Rhapontigenin

Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1?inactivator (IC₅₀ ?= 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively^[1]. In Vitro: Rhapontigenin (0-250 μM; 24 hours) demonstrates concentration-dependent?anti-cancer?activity with an IC₅₀ 115μM in HEP G2 cells^[1].
Rhapontigenin (20 μM; 20 hours) pre-treatment decreases TGF-β triggered increased snail expression in diverse cancer cells^[2].
Rhapontigenin (0-20 μM; 6 hours) inhibits TGF-β-induced expression of N-cadherin, vimentin, and CA9 in a dose-dependent manner^[2].
Rhapontigenin inhibits ADP- and collagen-induced platelet aggregation with IC₅₀ values of 4 and 70 μg/ml, respectively^[3].
Rhapontigenin demonstrates a strong inhibitory activity on the 13-hexosaminidase release induced by DNP-BSA, it exhibits IC₅₀ value of 0.03 mM in RBL 2H3 cells^[3].
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].