Abstract
Minor prenylated hop compounds have been attracting increasing attention due to their promising anticarcinogenic properties. Even after intensive purification from natural raw extracts, allocating certain activities to single compounds or complex interactions of the main compound with remaining impurities in very low concentration is difficult. In this study, dose-dependent antiproliferative and cytotoxic effects of the promising xanthohumol (XN) analogue xanthohumol C (XNC) were evaluated and compared to XN and a XN-enriched hop extract (XF). It was demonstrated that the cell growth inhibition of human breast cancer cell line (MCF-7) significantly increases after being treated with XNC compared to XN and XF. Based on label-free data-dependent acquisition proteomics, physiological influences on the proteome of MCF-7 cells were analyzed. Different modes of action between XNC and XN treated MCF-7 cells could be postulated. XNC causes ER stress and seems to be involved in cell-cell adhesion, whereas XN influences cell cycles and DNA replication as well as type I interferon signaling pathway. The results demonstrate the utility of using quantitative proteomics for bioactivity screenings of minor hop compounds and underscore the importance of isolating highly pure compounds into their distinct forms to analyze their different and possibly synergistic activities and modes of action.
Highlights
Hop (Humulus lupulus L.) is well known as a medical plant with many bioactive effects
Protein expression in the MCF-7 cell line after XN and xanthohumol C (XNC) treatment was analyzed by label-free data-dependent acquisition proteomics and the results evaluated by various bioinformatics tools, such as Perseus, PANTHER, STRING, and GOrilla
XNC was evaluated for its antiproliferative and cytotoxic effects on breast cancer cells (MCF-7) and its activity is compared to the reference XN and the XN-enriched hop extract Xantho-Flav (XF) containing a high amount of XN (65–85%) as well as a huge variety of different minor hop compounds in very low concentrations
Summary
Hop (Humulus lupulus L.) is well known as a medical plant with many bioactive effects. Due to the trend of evaluating natural compounds for its diverse bioactive effects, hop has been attracting increasing interest as a natural resource for promising biologically active phenolic compounds. In this context, natural compounds have shown promise due to their antimicrobial, antiviral and anticarcinogenic or (chemo)preventive effects [1, 2]. Hop contains a huge variety of prenylated phenolic compounds [3,4,5,6]. The most abundant prenylated chalcone in hops is xanthohumol (XN) [7].
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