febrifugine

Febrifugine is a **quinazolinone alkaloid** that is the active principal isolated from the Chinese herb *Dichroa febrifuga* (Chang Shan), used traditionally for the treatment of malaria and fever[10][1][4][7]. It is also detected in *Hydrangea* species[10][8]. Febrifugine and its analogues exhibit potent **antimalarial properties**, with in vitro inhibitory concentrations (IC50) in the sub-nanomolar range against *Plasmodium falciparum*, and show efficacy in animal models infected with malaria parasites[1][4][7][3]. The likely mechanism of action is **inhibition of prolyl-tRNA synthetase**, thus blocking protein synthesis in both malaria parasites and host cells[9]. However, febrifugine's therapeutic development has been limited due to its significant gastrointestinal toxicity, including emesis and intestinal injury, although analogues such as halofuginone have improved therapeutic indices and reduced host toxicity[1][4][7]. Febrifugine and derivatives have also been investigated for anticoccidial and other antiparasitic activities[12].

Other names

(+)-Febrifugineβ-dichroinebeta-febrifuginefebrifugin3-(3-(3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinone4(3H)-Quinazolinone, 3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-.BETA.-DICHROIN.BETA.-DICHROINE