Hellebrin

Hellebrin is a cardiac glycoside that potently inhibits the Na⁺/K⁺-ATPase by binding to it and blocking its non-canonical function as a receptor for cardiac glycosides.^1,2 Hellebrin has a higher affinity for the α₁β₁ subunit of the Na⁺/K⁺-ATPase than the α₂β₁ or α₃β₁ complexes, in contrast to other cardiac glycosides.¹ This affinity for the α₁β₁ complex correlates with its cancer cell growth inhibition (GI₅₀ = 6-58 nM in various human cancer cell lines). Hellebrin also induces caspase-dependent apoptosis in Jurkat T cells.³

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1. Moreno, Y.B.L., Katz, A., Miklos, W., et al. Hellebrin and its aglycone form hellebrigenin display similar in vitro growth inhibitory effects in cancer cells and binding profiles to the alpha subunits of the Na⁺/K⁺-ATPase. Mol. Cancer 12, 1-14 (2013).

2. Ogawa, H., Shinoda, T., Cornelius, F., et al. Crystal structure of the sodium-potassium pump (Na⁺,K⁺-ATPase) with bound potassium and ouabain. Proc. Natl. Acad. Sci. USA 106(33), 13742-13747 (2009).

3. Daniel, D., Süsal, C., Kopp, B., et al. Apoptosis-mediated selective killing of malignant cells by cardiac steroids: Maintenance of cytotoxicity and loss of cardiac activity of chemically modified derivatives. Int. Immunopharmacol. 3, 1791-1801 (2003).