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Scientific Name:
Humulus lupulus
Family Name:
Common Name:
hop, hops
Evidence of Activity
Xanthohumol inhibited proliferation, migration, and invasion of non-small cell lung cancer cells in vitro via inhibition of T-lymphokine-activated killer cell-originated protein kinase (TOPK). Zhao 2023
Humulus lupulus bioactive compounds exhibited antiviral properties against Chikungunya virus, with the strongest virucidal activity presented by the β-acids fraction. Mandova 2023
Xanthohumol demonstrated antimicrobial activity against multi-species biofilm, including Streptococcus oralis, Actinomyces naeslundii, Veillonella parvula, Fusobacterium nucleatum, Porphyromonas gingivalis, and Aggregatibacter actinomycetemcomitans, formed over dental implants in vitro. Alonso-Español 2023
Xanthohumol attenuated biochemical and histopathological responses, reduced necrosis, inflammation, oxidative stress, and autophagy impairment partially via inhibition of AKT/mTOR in models of severe acute pancreatitis. Huangfu 2023
Xanthohumol improved the viability of human kidney cells under high-glucose conditions, inhibited the oxidative stress, and significantly decreased serum creatinine, blood urea nitrogen, urea protein, and kidney weight/body weight ratio in a mouse model of diabetic nephropathy. Li 2023
Antiprotozoal activity of a hops extract is reported in this study. Cheremnykh 2022
Fractions of hop (Humulus lupulus) extracts containing xanthohumol and α- and β-acids showed antimicrobial activiy against Staphylococcus aureus. Kolenc 2022
Xanthohumol suppressed TGF-β1-induced expression of fibrosis-associated genes in human intestinal fibroblasts, mainly by affecting TGF-β/Smad and NF-κB signaling, in vitro. Yun 2022
Xanthohumol derivatives exhibited rapid bactericidal activity against methicillin-resistant Staphylococcus aureus (MRSA) in vitro and in vivo. Cheng 2022
A study aiming to provide comparative analysis of efficacy of xanthohumol vs. currently available anticancer drugs found that the hop compound showed significant binding affinity to several major targets of anti-breast cancer therapy, including HER2, with only a single violation of Lipinski's rule of five. Gupta 2022
Extracts of brewers' spent hops with high levels of cis-iso-α-cohumulone and 8-prenylnaringenin showed anti-elastase activity, thus demonstrating a potential for use in novel cosmetic products. Paredes-Ramos 2022
A spent hops (Humulus lupulus) extract inhibited the invasion (by up to 98.5%) and migration (99%) capacities of colorectal adenocarcinoma SW-480 and HT-29 cells, and demonstrated anti-angiogenic potential, in vitro. Caban 2022
Xanthohumol induced apoptosis of hepatocellular carcinoma HepG2 cells at micromolar concentrations without affecting the viability of primary rat hepatocytes, in vitro. Zhang 2022
Xanthohumol and nobiletin pretreatment inhibited the effects of TNF-α on human endothelial cell migration and invasion capabilities, suggesting anti-angiogenic properties, in vitro. Corrado 2022
A study evaluated the potential of hop (varieties Cascade, Saaz, Tettnang, and Summit) against Alzheimer's disease by testing their ability to hinder aggregation and cytotoxicity of amyloid β peptide and to enhance autophagy in a human neuroblastoma cell line, as well as in a transgenic Caenorhabditis elegans model. Palmioli 2022
Xanthohumol exhibited an anti-inflammatory effect by decreasing mechanical compression-induced IL-6 levels in a model of early-phase orthodontic tooth movement, concentration-dependently increasing (at 0.2 and 0.8 µM) or decreasing (4-8 µM) the viability of cementoblasts. Niederau 2022
Ethanolic and hydroethanolic hop extracts obtained by way of ultrasound- or microwave-assisted extraction showed varying levels of cytotoxic activities and, at the highest concentrations tested, pro-oxidant or antioxidant effects correlating with differences in the constituent profile. Ramazzina 2022
Combinations of hop flavonoids 8-, 6-prenylnaringenin, and xanthohumol with statin drugs (simvastatin or mevastatin) inhibited the activity of Kv1.3 channels, viability, and induced apoptosis in human T cell leukemia cells more potently than individual agents. Teisseyre 2022
Dilutions of hop extracts with α-acid concentrations similar to those found in commercial beer significantly inhibited Streptococcus mutans biofilm formation, suggesting beneficial effects on dental caries. Gregory 2022
Xanthohumol markedly decreased glutamine uptake in breast cancer cells, known for 'glutamine addiction,' while exhibiting a cytotoxic and anti-proliferative effect. Carmo 2022
A computational study identified protein targets of xanthohumol and its metabolites isoxanthohumol and 6- and 8-prenylnaringenin associated with their anticarcinogenic properties, notably including matrix metalloproteinases MMP-2 and MMP-9, as well as acyl-protein thioesterase 2. Kores 2022
Xanthohumol pretreatment protected osteoblasts from amyloid β-protein induced injury, reducing apoptosis rates and improving cellular proliferation, differentiation, and mineralization, associated with PI3K/AKT/Nrf2 pathway activity. Xia 2022
Extracts of three different cultivars (Columbus, Chinook, and Hallertau Mittelfrüh) of hops (Humulus lupulus) inhibited LPS-induced prostaglandin E2 production by 73.5%-92.5%, in vitro, correlating with the levels of prenylated phloroglucinol and phenolic homologs. Nicácio 2022
Xanthohumol induced cell cycle arrest and apoptosis in nasopharyngeal carcinoma cells in vitro. Hsieh 2022
Xanthohumol inhibited cardiomyocyte ferroptosis by decreasing lipid peroxidation and iron chelation, and altering NRF2 and glutathione peroxidase 4 protein levels in ischemia/reperfusion cardiac injury models in vitro and ex vivo. Lin 2022
Xanthohumol accelerated diabetic wound healing, and protected cells from oxidative stress, apoptosis, and high glucose-induced cell damage, associated with activation of the expression and nuclear translocation of the transcription factor Nrf2, in vitro and in vivo. Lu 2022
Retinal ganglion cell protection by hop-flower extract as a novel neuroprotective strategy for glaucoma [No abstract] Hasegawa 2022
A hop extract showed antifibrotic properties by inhibiting fibronectin 1, collagen type I alpha 1, versican, and the profibrotic growth factor activin A/inhibin beta A subunit in primary leiomyoma cells from women with symptomatic uterine fibroids. Islam 2021
A study reports on the positive effects of the hop (H. lupulus) constituent 8-prenylnaringenin on neurogenesis and neurodifferentiation along with the inhibitory activity against human monoacylglycerol lipase, an enzyme that metabolizes the endocannabinoid 2-arachidonoglycerol and participates in neuroinflammation associated with Alzheimer's and Parkinson's diseases. Tung 2021
Hops (Humulus lupulus) extract and its constituent 6-prenylnaringenin showed estrogenic activity by activating both the estrogen receptor α signaling pathway and genes involved in estrogen metabolism (CYP1A1, CYP1B1), as well as the aryl hydrocarbon receptor pathway, in human cells in vitro. Zanardi 2021
A mixture of Saaz-Saphir hops, administered orally for 3 weeks, increased sleep time, as well as the γ-amino butyric acid (GABA) brain content and the expression of the GABA(A) receptor, in a caffeine-induced model of insomnia. Min 2021
A low dose of xanthohumol suppressed the metabolism and pro-inflammatory gene expression in primary colon cancer cells. Torrens-Mas 2021
A specific fraction, obtained from Humulus lupulus by liquid chromatography-based fractionation, inhibited the production of inflammatory cytokines such as IL-6, IL-1α, IL-1β, and TNF by dendritic cells, via a molecular mechanism different from quercetin. Sommella 2021
Xanthohumol showed pan-inhibitory activity against different coronaviruses. including the SARS-CoV-2 betacoronavirus and PEDV alphacoronavirus, via inhibition of the viral main proteases, and restricted the SARS-CoV-2 and PEDV replication in Vero-E6 cells. Lin 2021
Xanthohumol inhibited SARS-CoV-2 infection of human pluripotent stem cell-derived airway organoids, associated with inhibition of fatty acid biosynthesis. Duan 2021
In a comparative study of five flavonoids, xanthohumol showed the best antitumor activity against colorectal cancer cell lines, performing even better than the chemotherapeutic drug 5-fluorouracil, with no synergistic effects. Fernández 2021
Xanthohumol prevented extracellular matrix degradation by reversing the expression of matrix metalloproteinase 13 in osteoarthritic chondrocytes model of osteoarthritis, in vitro. Zheng 2021
Isoxanthohumol and lupulone, isolated from the hop plant (Humulus lupulus), noncompetitively inhibited α-glucosidase via direct binding. Wang 2021
An in-silico investigation of the potential of medicinal plant constituents for the interaction with four SARS-CoV-2 protein drug targets (including S protein, 3CLpro, RdRp, and N protein) identified Humulus lupulus compounds among those with the highest affinity to the viral proteins. Mahmoudi 2021
Prenylflavonoids extracted from Humulus lupulus, alone and synergistically with 5-fluorouracil and oxaliplatin chemotherapy, suppressed the clonogenic potential of colorectal cancer stem cells and affected the metastatic spread in colorectal cancer patients. Turdo 2021
Xanthohumol decreased DNA damage by aflatoxin B1 in cultured HepG2 cells. Štern 2021
Xanthohumol inhibited the metastatic potential of human lung cancer cells by suppressing the expression of MMP-9, VEGF, TGF-β, and mesenchymal markers N-cadherin, vimentin, and Snail-1, and increasing the expression of TIMP-1, E-cadherin, and α-E-catenin. Sławińska-Brych
Hops (Humulus lupulus) constituents xanthohumol, 8-prenylnaringenin, and iso-xanthohumol induced cumulative-to-slightly synergistic estrogenic effects on human endometrial cells at low nanomolar concentrations, activity that may also occur after the consumption of strongly hopped beer. Aichinger 2021
Hops (Humulus lupulus) extracts and xanthohumol modulated adenosine receptors in neural cell models; however, xanthohumol did not reverse effects of oxidative stress in cells. Alonso 2021
Xanthohumol and its synthetic derivative tetrahydroxanthohumol, inhibited adipocytes differentiation, decreasing the expression of lipogenesis-related genes, and was shown by molecular docking studies to bind to the PPARγ ligand-binding domain pocket, consistent with its action as a PPARγ antagonist. Zhang 2021
Xanthohumol significantly attenuated inflammatory responses and extracellular matrix degradation by modulating HO-1 signaling and the C/EBPβ signaling pathway in osteoarthritic chondrocytes. Zhang 2021
Xanthohumol time- and dose dependently inhibited proliferation and death, and induced apoptosis, of rat glioma cells, effects associated with the apoptosis-inducing factor and mitochondial activity. Hou 2021
A crude extract from Humulus lupulus 'Marynka' Polish hop variety showed higher antibacterial and anticancer cell activities in comparison with xanthohumol. Klimek 2021
An ex vivo investigation of 10 medicinal plant extracts found Humulus lupulus (hops) to exhibit the most promising anti-proliferative and anti-inflammatory effects in psoriasis, actvivity associated with inhibition of anti-microbial peptides (β-defensin 2), the hyperproliferation marker keratin 17, and glucose transporter 1, along with downregulation of the nuclear translocation of NF-κB and pSTAT3. Gendrisch 2021
An evaluation of 17 fortified plant extracts using planar effect-directed assays reported a "comparatively high" level of antimicrobial activity in hops (Humulus lupulus). . Morlock 2021
Cinnamon and Hop Extracts as Potential Immunomodulators for Severe COVID-19 Cases. [No abstract] Lucas 2021
Xanthohumol inhibited melanin synthesis in human melanoma cells and increased intracellular tyrosinase activity without affecting ROS levels; in normal human melanocytes from darkly-pigmented skin, it suppressed cellular tyrosinase activity at nontoxic concentrations without affecting melanin synthesis. Goenka 2021
Xanthohumol, a flavonoid from hops, induced necrotic cell death in prostate and breast cancer cells, in vitro. Gieroba 2020
Humulone (an alpha acid) and 6-prenylnaringenin (a prenylflavonoid), both found in Humulus lupulus, exhibited a modulatory activity at GABA(A) receptors, at low micromolar concentrations. Benkherouf 2020
A structural bioinformatics approach uncovered the binding mechanism of hop (Humulus lupulus) constituents to bitter taste receptors. Dunkel 2020
Xanthohumol dramatically decreased the viability of human colon carcinoma cells in vitro. Liu 2019
Xanthohumol protected primary cortical neurons and astrocytes from corticosterone-induced toxicity, in vitro, in a Nrf2-dependent manner. Donoso 2019
Virtual screening of over 2300 compounds derived from common medicinal herbs and spices found hops to be particularly enriched in compounds possessing potential anti-diabetic activity. Pereira 2019
A study found xanthohumol to inhibit tau protein aggregation and disaggregate tau fibrils, as well as directly interact with the protein at specific sites. Zhang 2019
Xanthohumol induced acute lytic cell death (characterized by cell swelling and rupture) in human leukemia HL-60 cells, which could be alleviated by N-acetyl-cysteine or the addition of 2% serum. Wang 2019
Xanthohumol inhibited the growth of colorectal cancer cells in vitro and in vivo. Liu 2019
Xanthohumol suppressed the proliferation and induced cell cycle arrest and apoptosis in human chronic myelogenous leukemia cells, via inhibition of autophagy, enhancing the potential efficacy of imatinib, in vitro. Lu 2019
Xanthohumol inhibited cholesterol uptake (by up to approximately 32%) by human intestinal epithelial cells, in vitro, by suppressing the levels of Niemann-Pick C1-like 1 (NPC1L1), an essential cholesterol transport protein. Thang 2019
A hop-derived prenylflavonoid, ENDF1, very potently induced regrowth of rat dorsal root ganglion neurons in vitro, strongly enhancing the total neurite length and complexity, in a model of degenerative central nervous system diseases. Bieler 2019
Xanthohumol induced apoptosis in multiple myeloma cell lines in vitro. Slawinska-Brych 2019
Xanthohumol inhibited the proliferation of B16-F10 murine melanoma cells in vitro. Zhang 2019
8-Prenylnaringenin, found in hops and beer, inhibited the proliferation and induced apoptosis in human colon cancer cells in vitro. Koosha 2019
Beer raw materials and by-products (including hop pellets and spent hops) showed anti-thrombotic activities, total beer polar lipid extract being the strongest, suggesting synergistic interaction of the components as well as the influence of fermentation. Lordan 2019
Xanthohumol and its non-estrogenic derivatives dihydroxanthohumol and tetrahydroxanthohumol inhibited the proliferation of colon and hepatocellular carcinoma cell lines in vitro. Logan 2019
Phenolic constituents of hops (H. lupulus) potently inhibited methicillin-resistant Staphylococcus aureus (MRSA) strains, and showed antiparasitic activity against Trypanosoma brucei, in vitro. Bocquet 2019
Prenylflavonoids from hops xanthohumol, isoxanthohumol and 8-prenylnaringenin modified GABA(A) receptors in vitro. Benkherouf 2019
A novel heteropolysaccharide obtained from female flowers of Humulus lupulus promoted the differentiation, proliferation, and mineralization of osteoblast precursor cells from mice, more effectively than 17β-estradiol, suggesting benefits for osteoporosis. Chen 2019
A CO₂ hop extract (50% humulone and lupulone) suppressed the growth of Propionibacterium acnes (MIC, 3.1 µg/mL) and Staphylococcus aureus (MIC, 9.4 µg/mL) and reduced interleukin-6 expression (IC50: 0.8 µg/mL), as well as possessing antioxidative activity. Weber 2019
n-Humulone, adhumulone, and cohumulone (from Humulus lupulus) inhibited aldo-keto-reductase 1B10, which is known to promote carcinogenesis, in vitro. Seliger 2018
Xanthohumol decreased the viability of colon cancer cells in vitro. Sastre-Serra 2018
6- and 8-prenylnaringenin, found in hops, decreased the proliferation and viability of melanoma cells in vitro. Venturelli 2018
Xanthohumol exhibited higher antiproliferative activity than cisplatin against five cancer (ovarian, breast, prostate and colon) cell lines, whereas other hop compounds isoxanthohumol and 6-prenylnaringenin exhibited similar activities against breast cancer cell line. Bartmańska 2018
Ethanolic extracts of Humulus lupulus cones showed some of the highest levels of anti-inflammatory potential in a screening of 99 herbal extracts for their effects on TLR2 and TLR4 signaling pathways, in vitro. Schink 2018
Xanthohumol induced apoptosis and suppressed migration of gastric cancer cells, with no toxicity to normal gastric epithelial cells, in vitro. Wei 2018
Xanthohumol inhibited the proliferation and induced apoptosis in human papillary thyroid cancer cells. Carvalho 2018
The prenylated flavonoid-6-prenylnaringenin (found in hops) was much more effective in inhibiting voltage-gated Kv1.3 potassium channels than non-prenylated flavonoids chrysin, baicalein, and luteolin, among others. Teisseyre 2018
A hydroalcoholic extract of the female inflorescences of Humulus lupulus (hops) significantly inhibited replication of various (influenza) viral strains, at different times pre- or post-infection, partly via antioxidant effects. Di Sotto 2018
Spent hop extracts and hop flavonoids α,β-dihydroxanthohumol and 8-prenylnaringenin showed significant activity against methicillin-sensitive and resistant Staphylococcus aureus and S. epidermidis strains with the lowest MIC80 value of 0.5 µg/mL. Bartmańska 2018
Xanthohumol induced apoptosis in human gastric cancer cells in vitro. Guo 2018
Xanthohumol induced "beiging" of white adipocytes, lypolysis, and inhibited adipogenesis in differentiated mouse adipocytes and primary human subcutaneous preadipocytes, in vitro. Samuels 2018
Essential oil fractions from hops (H. lupulus) showed antimicrobial effects on Gram-negative bacteria Escherichia coli, Yersinia enterocolitica; Gram-positive Clostridium perfringens, Enterococcus faecalis, Staphylococcus aureus subs. aureus; as well as against Trypanosoma brucei. Jeliazkova 2018
Isoxanthohumol suppressed the activity of sterol regulatory element-binding proteins (transcription factors regulating fatty acid and cholesterol synthesis), via enhanced ubiquitin-proteasome-dependent degradation. Inoue 2018
Hop (Humulus lupulus) fractions, including α-bitter acids (humulones), β-bitter acids (lupulones), and xanthohumol, showed effectiveness against Gram-positive multidrug-resistant bacteria, but no effects against Gram-negative bacteria, xanthohumol being the most potent compound. Bogdanova 2018
Xanthohumol inhibited invasiveness of glioma cells via suppression of Stim1, associated with malignancy and poor survival in glioma patients. Ho 2018
Xanthohumol inhibited the accumulation of amyloid-β in a cellular model of Alzheimer's disease. Huang 2018
Xanthohumol, 3-hydroxy-xanthohumol, and 8-prenylnaringenin, isolated from hops (H. lupulus), were comparable to the model drug galanthamine [sic] in their inhibitory effects on acetylcholinesterase and butyrylcholinesterase, the key enzymes in the pathology of Alzheimer's disease. Orhan 2018
Minor hops prenylflavonoids (e.g., xanthohumol C, 1″,2″-dihydroxanthohumol K) exhibited anti-cancer activity comparable to cisplatin in vitro. Popłoński 2018
Xanthohumol, isoxanthohumol, and 8-prenylnaringenin were found to be potent, uncompetitive, tight-binding inhibitors of human aldo-keto reductases 1B1 and 1B10. Seliger 2018
Xanthohumol ameliorated the toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin (an environmental contaminant) to osteoblasts, in vitro. Suh 2018
Beta-bitter acids of hops (lupulones) induced Ca2+ influx across the plasma membrane in PC12 cells to the same extent as hyperforin, suggesting their involvement in the antidepressant activity of hops. Schulz 2018
Hop (H. lupulus) compounds (humulone, lupulone and xanthohumol) inhibited the growth of staphylococci (planktonic and biofilm-forming), the strongest effect seen for lupulone, followed by xanthohumol. Bogdanova 2018
Allulose-induced secretion of glucalon-like peptide 1 (GLP-1) was abolished in the presence of xanthohumol (a glucose/fructose transport inhibitor). Hayakawa 2018
Xanthohumol induced BDNF-VI mRNA expression in human neuronal cells in an in vitro model of corticosterone-induced stress. Gite 2018
Xanthohumol was found to act as an uncompetitive inhibitor of arachidonic acid (ARA) uptake in human first-trimester extravillous trophoblast cells, in vitro. In the reverse, high extracellular ARA prevented the deleterious effects of xanthohumol on the cells. Correia-Branco 2017
Prenylnaringenin, which can also be formed during wort boiling from the inactive hop flavonoid desmethylxanthohumol, was identified as the only estrogen active compound in hops. Schick 2017
Estrogenic activity of food supplements and beers of different brands, obtained in Helsinki, Finland, was evaluated using a yeast assay, with all the supplements and 81% of the beers found to be estrogenic. Omoruyi 2017
Humulus lupulus constituents humulone, lupulone and especially xanthohumol showed antimicrobial effects against anaerobic bacteria associated with diarrhea in hospital patients, at concentrations similar to conventional antibiotics. Cermak 2017
Xanthohumol protected osteoblast cells from methylglyoxal-induced toxicity, via sirtuin 1 activation, suggesting benefits in the prevention of diabetic osteopathy. Suh 2017
Xanthohumol (10-20 μM) increased cell-surface expression of low-density lipoprotein receptor in hepatic cells, and enhanced the LDL uptake activity, via interaction with liver X receptor (LXR) α ligand-binding domain. Synergistic interactions with simvastatin are also reported. Chen 2017
Xanthohumol showed the highest inhibition of cyclooxygenases (COX-1 and COX-2) activities, compared to other synthetic prenylated flavonoids, as well as the highest binding affinity toward human serum albumin. Tronina 2017
Xanthohumol (10 μg/mL) promoted neurite outgrowth and extracellular release of nerve growth factor (NGF), in neural cells, in vitro. Phan 2017
Xanthohumol induced paraptosis, characterized by dilation of the endoplasmic reticulum and/or mitochondria, in leukemia cells, in vitro. Mi 2017
Naringenin and 8-prenylnaringenin (the latter obtained from isoxanthohumol by O-demethylation) exhibited high selectivity for cancer cells, compared with normal cells, and showed promise for the treatment of gliomas, in vitro. Stompor 2017
Hop compounds 6- and 8-prenylnaringenin (but not xanthohumol and isoxanthohumol) prevented the disruption of the human intestinal epithelial cell layer integrity induced by TNF-α, while only the second compound reversed the dysfunction, in a Caco-2 cell model in vitro. Luescher 2017
The anti-tumor activity of xanthohumol, associated with inhibition of the valosin-containing protein, was further augmented by inhibition of the adenylate cyclase pathway in several human cancer cell lines in vitro and in vivo. Shikata 2017
The potential of xanthohumol to bind to human transcription factors (putative anti-cancer drug targets) was investigated through computer aided molecular docking predictions. Teimouri 2016
Xanthohumol (40 µM) inhibited the proliferation of, and induced apoptosis in laryngeal squamous cell carcinoma SCC4 cells, in vitro. Li 2016
Xanthohumol inhibited the viability and induced apoptosis in doxorubicin-resistant human breast cancer cells and suppressed stem cell-like properties of the cells (such as sphere formation and migration capacity), in vitro. Liu 2016
Effects of hops derived prenylflavonoids on TNF-α induced barrier dysfunction in intestinal epithelial cells. [No abstract] Luescher 2016
Antimicrobial properties of phenolic compounds from hops, Humulus lupulus L.: fight against multidrug resistance. [No abstract] Bocquet 2016
Xanthohumol showed antileishmanial activity against Leishmania amazonensis and L. tarentolae via inhibition of the mitochondrial electron transfer complex II/III, while showing little or no toxicity to macrophages, in vitro. Monzote 2016
Xanthohumol (1.5-6 μg/ml) attenuated ADP-induced blood platelet aggregation and reduced the expression of fibrinogen receptor on the surface of platelets, in vitro. Luzak 2016
Xanthohumol showed antiarrhythmic potential by stabilizing ryanodine receptor calcium(2+) channels in rat ventricular myocytes in vitro. Arnaiz-Cot 2016
Molecular interactions of hop prenylflavonoids (xanthohumol, isoxanthohumol, and 8-prenylnaringenin) with the farnesoid X receptor were studied using hydrogen deuterium exchange mass spectrometry (HDX-MS) and in silico modeling. Yang 2016
Interactions of prenylflavonoids from Humulus lupulus (xanthohumol, isoxanthohumol, and 8-prenylnaringenin) with the farnesoid X receptor, a nuclear receptor important in lipid metabolic disorders, were elucidated. Yang 2016
The anti-angiogenic activity of xanthohumol was shown to be more potent than that of epigallocatechin-3-gallate (of green tea), and involved increases in AMPK phosphorylation and activity, and inactivation of the AKT pathway. Gallo 2016
The cytotoxicity of xanthohumol to glioma cells was shown to involve upregulation of microRNA miR-204-3p and inhibition of IGFBP2 via c-Fos binding to its gene promoter region. Chen 2016
An aqueous extract of hop (Humulus lupulus) cones was one of the two extracts identified as the most potent modulators of the GABA(A) receptor, among the 10 aqueous extracts of food plants tested. Sahin 2016
Differential effects of xanthohumol on two different lung adenocarcinoma cell lines are described. Sławińska-Brych 2016
Xanthohumol from Humulus luupulus enhanced the cytotoxic and apoptotic effects of TRAIL in human prostate adenocarcinoma LNCaP cells. Kłósek 2016
A hop extract and 6-prenylnaringenin induced estrogen 2-hydroxylation in normal and cancerous human breast cells via preferential enhancement of P450 1A1/1B1 expression and/or activity. Wang 2016
Compounds of hops with antimicrobial activity against Staphylococcus aureus were identified using a novel method. Dušek 2016
Tetrahydro-iso-alpha acids decreased estradiol-stimulated transcriptional activity of estrogen receptor α (ERα) and proliferation of ERα-positive breast cancer cells. Lempereur 2016
Xanthohumol inhibited growth of Staphylococcus aureus in vitro. Stompor 2016
Hop bract polyphenol as well as its high-molecular-weight fraction inhibited PAR2 and PAR4 mRNA expression, proMMP9 activation, and cellular invasion, induced by Porphyromonas gingivalis gingipains in oral squamous cell carcinoma cells. Inaba 2016
Interaction between xanthohumol (XN) and myeloid differentiation protein 2 (MD-2) was found to occur by XN forming two stable hydrogen bonds with the Arg-90 and Tyr-102 residues of MD-2, thus occupying the hydrophobic pocket of the protein. Fu 2016
Xanthohumol (10-40 µM) inhibited proliferation and induced apoptosis in human liver cancer HepG2 cells, via an increase in caspase-3 activity, suppression of NF-κB expression, and up-regulation of p53. Zhao 2016
Using a "click chemistry" approach for the identification of target proteins of electrophilic compounds, it was confirmed that xanthohumol binds to Keap1, and a new candidate target protein was identified as glucose-6-phosphate dehydrogenase. Brodziak-Jarosz 2016
Xanthohumol induced cell cycle arrest and apoptosis in the human alveolar adenocarcinoma (non-small cell lung cancer) cell line A549, while showing relatively low cytotoxicity to the normal human lung fibroblast cell line MRC-5, in vitro. Yong 2015
Xanthohumol was shown to interact directly with the mitochondrial electron transfer chain complex I (NADH dehydrogenase), inhibit the oxidative phosphorylation, trigger the production of reactive oxygen species, and induce apoptosis in the result, in vitro. Zhang 2015
Xanthohumol inhibited cell cycle progression and proliferation of larynx cancer cells, in vitro. Sławińska-Brych 2015
Supercritical CO2 and ethanolic extracts of Humulus lupulus showed the best results, among GRAS (generally recognized as safe) plant species, on planktonic cultures of oral pathogenic microorganisms. Pilna 2015
The effects of xanthohumol were analyzed in multiple cell-based assays. Zenger 2015
Flavonoids isolated from hops inhibited the monophenolase and diphenolase activities of a mushroom tyrosinase. Kim 2015
Xanthohumol reduces the de novo synthesis of fatty acid and cholesterol via sterol regulatory element-binding protein inactivation. Miyata 2015
Xanthohumol, a hop compound, reduced cell viability, colony forming ability, and confluency of hepatocellular carcinoma cell, increased expression of pro-apoptotic and reduced expression of anti-apoptotic proteins, and inhibited the Notch signaling pathway. Kunnimalaiyaan 2015
Xanthohumol, a prenylated chalcone from hop, is identified as a potent inhibitor of iodothyronine deiodinases. Renko 2015
Xanthohumol, a prenylated chalcone found in hops, time- and concentration-dependently induced apoptosis in human pancreatic cancer cells, via the inhibition of the Notch1 signaling pathway. Kunnimalaiyaan 2015
Xanthohumol, a prenylated chalcone found in hop plants, induced growth inhibition and apoptosis in Ca Ski human cervical cancer cells. Yong 2015
8-Prenylnaringenin and 6-prenylnaringenin, two prenylflavonoids present in hops, demonstrated an unexpectedly pronounced, dose-dependent reduction of cellular proliferation of human PC-3 prostate cancer cells and UO.31 renal carcinoma cells. Busch 2015
Hop compounds 8-prenylnaringenin and 6-prenylnaringenin stimulate differentiation of neural precursor cells. Urmann 2015
The inhibitory effects of hop essential oil and its constituents on Listeria innocua, Staphylococcus aureus, Bacillus subtilis, Yersinia enterocolitica, Salmonella enteritidis, Salmonella typhimurium, Escherichia coli O157:H7, and other bacteria were examined. Akdemir Evrendilek 2015
Xanthohumol inhibited (3)H-deoxy-D-glucose uptake by breast cancer cells. Azevedo 2015
Xanthohumol and isoxanthohumol were shown to be inhibitors of Kv1.3 channels in human leukemic Jurkat T cells. Gąsiorowska 2015
The antiproliferative activity of six different hops extracts on various human cancer cells was studied. Cömert Önder 2015
Xanthohumol confers protection of rat neuronlike cells via activation of the transcription factor Nrf2 and upregulation of a panel of phase II cytoprotective genes and their gene products. Yao 2015
Eudesmol, an oxygenated sesquiterpene present at high concentrations in the essential oil of hop cultivar Hallertau Hersbrucker, activated transient receptor potential ankyrin 1 (TRPA1) in human embryonic kidney-derived cells. Ohara 2015
The molecular mechanisms of the antimicrobial activity of iso-α-acids from hops were studied. Schurr 2015
Hop extracts were screened for compounds with inhibitory activities against Janus kinase 2 (JAK2) and adenosine monophosphate kinase (AMPK). Martin 2015
8-Prenylnaringenin did not affect osteoblast proliferation but inhibited differentiation of osteoclast-like cells into osteoclasts, reduced the pit area of bone resorption, and inhibited the expression of receptor activator of nuclear factor-κB ligand (RANKL), in vitro. Luo 2014
Xanthohumol, a compound from hops, prevented estrogen receptor (ER) α-positive breast cancer cells growth, both in vitro and in vivo, via inhibition of the interaction between the BIG3 and prohibitin 2 (PHB2) proteins, while not suppressing the growth of normal mammary epithelial cells. Yoshimaru 2014
The kinetics of the interaction of 1-hydroxyethyl radical with hop prenylflavonoids 6-prenylnarigerin and xanthohumol was studied. de Almeida 2014
Lupulone, a compound in hops, inhibited Mycobacterium tuberculosis, the causative agent of tuberculosis, via differential regulation of the total of 540 genes. Wei 2014
Xanthohumol, a unique prenylated flavonoid from hops, inhibited α-glucosidase via direct binding and induction of minor conformational changes of the enzyme. Liu 2014
A hop extract showed spasmolytic and antispasmodic effects in rat ileum ex vivo. Hejazian 2014
The interactions of hops-derived flavonoids with phospholipid membrane models are described. Wesołowska 2014
Xanthohumol, a flavonoid from hops, inhibits hepatitis C virus replication in vitro. Lou 2014
The anticholinesterase activity of an aqueous-methanolic extract from hop was investigated. Jazayeri 2014
Humulone, a bitter acid from hop, suppressed respiratory syncytial virus replication and release of proinflammatory factors in human nasal epithelial cells. Fuchimoto 2013
8-Prenylnaringenin improved osteoblast differentiation and osteogenic function in cultured rat osteoblasts. Ming 2013
β-acids from hop inhibited the growth of prostate and colon cancer cells more strongly than α-acids, but the difference was ameliorated with the application of whole plant extracts. Farag 2013
Isoxanthohumol, a phytoestrogen from hop, inhibited angiogenesis and inflammation in human vascular smooth muscle and endothelial cells. Negrão 2013
8-prenylnaringenin inhibited rabbit osteoclasts in vitro. [Article in Chinese] Lv 2013
Lupulone, a β-acid from hops, exhibited potential anticancer activity towards prostate cancer cells. Mouratidis 2013
Xanthohumol changes the properties of a cellular membrane phospholipid bilayer model by transitioning to the vicinity of the phosphate group and complex formation with the phospholipid molecules. Arczewska 2013
Xanthohumol induces chemopreventive effects in normal liver cells, while showing cytotoxicity to hepatic carcinoma cells in vitro. Krajka-Kuźniak 2013
Linalool, a compound from hops, increased doxorubicin influx in tumor cells and in combination with doxorubicin significantly decreased tumor weight, compared with doxorubicin alone, in vivo. Miyashita 2013
Xanthohumol, the principal flavonoid in hops, sensitized adriamycin-resistant human breast cancer cells to ionizing radiation by decreasing the levels of anti-apoptotic proteins. Kang 2013
Isoxanthohumol and its colonic microflora metabolite 8-prenylnaringenin induce apoptosis and inhibit the invasiveness of colonic cancer cells in vitro. Allsopp 2013
Xanthohumol induces apoptosis and subsequent phagocytosis by human blood monocyte-derived macrophages of glioblastoma cells. Festa 2013
Xanthohumol, a compound from hops, reduced the ability of breast cancer cells to invade lymph nodes by inhibiting the cells interaction with the lymphendothelial barrier. Viola 2013
Xanthohumol inhibited hyaluronan export in fibroblasts. Kathagen 2013
Xanthohumol, a constituent of hops, inhibited the growth of and induced apoptosis in triple-negative breast cancer cells. Kim 2013
Different compounds in hops differentially affect breast cancer cells. Blanquer-Rosselló 2013
In a examination of herbs used for menopausal symptoms, the estrogenic activity of three licorice species was evaluated in comparison with hops. Hajirahimkhan 2013
Xanthohumol inhibits osteoclast formation in vitro. Suh 2013
The ability of hops-derived flavonoids for the stimulation of neuronal differentiation, neurite outgrowth, and neuroprotection is investigated. Oberbauer 2013
Hop extracts inhibit biofilm formation by gram-positive but not gram-negative bacteria. Rozalski 2013
Hops water extracts did not inhibit Vibrio cholera hemolysin. [Article in Russian] Markina 2013
Isoxanthohumol, a flavonoid from hops, inhibited gene activation induced by the proinflammatory cytokine transforming growth factor β in hepatic and breast cancer cell lines, and decreased angiogenesis in the breast cancer cells. Serwe 2012
Hop bitter acids (from a CO(2) hop extract) inhibited the proliferation of hepatic stellate cells and corresponding molecular events, indicating potential usefulness of the compounds in the treatment and/or prevention of hepatic fibrosis. Saugspier 2012
8-prenylnaringenin differentially regulated mRNA expression of several genes in rat raphe nuclei-derived cells, which may explain some of the effects of hop flavonoids on mood. Amer 2012
The bitter acids from beer, comprised of α-, β-, and iso-α-acids, were identified as potentially promoting gastric acid secretion and up-regulating the CHRM3 acetylcholine receptor expression in human gastric cancer cells. Walker 2012
8-Prenylnaringenin inhibited agonist-dependent platelet aggregation and platelet adhesion to collagen matrix. Di Vito 2012
8-Prenylnaringenin inhibited voltage-gated Kv1.3 potassium channels in human Jurkat T cells. Gąsiorowska 2012
Xanthohumol, a prenylated flavonoid from hops, inhibited cholesteryl ester transfer protein more effectively than any other natural plant product tested. However, isoxanthohumol and naringenin decreased the activity. Hirata 2012
8-Prenylnaringenin enhanced bone marrow stromal cells differentiation and mineralization. Ming 2012
A hops extract and, in particular, 8-phenylnaringenin, but not xanthohumol, inhibited the formation of oxidized and potentially carcinogenic estrogen metabolites and estrogen-induced malignant transformation in human mammary epithelial cells. Hemachandra 2012
Xanthohumol upregulates the expression of phase I (CYP1A1 and CYP1A2) and phase II (UGT1A1) enzymes in human hepatic cells, thus preventing the toxicity of heterocyclic aromatic amines to the cells, and is not mutagenic to Salmonella typhimurium TA98 nor genotoxic to the hepatoma cells. Viegas 2012
Xanthohumol suppressed chemokine receptor type 4 (CXCR4) in various cancer cell types. Wang 2012
Xanthohumol reversed the protective effect of arachidonic acid on palmitic acid-induced HIT-T15 pancreatic β cells. Cho 2012
Xanthohumol suppressed the migration ability of cholangiocarcinoma cell lines. Jongthawin 2012
Xanthohumol inhibited staphyloxanthin production by methicillin-resistant Staphylococcus aureus (MRSA). Sakai 2012
The activity of xanthohumol against human breast cancer and sarcoma cells is compared to those of prenyl and geranyl derivatives of phloroacetophenone. Cho 2012
Xanthohumol selectively inhibited the growth of glioblastoma cell while protecting normal human astrocytes against apoptosis. Zajc 2012
Xanthohumol potently inhibited platelet aggregation in human platelets in vitro. Lee 2012
A modified hop extract, META060, inhibited monocyte adhesion to endothelial cells, inflammatory molecules production, and expression of matrix metalloproteinase-9 by both types of cells. Desai 2012
Either α- or β-acids-rich hop extracts inhibited proliferation and invasiveness of hepatocellular carcinoma cells, and induced the release of aspartate transaminase by the cells, the effect of the β-acids-rich extract being more pronounced. Saugspier 2012
Xanthohumol was found to bind to histone family members H2A, H2B, and H4. Wyns 2012
Xanthohumol, among other chalcones, induces tumor cell death by increasing the expression of tumor necrosis factor-related apoptosis-inducing ligand receptors 1 and 2 (death receptors 4 and 5). Szliszka 2012
A hop water extract reduced the release of thymic stromal lymphopoietin, a key signaling factor in allergic rhinitis, from human nasal epithelial cells treated with a Toll-like receptor 3 ligand. Fuchimoto 2012
An ethanolic extract of hops inhibited rifampin-sensitive and -resistant Mycobacterium tuberculosis isolates. Serkani 2012
Xanthohumol binds to valosin-containing protein, thereby inhibiting autophagosome maturation and resulting in the accumulation of microtubule-associated protein 1 light chain 3-II (LC3-II), which may explain multiple biological activities of xanthohumol. Sasazawa 2012
Lupulone, a bitter acid from hop, triggers apoptosis in human colon cancer-derived metastatic cells via the p38 mitogen-activated protein kinase (MAPK), but not via JNK or ERK MAPKs. Lamy 2011
Prenylflavonoids from hop inhibited transport of hyaluronan by the ATP-binding cassette transporter multidrug resistance associated protein 5 (MRP5), thus potentially possessing antiosteoarthritic effects. Stracke 2011
8-Prenylnaringenin and isoxanthohumol differentially affected androgen production by rat Leydig cells, depending on the state of maturation of the cells and the activation stimulus. Izzo 2011
Xanthohumol, a major chalcone derivative isolated from hops commonly used in brewing due to its bitter flavors, inhibits the NRF2-ARE signaling pathway and upregulates the transcription of heme oxygenase-1, which explains its anti-inflammatory effects, in mouse microglial cells. Lee 2011
Xanthohumol and xanthohumol D were identified as quinone reductase-2 inhibitors. Choi 2011
A hop cone extract protected platelets from peroxynitrite-induced oxidative and nitrative damage. Olas 2011
Xanthohumol upregulated the activity of alkaline phosphatase, an osteoblast marker, and increased the expression of a factor of osteoblast differentiation. Jeong 2011
Xanthohumol decreases Notch1 expression and induces apoptosis in ovarian cancer cells. Drenzek 2011
The effect of xanthohumol, among other polyphenols in alcoholic beverages, on constitutive androstane receptor was studied. Yao 2011
Xanthohumol induced apoptosis in human malignant glioblastoma cells. Festa 2011
8-Prenylnaringenin showed strong estrogenic activity in raphe nuclei cells of the rat brain. Amer 2010
Lupulone, a bitter acid from hops, differentially affects human colon adenocarcinoma cells and lymph node metastasis cells derived from the same patient. Lamy 2010
Prenylated flavonoids, such as xanthohumol, showed greater binding activity to cancer-relevant cellular proteins than non-prenylated flavonoids used in this study. Cassidy 2010
Xanthohumol synergistically increased the antiviral activity of interferon-alpha against bovine viral diarrhea virus, a surrogate model of hepatitis C virus. Zhang 2010
The mechanism of yeast resistance to hop iso-alpha-acids was studied. Hazelwood 2010
Xanthohumol induces apoptosis, inhibits proliferation and migration in hepatocellular carcinoma cells, while being not cytotoxic to normal human hepatocytes. Dorn 2010
Xanthohumol inhibited proliferation of medullary thyroid cancer cells and suppressed the expression of achaete-scute complex-like 1. Cook 2010
Prenylflavonoids from hop suppress the inflammatory activities of human monocytic THP-1 cells by interfering with Toll-like receptor 4 (TLR4) coreceptor MD-2 and TLR4 directly. Peluso 2010
Xanthohumol induced apoptosis in mouse dendritic cells. Xuan 2010
Xanthohumol induces oxidative stress in human cancer cells, benign prostate hyperplasia cells, and murine macrophages, via interaction with mitochondria. Strathmann 2010
Xanthohumol inhibited the activities of matrixmetalloproteinases 1, 2, and 9 and elastin, and up-regulated the expression of collagen types I, III, and V, elastin, and fibrillin-1 and -2 in dermal fibroblasts. Philips 2010
8-Prenylnaringenin inhibits multidrug resistance-associated transporters P-glycoprotein and MRP1, but does not suppress drug resistance in cancer cells. Wesołowska 2010
Hop compounds and their metabolites differentially affect the processes of angiogenesis and inflammation in identical conditions. Negrão 2010
Prostate cancer cells are found to be highly sensitive to xanthohumol. Deeb 2010
Xanthohumol does not scavenge the superoxide radicals, and may instead contribute to their generation. Schempp 2010
8-Prenylnaringenin inhibits epidermal growth factor-induced MCF-7 breast cancer cell proliferation by direct suppression of phosphatidylinositol-3-OH kinase (PI3K). Brunelli 2009
Xanthohumol induced apoptosis in leukemia and myeloma cells via the down-regulation of NFκB activation and IκBα kinase (IKK) activity by interacting with their cysteine residues. Harikumar 2009
Xanthohumol increased IL-2 production in mouse T cells via up-regulation of the IL-2 promoter. Choi 2009
Hop constituents showed potential anti-acne activity. Yamaguchi 2009
Hop proanthocyanidins induce apoptosis in human colon cancer cells via formation of oxidative protein modifications and disruption of the actin cytoskeleton. Chung 2009
The effect of 8-prenylapigenin on breast cancer cell prolliferation was investigated. Brunelli 2009
Xanthohumol suppressed T cell proliferation, development of interleukin-2 (IL-2) activated killer cells (LAK) and cytotoxic T lymphocytes, and the production of Th1 cytokines (IL-2, IFN-γ, and TNF-α). Gao 2009
Hop constituents inhibited LPS-induced release of monocyte chemoattractant protein-1 (MCP-1) and tumor necrosis factor-α (TNF-α) in mouse macrophages and human monocytes. Lupinacci 2009
Xanthohumol inhibited erythrocyte death, induced by oxidative stress or glucose depletion, in vitro. Qadri 2009
Xanthohumol inhibited cytopathic effects of bovine viral diarrhea virus, a surrogate model of hepatitis C virus. Zhang 2009
Xanthohumol combination with guggulsterone synergistically enhanced lipolysis, decreased lipid accumulation, and induced apoptosis in 3T3-L1 adipocytes. Rayalam 2009
Xanthohumol offered antioxidant and anti-inflammatory activities, increased the expression of antioxidant enzymes, but induced apoptosis in pretreated liver tissue after ischemia/reperfusion, a widely accepted model of oxidative stress generation. Hartkorn 2009
Unfolded protein response-related proteins are implicated in xanthohumol-induced apoptosis of chronic lymphocytic leukemia cells. Lust 2009
Xanthohumol, among other chalcones, induced apoptosis in prostate cancer cells. Szliszka 2009
Lupulone, a hop bitter acid, induced apoptosis of both TRAIL-sensitive human colon cancer cells and their derived TRAIL-resistant metastatic cells via the up-regulation of TRAIL DR4/DR5 death receptors at the cell surface. Lamy 2008
Xanthohumol, isoxanthohumol, 8-prenylnaringenin, and 6-prenylnaringenin induced death of prostate cancer cells. Delmulle 2008
Xanthohumol was identified as the antimutagenic agent from hops. Kac 2008
Positive antibacterial co-action of hop constituents lupulone and xanthohumol, with or without several antibiotics, was explored. Natarajan 2008
Hop bract polyphenol inhibited pro-inflammatory responses in human gingival epithelial cells induced by Porphyromonas gingivalis membrane vesicles. Kou 2008
Hop polyphenols inhibited prostaglandin E2 production by human gingival epithelial cells stimulated with Porphyromonas gingivalis components. Inaba 2008
Xanthohumol reduced the expression of TLR4 and MD2 LPS receptor components resulting in the suppression of NF-kappaB activation in LPS-activated mouse macrophages, and reduced the binding activity of STAT-1α and IRF-1 in the IFN-γ stimulated cells. Cho 2008
The cytotoxic and antioxidant activities of several secondary metabolites from hops were investigated using their synthetic equivalents. Vogel 2008
Xanthohumol in combination with honokiol from Magnolia officinalis decreased viability and induced apoptosis in mouse adipocytes. Yang 2008
Xanthohumol decreased apical uptake of 3H-2-deoxy-D-glucose by a human choriocarcinoma cell line. Araújo 2008
Xanthohumol inhibited melanogenesis in melanoma cells, with little cytotoxicity at the effective concentrations. Koo 2008
The interaction between the hop constituent colupulone and human pregnane X receptor, the nuclear xenobiotic receptor, is elucidated on the structural level. Teotico 2008
Xanthohumol induced apoptosis in human hepatocellular carcinoma cell lines, while showing lower cytotoxicity to normal hepatocytes. Ho 2008
Beta acids from hops suppressed the growth of Listeria monocytogenes in a culture broth. Shen 2008
Xanthohumol reduced adipocyte differentiation, increased apoptosis in adipocytes and preadipocytes, and increased NFκB activity in preadipocytes. Mendes 2008
Xanthohumol induced apoptosis in Bcr-Abl+ myeloid leukemia cells, including imatinib mesylate-resistant cell line, and inhibited cellular invasion, metalloprotease production, and adhesion to endothelial cells. Monteghirfo 2008
8-Prenylnaringenin, a flavonoid from hops, induced apoptosis in breast cancer cells, in contrast with the action of 17beta-estradiol. Brunelli 2007
Lupulones, or hop beta-acids, inhibited the growth of a human colon metastatic cancer cell line in vitro, and of chemically induced colon cancer in rats. Lamy 2007
Xanthohumol protected human cells against the genotoxic effects of benzo(a)pyrene, 2-amino-3-methylimidazo[4,5-f]quinoline, and tert-butyl hydroperoxide. Plazar 2007
Xanthohumol and its metbolites isoxanthohumol and 8-prenylnaringenin inhibited the activity of estrogen synthase, decreased proliferation and induced apoptosis in breast cancer cells. Monteiro 2007
Prenylflavanones from hops inhibited proliferation and induced apoptosis in a Burkitt lymphoma cell line. Diller 2007
Xanthohumol inhibited cell proliferation, induced apoptosis, reduced VEGF secretion, decreased cell invasion, metalloprotease production, and adhesion to endothelial cells of acute and chronic myelogenous leukemia cell lines. Dell'Eva 2007
Xanthohumol and isoxanthohumol induced apoptosis in mature adipocytes, inhibited maturation and reduced lipid content in preadipocytes, with xanthohumol being more effective in both instances. Yang 2007
Two chalcones from hops exhibited cytotoxicity against human neuroblastoma cells. Nishimura 2007
Xanthohumol upregulates the antioxidant response element (ARE) via alkylation of the Keap1 protein. Luo 2007
Xanthohumol inhibits growth, viability, and capillary-like structures formation of human endothelial cells, but not when they are co-cultured with smooth muscle cells. Negrão 2007
A hops extract significantly inhibited the activity of glutamic acid decarboxylase, a gamma-aminobutyric acid (GABA)-metabolizing enzyme. Awad 2007
Xanthohumol was the most active of the hops constituents analyzed to inhibit growth of several human cancer cell lines. Lee 2007
The effects of humulone, a bitter acid from hops, on cyclooxygenase-2 expression in mouse skin stimulated with the tumor promoter 12-O-tetradecanoylphorbol-13-acetate were investigated. Lee 2007
Xanthohumol from hops and its oxidation product may be potentially useful as chemopreventive agents in prostate hyperplasia and prostate carcinogenesis, acting via induction of apoptosis and down-regulation of NFkappaB activation in prostate cells. Colgate 2007
The effects of 8-prenylnaringenin on mouse sperm were investigated. Fraser 2006
The antiallergic properties of hop water extract were studied by evaluating histamine release from human basophilic KU812 cells induced by calcium ionophore A23187. Segawa 2006
It was evidenced for the first time that the family of prenylated flavonoids from hops effectively inhibits proliferation of prostate cancer cells in vitro. Delmulle 2006
The influence of the xanthohumol from Humulus lupulus L. on the binding of muscimol-Alexa Fluor 532, a fluorescently labeled GABAA receptor agonist, was studied by fluorescence correlation spectroscopy. Meissner 2006
Prenylflavonoids from hops are able to modulate aromatase activity, decreasing estrogen synthesis, with relevance for the prevention and treatment of estrogen-dependent disorders such as breast cancer. Monteiro 2006
It is suggested that the estrogenicity of hop constituents in vivo will depend in part on metabolic conversion that may show individual variation. Guo 2006
The pentane extract of the beer, hop (Humulus lupulus L.) oil, and myrcenol potentiated the gamma-aminobutyric acid receptor (GABA(A)) response elicited by GABA. Aoshima 2006
Xanthohumol (XN), the principal flavonoid of Humulus lupulus repressed both the NF-kappaB and Akt pathways in endothelial cells, indicating that components of these pathways are major targets in the molecular mechanism of XN. Albini 2006
The standardized CO(2) extract of Humulus lupulus could be a useful agent for intervention strategies targeting inflammatory disorders and/or inflammatory pain. Hougee 2006
The estrogenic activity of 8-prenylnaringenin was compared to those of other phytoestrogens. Matsumura 2005
The ability of chalcone derivatives of hops to interfere with the haemin-degradation process of P. falciparum was demonstrated. This effect might contribute to their antiplasmodial activity. Frolich 2005
The estrogenic activity of 8-prenylnaringenin is compared to that of other phytoestrogens. Zierau 2005
The enzyme activities encoded in five cDNAs for chalcone synthase homologs from hop were investigated which revealed that flavonoid depends mainly on chalcone synthase (CHS H1) while bitter acid biosynthesis depends mainly on valerophenone synthase and CHSH1. Okada 2005
The chemopreventive mechanism of hops was analyzed by studying the antioxidative activities of the latter and its effect on detoxification of menadione, and it was revealed that xanthohumol inhibited menadione-induced DNA damage through induction of quinone reductase. Dietz 2005
Extracts of hops and red clover and their individual constituents including 8-prenylnaringenin (8-PN), 6-PN from hops and daidzein, formononetin, biochanin A, and genistein from red clover were compared using a variety of in vitro estrogenic assays. Overk 2005
Analysis of the influence of xanthohumol, a prenylated chalcone from hops (Humulus lupulus), on the iodide uptake in a cell culture model of normal, nontransformed rat thyrocytes revealed that Xanthohumol stimulates iodide uptake in rat thyroid-derived FRTL-5 cells. Radovic 2005
The review summarizes the capacity of xanthohumol in comparison with additional hop constituents and metabolites to act as an antiinfective agent against microorganisms including bacteria, viruses, fungi and malarial protozoa. Gerhauser 2005
The modulating action of xanthohumol (XN) on the farnesoid X receptor (FXR) in vitro and in vivo was examined which showed that XN acts on FXR through a selective bile acid receptor modulator like guggulsterone or polyunsaturated fatty acids. Nozawa 2005
Xanthohumol, the main prenylated chalcone in hops (Humulus lupulus), was investigated for its antiinvasive activity on human breast cancer cell lines (MCF-7 and T47-D) in vitro which showed that Xanthohumol upregulates the function of the E-cadherin/catenin complex and inhibits invasion in vitro. Vanhoecke 2005
Investigation of the cell growth inhibitory potential of xanthohumol on cultured human colon cancer cells showed that xanthohumol reduced proliferation of the HCT 116-derived colon cancer cell line 40--16. Pan 2005
The pro-estrogenic hop-derived compounds 8-prenylnaringenin, 6-prenylnaringenin, xanthohumol, and isoxanthohumol affect the gene expression in osteoblast cells and increase proliferation of breast cancer cells. Effenberger 2005
8-Prenylnaringenin, a phytoestrogen from hops, inhibited angiogenesis induced by basic fibroblast growth factor, vascular endothelial growth factor, or their combination. Pepper 2004
The cell toxicity of 8-prenylnaringenin was examined. Unlike the typical flavonoid quercetin, the hop compound exhibited no antioxidant effects and no mitochondrial membrane potential-disrupting activity. Tokalov 2004
The anti-endothelial effects of isoxanthohumol were assessed. Bertl 2004
Two major metabolites of 8-prenylnaringenin were shown to be estrogenic in vitro. Zierau 2004
The expression and subcellular localization of extracellular signal-regulated kinase 1 or 2 (ERK1/2) homologues (HLERK1/2) during the process of organogenic nodule formation in Humulus lupulus var. Nugget was studied using antibodies specific for ERK1 and ERK2. Sousa Silva 2004
Xanthohumol inhibited HIV-1 induced cytopathic effects, the production of viral p24 antigen and reverse transcriptase in C8166 lymphocytes at non-cytotoxic concentration. Wang 2004
It is shown that the principle estrogen 8-prenylnaringenin from hops is an artifact formed along with its positional isomer 6-prenylnaringenin through the spontaneous isomerization of the pro-estrogenic chalcone DMX. Chadwick 2004
It is proposed that GC-MS of derivatised components of lipophilic extracts of hops be a first step before antimycobacterial bioassay-guided study, as this technique is the method of choice for dereplication of fatty acids. Stavri 2004
The antiviral activities of various hop constituents were analyzed. Buckwold 2004
Hop bitter acids displayed a strong growth-inhibitory effect against human leukemia HL-60 cells, with an estimated IC(50) value of 8.67 microg/mL, but were less effective against human histolytic lymphoma U937 cells. Chen 2004
8-Prenylnaringenin, a phytoestrogen from hops, significantly stimulated capacitation, acrosome reactions, and sperm fertilizing ability in uncapacitated mouse sperm cells, and acrosome reactions in capacitated cells. Adeoya-Osiguwa 2003
8-Prenylnaringenin, a hop-derived compound in beer, was found to have estrogenic activity, which was assessed to be 10-times as high as that of genistein (a compound from soy) and 100-times less than that of 17beta-estradiol. Takamura-Enya 2003
8-Prenyl naringenin is a potent ERalpha selective phytoestrogen present in hops and beer. [No abstract] Schaefer 2003
8-Prenylnaringenin, a phytoestrogen from hops, did not show any observable antiandrogenic activity. Zierau 2003
Prenylated 2'-hydroxychalcones and flavanones from the inflorescences of the female hop plant (Humulus lupulus) were shown to inhibit peroxynitrite-mediated oxidation of low-density lipoproteins (LDL) at low micromolar concentrations. Stevens 2003
The inhibitory effect of Humulus lupulus L. on both production of NO & expression of inducible NO synthase (iNOS) in mouse macrophage RAW 264.7 cells was investigated, revealing that chalcones, including xanthohumol, inhibited the production of NO by suppressing the expression of iNOS. Zhao 2003
The estrogenic activity of 8-prenylnaringenin was characterized. The compound showed comparable binding activity to both estrogen receptor isoforms (ER alpha and ER beta). Both (R)- and (S)- enantiomers showed similar bioactivity in vitro. Milligan 2002
Surveys of microfungi in a former industrial area in Duisburg-Nord indicates that new for Germany are Ceratopycnis clematidis Hohn. on Clematis vitalba L., Dasyscyphus aff. humuli Dennis on Humulus lupulus L., etc. Feige 2002
Xanthohumol, a compound from hops (Humulus Iupulus), demonstrated a broad spectrum of inhibitory activities on carcinogenesis, including modulation of the activity of enzymes involved in carcinogen metabolism and detoxification, anti-inflammatory properties, induction of apoptosis, and others. Gerhauser 2002
8-Prenylnaringenin, a compound from hops, demonstrated strong estrogenic activities. Zierau 2002
Hop-derived chalcones diprenylxanthohumol and tetrahydroxanthohumol enhanced Fe(3+)-ADP/NADPH-induced lipid peroxidation in rat liver microsomes, while xanthohumol and 5'-prenylxanthohumol protected cultured rat hepatocytes from tert-butyl hydroperoxide toxicity. Rodriguez 2001
8-Prenylnaringenin, a phytoestrogen found in hops, stimulated E-cadherin-dependent aggregation and growth of invasive human mammary carcinoma cells in vitro, mimicking the effects of 17beta-estradiol, but did not affect the invasion of the cells in the chick heart assay. Rong 2001
Humulone, a bitter acid from beer hop extract, showed anti-angiogenic effects in vitro and in vivo, and suppressed the proliferation of endothelial cells and the production of vascular endothelial growth factor in endothelial and tumor cells. Shimamura 2001
Among 8 botanical preparations that are commonly used for the treatment of menopausal symptoms, methanol extracts of red clover, chasteberry and hops (Humulus lupulus L.) showed significant competitive binding to estrogen receptors alpha and beta. Liu 2001
It is indicated that the endocrine properties of hops and hop products are due to the very high estrogenic activity of 8-prenylnaringenin. Milligan 2000
It is suggested that the hop flavonoids are potent and selective inhibitors of human cytochrome P450. Henderson 2000
The presence of 8-prenylnaringenin in hops may provide an explanation for the accounts of menstrual disturbances in female hop workers and this phytoestrogen can also be detected in beer. Milligan 1999
Six flavonoids, including xanthohumol and isoxanthohumol from hops (Humulus lupulus), were tested for their antiproliferative activity in human breast cancer, colon cancer, and ovarian cancer cells in vitro. Miranda 1999
Hexahydro-colupulone shows a wide spectrum of activity against a number of established human tumor cell lines Stephan 1998
Humulone inhibited the growth of monoblastic leukemia U937 cells and enhanced the differentiation-inducing action of vitamin D3 Honma 1998
Hop bract polyphenols (HBP) have an inhibitory effect on cariogenic streptococci. Tagashira 1997
Humulone strongly inhibits bone resorption in the pit formation assay, IC50 = 5.9 x 10(-9)M. Xanthohumol is also inhibitory Tobe 1997
Humulone, a bone resorption inhibitor from hop extract, induced apoptosis in the premyocytic leukemia cell line HL-60 at 1 - 100 micrograms/ml Tobe 1997
Hop bitter acids, humulones and lupulones, scavenge radicals and inhibit lipid peroxidation. Tagashira 1995
[Neurological stamp. Humulus lupulus (hop).] Haas 1995
The antibacterial activity of trans-isohumulone was around 20 times greater than that of humulone, 11 times greater than of colupulone and 9 times greater than of trans-humulinic acid when the degree of ionization was taken into account. Simpson 1992
Hop oils were shown to be antimicrobial against Gram-positive Bacillus subtilis, Staphylococcus aureus, and the fungus Trichophyton mentagrophytes, but have almost no activity against Gram-negative Escherichia coli and the yeast Candida albicans. Langezaal 1992
[The sedative-hypnotic action of hops. 4. Pharmacology of the hop substance 2-methyl-3-buten-2-ol]. [Article in German] Wohlfart 1983
[Pharmacodynamic study of the lupulus' (Humulus lupulus L.) tranquilizing action]. Bravo 1974
Membrane leakage in Bacillus subtilis 168 induced by the hop constituents lupulone, humulone, isohumulone and humulinic acid. [No abstract] Teuber 1973
Isohumulone is reported to have low antibiotic potency, with 15-30 times less inhibitory activity on the growth of gram-positive bacteria than two other hop compounds lupulone or humulone. Teuber 1970
[Attempts to identify sedative-hypnotic active substances in hops]. Hansel 1967
[Phytoncides. I. Lupulone and humulone; their antibacterial action and their use in tuberculous infections]. [Article in an undetermined language] [No abstract] Erdmann 1951
History of Record
November 1999
MAJOR REVISION BY: Michael C. Tims, PhD. candidate
June 2001
March 2023