatives are a group of drugs used against Plasmodium falciparum malaria.[1]
It is isolated from the plant Artemisia annua, sweet wormwood, a herb employed in Chinese traditional medicine. Artemisinin was discovered by a Chinese scientist, Tu Youyou, who was awarded half of the 2015 Nobel Prize in Medicine for her discovery.[2]
Treatments containing an artemisinin derivative (artemisinin-combination therapies, ACTs) are now standard treatment worldwide for P. falciparum malaria.[3]
Its dimers or trimers which have been invented the scientist of Friedrich-Alexander-Universität Erlangen-Nürnberg have increased in vitro activity against Plasmodiumfalciparum 3D7 strain, leukemia cells (CCRF-CEM and multidrug-resistant subline CEM/ADR5000) and human cytomegalovirus (HCMV). [4]
Trimer TF 27 displays superior potency against both leukemia cell lines (IC50 up to 0.002 μM for CCRF-CEM and IC50 up to 0.20 μM for CEM/ADR5000) and is even more active than clinically used doxorubicin (IC50 1.61 μM for CEM/ADR5000).
With respect to anti-HCMV activity, this trimer is the most efficient hybrid (IC50 0.04 μM) outperforming ganciclovir (IC50 2.6 μM), dihydroartemisinin (IC50 >10 μM) and artesunic acid (IC50 3.8 μM).
The following derivatives are available:
Artemisinin
Dihidro-Artemisinin
Acetoxy- Dihidro-Artemisinin (TF 1)
Artesunic acid
Trimer Artemisinin (TF 27)
[2] “The Nobel Prize in Physiology or Medicine 2015″ (PDF). Nobel Foundation.
[3] Guidelines for the Treatment of Malaria. Geneva: World Health Organization. 2006. ISBN 92-4-154694-8.