Xanthohumol is a hop-derived flavonoid that has been widely examined for its health-protecting and antitumorigenic properties, but not yet in a natural beer matrix. The aim of the study was to investigate the antitumorigenic potential of a xanthohumol-enriched beer in vivo. Four groups of 4 × 10 nude mice were formed. Following the injection of HeLa tumorigenic cell lines, the treatment groups were administered a xanthohumol supplementation for 100 days, either dissolved in beer or in an ethanolic solution with the same alcohol strength as beer. The control groups received un-supplemented material. The terminal tumor masses, liver weights, and plasma antioxidant capacities (FRAP and ABTS methods) were measured. For the statistical analysis, a two-way ANOVA test was performed (p < 0.05). There were no statistically significant differences in tumor size between the groups. Xanthohumol did not induce higher levels of plasma antioxidant capacity, neither in beer nor in the water-ethanol matrix. The terminal liver weights were significantly higher in the control group receiving the unsupplemented ethanol solution. Xanthohumol dissolved in beer or in the water-alcohol matrix did not have a protective effect on tumor growth, nor did it have a positive effect on plasma antioxidant capacity either. However, beer with added xanthohumol had a less harmful effect on the liver compared to the supplemented water-ethanol solution. Our results indicate the possible negative countereffect of ethanol; however, further investigations are needed.
- MeSH
- antioxidancia * farmakologie analýza MeSH
- ethanol analýza MeSH
- flavonoidy farmakologie analýza MeSH
- HeLa buňky MeSH
- lidé MeSH
- myši nahé MeSH
- myši MeSH
- pivo analýza MeSH
- propiofenony * farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Prenylflavonoids in the human organism exhibit various health-beneficial activities, although they may interfere with drugs via the modulation of the expression and/or activity of drug-metabolizing enzymes. As intestinal cells are exposed to the highest concentrations of prenylflavonoids, we decided to study the cytotoxicity and modulatory effects of the four main hop-derived prenylflavonoids on the activities and mRNA expression of the main drug-conjugating enzymes in human CaCo-2 cells. Proliferating CaCo-2 cells were used for these purposes as a model of colorectal cancer cells, and differentiated CaCo-2 cells were used as an enterocyte-like model. All the tested prenylflavonoids inhibited the CaCo-2 cells proliferation, with xanthohumol proving the most effective (IC50 8.5 μM). The prenylflavonoids modulated the activities and expressions of the studied enzymes to a greater extent in the differentiated, as opposed to the proliferating, CaCo-2 cells. In the differentiated cells, all the prenylflavonoids caused a marked increase in glutathione S-transferase and catechol-O-methyltransferase activities, while the activity of sulfotransferase was significantly inhibited. Moreover, the prenylflavonoids upregulated the mRNA expression of uridine diphosphate (UDP)-glucuronosyl transferase 1A6 and downregulated that of glutathione S-transferase 1A1/2.
- MeSH
- buněčná diferenciace účinky léků genetika MeSH
- Caco-2 buňky MeSH
- exprese genu účinky léků MeSH
- flavonoidy izolace a purifikace farmakologie MeSH
- glukuronosyltransferasa genetika metabolismus MeSH
- glutathiontransferasa genetika metabolismus MeSH
- Humulus chemie MeSH
- katechol-O-methyltransferasa genetika metabolismus MeSH
- lidé MeSH
- neopren izolace a purifikace farmakologie MeSH
- proliferace buněk účinky léků genetika MeSH
- propiofenony izolace a purifikace farmakologie MeSH
- sulfotransferasy genetika metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Beer, the most popular beverage containing hops, is also frequently consumed by cancer patients. Moreover, non-alcoholic beer, owing to its nutritional value and high content of biological active compounds, is sometimes recommended to patients by oncologists. However, the potential benefits and negatives have to date not been sufficiently evaluated. The present study was designed to examine the effects of four main hop-derived prenylflavonoids on the viability, reactive oxygen species (ROS) formation, activity of caspases, and efficiency of the chemotherapeutics 5-fluorouracil (5-FU), oxaliplatin (OxPt) and irinotecan (IRI) in colorectal cancer cell lines SW480, SW620 and CaCo-2. All the prenylflavonoids exerted substantial antiproliferative effects in all cell lines, with xanthohumol being the most effective (IC50 ranging from 3.6 to 7.3 μM). Isoxanthohumol increased ROS formation and the activity of caspases-3/7, but 6-prenylnaringenin and 8-prenylnaringenin exerted antioxidant properties. As 6-prenylnaringenin acted synergistically with IRI, its potential in combination therapy deserves further study. However, other prenylflavonoids acted antagonistically with all chemotherapeutics at least in one cell line. Therefore, consumption of beer during chemotherapy with 5-FU, OxPt and IRI should be avoided, as the prenylflavonoids in beer could decrease the efficacy of the treatment.
- MeSH
- antioxidancia MeSH
- Caco-2 buňky MeSH
- fixní kombinace léků MeSH
- flavanony farmakologie terapeutické užití MeSH
- flavonoidy farmakologie terapeutické užití MeSH
- fluoruracil terapeutické užití MeSH
- fytogenní protinádorové látky farmakologie terapeutické užití MeSH
- Humulus chemie MeSH
- irinotekan terapeutické užití MeSH
- kaspasy metabolismus MeSH
- kolorektální nádory farmakoterapie metabolismus MeSH
- lékové interakce * MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- oxaliplatin terapeutické užití MeSH
- pivo * škodlivé účinky MeSH
- propiofenony farmakologie terapeutické užití MeSH
- protinádorové látky farmakologie terapeutické užití MeSH
- reaktivní formy kyslíku metabolismus MeSH
- rostlinné extrakty farmakologie terapeutické užití MeSH
- stravovací zvyklosti MeSH
- výsledek terapie MeSH
- xantony farmakologie terapeutické užití MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Bacterial biofilms pose a serious medical problem due to their significant resistance to antimicrobials, and staphylococci are recognized as the most frequent cause of biofilm-associated infections. The hop plant (Humulus lupulus L.) contains substances that have been determined to act as anti-infective agents against bacteria, mainly in planktonic form. Therefore, we decided to investigate the antibiofilm properties of H. lupulus L.-derived compounds (humulone, lupulone and xanthohumol) against a selected group of Staphylococcus spp., including methicillin-susceptible and resistant strains. All tested hop compounds were shown to possess antimicrobial properties against all tested staphylococci, both planktonic and biofilm-dwelling, with no significant difference between resistant and susceptible strains. All compounds lowered the number of bacterial cells released from the biofilm, with the strongest effect seen for lupulone, followed by xanthohumol. Moreover, lupulone and xanthohumol were not only able to penetrate the biofilm and reduce the number of bacteria within it, but their higher concentrations (∼60 μg/mL for xanthohumol and ∼125 μg/mL for lupulone) reduced the number of surviving bacterial cells to zero.
- MeSH
- antibakteriální látky farmakologie MeSH
- biofilmy účinky léků MeSH
- buněčné linie MeSH
- cyklohexeny farmakologie MeSH
- flavonoidy farmakologie MeSH
- Humulus chemie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- propiofenony farmakologie MeSH
- rostlinné extrakty farmakologie MeSH
- Staphylococcus účinky léků genetika růst a vývoj MeSH
- terpeny farmakologie MeSH
- viabilita buněk účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Historically, hop cones (Humulus lupulus) have been used since ancient times as a remedy for many ailments and, as a source of polyphenols and bitter acids, is very effective in the treatment of metabolic syndrome (MS). Hop flavonoids, particularly xanthohumol (XN), are substances with hypoglycemic, antihyperlipidemic, and antiobesity activities. Iso-α-acids (IAA) and matured hop bitter acids (MHBA) improve health by influencing lipid metabolism, glucose tolerance, and body weight. The modulatory effect of IAA and MHBA on lipid metabolism may also be responsible for a loss in body weight. These results suggest promising applications for IAA, MHBA, and XN in humans, particularly in the prevention of diet-induced obesity and diabetes.
- MeSH
- flavonoidy chemie farmakologie terapeutické užití MeSH
- fytonutrienty chemie farmakologie terapeutické užití MeSH
- glukózový toleranční test MeSH
- Humulus chemie MeSH
- lidé MeSH
- metabolický syndrom farmakoterapie prevence a kontrola MeSH
- metabolismus lipidů účinky léků MeSH
- molekulární struktura MeSH
- propiofenony farmakologie terapeutické užití MeSH
- tělesná hmotnost účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Anaerobic bacteria, such as Bacteroides fragilis or Clostridium perfringens, are part of indigenous human flora. However, Clostridium difficile represents also an important causative agent of nosocomial infectious antibiotic-associated diarrhoea. Treatment of C. difficile infection is problematic, making it imperative to search for new compounds with antimicrobial properties. Hops (Humulus lupulus L.) contain substances with antibacterial properties. We tested antimicrobial activity of purified hop constituents humulone, lupulone and xanthohumol against anaerobic bacteria. The antimicrobial activity was established against B. fragilis, C. perfringens and C. difficile strains according to standard testing protocols (CLSI, EUCAST), and the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBC) were calculated. All C. difficile strains were toxigenic and clinically relevant, as they were isolated from patients with diarrhoea. Strongest antimicrobial effects were observed with xanthohumol showing MIC and MBC values of 15-107 μg/mL, which are close to those of conventional antibiotics in the strains of bacteria with increased resistance. Slightly higher MIC and MBC values were obtained with lupulone followed by higher values of humulone. Our study, thus, shows a potential of purified hop compounds, especially xanthohumol, as alternatives for treatment of infections caused by select anaerobic bacteria, namely nosocomial diarrhoea caused by resistant strains.
- MeSH
- anaerobióza fyziologie MeSH
- antibakteriální látky izolace a purifikace farmakologie MeSH
- Bacteroides fragilis účinky léků růst a vývoj MeSH
- Clostridioides difficile účinky léků růst a vývoj patogenita MeSH
- Clostridium perfringens účinky léků růst a vývoj MeSH
- cyklohexeny izolace a purifikace farmakologie MeSH
- flavonoidy izolace a purifikace farmakologie MeSH
- Humulus chemie MeSH
- infekce spojené se zdravotní péčí mikrobiologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- propiofenony izolace a purifikace farmakologie MeSH
- průjem mikrobiologie MeSH
- pseudomembranózní enterokolitida mikrobiologie MeSH
- rostlinné extrakty chemie MeSH
- symbióza fyziologie MeSH
- terpeny izolace a purifikace farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- MeSH
- beta-aminoethylisothiomočovina farmakologie MeSH
- buněčné dělení MeSH
- buňky kostní dřeně MeSH
- chemická deprese MeSH
- cystamin farmakologie MeSH
- dinitrofenoly farmakologie MeSH
- experimentální radiační poranění farmakoterapie MeSH
- fluoracetáty farmakologie MeSH
- hematopoetický systém účinky léků MeSH
- kostní dřeň účinky léků MeSH
- kyslík metabolismus MeSH
- myši MeSH
- propiofenony farmakologie MeSH
- radioprotektivní látky farmakologie MeSH
- serotonin farmakologie MeSH
- slezina cytologie metabolismus MeSH
- transplantace kostní dřeně MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
