Plant Molecular Biology 33: 199–209, 1997.
1997 Kluwer Academic Publishers. Printed in Belgium.
State of the art of the production of the antimalarial compound artemisinin
Els Van Geldre, Annemieke Vergauwe and Elfride Van den Eeckhout
Laboratorium voor Farmaceutische Biotechnologie, Universiteit Gent, Harelbekestraat 72, 9000 Gent, Belgium
author for correspondence)
Received 13 September 1996; accepted 16 September 1996
Key words: antimalarial drugs, Artemisia annua L., artemisinin
For more than three centuries we have relied on the extracts of the bark of Cinchona species to treat malaria. Now, it
seems we may be changing to the leaves of a Chinese weed, Artemisia annua, and its active compound artemisinin.
Artemisinin-derived drugs have been proved particularly effective treatments for severe malaria, even for multi-
drug-resistant malaria. However, this promising antimalarial compound remains expensive and is hardly available
on a global scale. Therefore, many research groups have directed their investigations toward the enhancement of
artemisinin production in A. annua cell cultures or whole plants in order to overproduce artemisinin or one of its
precursors. This article provides a brief review of the state of art of the different aspects in A. annua research.
‘If we take as our standard of importance the greatest harm
to the greatest number, then there is no question that
malaria is the most important of all infectious dis-
Sir Macfarlane Burnet, Natural History of Infectious Dis-
Malaria, one of the most devastating diseases in the
tropical world, is on the increase with no clear solution
nearby . During the past 40 years, malaria control
strategies have relied on insecticides against the vec-
tor and antimalarial drugs as prophylaxis or treatment.
The emergence of resistance by both vectors and para-
sites has emphasizedthe need for improved methodsof
malaria treatment and biological control of the anoph-
eline vector . Due to the multiple ways in which
Plasmodium replicates, much of the work in vaccine
development to date has remained in a preclinical sta-
dium. Therefore, there is an urgent need for new efﬁ-
cient antimalarial drugs for malaria prophylaxis. The
ﬁrst effective antimalarial drug was quinine, which
was isolated from the barks of several South Americ-
an species of Cinchona. For a long time this was the
ideal drug for prophylaxis since it is not toxic, works
fast and efﬁciently and has also a long half-life time.
However, Plasmodium parasites have built resistance
against this drug. The interest in plants as potential
sources of new antimalarial drugs has been stimulated
by the isolation and clinical use of the endoperoxide
sesquiterpene artemisinin, the active principle of the
Chinese medicinal herb Artemisia annua .
Artemisia annua (Compositae) is an aromatic annu-
al herb that occurs naturally as part of a steppe veget-
ation in the northern parts of Chahar and Suiyuan
E) in China, at 1000 to
1500 m above sea level . However, the plant now
grows wild in many other countries such as the former