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https://www.readbyqxmd.com/read/28335518/new-chiral-ebselen-analogues-with-antioxidant-and-cytotoxic-potential
#1
Agata J Pacuła, Katarzyna B Kaczor, Jędrzej Antosiewicz, Anna Janecka, Angelika Długosz, Tomasz Janecki, Andrzej Wojtczak, Jacek Ścianowski
New chiral camphane-derived benzisoselenazol-3(2H)-ones and corresponding diselenides have been synthetized using a convenient one-pot procedure. Se-N bond was efficiently converted to an Se-Se bond, which could also be easily re-oxidized to the initial benzisoselenazolone moiety. The antioxidant activity of camphor derivatives was evaluated and compared to the reactivity of a series of N-amino acid benzisoselenazol-3(2H)-ones obtained by a modified procedure involving the improved synthesis and isolation of the diseleno bis(dibenzoic) acid...
March 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#2
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28330275/phytochemicals-of-moringa-oleifera-a-review-of-their-nutritional-therapeutic-and-industrial-significance
#3
REVIEW
Ramesh Kumar Saini, Iyyakkannu Sivanesan, Young-Soo Keum
Moringa oleifera Lam., also known as the 'drumstick tree,' is recognized as a vibrant and affordable source of phytochemicals, having potential applications in medicines, functional food preparations, water purification, and biodiesel production. The multiple biological activities including antiproliferation, hepatoprotective, anti-inflammatory, antinociceptive, antiatherosclerotic, oxidative DNA damage protective, antiperoxidative, cardioprotective, as well as folk medicinal uses of M. oleifera (MO) are attributed to the presence of functional bioactive compounds, such as phenolic acids, flavonoids, alkaloids, phytosterols, natural sugars, vitamins, minerals, and organic acids...
December 2016: 3 Biotech
https://www.readbyqxmd.com/read/28330099/thermomyces-lanuginosus-lipase-catalyzed-synthesis-of-natural-flavor-esters-in-a-continuous-flow-microreactor
#4
Ahmad Mohammed Gumel, M S M Annuar
Enzymatic catalysis is considered to be among the most environmental friendly processes for the synthesis of fine chemicals. In this study, lipase from Thermomyces lanuginosus (Lecitase Ultra™) was used to catalyze the synthesis of flavor esters, i.e., methyl butanoate and methyl benzoate by esterification of the acids with methanol in a microfluidic system. Maximum reaction rates of 195 and 115 mM min(-1) corresponding to catalytic efficiencies (k cat/K M) of 0.30 and 0.24 min(-1) mM(-1) as well as yield conversion of 54 and 41 % were observed in methyl butanoate and methyl benzoate synthesis, respectively...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28326230/methods-for-preparing-polymer-decorated-single-exchange-biased-magnetic-nanoparticles-for-application-in-flexible-polymer-based-films
#5
Laurence Ourry, Delphine Toulemon, Souad Ammar, Fayna Mammeri
Background: Magnetic nanoparticles (NPs) must not only be well-defined in composition, shape and size to exhibit the desired properties (e.g., exchange-bias for thermal stability of the magnetization) but also judiciously functionalized to ensure their stability in air and their compatibility with a polymer matrix, in order to avoid aggregation which may seriously affect their physical properties. Dipolar interactions between NPs too close to each other favour a collective magnetic glass state with lower magnetization and coercivity because of inhomogeneous and frustrated macrospin cluster freezing...
2017: Beilstein Journal of Nanotechnology
https://www.readbyqxmd.com/read/28325791/individual-variations-in-nitric-oxide-synthase-dependent-sweating-in-young-and-older-males-during-exercise-in-the-heat-role-of-aerobic-power
#6
Tatsuro Amano, Naoto Fujii, Jeffrey C Louie, Robert D Meade, Glen P Kenny
We evaluated the association between aerobic power (defined by peak oxygen consumption; VO2peak) and the contribution of nitric oxide synthase (NOS) to the sweating response in young and older individuals during exercise in the heat. Data from 44 young (24 ± 1 years) and 48 older (61 ± 2 years) males with mean VO2peak of 47.8 ± 2.4 (range, 28.0-62.3) and 39.1 ± 2.3 (range, 26.4-55.7) mLO2 kg(-1) min(-1), respectively, were compiled from our prior studies. Participants performed two 15- to 30-min bouts of exercise at a fixed rate of metabolic heat production of 400 or 500 W, each separated by 15-20 min recovery in the heat (35°C, relative humidity of 20%)...
March 2017: Physiological Reports
https://www.readbyqxmd.com/read/28325349/nanocrystalline-cellulose-fullerene-novel-conjugates
#7
A Herreros-López, M Carini, T Da Ros, T Carofiglio, C Marega, V La Parola, V Rapozzi, L E Xodo, Ali A Alshatwi, C Hadad, M Prato
The covalent grafting of two amino-fullerene C60 derivatives (C60-LC-NH2 and C60-SC-NH2, LC=long chain and SC=short chain) onto the surface of TEMPO oxidized nanocrystalline cellulose (NCC-COOH) has been reported for the first time. These hybrids (NCC-LC-C60 and NCC-SC-C60) form stable colloidal suspensions at concentrations up to 0.5mg/mL and act as effective photosensitizers for singlet oxygen production as demonstrated by the oxidation of L-methionine-methyl ester to the corresponding sulphoxide. Using the same approach, in a one-pot reaction both a fluorescent target molecule (FITC-LC-NH2) and the C60-LC-NH2 derivative have been successfully attached covalently onto the NCC-COOH surface...
May 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28325345/novel-modified-nanocellulose-applicable-as-reinforcement-in-high-performance-nanocomposites
#8
Jelena D Rusmirović, Jasna Z Ivanović, Vladimir B Pavlović, Vesna M Rakić, Milica P Rančić, Veljko Djokić, Aleksandar D Marinković
The influence of modification and vacuum/supercritical CO2 (scCO2) drying methods on the surface properties, morphology and thermal stability of cellulose nanocrystals (NC) was presented in this study. Introduction of reactive vinyl groups on NC surface was performed by either direct esterification with oleic acid, linseed or sunflower oil fatty acids; or by amidation of maleic acid/ethylene diamine with methyl ester of fatty acid. Obtained modified NC (m-NC) were characterized using FTIR and Raman spectroscopy; and by determination of acid, iodine and ester values...
May 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28324817/developmental-toxicity-and-induction-of-vitellogenin-in-embryo-larval-stages-of-zebrafish-danio-rerio-exposed-to-methyl-paraben
#9
Vrinda Yatin Dambal, Karthikeyan Ponnien Selvan, Christy Lite, S Barathi, Winkins Santosh
MethylParaben (MP), a methyl ester of p-hydroxybenzoic acid, is used as an anti-microbial preservative in foods, drugs and cosmetics for decades. It enters the aquatic environment, and can have toxic effects on aquatic organisms. Little is known on the developmental toxicity of MP exposure to zebrafish during early life stages. In this study, the developmental effects of MP were evaluated in embryo-larval zebrafish (at concentrations ranging from 100μM, 200μM, 400µM, 800μM and 1000μM for 96h post fertilization (hpf)...
March 18, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28323403/discovery-of-potent-antiallodynic-agents-for-neuropathic-pain-targeting-p2x3-receptors
#10
Young-Hwan Jung, Yong-Chul Kim, Yeo Ok Kim, Hai Lin, Joong-Heui Cho, Jin-Hee Park, So-Deok Lee, Jinsu Bae, Koon Mook Kang, Yoon Gyoon Kim, Ae Nim Pae, Hyojin Ko, Chul-Seung Park, Myung Ha Yoon
Antagonism of the P2X3 receptor is one of the potential therapeutic strategies for the management of neuropathic pain because P2X3 receptors are predominantly localized on small to medium diameter C- and Aδ-fiber primary afferent neurons, which are related to the pain-sensing system. In this study, 5-hydroxy pyridine derivatives were designed, synthesized, and evaluated for their in vitro biological activities by two-electrode voltage clamp assay at hP2X3 receptors. Among the novel hP2X3 receptor antagonists, intrathecal treatment of compound 29 showed parallel efficacy with pregabalin (calcium channel modulator) and higher efficacy than AF353 (P2X3 receptor antagonist) in the evaluation of its antiallodynic effects in spinal nerve ligation rats...
March 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28322518/determination-of-fatty-acid-methyl-esters-derived-from-algae-scenedesmus-dimorphus-biomass-by-gc-ms-with-one-step-esterification-of-free-fatty-acids-and-transesterification-of-glycerolipids
#11
Satya Girish Chandra Avula, Joanne Belovich, Yan Xu
Algae can synthesize, accumulate and store large amounts of lipids in its cells, which holds immense potential as a renewable source of biodiesel. In this work, we have developed and validated a GC-MS method for quantitation of fatty acids and glycerolipids in forms of fatty acid methyl esters derived from algae biomass. Algae Scenedesmus dimorphus dry mass was pulverized by mortar and pestle, then, extracted by the modified Folch method and fractionated into free fatty acids and glycerolipids on aminopropyl solid-phase extraction cartridges...
March 21, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28321989/expansion-of-the-%C3%AF-oxidation-system-alkbgtl-of-pseudomonas-putida-gpo1-with-alkj-and-alkh-results-in-exclusive-mono-esterified-dicarboxylic-acid-production-in-e-%C3%A2-coli
#12
Youri M van Nuland, Fons A de Vogel, Gerrit Eggink, Ruud A Weusthuis
The AlkBGTL proteins coded on the alk operon from Pseudomonas putida GPo1 can selectively ω-oxidize ethyl esters of C6 to C10 fatty acids in whole-cell conversions with Escherichia coli. The major product in these conversions is the ω-alcohol. However, AlkB also has the capacity to overoxidize the substrate to the ω-aldehyde and ω-acid. In this study, we show that alcohol dehydrogenase AlkJ and aldehyde dehydrogenase AlkH are able to oxidize ω-alcohols and ω-aldehydes of esterified fatty acids respectively...
March 20, 2017: Microbial Biotechnology
https://www.readbyqxmd.com/read/28320617/synthesis-and-bioactivities-of-phenazine-1-carboxylic-acid-derivatives-based-on-the-modification-of-pca-carboxyl-group
#13
Zhipeng Xiong, Junfan Niu, Hao Liu, Zhihong Xu, Junkai Li, Qinglai Wu
Phenazine-1-carboxylic acid (PCA) as a natural product widely exists in microbial metabolites of Pseudomonads and Streptomycetes and has been registered for the fungicide against rice sheath blight in China. To find higher fungicidal activities compounds and study the effects on fungicidal activities after changing the carboxyl group of PCA, we synthesized a series of PCA derivatives by modifying the carboxyl group of PCA and their structures were confirmed by (1)H NMR and HRMS. Most compounds exhibited significant fungicidal activities in vitro...
March 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28319392/scaffold-repurposing-of-nucleosides-adenosine-receptor-agonists-enhanced-activity-at-the-human-dopamine-and-norepinephrine-sodium-symporters
#14
Dilip K Tosh, Aaron Janowsky, Amy J Eshleman, Eugene Warnick, Zhan-Guo Gao, Zhoumou Chen, Elizabeth Gizewski, John A Auchampach, Daniela Salvemini, Kenneth A Jacobson
We have repurposed (N)-methanocarba adenosine derivatives (A3 adenosine receptor (AR) agonists) to enhance radioligand binding allosterically at the human dopamine (DA) transporter (DAT) and inhibit DA uptake. We extended the structure-activity relationship of this series with small N(6)-alkyl substitution, 5'-esters, deaza modifications of adenine, and ribose restored in place of methanocarba. C2-(5-Halothien-2-yl)-ethynyl 5'-methyl 9 (MRS7292) and 5'-ethyl 10 (MRS7232) esters enhanced binding at DAT (EC50 ∼ 35 nM) and at the norepinephrine transporter (NET)...
March 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28317768/effect-of-xanthan-gum-on-the-release-of-strawberry-flavor-in-formulated-soy-beverage
#15
Jiao Xu, Zhiyong He, Maomao Zeng, Bingbing Li, Fang Qin, Linxiang Wang, Shengfang Wu, Jie Chen
The effects of xanthan gum on the release of strawberry flavor compounds in formulated soy protein isolate (SPI) beverage were investigated by headspace gas chromatography (GC). Seven strawberry flavor compounds (limonene, ethyl hexanoate, (Z)-3-hexenyl acetate, ethyl 2-methylbutanoate, ethyl butanoate, (Z)-3-hexen-1-ol and diacetyl) could be detected by GC and hence analyzed the gas-matrix partition coefficients (K). The release of flavor compounds was restrained in SPI and/or xanthan gum solution. The retention of (Z)-3-hexen-1-ol, limonene and diacetyl significantly changed (p<0...
August 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28316802/crystal-structure-of-erioflorin-isolated-from-podanthus-mitiqui-l
#16
Cristian Paz, Leandro Ortiz, Uwe Schilde
The title compound, erioflorin, C19H24O6 [systematic name: (1aR,3S,4Z,5aR,8aR,9R,10aR)-1a,2,3,5a,7,8,8a,9,10,10a-deca-hydro-3-hy-droxy-4,10a-dimethyl-8-methyl-idene-7-oxooxireno[5,6]cyclo-deca-[1,2-b]furan-9-yl methacrylate], is a tricyclic germacrane sesquiterpene lactone, which was isolated from Podanthus mitiqui (L.). The compound crystallizes in the space group P212121, and its mol-ecular structure consists of a methacrylic ester of a ten-membered ring sesquiterpenoid annelated with an epoxide and a butyrolactone...
March 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28315670/sulfatase-activity-assay-using-an-activity-based-probe-by-generation-of-n-methyl-isoindole-under-reducing-conditions
#17
Hey Young Yoon, Jong-In Hong
Sulfatases catalyze the hydrolysis of sulfate esters that are present in a range of biomolecules. This is an important step in several biological processes such as cellular degradation, hormone regulation, and cell signaling. We have developed a new activity-based sulfatase probe (probe 1) that generates a fluorescent N-methylisoindole upon hydrolysis by sulfatase. Because of the autoxidation of N-methylisoindole, the sulfatase activity was also tested under reducing conditions, containing either glutathione (GSH) or tris(2-carboxyethyl)phosphine (TCEP), exhibiting little change in kinetic parameters compared to non-reducing conditions...
March 16, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28303757/evaluation-of-microalgae-production-coupled-with-wastewater-treatment
#18
Davide De Francisci, Yixi Su, Arvo Iital, Irini Angelidaki
In the present study the feasibility of microalgae production coupled with wastewater treatment was assessed. Continuous cultivation of Chlorella sorokiniana with wastewater was tested in lab-scale flat panel photobioreactors. Biomass productivity was determined for four dilution rates (4.32 d(-1), 3.6 d(-1), 1.8 d(-1) and 0.72 d(-1)). The productivity peak was 1.524 g l(-1)d(-1) at the dilution rate of 2.41 d(-1). Nitrogen and phosphorus removals were found to be inversely proportional to dilution rates, while COD removal was found to be 50% at all the tested conditions...
March 17, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28302929/heartworm-extract-induces-relaxation-of-isolated-rat-thoracic-aorta
#19
Katsuya Kitoh, Hiroaki Nakamura, Hitoshi Kitagawa, Toshihiro Unno, Seiichi Komori, Shin-Pin Chiou, Yasuhiro Takashima
Isolated rat thoracic aortic strips undergoing noradrenaline-induced contraction were treated with an adult heartworm (HW) crude extract and then examined for isometric changes in tension. HW extract caused relaxation of endothelium-intact strips, but not endothelium-denuded strips. This effect was inhibited by treatment with N(G)-nitro-L-arginine methyl ester hydrochloride (L-NAME) and could be reversed by additional treatment with L-arginine. However, HW extract at a high concentration caused slight relaxation of endothelium-denuded strips, and relaxation persisted after L-NAME treatment in endothelium intact-strips...
March 8, 2017: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/28298687/composition-of-volatile-aromatic-compounds-and-minerals-of-tarhana-enriched-with-cherry-laurel-laurocerasus-officinalis
#20
Hasan Temiz, Zekai Tarakçı
Different concentrations of cherry laurel pulp (0, 5, 10, 15 and 20%) were used to produce tarhana samples. Volatile aromatic compounds and minor mineral content were investigated. Volatile aromatic compounds were analyzed by using GC-MS with SPME fiber and minor mineral values were evaluated with inductively coupled plasma optical emission spectrometer. The statistical analysis showed that addition of pulp affected volatile aromatic compounds and minor mineral content significantly. Thirty five volatile aromatic compounds were found in tarhana samples...
March 2017: Journal of Food Science and Technology
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