| Chemical Properties | Back Directory | [Melting point ]
180-182 °C(Solv: acetone (67-64-1); dichloromethane (75-09-2)) | [Boiling point ]
466.6±45.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Definition]
ChEBI: A sesquiterpene lactone that is 3,3a,4,4a,7a,8,9,9a-octahydroazuleno[6,5-b]furan-2,5-dione substituted by methyl groups at positions 4a and 8, a methylidene group at position 3 and an acetoxy group at position 4. Isolated from Inula hupe
ensis, it exhibits antineoplastic activity. | [in vivo]
Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model[1].
| Animal Model: | HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1]. | | 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.
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| [References]
[1] Bei Wang, et al. Bigelovin, a sesquiterpene lactone, suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation in liver cancer. Biochem Biophys Res Commun. 2018 May 5;499(2):156-163. DOI:10.1016/j.bbrc.2018.03.091 |
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| Company Name: |
Shaanxi Dideu Medichem Co. Ltd
|
| Telephone: |
+86-029-81138252 +86-173 9270 1263 |
| Website: |
https://www.chemicalbook.com/manufacturer/shaanxi-dideu-medichem-222/ |
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