Herbacetin

Herbacetin is a natural product that acts as a selective inhibitor of ornithine decarboxylase (ODC).¹ It inhibits recombinant and HCT116 and HT29 colon cancer cell-derived ODC in a dose-dependent manner while having no effect on 13 tested kinases or S-adenosylmethionine decarboxylase in vitro. Herbacetin suppresses anchorage-independent growth, activation of activator protein-1 (AP-1), a MAP kinase transcription factor, and phosphorylation of ERK1/2 and p90^RSK in vitro. It suppresses HCT116 xenograft tumor growth in mice without significant body weight loss when administered i.p. or orally. Herbacetin also inhibits acetylcholinesterase (AChE; IC₅₀ = 1.37 μM) in vitro.²

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1. Kim, D.J., Roh, E.J., Lee, M.-H., et al. Herbacetin is a novel allosteric inhibitor of ornithine decarboxylase with antitumor activity. Cancer Res. 76(5), 1146-1157 (2016).

2. Li, F.J., Liu, Y., Yuan, Y., et al. Molecular interaction studies of acetylcholinesterase with potential acetylcholinesterase inhibitors from the root of Rhodiola crenulata using molecular docking and isothermal titration calorimetry methods. Int. J. Biol. Macromol. 104(Pt. A), 527-532 (2017).