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Shuhao Su, Meng Cao, Guangyuan Wu, Zi Long, Xiaodong Cheng, Junshu Fan, Zhongrui Xu, Hongfei Su, Yiming Hao, Ge Li, Jie Peng, Shuang Li, Xin Wang
The worldwide prevalence of diabetes and associated metabolic diseases has dramatically increased. Pharmacological treatment of diabetes is still limited. Hordenine (HOR), a phenethylamine alkaloid, is a natural constituent in many plants. The present study was designed to explore the possible anti-diabetic effect of HOR in streptozotocin (STZ)-induced diabetic mice. Combined treatment of HOR and insulin significantly reduced fasting and postprandial blood glucose level in diabetic mice. HOR and insulin did not show evident protective effect against structural and functional injuries of pancreas...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Miho Chikazawa, Ryuichiro Sato
Maintaining skeletal muscle functions by controlling muscle metabolism is of utmost importance. β2 -Adrenergic receptor (β2 -AR), which is expressed in skeletal muscle, is a member of the G-protein-coupled receptor family that plays a critical role in the maintenance of muscle mass. In the present study, using luciferase reporter assays in β2 -AR-expressing HEK293 cells, we discovered several food factors that exhibited agonistic activity at mouse or human β2 -AR. Osthole, gramine, and hordenine were identified as both mouse and human β2 -AR agonists, whereas berberine was identified as a mouse β2 -AR agonist only...
2018: Journal of Nutritional Science and Vitaminology
Jianping Zhao, Mei Wang, Bharathi Avula, Ikhlas A Khan
Phenethylamines (PEAs) are popular substances found in weight-loss and sports nutrition supplements. They are generally pharmacologically active and primarily affect the sympathetic nervous system. Many PEAs are synthetic chemicals and are on the prohibited list of the World Anti-Doping Agency. In this study, nuclear magnetic resonance (NMR) spectroscopy was applied to detect and identify the presence of PEAs in sports dietary supplements without the need for chromatographic separation or pre-knowledge on formulation...
March 20, 2018: Journal of Pharmaceutical and Biomedical Analysis
Jin-Wei Zhou, Huai-Zhi Luo, Huan Jiang, Ting-Kun Jian, Zi-Qian Chen, Ai-Qun Jia
The quorum sensing (QS) inhibitory activity of hordenine from sprouting barley against foodborne pathogen Pseudomonas aeruginosa was evaluated for the first time here. At concentrations ranging from 0.5 to 1.0 mg mL-1 , hordenine inhibited the levels of acyl-homoserine lactones. The enhanced susceptibility of hordenine with netilmicin on P. aeruginosa PAO1 biofilm formation as well as their efficiency in disrupting preformed biofilms was also evaluated using scanning electron microscopy and confocal laser scanning microscopy (CLSM)...
February 21, 2018: Journal of Agricultural and Food Chemistry
Jobina Rajkumari, Himani Meena, Muralitharan Gangatharan, Siddhardha Busi
Pseudomonas aeruginosa is a notorious pathogen that causes biofilm aided infections in patients with cystic fibrosis and burn wounds, resulting in significant mortality in immunocompromised individuals. This study reports a novel one-step biosynthesis of gold nanoparticles using phytocompound, hordenine (HD), as a reducing and capping agent. The synthesis of the anisotropic hordenine-fabricated gold nanoparticles (HD-AuNPs) with an average particle size of 136.87 nm was achieved within 12 h of incubation at room temperature...
December 2017: IET Nanobiotechnology
Kishore Natte, Helfried Neumann, Rajenahally V Jagadeesh, Matthias Beller
N-Methylated amines play an important role in regulating the biological and pharmaceutical properties of all kinds of life science molecules. In general, this class of compounds is synthesized via reductive amination reactions using high pressure of molecular hydrogen. Thus, on laboratory scale especially in drug discovery, activated (toxic) methyl compounds such as methyl iodide and dimethyl sulfate are still employed, which also generate significant amounts of waste. Therefore, the development of more convenient and operationally simple processes for the synthesis of advanced N-methylamines is highly desired...
November 7, 2017: Nature Communications
Marwa Bannour, Dirk W Lachenmeier, Irene Straub, Matthias Kohl-Himmelseher, Ayda Khadhri, Samira Aschi-Smiti, Thomas Kuballa, Hanchi Belgacem
This study is the first to evaluate the potential of Calligonum azel Maire as a food ingredient. The plant materials flowers, leaves, stems and roots were analyzed by wet-chemical and instrumental methods for major and minor composition. The highest protein and sugar contents were recorded in the flowers (17.8% and 1.6% respectively), while the fat content was most abundant in the leaves (2.9%). Hexane extracts screened by gas chromatography (GC) for fatty acid composition showed 14 major compounds such as oleic acid, linoleic acid and palmitic acid, but also ω3 and ω6 unsaturated fatty acids...
November 2016: Food Research International
Hankum Park, Jaeyoung Ha, Ja Young Koo, Jongmin Park, Seung Bum Park
Target engagement is a prerequisite for the therapeutic effects of bioactive small molecules, and unbiased identification of their target proteins can facilitate drug discovery and chemical biology research. Structural modifications of bioactive natural products for target identification exhibit potential limitations such as synthetic difficulties, limited supplies from natural sources, and loss of original efficacy. Herein, we developed a label-free method for proteome-wide target identification using in-gel fluorescence difference caused by thermal stability shift, namely TS-FITGE...
February 1, 2017: Chemical Science
Thomas Sommer, Harald Hübner, Ahmed El Kerdawy, Peter Gmeiner, Monika Pischetsrieder, Timothy Clark
The dopamine D2 receptor (D2R) is involved in food reward and compulsive food intake. The present study developed a virtual screening (VS) method to identify food components, which may modulate D2R signalling. In contrast to their common applications in drug discovery, VS methods are rarely applied for the discovery of bioactive food compounds. Here, databases were created that exclusively contain substances occurring in food and natural sources (about 13,000 different compounds in total) as the basis for combined pharmacophore searching, hit-list clustering and molecular docking into D2R homology models...
March 10, 2017: Scientific Reports
Árpád Könczöl, Kata Rendes, Miklós Dékány, Judit Müller, Eszter Riethmüller, György Tibor Balogh
The linkage between the central nervous system availability and neuropharmacological activity of the constituents of Ginkgo biloba L. extracts (GBE) is still incomplete. In this study, the in vitro blood-brain barrier (BBB) permeability profile of the standardised GBE was investigated by the parallel artificial membrane permeability assay (PAMPA). Biomarkers, such as terpene trilactones, flavonoid aglycones and ginkgotoxin exerted moderate or good BBB-permeability potential (BBB+), while glycosides and biflavones were predicted as unable to pass the BBB...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
Irina Steiner, Gernot Brauers, Oliver Temme, Thomas Daldrup
We present the determination of the alkaloid hordenine and its forensic relevance as a qualitative and quantitative marker for beer consumption. A simple, rapid and sensitive ultra-performance liquid chromatography (UPLC)-tandem mass spectrometry (MS/MS) method for the determination of hordenine in human serum samples was developed and validated. The application was tested with serum samples after enzymatic cleavage. After addition of the synthesized internal standard hordenine-D 4, a liquid-liquid extraction with dichloromethane and diethyl ether was performed...
March 2016: Analytical and Bioanalytical Chemistry
Ashton D Lesiak, Robert B Cody, Masaaki Ubukata, Rabi A Musah
We demonstrate the utility of direct analysis in real time ionization coupled with high resolution time-of-flight mass spectrometry (DART-HRTOFMS) in revealing the adulteration of commercially available Sceletium tortuosum, a mind-altering plant-based drug commonly known as Kanna. Accurate masses consistent with alkaloids previously isolated from S. tortuosum plant material enabled identification of the products as Kanna, and in-source collision-induced dissociation (CID) confirmed the presence of one of these alkaloids, hordenine, while simultaneously revealing the presence of an adulterant...
March 2016: Forensic Science International
Carine Viana, Gabriela M Zemolin, Larissa S Müller, Thaís R Dal Molin, Helena Seiffert, Leandro M de Carvalho
Methyl-xanthines and adrenergic stimulants, such as caffeine and synephrine, are commonly added to food supplements due to their stimulating and thermogenic effects. In addition, the abusive consumption of food supplements with ergogenic and aesthetic purposes has been observed worldwide. This work describes the study of caffeine, p-synephrine, hordenine, octopamine, tyramine, ephedrine and salicin as stimulants in dietary supplements marketed in Brazil for weight loss and physical fitness claims. A total of 94 different products were acquired from 30 Brazilian websites...
2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Nícolas de Castro Campos Pinto, Ana Paula do Nascimento Duque, Natália Ramos Pacheco, Renata de Freitas Mendes, Erick Vicente da Silva Motta, Paula Maria Quaglio Bellozi, Antônia Ribeiro, Marcos José Salvador, Elita Scio
CONTEXT: Pereskia aculeata Miller (Cactaceae) is a cactus distributed from south to northeast of Brazil, where its leaves are commonly used as a vegetable, in skin wound healing, and to treat inflammation. OBJECTIVES: The objective of this study was to perform the chemical characterization and to evaluate the antinociceptive activity of the hydromethanolic fraction obtained from the methanol extract of P. aculeata leaves. MATERIALS AND METHODS: Chemical characterization was performed by UPLC-MS analysis...
2015: Pharmaceutical Biology
Jianshe Ma, Shuanghu Wang, Xueli Huang, Peiwu Geng, Congcong Wen, Yunfang Zhou, Linsheng Yu, Xianqin Wang
Hordenine is an active compound found in several foods, herbs and beer. In this work, a sensitive and selective UPLC-MS/MS method for determination of hordenine in rat plasma was developed. After addition of caulophylline as internal standard (IS), protein precipitation by acetonitrile-methanol (9:1, v/v) was used as sample preparation. Chromatographic separation was achieved on a UPLC BEH HILIC (2.1 mm × 100 mm, 1.7 μm) with acetonitrile (containing 10mM ammonium formate) and water (containing 0.1% formic acid and 10 mM ammonium formate) as mobile phase with gradient elution...
2015: Journal of Pharmaceutical and Biomedical Analysis
Shuanghu Wang, Haiya Wu, Xueli Huang, Peiwu Geng, Congcong Wen, Jianshe Ma, Yunfang Zhou, Xianqin Wang
In this work, a sensitive and selective UPLC-MS/MS method for determination of N-methylcytisine in rat plasma is developed. After addition of hordenine as an internal standard (IS), protein precipitation by acetonitrile-methanol (9:1, v/v) was used to prepare samples. Chromatographic separation was achieved on a UPLC BEH HILIC (2.1 mm×100mm, 1.7μm) with acetonitrile (containing 10mM ammonium formate) and water (containing 0.1% formic acid and 10mM ammonium formate) as the mobile phase with gradient elution...
May 15, 2015: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Yonggang Chen, Junhua Meng, Jili Zou, Jing An
Hordenine is an active compound found in several foods, herbs and beer. In this work, a novel sorbent was fabricated for selective solid-phase extraction (SPE) of hordenine in biological samples. The organic polymer sorbent was synthesized in one step in the plastic barrel of a syringe by a pre-polymerization solution consisting of methacrylic acid (MAA), 4-vinylphenylboronic acid (VB) and ethylene glycol dimethacrylate (EGDMA). The conditions for preparation were optimized to generate a poly(MAA-VB-EGMDA) monolith with good permeability...
June 2015: Biomedical Chromatography: BMC
Amélie Beury-Cirou, Mélanie Tannières, Corinne Minard, Laurent Soulère, Tsiry Rasamiravaka, Robert H Dodd, Yves Queneau, Yves Dessaux, Catherine Guillou, Olivier M Vandeputte, Denis Faure
N-acylhomoserine lactone (AHL)-mediated quorum-sensing (QS) regulates virulence functions in plant and animal pathogens such as Agrobacterium tumefaciens and Pseudomonas aeruginosa. A chemolibrary of more than 3500 compounds was screened using two bacterial AHL-biosensors to identify QS-inhibitors (QSIs). The purity and structure of 15 QSIs selected through this screening were verified using HPLC MS/MS tools and their activity tested on the A. tumefaciens and P. aeruginosa bacterial models. The IC50 value of the identified QSIs ranged from 2...
2013: PloS One
Frank Musshoff, Lidia Hottmann, Cornelius Hess, Burkhard Madea
The appearance of dangerous and insufficiently studied designer drugs has increased substantially within the last few years. Mixtures containing centrally active compounds are often declared as "bath salt", "incense", "plant food", "bong cleaners" and are marketed in head shops and on the Internet. As the majority of the ingredients of such products are not subject to regulations of the German Narcotics Law (Betäubungsmittelgesetz, BtMG), the vendors and consumers mistake the sale of such products for legal...
September 2013: Archiv Für Kriminologie
E Meyer
Hordenine is biosynthesized in young roots of barley by subsequent N-methylation of tyramine. It was shown that two distinct enzymes are responsible for these methylation reactions. They differed in their pH-optimum, their stability in dependence of the pH-value, and were partially resolved by DEAE-chromatography. More than 200-fold purification and almost complete separation were achieved by elution of the enzymes from an affinity column which was prepared by coupling S-adenosylhomocysteine to aminohexyl-Sepharose 4 B...
December 1982: Plant Cell Reports
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