Hesperetin

520-33-2

C16H14O6

DMSO : >= 33 mg/mL (109.17 mM)

MAPK/ERK Pathway; Apoptosis

Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. In Vitro: Hesperetin has the retention of antioxidant potential in self nano-emulsifying drug delivery system^[1]. Hesperetin and NGR display broad-spectrum inhibition against human UGTs. Besides, Hesperetin exhibits strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC₅₀ and K_i values lower than 10 uM) and moderately inhibits UGT1A4, UGT1A7, UGT1A8 (IC₅₀ values 29.68-63.87 uM)^[2]. Hesperetin interacts with different types of proteins involving hydrogen bonds, pi-pi effects, pi-cation bonding and pi-sigma interactions with varying binding energies. Hesperetin exhibits drug-like properties which projects its potential as a therapeutic option for CHIKV infection^[3]. Hesperetin dose-dependently reduces GCDCA-induced caspase-3 activity in cultured primary rat hepatocytes. Hesperetin also dose-dependently reduces CM-induced Nos2 (iNOS) expression in hepatocytes. Interestingly, hesperetin-induced expression of the antioxidant gene haem oxygenase 1 (HO-1) about fourfold compared with cytokine mixture alone^[5]. In Vivo: Preadministration of Hesperetin (40 mg/kg b.w., oral) significantly attenuates the Cd-induced oxidative stress and mitochondrial dysfunction, restores the antioxidant and membrane-bound enzyme activities and decreases apoptosis in the brain of rats^[4]. Hesperetin (200 mg/kg) attenuates Con A-induced hepatocyte apoptosis and hepatic Nos2 (iNOS) expression in mice. Hesperetin co-treatment also decreases the occurrence of apoptotic bodies, hydropic degeneration, nuclear fragments, autolysis and haemorrhage. The number of leukocytes infiltrated in liver tissue of mice with D-GalN/LPS-induced fulminant hepatitis are significantly decreased by hesperetin in a murine model^[5].