Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. It 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.1 At higher concentrations, rhapontigenin inhibits the proliferation of Hep-G2 and HL-60R cancer cell lines (IC50 = 48 μM).2,3
1
Chun, Y.J., Ryu, S.Y., Jeong, T.C., et al. Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin. Drug Metab Dispos29(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 Pharm Sci8(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 Chem463546-3554(2003).
Room temperature
in continental US; may vary elsewhere
SMILES
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COc1ccc(/C=C\c2cc(O)cc(O)c2)cc1O
Background Reading
Ohinata, Y., Payer, B., O'Carroll, D., et al. Blimp1 is a critical determinant of the germ cell lineage in mice. Nature436207-213(2005).
Chun, Y.J., Ryu, S.Y., Jeong, T.C., et al. Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin. Drug Metab Dispos29(4)389-393(2001).
Roberti, M., Pizzirani, D., Simoni, D., et al. Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents. J Med Chem463546-3554(2003).
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 Pharm Sci8(3)374-386(2005).