Bigelovin

Research use only, not for human use.

Bigelovin 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.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.

Bigelovin 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.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.

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.

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.

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Apoptosis

Apoptosis

Apoptosis|Reactive Oxygen Species|retinoid X receptor α

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3668-14-2

304.34

C17H20O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (328.58 mM)

C[C@H](C[C@@H]([C@H]([C@@H]([C@]12C)OC(C)=O)C3=C)OC3=O)[C@@H]2C=CC1=O

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(-20℃)

With Ice Pack

≥ 2 years