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https://www.readbyqxmd.com/read/28642370/in-vitro-cytochrome-p450-46a1-cyp46a1-activation-by-neuroactive-compounds
#1
Natalia Mast, Kyle W Anderson, Kevin M Johnson, Thanh T N Phan, F Peter Guengerich, Irina A Pikuleva
Cytochrome P450 46A1 (CYP46A1, cholesterol 24-hydroxylase) is the enzyme responsible for the majority of cholesterol elimination from the brain. Previously, we found that the anti-HIV drug efavirenz (EFV) can pharmacologically activate CYP46A1 in mice. Herein, we investigated whether CYP46A1 could also be activated by endogenous compounds, including major neurotransmitters. In vitro experiments with purified recombinant CYP46A1 indicated that CYP46A1 is activated by L-glutamate (L-Glu), L-aspartate, γ-aminobutyric acid, and acetylcholine, with L-Glu eliciting the highest increase (3-fold) in CYP46A1-mediated cholesterol 24-hydroxylation...
June 22, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28622467/h2o-adsorption-on-wo3-and-wo3-x-001-surfaces
#2
Elisa Albanese, Cristiana Di Valentin, Gianfranco Pacchioni
The nature of interaction of water with WO3 surface is of crucial importance for the use of this semiconductor oxide in photocatalysis. In this work, we investigate water adsorption and dissociation on both clean and O-deficient (001) WO3 surfaces by means of an accurate DFT approach. The O vacancy formation energy (computed with respect to O2) has been evaluated for all possible surface configurations and the removal of the terminal O atom along the c axis is found to be preferred, costing about half the corresponding energy in the bulk...
June 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28618346/structural-analysis-of-photocrosslinkable-methacryloyl-modified-protein-derivatives
#3
Kan Yue, Xiuyu Li, Karsten Schrobback, Amir Sheikhi, Nasim Annabi, Jeroen Leijten, Weijia Zhang, Yu Shrike Zhang, Dietmar W Hutmacher, Travis J Klein, Ali Khademhosseini
Biochemically modified proteins have attracted significant attention due to their widespread applications as biomaterials. For instance, chemically modified gelatin derivatives have been widely explored to develop hydrogels for tissue engineering and regenerative medicine applications. Among the reported methods, modification of gelatin with methacrylic anhydride (MA) stands out as a convenient and efficient strategy to introduce functional groups and form hydrogels via photopolymerization. Combining light-activation of modified gelatin with soft lithography has enabled the materialization of microfabricated hydrogels...
September 2017: Biomaterials
https://www.readbyqxmd.com/read/28597389/enhanced-fenton-like-degradation-of-tce-in-sand-suspensions-with-magnetite-by-nta-edta-at-circumneutral-ph
#4
Na Wang, Daqing Jia, Yaoyao Jin, Sheng-Peng Sun, Qiang Ke
The present study investigated the degradation of trichloroethylene (TCE) in sand suspensions by Fenton-like reaction with magnetite (Fe3O4) in the presence of various chelators at circumneutral pH. The results showed that ethylenediaminetetraacetic acid (EDTA) and nitrilotriacetic acid (NTA) greatly improved the rate of TCE degradation, while [S,S]-ethylenediaminedisuccinic acid (s,s-EDDS), malonate, citrate, and phytic acid (IP6) have minimal effects on TCE degradation. Quenching tests suggested that TCE was mainly degraded by hydroxyl radical (HO(·)) attack, with about 90% inhibition on TCE degradation by the addition of HO(·) scavenger 2-propanol...
June 8, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28593636/biosynthesis-of-1%C3%AE-hydroxycorticosterone-in-the-winter-skate-leucoraja-ocellata-evidence-to-suggest-a-novel-steroidogenic-route
#5
J Wiens, R Ho, A K Brassinga, C A Deck, P J Walsh, R N Ben, K Mcclymont, T Charlton, A N Evans, W G Anderson
The present study explores the ability of intracellular bacteria within the renal-inter-renal tissue of the winter skate Leucoraja ocellata to metabolize steroids and contribute to the synthesis of the novel elasmobranch corticosteroid, 1α-hydroxycorticosterone (1α-OH-B). Despite the rarity of C1 hydroxylation noted in the original identification of 1α-OH-B, literature provides evidence for steroid C1 hydroxylation by micro-organisms. Eight ureolytic bacterial isolates were identified in the renal-inter-renal tissue of L...
June 7, 2017: Journal of Fish Biology
https://www.readbyqxmd.com/read/28587962/an-overview-on-cellulose-based-material-in-tailoring-bio-hybrid-nanostructured-photocatalysts-for-water-treatment-and-renewable-energy-applications
#6
REVIEW
Mohamad Azuwa Mohamed, Muhazri Abd Mutalib, Zul Adlan Mohd Hir, M F M Zain, Abu Bakar Mohamad, Lorna Jeffery Minggu, Nor Asikin Awang, W N W Salleh
A combination between the nanostructured photocatalyst and cellulose-based materials promotes a new functionality of cellulose towards the development of new bio-hybrid materials for various applications especially in water treatment and renewable energy. The excellent compatibility and association between nanostructured photocatalyst and cellulose-based materials was induced by bio-combability and high hydrophilicity of the cellulose components. The electron rich hydroxyl group of celluloses helps to promote superior interaction with photocatalyst...
June 3, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28581643/regioselective-synthesis-biological-evaluation-and-molecular-docking-of-dihydropyrimidin-4-ols-as-acetylcholinesterase-inhibitors
#7
Andreia M P W da Silva, Fabio M da Silva, Pablo A Nogara, Eduardo J M Dutra, Jonas D S Serres, Rogério A Saraiva, Bruna C Piccoli, Cláudia S Oliveira, Maria R C Schetinger, Vera M M Morsch, João B T Rocha, Helio G Bonacorso, Marcos A P Martins, Nilo Zanatta
A new series of 3,6-disubstituted 2-(methylthio)-4-(trifluoromethyl)-3,4-dihydropyrimidin-4-ols displaying methyl, phenyl, aryl, and heteroaryl groups at the 6-position; and methyl, ethyl, allyl, and phenyl groups at the 3-position of the dihydropyrimidine ring, were synthesized and evaluated in vitro for acetylcholinesterase (AChE) inhibitory activity. Seven compounds showed activity with IC50 values in the lower micromolar range. The compound 4-trifluoromethyl-6-(4-fluorophenyl)-3-methyl-2-methylthio-3,4-dihydropyrimidin-4-ol (6e) had the best inhibitory activity (IC50 2...
June 5, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28580552/ability-of-t1-lipase-to-degrade-amorphous-p-3hb-structural-and-functional-study
#8
Rauda A Mohamed, Abu Bakar Salleh, Adam Thean Chor Leow, Normi M Yahaya, Mohd Basyaruddin Abdul Rahman
An enzyme with broad substrate specificity would be an asset for industrial application. T1 lipase apparently has the same active site residues as polyhydroxyalkanoates (PHA) depolymerase. Sequences of both enzymes were studied and compared, and a conserved lipase box pentapeptide region around the nucleophilic serine was detected. The alignment of 3-D structures for both enzymes showed their active site residues were well aligned with an RMSD value of 1.981 Å despite their sequence similarity of only 53...
June 3, 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/28555391/improved-recovery-and-biological-activities-of-an-engineered-polyene-npp-analogue-in-pseudonocardia-autotrophica
#9
Hyung-Jin Won, Hye-Jin Kim, Jin-Young Jang, Seung-Hoon Kang, Si-Sun Choi, Eung-Soo Kim
NPP A1 produced by Pseudonocardia autotrophica is a unique disaccharide-containing polyene macrolide. NPP A1 was reported to have higher water solubility and lower hemolytic toxicity than nystatin A1 while retaining its antifungal activity. An engineered NPP A1 analogue, NPP A2, was generated by inactivation of the nppL gene, encoding a P450 monooxygenase in P. autotrophica. The resulting compound exhibited the corresponding chemical structure of NPP A1 but lacked a C10 hydroxyl group. In this study, newly developed crystallization recovery methods for NPP A2 purification, followed by an evaluation of in vitro antifungal activity and hemolytic activity, were performed...
May 29, 2017: Journal of Industrial Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28554477/the-arabidopsis-gasa10-gene-encodes-a-cell-wall-protein-strongly-expressed-in-developing-anthers-and-seeds
#10
Menelaos Trapalis, Song Feng Li, Roger W Parish
The Arabidopsis GASA10 gene encodes a GAST1-like (Gibberellic Acid-Stimulated) protein. Reporter gene analysis identified consistent expression in anthers and seeds. In anthers expression was developmentally regulated, first appearing at stage 7 of anther development and reaching a maximum at stage 11. Strongest expression was in the tapetum and developing microspores. GASA10 expression also occurred throughout the seed and in root vasculature. GASA10 was shown to be transported to the cell wall. Using GASA1 and GASA6 as positive controls, gibberellic acid was found not to induce GASA10 expression in Arabidopsis suspension cells...
July 2017: Plant Science: An International Journal of Experimental Plant Biology
https://www.readbyqxmd.com/read/28552108/pistacia-chinensis-strong-antioxidant-and-potent-testicular-toxicity-amelioration-agent
#11
Farah Noureen, Muhammad Rashid Khan, Naseer Ali Shah, Rahmat Ali Khan, Kiran Naz, Saadia Sattar
OBJECTIVES: To evaluate in vitro and in vivo antioxidant potency of Pistacia chinensis (P. chinensis) bark and leaves extracts along with its protective role against CCl4 induced toxicity in testis of the rat. METHODS: Various in vitro models such as DPPH, ABTS, hydrogen peroxide, superoxide, hydroxyl and nitric oxide scavenging activities, anti-lipid peroxidation activity, phospho-molybdenum activity, β carotene bleaching assay was used for analysis of antioxidant potential...
April 2017: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/28545850/renal-response-to-intravascular-volume-expansion-in-euvolemic-heart-failure-patients-with-reduced-ejection-fraction-mechanistic-insights-and-clinical-implications
#12
Petra Nijst, Frederik H Verbrugge, Pieter Martens, Matthias Dupont, W H Wilson Tang, Wilfried Mullens
BACKGROUND: Untreated and preclinical heart failure patients with reduced ejection fraction (HFrEF) have an impaired ability to alleviate excess intravascular volume. OBJECTIVES: To investigate 1) the renal response to intravascular volume expansion in euvolemic and optimally treated HFrEF patients and 2) loop diuretic efficiency. METHODS: 14 healthy and 28 HFrEF patients underwent intravascular volume expansion with 1l hydroxyl ethyl starch 6% during 3h after which a loop diuretic was administered...
May 14, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28541047/multitargeted-flavonoid-inhibition-of-the-pathogenic-bacterium-staphylococcus-aureus-a-proteomic-characterization
#13
Wael A Elmasri, Rui Zhu, Wenjing Peng, Moustafa Al-Hariri, Firas Kobeissy, Phat Tran, Abdul N Hamood, Mohamed F Hegazy, Paul W Paré, Yehia Mechref
Growth inhibition of the pathogen Staphylococcus aureus with currently available antibiotics is problematic in part due to bacterial biofilm protection. Although recently characterized natural products, including 3',4',5-trihydroxy-6,7-dimethoxy-flavone [1], 3',4',5,6,7-pentahydroxy-flavone [2], and 5-hydroxy-4',7-dimethoxy-flavone [3], exhibit both antibiotic and biofilm inhibitory activities, the mode of action of such hydroxylated flavonoids with respect to S. aureus inhibition is yet to be characterized...
May 25, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28537398/discovery-of-clinical-candidate-2-2s-6s-2-phenyl-6-hydroxyadamantan-2-yl-1-3-hydroxyazetidin-1-yl-ethanone-bms-816336-an-orally-active-novel-selective-11%C3%AE-hydroxysteroid-dehydrogenase-type-1-inhibitor
#14
Xiang-Yang Ye, Stephanie Y Chen, Shung Wu, David S Yoon, Haixia Wang, Zhenqiu Hong, Stephen P O'Connor, Jun Li, James J Li, Lawrence J Kennedy, Steven J Walker, Akbar Nayeem, Steven Sheriff, Daniel M Camac, Vidyhashankar Ramamurthy, Paul E Morin, Rachel Zebo, Joseph R Taylor, Nathan N Morgan, Randolph P Ponticiello, Thomas Harrity, Atsu Apedo, Rajasree Golla, Ramakrishna Seethala, Mengmeng Wang, Timothy W Harper, Bogdan G Sleczka, Bin He, Mark Kirby, David K Leahy, Jianqing Li, Ronald L Hanson, Zhiwei Guo, Yi-Xin Li, John D DiMarco, Raymond Scaringe, Brad Maxwell, Frederick Moulin, Joel C Barrish, David A Gordon, Jeffrey A Robl
BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000-fold selectivity over human 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2). 6n-2 exhibits a robust acute pharmacodynamic effect in cynomolgus monkeys (ED50 0.12 mg/kg) and in DIO mice. It is orally bioavailable (%F ranges from 20 to 72% in preclinical species) and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans...
June 5, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28530710/engineering-protein-stability-with-atomic-precision-in-a-monomeric-miniprotein
#15
Emily G Baker, Christopher Williams, Kieran L Hudson, Gail J Bartlett, Jack W Heal, Kathryn L Porter Goff, Richard B Sessions, Matthew P Crump, Derek N Woolfson
Miniproteins simplify the protein-folding problem, allowing the dissection of forces that stabilize protein structures. Here we describe PPα-Tyr, a designed peptide comprising an α-helix buttressed by a polyproline II helix. PPα-Tyr is water soluble and monomeric, and it unfolds cooperatively with a midpoint unfolding temperature (TM) of 39 °C. NMR structures of PPα-Tyr reveal proline residues docked between tyrosine side chains, as designed. The stability of PPα is sensitive to modifications in the aromatic residues: replacing tyrosine with phenylalanine, i...
July 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28521107/formation-of-fluorohydroxyapatite-with-silver-diamine-fluoride
#16
M L Mei, F Nudelman, B Marzec, J M Walker, E C M Lo, A W Walls, C H Chu
Silver diamine fluoride (SDF) is found to promote remineralization and harden the carious lesion. Hydroxyapatite crystallization is a crucial process in remineralization; however, the role of SDF in crystal formation is unknown. We designed an in vitro experiment with calcium phosphate with different SDF concentrations (0.38, 1.52, 2.66, 3.80 mg/mL) to investigate the effect of this additive on the nucleation and growth of apatite crystals. Two control groups were also prepared-calcium phosphate (CaCl2·2H2O + K2HPO4 in buffer solution) and SDF (Ag[NH3]2F in buffer solution)...
May 1, 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/28521100/single-step-synthesis-of-small-azide-functionalized-gold-nanoparticles-versatile-water-dispersible-reagents-for-click-chemistry
#17
Edward W Elliott, Aurora L Ginzburg, Zachary C Kennedy, Zhenshuo Feng, James E Hutchison
Nanoparticles possessing functional groups that can be readily conjugated (e.g., through click chemistry) are important precursors for the preparation of customized nanohybrid products. Such nanoparticles, if they are stable against agglomeration, are easily dispersible and have well-defined surface chemistry and size. As click-ready reagents, they can be stored until their time of use and then simply dispersed and reacted with an appropriate substrate. Gold nanoparticles (AuNPs) are excellent candidates for this purpose, and some clickable gold nanoparticles have been developed; however, AuNPs for use in aqueous systems are often prepared through difficult multistep processes and/or can be poorly dispersible in water...
June 1, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28520746/dna-recognition-by-an-rna-guided-bacterial-argonaute
#18
Kevin W Doxzen, Jennifer A Doudna
Argonaute (Ago) proteins are widespread in prokaryotes and eukaryotes and share a four-domain architecture capable of RNA- or DNA-guided nucleic acid recognition. Previous studies identified a prokaryotic Argonaute protein from the eubacterium Marinitoga piezophila (MpAgo), which binds preferentially to 5'-hydroxylated guide RNAs and cleaves single-stranded RNA (ssRNA) and DNA (ssDNA) targets. Here we present a 3.2 Å resolution crystal structure of MpAgo bound to a 21-nucleotide RNA guide and a complementary 21-nucleotide ssDNA substrate...
2017: PloS One
https://www.readbyqxmd.com/read/28516768/trimetallic-nitride-endohedral-fullerenes-carboxyl-gd3n-c80-a-new-theranostic-agent-for-combating-oxidative-stress-and-resolving-inflammation
#19
Tinghui Li, Li Xiao, Jiezuan Yang, Mengmeng Ding, Zhiguo Zhou, Leslie LaConte, Li Jin, Harry C Dorn, Xudong Li
Antioxidative and anti-inflammatory effects of trimetallic nitride endohedral fullerenes carboxyl-Gd3N@C80, a newly developed magnetic resonance imaging (MRI) contrast agent, were investigated. All hydrochalarone and carboxyl-functionalized fullerenes showed effective radical (hydroxyl and superoxide anion) scavenging, whereas the carboxyl-Gd3N@C80 more efficiently attenuated lipopolysaccharide (LPS) induced oxidative stress in macrophages. Carboxyl-Gd3N@C80 also suppressed LPS-elicited mRNA expression of pro-inflammatory inducible nitric oxide synthase and tumor necrosis factor-alpha, and upregulated antioxidative enzyme axis Nrf2 and heme oxygenase-1, possibly via ERK but not AKT signaling pathways...
May 31, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28514863/surface-dependent-contact-activation-of-factor-xii-and-blood-plasma-coagulation-induced-by-mixed-thiol-surfaces
#20
James W Bauer, Li-Chong Xu, Erwin A Vogler, Christopher A Siedlecki
Studies of the activation of FXII in both platelet poor plasma and in neat buffer solutions were undertaken for a series of mixed thiol self-assembled monolayers spanning a broad range of water wettability. A wide spectrum of carboxyl/methyl-, hydroxyl/methyl-, and amine/methyl-thiol modified surfaces were prepared, characterized, and then utilized as the procoagulant materials in a series of FXII activation studies. X-ray photoelectron spectroscopy was utilized to verify the sample surface's thiol composition and contact angles measured to determine the sample surface's wettability...
May 17, 2017: Biointerphases
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