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Suman B Iyer, Anshuman Dube, N M Dube, Pratik Roy, R R N Sailaja
The development of a suitable polymeric bioactive composite with hydroxyapatite as a filler is one of the very actively pursued areas in bioapplications. This report concerns development of such a novel polymeric biocomposite viz. poly (aryl ether) ketone-poly (dimethylsiloxane) with a small percentage of nano carbon fibres and varying percentages of nanohydroxyapatite particulates as fillers. The earlier characterization of this material involving mechanical, thermal and bio-compatibility studies showed optimum improved behaviour at about 7% nanohydroxyapatite loading as reported elsewhere...
June 6, 2018: Journal of the Mechanical Behavior of Biomedical Materials
Amparo Sanz-Marco, Samuel Martinez Erro, Belén Martín-Matute
The first method to access unsymmetrical aliphatic acyloins is presented. The method relies on a fast 1,3-hydride shift mediated by an Ir(III) complex in allylic alcohols followed by oxidation with TEMPO+. The direct conversion of allylic alcohols into acyloins is achieved in a one-pot procedure. Further functionalization of the Cα´ of the α-aminooxy ketone products gives access to highly functionalized unsymmetrical aliphatic ketones, which further highlights the utility of this transformation.
June 21, 2018: Chemistry: a European Journal
Qutuba G Karwi, Golam M Uddin, Kim L Ho, Gary D Lopaschuk
To maintain its high energy demand the heart is equipped with a highly complex and efficient enzymatic machinery that orchestrates ATP production using multiple energy substrates, namely fatty acids, carbohydrates (glucose and lactate), ketones and amino acids. The contribution of these individual substrates to ATP production can dramatically change, depending on such variables as substrate availability, hormonal status and energy demand. This "metabolic flexibility" is a remarkable virtue of the heart, which allows utilization of different energy substrates at different rates to maintain contractile function...
2018: Frontiers in Cardiovascular Medicine
Luis Bering, Melina Vogt, Felix M Paulussen, Andrey P Antonchick
Selective oxidative homo- and cross-coupling of electron-rich phenols and anilides was developed using nitrosonium tetrafluoroborate as a catalyst. Oxidative coupling of phenols revealed unusual selectivities, which translated into the unprecedented synthesis of inverse Pummerer-type ketones. Mechanistic studies suggest that oxidative coupling of phenols and anilides shares a common pathway via homolytical heteroatom-hydrogen bond cleavage. Nitrosonium salt catalysis was applied for cross-dehydrogenative coupling initiated by generation of heteroatom-centered radicals...
June 21, 2018: Organic Letters
Zhargal Alexandrovich Tykheev, Svetlana Vasilievna Zhigzhitzhapova, Faqi Zhang, Vasiliy Vladimirovich Taraskin, Oleg Arnoldovich Anenkhonov, Larisa Dorzhievna Radnaeva, Shilong Chen
The essential oils and lipid fraction extracted from the aerial parts of Bupleurum scorzonerifolium were determined by a GC-MS method. In total, up to 67 components were identified. cis - β -Ocimene, trans - β -ocimene, limonene, α -pinene, α -copaene, β -elemene, and caryophyllene oxide were recognized as consistent components of the essential oil extracted from the aerial parts of B. scorzonerifolium , regardless of the habitat. The content of these components varied from traces to a significant amount...
June 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Tianqi Li, Shanshan Sun, Jinyue Zhang, Kai Qu, Liu Yang, Changlu Ma, Xiangju Jin, Haibo Zhu, Yinghong Wang
ABSTRACT:Hyperlipidemia is one of the main causes of obesity, type 2 diabetes mellitus (T2DM) and atherosclerosis. The adenosine derivative, 2', 3', 5'-tri-acetyl-N6-(3-hydroxylaniline) adenosine (IMM-H007) is an effective lipid-lowering compound that has important implications for the development of lipid-lowering drugs. Metabolomic analysis based on 1H-NMR was used to monitor dynamic changes in diverse biological media including serum, liver, urine, and feces in response to high-fat diet (HFD) and IMM-H007 treatments...
June 21, 2018: Journal of Proteome Research
Yu-Mou Chou, Chen-June Seak, Zhong Ning Leonard Goh, Joanna Chen-Yeen Seak, Chen-Ken Seak, Chih-Chuan Lin
RATIONALE: Diabetic ketoacidosis is a serious and potentially life-threatening acute complication of diabetes mellitus (DM). Euglycemic diabetic ketoacidosis (eDKA) is however challenging to identify in the emergency department (ED) due to absence of marked hyperglycemia, often leading to delayed diagnosis and treatment. eDKA has been recently found to be associated with sodium-glucose cotransporter 2 (SGLT2) inhibitors, one of the newest classes of antidiabetics, though there are very limited reports implicating dapagliflozin as the offending agent in ED patients...
June 2018: Medicine (Baltimore)
Kaiqing Ma, Brandon S Martin, Xianglin Yin, Mingji Dai
Covering: 2000-2018In this review, we highlight recent examples of natural product total syntheses employing transition metal-mediated/catalyzed carbonylative cyclization strategies to build key ring systems. It mainly covers carbonylative cyclizations for the construction of O-heterocycles, N-heterocycles and carbocycles including cyclic ketones and phenols. The reaction types include carbonylation of epoxide to β-lactones, carbonylative (macro)lactonization/lactamization, the Semmelhack reaction, tandem hydroformylation-cyclization, the Pauson-Khand reaction, carbonylative C-H activation cyclization, the Stille/Suzuki carbonylation, [n + m + 1] carbonylative cycloaddition, the Dötz annulation, and others...
June 20, 2018: Natural Product Reports
Meng Wang, Hua-Li Qin, Jing Leng, Ameeduz Zafar, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja, Muhammad Ajaz Hussain, Syed Nasir Abbas Bukhari
In the current study, a series of new ligustrazine-based chalcones was synthesized. For insertion of tetramethylpyrazine (TMP, also designated as ligustrazine) in chemical backbone of chalcone a new ligustrazine-based aldehyde was prepared. New ketones were synthesized for inclusion of quinazolin-4-yl amino and pyrazin-2-yl amino moieties. The newly synthesized compounds were screened for acetylcholinesterase, butyrylcholinesterase and monoamine oxidases (MAO) inhibitory activities and also for in vitro cytotoxicity on PC12 cells...
June 19, 2018: Chemical Biology & Drug Design
A Melmer, P Kempf, L Lunger, T R Pieber, J K Mader, C Stettler, H Tilg, C F Ebenbichler, M Laimer
We investigated short-term effects of dapagliflozin as adjunct to insulin on insulin sensitivity, postprandial glucose excursions, and ketone body production in T1DM. Seven male patients completed the randomized, double-blind, placebo controlled cross-over trial and received 10mg of dapagliflozin daily for 3 days followed by placebo, or reverse. At day 3, hyperinsulinemic, euglycemic clamps and oral glucose tolerance test clamps with repeated blood sampling were performed. Required glucose infusion and blood glucose excursions did not differ significantly between dapagliflozin and placebo (p=0...
June 19, 2018: Diabetes, Obesity & Metabolism
Christopher L Rock, Thomas L Groy, Ryan J Trovitch
The synthesis of alkylphosphine-substituted α-diimine (DI) ligands and their subsequent addition to Ni(COD)2 allowed for the preparation of (iPr2PPrDI)Ni and (tBu2PPrDI)Ni. The solid state structures of both compounds were found to feature a distorted tetrahedral geometry that is largely consistent with the reported structure of the diphenylphosphine-substituted variant, (Ph2PPrDI)Ni. To explore and optimize the synthetic utility of this catalyst class, all three compounds were screened for benzaldehyde hydrosilylation activity at 1...
June 20, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Robert H Morris
This perspective reviews our efforts to use a mechanism-based approach to develop catalysts for the asymmetric hydrogenation of prochiral ketones and imines. A goal is to discover catalysts based on the abundant 3d transition metals, particularly iron.
June 20, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Fei Zhao, Xiao-Yu Guo, Zhen-Peng Dong, Zhi-Liang Liu, Yan-Qin Wang
Five new 3D isostructural lanthanide metal organic frameworks (Ln-MOFs), [Ln(HL)1.5(H2O)(DMF)]·2H2O (Ln = GdIII (1), SmIII (2), DyIII (3), EuIII (4) and TbIII (5), H3L = 5-(3',5'-dicarboxylphenyl) nicotinic acid) were synthesized by solvothermal methods and studied by structural analyses, magnetic analyses and luminescence sensing. Crystallographic studies revealed that these compounds are 3D frameworks in which the LnIII-COO chains with alternating four and two carboxylate bridges are interlinked by the organic ligands L, and contain microporous channels with accessible Lewis-base sites, coordinated water molecules and uncoordinated carboxyl groups, which are easy to combine and recognise various analytes...
June 20, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Xiao-Wei Ma, Mu-Qing Su, Hong-Xia Wu, Yi-Gang Zhou, Song-Biao Wang
Despite abundant published research on the volatile characterization of mango germplasm, the aroma differentiation of Chinese cultivars remains unclear. Using headspace solid phase microextraction (HS-SPME) coupled with gas chromatography⁻mass spectrometry (GC-MS), the composition and relative content of volatiles in 37 cultivars representing the diversity of Chinese mango germplasm were investigated. Results indicated that there are distinct differences in the components and content of volatile compounds among and within cultivars...
June 19, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Krishna Pillai Kaliappan, Parthasarathi Subramanian
An efficient multicomponent reaction leading to the synthesis of stereo-enriched cyclopentyl-isoxazoles from camphor derived α-oxime, alkynes and MeOH is reported. Our method involves a series of cascade transformations such as in situ generation of catalyst I(III) which catalyzes the addition MeOH into a sterically hindered ketone, oxime oxidation and α-hydroxyiminium ion rearrangement to generate in situ nitrile oxide which upon [3+2]-cycloaddition reaction with alkynes delivers regioselective products...
June 19, 2018: Chemistry, An Asian Journal
Zia Ud Din, Marilia Almeida Trapp, Lívia Soman de Medeiros, Danielle Lazarin-Bidóia, Francielle Pelegrin Garcia, Francieli Peron, Celso Vataru Nakamura, Ihosvany Camps Rodríguez, Abdul Wadood, Edson Rodrigues-Filho
Symmetrical and unsymmetrical bis-aryl-α,β-unsaturated ketones were synthesized in moderate to excellent yield by treating cyclohexanone with various aldehydes. Dimethylammonium dimethylcarbamate (DIMCARB) was used as both catalyst and reaction medium for the synthesis of monoarylidenes cycloadduct intermediates, which was further used to produce diarylidene cyclohexanones. All the 34 compounds synthesized were evaluated for their anti-proliferative activity, particularly against promastigote of Leishmania amazonensis, epimastigoteand trypomastigoteof Trypanosoma cruzi...
June 14, 2018: European Journal of Medicinal Chemistry
Jian Li, Shuhua Bai, Yang Li, Zhengbing Wang, Xiaoyu Huo, Li Liu
A Cu-catalyzed three-component cascade cyclization among 2-formylbenzonitrile, cyclopropyl ketones and diaryliodonium salts for construction of fused isoindolin-1-one compounds is achieved. Pentacyclic isoindolinone derivatives could be obtained in moderate to good yields. The proposed mechanism involved ring expansion of cyclopropyl ketones / formation of N-acyliminium / hetero- [4+2]-cycloaddition process is described.
June 19, 2018: Journal of Organic Chemistry
Ying-Na Yue, Sheng Zeng, Hui Wang, Shuo Wang, Huan Wang, Jia-Xing Lu
A simple protocol to synthesize D-phenylalanine (D-PHE)-functionalized multi-walled carbon nanotubes (MWCNTs) via one-pot method was established by grafting D-PHE onto MWCNTs to obtain D-PHE-MWCNTs under mild reaction conditions. The resulting D-PHE-MWCNTs were detailedly characterized via spectroscopy and surface analysis. The electroreduction of 2,2,2-trifluoroacetophenone at D-PHE-MWCNTs cathode afforded (S)-α-(trifluoromethyl) benzyl alcohol whose yield was 65% and the enantiomeric excess was 40%. No extra catalysts were required in this electrochemical reaction solution compared with other reactions requiring homogeneous catalysis...
June 19, 2018: ACS Applied Materials & Interfaces
P Alarcon, C Manosalva, M D Carretta, A I Hidalgo, C D Figueroa, A Taubert, C Hermosilla, M A Hidalgo, R A Burgos
Fatty and hydroxycarboxylic acids are one of the main intermediates of energy metabolism in ruminants and critical in the milk production of cattle. High production demands on a dairy farm can induce nutritional imbalances and metabolism disorders, which have been widely associated with the onset of sterile inflammatory processes and increased susceptibility to infections. The literature suggests that short-chain fatty acids (SCFA), long-chain fatty acids (LCFA) and hydroxycarboxylic acids are relevant modulators of the host innate inflammatory response...
July 2018: Veterinary Immunology and Immunopathology
Mark Christian Manio, Shigenobu Matsumura, Kazuo Inoue
BACKGROUND: Diets containing fats of different proportions and types have been demonstrated to influence metabolism. These fats differ in long chain fatty acids (LCFAs) or medium chain fatty acids (MCFAs) content. In our laboratory using swimming as the training modality, MCFAs increased endurance attributed to increased activities of oxidative enzymes. How it affects whole-body metabolism remains unexplored. The present study investigated the metabolic, biochemical and genetic adaptations with treadmill running as the training modality...
June 18, 2018: Journal of the International Society of Sports Nutrition
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