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Review

Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets

1
Department of Pharmaceutics, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara 144 411, Punjab, India
2
Department of Experimental Embryology, Institute of Genetics and Animal Biotechnology of the Polish Academy of Sciences, 05-552 Jastrzebiec, Poland
3
Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA
4
Department of Pharmacognosy, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara 144 411, Punjab, India
*
Authors to whom correspondence should be addressed.
Academic Editor: Ignazio Barbagallo
Int. J. Mol. Sci. 2021, 22(9), 4478; https://doi.org/10.3390/ijms22094478
Received: 31 March 2021 / Revised: 19 April 2021 / Accepted: 23 April 2021 / Published: 25 April 2021
(This article belongs to the Special Issue Biological Properties of Secondary Metabolites and Natural Compounds)
Xanthohumol (XH) is an important prenylated flavonoid that is found within the inflorescence of Humulus lupulus 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. View Full-Text
Keywords: xanthohumol; Humulus lupulus L.; cancer; proliferation; apoptosis; therapy; prevention; molecular targets xanthohumol; Humulus lupulus L.; cancer; proliferation; apoptosis; therapy; prevention; molecular targets
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MDPI and ACS Style

Harish, V.; Haque, E.; Śmiech, M.; Taniguchi, H.; Jamieson, S.; Tewari, D.; Bishayee, A. Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets. Int. J. Mol. Sci. 2021, 22, 4478. https://doi.org/10.3390/ijms22094478

AMA Style

Harish V, Haque E, Śmiech M, Taniguchi H, Jamieson S, Tewari D, Bishayee A. Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets. International Journal of Molecular Sciences. 2021; 22(9):4478. https://doi.org/10.3390/ijms22094478

Chicago/Turabian Style

Harish, Vancha, Effi Haque, Magdalena Śmiech, Hiroaki Taniguchi, Sarah Jamieson, Devesh Tewari, and Anupam Bishayee. 2021. "Xanthohumol for Human Malignancies: Chemistry, Pharmacokinetics and Molecular Targets" International Journal of Molecular Sciences 22, no. 9: 4478. https://doi.org/10.3390/ijms22094478

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