Bufalin

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Chemical Structure| 465-21-4 同义名 : NSC 89595; BF
CAS号 : 465-21-4
货号 : A206803
分子式 : C24H34O4
纯度 : 98%
分子量 : 386.52
MDL号 : MFCD00056525
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(271.65 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
生物活性
描述 Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively[3]. Bufalin caused significant cytotoxicity in NCI-H460 cells at a concentration as low as 1 μM. DNA condensation was observed in bufalin-treated cells in a dose-dependent manner. Bufalin injected intraperitoneally in a dose-dependent manner reduced tumor size in BALB/C nu/nu mice implanted with NCI-H460 cells. Bufalin injection did not produce significant drug-related toxicity in experimental animals except at a high dose (0.4 mg/kg)[4]. Bufalin-induced disruption of the SRC-1 (steroid receptor coactivator) isoform/ERβ (estrogen receptor) axis might induce apoptosis, pyroptosis and ERS (endoplasmic reticulum-stress) signaling in endometriotic lesions, causing the suppression of endometriosis[5]. Bufalin inhibits cell proliferation and migration of HCC (hepatocellular carcinoma) cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.87mL

5.17mL

2.59mL
参考文献

[1]Jiang L, Zhao MN, et al. Bufalin induces cell cycle arrest and apoptosis in gallbladder carcinoma cells. Tumour Biol. 2014 Nov;35(11):10931-41.

[2]Wu SH, Wu TY, et al. Bufalin induces cell death in human lung cancer cells through disruption of DNA damage response pathways. Am J Chin Med. 2014;42(3):729-42.

[3]Katz A, Lifshitz Y, Bab-Dinitz E, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010;285(25):19582-19592

[4]Wu SH, Bau DT, Hsiao YT, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017;32(4):1305-1317

[5]Cho YJ, Lee JE, Park MJ, O'Malley BW, Han SJ. Bufalin suppresses endometriosis progression by inducing pyroptosis and apoptosis. J Endocrinol.2018;237(3):255-269

[6]Yang Z, Tao Y, Xu X, Cai F, Yu Y, Ma L. Bufalin inhibits cell proliferation and migration of hepatocellular carcinoma cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway. Biochem Biophys Res Commun.2018;503(3):2124-2131