In vitro glucuronidation of xanthohumol, a flavonoid in hop and beer, by rat and human liver microsomes

Yilmazer, Meltem; Stevens, Jan F.; Buhler, Donald R.

doi:10.1016/s0014-5793(01)02210-4

Cited by 93 publications

(110 citation statements)

References 18 publications

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“…The bioavailability of xanthohumol has not yet been completely elucidated. Yilmazer et al reported the metabolism of xanthohumol using rat and human microsomes 29,30 .…”

Section: Discussionmentioning

confidence: 99%

Effects of Xanthohumol-rich Extract from the Hop on Fatty Acid Metabolism in Rats Fed a High-fat Diet

2014

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“…The bioavailability of xanthohumol has not yet been completely elucidated. Yilmazer et al reported the metabolism of xanthohumol using rat and human microsomes 29,30 .…”

Section: Discussionmentioning

confidence: 99%

Effects of Xanthohumol-rich Extract from the Hop on Fatty Acid Metabolism in Rats Fed a High-fat Diet

2014

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“…The major chalcone xanthohumol, as well as the flavanones isoxanthohumol, and 6PN and 8PN show various forms of antioxidant activity in vitro in the micromolar range, and are weakly cytotoxic to certain cancer cell lines (Gerhäuser et al, 2001a;Gerhäuser et al, 2001b;Milligan et al, 1999;Miranda et al, 2000a;Miranda et al, 2000b). In addition, the metabolism of prenylated chalcones and flavanones from hops in vitro and in vivo has been investigated (Nikolic, 2004;Nookandeh, 2004;Yilmazer, 2001aYilmazer, , 2001b.…”

Section: Other Activitiesmentioning

confidence: 99%

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

2006

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SummaryAs the population ages, there is an ever-increasing need for therapeutic agents that can be used safely and efficaciously to manage symptoms related to postmenopausal estrogen deficiency. Endogenous estrogens, e.g., 17β-estradiol, of exogenous mammalian origin, e.g., horses, have long been used to manage such symptoms. There are more than twenty different classes of phytochemicals that have demonstrated affinity for human estrogen receptors in vitro. Some studies on exogenous estrogenic substances of botanical origin ("phytoestrogens"), such as standardized formulations of plant extracts with in vitro and in vivo estrogenic activity from soy (Glycine max Merill.) and red clover (Trifolium pratense L.), suggest clinical efficacy. Few clinical data for phytoestrogens other than isoflavonoids are available. In an exhaustive review of the literature through 2003, only two clinical trials were identified that were designed to evaluate the effect of hops (Humulus lupulus L.) on symptoms related to manopause. Folkloric, chemical, and biological literature relating primarily to the use of hops for their estrogenic activity, and two human clinical trials, are reviewed.

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“…In contrast to many other chalcones, the metabolism of XN was extensively studied, and both in vitro and in vivo studies have been conducted (Hanske et al, 2010;Henderson et al, 2000;Yilmazer et al, 2001aYilmazer et al, , 2001b. These studies have revealed, that on the one hand XN is a potent inhibitor of P450 enzymes (Henderson et al, 2000), but on the other hand it is also heavily metabolized by liver cells (Hanske et al, 2010;Nikolic et al, 2005) and microorganisms (Kim and Lee, 2006;Nookandeh et al, 2004) into several other, prenylated and non-prenylated chalcones.…”

Section: Introductionmentioning

confidence: 99%

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

et al. 2015

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CitationIn vitro structure-toxicity relationship of chalcones in human hepatic stellate cells 2015 Toxicology This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. In vitro AbstractXanthohumol (XN), the major prenylated chalcone from hops (Humulus lupulus L.), has received much attention within the last years, due to its multiple pharmacological activities including anti-proliferative, anti-inflammatory, antioxidant, pro-apoptotic, anti-bacterial and anti-adhesive effects. However, there exists a huge number of metabolites and structurallyrelated chalcones, which can be expected, or are already known, to exhibit various effects on cells. We have therefore analyzed the effects of XN and 18 other chalcones in a panel, consisting of multiple cell-based assays. Readouts of these assays addressed distinct aspects of cell-toxicity, like proliferation, mitochondrial health, cell cycle and other cellular features. Besides known active structural elements of chalcones, like the Michael system, we have identified several moieties that seem to have an impact on specific effects and toxicity in human liver cells in vitro. Based on these observations, we present a structure-toxicity model, which will be crucial to understand the molecular mechanisms of wanted effects and unwanted side-effects of chalcones.

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In vitro glucuronidation of xanthohumol, a flavonoid in hop and beer, by rat and human liver microsomes

Cited by 93 publications

References 18 publications

Effects of Xanthohumol-rich Extract from the Hop on Fatty Acid Metabolism in Rats Fed a High-fat Diet

Effects of Xanthohumol-rich Extract from the Hop on Fatty Acid Metabolism in Rats Fed a High-fat Diet

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

In vitro structure-toxicity relationship of chalcones in human hepatic stellate cells

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