Background:

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[1][2]. Anti-cancer activity[2].

Bufalin (0, 1, 2, 4 μM for 48 hours) decreases cell viability in NCI-H460 cells[2].Bufalin (2 μM) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78 mRNA expression[2].

Bufalin (0.1, 0.2, or 0.4 mg/kg, i.p., daily for 14 days) shows significant anti-tumor activity in mice bearing NCI-H460 cells[2].

参考文献:
[1]. Katz A, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010 Jun 18;285(25):19582-92.
[2]. Wu SH, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017 Apr;32(4):1305-1317.