Abstract

Xanthohumol is the principal prenylated flavonoid of the female inflorescences of the hop plant. In recent years, various beneficial xanthohumol effects including anti-inflammatory, antioxidant, hypoglycemic activities, and anticancer effects have been revealed. This review summarizes present studies indicating that xanthohumol also inhibits several critical pathophysiological steps during the development and course of chronic liver disease, including the activation and pro-fibrogenic genotype of hepatic stellate cells. Also the various mechanism of action and molecular targets of the beneficial xanthohumol effects will be described. Furthermore, the potential use of xanthohumol or a xanthohumol-enriched hop extract as therapeutic agent to combat the progression of chronic liver disease will be discussed. It is notable that in addition to its hepatoprotective effects, xanthohumol also holds promise as a therapeutic agent for treating obesity, dysregulation of glucose metabolism and other components of the metabolic syndrome including hepatic steatosis. Thus, therapeutic xanthohumol application appears as a promising strategy, particularly in obese patients, to inhibit the development as well as the progression of non-alcoholic fatty liver disease.

Highlights

  • Hop (Humulus lupulus L.) has been used since ancient times as a medicinal plant

  • This review summarizes present studies indicating that xanthohumol inhibits several critical pathophysiological steps during the development and course of chronic liver disease, including the activation and pro-fibrogenic genotype of hepatic stellate cells

  • We provide a summary of present studies indicating the potential of this hop constituent as a therapeutic agent to beneficially affect hepatic fibrosis as well as various further pathological mechanisms during the course of chronic liver disease

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Summary

Introduction

Hop (Humulus lupulus L.) has been used since ancient times as a medicinal plant. Traditional medicinal indications included the treatment of anxiety and insomnia, mild pain reduction or combating dyspepsia (Zanoli and Zavatti, 2008). Hops are used in the manufacturing of beer and female infertile plants are cultivated on high trolleys especially for brewing (Figure 1A). Active substances, which are important for brewing, are concentrated inside hop cones (Figure 1B) in lupulin glands (Figure 1C) which contain hop resins, bitter acids, essential oils and prenylated flavonoids. These lupulin glands are tiny yellow sacs that are located at the base of the petals of the hop cone (Figure 1D) that are found in female plants, while cones from the male hop plant contain relatively few lupulin glands. Xanthohumol (XN; 3′-[3,3-dimethyl allyl]-2′,4′,4-trihydroxy-6′-methoxychalcone) is the principal prenylated chalcone of the hop plant (Figure 1E).

Hepatoprotective effects of xanthohumol
Effects of Xanthohumol on Hepatic Stellate Cells in vitro
XN Effects on Hepatocellular Cancer Cells and Primary Hepatocytes
XN Effects in Models of Acute Liver Injury
Effect of XN in Models of Chronic Liver Injury
XN reduced hepatitis C virus RNA levels
XN protects against DNA damage and cancer
Pharmacokinetics and Effective Dose of XN
Potential Forms of XN Application
Findings
Summary and Conclusion

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