Cinobufagin

Cinobufagin is a cardiotonic steroid that has been found in the skin of toads of genus Bufo and has diverse biological activities.^1,2,3,4 It inhibits Na⁺/K⁺-ATPase activity in guinea pig heart ventricular muscle homogenates by 45% when used at a concentration of 0.3 μM.¹ Cinobufagin is cytotoxic to HCT116 colorectal cancer cells in vitro with IC₅₀ values of less than 50 ng/ml at 48- and 72-hour time points and induces apoptosis in a concentration-dependent manner.² In vivo, cinobufagin (10 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model. Cinobufagin (1 μg/ml) inhibits LPS-induced expression of MHC class II, CD80, and CD86 and release of IL-6, IL-8, TNF-α, and IL-10 in human monocyte-derived dendritic cells.³ It also increases expression of the antimicrobial peptides hBD2 and hBD3 in dendritic cells. Cinobufagin exhibits dose-dependent antinociceptive effects in the hot-plate, acetic acid writhing, and formalin tests in mice.⁴

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1. Tõma, S., Morishita, S., Kuronuma, K., et al. Metabolism and pharmacokinetics of cinobufagin. Xenobiotica 17(10), 1195-1202 (1987).

2. Lu, X.-s., Qiao, Y.-b., Li, Y., et al. Preclinical study of cinobufagin as a promising anti-colorectal cancer agent. Oncotarget 8(1), 988-998 (2017).

3. Xie, S., Spelmink, L., Codemo, M., et al. Cinobufagin modulates human innate immune responses and triggers antibacterial activity. PLoS One 11(8), e0160734 (2016).

4. Xu, L., Zhang, X., Feng, Q., et al. Alpha-7 nicotinic receptor-targeted cinobufagin induces antinociception and inhibits NF-κB signaling pathway in DRG neurons. ACS Chem. Neurosci. 10(1), 497-506 (2019).