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| Expanding the Therapeutic Spectrum of Artemisinin:Activity Against Infectious Diseases Beyond Malaria andNovel Pharmaceutical Developments |
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| DOI：10.15806/j.issn.2311-8571.2016.0002 |
| KeyWord:Artemisinin derivatives, Artemisia annua, Asteraceae, Antimalarial drugs, Anti-pathogen activity, Antiviral properties,
Artemisinin-loaded nanocarriers, Traditional Chinese Medicine |
| Author | Institution |
| Thomas Effertha* |
a.Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany |
| Marta R. Romerob |
b.Experimental Hepatology and Drug Targeting HEVEFARM, CIBERehd, IBSAL, University of Salamanca, Campus Miguel de Unamuno, 37007,Salamanca, Spain. |
| Anna Rita Biliac |
c.Department of Chemistry “Ugo Schiff”, University of Florence, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy |
| Ahmed Galal Osmand |
d.National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA |
| Mahmoud ElSohlya |
a.Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany |
| Michael Winkf |
f.Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls University, Im Neuenheimer Feld 364, 69120 Heidelberg, Germany |
| Rudolf Bauerg |
g.Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Universitätsplatz 4, 8010 Graz, Austria |
| Ikhlas Khandh |
d.National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA;h.Devision of Pharmacognosy, Department of Biomolecular Sciences, University of Mississippi, University, MS 38677, USA |
| Maria Camilla Bergonzic |
c.Department of Chemistry “Ugo Schiff”, University of Florence, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy |
| Jose J.G. Marinb |
b.Experimental Hepatology and Drug Targeting HEVEFARM, CIBERehd, IBSAL, University of Salamanca, Campus Miguel de Unamuno, 37007,Salamanca, Spain |
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| Abstract: |
| The interest of Western medicine in Traditional Chinese Medicine (TCM) as a source of drug leads/new drugs to treat diseases without available
efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCMover thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin (qinghaosu), which is extracted from the medicinal plant Artemisia annua L. (qinghao). The unexpected success of
artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou
Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the
oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives (artemisinins) exert profound
activities towards other protozoans (Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes (Schistosoma, liver
flukes), and viruses (human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising
results of artemisinin and the first generation derivatives (artesunate, artemether, arteether), novel drug development strategies have been pursued.
These included the synthesis of acetal- and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, e.g.
artemisinin-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The
current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types
of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in their drug delivery systems utilizing
pharmaceutical technology. It would be expected that different therapeutic strategies based on the second and third generation artemisinin
derivatives and artemisinin-based drug technologies would be available in the near future to treat specific infectious diseases. |
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