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Xanthohumol AND Hops

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https://www.readbyqxmd.com/read/28036030/xanthohumol-a-prenylated-chalcone-from-hops-inhibits-the-viability-and-stemness-of-doxorubicin-resistant-mcf-7-adr-cells
#1
Ming Liu, Hua Yin, Xiaokun Qian, Jianjun Dong, Zhonghua Qian, Jinlai Miao
Xanthohumol is a unique prenylated flavonoid in hops (Humulus lupulus L.) and beer. Xanthohumol has been shown to possess a variety of pharmacological activities. There is little research on its effect on doxorubicin-resistant breast cancer cells (MCF-7/ADR) and the cancer stem-like cells exiting in this cell line. In the present study, we investigate the effect of xanthohumol on the viability and stemness of MCF-7/ADR cells. Xanthohumol inhibits viability, induces apoptosis, and arrests the cell cycle of MCF-7/ADR cells in a dose-dependent manner; in addition, xanthohumol sensitizes the inhibition effect of doxorubicin on MCF-7/ADR cells...
December 28, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27976466/fast-sampling-analyses-and-chemometrics-for-plant-breeding-bitter-acids-xanthohumol-and-terpenes-in-lupulin-glands-of-hops-humulus-lupulus
#2
Daniel P Killeen, Oliver C Watkins, Catherine E Sansom, David H Andersen, Keith C Gordon, Nigel B Perry
INTRODUCTION: The valuable secondary metabolites in hops (bitter acids, xanthohumol, volatile monoterpenes and sesquiterpenes) are sequestered in lupulin glands (extracellular trichomes) which can be collected and analysed with little or no sample preparation. OBJECTIVES: To determine whether high throughput screening of lupulin glands composition, by fast analyses and chemometrics, could be used for breeder selection of hops with key flavour attributes. METHODS: Lupulin glands from 139 plants (39 cultivars/advanced selections) were analysed by Raman and (1) H NMR spectroscopy, and head-space solid-phase microextraction (HS-SPME) GC-FID...
January 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/27923802/xanthohumol-prevents-dna-damage-by-dietary-carcinogens-results-of-a-human-intervention-trial
#3
Christoph Pichler, Franziska Ferk, Halh Al-Serori, Wolfgang Huber, Walter Jäger, Monika Waldherr, Miroslav Mišík, Michael Kundi, Armen Nersesyan, Irene Herbacek, Siegfried Knasmueller
Xanthohumol (XN) is a hop flavonoid contained in beers and soft drinks. In vitro and animal studies indicated that XN has DNA and cancer protective properties. To find out if it causes DNA protective effects in humans, an intervention trial was conducted in which the participants (n = 22) consumed a XN containing drink (12 mg XN/P/d). We monitored prevention of DNA damage induced by representatives of major groups of dietary carcinogens [i.e., nitrosodimethylamine (NDMA) benzo(a)pyrene (B(a)P) and the heterocyclic aromatic amine 2-amino-3-methylimidazo[4,5-f]quinoline (IQ)]...
December 6, 2016: Cancer Prevention Research
https://www.readbyqxmd.com/read/27904394/dose-dependent-protective-and-inductive-effects%C3%A2-of-xanthohumol-on-oxidative-dna-damage-in%C3%A2-saccharomyces-cerevisiae
#4
Daniel O Carvalho, Rui Oliveira, Björn Johansson, Luís F Guido
The effect of xanthohumol, a prenylflavonoid isolated from the hop plant (Humulus lupulus L.), on Saccharomyces cerevisiae DNA oxidative damage and viability was evaluated. Yeast cultures under oxidative stress, induced by H2O2, displayed stronger growth in the presence of 5 mg/L of xanthohumol than cultures with only H2O2. Likewise, DNA damage assessed by the comet assay was significantly lower in cells co-incubated with xanthohumol and H2O2. Accordingly, fluorescence of dichlorofluorescein in cells treated with H2O2 and xanthohumol was considerably lower than in cells exclusively treated with H2O2, indicative of a reactive oxygen species scavenging mechanism and consequent formation of oxidation products, as detected by mass spectrometry...
March 2016: Food Technology and Biotechnology
https://www.readbyqxmd.com/read/27855519/xanthohumol-from-hop-cones-humulus-lupulus-l-prevents-adp-induced-platelet-reactivity
#5
Boguslawa Luzak, Hassan Kassassir, Edward Rój, Lidia Stanczyk, Cezary Watala, Jacek Golanski
Hop cones (Humulus lupulus L.), very rich source of phenolic compounds, possessing anticancer, antioxidant and anti-inflammatory activities, are considered as beneficial diet ingredients improving human health. In this study, the antiplatelet action of xanthohumol (XN), the principal flavonoid in hop cones, was investigated. XN significantly attenuated ADP-induced blood platelet aggregation (97.2 ± 35.7 AU for 6 μg/ml of XN vs. 120.4 ± 30.1 AU for 0.17% dimethyl sulfoxide (DMSO), p < 0...
November 18, 2016: Archives of Physiology and Biochemistry
https://www.readbyqxmd.com/read/27815365/xanthohumol-modulates-calcium-signaling-in-rat-ventricular-myocytes-possible-antiarrhythmic-properties
#6
Juan Jose Arnaiz-Cot, Lars Cleemann, Martin Morad
Cardiac arrhythmia is a major cause of mortality in cardiovascular pathologies. A host of drugs targeted to sarcolemmal Na(+), Ca(2+), and K(+) channels has had limited success clinically. Recently, Ca(2+) signaling has been target of pharmacotherapy based on finding that leaky ryanodine receptors elevate local Ca(2+) concentrations causing membrane depolarizations that trigger arrhythmias. In this study, we report that xanthohumol, an antioxidant extracted from hops showing therapeutic effects in other pathologies, suppresses aberrant ryanodine receptor Ca(2+) release...
January 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27617238/hops-for-menopausal-vasomotor-symptoms-mechanisms-of-action
#7
EDITORIAL
Fatemeh Abdi, Hamid Mobedi, Nasibeh Roozbeh
Menopause is a critical stage of women's life associated with various complaints and distresses. Vasomotor symptoms (VMS), such as hot flushes, night sweats, sleep disturbances, and fatigue, are the most common menopause symptoms affecting about 50% to 80% of middle-aged women. Obviously, these symptoms, resulting from estrogen deficiency during menopause, can exert negative effects on women's health and quality of life and thus require to be managed through approaches such as hormone replacement therapy (HRT)...
August 2016: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/27596062/conformational-modulation-of-the-farnesoid-x-receptor-by-prenylflavonoids-insights-from-hydrogen-deuterium-exchange-mass-spectrometry-hdx-ms-fluorescence-titration-and-molecular-docking-studies
#8
Liping Yang, David Broderick, Yan Campbell, Adrian F Gombart, Jan F Stevens, Yuan Jiang, Victor L Hsu, William H Bisson, Claudia S Maier
We report on the molecular interactions of the farnesoid X receptor (FXR) with prenylflavonoids, an emerging class of FXR modulators. FXR is an attractive therapeutic target for mitigating metabolic syndromes (MetS) because FXR activates the inhibitory nuclear receptor, small heterodimer partner (SHP), thereby inhibiting both gluconeogenesis and de novo lipogenesis. We and others have shown that xanthohumol (XN), the principal prenylflavonoid of the hop plant (Humulus lupulus L.), is a FXR agonist based on its ability to affect lipid and glucose metabolism in vivo and to induces FXR target genes in biliary carcinoma cells and HEK293 cells...
December 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27494895/hop-derived-flavonoid-xanthohumol-inhibits-endothelial-cell-functions-via-ampk-activation
#9
Cristina Gallo, Katiuscia Dallaglio, Barbara Bassani, Teresa Rossi, Armando Rossello, Douglas M Noonan, Gabriele D'Uva, Antonino Bruno, Adriana Albini
Angiogenesis, a process characterized by the formation of new blood vessels from pre-existing ones, is a crucial step in tumor growth and dissemination. Recently, increased attention has been addressed to the ability of flavonoids to prevent cancer by suppressing angiogenesis, strategy that we named "angioprevention". Several natural compounds exert their anti-tumor properties by activating 5' adenosine monophosphate-activated protein kinase (AMPK), a key regulator of metabolism in cancer cells. Drugs with angiopreventive activities, in particular metformin, regulate AMPK in endothelial cells...
September 13, 2016: Oncotarget
https://www.readbyqxmd.com/read/27487563/the-mir-204-3p-targeted-igfbp2-pathway-is-involved-in-xanthohumol-induced-glioma-cell-apoptotic-death
#10
Peng-Hsu Chen, Cheng-Kuei Chang, Chwen-Ming Shih, Chia-Hsiung Cheng, Cheng-Wei Lin, Chin-Cheng Lee, Ann-Jeng Liu, Kuo-Hao Ho, Ku-Chung Chen
Xanthohumol (XN), a prenylated chalcone extracted from hop plant Humulus lupulus L. (Cannabaceae), has potential for cancer therapy, including gliomas. Micro (mi)RNAs are small noncoding RNAs that control gene expression. Several miRNAs have been identified to participate in regulating glioma development. However, no studies have demonstrated whether miRNA is involved in XN cytotoxicity resulting in glioma cell death. This study investigated the effects of XN-mediated miRNA expression in activating apoptotic pathways in glioblastoma U87 MG cells...
November 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27392499/the-putative-role-of-transcription-factors-from-hlwrky-family-in-the-regulation-of-the-final-steps-of-prenylflavonid-and-bitter-acids-biosynthesis-in-hop-humulus-lupulus-l
#11
Jaroslav Matoušek, Tomáš Kocábek, Josef Patzak, Jindřich Bříza, Kristýna Siglová, Ajay Kumar Mishra, Ganesh Selvaraj Duraisamy, Anna Týcová, Eiichiro Ono, Karel Krofta
Lupulin glands localized in female hop (Humulus lupulus L.) cones are valuable source of bitter acids, essential oils and polyphenols. These compounds are used in brewing industry and are important for biomedical applications. In this study we describe the potential effect of transcription factors from WRKY family in the activation of the final steps of lupulin biosynthesis. In particular, lupulin gland-specific transcription factor HlWRKY1 that shows significant similarity to AtWRKY75, has ability to activate the set of promoters driving key genes of xanthohumol and bitter acids biosynthesis such as chalcone synthase H1, valerophenone synthase, prenyltransferase 1, 1L and 2 and O-methyltransferase-1...
October 2016: Plant Molecular Biology
https://www.readbyqxmd.com/read/27269377/hop-humulus-lupulus-l-extract-and-6-prenylnaringenin-induce-p450-1a1-catalyzed-estrogen-2-hydroxylation
#12
Shuai Wang, Tareisha L Dunlap, Caitlin E Howell, Obinna C Mbachu, Emily A Rue, Rasika Phansalkar, Shao-Nong Chen, Guido F Pauli, Birgit M Dietz, Judy L Bolton
Humulus lupulus L. (hops) is a popular botanical dietary supplement used by women as a sleep aid and for postmenopausal symptom relief. In addition to its efficacy for menopausal symptoms, hops can also modulate the chemical estrogen carcinogenesis pathway and potentially protect women from breast cancer. In the present study, an enriched hop extract and the key bioactive compounds [6-prenylnarigenin (6-PN), 8-prenylnarigenin (8-PN), isoxanthohumol (IX), and xanthohumol (XH)] were tested for their effects on estrogen metabolism in breast cells (MCF-10A and MCF-7)...
July 18, 2016: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/27187329/antimicrobial-activity-of-xanthohumol-and-its-selected-structural-analogues
#13
Monika Stompor, Barbara Żarowska
The objective of this study was to evaluate the antimicrobial activity of structural analogues of xanthohumol 1, a flavonoid compound found in hops (Humulus lupulus). The agar-diffusion method using filter paper disks was applied. Biological tests performed for selected strains of Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria, fungi (Alternaria sp.), and yeasts (Rhodotorula rubra, Candida albicans) revealed that compounds with at least one hydroxyl group-all of them have it at the C-4 position-demonstrated good activity...
May 11, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/26976708/xanthohumol-improves-dysfunctional-glucose-and-lipid-metabolism-in-diet-induced-obese-c57bl-6j-mice
#14
Cristobal L Miranda, Valerie D Elias, Joshua J Hay, Jaewoo Choi, Ralph L Reed, Jan F Stevens
Xanthohumol (XN) is a prenylated flavonoid found in hops (Humulus lupulus) and beer. The dose-dependent effects of XN on glucose and lipid metabolism in a preclinical model of metabolic syndrome were the focus of our study. Forty-eight male C57BL/6J mice, 9 weeks of age, were randomly divided into three XN dose groups of 16 animals. The mice were fed a high-fat diet (60% kcal as fat) supplemented with XN at dose levels of 0, 30, or 60 mg/kg body weight/day, for 12 weeks. Dietary XN caused a dose-dependent decrease in body weight gain...
June 1, 2016: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/26918635/humudifucol-and-bioactive-prenylated-polyphenols-from-hops-humulus-lupulus-cv-cascade
#15
Martino Forino, Simona Pace, Giuseppina Chianese, Laura Santagostini, Markus Werner, Christina Weinigel, Silke Rummler, Gelsomina Fico, Oliver Werz, Orazio Taglialatela-Scafati
Humulus lupulus (hop plant) has long been used in traditional medicine as a sedative and antimicrobial agent. More recently, attention has been devoted to the phytoestrogenic activity of the plant extracts as well as to the anti-inflammatory and chemopreventive properties of the prenylated chalcones present. In this study, an Italian sample of H. lupulus cv. "Cascade" has been investigated and three new compounds [4-hydroxycolupulone (6), humudifucol (7) and cascadone (8)] have been purified and identified by means of NMR spectroscopy along with four known metabolites...
March 25, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/26869767/determination-of-the-binding-mode-for-anti-inflammatory-natural-product-xanthohumol-with-myeloid-differentiation-protein-2
#16
Weitao Fu, Lingfeng Chen, Zhe Wang, Chengwei Zhao, Gaozhi Chen, Xing Liu, Yuanrong Dai, Yuepiao Cai, Chenglong Li, Jianmin Zhou, Guang Liang
It is recognized that myeloid differentiation protein 2 (MD-2), a coreceptor of toll-like receptor 4 (TLR4) for innate immunity, plays an essential role in activation of the lipopolysaccharide signaling pathway. MD-2 is known as a neoteric and suitable therapeutical target. Therefore, there is great interest in the development of a potent MD-2 inhibitor for anti-inflammatory therapeutics. Several studies have reported that xanthohumol (XN), an anti-inflammatory natural product from hops and beer, can block the TLR4 signaling by binding to MD-2 directly...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/26842182/xanthohumol-inhibits-cellular-proliferation-in-a-breast-cancer-cell-line-mda-mb231-through-an-intrinsic-mitochondrial-dependent-pathway
#17
Y B Yoo, K S Park, J B Kim, H J Kang, J H Yang, E K Lee, H Y Kim
AIMS: Xanthohumol isolated from hops has been reported to exhibit anticancer effects in diverse human cancers. However, its effect on breast cancer has not yet been clearly defined. The purpose of this study was to investigate the effects of xanthohumol on breast cancer cell proliferation. MATERIALS AND METHODS: After treatment with 5 μM, 10 μM, and 20 μM xanthohumol for 48 h, cells from the human breast cancer cell line MDA-MB-231 were studied using colony assay, flow cytometry, and western blotting...
October 2014: Indian Journal of Cancer
https://www.readbyqxmd.com/read/26840505/impact-of-xanthohumol-a-prenylated-flavonoid-from-hops-on-dna-stability-and-other-health-related-biochemical-parameters-results-of-human-intervention-trials
#18
RANDOMIZED CONTROLLED TRIAL
Franziska Ferk, Miroslav Mišík, Armen Nersesyan, Christoph Pichler, Walter Jäger, Thomas Szekeres, Rodrig Marculescu, Henrik E Poulsen, Trine Henriksen, Roberto Bono, Valeria Romanazzi, Halh Al-Serori, Martin Biendl, Karl-Heinz Wagner, Michael Kundi, Siegfried Knasmüller
SCOPE: Xanthohumol (XN) is a hop flavonoid found in beers and refreshment drinks. Results of in vitro and animal studies indicate that it causes beneficial health effects due to DNA protective, anti-inflammatory, antioxidant, and phytoestrogenic properties. Aim of the present study was to find out if XN causes alterations of health-related parameters in humans. METHODS AND RESULTS: The effects of the flavonoid were investigated in a randomized crossover intervention trial (n = 22) in which the participants consumed a XN drink (12 mg XN/P/day)...
April 2016: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/26794001/xanthohumol-inhibits-stat3-activation-pathway-leading-to-growth-suppression-and-apoptosis-induction-in-human-cholangiocarcinoma-cells
#19
Hasaya Dokduang, Puangrat Yongvanit, Nisana Namwat, Chawalit Pairojkul, Sakkarn Sangkhamanon, Mika Sakurai Yageta, Yoshinori Murakami, Watcharin Loilome
STAT3 plays a significant role in the development of cholangiocarcinoma (CCA) associated with the liver fluke (Opisthorchis viverrini; Ov). Xanthohumol (XN), a prenylated flavonoid extracted from hops, has known anticancer activity and could potentially target STAT3. The present study determined the effect of XN on STAT3, as well as ascertained its usefulness against CCA. The CCA cell proliferation at 20 µM and 50 µM of XN was shown to inhibited, while 20 µM partially inhibited IL-6-induced STAT3 activation...
April 2016: Oncology Reports
https://www.readbyqxmd.com/read/26748658/a-click-chemistry-approach-identifies-target-proteins-of-xanthohumol
#20
Lidia Brodziak-Jarosz, Yuuta Fujikawa, Daniel Pastor-Flores, Sonay Kasikci, Petr Jirásek, Sebastian Pitzl, Robert W Owen, Karel D Klika, Clarissa Gerhäuser, Sabine Amslinger, Tobias P Dick
SCOPE: Many phytochemicals with beneficial pharmacological properties contain electrophilic sites, e.g. α,β-unsaturated carbonyl (enone) groups. There is increasing evidence that many biological effects of electrophilic compounds depend on covalent conjugation to reactive protein thiols. For example, the reaction of electrophiles with cysteinyl residues of the sensor protein Keap1 activates the cell-protective Nrf2 response. Thus it is of interest to identify more generally the proteins to which small molecule electrophiles bind covalently...
April 2016: Molecular Nutrition & Food Research
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