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Alicia Jiménez-Almarza, Daniel Diez-Iriepa, Mourad Chioua, Beatriz Chamorro, Isabel Iriepa, Ricardo Martínez-Murillo, Dimitra Hadjipavlou-Litina, María Jesús Oset-Gasque, José Marco-Contelles
In this work six PBN-related indanonitrones 1-6 have been designed, synthesized, and their neuroprotection capacity tested in vitro, under OGD conditions, in SH-SY5Y human neuroblastoma cell cultures. As a result, we have identified indanonitrones 1, 3 and 4 (EC50  = 6.64 ± 0.28 μM) as the most neuroprotective agents, and in particular, among them, indanonitrone 4 was also the most potent and balanced nitrone, showing antioxidant activity in three experiments [LOX (100 μM), APPH (51%), DPPH (36...
February 1, 2019: Bioorganic Chemistry
H M Kasralikar, S C Jadhavar, S V Goswami, N S Kaminwar, S R Bhusare
A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via the formation of 2-imino-3-(4-substituted-arylthiazol-2-yl)-thiazolidin-4-ones 3 using substituted aldehydes 4. The 5-acrylidene derivative 5 on cyclisation with phenyl hydrazine give the pyrazolo [3, 4, d] thiazole derivatives 6...
February 8, 2019: Bioorganic Chemistry
Reem Hatamleh, Sanaa Abujilban, Asma'a Shaker AbdelMahdi AbuAbed, Sawsan Abuhammad
OBJECTIVE: This study aimed to examine the effectiveness of a childbirth preparation course on birth outcomes among nulliparous Jordanian women. DESIGN: A randomized control trial pre-test/post-test design was used to assess the effects of a childbirth preparation course conducted in a military hospital in Amman, Jordan from 1 July to 15 September 2016. A total of 133 low-risk nulliparous women were recruited and randomly assigned to either (1) a control group who received standard care in antenatal clinics or (2) an intervention group who received standard care in antenatal clinics as well as a childbirth preparation course specifically designed for the purpose of this study...
February 7, 2019: Midwifery
Bin-Rong Yao, Yue Sun, Shuang-Long Chen, Hao-Dong Suo, Yu-Long Zhang, Hao Wei, Chun-Hua Wang, Feng Zhao, Wei Cong, Wen-Yu Xin, Gui-Ge Hou
To get new anti-hepatoma agents with anti-inflammatory activity and hypotoxicity, a series of dissymmetric pyridyl-substituted 3,5-bis(arylidene)-4-piperidones (BAPs, 25-82) were designed and synthesized. Many of them exhibited potential anti-hepatoma properties against human hepatocellular carcinoma cell lines (HepG2, QGY-7703, SMMC-7721) and hypotoxicity for human normal heptical cell line (HHL-5, LO2), and prominently inhibited lipopolysaccharides (LPS) induced IL-6, TNF-α secretion to exert its anti-inflammatory effect...
February 7, 2019: European Journal of Medicinal Chemistry
Ehab D AlFadly, Perihan A Elzahhar, Anna Tramarin, Salwa Elkazaz, Hossam Shaltout, Marwa M Abu-Serie, Jana Janockova, Ondrej Soukup, Doaa A Ghareeb, Ahmed F El-Yazbi, Rim W Rafeh, Nour-Mounira Z Bakkar, Firas Kobeissy, Isabel Iriepa, Ignacio Moraleda, Manal N S Saudi, Manuela Bartolini, Ahmed S F Belal
Neuroinflammation and cholinergic deficit are key detrimental processes involved in Alzheimer's disease. Hence, in the search for novel and effective treatment strategies, the multi-target-directed ligand paradigm was applied to the rational design of two series of new hybrids endowed with anti-inflammatory and anticholinesterase activity via triple targeting properties, namely able to simultaneously hit cholinesterases, cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX) enzymes. Among the synthesized compounds, triazoles 5b and 5d, and thiosemicarbazide hybrid 6e emerged as promising new hits, being able to effectively inhibit human butyrylcholinesterase (hBChE), COX-2 and 15-LOX enzymes with a higher inhibitory potency than the reference inhibitors tacrine (for hBChE inhibition), celecoxib (for COX-2 inhibition) and both NDGA and Zileuton (for 15-LOX inhibition)...
February 8, 2019: European Journal of Medicinal Chemistry
Yuying Fang, Huihao Zhou, Qiong Gu, Jun Xu
A novel series of tetrahydroisoquinoline-benzimidazole hybrids have been designed and synthesized as multifunctional agents against Alzheimer's disease (AD). These compounds were evaluated for their inhibition of neuroinflammation and human β-secretase (hBACE1), and neuroprotective activity. Among them, compound BD3 possessed significant anti-neuroinflammatory activity (IC50  = 5.07 μM against nitric oxide production) through inhibiting the expression and secretion of proinflammatory cytokines in BV2 cells...
February 4, 2019: European Journal of Medicinal Chemistry
Zhanying Ma, Lingjuan Deng, Guang Fan, Yangqing He
Construction of heterojunctions with band-suitable different semiconductors has been demonstrated to be an efficient approach to enhance the separation of photoinduced electrons and holes. In this paper, highly efficient heterojuction photocatalysts consisted of porous-C3 N4 (p-C3 N4 ) and flowerlike-BiOBr (f-BiOBr) were successfully synthesized via a deposition-hydrothermal method. The SEM and HRTEM images indicated that BiOBr were successfully deposited on the surface of p-C3 N4 and the layered p-C3 N4 /f-BiOBr heterojunctions were formed between p-C3 N4 and f-BiOBr...
February 7, 2019: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Xianglai Li, Xiaolin Shen, Jia Wang, Hyon Il Ri, Chang Yong Mi, Yajun Yan, Xinxiao Sun, Qipeng Yuan
3, 4-Dihydroxyphenylacetic acid (3, 4-DHPA) is a phenolic acid with strong anti-oxidative activity, showing potential applications in food and pharmaceutical industries. In this study, a 3, 4-DHPA biosynthetic pathway was designed by connecting 4-hydroxyphenylacetic acid (4-HPA) biosynthesis with its hydroxylation. The starting strain produced only 46 mg/L of 4-HPA in 48 h. Enhancing the shikimate pathway increased the titer by 19-fold to 923 ± 57 mg/L. Furthermore, pykA and pykF were disrupted to conserve phosphoenolpyruvate for 4-HPA production...
February 13, 2019: Journal of Biotechnology
Gayong Shim, Quoc-Viet Le, Juhan Suh, Sunhee Choi, Gunwoo Kim, Han-Gon Choi, Young Bong Kim, M B Macgregor, Yu-Kyoung Oh
The combination of imaging and anticancer therapy has recently emerged as a promising strategy. However, nonspecific imaging signals and distribution of anticancer drugs at normal tissues limit the specificity of the combination therapy. To overcome the challenges, we designed a system which can selectively visualize cancer tissues and initiate the subsequent action of therapeutic molecules in tumor microenvironment. Exploiting the overexpression of matrix metalloproteinase (MMP) in the tumor microenvironment, we designed a graphene oxide (GO)-based nanosheet system loaded with a pegylated MMP-cleavable imaging probe and an anticancer peptide shielded under the imaging probe...
February 13, 2019: Journal of Controlled Release: Official Journal of the Controlled Release Society
Anamarija Rogina, Andrea Lončarević, Maja Antunović, Inga Marijanović, Marica Ivanković, Hrvoje Ivanković
The synthesis of biologically active scaffolds is focused on the design of cell-sensitive surface by applying cell-adhesive proteins or bioceramic micro (nano) particles. The emerging new strategy for manipulating the biological properties lies in the modification by trace metals found in the living organism. In this work, we have prepared biocompatible chitosan hydrogels modified by copper (II) and zinc (II) ions through complexation interactions. Due to the strong affinity of metal ions towards amino groups of chitosan, we obtained defined and ordered structures of metal ion-chitosan hydrogel without the formation of additional metal species...
February 13, 2019: International Journal of Biological Macromolecules
Marie-Luise Buchholzer, Marion Kirch, Christiane Kirchner, Werner Knoess
The considerable number of homeopathic medicinal products (HMP) on the German market and the staggering breadth of active substances of various origin along with the specific legal requirements of adequate safety principles posed the need to compile data on toxicologically evaluated raw materials. In line with the European regulatory framework, HMP applications must consider appropriate safety standards in analogy to conventional human medicinal products. This review presents an option for a systematic and scientifically substantiated approach for regulatory use...
February 13, 2019: Regulatory Toxicology and Pharmacology: RTP
Shuisheng Hu, Lin Zhu, Cheong Wing Lam, Longhua Guo, Zhenyu Lin, Bin Qiu, Kwok Yin Wong, Guonan Chen, Zhenhua Liu
A copper(II)-based two-dimensional metal-organic framework with nanosheet structure (CuBDC NS) that possesses peroxidase (POx) mimicking activity was prepared. In the presence of hydrogen peroxide, the system catalyses the oxidation of terephthalic acid to a blue-fluorescent product (excitation = 315 nm; emission = 425 nm). Pyrophosphate has a very strong affinity for Cu2+ ion and blocks the POx-mimicking activity of the CuBDC NS. If, however, inorganic pyrophosphatase is present, the POx mimicking activity is gradually restored because pyrophosphate is hydrolyzed...
February 15, 2019: Mikrochimica Acta
Sha Zhu, Xiaoying Wang, Cheng Jing, Yongmei Yin, Nandi Zhou
A colorimetric assay for ATP is described that uses a strategy that combines the concept of split Mg(II)-dependent DNAzyme, split aptamer, and hybridization-induced aggregation of gold nanoparticles (AuNPs). Both ATP aptamer and Mg(II)-dependent DNAzyme are split into two fragments which are allocated to two well-designed DNA probes. The probes also possess mutually complementary stem sequences and spacer sequences. In the presence of ATP, the separated DNAzyme sequences in the two probes assemble via the synchronous recognition of ATP with two fragments of the aptamer...
February 15, 2019: Mikrochimica Acta
Ning Sui, Shuai Li, Yukai Wang, Qingbo Zhang, Shufeng Liu, Qiang Bai, Hailian Xiao, Manhong Liu, Lina Wang, William W Yu
Etched PtCu nanowires (NWs) were synthesized by a hydrothermal reaction and chemical etching process. The NWs are shown to be viable peroxidase (POx) mimics capable of catalyzing the oxidation of the substrate 3,3',5,5'-tetramethylbenzidine (TMB) in the presence of H2 O2 to form a blue-green coloration. The mechanism of catalysis was investigated and the results demonstrated that H2 O2 is decomposed to form hydroxyl radicals which oxidize TMB in the presence of the NWs. Under optimized conditions, a steady-state kinetic analysis revealed that the NWs possess a stronger affinity for H2 O2 and TMB compared to the enzyme horseradish POx...
February 15, 2019: Mikrochimica Acta
Kela Xiao, Xingyong Wang, Haibo Yu
Streptococcus pneumoniae (S. pneumoniae) is a leading human pathogen, which takes large responsibility for severe otitis media, acute meningitis and septicaemia. It encodes up to three distinct sialidases: NanA, NanB and NanC, which are promising drug targets. Recent experimental studies have shown that these three sialidases might work together up to the ultimate step, where NanA and NanB produce N-acetylneuraminic acid (Neu5Ac) and 2,7-anhydro-Neu5Ac following the functions of sialidase and intramolecular trans-sialidase, whilst NanC carries on a ping-pong mechanism that produces or removes 2-deoxy-2,3-didehydro-Neu5AC...
February 15, 2019: Scientific Reports
Ismail Ben Soussia, Sonia El Mouridi, Dawon Kang, Alice Leclercq-Blondel, Lamyaa Khoubza, Philippe Tardy, Nora Zariohi, Marie Gendrel, Florian Lesage, Eun-Jin Kim, Delphine Bichet, Olga Andrini, Thomas Boulin
Mutations that modulate the activity of ion channels are essential tools to understand the biophysical determinants that control their gating. Here, we reveal the conserved role played by a single amino acid position (TM2.6) located in the second transmembrane domain of two-pore domain potassium (K2P) channels. Mutations of TM2.6 to aspartate or asparagine increase channel activity for all vertebrate K2P channels. Using two-electrode voltage-clamp and single-channel recording techniques, we find that mutation of TM2...
February 15, 2019: Nature Communications
Jeong-Hwa Baek, Hong Shik Yun, Gyoo Taik Kwon, Janet Lee, Ju-Young Kim, Yunhui Jo, Jae-Min Cho, Chang-Woo Lee, Jie-Young Song, Jiyeon Ahn, Jae-Sung Kim, Eun Ho Kim, Sang-Gu Hwang
Current lung cancer treatments are far from satisfactory; thus, finding novel treatment targets is crucial. We recently identified procollagen-lysine, 2-oxoglutarate 5-dioxygenase 3 (PLOD3), which is involved in fibrosis and tissue remodeling as a radioresistance-related protein in lung cancer cells; however, its mechanism is unclear. In this study, we designed human PLOD3-specific short interfering (si)RNAs and tested their effects on tumor growth inhibition in vitro and in vivo. PLOD3 knockdown overcame chemoresistance and decreased radioresistance by inducing caspase-3-dependent apoptosis in lung cancer cells...
February 15, 2019: Cell Death & Disease
Da Sol Kim, Seon Woong Kim, Jae Min Song, Soon Young Kim, Kwang-Chul Kwon
BACKGROUND: Despite the growing demand for antimicrobial peptides (AMPs) for clinical use as an alternative approach against antibiotic-resistant bacteria, the manufacture of AMPs relies on expensive, small-scale chemical methods. The small ubiquitin-related modifier (SUMO) tag is industrially practical for increasing the yield of recombinant proteins by increasing solubility and preventing degradation in expression systems. RESULTS: A new vector system, pKSEC1, was designed to produce AMPs, which can work in prokaryotic systems such as Escherichia coli and plant chloroplasts...
February 15, 2019: BMC Biotechnology
Lawrence D Frank, Jennifer L Kuntz, James E Chapman, Eric H Fox, John F Dickerson, Richard T Meenan, Brian E Saelens, Deborah R Young, Janne Boone-Heinonen, Stephen P Fortmann
BACKGROUND: The health impacts of community design have been studied extensively over the past two decades. In particular, public transportation use is associated with more walking between transit stops and shops, work, home and other destinations. Change in transit access has been linked with physical activity and obesity but seldom to health outcomes and associated costs, especially within a causal framework. Health related fiscal impacts of transit investment should be a key consideration in major transit investment decisions...
February 15, 2019: BMC Public Health
Bridie Angela Evans, Alison Porter, Helen Snooks, Vanessa Burholt
BACKGROUND: Public and patient involvement is a routine element of health services research methods to produce better designed and reported studies. Although co-production is recommended when involving people in research, methods for involving people are usually designed and managed by researchers and there is little evidence about methods to co-produce models for effective public and patient involvement. We report the method used by a group of patient and carer service users to develop and implement a model for involving public members in research...
February 15, 2019: BMC Medical Research Methodology
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