锦菊素
中文名称 | 锦菊素 |
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中文同义词 | 锦菊素;贝莱洛比 |
英文名称 | bigelovin |
英文同义词 | bigelovin;inhibit,Autophagy,Inhibitor,Retinoic acid receptors,Bigelovin,Retinoid X receptors,Apoptosis,Reactive Oxygen Species,RAR/RXR;Azuleno[6,5-b]furan-2,5-dione, 4-(acetyloxy)-3,3a,4,4a,7a,8,9,9a-octahydro-4a,8-dimethyl-3-methylene-, (3aR,4S,4aR,7aR,8R,9aS)- |
CAS号 | 3668-14-2 |
分子式 | C17H20O5 |
分子量 | 304.34 |
EINECS号 | |
相关类别 | 标准品-对照品;新品;标准品,对照品 |
Mol文件 | 3668-14-2.mol |
结构式 |
锦菊素 性质
熔点 | 180-182 °C(Solv: acetone (67-64-1); dichloromethane (75-09-2)) |
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沸点 | 466.6±45.0 °C(Predicted) |
密度 | 1.22±0.1 g/cm3(Predicted) |
储存条件 | 4°C, protect from light |
形态 | 固体 |
颜色 | 白色至米白色 |
Bigelovin (0-20 μM, 24-72 h) significantly inhibits cell viability of liver cancer cells and induces apoptosis and autophagy.
Bigelovin causes a significant increase of p62, LC3B-II, Beclin-1 and a corresponding decrease of p62 levels in a time-dependent manner.
Bigelovin induces cell death involves the suppression of mTOR pathway regulated by ROS production.
Cell Viability Assay
Cell Line: | HepG2 and SMMC-7721 cells. |
Concentration: | 0-20 μM. |
Incubation Time: | 24, 48, 72 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. |
Western Blot Analysis
Cell Line: | HepG2 and SMMC-7721 cells. |
Concentration: | 0-10 μM. |
Incubation Time: | 24 h. |
Result: |
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.
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Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model.
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. |
Result: |
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. |