Cinobufagin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cinobufagin 是一种选择性 Na+/K+-ATPase 抑制剂。华蟾素的活性与哇巴因相同。

Cinobufagin is a cardiotoxic bufanolide steroid secreted by the Asiatic toad Bufo gargarizans. It has similar effects to digitalis and is used in traditional Chinese medicine. Cinobufagin has been shown to have clinical applications in cancer treatment as well as immunomodulatory and analgesic properties. Cinobufagin induces apoptosis of osteosarcoma cells through inactivation of Notch signaling. Cinobufagin induces autophagy-mediated cell death in human osteosarcoma U2OS cells through the ROS/JNK/p38 signaling pathway.

Cell Proliferation Assay Cell Line:OCM1 cell Concentration:30,100,300 nMIncubation Time:7 daysResult:Exerted potent cytotoxic in OCM1 cells with an IC50 of 8.023 nM. Apoptosis Analysis Cell Line:OCM1 cell Concentration:30,100,300 nM Incubation Time:24 hours Result:Induced cell apoptosis and upregulate the expression levels of cleaved caspase-3, cleaved poly(ADP-ribose) polymerase (PARP), and cleaved caspase-9. Activated the intrinsic mitochondrial apoptosis pathway, which was demonstrated by increased cell apoptosis with increased expression of Bad and Bax, decreased expression of Bcl-2 and Bcl-xl, and reduced mitochondrial membrane potential (MMP).

Animal Model:OCM1 cells tumor xenograft in Nu/Nu nude mice Dosage:5 mg/kg Administration:Intraperitoneal injection (i.p.), once a day for 10 days Result:Made the tumors grew more slowly than those treated with intraperitoneal injection of saline or untreated. Increased the expression of caspase-3 and PARP in tumor tissues and decreased Bcl-2 and Bcl-xl expression in mouse tumor tissues and increased expression of Bad and Bax. Animal Model:U87MG-EGFR subcutaneous and intracranial xenograft model Dosage:5 mg/kg Administration:Intraperitoneal injection (i.p.), once a day for 10 days Result:Decreased the luminescence intensity of brain tumor about 70%.Decreased p-EGFR, p-STAT3, and p-Akt levels in the intracranial tumors as compared with the vehicles.Decreased Ki67 and active caspase-3 immunostaining of intracranial tumors.

Cinobufagin | Cinobufagine | Cino-bufagin

Microbiology/Virology

Antifungal

Na+/K+-ATPase

Cancer

——

470-37-1

442.55

C26H34O6

>98% (HPLC)

DMSO : ≥ 43 mg/mL; 97.17 mM

CC(=O)O[C@@H]1[C@@H]([C@]2(CC[C@H]3[C@H]([C@]42[C@@H]1O4)CC[C@H]1[C@@]3(CC[C@@H](C1)O)C)C)c1coc(=O)cc1

(1R,2R,2aR,3aS,3bS,5aR,7S,9aS,9bR,11aS)-7-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-4-yl)hexadecahydronaphtho[1',2':6,7]indeno[1,7a-b]oxiren-2-yl acetate

(-20℃)

With Ice Pack

≥ 2 years