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.

• Klíčová slova
• 5-fluorouracil, caspase activity, colorectal carcinoma cells, irinotecan, isoxanthohumol, naringenin, oxaliplatin, prenylflavonoids,
• 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
• Názvy látek
• 6-prenylnaringenin MeSH Prohlížeč
• 8-prenylnaringenin MeSH Prohlížeč
• antioxidancia MeSH
• fixní kombinace léků MeSH
• flavanony MeSH
• flavonoidy MeSH
• fluoruracil MeSH
• fytogenní protinádorové látky MeSH
• irinotekan MeSH
• isoxanthohumol MeSH Prohlížeč
• kaspasy MeSH
• oxaliplatin MeSH
• propiofenony MeSH
• protinádorové látky MeSH
• reaktivní formy kyslíku MeSH
• rostlinné extrakty MeSH
• xanthohumol MeSH Prohlížeč
• xantony MeSH

Membrane organic anion-transporting polypeptides (OATPs) are responsible for the drug transmembrane transport within the human body. The function of OATP2B1 transporter can be inhibited by various natural compounds. Despite increased research interest in soya as a part of human diet, the effect of its active components to interact with hOATP2B1 has not been elucidated in a complex extent. This in vitro study examined the inhibitory effect of main soy isoflavones (daidzin, daidzein, genistin, genistein, glycitin, glycitein, biochanin A, formononetin) and their metabolites formed in vivo (S-equol, O-desmethylangolensin) towards human OATP2B1 transporter. MDCKII cells overexpressing hOATP2B1 were employed to determine quantitative inhibitory parameters of the tested compounds and to analyze mechanism/s of the inhibitory interaction. The study showed that aglycones of soy isoflavones and the main biologically active metabolite S-equol were able to significantly inhibit hOATP2B1-mediated transport. The Ki values for most of aglycones range from 1 to 20 μM. In contrast, glucosides did not exhibit significant inhibitory effect. The kinetic analysis did not indicate a uniform type of inhibition towards the hOATP2B1 although predominant mechanism of inhibition seemed to be competitive. These findings may suggest that tested soy isoflavones and their metabolites might affect transport of xenobiotics including drugs across tissue barriers via hOATP2B1.

• Klíčová slova
• Drug transporter, Flavonoids, OATP, SLCO, Soy isoflavones,
• MeSH
• buňky MDCK MeSH
• Glycine max * MeSH
• isoflavony farmakologie   MeSH
• kinetika MeSH
• přenašeče organických aniontů antagonisté a inhibitory   genetika   metabolismus   MeSH
• psi MeSH
• transfekce MeSH
• zvířata MeSH
• Check Tag
• psi MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• isoflavony MeSH
• přenašeče organických aniontů MeSH
• SLCO2B1 protein, human MeSH Prohlížeč

Public interest in natural therapies has increased significantly over past decades. Herbs and herbal products are extensively consumed worldwide and they are generally considered as safe. However, this may not always be true as many cases of herb-induced liver injury are reported every year. The liver is a frequent target tissue of toxicity from all classes of toxicants as liver structure and function predispose it to high sensitivity to xenobiotics. The present review is focused on the hepatotoxic properties of monoterpenes and sesquiterpenes, plant secondary metabolites that represent the major components of essential oils wildly used in folk medicines, pharmaceutical industry and cosmetics. Most of these terpenes easily enter the human body by oral absorption, penetration through the skin, or inhalation leading to measurable blood concentrations. Several studies showed that some monoterpenes (e.g., pulegone, menthofuran, camphor, and limonene) and sesquiterpenes (e.g., zederone, germacrone) exhibited liver toxicity, which is mainly based on reactive metabolites formation, increased concentration of reactive oxygen species and impaired antioxidant defense. There is a high probability that many other terpenes, without sufficiently known metabolism and effects in human liver, could also exert hepatotoxicity. Especially terpenes, that are important components of essential oils with proved hepatotoxicity, should deserve more attention. Intensive research in terpenes metabolism and toxicity represent the only way to reduce the risk of liver injury induced by essential oils and other terpenes-containing products.

• Klíčová slova
• Essential oil, Herb-induced liver injury, Oxidative stress, Reactive metabolites, Terpenes,
• MeSH
• játra účinky léků   metabolismus   MeSH
• lékové postižení jater etiologie   MeSH
• lidé MeSH
• monoterpeny chemie   toxicita   MeSH
• oleje prchavé chemie   toxicita   MeSH
• reaktivní formy kyslíku metabolismus   MeSH
• rostliny chemie   metabolismus   MeSH
• seskviterpeny chemie   toxicita   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• monoterpeny MeSH
• oleje prchavé MeSH
• reaktivní formy kyslíku MeSH
• seskviterpeny MeSH