Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. Rhapontigenin is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. At higher concentrations, Rhapontigenin inhibits the proliferation of Hep-G2 and HL-60R cancer cell lines (IC50 = 48 μM).
1 Chun, Y.J., Ryu, S.Y., Jeong, T.C., et al. Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin. Drug Metab Dispos 29(4) 389-393 (2001).
2 Roupe, K.A., Helms, G.L., Halls, S.C., et al. Preparative enzymatic synthesis and HPLC analysis of rhapontigenin: Applications to metabolism, pharmacokinetics and anti-cancer studies. J Pharm Pharmaceut Sci 8(3) 374-386 (2005).
3 Roberti, M., Pizzirani, D., Simoni, D., et al. Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents. J Med Chem 46 3546-3554 (2003).
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PMID: # 28248427 Paasela, T. et al. 2017. New Phytol. 214: 1537-1550.
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