| Description | Arenobufagin is a natural bufadienolide from toad venom with potent antineoplastic activity against HCC HepG2 cells and corresponding multidrug-resistant HepG2/ADM cells. |
| In vitro | Arenobufagin在HCC细胞中诱导线粒体介导的凋亡，表现为线粒体电位下降以及Bax/Bcl-2表达比率增加，Bax从细胞质转移到线粒体。Arenobufagin还在HepG2/ADM细胞中诱导自噬。自噬特异性抑制剂(3-甲基腺嘌呤、氯喹和bafilomycin A1)或Beclin1和Atg 5小干扰RNA (siRNAs)能增强Arenobufagin诱导的凋亡，表明Arenobufagin介导的自噬可能保护HepG2/ADM细胞免遭凋亡性细胞死亡[1]。Arenobufagin抑制了血管内皮生长因子(VEGF)诱导的人脐静脉内皮细胞(HUVECs)的活力、迁移、侵袭以及管状形成，体外试验显示[2]。Arenobufagin以剂量依赖性方式阻断Na+/K+泵电流，半最大效应浓度为0.29μM，希尔系数为1.1 [3]。 |
| In vivo | Arenobufagin抑制了HepG2/ADM异种移植瘤的生长，这与poly (ADP-ribose) polymerase的裂解、light chain 3-II的激活和mTOR的抑制有关[1]。Arenobufagin还在体外模型中抑制了VEGF处理的主动脉环的萌芽形成[2]。 |
| Synonyms | 沙蟾毒精, 沙蟾毒经 |
| molecular weight | 416.51 |
| Molecular formula | C24H32O6 |
| CAS | 464-74-4 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 83 mg/mL (199.27 mM ), Sonication is recommended. Ethanol: 10 mg/mL (24.1 mM) |
| References | 1. Zhang DM, et al. Arenobufagin, a natural bufadienolide from toad venom, induces apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Carcinogenesis. 2013 Jun;34(6):1331-42. 2. Li M, et al. Arenobufagin, a bufadienolide compound from toad venom, inhibits VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway. Biochem Pharmacol. 2012 May 1;83(9):1251-60. 3. Cruz Jdos S, et al. Arenobufagin, a compound in toad venom, blocks Na(+)-K+ pump current in cardiac myocytes. Eur J Pharmacol. 1993 Aug 3;239(1-3):223-6. |