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artemisinin,
isolated from Chinese-Vietnamese plant Artemisia
annua L., locally called "qing hao", is a new
class anti-malarial drugs. It is a white
crystalline powder with a bitter taste;
practically insoluble in water, soluble in
chloroform, acetone, and alcohols. Its chemical
designation is (3R,5aS,6R,8aS,9R,12S,12aR)-
octahydro-3,6,9-trimethyl-3,12-epoxy-
12H-pyrano[4.3-j]-1,2-benzodioxepin-10(3H)-one.
Malaria is one of leading re-emerging infectious
disease due to murative malarial parasite
developed resistance to chloroquine.
Sulfadoxine-pyrimethamine is an alternative can
be used in the treatment of the disease
resistant to chloroquine, but resistance to
sulfadoxine-pyrimethamine has been reported also
in some areas. Artemisinin is an alternative
used in areas where the disease has become
highly resistant to sulfadoxine-pyrimethamine.
Dihydroartemisinin, its methyl ether (artemether),
its ehyl ether (its (arteether) and its
hemisuccinate ester (artesunate) are known as
more effective than its parent material -
artemisinin. Artemisinin is a peroxide-bridged
sesquiterpene lactone compound which has no N
atom, unlike quinine class anti-malarial drugs.
The characteristic peroxide lactone structure is
indispensable for anti-malarial activity. The
term of artemotil refers to the pure beta-epimer
of arteether. |