Febrifugine

Febrifugine is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids^[1][2][3]. In Vitro:Febrifugine (7-70 nM; 90 minutes) increases eIF2α phosphorylation in a dose-dependent manner in asynchronous P. falciparum Dd2 cultures^[1].
Febrifugine inhibits the asexual blood stage of the P. falciparum 3D7 parasite strain with an EC₅₀ of 4.0 nM^[1].
Febrifugine (0-0.225 μM; 48 h) effectively inhibits the proliferation growth of bladder cancer cells T24 and SW780 with IC₅₀ of 0.02 μM and 0.018 μM, respectively^[3].
Febrifugine (0.05-0.2 μM; 24 h) increases the number of cells in the G1 phase, and decreases the number in the G2 phase^[3].
Febrifugine (0.05-0.15 μM) inhibits cell proliferation by suppressing DNA synthesis and induces cell death by reducing steroidogenesis and promoting apoptosis^[3].
Febrifugine (0.025 μM) downregulates low density lipoprotein receptor-associated protein, lanosterol synthase, cholesterol biosynthesis second rate-limiting enzyme, 7-dehydrocholesterol reductase, flavin adenine dinucleotide dependent oxidoreductase and other factors to inhibit the production of intracellular steroids in bladder cancer T24 cells^[3].
In Vivo:Febrifugine (1 mg/kg/day; p.o.; once a day for 3 consecutive days before parasite infection) significantly reduces the mortality and the level of parasitemia^[2].
Febrifugine (0.1 mg/kg; once every 3 days; 10 doses) effectively inhibits bladder cancer xenograft proliferation in BALB/c nude mice^[3].