Hesperetin is a flavanone extracted from the peel of citrus that exhibits inhibition of PDE4 and UGT. Hesperetin has antioxidative and anti-inflammatory effects as well. Hesperetin dose-dependently inhibited cleavage activity of the 3CLpro with IC50 value of 8.3μM in the cell-based assay.
Hesperetin is an effective antioxidant and anti-inflammatory agent. Hesperetin conferred neuroprotection by regulating the TLR4/NF-κB (Toll-like receptor-4) signaling pathway against the detrimental effects of LPS(lipopolysaccharide) [3]. Hesperetin (HET) and naringenin (NGR) are flavanones found in citrus (oranges and grapefruit) and Aurantii Fructus Immaturus. HET and NGR displayed broad-spectrum inhibition against human UGTs. HET exhibited strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC50 and Ki values lower than 10 µM) [4]. 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[5]. Preadministration of Hesperetin (40 mg/kg b.w., oral) significantly attenuated the Cd-induced (cadmium) oxidative stress and mitochondrial dysfunction, restored the antioxidant and membrane-bound enzyme activities and decreased apoptosis in the brain of rats[6]. Hesperetin (200 mg/kg) attenuates Con A-induced hepatocyte apoptosis and hepatic Nos2 (iNOS) expression in mice. Hesperetin blocked bile acid-induced apoptosis and cytokine-induced inflammation in rat hepatocytes[7].
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