Tehranolide, A sesquiterpene lactone with an endoperoxide group that probably has the same effect as the antimalarial agent Artemisinin

The malaria situation is aggravated by the appearance of strains of Plasmodium falciparum resistant to antimalarial drugs as well as by the resistance of vector Anopheles mosquitoes to DDT and other insecticides. Nearly 300–500 million people are infected by malaria and the incidence of this disease is dramatically increasing, since many strains of Plasmodium falciparum, the parasite responsible for the majority of fatal malaria infections, have become resistant to chloroquine and other traditional antimalarial drugs. Fortunately, these strains are still susceptible to the artemisinin derivatives. All of the artemisinin compounds contain stable endoperoxide bridges. The extract of the aerial parts of A. diffusa collected in the Province of Khorassan (Iran) afforded, in addition to several eudesmanolides, a new type of sesquiterpene lactone (Tehranolide) with an endoperoxide group. Previously, we reported antimalarial effect of extract of A. diffusa against P. berghei. Since the endoperoxide group is an essential requirement for the antimalarial activity of artemisinin, we have presumed the antimalarial properties of the crude extract are attributed to Tehranolide. We report here the in vivo laboratory evaluation of anti-malarial effects of Tehranolide, was done on P. berghei infected NMRI mice. The antimalarial effects of Tehranolide in 27mg/ml concentration (high dose) were injected s.c. every day for 12 days after infection in malaria mice. Three groups of mice (n=5) were investigated for antimalarial efficacy, the degree of parasitaemia, assessment of pathology including body weight, physiological activities, hepatomegaly and splenomegaly. Parasitaemia was measured every other day by counting Geimsa-stained blood smears which were taken from end tail cutting.

Tehranolide

References: Rustaiyan, A. et al. (2009) PHCOG MAG 4:1–7.