Cinobufotalin

Cinobufotalin is a steroid glycoside originally isolated from the Asiatic toad (B. gargarizans) and has diverse biological activities.^1,2 It reduces SRC-3 protein levels in MCF-7 breast cancer cells when used at concentrations ranging from 10 to 100 nM.¹ Cinobufotalin (1 μM) reduces Na⁺/K⁺ pump activity, viability, and cell attachment of C7-MDCK cells.² It reduces expression of the epithelial-mesenchymal (EMT) markers E-cadherin, vimentin, ZEB1, and Slug in and migration and invasion of PC3 cells.³ Cinobufotalin (0.1-10 μM) is cytotoxic to A549, H460, and HTB-58 lung cancer cells.⁴ In vivo, cinobufotalin (1 and 5 mg/kg) reduces tumor volume and increases survival in an A549 mouse xenograft model.

1.Wang, Y., Lonard, D.M., Yu, Y., et al.Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1Cancer Res.74(5)1506-1517(2014) 2.Akimova, O.A., Bagrov, A.Y., Lopina, O.D., et al.Cardiotonic steroids differentially affect intracellular Na+ and [Na+]i/[K+]i-independent signaling in C7-MDCK cellsJ. Biol. Chem.280(1)832-839(2005) 3.Chen, L., Mai, W., Chen, M., et al.Arenobufagin inhibits prostate cancer epithelial-mesenchymal transition and metastasis by down-regulating β-cateninPharmacol. Res.123130-142(2017) 4.Kai, S., Lu, J.-H., Hui, P.-P., et al.Pre-clinical evaluation of cinobufotalin as a potential anti-lung cancer agentBiochem. Biophys. Res. Commun.452(3)768-774(2014)