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Na-Ra Han, Phil-Dong Moon, Min-Sun Yoo, Ka-Jung Ryu, Hyung-Min Kim, Hyun-Ja Jeong
The aim of this study is to determine whether AST2017-01 which consists of Rumex crispus and Cordyceps militaris would improve atopic dermatitis (AD). We analyzed anti-AD effects of AST2017-01 and chrysophanol, a bioactive compound of AST2017-01, using a 2,4-dinitrofluorobenzene-induced AD murine model. AST2017-01 and chrysophanol relieved clinical severity in AD-like skin lesions and significantly decreased scratching behavior. The thickness of epidermis and infiltration of inflammatory cells in AD-like skin lesions were reduced by AST2017-01 or chrysophanol...
July 16, 2018: International Immunopharmacology
M Delannoy, S Yehya, D Techer, A Razafitianamaharavo, A Richard, G Caria, M Baroudi, E Montargès-Pelletier, G Rychen, C Feidt
Chlordecone (Kepone or CLD) is a highly persistent pesticide formerly used in French West Indies. Nowadays high levels of this pesticide are still found in soils which represent a subsequent source of contamination for outdoor-reared animals. In that context, sequestering matrices like biochars or activated carbons (ACs) are believed to efficiently decrease the bioavailability of such compounds when added to contaminated soils. The present study intends to test the respective efficiency of soil amendment strategies using commercial ACs or biochars (obtained by a 500 °C or 700 °C pyrolysis of 4 distinct type of wood)...
May 30, 2018: Chemosphere
Yuting Chen, Na Zhu, Yuyi Luo, Keqi Hu, Yungang Liu
Polychlorinated biphenyls (PCBs) as a group of persistent organic pollutants are confirmed human carcinogens; however, their mutagenicity remains mostly unknown. We have reported the mutagenicity of some PCBs with one to four chlorines in mammalian cells expressing human CYP2E1. To further explore the structural requirements for the mutagenicity of PCBs, eight tri- and tetrachlorobiphenyls untested before were investigated for the induction of gene mutations and micronuclei in a V79-derived cell line expressing both human CYP2E1 and sulfotransferase (SULT) 1A1 (V79-hCYP2E1-hSULT1A1), with SULT1A1 activity inhibited by pentachlorophenol, a potent SULT1 inhibitor...
July 11, 2018: Chemosphere
Islam Zaki, Mohammed K Abdelhameid, Ibrahim M El-Deen, Abdel Hady A Abdel Wahab, Abeer M Ashmawy, Khaled O Mohamed
Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show a potent inhibitory activity of cell proliferation and cell cycle arrest at G2 /M phase. Compounds 4c, 5e and 7c exhibit low to moderate β-tubulin polymerization inhibition percentage. Meanwhile, compound 6c displayed excellent β-tubulin percentage of polymerization inhibition equivalent to that exhibited by podo...
July 7, 2018: European Journal of Medicinal Chemistry
Martín Estrada Valencia, Clara Herrera-Arozamena, Lucía de Andrés, Concepción Pérez, José A Morales-García, Ana Pérez-Castillo, Eva Ramos, Alejandro Romero, Dolores Viña, Matilde Yáñez, Erik Laurini, Sabrina Pricl, María Isabel Rodríguez-Franco
In this work we describe neurogenic and neuroprotective donepezil-flavonoid hybrids (DFHs), exhibiting nanomolar affinities for the sigma-1 receptor (σ1 R) and inhibition of key enzymes in Alzheimer's disease (AD), such as acetylcholinesterase (AChE), 5-lipoxygenase (5-LOX), and monoamine oxidases (MAOs). In general, new compounds scavenge free radical species, are predicted to be brain-permeable, and protect neuronal cells against mitochondrial oxidative stress. N-(2-(1-Benzylpiperidin-4-yl)ethyl)-6,7-dimethoxy-4-oxo-4H-chromene-2-carboxamide (18) is highlighted due to its interesting biological profile in σ1 R, AChE, 5-LOX, MAO-A and MAO-B...
July 11, 2018: European Journal of Medicinal Chemistry
Dora C S Costa, Gabriella Silva de Almeida, Vitor Won-Held Rabelo, Lucio Mendes Cabral, Plínio Cunha Sathler, Paula Alvarez Abreu, Vitor Francisco Ferreira, Luiz Cláudio Rodrigues Pereira da Silva, Fernando de C da Silva
Naphthoquinones and 1,2,3-triazoles are structural pharmacophore that is known to impart several cancer cells. This work shows a synthetic methodology to obtain hybrid molecules involving naphthoquinone and triazol scaffold as multiple ligands. A simple and efficient synthetic route was used to prepare a series of sixteen compounds being eight 2-(1-aryl-1H-1,2,3-triazol-4-yl)-2,3-dihydronaphtho[1,2 b]furan-4,5-diones and eight 2-(1-aryl-1H-1,2,3-triazol-4-yl)-2,3-dihydronaphtho[2,3-b]furan-4,9-diones. These compounds were tested in MDA-MB231, Caco-2 and Calu-3 human cancer cells, and among them 7a was the most selective compound on Caco-2 cells, the most sensitized cell line in this study...
July 9, 2018: European Journal of Medicinal Chemistry
Michał Antoszczak, Alicja Urbaniak, Magdalena Delgado, Ewa Maj, Björn Borgström, Joanna Wietrzyk, Adam Huczyński, Youzhong Yuan, Timothy C Chambers, Daniel Strand
The polyether ionophore salinomycin has recently captured much interest due to its potent activity against multi-drug resistant cancer cells and cancer stem cells. Previous studies have shown that either acylation of the C20 position or esterification/amidation of the C1 carboxylate moiety is beneficial in terms of biological properties. In this paper, we present the first analogs combining such modifications. Evaluation of the anti-proliferative activity against a series of cancer cell lines showed that acylation of the C20 hydroxyl group improves the activity of salinomycin C1 amides but not of the corresponding C1 esters...
July 10, 2018: European Journal of Medicinal Chemistry
Jie Quan Wang, Xiaobin Wang, Yang Wang, Wen Jian Tang, Jing Bo Shi, Xin Hua Liu
In this study, twenty curcumin analogue hybrids as potential anticancer agents through regulation protein of TrxR were designed and synthesized. Results of anticancer activity showed that 5,7-dimethoxy-3-(3-(2-((1E, 4E)-3-oxo-5-(pyridin-2-yl)penta-1,4-dien-1- yl)phenoxy)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one (compound 7d) could induce gastric cancer cells apoptosis by arresting cell cycle, break mitochondria function and inhibit TrxR activity. Meanwhile, western blot revealed that this compound could dramatically up expression of Bax/Bcl-2 ratio and high expression of TrxR oxidation...
July 10, 2018: European Journal of Medicinal Chemistry
Yiming Xu, Lichuan Wu, Haroon Ur Rashid, Dewang Jing, Xiaole Liang, Haodong Wang, Xu Liu, Jun Jiang, Lisheng Wang, Peng Xie
Based on the mechanism of action, novel scaffolds as Topo I inhibitors bearing indole and sophoridinine were designed. Preliminary docking study revealed that some molecules among the designed series possessed promising Topo I inhibitor properties. Subsequently, thirty new compounds were synthesized and characterized by 1 H NMR, 13 C NMR, and Mass spectral analyses. The compounds were then screened for their antiproliferative and enzymatic inhibitory activities. The results affirmed the consistency between docking and activities and the rationality of the design strategy...
July 16, 2018: European Journal of Medicinal Chemistry
Nada M Ghanem, Faten Farouk, Riham F George, Safinaz E S Abbas, Ossama M El-Badry
New imidazo[4,5-b]pyridine derivatives were designed, synthesized and screened for their anticancer activity against breast (MCF-7) and colon (HCT116) cancer cell lines. Nine compounds (I, II, IIIa, IIIb, IV, VI, VIIa, VIII, IX) showed significant activity against MCF-7, while six compounds (I, VIIc, VIIe, VIIf, VIII, IX) elicited a remarkable activity against HCT116. Compounds showing significant anticancer activity revealed remarkable CDK9 inhibitory potential (IC50  = 0.63-1.32 μM) relative to sorafenib (IC50  = 0...
July 6, 2018: Bioorganic Chemistry
L F Estrella, V B Ferreira, C Gallistl, M G R Alves, W Vetter, O Malm, F D B Abadio Finco, J P M Torres
Natural compounds from the metabolism of marine organisms have been detected at high concentrations in environmental samples which are not the producers of these compounds. These natural substances are known as halogenated natural products (HNPs). HNPs are possibly toxic halogenated compounds analogous to POPs that may bioaccumulate and biomagnify along the food web and pose a further risk to human and environmental health. The present study analyzed the occurrence of HNPs in the edible muscle of the three most consumed commercial fish species in the state of Rio de Janeiro: sardine (Sardinella brasiliensis), whitemouth croaker (Micropogonias furnieri) and mullet (Mugil liza) from the highly polluted Guanabara Bay (GB) and the less polluted Ilha Grande Bay (IGB)...
July 11, 2018: Environmental Pollution
Cheng Huang, Qingyao Hu, Hanyu Wang, Liping Qiao, Sheng'ao Jing, Hongli Wang, Min Zhou, Shuhui Zhu, Yingge Ma, Shengrong Lou, Li Li, Shikang Tao, Yingjie Li, Diming Lou
On-board emissions measurements were performed on a Handysize-class bulk carrier operating under real-world conditions. Emission factors (EFs) were determined for criteria pollutants such as NOx , CO, total hydrocarbons (THC), and PM; PM composition, including organic and elemental carbon (OC and EC), inorganic species, and a variety of organic compounds and VOC species (including alkanes, alkenes, single-ring aromatics, and oxygenated VOCs) were also analyzed. To investigate the impacts of engine type, fuel, and operating conditions on emissions, measurements were conducted on one main and one auxiliary engines using low- and high-sulfur fuels (LSF and HSF) under actual operating conditions, including at-berth, maneuvering, and cruising at different engine loads...
July 16, 2018: Environmental Pollution
Yu-Hong Huang, Xue-Jing Huang, Xiao-Hong Chen, Quan-Ying Cai, Shaohua Chen, Ce-Hui Mo, Huixiong Lü, Ming-Hung Wong
Di-butyl phthalate (DBP) is a widely used plasticizer, recalcitrant and hazardous organic compound with high detection frequencies and concentrations in water and soil that pose a great threat to human health. A novel endphytic bacterium strain N-1 capable of efficiently degrading DBP and utilizing it as sole carbon source was isolated from Ageratum conyzoides. This bacterium was identified as Bacillus subtilis based on its morphological characteristics and 16S rDNA sequence analysis. Under the optimal culture conditions (pH 7...
July 11, 2018: Journal of Environmental Management
Meghan E Breen, Anna K Mapp
Dysregulation of transcription is found in nearly every human disease, and as a result there has been intense interest in developing new therapeutics that target regulators of transcription. CREB binding protein (CBP) and its paralogue p300 are attractive targets due to their function as `master coactivators'. Although inhibitors of several CBP/p300 domains have been identified, the selectivity of many of these compounds has remained underexplored. Here, we review recent successes in the development of chemical tools targeting several CBP/p300 domains with selectivity acceptable for use as chemical probes...
July 16, 2018: Current Opinion in Chemical Biology
Linh Tran, Julia Kaffy, Sandrine Ongeri, Tâp Ha-Duong
We recently reported that a glycopeptidomimetic molecule significantly delays the fibrillization process of Aβ42 peptide involved in Alzheimer's disease. However the binding mode of this compound, named 3β, was not determined at the atomic scale, hindering our understanding of its mechanism of action and impeding structure-based design of new inhibitors. In the present study, we performed molecular docking calculations and molecular dynamics simulations to investigate the most probable structures of 3β complexed with Aβ protofibrils...
July 19, 2018: ACS Chemical Neuroscience
Shasha Liu, Xiaoxia Liu, Xun Zhang, Meiyun Shi, Hecheng Wang, Yajun Liu
Crizotinib, a drug for anaplastic lymphoma kinase (ALK) positive and c-ros oncogene 1 receptor tyrosine kinase (ROS1) positive non-small cell lung cancer (NSCLC), was structurally optimized via a strategy of structure based fragment replacing. Computational study showed it was beneficial for interaction of crizotinib and ALK to increase the distance between pyridyl ring and phenyl ring in crizotinib, and thus a series of novel glycol diaryl ethers were synthesized. The in vitro anti-tumor activity of synthesized compounds was studied in NSCLC cell line H2228 and neurobalstoma cell line SH-SY5Y...
July 19, 2018: Chemical Biology & Drug Design
Dirk Alpers, Kevin Cole, Corey Stephenson
The photocatalytic preparation of aminoalkylated heteroarenes from haloalkylamides via a 1,4-aryl migration from nitrogen to carbon, conceptually analogous to a radical Smiles rearrangement, is reported. This method enables the substitution of amino groups in heteroaromatic compounds with aminoalkyl motifs under mild, iridium(III)-mediated photoredox conditions. It provides rapid access to thienoazepinone, a pharmacophore present in multiple drug candidates for potential treatment of different conditions, including inflammation and psychotic disorders...
July 19, 2018: Angewandte Chemie
Christian Ottmann, Sebastian A Andrei, Pim de Vink, Eline Sijbesma, Ling Han, Luc Brunsveld, Nobuo Kato, Yusuke Higuchi
The natural product family of fusicoccanes are stabilizers of 14-3-3 mediated protein-protein interactions (PPIs), some of which possess antitumor activity. In this study, we present the first use of molecular dynamics (MD) to rationally design PPI stabilizers with increased potency. Synthesis of a focused library, followed by characterization by fluorescence polarization, mutational studies and X-ray crystallography confirmed the power of the MD-based design approach, revealing the potential for an additional hydrogen bond with the 14-3-3 protein which significantly increased potency...
July 19, 2018: Angewandte Chemie
Reiko Ueoka, Agneya Bhushan, Silke I Probst, Walter M Bray, R Scott Lokey, Roger G Linington, Jörn Piel
The large number of sequenced bacterial genomes provides the opportunity to bioinformatically identify rich natural product sources among previously neglected microbial groups. Testing this discovery strategy, unusually high biosynthetic potential was suggested for the Oceanospirillales member Gynuella sunshinyii, a Gram-negative marine bacterium from the rhizosphere of the halophilic plant Carex scabrifolia. Its genome contains numerous unusual biosynthetic gene clusters for diverse types of metabolites. Genome-guided isolation yielded representatives of four different natural product classes, of which only alteramide A was known...
July 19, 2018: Angewandte Chemie
Stevie van der Mierden, Sergey A Savelyev, Joanna IntHout, Rob B M de Vries, Cathalijn H C Leenaars
Microdialysis is a method to study the extracellular space in vivo, based on the principle of diffusion. It can be used to measure various small molecules including the neuroregulator adenosine. Baseline levels of the compounds measured with microdialysis vary over studies. We systematically reviewed the literature to investigate the full range of reported baseline concentrations of adenosine and AMP in microdialysates. We performed a meta-regression analysis to study the influence of flow rate, probe membrane surface area, species, brain area, and anaesthesia versus freely behaving, on the adenosine concentration...
July 19, 2018: Journal of Neurochemistry
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