NSC403140
NSC403140 用途与合成方法
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.
Cell Viability Assay
| Cell Line: | A2780 ovarian cancer cells |
| Concentration: | 1 µM, 10 µM, 50 µM, 100 µM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | Showed a time- and dose-dependent decrease in cell viability. |
Cell Proliferation Assay
| Cell Line: | A2780 ovarian cancer cells |
| Concentration: | 10 µM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Led to a significant inhibition of A2780 cell proliferation. |
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.
