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Chemical Compound Review

Protigenin     5-[(E)-2-(3-hydroxy-4- methoxy...

Synonyms: Rhapontigenin, CHEMBL113029, SureCN1486816, AC-7022, ZINC26981407, ...
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Disease relevance of Rhapontigenin


High impact information on Rhapontigenin


Biological context of Rhapontigenin

  • Resveratrol (1) and rhapontigenin (5) demonstrated significant inhibitions upon the release of beta-hexosaminidase from the cultured RBL-2H3 cells in a dose-dependent manner and the IC50 values were calculated as 14 and 15 microM, respectively [7].
  • We have further investigated the inhibition kinetics of P450 1A1 by rhapontigenin [5].
  • Rhapontigenin intravenous dosing yielded the plasma AUC, urine t(1/2), CL and V(d) values of 8.39+/-0.10 mug h mL(-1), 25.31+/-1.46 h, 1.18+/-0.035 Lh(-1) kg(-1) and 11.05+/-0.17 L kg(-1)(mean+/-s.e.m.), respectively [6].
  • The obtained results show that rhapontigenin maintains significant cell viability in a dose-dependent manner and it exerts a protective effect on mitochondrial functionality, as evidenced by mitochondrial oxygen consumption experiments [1].
  • Rhapontigenin intraperitoneally administered showed the strongest inhibitory activity and significantly inhibited PCA at doses of 25 and 50 mg/kg, with inhibitory activities of 48 and 85%, respectively [2].

Anatomical context of Rhapontigenin


Analytical, diagnostic and therapeutic context of Rhapontigenin


  1. Protective effect of rhubarb derivatives on amyloid beta (1-42) peptide-induced apoptosis in IMR-32 cells: A case of nutrigenomic. Misiti, F., Sampaolese, B., Mezzogori, D., Orsini, F., Pezzotti, M., Giardina, B., Clementi, M.E. Brain Res. Bull. (2006) [Pubmed]
  2. Antithrombotic and antiallergic activities of rhaponticin from Rhei Rhizoma are activated by human intestinal bacteria. Park, E.K., Choo, M.K., Yoon, H.K., Kim, D.H. Arch. Pharm. Res. (2002) [Pubmed]
  3. Preparative enzymatic synthesis and HPLC analysis of rhapontigenin: applications to metabolism, pharmacokinetics and anti-cancer studies. Roupe, K.A., Helms, G.L., Halls, S.C., Yáñez, J.A., Davies, N.M. Journal of pharmacy & pharmaceutical sciences [electronic resource] : a publication of the Canadian Society for Pharmaceutical Sciences, Société canadienne des sciences pharmaceutiques. (2005) [Pubmed]
  4. Cytochrome P450 1B1: a target for inhibition in anticarcinogenesis strategies. Peter Guengerich, F., Chun, Y.J., Kim, D., Gillam, E.M., Shimada, T. Mutat. Res. (2003) [Pubmed]
  5. Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin. Chun, Y.J., Ryu, S.Y., Jeong, T.C., Kim, M.Y. Drug Metab. Dispos. (2001) [Pubmed]
  6. Pharmacokinetics of selected stilbenes: rhapontigenin, piceatannol and pinosylvin in rats. Roupe, K.A., Y????ez, J.A., Teng, X.W., Davies, N.M. J. Pharm. Pharmacol. (2006) [Pubmed]
  7. Anti-allergic action of resveratrol and related hydroxystilbenes. Cheong, H., Ryu, S.Y., Kim, K.M. Planta Med. (1999) [Pubmed]
  8. Anti-platelet aggregation activity of stilbene derivatives from Rheum undulatum. Ko, S.K., Lee, S.M., Whang, W.K. Arch. Pharm. Res. (1999) [Pubmed]
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