中文名 | NSC403140 |
英文名 | NSC403140 |
别名 | 化合物 T11534 |
英文别名 | NSC403140 Natalensine Hemanthamine Haemanthamine 3-Epicrinamine |
CAS | 466-75-1 |
化学式 | C17H19NO4 |
分子量 | 301.33706 |
体外研究 | 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. |
体内研究 | 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. |