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Resibufogenin

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Chemical Structure| 465-39-4 同义名 : 蟾力苏 ;Bufogenin;Recibufogenin;Bufotenine;RBG;Respigon;NSC 90783
CAS号 : 465-39-4
货号 : A151203
分子式 : C24H32O4
纯度 : 98%
分子量 : 384.509
MDL号 : MFCD00210361
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(273.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PI3K
描述 Necrosis can occur in a highly regulated and genetically controlled manner. Necroptotic susceptibility is probably an intrinsic weakness of cancer. Resibufogenin is a major bioactive compound that belongs to bufadienolide family. It is isolated from toad venom. Resibufogenin decreased the cell viability dose-dependently in HCT116 cells. The clonogenic cell survival assay showed that resibufogenin significantly reduced the number of cell clones as compared to the control group, provided further evidence that resibufogenin is an effective antineoplastic agent through inhibiting cell proliferation. Extensive organelle and cell swelling, cytoplasmic vacuolation were observed in resibufogenin-treated SW480 and HCT116. Intracellular ROS (reactive oxygen species) level was also increased in a dose-dependent manner in resibufogenin treated cells. After administration (i.p.) of resibufogenin at 5 and 10 mg/kg/day in mice for 21 days, the weight of tumor in situ were significantly reduced by 27 and 41%, respectively. Vernier caliper measurement showed that resibufogenin decreased the tumor volume in a dose-dependent manner. The weight loss caused by tumor growth was significantly ameliorated by high dose of resibufogenin. These results provide strong evidence that resibufogenin suppresses tumor growth of CRC (colorectal cancer) and ameliorates the weight loss in tumor-bearing mice. Remarkable increase in levels of PYGL, GLUD1 and GLUL as well as increase of RIP3 in resibufogenin-treated mice compared with the control group suggests that resibufogenin inhibits tumor growth through inducing RIP3-mediated activation of PYGL, GLUD1 and GLUL to induce necroptosis in CRC cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL
参考文献

[1]Ning J, Yu ZL, et al. Characterization of phase I metabolism of resibufogenin and evaluation of the metabolic effects on its antitumor activity and toxicity. Drug Metab Dispos. 2015 Mar;43(3):299-308.

[2]Zhu ZT, Deng S, et al. Isolation and identification of phase I metabolites of resibufogenin in rats. Xenobiotica. 2013 May;43(5):479-85.

[3]Han Q, Ma Y, Wang H, et al. Resibufogenin suppresses colorectal cancer growth and metastasis through RIP3-mediated necroptosis. J Transl Med. 2018;16(1):201