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Mustafa Ceylan, Umit M Kocyigit, Necibe Canan Usta, Belma Gürbüzlü, Yusuf Temel, Saleh H Alwasel, İlhami Gülçin
Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells...
October 25, 2016: Journal of Biochemical and Molecular Toxicology
Merja Kokki, Marja Heikkinen, Pyry Välitalo, Heidi Hautajärvi, Juho Hokkanen, Hanna Pitkänen, Ulla Sankilampi, Veli-Pekka Ranta, Hannu Kokki
BACKGROUND AND OBJECTIVES: This study aimed to characterize the pharmacokinetics of oxycodone and its major metabolites in infants and covered the age range between extremely preterm neonates and 2-year old infants. METHODS: Seventy-nine infants (gestational age 23-42 weeks; postnatal age 0-650 days) received intravenous oxycodone hydrochloride trihydrate at a dose of 0.1 mg/kg during or after surgery. Three to seven blood samples were taken from each infant, and plasma concentrations of oxycodone, noroxycodone, oxymorphone, and noroxymorphone were quantified...
October 25, 2016: British Journal of Clinical Pharmacology
Max Kolton, Ellen R Graber, Ludmila Tsehansky, Yigal Elad, Eddie Cytryn
The 'biochar effect' depicts a phenomenon in which biochar soil amendment enhances plant performance by promoting growth and suppressing disease. Although this phenomenon has been observed in numerous studies, the mode of action that explains it is currently unknown. In order to elucidate mechanisms responsible for the 'biochar effect', we comprehensively monitored tomato plant development and resistance to the foliar fungal pathogen Botrytis cinerea, in biochar-amended and nonamended soils using native biochar and washed biochar, striped of labile chemical constituents...
October 25, 2016: New Phytologist
Peter Werner Roesky, Claude Kiefer, Sebastian Bestgen, Michael T Gamer, Michael Kühn, Sergei Lebedkin, Florian Weigend, Manfred M Kappes
Bis-phenylpropynyl-functionalized imidazolium salts and their corresponding gold and copper NHC complexes were prepared in order to investigate their potential application for the synthesis of heterometallic coinage metal compounds. By transmetallation reactions with different precious metal sources including copper and silver phenylacetylides [MCCPh]x (M = Cu, Ag), polynuclear molecules were obtained, which were further investigated for their photoluminescence properties. Additionally, one gold NHC complex was post-functionalized by autocatalytic hydration of the alkynyl side chains...
October 25, 2016: Chemistry: a European Journal
Tal Hoffmann, Katrin Kistner, Richard W Carr, Mohammed A Nassar, Peter W Reeh, Christian Weidner
The upregulation of the tetrodotoxin-resistant voltage-gated sodium channel NaV1.9 has previously been associated with inflammatory hyperalgesia. Na1.9 knockout (KO) mice, however, did not seem insensitive in conventional tests of acute nociception. Using electrophysiological, neurochemical, and behavioral techniques, we now show NaV1.9-null mice exhibit impaired mechanical and thermal sensory capacities and reduced electrical excitability of nociceptors. In single-fiber recordings from isolated skin, the electrical threshold of NaV1...
September 15, 2016: Pain
Nicola Gaetano Gatta, Gaetano Cammarota, Martina Iannaccone, Enrica Serretiello, Vittorio Gentile
OBJECTIVES: Curcumin, a naturally occurring compound derived from turmeric (Curcuma longa) has long been suggested to have strong therapeutic or preventive potential against human diseases because of its antioxidative, anticancerous, and anti-inflammatory effects. Curcumin is known to exert anti-inflammatory effects by interrupting NF-κB signaling at multiple levels. Many observations indicate that curcumin shows its valuable potential by inhibiting the activity of I-κB kinase. Transglutaminase 2 (TG2) expression is increased in inflammatory diseases...
October 26, 2016: Neuroimmunomodulation
Joby Jose, A T Dhanya, Karickal R Haridas, T M Sumesh Kumar, Sony Jayaraman, E Jayadevi Variyar, Sudheesh Sudhakaran
The study was initiated to determine the anticancer activity of a novel compound isolated from the plant Mimosa pudica. The structure of the compound was identified as a derivative of myricetin having alkyl, hydroxy alkyl and methyl substitutions on the basis of spectral evidences (UV-vis, FT-IR, (1)H NMR and Mass spectra). The isolated compound was interpreted as 2-(2',6'-dimethyl-3',4',5'-alkyl or hydroxy alkyl substituted phenyl)-3-oxy-(alkyl or hydoxy alkyl)- 5,7-dihydroxy-chromen-4-one. In vitro evaluation of anticancer activity against human lung adenocarcinoma cell line (A549) and human erythroleukemic cell line (K562) were conducted using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay...
October 22, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Jong Phil Bak, Young Mi Cho, Inhye Kim, Dae Won Park, Jung Eun Kwon, Yong Joon Jeong, Jong Hwan Kwak, Se Chan Kang
Anemarrhena asphodeloides is known to suppress inflammation and lower various fevers. To determine the active component of A. asphodeloides, ethanol (EtOH) extract of A. asphodeloides rhizomes was fractionized. The compounds isolated from the dichloromethane (CH2Cl2) soluble fraction were identified as 4'-O-methylnyasol (1), nyasol (2), 3″-methoxynyasol (3), 3″-hydroxy-4″-methoxy-4″-dehydroxynyasol (4), 4-hydroxybenzaldehyde (5), and 4-hydroxyacetophenone (6). The four norlignans (1-4) potently inhibited the release of β-hexosaminidase from immunoglobulin E (IgE)/dinitrophenol-conjugated bovine serum albumin (DNP-BSA)-treated rat basophilic leukemia (RBL)-2H3 and A23187 plus phorbol 12-myristate 13-acetate co-treated isolated rat primary mast cells, as markers of degranulation and histamine release...
October 22, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Sai Zheng, Jia-Chen Shi, Jian-Ying Hu, Wen-Xin Hu, Jing Zhang, Bing Shao
The reaction kinetics and transformation pathways between bisphenol F (BPF) and sodium hypochlorite were investigated at pH values ranging from 6.5 to 8.5 and with different initial concentration ratios. The reaction rate was pH- and free available chlorine (FAC)-dependent: the reaction rate at pH 8.5 was almost 10 times than that at pH 6.5. A total of 40 compounds were tentatively identified as chloro-substituted BPF and polyphenolic compounds by liquid chromatography quadrupole time-of-flight mass spectrometry operating in electrospray ionization mode (LC-ESI-Q-ToF), and 4 main byproducts were confirmed by (1)H and (13)C nuclear magnetic resonance (NMR)...
October 19, 2016: Water Research
Blanka Bucsella, Antoine Fornage, Catherine Le Denmat, Franka Kálmán
In biotechnological processes the intracellular level of nucleotides and nucleotide sugars have a direct impact on the post-translational modification (glycosylation) of the therapeutic protein products and on the exopolysaccharide pattern of the cells. Thus, they are precursors and also key components in the production of glycoproteins and glycolipids. All four nucleotides (at different phosphorylation stages) and their natural sugar derivatives coexist in biological samples. Their relative ratios depend on the actual conditions under which the cells are grown...
October 2016: Chimia
Mark Hoppé, Ottmar F Hueter, Andy Bywater, Philip Wege, Peter Maienfisch
Malaria is a vector-borne and life-threatening disease caused by parasites that are transmitted to people through the bites of infected female Anopheles mosquitoes. The vector control insecticide market represents a small fraction of the crop protection market and is estimated to be valued at up to $500 million at the active ingredient level. Insecticide resistance towards the current WHOPES-approved products urgently requires the development of new tools to protect communities against the transmission of malaria...
October 2016: Chimia
James M Mutunga, Qiao-Hong Chen, Dawn M Wong, Polo C-H Lam, Jianyong Li, Maxim M Totrov, Aaron D Gross, Paul R Carlier, Jeffrey R Bloomquist
Widespread pyrethroid resistance has caused an urgent need to develop new insecticides for control of the malaria mosquito, Anopheles gambiae. Insecticide discovery efforts were directed towards the construction of bivalent inhibitors that occupy both the peripheral and catalytic sites of the mosquito acetylcholinesterase (AChE). It was hypothesized that this approach would yield a selective, high potency inhibitor that would also circumvent known catalytic site mutations (e.g. G119S) causing target site resistance...
October 2016: Chimia
Ottmar F Hueter, Mark Hoppé, Philip Wege, Peter Maienfisch
A significant proportion of the world's population remains at risk from malaria, and whilst great progress has been made in reducing the number of malaria cases globally through the use of vector control insecticides, these gains are under threat from the emergence of insecticide resistance. The spread of resistance in the vector populations, principally to pyrethroids, is driving the need for the development of new tools for malaria vector control. In order to identify new leads 30,000 compounds from the Syngenta corporate chemical collection were tested in a newly developed screening platform...
October 2016: Chimia
Alexander Arlt, Niels Böhnke, Sebastian Horstmann, Arnoldus W P Vermeer, Stefan Werner, Robert Velten
During our continuous search for new resistance-breaking insecticides applicable to malaria vector control, a new class of α,β-unsaturated imines was identified by applying the principle of conformational rigidification as a powerful tool for compound optimisation. Herein we describe the successful synthesis of these compounds and their biological test results. Our lead compound 16 from this insecticidal class outperforms market standards, notably for the control of mosquito strains that exhibit either metabolic or target-site resistance to these established insecticides...
October 2016: Chimia
Sandra Maria Barbalho, Marcelo Dib Bechara, Ricardo de Alvares Goulart, Karina Quesada, Rodrigo Galhardi Gasparini, Antonely de Cássio Alves de Carvalho, Adriana Maria Ragassi Fiorini
Ulcerative colitis and Crohn's disease are two major forms of the inflammatory bowel diseases (IBDs). Vitamin A (VA) and vitamin D (VD) may be associated with reduction in inflammation in these disorders. The aim of this review was to show the current evidence that may associate VA and VD with IBDs. Data linking VA, VD, and IBDs were studied. Both VA and VD may be related to the immune system in different manners. The active form of VA, retinoic acid, may be related to the growth factor-β and release of interleukin-10 (IL-10), thus involved with the resolution of the inflammation...
October 25, 2016: Journal of Medicinal Food
Alena Vanduchova, Veronika Tomankova, Pavel Anzenbacher, Eva Anzenbacherova
The influence of metabolites of sulforaphane, natural compounds present in broccoli (Brassica oleracea var. botrytis italica) and in other cruciferous vegetables, on drug-metabolizing cytochrome P450 (CYP) enzymes in human liver microsomes and possible entry of sulforaphane into human hepatic cells were investigated. Metabolites studied are compounds derived from sulforaphane by the mercapturic acid pathway (conjugation with glutathione and by following reactions), namely sulforaphane glutathione and sulforaphane cysteine conjugates and sulforaphane-N-acetylcysteine...
October 25, 2016: Journal of Medicinal Food
Nicolas Sotto, Clément Cazorla, Carole Villette, Muriel Billamboz, Christophe Len
The first continuous flow pinacol coupling reaction of carbonyl compounds was successfully achieved within only 2 minutes during a single-pass through a cartridge filled with zinc(0). The optimized method allowed the efficient production of gramm-scale value-added compounds with high productivity. The developed methodology is efficient for aromatic or alpha,beta-unsaturated aldehydes but give moderate results for much stable acetophenone derivatives. Moreover, the flow method displayed better results in terms of yield and selectivity than the corresponding batch methodology...
October 25, 2016: Journal of Organic Chemistry
Ursula R Rodgers, Thomas Lanyon-Hogg, Naoko Masumoto, Markus Ritzefeld, Rosemary Burke, Julian Blagg, Anthony I Magee, Edward W Tate
The Sonic Hedgehog (Shh) signaling pathway plays a critical role during embryonic development and cancer progression. N-terminal palmitoylation of Shh by Hedgehog acyltransferase (Hhat) is essential for efficient signaling, raising interest in Hhat as a novel drug target. A recently identified series of dihydrothienopyridines has been proposed to function via this mode of action; however, the lead compound in this series (RUSKI-43) was subsequently shown to possess cytotoxic activity unrelated to canonical Shh signaling...
October 25, 2016: ACS Chemical Biology
Zhen Liu, Tian Zeng, Kin S Yang, Keary M Engle
A palladium(II)-catalyzed 1,2-dicarbofunctionalization reaction of unactivated alkenes has been developed, wherein a cleavable bidentate directing group is used to control regioselectivity and stabilize the putative alkylpalladium(II) intermediate. Under the optimized reaction conditions, a broad range of nucleophiles and electrophiles were found to participate in this transformation, providing moderate to high yields. 3-Butenoic acid derivatives containing internal alkenes and α-substituents were reactive substrates, offering a powerful platform for preparing β,γ-substituted carbonyl compounds with multiple stereocenters...
October 25, 2016: Journal of the American Chemical Society
Serge Ruccolo, Wesley Sattler, Yi Rong, Gerard Parkin
Bond lengths between pairs of atoms in covalent molecules are generally predicted well by the sum of their respective covalent radii, such that there are usually only small variations in related compounds. It is, therefore, significant that we have demonstrated that the incorporation of appropriately sized linkers between carbon and a metal center provides a means to modulate the length and nature of a metal-carbon interaction. Specifically, X-ray diffraction studies on a series of tris(1-methylimidazol-2-ylthio)methyl zinc complexes, [Titm(Me)]ZnX, demonstrate how the Zn-C bond lengths are highly variable (2...
October 25, 2016: Journal of the American Chemical Society
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