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C-H activation

D Yuan, X-M Liu, Z Fang, L-L Du, J Chang, S-H Lin
OBJECTIVE: Diabetic nephropathy (DN) can cause chronic renal insufficiency and significantly reduce the life quality of patients with diabetes mellitus, and may eventually lead to death. The study investigated the expression of endoplasmic reticulum stress-related factors, which have important roles in the progress of DN and to explore effects of resveratrol on DN and the possible mechanism. MATERIALS AND METHODS: Specific pathogen free (SPF) grade healthy male Sprague Dawley (SD) rats were divided into different groups for different treatments...
March 2018: European Review for Medical and Pharmacological Sciences
Y-X Cao, Z-Q Wang, J-X Kang, K Liu, C-F Zhao, Y-X Guo, B-H Jiao
OBJECTIVE: It's of great significance to investigate the novel targets of drugs for the treatment of stroke. In this study, we explored the neuroprotective role of miR-424 in oxygen glucose deprivation (OGD)-induced injuries in PC-12 cells. MATERIALS AND METHODS: PC-12 cells were subjected to OGD stimulation to mimic ischemic injury. The expressions of miR-424 and mitogen-activated protein kinase phosphatase-1 (MKP-1) were altered by transient transfection with miR-424 mimic, miR-424 inhibitor, pEX-MKP-1, or sh-MKP-1...
March 2018: European Review for Medical and Pharmacological Sciences
Y-M Weng, C-R Ke, J-Z Kong, H Chen, J-J Hong, D-S Zhou
OBJECTIVE: To observe the effects of autophagy-related gene 5 (ATG5) on the proliferation, differentiation, and apoptosis of Mc3T3-E1 osteoblast as well as the effects of ATG5 on apoptosis of osteoblasts under the conditions of non-oxidative stress and oxidative stress. MATERIALS AND METHODS: ATG5 overexpressing and silencing cell lines were established in this experiment with lentiviral vector and transcription activator-like effect or nuclease (Talen) technique, respectively, using Mc3T3-E1 cells...
March 2018: European Review for Medical and Pharmacological Sciences
Nagarjuna Reddy K, Subhadra U, Sridhar B, Subba Reddy B V
A novel one-pot strategy has been developed for the construction of spiro-isoindolinone-benzosultams through a Ru(ii)-catalyzed sequential C-C and C-N bond formation. This method is highly atom-economical and compatible with a wide range of substituents. This is the first report on the spirocyclization of 3-aryl N-sulfonyl ketimines with aryl isocyanates to produce highly rigid and pharmaceutically relevant spirocycles through a C-H bond activation.
March 22, 2018: Organic & Biomolecular Chemistry
Jing Tao, Yu-Qin Zhao, Chang-Feng Chi, Bin Wang
In the experiment, crude proteins from spotless smoothhound ( Mustelus griseus ), cartilages were isolated by HCl-Guanidine buffer, and its hydrolysate was prepared using trypsin at pH 8.0, 40 °C with a total enzyme dose of 2.5%. Subsequently, three antioxidant peptides were purified from the hydrolysate using membrane ultrafiltration, anion-exchange chromatography, gel filtration chromatography, and reverse phase high-performance liquid chromatography. The amino acid sequences of isolated peptides were identified as Gly-Ala-Glu-Arg-Pro (MCPE-A); Gly-Glu-Arg-Glu-Ala-Asn-Val-Met (MCPE-B); and Ala-Glu-Val-Gly (MCPE-C) with molecular weights of 528...
March 22, 2018: Marine Drugs
Kyoung In Jung, Yong Chan Kim, Chan Kee Park
Glaucoma is a leading cause of loss of sight. High intraocular pressure (IOP) is the most critical risk factor. However, glaucoma develops even within a normal IOP range. Normal tension glaucoma (NTG) is more common in Asia, whereas high tension glaucoma is more common in Western countries. The pathogenesis of glaucoma, especially NTG, is poorly understood. We evaluated the correlation between dietary nutrient intake and glaucoma using data from subjects ≥40 years old from the ongoing, nationwide, population-based study, the Korean National Health and Nutrition Examination Survey V (2008-2012)...
March 22, 2018: Nutrients
Mingchun Gao, Rongxuan Ye, Weijia Shen, Bin Xu
Copper has been explored as an ideal candidate for replacing noble metals in organic synthesis, especially for practical large scale preparation. Recent decades have witnessed the renaissance and improvement of copper-catalyzed and copper-mediated organic reactions. Copper nitrate is a common inorganic copper salt which has been proved to be a ubiquitous reactant in organic synthesis due to its commercial availability, stability, inexpensiveness and environmentally benign nature. Copper nitrate could be used as a nitration reagent, oxidant, catalyst or promoter, and Lewis acid as well...
March 22, 2018: Organic & Biomolecular Chemistry
Meng-Yi Xu, Albert H C Wong
Schizophrenia is considered primarily as a cognitive disorder. However, functional outcomes in schizophrenia are limited by the lack of effective pharmacological and psychosocial interventions for cognitive impairment. GABA (gamma-aminobutyric acid) interneurons are the main inhibitory neurons in the central nervous system (CNS), and they play a critical role in a variety of pathophysiological processes including modulation of cortical and hippocampal neural circuitry and activity, cognitive function-related neural oscillations (eg, gamma oscillations) and information integration and processing...
March 22, 2018: Acta Pharmacologica Sinica
Kisantini Murugesu, Vikneswaran Murugaiyah, Sultan Ayesh Mohammed Saghir, Mohd Zaini Asmawi, Amirin Sadikun
BACKGROUND: Ethanolic extract of G. procumbens leaves has been previously shown to pos-sess antihyperlipidemic effects. OBJECTIVE: This study was designed to prepare caffeoylquinic acids rich and poor fractions of the ethanol-ic extract using resin column technology and compare their antihyperlipidemic and antioxidant potentials. RESULTS: Among the treatment groups, caffeoylquinic acids rich fraction (F2) and chlorogenic acid (CA, one of the major caffeoylquinic acids) showed potent antihyperlipidemic effects, with significant reduc-tions in total cholesterol (TC), triglycerides (TG), low-density lipoprotein-cholesterol (LDL-C), very low-density lipoprotein-cholesterol (VLDL-C), atherogenic index (AI) and coronary risk index (CRI) (p<0...
March 21, 2018: Current Pharmaceutical Biotechnology
Yuichi Nomura, Yoshitaka Asano, Jun Shinoda, Hirohito Yano, Yuka Ikegame, Tomohiro Kawasaki, Noriyuki Nakayama, Takashi Maruyama, Yoshihiro Muragaki, Toru Iwama
PURPOSE: The aim of this study was to assess whether dynamic PET with11 C-methionine (MET) (MET-PET) is useful in the diagnosis of brain tumors. METHODS: One hundred sixty patients with brain tumors (139 gliomas, 9 meningiomas, 4 hemangioblastomas and 8 primary central nervous system lymphomas [PCNSL]) underwent dynamic MET-PET with a 3-dimensional acquisition mode, and the maximum tumor MET-standardized uptake value (MET-SUV) was measured consecutively to construct a time-activity curve (TAC)...
March 21, 2018: Journal of Neuro-oncology
Ruirui Li, Pengfei Gu, Xiangyu Fan, Junyu Shen, Yulian Wu, Lixuan Huang, Qiang Li
A polyhydroxyalkanoate (PHA)-producing strain was isolated from propylene oxide (PO) saponification wastewater activated sludge and was identified as Brevundimonas vesicularis UJN1 through 16S rDNA sequencing and Biolog microbiological identification. Single-factor and response surface methodology experiments were used to optimize the culture medium and conditions. The optimal C/N ratio was 100/1.04, and the optimal carbon and nitrogen sources were sucrose (10 g/L) and NH4 Cl (0.104 g/L) respectively. The optimal culture conditions consisted of initial pH of 6...
March 21, 2018: Applied Biochemistry and Biotechnology
Youzhi Miao, Yanqiong Kong, Pan Li, Guangqi Li, Dongyang Liu, Qirong Shen, Ruifu Zhang
Xylanase with a high thermostability will satisfy the needs of raising the temperature of hydrolysis to improve the rheology of the broth in industry of biomass conversion. In this study, a xylanase gene (xyn10A), predicted to encode a hydrolase domain of GH10, a linker region and a CBM1 domain, was cloned from a superior lignocellulose degrading strain Aspergillus fumigatus Z5 and successfully expressed in Pichia pastoris X33. Xyn10A has a specific xylanase activity of 34.4 U mg-1 , and is optimally active at 90 °C and pH 6...
March 21, 2018: AMB Express
Andrew T Hale, Kelly Pekala, Benjamin Theobald, Katherine Kelly, Michael Wolf, John C Wellons, Truc Le, Chevis N Shannon
PURPOSE: In traumatic brain injury (TBI), hyperglycemia and hypothermia are thought to be associated with poor outcomes, but have not been systematically studied in children. Thus, our aim was to evaluate whether serum glucose and temperature at admission, among other clinical variables, were associated with need for post hospital-discharge seizure medication in children diagnosed with TBI. METHODS: We performed a retrospective study of 1814 children who were diagnosed with TBI at a tertiary pediatric hospital...
March 21, 2018: Child's Nervous System: ChNS: Official Journal of the International Society for Pediatric Neurosurgery
Vikas Pathak, Robert Aris, Brian C Jensen, Wei Huang, Hubert James Ford
BACKGROUND: Plasma pro-BNP (brain natriuretic peptide) levels are often elevated in response to right ventricular (RV) volume and pressure overload, parameters potentially affected by exercise. Plasma pro-BNP levels change in association with long-term changes in pulmonary hemodynamics, thereby serving as a potential biomarker in pulmonary arterial hypertension (PAH). The 6-min Walk Test (6MWT) and pro-BNP level are often checked in a single office visit. There is no universal standard for measuring Pro-BNP levels relative to the timing of the 6MWT...
March 21, 2018: Lung
Yang Q Xia, Ren J Hua, Chen Juan, Zhou H Zhong, Cheng S Tao, Ren Fang, He Lin, Gong Rui, Chen Yong
Multidrug resistance (MDR) due to overexpression of MDR1 is a major obstacle that hinders the treatment of hepatocellular carcinoma (HCC). In this study, we explored the function and underlying molecular mechanism of SIRT6 in MDR of HCC. Chemotherapeutic agents (doxorubicin, cisplatin, and sorafenib) treatment increased SIRT6 mRNA and protein level in two HCC cell lines in a dose-dependent manner. SIRT6 depletion resulted in decreased cell viability and increased apoptosis in HCC cells treated with chemotherapeutic agents...
2018: Frontiers in Pharmacology
L R Brewster, J J Dale, T L Guttridge, S H Gruber, A C Hansell, M Elliott, I G Cowx, N M Whitney, A C Gleiss
Discerning behaviours of free-ranging animals allows for quantification of their activity budget, providing important insight into ecology. Over recent years, accelerometers have been used to unveil the cryptic lives of animals. The increased ability of accelerometers to store large quantities of high resolution data has prompted a need for automated behavioural classification. We assessed the performance of several machine learning (ML) classifiers to discern five behaviours performed by accelerometer-equipped juvenile lemon sharks ( Negaprion brevirostris ) at Bimini, Bahamas (25°44'N, 79°16'W)...
2018: Marine Biology
Shunji Xie, Zebin Shen, Jiao Deng, Pu Guo, Qinghong Zhang, Haikun Zhang, Chao Ma, Zheng Jiang, Jun Cheng, Dehui Deng, Ye Wang
The development of new methods for the direct transformation of methanol into two or multi-carbon compounds via controlled carbon-carbon coupling is a highly attractive but challenging goal. Here, we report the first visible-light-driven dehydrogenative coupling of methanol into ethylene glycol, an important chemical currently produced from petroleum. Ethylene glycol is formed with 90% selectivity and high efficiency, together with hydrogen over a molybdenum disulfide nanofoam-modified cadmium sulfide nanorod catalyst...
March 21, 2018: Nature Communications
D Dumuid, L K Lewis, T S Olds, C Maher, C Bondarenko, L Norton
OBJECTIVE: Older adults' health has been linked with time in moderate-to-vigorous physical activity (MVPA), and recent studies suggest time in sedentary behaviour may also be important. Time-use behaviours (MVPA, light physical activity, sedentary time and sleep) are co-dependent, and therefore their associations with health should be examined in an integrated manner. This is the first study to investigate the relationship between older adults' reallocation of time among these time-use behaviours and markers of cardio-respiratory fitness, obesity and cardio-metabolic risk...
April 2018: Maturitas
Richard P Tan, Alex H P Chan, Katarina Lennartsson, Maria M Miravet, Bob S L Lee, Jelena Rnjak-Kovacina, Zoe E Clayton, John P Cooke, Martin K C Ng, Sanjay Patel, Steven G Wise
BACKGROUND: Induced pluripotent stem-cell derived endothelial cells (iPSC-ECs) can be generated from any somatic cell and their iPSC sources possess unlimited self-renewal. Previous demonstration of their proangiogenic activity makes them a promising cell type for treatment of ischemic injury. As with many other stem cell approaches, the low rate of in-vivo survival has been a major limitation to the efficacy of iPSC-ECs to date. In this study, we aimed to increase the in-vivo lifetime of iPSC-ECs by culturing them on electrospun polycaprolactone (PCL)/gelatin scaffolds, before quantifying the subsequent impact on their proangiogenic function...
March 21, 2018: Stem Cell Research & Therapy
Alan Jiang, Qiufeng Liu, Ruifeng Wang, Peng Wei, Yang Dai, Xin Wang, Yechun Xu, Yuchi Ma, Jing Ai, Jingkang Shen, Jian Ding, Bing Xiong
Fibroblast growth factor receptors (FGFRs), a subfamily of receptor tyrosine kinases, are aberrant in various cancer types, and considered to be promising targets for cancer therapy. We started with a weak-active compound that was identified from our internal hepatocyte growth factor receptor (also called c-Met) inhibitor project, and optimized it with the guidance of a co-crystal structure of compound 8 with FGFR1. Through rational design, synthesis, and the biological evaluation of a series of 5 H -pyrrolo[2,3- b ]pyrazine derivatives, we discovered several potent FGFR kinase inhibitors...
March 19, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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