- Long-lasting muscle relaxant activity of eperisone hydrochloride after percutaneous administration in rats
Eisai Tsukuba Research Laboratories, Ibaraki, Japan
Jpn J Pharmacol 73:215-20. 1997
..These results suggest that percutaneously administered eperisone is absorbed efficiently and shows potent and long-lasting muscle relaxant activity...
- Methcathinone: a new postindustrial drug
Groupe Santé Recherche, 35 rue Bernard de Ventadour, 31300 Toulouse, France
Forensic Sci Int 153:99-101. 2005
..However, this specific case suggests that in spite of a very high bromazepam concentration in presence of the potentiator alcohol, the vital respiratory function would be probably maintained, thanks to the association with methcathinone...
- In vitro evaluation of antibacterial, anticollagenase, and antioxidant activities of hop components (Humulus lupulus) addressing acne vulgaris
Betal, LLC, 5185 MacArthur Blvd, NW, Suite 300, Washington, DC 20016, USA
Phytomedicine 16:369-76. 2009
..Xanthohumol showed the highest activity in total oxygen radical absorbance capacity as well as singlet oxygen absorbance capacity...
- Inhibition of topoisomerase I activity and efflux drug transporters' expression by xanthohumol. from hops
Sung Ho Lee
College of Pharmacy, Chonnam National University, Gwangju 500 757, Korea
Arch Pharm Res 30:1435-9. 2007
- Positive antibacterial co-action between hop (Humulus lupulus) constituents and selected antibiotics
School of Natural Sciences, Fairleigh Dickinson University, Teaneck, NJ, USA
Phytomedicine 15:194-201. 2008
..Ideas for other practical applications of this effect are put forth. The mechanism of the synergistic effect is briefly discussed but no attempt was made to prove it experimentally...
- Broad spectrum anti-infective potential of xanthohumol from hop (Humulus lupulus L.) in comparison with activities of other hop constituents and xanthohumol metabolites
Division of Toxicology and Cancer Risk Factors, German Cancer Research Center, Heidelberg, Germany
Mol Nutr Food Res 49:827-31. 2005
..Overall, these activities further contribute to the broad spectrum of biological effects observed with XN...
- Search method for inhibitors of Staphyloxanthin production by methicillin-resistant Staphylococcus aureus
Graduate School of Pharmaceutical Sciences, Kitasato University, 5 9 1 Shirokane, Minato ku, Tokyo 108 8641, Japan
Biol Pharm Bull 35:48-53. 2012
..These results suggested that this screening method is useful and effective to find compounds targeting staphyloxanthin production, leading to a new type of chemotherapeutics against MRSA infection...
- [A case of eperisone hydrochloride (myonal)--induced drug eruption leading to erythema and angioedema]
Department of Dermatology, Nippon Medical School
Arerugi 56:709-13. 2007
..Some cases took several hours to exhibit symptoms even for urticaria/anaphylaxis types that were confirmed to induce an immediate allergic reaction...
- Influence of xanthohumol on the binding behavior of GABAA receptors and their lateral mobility at hippocampal neurons
Department of Pharmaceutical Biology, University of Marburg, Marburg, Germany
Planta Med 72:656-8. 2006
..11 +/- 0.03) microm2/s] as described with midazolam...
- Synthesis, cytotoxicity, and antioxidative activity of minor prenylated chalcones from Humulus lupulus
Institute of Pharmacy, University of Regensburg, Universitatsstrasse 31, 93053 Regensburg, Germany
J Nat Prod 71:1237-41. 2008
..2-19.2 microM). The ORAC-fluorescein assay revealed potent antioxidative activity for 7 and 8 with 5.2 and 4.8 Trolox equivalents, respectively...
- Antiviral activity of hop constituents against a series of DNA and RNA viruses
Victor E Buckwold
Infectious Disease Research Department, Southern Research Institute, 431 Aviation Way, Frederick, MD 21701, USA
Antiviral Res 61:57-62. 2004
..These hop constituents might serve as interesting lead compounds from which more active anti-HCV, anti-Rhino and anti-herpesvirus antiviral agents could be synthesized...
- Cancer chemopreventive activity of Xanthohumol, a natural product derived from hop
Deutsches Krebstforschungszentrum, Abteilung Toxikologie und Krebsrisikofaktoren, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
Mol Cancer Ther 1:959-69. 2002
..Together, our data provide evidence for the potential application of XN as a novel, readily available chemopreventive agent, and clinical investigations are warranted once efficacy and safety in animal models have been established...
- EST analysis of hop glandular trichomes identifies an O-methyltransferase that catalyzes the biosynthesis of xanthohumol
National Research Council Plant Biotechnology Institute, Saskatoon, Saskatchewan, Canada S7N 0W9
Plant Cell 20:186-200. 2008
..OMT3 was inactive with all substrates tested. The lupulin gland-specific EST data set expands the genomic resources for H. lupulus and provides further insight into the metabolic specialization of glandular trichomes...
- Sensitive electrochemical detection method for alpha-acids, beta-acids and xanthohumol in hops (Humulus lupulus L.)
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SI 1000 Ljubljana, Slovenia
J Chromatogr B Analyt Technol Biomed Life Sci 850:531-7. 2007
..This is the first study demonstrating a very sensitive and validated method for the quantification of xanthohumol, alpha- or beta-acids in hop samples with the use of the electrochemical detector...
- Microbial metabolism of the prenylated chalcone xanthohumol
Hyun Jung Kim
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500 757, Korea
J Nat Prod 69:1522-4. 2006
- Total synthesis of xanthohumol
Rahul S Khupse
Center for Drug Design and Development, College of Pharmacy, The University of Toledo, Toledo, Ohio 43606 3390, USA
J Nat Prod 70:1507-9. 2007
..A Claisen-Schmidt condensation was deployed to construct the chalcone scaffold followed by removal of MOM protecting groups under acidic conditions that were optimized to prevent concomitant cyclization to the flavone...
- Relevance of organic farming and effect of climatological conditions on the formation of alpha-acids, beta-acids, desmethylxanthohumol, and xanthohumol in hop (Humulus lupulus L.)
Jelle De Keukeleire
Institute for Agricultural and Fisheries Research, Unit Plant, Research Domain Genetics and Breeding, Caritasstraat 21, 9090 Melle, Belgium
J Agric Food Chem 55:61-6. 2007
..WC proved to be a rich source of bioactive chalcones, particularly desmethylxanthohumol...
- The prenylflavonoid isoxanthohumol from hops (Humulus lupulus L.) is activated into the potent phytoestrogen 8-prenylnaringenin in vitro and in the human intestine
Unit on Ecology and Physiology of the Digestive Tract UEPSD, National Institute for Agricultural Research INRA, F 78352 Jouy en Josas Cedex, France
J Nutr 136:1862-7. 2006
..6417, P < 0.01). These data show that intestinal conversion of IX upon moderate beer consumption can lead to 8-PN exposure values that might fall within the range of human biological activity...
- Binding of the hop (Humulus lupulus L.) chalcone xanthohumol to cytosolic proteins in Caco-2 intestinal epithelial cells
Department of Medicinal Chemistry and Pharmacognosy, UIC NIH Center for Botanical Dietary Supplements Research, University of Illinois College of Pharmacy, Chicago, IL 60612, USA
Mol Nutr Food Res 51:872-9. 2007
..These data suggest that specific binding of xanthohumol to cytosolic proteins in intestinal epithelial cells contributes to the poor oral bioavailability observed previously in vivo...
- Metabolism of xanthohumol and isoxanthohumol, prenylated flavonoids from hops (Humulus lupulus L.), by human liver microsomes
Department of Medicinal Chemistry and Pharmacognosy, UIC NIH Center for Botanical Dietary Supplements Research, College of Pharmacy, University of Illinois at Chicago, 833 S Wood Street, Chicago, Illinois 60612 7231, USA
J Mass Spectrom 40:289-99. 2005
..Since XN can be converted to IX through acid-catalyzed cyclization in the stomach, XN might contribute to the in vivo levels of estrogenic 8-PN following consumption of hops extracts...
- Activation of proestrogens from hops (Humulus lupulus L.) by intestinal microbiota; conversion of isoxanthohumol into 8-prenylnaringenin
Laboratory of Microbial Ecology and Technology LabMET, Faculty of Bioscience Engineering, Gent University UGent, Coupure Links 653, Gent, Belgium
J Agric Food Chem 53:6281-8. 2005
- 13C-labelling of xanthohumol in hop cones (Humulus lupulus)
Pharmakognosie and Analytische Phytochemie, Universitat des Saarlandes, Saarbrucken, Germany
Planta Med 71:530-4. 2005
..36 +/- 0.27 % enrichment) confirmed the biosynthetic origin to be MEP pathway-derived. On the basis of these results radiolabelling of Xn will be performed for in vivo bioavailability studies...
- Xanthohumol isolated from Humulus lupulus Inhibits menadione-induced DNA damage through induction of quinone reductase
Birgit M Dietz
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, M C 781, Chicago, Illinois 60612 7231, USA
Chem Res Toxicol 18:1296-305. 2005
..This suggests that XH induces QR by covalently modifying the Keap1 protein. Therefore, XH and hops dietary supplements might function as chemopreventive agents, through induction of detoxification enzymes such as QR...
- Xanthohumol induces apoptosis in cultured 40-16 human colon cancer cells by activation of the death receptor- and mitochondrial pathway
Division of Toxicology and Cancer Risk Factors, German Cancer Research Center, Heidelberg, Germany
Mol Nutr Food Res 49:837-43. 2005
..We conclude that induction of apoptosis by downregulation of Bcl-2 and activation of the caspase cascade may contribute to the chemopreventive or therapeutic potential of XN...
- Xanthohumol and related prenylflavonoids from hops and beer: to your good health!
Jan F Stevens
Department of Chemistry and the Linus Pauling Institute, Oregon State University, 117 Weniger Hall, Corvallis, OR 97331, USA
Phytochemistry 65:1317-30. 2004
..The prenylflavonoid pathway is a possible target for breeding or biotechnological modification of hops with the aim of increasing xanthohumol levels for beer brewing and 8-prenylnaringenin levels for pharmaceutical production...
- Xanthohumol, a prenylflavonoid derived from hops induces apoptosis and inhibits NF-kappaB activation in prostate epithelial cells
Emily C Colgate
Department of Nutrition and Exercise Sciences, Oregon State University, Corvallis, OR 97331, USA
Cancer Lett 246:201-9. 2007
- Effect of hop (Humulus lupulus L.) flavonoids on aromatase (estrogen synthase) activity
Department of Biochemistry, Faculty of Medicine, University of Porto, 4200 319 Porto, Portugal
J Agric Food Chem 54:2938-43. 2006
..In conclusion, prenylflavonoids are able to modulate aromatase activity, decreasing estrogen synthesis, with relevance for the prevention and treatment of estrogen-dependent disorders such as breast cancer...
- Xanthohumol, the chalcone from beer hops (Humulus lupulus L.), is the ligand for farnesoid X receptor and ameliorates lipid and glucose metabolism in KK-A(y) mice
R and D Laboratory, Functional Food Division, Kirin Brewery Co, Ltd, 3 Miyahara, Takasaki, Gunma 370 1295, Japan
Biochem Biophys Res Commun 336:754-61. 2005
..From the present results, it is suggested that XN acts on FXR through a selective bile acid receptor modulator (SBARM) like guggulsterone or polyunsaturated fatty acids, which have previously been reported as SBARMs...
- In vitro glucuronidation of xanthohumol, a flavonoid in hop and beer, by rat and human liver microsomes
Department of Environmental and Molecular Toxicology, Oregon State University, Corvallis 97331, USA
FEBS Lett 491:252-6. 2001
..Release of the aglycone by enzymatic hydrolysis with beta-glucuronidase followed by liquid chromatography/mass spectrometry and nuclear magnetic resonance analysis revealed that these were C-4' and C-4 monoglucuronides of XN...
- Metabolism of the new designer drug alpha-pyrrolidinopropiophenone (PPP) and the toxicological detection of PPP and 4'-methyl-alpha-pyrrolidinopropiophenone (MPPP) studied in rat urine using gas chromatography-mass spectrometry
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D 66421 Homburg Saar, Germany
J Chromatogr B Analyt Technol Biomed Life Sci 796:253-66. 2003
..The same toxicological detection procedure can be applied to other designer drugs of the pyrrolidinophenone type, like MOPPP, MDPPP, MPHP, and MPPP. The detection of the latter will also be presented here...
- Metabolism and toxicological detection of the new designer drug 4'-methoxy-alpha-pyrrolidinopropiophenone studied in rat urine using gas chromatography-mass spectrometry
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D 66421 Homburg Saar, Germany
J Chromatogr B Analyt Technol Biomed Life Sci 793:331-42. 2003
..Based on these data, MOPPP could be detected in urine via its metabolites by full-scan GC-MS using MS for screening and library search for identification by comparison of the spectra with reference spectra...
- Cytotoxic and anticonvulsant aryloxyaryl Mannich bases and related compounds
Sarvesh C Vashishtha
College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N 5C9, Canada
Eur J Med Chem 39:27-35. 2004
..Anticonvulsant properties were demonstrated by a number of compounds in the maximal electroshock (MES) screen when administered intraperitoneally to mice while 4c and 6e afforded protection in the MES test when given orally to rats...
- Enrichment of xanthohumol in the brewing process
Lehrstuhl für Technologie der Brauerei I, TU München Weihenstephan, Germany
Mol Nutr Food Res 49:874-81. 2005
..Results obtained led to a brewing technology that produced on an industrial scale pale wheat beer with more than 1 mg XN/L...
- In vitro phase II metabolism of xanthohumol by human UDP-glucuronosyltransferases and sulfotransferases
Corinna E Ruefer
Institute of Nutritional Physiology, Federal Research Centre for Nutrition and Food, Karlsruhe, Germany
Mol Nutr Food Res 49:851-6. 2005
..Considering the tissue distribution of the tested UGT and SULT enzyme forms, these findings suggest a prominent role for the glucuronidation and sulfation of XN in the liver as well as in the gastrointestinal tract...
- New bioactive chalcones in propolis from El Salvador
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Sofia
Z Naturforsch C 56:593-6. 2001
..The compounds showed significant antibacterial and antifungal activity and moderate toxicity to Artemia salina nauplii...
- Liquid chromatographic enantioseparation of aryl alpha-amino ketones on a crown ether-based chiral stationary phase
Myung Ho Hyun
Department of Chemistry, Pusan National University, Pusan 609 735, Republic of Korea
Biomed Chromatogr 19:208-13. 2005
..60 and 11.10. The chromatographic resolution behaviour was dependent on the type and the content of organic and acidic modifiers and the ammonium acetate concentration in aqueous mobile phase and the column temperature...
- High-performance liquid chromatographic determination of xanthohumol in rat plasma, urine, and fecal samples
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, The University of Mississippi, MS 38677, USA
J Chromatogr Sci 42:378-82. 2004
..XN and its metabolites are excreted mainly in feces within 24 h of administration. The method is a reliable tool for performing studies of XN in different biological material...
- Constituents of Asarum sieboldii with inhibitory activity on lipopolysaccharide (LPS)-induced NO production in BV-2 microglial cells
Ah Reum Han
BK21 Oriental Medical Science Center, College of Oriental Medicine, Kyung Hee University, 1 Hoeki dong, Dongdaemun Gu, Seoul 130 701, Korea
Chem Biodivers 5:346-51. 2008
..Among the ten known isolates, compounds 1, 2, and 5 were found for the first time in this plant...
- Stereoselective biosynthesis of chloroarylpropane diols by the basidiomycete Bjerkandera adusta
P J Silk
Department of Chemical and Biotechnical Services, Research and Productivity Council, 921 College Hill Road, Fredericton, New Brunswick, Canada E3B 6Z9
Chemosphere 52:503-12. 2003
..analogues, as well as into the corresponding alpha-ketols (phenyl acetyl carbinols (PAC's) and 2-hydroxy propiophenones (2-HPP's)) the presumed precursors of the diols...
- Oral muscle relaxant may induce immediate allergic reactions
Gyu Young Hur
Department of Internal Medicine, Korea University College of Medicine, Seoul, Korea
Yonsei Med J 53:863-5. 2012
..Since oral muscle relaxants such as eperisone and afloqualone are commonly prescribed for chronic muscle pain and can induce severe allergic reactions, we should prescribe them carefully...
- Anti-proliferative properties of prenylated flavonoids from hops (Humulus lupulus L.) in human prostate cancer cell lines
Ghent University Ugent, Faculty of Pharmaceutical Sciences, Laboratory of Pharmacognosy and Phytochemistry, and Ghent University Hospital, Department of Endocrinology, Belgium
Phytomedicine 13:732-4. 2006
..4+/-1.1 microM for DU145). DMX was the least active compound. It was evidenced for the first time that this family of prenylated flavonoids from hops effectively inhibits proliferation of prostate cancer cells in vitro...
- Xanthohumol, a new all-rounder?
Mol Nutr Food Res 49:821-3. 2005
- Chiral separation and identification of beta-aminoketones of pharmacological interest by high performance liquid chromatography and capillary electrophoresis
Ana Luisa Simplicio
School of Pharmacy, Trinity College, Dublin 2, Ireland
J Chromatogr A 1120:89-93. 2006
..5-3 using sulfated-beta-cyclodextrin or mixtures of neutral beta-cyclodextrins as chiral selectors...
- Detection and validated quantification of nine herbal phenalkylamines and methcathinone in human blood plasma by LC-MS/MS with electrospray ionization
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, Saarland University, D 66421 Homburg Saar, Germany
J Mass Spectrom 42:150-60. 2007
..The presented LC-MS/MS assay was found applicable for sensitive detection and accurate and precise quantification of all studied analytes in plasma...
- Differential regulation of detoxification enzymes in hepatic and mammary tissue by hops (Humulus lupulus) in vitro and in vivo
Birgit M Dietz
UIC NIH Center for Botanical Dietary Supplements Research, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612, USA
Mol Nutr Food Res 57:1055-66. 2013
..XH induces the detoxification enzyme, NAD(P)H-quinone oxidoreductase (NQO1) in vitro; however, the tissue distribution of XH and 8-prenylnaringenin and their tissue-specific activity have not been analyzed...
- Synthesis, crystal structure and antidiabetic activity of substituted (E)-3-(Benzo [d]thiazol-2-ylamino) phenylprop-2-en-1-one
Vijay S Patil
Department of Organic Chemistry, North Maharashtra University, Jalgaon 425001, India
Eur J Med Chem 59:304-9. 2013
..These compounds were evaluated for their antidiabetic activity, and most of the derivatives of (E)-3-(Benzo [d]thiazol-2-ylamino)phenylprop-2-en-1-one displayed significant antidiabetic activity...
- Simultaneous determination of 4-substituted cathinones (4-MMC, 4-MEC and 4-FMC) in human urine by HPLC-DAD
1Institute of Forensic Medicine, University of Pecs, H 7624 Pecs, Szigeti str 12, Hungary
J Chromatogr Sci 51:861-6. 2013
..The recovery rate of SPE was between 71 and 82% with a lower relative standard deviation than 2.35%. ..
- The molecular organization of prenylated flavonoid xanthohumol in DPPC multibilayers: X-ray diffraction and FTIR spectroscopic studies
Department of Biophysics, University of Life Sciences in Lublin, Akademicka 13, 20 950 Lublin, Poland
Biochim Biophys Acta 1828:213-22. 2013
..This is in compliance with reported changes in FTIR spectra where at pretransition XN moves from interface region between polar heads to the neighborhood of phosphate groups...
- Phenylpropene diglycosides from the bark of Machilus wangchiana
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China
J Asian Nat Prod Res 14:1046-53. 2012
..Their structures were determined by spectroscopic and chemical methods. In the preliminary assay, compounds 2 and 5-8 reduced dl-galactosamine (GalN)-induced hepatocyte (WB-F344 cells) damage with 37-41% inhibitions at 10 μM...
- Synthesis, characterization and biological evaluation of novel neutral fac-M(CO)3(SNO) complexes (M=Re, 99mTc) bearing the o-methoxyphenylpiperazine moiety
Institute of Radioisotopes, Radiodiagnostic Products, National Centre for Scientific Research Demokritos, Athens, Greece
Appl Radiat Isot 70:957-64. 2012
..Biodistribution studies in healthy animals showed high initial blood and liver uptake, fast blood and tissue depuration and negligible brain uptake...
- Protective effect of xanthohumol on toxin-induced liver inflammation and fibrosis
Department of Internal Medicine I, University Hospital Regensburg, Germany
Int J Clin Exp Pathol 5:29-36. 2012
..Thus, this study further indicates the potential of xanthohumol application to prevent or ameliorate the development and progression of liver fibrosis in response to hepatic injury...
- Protective effects of xanthohumol against the genotoxicity of heterocyclic aromatic amines MeIQx and PhIP in bacteria and in human hepatoma (HepG2) cells
Faculdade de Ciencias da Nutricao e Alimentacao da Universidade do Porto, Rua Dr Roberto Frias, 4200 465 Porto, Portugal
Food Chem Toxicol 50:949-55. 2012
..Our findings confirm the evidence that XN displays strong chemopreventive effects against genotoxicity of HAAs, and provides additional mechanistic information to assess its potential chemopreventive efficiency in humans...
- Flavonoid production in transgenic hop (Humulus lupulus L.) altered by PAP1/MYB75 from Arabidopsis thaliana L
Plant Breeding and Biotechnology, Institute for Plant Breeding, Seed Science and Population Genetics, University of Hohenheim, Stuttgart, Germany
Plant Cell Rep 31:111-9. 2012
- Polyphenols in alcoholic beverages activating constitutive androstane receptor CAR
Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Bunkyo ku, Tokyo, Japan
Biosci Biotechnol Biochem 75:1635-7. 2011
..Since CAR regulates many genes involved in energy metabolism, the possibility exists that these polyphenols would reduce the risk of certain alcohol-induced metabolic disorders with the help of CAR...
- [Encephalopathy caused by intravenous potassium permanganate used for illegal production of methcathinone (ephedrone) from medicines containing pseudoephedrine]
Zespół Profilaktyki i Leczenia Uzaleznień, Instytutu Psychiatrii i Neurologii w Warszawie
Przegl Lek 70:613-6. 2013
..Elimination of manganese with the use of chelating therapy as well as symptomatic treatment, mainly with the antyparkinsonic drugs, seems to be ineffective...
- Characterization of human cytochrome P450 enzymes involved in the biotransformation of eperisone
H H Yoo
Korea Institute of Science and Technology KIST, Doping Control Center, Seoul, Korea
Xenobiotica 39:1-10. 2009
..In addition, intestinal microsomes metabolized eperisone to M3 and M4 via CYP2J2- and CYP3A4-mediated reactions, which are supposed to contribute to presystemic metabolism of eperisone...
- Efficacy and safety of eperisone in patients with low back pain: a double blind randomized study
Clinica Ortopedica, Dipartimento di Scienze Medico Chirurgiche dell Università degli Studi di Milano, San Donato Milanese, Italy
Eur Rev Med Pharmacol Sci 12:229-35. 2008
..In conclusions, eperisone represents a valuable and safer alternative to other muscle relaxant agents for treatment of low back pain...
- Effect of xanthohumol on melanogenesis in B16 melanoma cells
Jeung Hyun Koo
Department of Biochemistry, Medical School and Institute for Medical Sciences, Chonbuk National University, Jeonju, Korea
Exp Mol Med 40:313-9. 2008
..These results suggest that XH might act as a hypo-pigmenting agent through the downregulation of MITF in the cAMP-dependent melanogenic pathway...
- Antimutagenicity of hops (Humulus lupulus L.): bioassay-directed fractionation and isolation of xanthohumol
Department of Pharmaceutical Biology, Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia
Phytomedicine 15:216-20. 2008
..These results indicate that xanthohumol is a very promising potential protective agent against genotoxicity of food borne carcinogens, which warrants further investigation...
- A protein-encapsulation technique by the sol-gel method for the preparation of monolithic columns for capillary electrochromatography
Department of Analytical Chemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan
Anal Chem 74:1915-21. 2002
..23% for the first peak, N = 10). Under optimized conditions, the theoretical plate number for the first peak of benzoin reached 72,000 plates/m...
- New prenylchalcones from the hops of Humulus lupulus
Wen Shu Wang
College of Chemistry and Molecular Engineering, Peking University, Beijing, China
J Asian Nat Prod Res 10:485-90. 2008
..Among the new prenylchalcones, compound 2 showed marginal cytotoxic activity against human stomach carcinoma BGC-823 and human hepatic carcinoma HepG2 cells...
- Interaction of prenylated chalcones and flavanones from common hop with phosphatidylcholine model membranes
Department of Biophysics, Wroclaw Medical University, ul Chalubinskiego 10, 50 368 Wroclaw, Poland Electronic address
Biochim Biophys Acta 1838:173-84. 2014
..It was assumed that IXH-rich and IXH-poor microdomains appeared within membrane. Present work constitutes the first experimental report describing interactions of prenylated hop polyphenols with phospholipid model membranes. ..
- Xanthohumol stimulates iodide uptake in rat thyroid-derived FRTL-5 cells
Institut für Experimentelle Endokrinologie und Endokrinologisches, Forschungszentrum EnForCé, Charite Universitatsmedizin Berlin, Berlin, Germany
Mol Nutr Food Res 49:832-6. 2005
- Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone
Sang In Yang
Laboratory of Pharmacology, College of Pharmacy, Sungkyunkwan University, Suwon, Korea
Pharmacology 71:150-6. 2004
..The transdermal patch form of eperisone will increase the efficacy and compliance in the clinical use of eperisone...
- [Assessment of the action of Sadamine Polfa and Mydocalm Richter preparations as based on photoplethysmography]
Pol Tyg Lek 30:2093-6. 1975
- A new 5-lipoxygenase selective inhibitor derived from Artocarpus communis strongly inhibits arachidonic acid-induced ear edema
Department of Pharmacology, Tokyo Metropolitan Institute of Gerontology, Japan
Biochem Pharmacol 37:2161-5. 1988
..Since the natural compound AC-5-1 can selectively inhibit 5-lipoxygenase and affect in vivo inflammation, it will be interesting to investigate the role of leukotrienes on inflammation and other physiological processes...
- Quantitative analysis of xanthohumol and related prenylflavonoids in hops and beer by liquid chromatography-tandem mass spectrometry
J F Stevens
Department of Chemistry, Oregon State University, Corvallis 97331, USA
J Chromatogr A 832:97-107. 1999
..Thirteen commercial beers were analysed with the method. Isoxanthohumol, formed by isomerization of xanthohumol during the brewing process, was the most abundant flavonoid in hopped beers, ranging from 0.04 to 3.44 mg/l...
- Inhibition of plasma membrane monoamine transporters by beta-ketoamphetamines
N V Cozzi
Department of Pharmacology, East Carolina University School of Medicine, Greenville, NC 27858, USA
Eur J Pharmacol 381:63-9. 1999
..Our results indicate that methcathinone and methylone potently inhibit plasma membrane catecholamine transporters but only weakly inhibit the vesicle transporter...
- Xanthohumol metabolites in faeces of rats
Institute for Pharmacognosy and Analytical Phytochemistry, University of the Saarland, 66041 Saarbrucken, Germany
Phytochemistry 65:561-70. 2004
..Their structures were elucidated by spectroscopic methods, especially using NMR spectroscopy. Twenty metabolites had a modified chalcone structure and two metabolites were flavanone derivatives...
- Relationship between the crystallization rates of amorphous nifedipine, phenobarbital, and flopropione, and their molecular mobility as measured by their enthalpy relaxation and (1)H NMR relaxation times
Division of Drugs, National Institute of Health Sciences, 1 18 1, Kamiyoga, Setagaya Ku, Tokyo 158, Japan
J Pharm Sci 89:408-16. 2000
..The faster crystallization of nifedipine than that of phenobarbital or flopropione observed at temperatures below its T(g) may be partly ascribed to its higher molecular mobility at these temperatures...
- Effects of TAK-637, a tachykinin receptor antagonist, on the micturition reflex in guinea pigs
Pharmaceutical Research Division, Takeda Chemical Industries, Ltd, 2 17 85, Jusohonmachi, Yodogawa ku, Osaka, Japan
Eur J Pharmacol 395:241-6. 2000
..Therefore, TAK-637 may represent a new class of drugs, which would be effective for abnormally frequent micturition without causing voiding difficulties due to decreased voiding pressure...
- Identification of cytochrome p450 enzymes involved in the metabolism of 4'-methyl-alpha-pyrrolidinopropiophenone, a novel scheduled designer drug, in human liver microsomes
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, Building 46, D 66421 Homburg Saar, Germany
Drug Metab Dispos 31:979-82. 2003
..01) turnover inhibition (11.8 +/- 1.6% of control). Based on kinetic data corrected for the relative activity factors, CYP2D6 is the enzyme mainly responsible for MPPP hydroxylation, confirmed by CYP2D6 inhibition studies...
- Biosynthetic (14)C-labelling of xanthohumol in hop cones
Pharmakognosie und Analytische Phytochemie, Universitat des Saarlandes, Saarbrucken, Germany
Mol Nutr Food Res 49:857-60. 2005
..Delivering the radioactive precursor at once resulted in Xn with a specific activity of 318 microCi.mmol(-1); if however the amount was supplied in aliquots over 4 days a specific activity of only 53.1 microCi.mmol(-1) Xn was obtained...
- Functional discovery via a compendium of expression profiles
T R Hughes
Rosetta Inpharmatics, Inc, Kirkland, Washington 98034, USA
Cell 102:109-26. 2000
..We also show that the compendium can be used to characterize pharmacological perturbations by identifying a novel target of the commonly used drug dyclonine...
- Fundamentals and health benefits of xanthohumol, a natural product derived from hops and beer
Paulo J Magalhães
REQUIMTE, Departamento de Química da Faculdade de Ciências da Universidade do Porto, Rua do Campo Alegre, 687, 4169 007 Porto, Portugal
Nat Prod Commun 4:591-610. 2009
..This paper reviews recent and important data with respect to the health benefits or biological activities of xanthohumol and beer. In addition, an overview of the chemistry and biotechnological aspects of xanthohumol is presented...
- Pitfalls in cell culture work with xanthohumol
Department of Pharmaceutical Biology, University of Regensburg, Germany
Pharmazie 67:91-4. 2012
..In contrast, experiments using fluorescence microscopy in living cells revealed that detection of cellular intake of xanthohumol is hampered by concentrations above 1% FCS...
- Triggering of dendritic cell apoptosis by xanthohumol
Nguyen Thi Xuan
Department of Physiology, University of Tubingen, Tubingen, Germany
Mol Nutr Food Res 54:S214-24. 2010
..In conclusion, xanthohumol stimulated Asm leading to caspase activation and apoptosis of bone marrow-derived DCs...
- New designer drug 4'-methyl-alpha-pyrrolidinohexanophenone: studies on its metabolism and toxicological detection in urine using gas chromatography-mass spectrometry
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D 66421 Saar, Homburg, Germany
J Chromatogr B Analyt Technol Biomed Life Sci 789:79-91. 2003
..The carboxy and/or hydroxy groups were found to be only partly conjugated. Based on these data, MPHP could be detected in urine via its metabolites by GC-MS using mass chromatography for screening and library search for identification...
- Xanthohumol inhibits growth and vascularization of developing endometriotic lesions
Institute for Clinical and Experimental Surgery, University of Saarland, Saar, Germany
Hum Reprod 27:1735-44. 2012
..In the present study, we analyzed, for the first time, whether this dietary compound may also be used for the treatment of endometriosis...
- Clinical, neuroimaging and neurophysiological features in addicts with manganese-ephedrone exposure
Department of Neurology and Neurosurgery, University of Tartu, Estonia
Acta Neurol Scand 121:237-43. 2010
..To identify biomarkers supporting the clinical diagnosis of manganism in patients several years after exposure to manganese (Mn)...
- Pharmacological properties of NK433, a new centrally acting muscle relaxant
Research Laboratories, Pharmaceuticals Group, Nippon Kayaku Co Ltd, Tokyo, Japan
Eur J Pharmacol 273:47-56. 1995
..In i.v. experiments, the effects of NK433 on decerebrate rigidities were similar to those of eperisone-HCl and tolperisone-HCl, but in p.o. experiments, NK433 was at least 3 times as potent as eperisone-HCl and tolperisone-HCl...
- Xanthohumol induces phase II enzymes via Nrf2 in human hepatocytes in vitro
Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Poznan, Poland
Toxicol In Vitro 27:149-56. 2013
..On the other hand its cytotoxicity towards HCC cells shown in this study indicates that it may also be considered as potentially chemotherapeutic...
- The evolution of sunscreen products in the United States--a 12-year cross sectional study
Steven Q Wang
Memorial Sloan Kettering Cancer Center, New York, NY, USA
Photochem Photobiol Sci 12:197-202. 2013
..In the past decade, sunscreen products have undergone fundamental improvements, the most significant of which is the breadth of protection against UVA I...
- Xanthohumol-supplemented beer modulates angiogenesis and inflammation in a skin wound healing model. Involvement of local adipocytes
Department of Biochemistry U38 FCT, University of Porto, Porto 4200 319, Portugal
J Cell Biochem 113:100-9. 2012
- Enantioselective carbonyl reduction of eperisone in human liver microsomes
Hye Hyun Yoo
College of Pharmacy, Hanyang University, Ansan, Gyeonggi, Korea
Xenobiotica 41:758-63. 2011
..Carbonyl reduction of eperisone by microsomal 11β-HSD 1 may significantly contribute to the metabolic disposition of eperisone in human and (-)-R-isomer is preferentially reduced by this enzyme...
- Regulation of intracellular pH by glycosaminoglycans
Institute of Physiological Chemistry and Pathobiochemistry, Muenster University, Hospital, Munster, Germany
J Cell Physiol 228:2071-5. 2013
..These observations indicated that extracellular glycosaminoglycans participate in intracellular pH regulation. The mechanism was explained by Donnan effects and molecular crowding...
- Xanthohumol decreases Notch1 expression and cell growth by cell cycle arrest and induction of apoptosis in epithelial ovarian cancer cell lines
Jessica G Drenzek
Department of Obstetrics and Gynecology, The University of Wisconsin School of Medicine and Public Health, Madison, WI 53792, USA
Gynecol Oncol 122:396-401. 2011
..We hypothesized that the Notch1 signaling pathway is targeted by xanthohumol leading to decreased ovarian cancer cell growth...
- A metabolomics-driven elucidation of the anti-obesity mechanisms of xanthohumol
Jay S Kirkwood
Linus Pauling Institute and the Department of Pharmaceutical Sciences, Oregon State University, Corvallis, Oregon 97331, USA
J Biol Chem 288:19000-13. 2013
..In addition, time course metabolomics appears to be an effective strategy for uncovering metabolic events that occur during a stress response. ..
- Effects of 3-(2-Hydroxyphenyl)-1-(5-methyl-furan-2-y-l) propenone (HMP) upon signalling pathways of lipopolysaccharide-induced iNOS synthesis in RAW 264.7 cells
Choi Yi Liew
Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia
Int Immunopharmacol 11:85-95. 2011
..We conclude that the synthetic HMP is a chalcone analogue that selectively inhibits the p38/ATF-2 and AP-1 signaling pathways in the NO synthesis by the macrophage RAW 264.7...
- Characterization of the UVA protection provided by avobenzone, zinc oxide, and titanium dioxide in broad-spectrum sunscreen products
Donathan G Beasley
Merck Consumer Care, Memphis, Tennessee 38151, USA
Am J Clin Dermatol 11:413-21. 2010
..To sustain its absorption capacity within a sunscreen film during UVR exposure, avobenzone needs to be formulated into sunscreen products using sound formulation strategies...
- Xanthohumol induces apoptosis in human malignant glioblastoma cells by increasing reactive oxygen species and activating MAPK pathways
Dipartimento di Scienze Farmaceutiche e Biomediche, Universita degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy
J Nat Prod 74:2505-13. 2011
..These findings suggest that xanthohumol (1) is a potential chemotherapeutic agent for the treatment of glioblastoma multiforme...
- TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats
Joseph F Cotten
Department of Anesthesia, Critical Care, and Pain Medicine, Massachusetts General Hospital, GRB 444, 55 Fruit St, Boston, MA 02114, USA
Anesth Analg 116:810-6. 2013
..PK-THPP and A1899 are potent and selective TASK-1 and TASK-3 antagonists. I hypothesized PK-THPP and A1899 are, like doxapram, breathing stimulants...
- A disposable simultaneous electrochemical sensor array based on a molecularly imprinted film at a NH2-graphene modified screen-printed electrode for determination of psychotropic drugs
Key Laboratory of Chemical Sensing and Analysis in Universities of Shandong, University of Jinan, Jinan 250022, China
Analyst 138:2704-11. 2013
..The disposable simultaneous strategy avoided crosstalk and the need of deoxygenation for the electrochemical sensor, thus, provided a promising potential in clinical applications...
- Preliminary in vitro study on the effect of xanthohumol on rumen methanogenesis
Department of Animal Nutrition and Feed Management, Poznan University of Life Sciences, Poznan, Poland
Arch Anim Nutr 66:66-71. 2012
..However, the practical utility of this supplement needs further investigation under long-term in vivo conditions...
- Xanthohumol prevents carbon tetrachloride-induced acute liver injury in rats
Department of Biochemistry and Molecular Biology, Science Faculty, Extremadura University, Av Elvas s n, 06006 Badajoz, Spain
Food Chem Toxicol 50:3405-12. 2012
- Polyamide nanocapsules and nano-emulsions containing Parsol® MCX and Parsol® 1789: in vitro release, ex vivo skin penetration and photo-stability studies
Faculty of Pharmacy, University of Paris Sud 11 UMR CNRS 8612, 5 rue J B Clement, 92296, Chatenay Malabry Cedex, France
Pharm Res 29:559-73. 2012
..To prepare polyamide nanocapsules for skin photo-protection, encapsulating α-tocopherol, Parsol®MCX (ethylhexyl methoxycinnamate) and/or Parsol®1789 (butyl methoxydibenzoylmethane)...
- Analytical characterization of three trifluoromethyl-substituted methcathinone isomers
Simon D Brandt
School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, Byrom Street, Liverpool L3 3AF, UK
Drug Test Anal 4:525-9. 2012
- Geranyl derivative of phloroacetophenone induces cancer cell-specific apoptosis through Bax-mediated mitochondrial pathway in MCF-7 human breast cancer cells
Mi Yeon Cho
College of Pharmacy, Yeungnam University, Yeungnam University 214 1 Dae Dong, Gyeongsan, Gyungbuk 712 749, Republic of Korea
Biol Pharm Bull 35:98-104. 2012
..The present results indicate that synthetic 3-GAP is a safe and effective anti-cancer agent, and the Bax-mediated mitochondrial pathway is the main apoptosis signaling pathway of 3-GAP in MCF-7 cells...
- Pharmacological examination of trifluoromethyl ring-substituted methcathinone analogs
Nicholas V Cozzi
Neuropharmacology Laboratory, 2695 Medical Sciences Center, Department of Cell and Regenerative Biology, University of Wisconsin School of Medicine and Public Health, 1300 University Avenue, Madison, WI 53706, USA
Eur J Pharmacol 699:180-7. 2013
..The TFMAPs might have a therapeutic value for a variety of medical and psychiatric conditions and may have lower abuse liability compared to methcathinone due to their decreased DAT activity...
- Sun protection strength of a hydroquinone 4%/retinol 0.3% preparation containing sunscreens
Joseph W Stanfield
Suncare Research Laboratories, LLC, Winston Salem, NC, USA
J Drugs Dermatol 5:321-4. 2006
..Formulas containing hydroquinone 4% are effective in these conditions. Since exposure to ultraviolet radiation (UVR) can worsen disease and complicate treatment, the incorporation of sunscreens can avert this problem...
- Antidepressants, metabolites, and apparent drug resistance
W Z Potter
Section on Clinical Pharmacology, National Institute of Mental Health, Bethesda, MD 20892
Clin Neuropharmacol 13:S45-53. 1990
..Finally, principles are deduced for identifying those cases in which metabolic considerations are most likely to be relevant to observed drug resistance...