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C G Hart, B E Voelz, K E Brockus, C O Lemley
Production from the corpus luteum (CL) and/or hepatic steroid inactivation impacts peripheral concentrations of P4, which can alter reproductive performance. Our primary objective was to examine hepatic steroid inactivating enzymes, portal blood flow, and luteal blood perfusion at 10 days post-insemination in pregnant versus non-pregnant beef and dairy cows. Twenty early lactation Holstein cows and 20 lactating commercial beef cows were utilized for this study. At day 10 post-insemination, hepatic portal blood flow and CL blood perfusion were measured via Doppler ultrasonography...
March 14, 2018: Reproduction in Domestic Animals, Zuchthygiene
Huisheng Wu, Chaoliang Tang, Lydia Wai Tai, Weifeng Yao, Peipei Guo, Junmou Hong, Xin Yang, Xinyi Li, Zhao Jin, Jianjuan Ke, Yanlin Wang
Background & Aims:  Ischemic stroke has been ranked the second cause of death in patients worldwide.Inflammation which is activated during cerebral ischemia/reperfusion is an important mechanism leading to brain injury. This study aimed to investigate the effect of flurbiprofen axetil on cerebral I/R injury and the role of inflammation in this process. Methods:  Rats were subjected to sham operation or global cerebral I/R with or without flurbiprofen axetil (5 mg/kg or 10 mg/kg). Global cerebral ischemia was achieved by occlusion of bilateral common carotid arteries combined with hypotension for 20 min followed by reperfusion for 72 h...
March 14, 2018: Bioscience Reports
Liying Cui, Dan Lv, Youming Wang, Zhijin Fan, Zhengming Li, Zhenghong Zhou
An asymmetric cascade reaction between β-keto acylpyrazoles and o-quinone methides in a formal [4 + 2] fashion to access potentially pharmacological active trans-3,4-dihydrocoumarins has been achieved efficiently by using a quinine-based chiral squaramide as the catalyst. The desired products were obtained in high yields with excellent diastereo- and enantioselectivities (up to 96% yield, >19/1 dr and 96% ee) under mild reaction conditions.
March 13, 2018: Journal of Organic Chemistry
Jan Moritz Seliger, Livia Misuri, Edmund Maser, Jan Hintzpeter
Xanthohumol (XN), a prenylated chalcone unique to hops (Humulus lupulus) and two derived prenylflavanones, isoxanthohumol (IX) and 8-prenylnaringenin (8-PN) gained increasing attention as potential anti-diabetic and cancer preventive compounds. Two enzymes of the aldo-keto reductase (AKR) superfamily are notable pharmacological targets in cancer therapy (AKR1B10) and in the treatment of diabetic complications (AKR1B1). Our results show that XN, IX and 8-PN are potent uncompetitive, tight-binding inhibitors of human aldose reductase AKR1B1 (Ki  = 15...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Valery F Traven, Dmitriy A Cheptsov, Maria V Bulanova, Natalya P Solovjova, Tatyana A Chibisova, Sergei M Dolotov, Ivan V Ivanov
New (1,5-diaryl-3-pyrazolinyl)coumarins have been synthesized. In opposite to (1,5-diaryl-3-pyrazolinyl)-4-hydroxycoumarins these compounds are not able to keto-enol tautomeric transformations with changes of the solvent. (1,5-Diaryl-3-pyrazolinyl)coumarins provide dehydrogenation reaction under irradiation in the presence of perchloroalkanes and manifest themselves as effective photogenerators of acidity. Several aspects of photodehydrogenation mechanism have been studied. Oxygen is shown not be involved in the reaction...
March 11, 2018: Photochemistry and Photobiology
Jeong Sang Yi, Minsuk Kim, Eun-Jung Kim, Byung-Gee Kim
Branched chain amino acids (BCAA) are catabolized into various acyl-CoA compounds, which are key precursors used in polyketide productions. Because of that, BCAA catabolism needs fine tuning of flux balances for enhancing the production of polyketide antibiotics. To enhance BCAA catabolism for pikromycin production in Streptomyces venezuelae ATCC 15439, three key enzymes of BCAA catabolism, 3-ketoacyl acyl carrier protein synthase III, acyl-CoA dehydrogenase, and branched chain α-keto acid dehydrogenase (BCDH) were manipulated...
March 10, 2018: Journal of Industrial Microbiology & Biotechnology
Yuya Nishimura, Terumi Matsui, Jun Ishii, Akihiko Kondo
BACKGROUND: To produce 1-propanol as a potential biofuel, metabolic engineering of microorganisms, such as E. coli, has been studied. However, 1-propanol production using metabolically engineered Saccharomyces cerevisiae, which has an amazing ability to produce ethanol and is thus alcohol-tolerant, has infrequently been reported. Therefore, in this study, we aimed to engineer S. cerevisiae strains capable of producing 1-propanol at high levels. RESULTS: We found that the activity of endogenous 2-keto acid decarboxylase and alcohol/aldehyde dehydrogenase is sufficient to convert 2-ketobutyrate (2 KB) to 500 mg/L 1-propanol in yeast...
March 9, 2018: Microbial Cell Factories
Jiewei Shao, Chengjie Li, Jiahui Kong, Haoran Jiang, Shuangliang Zhao, Minzhi Li, Xu Liang, Weihua Zhu, Yongshu Xie
Oxidation of neo-N-confused phlorin 1 with excessive FeCl3 leads to regioselective ring opening, generating three linear tetrapyrroles, i.e., (10 Z,15 Z)-biladienone 2, (10 Z,15 E)-biladienone 3, and 19-methoxy (10 Z,15 E)-biladiene 4 with an overall yield of 88%. The coordination of these compounds with Zn(II) is affected by the inverted terminal pyrrolic unit, and the presence of the electron-withdrawing keto moiety. The structural identities were also clearly elucidated by the crystal structures of 3 and 4-Zn and were rationalized by DFT calculations...
March 9, 2018: Organic Letters
Maryam Iravani, Reza Omidyan
Hydroxyphenyl-benzothiazole (HBT), is a well-known organic system based on its special character of the excited state hydrogen transfer (ESHT) following photoexcitation. However, the capability of this system regarding photochromism and photoswitching has not been addressed yet. In this study, we have investigated this subject by the aim of the MP2, CC2, ADC(2) and CASSCF theoretical methods. Also, we have considered several electron withdrawing groups and investigated their effects on photophysical characters and spectroscopic properties of enol and keto tautomeres of titled system...
March 9, 2018: Journal of Physical Chemistry. A
Tapaswini Nayak, Lingaraja Jena, Pranita Waghmare, Bhaskar C Harinath
Background: The Mycobacterium tuberculosis (MTB) uridine diphosphogalactofuranose (UDP)-galactopyranose mutase (UGM) is an essential flavoenzyme for mycobacterial viability and an important component of cell wall. It catalyzes the interconversion of UDP-galactopyranose into UDP-galactofuranose, a key building block for cell wall construction, essential for linking the peptidoglycan and mycolic acid cell wall layers in MTB through a 2-keto intermediate. Further, as this enzyme is not present in humans, it is an excellent therapeutic target for MTB...
January 2018: International Journal of Mycobacteriology
M Modzel, K A Solanko, M Szomek, S K Hansen, A Dupont, L J Nåbo, J Kongsted, D Wüstner
Analysis of intracellular cholesterol transport by fluorescence microscopy requires suitable fluorescent analogues of cholesterol. Most existing cholesterol analogues contain lipophilic dyes which can compromise the sterol properties in membranes. An alternative strategy is to introduce additional double bonds into the sterol ring system resulting in intrinsic fluorescence, while at the same time keeping the cholesterol-like properties of the analogues. Existing polyene sterols, such as dehydroergosterol (DHE) or cholestatrienol (CTL), however, contain only three double bonds and suffer from low brightness, significant photobleaching and excitation/emission in the ultraviolet region...
March 8, 2018: Journal of Microscopy
Davide Bressanello, Erica Liberto, Massimo Collino, Fausto Chiazza, Raffaella Mastrocola, Stephen E Reichenbach, Carlo Bicchi, Chiara Cordero
This study exploits the information potential of comprehensive two-dimensional gas chromatography configured with a parallel dual secondary column-dual detection by mass spectrometry and flame ionization (GC×2GC-MS/FID) to study changes in urinary metabolic signatures of mice subjected to high-fructose diets. Samples are taken from mice fed with normal or fructose-enriched diets provided either in aqueous solution or in solid form and analyzed at three stages of the dietary intervention (1, 6, and 12 weeks)...
March 7, 2018: Analytical and Bioanalytical Chemistry
Joni Keto, Tanja Kaartinen, Urpu Salmenniemi, Johanna Castrén, Jukka Partanen, Arno Hänninen, Matti Korhonen, Kaarina Lähteenmäki, Maija Itälä-Remes, Johanna Nystedt
Mesenchymal stromal cells (MSCs) are used as salvage therapy to treat steroid-refractory acute graft-versus-host disease (aGvHD). We studied the immunological response to MSC treatment in 16 aGvHD patients by assessing lymphocyte profiles and three proposed aGvHD serum markers during the MSC treatment. Surprisingly, there were no obvious differences in the lymphocyte profiles between the responders and non-responders. The numbers of T, B, and NK cells were below the normal reference interval in all patients...
June 15, 2018: Molecular Therapy. Methods & Clinical Development
Alexej Bubnov, Cyril Vacek, Michał Czerwiński, Terezia Vojtylová, Wiktor Piecek, Věra Hamplová
Several new lactic acid derivatives containing the keto linkage group far from the chiral part and short alkyl chains have been synthesized and characterised by polarising optical microscopy, differential scanning calorimetry, as well as electro-optic and dielectric spectroscopy. The materials possess a self-assembling behaviour on the nanoscale level as they form polar smectic liquid crystalline mesophases, namely the orthogonal paraelectric SmA* and the tilted ferroelectric SmC* phases, in a broad temperature range down to room temperature...
2018: Beilstein Journal of Nanotechnology
Roberta Bortolozzi, Silvia Bresolin, Elena Rampazzo, Maddalena Paganin, Francesca Maule, Elena Mariotto, Daniele Boso, Sonia Minuzzo, Valentina Agnusdei, Giampietro Viola, Geertruy Te Kronnie, Giovanni Cazzaniga, Giuseppe Basso, Luca Persano
BACKGROUND: Despite chemotherapy intensification, a subgroup of high-risk paediatric T-cell acute lymphoblastic leukemia (T-ALL) patients still experience treatment failure. In this context, we hypothesised that therapy resistance in T-ALL might involve aldo-keto reductase 1C (AKR1C) enzymes as previously reported for solid tumors. METHODS: Expression of NRF2-AKR1C signaling components has been analysed in paediatric T-ALL samples endowed with different treatment outcomes as well as in patient-derived xenografts of T-ALL...
March 8, 2018: British Journal of Cancer
Matthew S Dowling, Wenhua Jiao, Jie Hou, Yuchun Jiang, Shangsheng Gong
A straightforward method for preparing 3,6-disubstituted-1,2,4-triazines through a redox-efficient cyclodehydration of β-keto-N-acylsulfonamides with hydrazine salts is described. Two approaches for synthesizing the requisite β-keto-N-acylsulfonamides are presented, which allow for the late stage incorporation of either the C3 or C6 substituent in a flexible manner from acid chlorides or α-bromoketones, respectively. The scope of this methodology includes primary and secondary sp3-linked substituents at both the C3 and C6 positions, and the mild reaction conditions tolerate a variety of sensitive functionality...
March 7, 2018: Journal of Organic Chemistry
Hamid Reza Sadeghnia, Fatemeh Arjmand, Ahmad Ghorbani
Oxidative stress plays a key role in pathophysiology of brain ischemia. This study aimed to test whether B. serrata hydroalcoholic extract (BSE) and its active constituent 3-acetyl-1 1-keto-β-boswellic acid (AKBA) could protect neurons against ischemic condition induced by oxygen, glucose and serum deprivation (OGSD). First, PC12 neural cells were incubated with BSE (0-400 pg/mL) or AKBA (0-40 pg/mL) for 24 h to find non-cytotoxic concentrations of BSE and AKBA. Then, the cells were pre- (for 2 h) and co-treated with 1...
May 2017: Acta Poloniae Pharmaceutica
Dohyun Im, Daisuke Matsui, Takatoshi Arakawa, Kimiyasu Isobe, Yasuhisa Asano, Shinya Fushinobu
l-Amino acid oxidase/monooxygenase from Pseudomonas sp. AIU 813 (l-AAO/MOG) catalyzes both the oxidative deamination and oxidative decarboxylation of the α-group of l-Lys to produce a keto acid and amide, respectively. l-AAO/MOG exhibits limited specificity for l-amino acid substrates with a basic side chain. We previously determined its ligand-free crystal structure and identified a key residue for maintaining the dual activities. Here, we determined the structures of l-AAO/MOG complexed with l-Lys, l-ornithine, and l-Arg and revealed its substrate recognition...
March 2018: FEBS Open Bio
Tingting Ning, Changlong Leng, Lin Chen, Baomiao Ma, Xiaokang Gong
BACKGROUND: Understanding the process of relapse to abused drugs and ultimately developing treatments that can reduce the incidence of relapse remains the primary goal for the study of substance dependence. Therefore, exploring the metabolite characteristics during the relapse stage is valuable. METHODS: A heroin self-administered rat model was employed, and analysis of the1 H-nuclear magnetic resonance-based metabolomics was performed to investigate the characteristic metabolite profile upon reintroduction to the drug after abstinence...
March 5, 2018: BMC Neuroscience
Yusuke Sone, Shuto Nakamura, Makoto Sasaki, Fumihito Hasebe, Seung-Young Kim, Nobutaka Funa
1,8-Dihydroxynaphthalene (1,8-DHN) is a key intermediate in the biosynthesis of DHN melanin, which is specific to fungi. In this study, we characterized the enzymatic properties of the gene products of an operon consisting of soceCHS1 , bdsA , and bdsB from the gram-negative bacterium, Sorangium cellulosum Heterologous expression of soceCHS1 , bdsA , and bdsB in Streptomyces coelicolor caused secretion of a dark-brown pigment into the broth. High-performance liquid chromatography analysis of the broth revealed that the recombinant strain produced 1,8-DHN, indicating that the operon encoded a novel enzymatic system for the synthesis of 1,8-DHN...
March 2, 2018: Applied and Environmental Microbiology
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