Pharmacological Potentials of Artemisinin and Related Sesquiterpene Lactones: Recent Advances and Trends

  • María José Abad MartínezEmail author
  • Luis Miguel Bedoya del Olmo
  • Luis Apaza Ticona
  • Paulina Bermejo Benito


Natural products represent a goldmine of innovative therapeutic molecules to prevent and/or treat human diseases. For over 1,000 years, malaria has been one of the major causes of suffering and death for mankind. Artemisinin is an unusual sesquiterpene lactone (SL) endoperoxide that has been isolated as the active principle of the Chinese antimalarial herb Artemisia annua L. Since artemisinin was discovered to be the active component of A. annua in the early 1970s, hundred of papers have focused on the antiparasitic effects of artemisinin and its semi-synthetic analogues. Nowadays, artemisinin and its derivatives have become essential components of antimalarial treatment and are recommended by the World Health Organization (WHO) to treat especially multidrug-resistant forms of malaria. These features have prompted various scientists around the world to evaluate the potential of artemisinin and derivatives to control other human diseases. This review will centre on the significant achievements in recent years (2000 to date) with regard the chemistry and biological properties of SL from A. annua, with particular attention on artemisinin and related compounds. The discussion will also focus on the understanding of its mechanism of action and structure/activity relationships.


Visceral Leishmaniasis Bovine Viral Diarrhoea Virus Antimalarial Activity Sesquiterpene Lactone NLRP3 Inflammasome Activation 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



Antiretroviral therapy




Artemisinin-based combinatory therapies


Contact hypersensitivity


Cyclin-dependent kinase




Cytochrome P450




Delayed-type hypersensitivity


Deoxyribonucleic Acid




Epstein–Barr virus


Extracellular signal-regulated kinase


Herpes simplex virus type 1


Human immunodeficiency virus




Inducible nitric oxide synthase


Inhibitor of NF-kappaB


50 % Inhibitory concentration




Jun N-terminal kinase


Lethal concentration for 50 % mortality




Matrix metalloproteinase


Messenger ribonucleic acid


Mitogen-activated protein kinase


Nitric oxide


Non-nucleoside reverse transcriptase inhibitors


Nuclear factor-kappaB


Phorbol myristate acetate


Phosphorylated focal adhesion kinase


Prostaglandin E2


Protease inhibitors


Reactive oxygen species


Sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphate


Sesquiterpene lactone


Transforming growth factor-β1


2,4,6-trinitrobenzene sulphonic acid


Tumour necrosis factor-α


Vascular endothelial growth factor


von Willebrand factor


World Health Organization



The technical assistance of Ms. Brooke-Turner is gratefully acknowledged.


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Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  • María José Abad Martínez
    • 1
    Email author
  • Luis Miguel Bedoya del Olmo
    • 1
  • Luis Apaza Ticona
    • 1
  • Paulina Bermejo Benito
    • 1
  1. 1.Department of PharmacologyFaculty of Pharmacy, University ComplutenseMadridSpain

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