Resibufogenin

Bezeichnung:Resibufogenin

CAS-Nr465-39-4

Englisch Name:Resibufogenin

CBNumberCB6254472

SummenformelC24H32O4

Molgewicht384.51

MOL-Datei465-39-4.mol

Resibufogenin physikalisch-chemischer Eigenschaften

Schmelzpunkt	113-140°/155-168°
alpha	D22 -7.1° (c = 1.259 in chloroform); D16 -5.4° (c = 2.030 in chloroform)
Siedepunkt	431.17°C (rough estimate)
Dichte	1.0474 (rough estimate)
Brechungsindex	1.4860 (estimate)
storage temp.	under inert gas (nitrogen or Argon) at 2-8°C
Löslichkeit	DMF: 25 mg/mL; DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL; DMSO: 20 mg/mL; Ethanol: 5 mg/mL
Aggregatzustand	White to off-white solid.
pka	15.14±0.70(Predicted)
Farbe	White to off-white
Stabilität	Moisture Sensitive

Sicherheit

S-Sätze:	24/25
RIDADR	3172
HazardClass	6.1(a)
PackingGroup	II
HS Code	29322090
Toxizität	LD50 oral in mouse: 59800mg/kg

Gefahreninformationscode (GHS)

Resibufogenin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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.
Biologische Aktivität
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.
Pharmakokinetik
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

Target Value
RIP3
()
MLK
()
ROS
()
Caspase-3
()
Caspase-8
()
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Target	Value
RIP3 ()
MLK ()
ROS ()
Caspase-3 ()
Caspase-8 ()
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