Description
Rhapontigenin is a natural analog of resveratrol and an inhibitor of CYP1A1.
Description
Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-
cancer activity. It is a mechanism-
based, selective inactivator of cytochrome P450 1A1 (IC
50 = 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. At higher concentrations, rhapontigenin inhibits the proliferation of HepG2 and HL-
60R cancer cell lines (IC
50 = 48 μM).
Chemical Properties
Yellow crystalline powder, soluble in organic solvents such as methanol, ethanol, DMSO, etc., derived from Rheum officinale.
Uses
Rhapontigenin is a natural analog of resveratrol and an inhibitor of CYP1A1.
Uses
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. At higher concentrations, rhapontigenin inhibits the proliferation of HepG2 and HL-60R cancer cell lines (IC50 = 48 μM).[Cayman Chemical]
Definition
ChEBI: Rhapontigenin is a stilbenoid.
in vivo
Rhapontigenin (intraperitoneal injection; 25mg/kg) shows significant protection from death due to pulmonary thrombosis in mice, those samples are orally administered 90 min before tail vein injection of epinephrine and collagen[3].
| Animal Model: | ICR mice[3] |
| Dosage: | 25mg/kg |
| Administration: | 25mg/kg; intraperitoneal injection |
| Result: | Showed anti-thrombosis activity with 60% protection. |
IC 50
CYP1A1: 400 nM (IC
50)
References
[1]. chun yj, ryu sy, jeong tc, et al. mechanism-based inhibition of human cytochrome p450 1a1 by rhapontigenin. drug metab dispos. 2001 apr;29(4 pt 1):389-93.
[2]. roberti m1, pizzirani d, simoni d, et al. synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents. j med chem. 2003 jul 31;46(16):3546-54.
[3]. roupe ka1, helms gl, halls sc, et al. preparative enzymatic synthesis and hplc analysis of rhapontigenin: applications to metabolism, pharmacokinetics and anti-cancer studies. j pharm pharm sci. 2005 aug 22;8(3):374-86.
