NSC403140

Haemanthamine (1-100 μM; 24-48 hours; A2780 cells) treatment shows a time- and dose-dependent decrease in cell viability.
Haemanthamine (10 μM; 24-72 hours; A2780 cells) treatment leads to a significant inhibition of A2780 cell proliferation.
Haemanthamine binds at the A-site cleft of the peptidyl transferase center on the large ribosomal subunit, creating unique molecular interactions with the 25S rRNA. Haemanthamine has a highly specific inhibitory effect on pre-rRNA processing, leading to the activation of a p53-dependent antitumoral surveillance pathway known as nucleolar stress.

A pharmacokinetic study of Haemanthamine in rats shows a rapid distribution phase of 30 min, a half-life of 70.4 min, and a major clearance through renal elimination. The high distribution volume of 13.7 L/kg suggests a high intracellular penetration, and its plasmatic concentration remains higher than 1 μM for at least 1 hr after a single 10-mg/kg administration.