Abstract

Xanthohumol (XH) is an important prenylated flavonoid that is found within the inflorescence of L. (Hop plant). XH is an important ingredient in beer and is considered a significant bioactive agent due to its diverse medicinal applications, which include anti-inflammatory, antimicrobial, antioxidant, immunomodulatory, antiviral, antifungal, antigenotoxic, antiangiogenic, and antimalarial effects as well as strong anticancer activity towards various types of cancer cells. XH acts as a wide ranging chemopreventive and anticancer agent, and its isomer, 8-prenylnaringenin, is a phytoestrogen with strong estrogenic activity. The present review focuses on the bioactivity of XH on various types of cancers and its pharmacokinetics. In this paper, we first highlight, in brief, the history and use of hops and then the chemistry and structure-activity relationship of XH. Lastly, we focus on its prominent effects and mechanisms of action on various cancers and its possible use in cancer prevention and treatment. Considering the limited number of available reviews on this subject, our goal is to provide a complete and detailed understanding of the anticancer effects of XH against different cancers.

MeSH

Pharmacokinetics, Apoptosis, Neoplasms, Structure-Activity Relationship

Cited by

• Natural Dietary Compound Xanthohumol Regulates the Gut Microbiota and Its Metabolic Profile in a Mouse Model of Alzheimer's Disease. Molecules, 2022
• A Novel Look at Mechanisms and Applications of Xanthohumol (XN) in Dermatology and Cosmetology. Int J Mol Sci, 2024
• Xanthohumol-Enriched Beer Does Not Exert Antitumorigenic Effects on HeLa Cell Line In Vivo. Molecules, 2023
• Development of Guar Gum-Pectin-Based Colon Targeted Solid Self-Nanoemulsifying Drug Delivery System of Xanthohumol. Pharmaceutics, 2022
• Comparison of the Impact of Xanthohumol and Phenethyl Isothiocyanate and Their Combination on Nrf2 and NF-κB Pathways in HepG2 Cells In Vitro and Tumor Burden In Vivo. Nutrients, 2021
• An overview of natural herbal extracts and compounds for combating porcine epidemic diarrhea virus. Front Vet Sci, 2025
• Multivariate Data Analysis and Central Composite Design-Oriented Optimization of Solid Carriers for Formulation of Curcumin-Loaded Solid SNEDDS: Dissolution and Bioavailability Assessment. Pharmaceutics, 2022
• Ligand and Structure-Based Virtual Screening in Combination, to Evaluate Small Organic Molecules as Inhibitors for the XIAP Anti-Apoptotic Protein: The Xanthohumol Hypothesis. Molecules, 2022
• Antioxidants in Hops: Bioavailability, Health Effects and Perspectives for New Products. Antioxidants (Basel), 2022
• Two Important Anticancer Mechanisms of Natural and Synthetic Chalcones. Int J Mol Sci, 2022
• A Systematic Review: Quercetin-Secondary Metabolite of the Flavonol Class, with Multiple Health Benefits and Low Bioavailability. Int J Mol Sci, 2024
• Quality by Design (QbD) Based Method for Estimation of Xanthohumol in Bulk and Solid Lipid Nanoparticles and Validation. Molecules, 2023
• Xanthohumol Induces ROS through NADPH Oxidase, Causes Cell Cycle Arrest and Apoptosis. Oxid Med Cell Longev, 2022
• Differential Inhibite Effect of Xanthohumol on HepG2 Cells and Primary Hepatocytes. Dose Response, 2022
• A Review of Natural and Synthetic Chalcones as Anticancer Agents Targeting Topoisomerase Enzymes. Molecules, 2025
• SREBP2 as a central player in cancer progression: potential for targeted therapeutics. Front Pharmacol, 2025
• Modulation of Nrf2 and NF-κB Signaling Pathways by Naturally Occurring Compounds in Relation to Cancer Prevention and Therapy. Are Combinations Better Than Single Compounds? Int J Mol Sci, 2021
• Anticancer Potential of Xanthohumol and Isoxanthohumol Loaded into SBA-15 Mesoporous Silica Particles against B16F10 Melanoma Cells. Materials (Basel), 2022
• Quality by Design Based Formulation of Xanthohumol Loaded Solid Lipid Nanoparticles with Improved Bioavailability and Anticancer Effect against PC-3 Cells. Pharmaceutics, 2022
• Xanthohumol as a potential therapeutic strategy for acute myeloid leukemia: Targeting the FLT3/SRPK1 signaling axis. J Food Drug Anal, 2025