Page 219 - Phytochemistry 2 (06-PG 605)

4-Artemisinin
Artemisinin is isolated from Artemisia annua, Compositae
250 kg of leaves yields about 1 kg of pure artemisinin.

It contains endoperoxide bridge in a trioxolane structure
(ring containing three oxygen atoms).

Uses:
Artemisinin and its semi-synthetic derivatives are used against
Plasmodium falciparum malaria.
Its use as a mono therapy is discouraged by WHO, as the
parasites develope resistance to the drug.
Therapies that combine artemisinin or its derivatives
with some other antimalarial drug(chloroquine)are
the preferred treatment for malaria .

Mechanism of action:(antimalarial and cytotoxic).
The endoperoxide is responsible for the drug's mechanism
of action
*Reduction of the peroxide moiety, results in loss of activities

Artemisinin & its derivatives are pro drugs, iron activate them.Cells
need iron to replicate DNA when they divide.

Since cancer is characterized by out-of-control cell division,they
have much higher iron concentrations than do normal cells.