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Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis , is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation. In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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\ndependent manner. No significant difference observed in cell viability of normal liver cell lines, LO2 and\nLX2, after BigV treatment for 24, 48 or 72 h. Western Blot AnalysisCell 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. In Vivo Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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\nlevels. The inactivation of mTOR was also observed in tumor tissues\nisolated from BigV-treated mice. Form:Solid
中文名称
Bigelovin
英文名称
Bigelovin
中文别名
比格洛文
英文别名
-
CAS号
3668-14-2
分子式
C17H20O5
分子量
304.34 g/mol
精确质量
≥99%
PSA
69.700 Ų
Logp
2.000
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Bigelovin 5mg

Ketones, Aldehydes, Acids

品牌:阿拉丁
货号:B648670-5mg
级别: ≥99%
货期:30天
已售 883 件
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5mg

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