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Hyperoside, an active compound found in plants of the genera  Hypericum  and  Crataegus , is reported to exhibit antioxidant, anticancer, and anti-inflammatory activities. Induction of hepatic stellate cell (HSC) apoptosis is recognized as a promising strategy for attenuation of hepatic fibrosis. In this study, we investigated whether hyperoside treatment can exert antifibrotic effects in human LX-2 hepatic stellate cells. We found that hyperoside induced apoptosis in LX-2 cells and decreased levels of  α -smooth muscle actin ( α -SMA), type I collagen, and intracellular reactive oxygen species (ROS). Remarkably, hyperoside also inhibited the DNA-binding activity of the transcription factor NF- κ B and altered expression levels of NF- κ B-regulated genes related to apoptosis, including proapoptotic genes  Bcl-Xs ,  DR4 ,  Fas , and  FasL  and anti-apoptotic genes  A20 ,  c-IAP1 ,  Bcl-X    L  , and  RIP1 . Our results suggest that hyperoside may have potential as a therapeutic agent for the treatment of liver fibrosis.

Dietary Flavonoid Hyperoside Induces Apoptosis of Activated Human LX-2 Hepatic Stellate Cell by Suppressing Canonical NF-κB Signaling