Abstract
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.
Highlights
Tremendous interest has emerged toward bioactive natural compounds owing to their pharmacological activities in various chronic diseases, such as neoplasms, neurological diseases, viral and bacterial infections, and many more
Chemo- and radiosensitizing experiments on MCF-7/ADR cells revealed that XH was able to attenuate MCF-7/ADR cell sensitivity to adriamycin therapies and radiation that inhibited the expression of epidermal growth factor receptor (EGFR), signal transducer and activator of transcription 3 (STAT3), and multidrug resistance mutation 1 (MDR1), known as ATP binding cassette subfamily B member 1 (ABCB1)
This review summarized recent progress on XH, that inhibits carcinogenesis and metastasis in many cancers
Summary
Tremendous interest has emerged toward bioactive natural compounds owing to their pharmacological activities in various chronic diseases, such as neoplasms, neurological diseases, viral and bacterial infections, and many more. Among different naturally-occurring compounds, hops, which are obtained from the inflorescence (female) of Humulus lupulus L. XH is written as 3 -[3, 3-dimethyl allyl]-2 ,4 ,4-trihydroxy-6 -methoxychalcone [11] The prenylated flavonoids, such as isoxanthohumol, 6-prenylnaringenin, and 8prenylnaringenin (8-PN), are isomers of XH, which have potent anti-inflammatory, antineoplastic, antidiabetic, estrogenic, antiviral, and antibacterial activities [12]. There is limited information available about the bioavailability and bioactivity of XH in humans, but preclinical studies on XH suggests that it has a cancer-preventive effect. In 1935, a voyage of archaeologists from the Pennsylvania University Museum and the American Schools of Oriental Science in Mesopotamia discovered a seal baked into pottery that depicted the contents of a brewery vat which was stirred with long poles by two brewery workers This instance was dated back to 3500–3100 BC [13]. Hops alcohol extracts have been utilized in Chinese medicine for pulmonary tuberculosis and acute bacterial dysentery treatment as well as in Ayurvedic therapies in India [28]
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