Bigelovin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bigelovin 是一种选择性视黄醇 X 受体 α 激动剂。 Bigelovin 通过抑制 ROS 生成调节的 mTOR 通路，诱导细胞凋亡和自噬，从而抑制肿瘤生长。它也被称为来自旋覆花属的有效细胞毒性倍半萜内酯。

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.

——

Apoptosis

Apoptosis

Apoptosis|Reactive Oxygen Species|retinoid X receptor α

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years