Artemisinin and its derivatives

 

 Artemisinin is a new antimalarial drug of Chinese-Vietnamese origin, derived from the herb Artemisia annua L., locally known as "qing hao" ' sweet wormwood or annual wormwood, and belonging to the family of Asteraccae.

This plant has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria.

The earliest record of the medicinal use of "qing hao" was found in a recipe discovered in a tomb dating from 168 B.C. (Qinghaosu Antimalaria Coordinating Research Group, 1979; Klayman, 1985).

Stucture of Artemether

Artemisinin is a new antimalarial drug of Chinese-Vietnamese origin, derived from the herb Artemisia annua L., locally known as "qing hao" ' sweet wormwood or annual wormwood, and belonging to the family of Asteraccae.

This plant has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria.

The earliest record of the medicinal use of "qing hao" was found in a recipe discovered in a tomb dating from 168 B.C. (Qinghaosu Antimalaria Coordinating Research Group, 1979; Klayman, 1985).

Chinese chemists isolated the substance responsible for its medicinal action from the leafy portions of A. annua L. in 1972. They named the crystalline compound "qinghaosu". In the West it was called artemisinin (Klayman, 1985).

Artemisinin is poorly soluble in water. It is a sesquiterpene lactone that bears a peroxide group and unlike most other antimalarials, lacks a nitrogen-containing heterocyclic ring system.

The peroxide moiety of artemisinin appears to be indispensable for chemotherapeutic activity.

When artemisinin is treated with borohydride to give dihydroartemisinin, a lactol is formed in which the integrity of the peroxide group is retained and the schizonticidal activity is enhanced twofold.

Beta-Artemether is a novel antimalarial drug which is more active than the parent compound, artemisinin (WHO, 1986).

Beta-Artemether's is produced in Belgium under the trade name is ARTENAM.


See also WHO press release: Artesunate Rectocaps: a life-saving intervention