Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC₅₀ and a K_i of 61 µM and 22.8 µM for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects. IC50 & Target: IC50: 61 µM (CYP2A6)^[1]
Ki: 22.8 µM (CYP2A6)^[1] In Vitro: Gentiopicroside inhibits P450 activity, with an IC₅₀ and a K_i of 61 µM and 8.12 µM for CYP2A6, also slightly inhibits CYP2E1 activity with an IC₅₀ of 1.6 mM, but shows no inhibition on CYP1A2 and CYP3A4^[1]. Gentiopicroside (12.5, 25 and 50 μM) inhibits RANKL-induced osteoclast formation from mouse bone marrow macrophages (BMMs) in a dose-dependent manner, blocks the expression of osteoclast-related proteins, prevents receptor activator of nuclear factor-κB ligand (RANKL)-triggered JNK and NF-κB activation. Gentiopicroside (50 μM) also inhibits RANKL-induced bone resorption^[3]. In Vivo: Gentiopicroside (20, 40, and 80 mg/kg, p.o.) significantly reduces gastric ulcerindex in mice. Gentiopicroside (20, 40, and 80 mg/kg) also ovbiously decreases the levels of HSP-70, TNF-α, IL-6, MDA and increases ncreased GSH level and SOD activity. In addition, Gentiopicroside normalizes EGF and VEGF level in mice^[2].