Disease relevance of Rhapontigenin

• In this study, human neuroblastoma cells (IMR-32) was used as system model to evaluate the protective role of rhaponticin (3,3',5-trihydroxy-4'-methoxystilbene 3-O-d-glucoside) a stilbene glucoside extracted from rhubarb roots (Rhei rhizoma) and rhapontigenin, its aglycone metabolite, against amyloid beta (1-42)-dependent toxicity [1].
• Rhapontigenin showed significant protection from death due to pulmonary thrombosis in mice [2].
• Hep G2 hepatoma cells were treated with rhapontigenin or rhaponticin (0-250 microg/mL) and cell viability was measured [3].

High impact information on Rhapontigenin

• Further studies with rhapontigenin and synthetic stilbenes led to the discovery of 2,4,3',5'-tetramethoxystilbene, a selective inhibitor of P450 1B1 relative to other P450s [4].
• Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin [5].
• Of seven compounds tested, rhapontigenin (3,3',5-trihydroxy-4'-methoxystilbene) exhibited a potent and selective inhibition of human P450 1A1 with an IC50 value of 0.4 microM [5].
• The pharmacokinetics of piceatannol, pinosylvin and rhapontigenin were characterized in male Sprague-Dawley rats after single intravenous doses of 10 mg kg(-1) of each stilbene [6].
• Pharmacokinetics of selected stilbenes: rhapontigenin, piceatannol and pinosylvin in rats [6].

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

• In continued studies on cultivated Korean rhubarb rhizomes (Rheum undulatum), three known stilbenes (desoxyrhapontigenin, rhapontigenin, piceatannol) have been screened for activity on blood platelet aggregation [8].

Analytical, diagnostic and therapeutic context of Rhapontigenin

• Preparative enzymatic synthesis and HPLC analysis of rhapontigenin: applications to metabolism, pharmacokinetics and anti-cancer studies [3].

References