Apigenin is a natural flavonoid compound that has antioxidative, anti-inflammatory, and hepatoprotective effects, but the underlying mechanisms are still unclear. In this study, the effects of apigenin on ethanol-induced oxidative stress and lipopolysaccharide (LPS)-induced inflammatory cytokine production were examined in cultured rat hepatocytes. Following pretreatment of ethanol-stimulated hepatocytes with apigenin 6–24 mM for 2 h, the levels of cytochrome P450 2E1 (CYP2E1) protein expression and supernatant alanine aminotransferase and malondialdehyde were reduced (P < 0.05 or P < 0.01), while the activities of glutathione reductase and glutathione peroxidase were increased (P < 0.05 or P < 0.01). Likewise, the pretreatment of LPS-stimulated hepatocytes with the same concentrations of apigenin could decrease the levels of nuclear factor-κB protein expression and supernatant tumor necrosis factor-α and interleukin-6 (P < 0.05 or P < 0.01), and increase the level of IκB-α protein expression (P < 0.05 or P < 0.01). In all of these results, the concentration of 24 μM was the most effective. These findings demonstrate that apigenin may exert an inhibitory effect on ethanol-induced oxidative stress and LPS-induced inflammation in the cultured hepatocytes, and its mechanisms may be related to the reduction of CYP2E1 expression, increment of antioxidative ability, and regulation of inflammatory gene expression.

Leiyunshang Pharmaceutical Co Ltd Suzhou Jiangsu Province China

Nantong University School of Pharmacy Department of Pharmaceutical Laboratory Nantong Jiangsu Province China

Soochow University College of Pharmaceutical Sciences Department of Pharmacology Suzhou Jiangsu Province China

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