3668-14-2
中文名称
锦菊素
英文名称
bigelovin
CAS
3668-14-2
分子式
C17H20O5
分子量
304.338
MOL 文件
3668-14-2.mol
更新日期
2024/08/23 10:50:04
3668-14-2 结构式
物理化学性质
熔点180-182 °C(Solv: acetone (67-64-1); dichloromethane (75-09-2))
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Solid
颜色White to off-white
常见问题列表
用途
锦菊素提取自旋复花，可用作活性小分子。生物活性
Bigelovin 是可从海百合中分离得到的一种倍半萜内酯，是选择性的视黄素 X 受体 α (retinoid X receptor α) 的激动剂。Bigelovin 可通过诱导凋亡和自噬来发挥抗肿瘤活性。Bigelovin 通过抑制 ROS 的生成来调节 mTOR 信号通路。体外研究
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.
|
体内研究
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. |