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Bipradas Roy, Mary E Curtis, Letimicia S Fears, Samuel N Nahashon, Hugh M Fentress
Obesity and osteoporosis are two alarming health disorders prominent among middle and old age populations, and the numbers of those affected by these two disorders are increasing. It is estimated that more than 600 million adults are obese and over 200 million people have osteoporosis worldwide. Interestingly, both of these abnormalities share some common features including a genetic predisposition, and a common origin: bone marrow mesenchymal stromal cells. Obesity is characterized by the expression of leptin, adiponectin, interleukin 6 (IL-6), interleukin 10 (IL-10), monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-alpha (TNF-α), macrophage colony stimulating factor (M-CSF), growth hormone (GH), parathyroid hormone (PTH), angiotensin II (Ang II), 5-hydroxy-tryptamine (5-HT), Advance glycation end products (AGE), and myostatin, which exert their effects by modulating the signaling pathways within bone and muscle...
2016: Frontiers in Physiology
Jordy M Saya, Barry Oppelaar, Răzvan C Cioc, Gydo van der Heijden, Christophe M L Vande Velde, Romano V A Orru, Eelco Ruijter
We report a highly diastereoselective interrupted Ugi reaction to construct a broad range of structurally congested and stereochemically complex spiroindolines from tryptamine-derived isocyanides. The reaction is facilitated by using fluorinated alcohols (TFE or HFIP) as solvents and tolerates a broad range of amines, aldehydes and 2-isocyanoethylindoles to give polycyclic products in moderate to excellent yields.
October 13, 2016: Chemical Communications: Chem Comm
Ashley C Lindsay, Ivanhoe K H Leung, Jonathan Sperry
The total synthesis of the azepinobisindole alkaloid iheyamine A is described. The successful strategy hinged on an intermolecular cross-Mannich reaction between 5-methoxy-3-acetoxyindole and a protected tryptamine to access an unsymmetrical 2,2'-bisindole, which was subsequently converted into iheyamine A via a deep-blue 3-indolone intermediate. VT (1)H NMR infers that iheyamine A exists as a mixture of tautomers that undergo intermediate chemical exchange on the NMR time scale. The intermolecular cross-Mannich reaction described herein is a viable alternative to metal-catalyzed cross-coupling strategies commonly employed to access 2,2'-bisindoles...
October 5, 2016: Organic Letters
Markus R Meyer
This review article covers English-written and PubMed-listed review articles and original studies published between January 2015 and April 2016 dealing with the toxicodynamics and toxicokinetics of new psychoactive substances. Compounds covered include stimulants and entactogens, synthetic cannabinoids, tryptamines, NBOMes, phencyclidine-like drugs, benzodiazepines, and opioids. First, an overview and discussion is provided on timely review articles followed by an overview and discussion on recent original studies...
October 2016: Archives of Toxicology
Liliang Li, Yuhua Li, Junyi Lin, Jieqing Jiang, Meng He, Daming Sun, Ziqin Zhao, Yiwen Shen, Aimin Xue
BACKGROUND It is not uncommon that only mild coronary artery stenosis is grossly revealed after a system autopsy. While coronary artery spasm (CAS) is the suspected mechanism of these deaths, no specific biomarker has been identified to suggest antemortem CAS. MATERIAL AND METHODS To evaluate the potential of using phosphorylated myosin light chain 2 (p-MLC2) as a diagnostic marker of antemortem CAS, human vascular smooth muscle cells (VSMCs) were cultured and treated with common vasoconstrictors, including prostaglandins F2α (PGF2α), acetylcholine (ACh), and 5-hydroxy tryptamine (5-HT)...
September 19, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Simona Musella, Veronica di Sarno, Tania Ciaglia, Marina Sala, Antonia Spensiero, Maria Carmina Scala, Carmine Ostacolo, Graciela Andrei, Jan Balzarini, Robert Snoeck, Ettore Novellino, Pietro Campiglia, Alessia Bertamino, Isabel M Gomez-Monterrey
We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the indole nucleus. Modifications of this template through Mannich and Friedel-Crafts reactions, coupled with nucleophilic displacement and reductive aminations led to 23 final derivatives, which were pharmacologically tested. Tryptamine derivative 17a was found to have a selective inhibitory activity against human varicella zoster virus (VZV) replication in vitro, being inactive against a variety of other DNA and RNA viruses...
September 7, 2016: European Journal of Medicinal Chemistry
Rosa Guarcello, Maria De Angelis, Luca Settanni, Sabino Formiglio, Raimondo Gaglio, Fabio Minervini, Giancarlo Moschetti, Marco Gobbetti
: Accumulation of biogenic amines (BAs) in cheese and other foods is a matter of public health concern. This study aimed at identifying enzyme activities responsible for BAs degradation in lactic acid bacteria, which were previously isolated from traditional Sicilian and Apulian cheeses. Selected strains would control the concentration of BAs during cheese manufacture. First, 431 isolates, not showing genes encoding for decarboxylases responsible for BA formation, were selected using PCR-based methods...
September 16, 2016: Applied and Environmental Microbiology
Somandla Ncube, Anna Poliwoda, Hlanganani Tutu, Piotr Wieczorek, Luke Chimuka
A liquid phase microextraction based on hollow fibre followed by liquid chromatographic determination was developed for the extraction and quantitation of the hallucinogenic muscimol from urine samples. Method applicability on polar hallucinogens was also tested on two alkaloids, a psychedelic hallucinogen, tryptamine and a polar amino acid, tryptophan which exists in its charged state in the entire pH range. A multivariate design of experiments was used in which a half fractional factorial approach was applied to screen six factors (donor phase pH, acceptor phase HCl concentration, carrier composition, stirring rate, extraction time and salt content) for their extent of vitality in carrier mediated liquid microextractions...
October 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Kyoungwhan Back, Dun-Xian Tan, Russel J Reiter
Melatonin is an animal hormone as well as a signaling molecule in plants. It was first identified in plants in 1995, and almost all enzymes responsible for melatonin biosynthesis had already been characterized in these species. Melatonin biosynthesis from tryptophan requires four-step reactions. However, six genes, i.e., TDC, TPH, T5H, SNAT, ASMT, and COMT, have been implicated in the synthesis of melatonin in plants, suggesting the presence of multiple pathways. Two major pathways have been proposed based on the enzyme kinetics: one is the tryptophan/tryptamine/serotonin/N-acetylserotonin/melatonin pathway, which may occur under normal growth conditions; the other is the tryptophan/tryptamine/serotonin/5-methoxytryptamine/melatonin pathway, which may occur when plants produce large amounts of serotonin, e...
September 7, 2016: Journal of Pineal Research
Alberto Mazza, Egle M Beccalli, Alessandro Contini, Aida Nelly Garcia-Argaez, Lisa Dalla Via, Maria Luisa Gelmi
The synthesis of a new hexacyclic system was realized starting from tryptamines and exploiting as a key step a sequential Pd-catalyzed N-arylation/acylation reaction. Having topoisomerases as biological target and the campthotecins class as benchmark, the new scaffold was decorated with substituents having different polarity and tested as Topoisomerase I inhibitors.
August 23, 2016: European Journal of Medicinal Chemistry
Santanu Hati, Sayantan Tripathy, Pratip Kumar Dutta, Rahul Agarwal, Ramprasad Srinivasan, Ashutosh Singh, Shailja Singh, Subhabrata Sen
The spiro[pyrrolidine-3, 3´-oxindole] moiety is present as a core in number of alkaloids with substantial biological activities. Here in we report design and synthesis of a library of compounds bearing spiro[pyrrolidine-3, 3´-oxindole] motifs that demonstrated exceptional inhibitory activity against the proliferation of MCF-7 breast cancer cells. The synthesis involved a one pot Pictet Spengler-Oxidative ring contraction of tryptamine to the desired scaffolds and occurred in 1:1 THF and water with catalytic trifluoroacetic acid and stoichiometric N-bromosuccinimide as an oxidant...
2016: Scientific Reports
Fausto Gardini, Yesim Özogul, Giovanna Suzzi, Giulia Tabanelli, Fatih Özogul
Biogenic amines (BAs) are molecules, which can be present in foods and, due to their toxicity, can cause adverse effects on the consumers. BAs are generally produced by microbial decarboxylation of amino acids in food products. The most significant BAs occurring in foods are histamine, tyramine, putrescine, cadaverine, tryptamine, 2-phenylethylamine, spermine, spermidine, and agmatine. The importance of preventing the excessive accumulation of BAs in foods is related to their impact on human health and food quality...
2016: Frontiers in Microbiology
Eun-Hye Jung, Ji-Sun Hwang, Mi-Youn Kwon, Kyung-Hong Kim, Hyeongjin Cho, In Kyoon Lyoo, Sujeong Shin, Jeong-Ho Park, Inn-Oc Han
In the present study, we synthesized and evaluated the anti-inflammatory effects of three tryptamine (Trm) hybrid compounds, HBU-375, HBU-376 and HBU-379. The Click reaction between the azido-Trm and 2- or 4-propazylated paeonol moiety resulted in HBU-376 and HBU-375, respectively. HBU-379 was generated by hybridizing Trm with propazylated acetyl-syringic acid. HBU-376 and HBU-375 dose-dependently inhibited LPS and caused nitric oxide (NO) generation in BV2 cells, whereas HBU-379 minimally inhibited NO generation, indicating that the paeonol unit plays an important role in the anti-inflammatory effect of Trm hybrid compounds...
August 25, 2016: Neurochemistry International
Kun Luo, Hélène Rocheleau, Peng-Fei Qi, You-Liang Zheng, Hui-Yan Zhao, Thérèse Ouellet
Fusarium graminearum is a devastating pathogenic fungus causing fusarium head blight (FHB) of wheat. This fungus can produce indole-3-acetic acid (IAA) and a very large amount of IAA accumulates in wheat head tissues during the first few days of infection by F. graminearum. Using liquid culture conditions, we have determined that F. graminearum can use tryptamine (TAM) and indole-3-acetonitrile (IAN) as biosynthetic intermediates to produce IAA. It is the first time that F. graminearum is shown to use the l-tryptophan-dependent TAM and IAN pathways rather than the indole-3-acetamide or indole-3-pyruvic acid pathways to produce IAA...
September 2016: Fungal Biology
Olga I Shmatova, Victor N Khrustalev, Valentine G Nenajdenko
An efficient (one- and two-step) synthesis of trifluoromethylated derivatives of the natural alkaloids nazlinine, trypargine, and homotrypargine was elaborated. Trifluoromethyl-substituted 5-7-membered cyclic imines were used as a masked carbonyl component in the Pictet-Spengler reaction with various tryptamines. As a result, this approach opens access to a family of alkaloid-like compounds bearing a CF3 group at position 1 of tetrahydro-β-carboline.
September 16, 2016: Organic Letters
Odd Martin Vallersnes, Alison M Dines, David M Wood, Christopher Yates, Fridtjof Heyerdahl, Knut Erik Hovda, Isabelle Giraudon, Paul I Dargan
BACKGROUND: Psychosis can be associated with acute recreational drug and novel psychoactive substance (NPS) toxicity. However, there is limited data available on how common this is and which drugs are most frequently implicated. We describe a European case series of psychosis associated with acute recreational drug toxicity, and estimate the frequency of psychosis for different recreational drugs. METHODS: The European Drug Emergencies Network (Euro-DEN) collects data on presentations to Emergency Departments (EDs) with acute recreational drug and NPS toxicity at 16 centres in ten countries...
2016: BMC Psychiatry
Shariq Najeeb, Zohaib Khurshid, Sana Zohaib, Muhammad Sohail Zafar
Melatonin (N-acetyl-5-methoxy tryptamine) is a substance secreted by multiple organs in vertebrates. In addition to playing a part in the circadian cycle of the body, melatonin is known to have antioxidant, antiinflammatory, and antioncotic effects on human tissues. Oral cavity is affected by a number of conditions such as periodontitis, mucositis, cancers, and cytotoxicity from various drugs or biomaterials. Research has suggested that melatonin is effective in treating the aforementioned pathologies. Furthermore, melatonin has been observed to enhance osseointegration and bone regeneration...
August 2016: Kaohsiung Journal of Medical Sciences
Samar S A Mourshid, Jihan M Badr, April L Risinger, Susan L Mooberry, Diaa T A Youssef
Two new antimicrobial fatty acid esters, penicilloitins A and B (1 and 2), along with α-cyclopiazonic acid (3), tryptamine (4) and indole-3-carbaldehyde (5), were isolated from mycelial extracts and the culture broth of a marine endophytic Penicillium species and their structures established by spectroscopic techniques including 1D (1H NMR and 13C NMR) and 2D NMR (COSY, multiplicity-edited HSQC, and HMBC) as well as HRESIMS. Of these compounds, 1, 3 and 4 displayed modest antimicrobial activity.
August 13, 2016: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Sunil Kumar, Ranjana Aggarwal, Virender Kumar, Rachna Sadana, Bhumi Patel, Pawan Kaushik, Dhirender Kaushik
Synthesis of fourteen analogues of bacillamide, a bioactive tryptamide alkaloid of marine origin, has been accomplished through a highly efficient convergent route. The present solvent-free protocol involves the formation of thiazole ring in the initial step followed by amide coupling between substituted ethyl 2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxylates and tryptamine in presence of 2-hydroxy-4,6-dimethylpyrimidine, a solid phase catalyst to yield N-[2-(1H-indol-3-yl)ethyl]-2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxamides as bacillamide analogues having structural variation at position-2 of thiazole ring...
November 10, 2016: European Journal of Medicinal Chemistry
Fabio Vaiano, Francesco P Busardò, Diego Palumbo, Chrystalla Kyriakou, Alessia Fioravanti, Valeria Catalani, Francesco Mari, Elisabetta Bertol
Identification and quantification of new psychoactive substances (NPS), both in biological and non-biological samples, represent a hard challenge for forensic toxicologists. NPS are increasingly emerging on illegal drug market. Many cases of co-consumption of NPS and other substances have also been reported. Hence, the development of analytical methods aiming at the detection of a broad-spectrum of compounds (NPS and "traditional" drugs) could be helpful. In this paper, a fully validated screening method in blood for the simultaneous detection of 69 substances, including 64 NPS (28 synthetic cannabinoids, 19 synthetic cathinones, 5 phenethylamines, 3 indanes, 2 piperazines, 2 tryptamines, 2 phencyclidine, methoxetamine, ketamine and its metabolite) and 5 amphetamines (amphetamine, methamphetamine, MDMA, MDA, 3,4-methylenedioxy-N-ethylamphetamine - MDEA-) by a dynamic multiple reaction monitoring analysis through liquid chromatography - tandem mass spectrometry (LC-MS/MS) is described...
September 10, 2016: Journal of Pharmaceutical and Biomedical Analysis
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