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O Lidický, M Šírová, T Etrych
In this paper, we describe the synthesis, physicochemical characterization, drug release kinetics and preliminary biological evaluation of several N-(2-hydroxypropyl)methacrylamide (HPMA)-based polymer-retinoid conjugates designed for solid tumor immunotherapy. The conjugates are supposed to inhibit the immunosuppressive activity of myeloid-derived suppressor cells (MDSC) accumulated in the solid tumor microenvironment. All-trans retinoic acid (ATRA) was derivatized to hydrazide (AtrHy) and then attached to the polymer backbone via a spacer that is stable at the normal pH of blood (7...
October 20, 2016: Physiological Research
Carlo Barnaba, Maria Teresa Rodríguez-Estrada, Giovanni Lercker, Hugo Sergio García, Ilce Gabriela Medina-Meza
In this work we studied the effect of polyunsaturated fatty acids (PUFAs) methyl esters on cholesterol photo-induced oxidation. The oxidative routes were modeled with a chemical reaction network (CRN), which represents the first application of CRN to the oxidative degradation of a food-related lipid matrix. Docosahexaenoic acid (DHA, T-I), eicosapentaenoic acid (EPA, T-II) and a mixture of both (T-III) were added to cholesterol using hematoporphyrin as sensitizer, and were exposed to a fluorescent lamp for 48h...
October 15, 2016: Steroids
K Bridget Brosnihan, Victor M Pulgar, Manish S Bharadwaj, Liomar A A Neves, Liliya M Yamaleyeva
BACKGROUND: Cyclooxygenase (COX)-derived prostanoids (PGE2, PGI2) are important contributors to the process of decidualization. Previous studies showed the presence of Ang-(1-7) in the primary and secondary decidualized zones of the implantation site at early pregnancy. Decreased concentrations of Ang-(1-7) were found in the decidualized uterus compared to the non-decidualized uterus of pseudopregnant rats, suggesting that low levels of Ang-(1-7) are required for successful decidualization at early pregnancy...
October 18, 2016: Reproductive Biology and Endocrinology: RB&E
Sophie Front, Anna Biela-Banaś, Patricie Burda, Diana Ballhausen, Katsumi Higaki, Anna Caciotti, Amelia Morrone, Julie Charollais-Thoenig, Estelle Gallienne, Stéphane Demotz, Olivier R Martin
This report is about the identification, synthesis and initial biological characterization of derivatives of 4-epi-isofagomine as pharmacological chaperones (PC) for human lysosomal β-galactosidase. The two epimers of 4-epi-isofagomine carrying a pentyl group at C-5a, namely (5aR)- and (5aS)-5a-C-pentyl-4-epi-isofagomine, were prepared by an innovative procedure involving in the key step the addition of nitrohexane to a keto-pentopyranoside. Both epimers were evaluated as inhibitors of the human β-galactosidase: the (5aR)-stereoisomer (compound 1) was found to be a very potent inhibitor of the enzyme (IC50 = 8 nM, 30× more potent than 4-epi-isofagomine at pH 7...
September 29, 2016: European Journal of Medicinal Chemistry
Nur Ahmad Hussin, Ruvini U Pathirana, Sahar Hasim, Swetha Tati, Jessica A Scheib-Owens, Kenneth W Nickerson
Due to the increased number of immunocompromised patients, infections with the pathogen Candida albicans have significantly increased in recent years. C. albicans transition from yeast to germ tubes is one of the essential factors for virulence. In this study we noted that Lee's medium, commonly used to induce filamentation, contained 500-fold more biotin than needed for growth and 40-fold more biotin than is typically added to growth media. Thus, we investigated the effects of excess biotin on growth rate and filamentation by C...
September 21, 2016: Microorganisms
Chen Wei, Huibo Wei, Weibo Yan, Zifeng Zhao, Zelun Cai, Boxun Sun, Zhaosha Meng, Zhiwei Liu, Zuqiang Bian, Chunhui Huang
Two highly luminescent and water-soluble Eu(III) complexes, Eu1 and Eu2, based on novel carboxyl-functionalized 1,5-naphthyridine derivatives 8-hydroxy-1,5-naphthyridine-2-carboxylic acid (H2L1) and 7-cyano-8-hydroxy-1,5-naphthyridine-2-carboxylic acid (H2L2), respectively, are designed and synthesized. The crystal structure of Eu2 indicates that the central Eu(III) ion is nine-coordinated by three tridentate ligands (O^N^O). Both Eu1 and Eu2 show strong luminescence in aqueous solution with quantum yields (lifetimes) of 28% (1...
October 17, 2016: Inorganic Chemistry
Rossella Attini, Filomena Leone, Silvia Parisi, Federica Fassio, Irene Capizzi, Valentina Loi, Loredana Colla, Maura Rossetti, Martina Gerbino, Stefania Maxia, Maria Grazia Alemanno, Fosca Minelli, Ettore Piccoli, Elisabetta Versino, Marilisa Biolcati, Paolo Avagnina, Antonello Pani, Gianfranca Cabiddu, Tullia Todros, Giorgina B Piccoli
BACKGROUND: Pregnancy in women with advanced CKD becoming increasingly common. However, experience with low-protein diets in CKD patients in pregnancy is still limited. Aim of this study is to review the results obtained over the last 15 years with moderately restricted low-protein diets in pregnant CKD women (combining: CKD stages 3-5, proteinuria: nephrotic at any time, or > =1 g/24 at start or referral; nephrotic in previous pregnancy). CKD patients on unrestricted diets were employed for comparison...
2016: BMC Nephrology
Onur Yücel, Steffen Drees, Nina Jagmann, Thomas Patschkowski, Bodo Philipp
Bile salts such as cholate are surface-active steroid compounds with functions for digestion and signaling in vertebrates. Upon excretion into soil and water bile salts are an electron- and carbon-rich growth substrate for environmental bacteria. Degradation of bile salts proceeds via intermediates with a 3-keto-Δ(1,4) -diene structure of the steroid skeleton as shown for e.g. Pseudomonas spp. Recently, we isolated bacteria degrading cholate via intermediates with a 3-keto-7-deoxy-Δ(4,6) -structure of the steroid skeleton suggesting the existence of a second pathway for cholate degradation...
September 20, 2016: Environmental Microbiology
Cristiana David, Ileana Peride, Andrei Niculae, Alexandra Maria Constantin, Ionel Alexandru Checherita
BACKGROUND: Native arteriovenous fistula (AVF) is the most appropriate type of vascular access for chronic dialysis. Its patency rates depend on vascular wall characteristics. Ketoacid analogues of essential amino acids (KA/EAA) are prescribed in end-stage renal disease (ESRD) pre-dialysis patients to lower toxic metabolic products generation and improve nutritional status. We hypothesized that very-low protein diet (VLPD) supplemented with KA/EAA may influence arterial wall stiffness and affect AVF maturation rates and duration in pre-dialysis ESRD patients...
September 20, 2016: BMC Nephrology
Aaron M Marcella, Adam W Barb
The development of biorenewable chemicals will support green chemistry initiatives and supplement the catalog of starting materials available to the chemical industry. Bacterial fatty acid biosynthesis is being pursued as a source of protein catalysts to synthesize novel reduced carbon molecules in fermentation systems. The availability of methods to measure enzyme catalysis for native and engineered enzymes from this pathway remains a bottleneck because a simple quantitative enzyme assay for numerous enzymes does not exist...
2016: Journal of Biological Methods
Magdalena Szymanska, Agnieszka Blitek
The aim of the study was to determine how supplementation with exogenous progesterone (P4) affects the expression of genes important for endometrial receptivity and conceptus development during the peri-implantation period in pigs. Gilts with PMSG/hCG-induced first estrus received daily injections of corn oil (CO; n=7) or P4 (n=7) on days 3 to 10 after insemination. The dose of P4 was 25mg/100kg BW on days 3 and 4 of gestation, then increased to 50mg/100kg BW on days 5 to 10. Blood samples were collected each day to monitor concentrations of circulating P4...
September 9, 2016: Animal Reproduction Science
Eva Pušavec Kirar, Miha Drev, Jona Mirnik, Uroš Grošelj, Amalija Golobič, Georg Dahmann, Franc Požgan, Bogdan Štefane, Jurij Svete
Two cyclic azomethine imines, 7-methyl- and 7-phenyl-2-oxo-Δ(7)-hexahydropyrazolo[1,5-a]pyridin-8-ium-1-ide, were prepared in seven steps from the respective commercially available δ-keto acids. The addition of Grignard reagents followed by N-alkylation at position 1 afforded the 1,7,7-trisubstituted hexahydropyrazolo[1,5-a]pyridin-2(1H)-ones, whereas 1,3-dipolar cycloadditions of these dipoles to typical acetylenic and olefinic dipolarophiles gave 4a-substituted 2a,2a(1)-diazacyclopenta[cd]indene derivatives as the first representatives of a novel heterocyclic system...
October 7, 2016: Journal of Organic Chemistry
Junhong Guo, Li Hong, Xiaoxia Z West, Hua Wang, Robert G Salomon
Oxidative stress causes lipid-derived oxidative modification of biomolecules that has been implicated in many pathological states. Phospholipids containing polyunsaturated fatty acids are major targets of free radical-initiated oxidation. Phospholipids that incorporate docosahexaenoate (DHA) are highly enriched in important neural structures including the brain and retina, where DHA comprises 40% and 60% of total fatty acids, respectively. Oxidative fragmentation of 2-docosahexaenoyl-1-palmityl-sn-glycerophosphocholine generates esters of 4-hydroxy-7-oxohept-5-enoic acid (HOHA) and 4-keto-7-oxohept-5-enoic acid (KOHA) with 2-lysophosphatidylcholine, HOHA-PC, and KOHA-PC...
October 17, 2016: Chemical Research in Toxicology
R S Scurachio, F Mattiucci, W G Santos, L H Skibsted, D R Cardoso
Caffeine metabolites were found to bind riboflavin with dissociation constant in the millimolar region by an exothermic process with positive entropy of reaction, which was found by (1)H NMR and fluorescence spectroscopy to occur predominantly by hydrogen bonding with water being released from riboflavin solvation shell upon caffeine metabolite binding to riboflavin. The caffeine metabolites 1-methyl uric acid and 1,7-dimethyl uric acid were shown by transient absorption laser flash photolysis to be efficient as quenchers of triplet riboflavin with second-order rate constant of 1...
October 2016: Journal of Photochemistry and Photobiology. B, Biology
Silvia Savastio, Francesco Cadario, Giulia Genoni, Giorgio Bellomo, Marco Bagnati, Gioel Secco, Raffaella Picchi, Enza Giglione, Gianni Bona
BACKGROUND: Vitamin D (25OHD) effects on glycemic control are unclear in children and adolescents with type 1 diabetes. Aims of this study were to investigate 25OHD status among children with T1DM and its relationship with insulin sensitivity and glycemic status. SUBJECTS AND METHODS: A cross sectional study was carried out between 2008-2014. A total of 141 patients had a T1DM >12 months diagnosis and were enrolled in the present study. Of these 35 (24.8%) were migrants and 106 (75...
2016: PloS One
Shengke Li, Yuan-Fu Ding, Hang Yin, Chunming Wang, David Bardelang, Lian-Hui Wang, Ruibing Wang
As determined by both (1) H NMR and UV/Vis spectroscopic titration, ESI-MS, isothermal titration calorimetry, and DFT molecular modeling, advanced glycation end products (AGE) breaker alagebrium (ALA) formed 1:1 guest-host inclusion complexes with cucurbit[7]uril (CB[7]), with a binding affinity, Ka , in the order of magnitude of 10(5)  m(-1) , thermodynamically driven by both enthalpy (ΔH=-6.79 kcal mol(-1) ) and entropy (TΔS=1.21 kcal mol(-1) ). For the first time, a dramatic inhibition of keto-enol tautomerism of the carbonyl α-hydrogen of ALA has been observed, as evidenced by over an order of magnitude decrease of both the first step rate constant, k1 , and the second step rate constant, k2 , during hydrogen/deuterium exchange in D2 O...
September 8, 2016: Chemistry, An Asian Journal
Garrett T Dow, James B Thoden, Hazel M Holden
Kijanimicin is an antitumor antibiotic isolated from Actinomadura kijaniata. It is composed of three distinct moieties: a pentacyclic core, a monosaccharide referred to as d-kijanose, and a tetrasaccharide chain composed of l-digitoxose units. d-Kijanose is a highly unusual nitro-containing tetradeoxysugar, which requires at least ten enzymes for its production. Here we describe a structural analysis of one of these enzymes, namely KijD1, which functions as a C-3'-methyltransferase using S-adenosylmethionine as its cofactor...
September 6, 2016: Protein Science: a Publication of the Protein Society
Si Chen, Nan Jia, Ming-Zhu Ding, Ying-Jin Yuan
Improving the yield of 2-keto-L-gulonic acid (2-KGA), the direct precursor of vitamin C, draws more and more attention in industrial production. In this study, we try to increase the 2-KGA productivity by computer-aided selection of genes encoding L-sorbose dehydrogenases (SDH) of Ketogulonicigenium vulgare. First, six SDHs were modeled by docking strategy to predict the binding mode with co-factor PQQ. The binding energy between SSDA1-H/SSDA1-L and PQQ was the highest, followed by SSDA3/SSDA2. The binding energy between SSDA1-P/SSDB and PQQ was the lowest...
November 2016: Journal of Industrial Microbiology & Biotechnology
Margarita E Aliaga, Angelica Fierro, Ivan Uribe, Luis Garcia-Rio, Alvaro Cañete
The inclusion of the fluorescent organic dye, alkyl 3-(7-hydroxy-2-oxo-2H-chromen-3-yl)-3-oxopropanoate (1) by the host -cyclodextrin (-CD), and its response toward mercuric ions (Hg2+), was studied by UV-Vis and fluorescence spectroscopies, 1H-NMR, mass spectrometry and molecular modeling studies.1H-NMR measurements together with molecular modeling studies for dye 1 demonstrate that it exhibits two tautomeric forms (keto and enol); however when the dye is included into the -CD cavity, the enol form is the predominant one...
August 16, 2016: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
S S Chavan, S B Pawal, M S More, A C Willis
Copper(I) complexes of the formula [Cu(L)(PPh3)2]X (1-4) (X = Cl(1), ClO4(2), BF4(3) and PF6(4)) [where L = N-(2-{[(2E)-2-(4-nitrobenzylidenyl)hydrazinyl]carbonyl}phenyl)benzamide; PPh3 = triphenylphosphine] have been prepared by the condensation of N-[2-(hydrazinocarbonyl)phenyl]benzamide with 4-nitrobenzaldehyde followed by the reaction with CuCl, [Cu(MeCN)4]ClO4, [Cu(MeCN)4]BF4 and [Cu(MeCN)4]PF6 in presence of triphenylphosphine as a coligand. Complexes 1-4 were then characterized by elemental analyses, FTIR, UV-visible and (1)H NMR spectroscopy...
August 15, 2016: Journal of Fluorescence
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