Molecular Formula | C17H20O5 |
Molar Mass | 304.3377 |
Storage Condition | 2-8℃ |
Use | The aurantia extract can be used as an active small molecule. |
biological activity | Bigelovin is a sesquiterpene lactone that can be isolated from sea lily, it is a selective agonist of retinoid X receptor alpha. Bigelovin can exert anti-tumor activity by inducing apoptosis and autophagy. Bigelovin regulates the mTOR signaling pathway by inhibiting the production of ROS. |
Cell Line: | HepG2 and SMMC-7721 cells. HepG2 and SMMC-7721 cells. |
Concentration: | 0-20 μM. 0-10 μM. |
Incubation Time: | 24, 48, 72 h. 24 h. |
Result: | Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time
dependent manner. No significant difference observed in cell viability of normal liver cell lines, LO2 and
LX2, after BigV treatment for 24, 48 or 72 h. The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment. The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight. No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration. Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII levels. The inactivation of mTOR was also observed in tumor tissues isolated from BigV-treated mice. |
Animal Model: | HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g). |
Dosage: | 5, 10, 20 mg/kg. |
Administration: | Intravenous injection every 2 days. |