Resibufogenin Chemical Properties

Melting point:

113-140°/155-168°

alpha 

D22 -7.1° (c = 1.259 in chloroform); D16 -5.4° (c = 2.030 in chloroform)

Boiling point:

431.17°C (rough estimate)

Density 

1.0474 (rough estimate)

refractive index 

1.4860 (estimate)

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

solubility 

DMF: 25 mg/mL; DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL; DMSO: 20 mg/mL; Ethanol: 5 mg/mL

form 

White to off-white solid.

pka

15.14±0.70(Predicted)

Stability:

Moisture Sensitive

Safety Information

Safety Statements 

24/25

RIDADR 

3172

HazardClass 

6.1(a)

PackingGroup 

II

HS Code 

29322090

Toxicity

LD50 oral in mouse: 59800mg/kg

MSDS

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Resibufogenin Usage And Synthesis

Description

As one of the active components of Bufonis bufa, Resibufogenin is speculated that Etobufaxin can inhibit the proliferation of tumor cells by inducing apoptosis of osteosarcoma cells.

Uses

Resibufogenin is used for content determination/identification/pharmacological experiments, etc.

Definition

ChEBI: Bufogenin is a steroid lactone of Chan su (toad venom), a Chinese medicine obtained from the skin venom gland of toads. A specific Na/K-ATPase protein inhibitor, it is used as a cardiotonic and central nervous system (CNS) respiratory agent, an analgesic and anesthetic, and as a remedy for ulcers. It has a role as an EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor. It is a steroid lactone and an epoxy steroid. It is functionally related to a bufanolide.

Biological Activity

Resibufogenin (Bufogenin, Recibufogenin) is the anticancer component of huachansu cinobufogenin, which triggers necrosis by up-regulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating Ser358 of mixed lineage kinase domain-like protein. It exerts cytotoxic effects by inducing the accumulation of reactive oxygen species (ROS). Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Also it increases Bax/Bcl-2 expression and inhibits protein expression of cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin.

Pharmacokinetics

The main pharmacological action of acetobufaxin is anti-tumor. The cinobufavidin injection was separated by modern chromatographic techniques, and the exobufaxin compounds were obtained. The main monomers of exobufaxin were analyzed and identified by HPLC-DAD-FT-ICR-MS. The anti-tumor activity of exobufaxin was screened in vitro, and the pancreatic cancer tumor-bearing nude mouse model was established in vivo to evaluate the efficacy of exobufaxin.

target

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