Xanthohumol inhibits hepatitis B virus replication in vitro

Xanthohumol is the principal prenylated chalcone of the female inflorescences of the hop plant, and it has been shown to have several beneficial biological activities, with its chemopreventive and anti-inflammatory properties being the most extensively investigated. Previously, we have shown that xanthohumol inhibits hepatic inflammation and fibrosis in a murine model of non-alcoholic steatohepatitis as well as the tumorigenicity of hepatocellular carcinoma (HCC) cells in vitro. Chronic hepatitis B virus (HBV) infection is one of the most frequent liver disease worldwide. It harbors a high risk to progress to cirrhosis and HCC, and HBV viral load is associated with a high risk of fibrosis progression and malignant transformation.

The aim of this study was to analyze the effect of xanthohumol on HBV-replication.

Methods and Results: The HBV producing cell line HepG2.2.15 was incubated with different concentrations of xanthohumol, and after 24h HBV DNA was analyzed in the supernatant by RT-PCR. In the range of 5–10µM xanthohumol incubation lead to a dose-dependent reduction of DNA copies. In this dose-range xanthohumol did not affect viability or proliferation of HepG2.2.15 as evidenced by morphological analysis, determination of LDH-release, cell-counting, and analysis of mitochondrial activity. Furthermore and importantly, xanthohumol did not affect viability of primary human hepatocytes in a dose-range up to 100µM.

Conclusions: Our in vitro data indicate the potential of xanthohumol to inhibit HBV replication, and herewith, a crucial pathophysiological factor for the progression of HBV related liver disease. Previous studies have shown the safety of even long term application of hop extracts in man, and thus, our data suggest the potential use of xanthohumol as a functional nutrient for HBV infected patients.