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https://www.readbyqxmd.com/read/28088783/%C3%AE-asarone-blocks-7%C3%AE-hydroxycholesterol-exposed-macrophage-injury-through-blocking-elf2%C3%AE-phosphorylation-and-prompting-beclin-1-dependent-autophagy
#1
Sin-Hye Park, Min-Kyung Kang, Yean-Jung Choi, Yun-Ho Kim, Lucia Dwi Antika, Dong Yeon Kim, Eun-Jung Lee, Soon Sung Lim, Young-Hee Kang
Macrophage apoptosis is salient in advanced atherosclerotic lesions and is induced by several stimuli including endoplasmic reticulum (ER) stress. This study examined that α-asarone present in purple perilla abrogated macrophage injury caused by oxysterols via ER stress- and autophagy-mediated mechanisms. Nontoxic α-asarone at 1-20 μM attenuated 7β-hydroxycholesterol-induced activation of eukaryotic initiation factor 2α in macrophages leading to C/EBP homologous protein (CHOP) expression and apoptosis due to sustained ER stress...
January 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28088720/role-of-dissolved-mn-iii-in-transformation-of-organic-contaminants-non-oxidative-versus-oxidative-mechanisms
#2
Erdan Hu, Ya Zhang, Shuyan Wu, Jun Wu, Liyuan Liang, Feng He
Mn(III) is a strong oxidant for one electron transfer, which may be important in the transformation of organic contaminants during water/wastewater treatment and biogeochemical redox processes. This study explored the reaction mechanisms of dissolved Mn(III) with organics. The role of dissolved Mn(III) either as a catalyst or an oxidant in reactions with organics was recognized. Aquo and/or hydroxo (or free) Mn(III), generated from the bisulfite activated permanganate process, facilitated efficient N-dealkylation of atrazine via a β-elimination mechanism, resulting no net redox reaction...
January 7, 2017: Water Research
https://www.readbyqxmd.com/read/28088709/characterization-of-smokeless-powders-using-multiplexed-collision-induced-dissociation-mass-spectrometry-and-chemometric-procedures
#3
Kristen L Reese, A Daniel Jones, Ruth Waddell Smith
This work demonstrates a non-targeted mass spectrometry approach for identification of organic compounds in smokeless powders. Unburned powders were removed from various commercial ammunitions of different brand, primer composition, caliber, and age. The unburned powders and corresponding fired residues were analyzed by liquid chromatography-atmospheric pressure chemical ionization-time-of-flight mass spectrometry (LC-APCI-TOFMS). Multiplexed collision-induced dissociation was performed at increasing collision potentials resulting in successive fragmentation that provided structural information for compound identification in a non-targeted manner...
December 21, 2016: Forensic Science International
https://www.readbyqxmd.com/read/28088700/chlorogenic-acid-ameliorated-concanavalin-a-induced-hepatitis-by-suppression-of-toll-like-receptor-4-signaling-in-mice
#4
Yinglin Yuan, Xia Gong, Li Zhang, Rong Jiang, Junxia Yang, Bin Wang, Jingyuan Wan
Chlorogenic acid (CGA), one of the most abundant dietary polyphenolic compounds, has been reported to exhibit anti-inflammatory ability. However, the hepatoprotective effects and molecular mechanisms of CGA on concanavalin A (Con A)-induced hepatitis have not been explored. In the present study, we found that pretreatment with CGA dose-dependently inhibited the elevation of plasma aminotransferases and alleviated hepatic pathological damage as well as hepatocyte apoptosis in Con A-exposed mice. Additionally, CGA markedly suppressed the production of serum tumor necrosis factor (TNF)-α and interferon (IFN)-γ, alleviated the infiltration of hepatic macrophages, neutrophils, and activated CD4(+) T lymphocytes in Con A-primed mice...
January 12, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28088663/development-and-validation-of-a-sensitive-and-fast-uplc-ms-ms-method-for-simultaneous-determination-of-seven-bioactive-compounds-in-rat-plasma-after-oral-administration-of-guizhi-gancao-decoction
#5
Bin Ji, Limeng Zhuo, Bin Yang, Yang Wang, Lin Li, Miao Yu, Yunli Zhao, Zhiguo Yu
Rapid, sensitive, selective and accurate UPLC-MS/MS method was developed and fully validated for simultaneous determination of cinnamaldehyde, cinnamic acid, 2-methoxy cinnamic acid, glycyrrhizic acid, glycyrrhetinic acid, liquiritigenin and isoliquiritin in rat plasma after oral administration of Guizhi-gancao decoction. Plasma samples were processed with a simple protein precipitation technique using acetonitrile, followed by chromatographic separation using a Thermo Hypersil GOLD C18 column. A 11.0min linear gradient elution was used at a flow rate of 0...
January 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28088633/quantitative-analysis-of-lab-to-lab-variability-in-caco-2-permeability-assays
#6
Jong Bong Lee, Atheer Zgair, Dhiaa A Taha, Xiaowei Zang, Leonid Kagan, Tae Hwan Kim, Min Gi Kim, Hwi-Yeol Yun, Peter M Fischer, Pavel Gershkovich
In this study, Caco-2 permeability results from different laboratories were compared. Six different sets of apparent permeability coefficient (Papp) values reported in the literature were compared to experimental Papp obtained in our laboratory. The differences were assessed by determining the root mean square error (RMSE) values between the datasets, which reached levels as high as 0.581 for the training set compounds, i.e. ten compounds with known effective human permeability (Peff). The consequences of these differences in Papp for prediction of oral drug absorption were demonstrated by introducing the Papp into the absorption and pharmacokinetics simulation software application GastroPlus(TM) for prediction of the fraction absorbed (Fa) in humans using calibrated "user-defined permeability models"...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088631/an-esipt-based-two-photon-fluorescent-probe-detection-of-hydrogen-peroxide-in-live-cells-and-tissues
#7
Liyi Zhou, Yongbo Peng, Qianqian Wang, Qinlu Lin
A variety of diseases associated with human aging, which have a strong oxidative stress, but connecting age-related diseases and oxidative stress of the basic molecular mechanisms still insufficiently understood. Oxidative stress origins from the unregulated production of reactive oxygen species (ROS), and oxidative damaging to tissues and organs from subsequent oxidation-reduction chemistry by cellular mismanagement. In particular, H2O2 is a major by-product of ROS in live organisms and a common marker for oxidative stress, and its dynamic equilibrium can have various physiological and pathological consequences...
January 9, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28088572/bcs-class-iv-drugs-highly-notorious-candidates-for-formulation-development
#8
REVIEW
Rohan Ghadi, Neha Dand
BCS class IV drugs (e.g., amphotericin B, furosemide, acetazolamide, ritonavir, paclitaxel) exhibit many characteristics that are problematic for effective oral and per oral delivery. Some of the problems associated include low aqueous solubility, poor permeability, erratic and poor absorption, inter and intra subject variability and significant positive food effect which leads to low and variable bioavailability. Also, most of the class IV drugs are substrate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further potentiates the problem of poor therapeutic potential of these drugs...
January 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28088544/off-site-impacts-of-wildfires-on-aquatic-systems-biomarker-responses-of-the-mosquitofish-gambusia-holbrooki
#9
Bruno Nunes, Vera Silva, Isabel Campos, Joana Luísa Pereira, Patrícia Pereira, Jan Jacob Keizer, Fernando Gonçalves, Nelson Abrantes
The number of wildfires has markedly increased in Mediterranean Europe, including in Portugal. Wildfires are environmentally concerning, not only due to the loss of biodiversity and forest area, but also as a consequence of environmental contamination by specific compounds including metals and polycyclic aromatic compounds (PAHs). These contaminants, mostly bound to ashes, can reach downstream water bodies, namely through surface runoff, being ultimately dispersed by vast areas and contacting with aquatic biota...
January 11, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28088540/multiplexed-site-specific-genome-engineering-for-overproducing-bioactive-secondary-metabolites-in-actinomycetes
#10
Lei Li, Guosong Zheng, Jun Chen, Mei Ge, Weihong Jiang, Yinhua Lu
Actinomycetes produce a large variety of pharmaceutically active compounds, yet production titers often require to be improved for discovery, development and large-scale manufacturing. Here, we describe a new technique, multiplexed site-specific genome engineering (MSGE) via the 'one integrase-multiple attB sites' concept, for the stable integration of secondary metabolite biosynthetic gene clusters (BGCs). Using MSGE, we achieved five-copy chromosomal integration of the pristinamycin II (PII) BGC in Streptomyces pristinaespiralis, resulting in the highest reported PII titers in flask and batch fermentations (2...
January 11, 2017: Metabolic Engineering
https://www.readbyqxmd.com/read/28088493/apoptosis-induced-by-the-methanol-extract-of-salvia-miltiorrhiza-bunge-in-non-small-cell-lung-cancer-through-pten-mediated-inhibition-of-pi3k-akt-pathway
#11
Yin-Tao Ye, Wei Zhong, Pei Sun, Dong Wang, Chen Wang, Li-Min Hu, Jun-Qiang Qian
ETHNOPHARMACOLOGICAL RELEVANCE: Salvia miltiorrhiza Bunge, a well-known traditional Chinese medicinal (TCM) plant, has been used to treat cardiovascular diseases since thousands of years. Many studies have reported that the active component tanshinones displayed a variety of biological activities: antithrombous, antiplatelet aggregation, antioxidant and antitumor promoting. But the mechanism of how the active components working still need to be clarified. The anti-tumor effect of compounds of tanshinone (CTN), the methanol extract of Salvia miltiorrhiza Bunge roots, was investigated...
January 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28088443/quantifying-confidence-in-the-reporting-of-metabolic-biotransformations
#12
David J Ponting, Ernest Murray, Anthony Long
How confident can we be in the assignment of metabolite structures? Are the analytical techniques used sufficient to support hypotheses about what is being formed? In this Feature, we discuss the results of an extensive survey into the analytical techniques used, and their value in the characterisation of metabolites. The survey covers the structures of over 16 000 metabolites formed from 1732 query compounds, covering over 35 years of the literature and a variety of journals. The value of different characterisation techniques is considered, alongside or in the absence of synthetic standards...
January 11, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28088441/resveratrol-limits-epithelial-to-mesenchymal-transition-through-modulation-of-khsrp-hnrnpa1-dependent-alternative-splicing-in-mammary-gland-cells
#13
Arfa Moshiri, Margherita Puppo, Martina Rossi, Roberto Gherzi, Paola Briata
Resveratrol (RESV) is a natural polyphenolic compound endowed with anti-inflammatory, anti-proliferative, as well as pro-apoptotic activities that make it a potential anti-tumor compound. Here we show that RESV counteracts the TGF-β-induced Epithelial to Mesenchymal Transition (EMT) phenotype in mammary gland cells and affects the alternative exon usage of pre-mRNAs that encode crucial factors in adhesion and migration -including CD44, ENAH, and FGFR2- in a panel of immortalized and transformed mammary gland cells...
January 11, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28088406/short-communication-effects-of-vacuum-freeze-drying-on-inactivation-of-cronobacter-sakazakii-atcc29544-in-liquid-media-with-different-initial-inoculum-levels
#14
Rui Jiao, Jina Gao, Xiyan Zhang, Maofeng Zhang, Jiren Chen, Qingping Wu, Jumei Zhang, Yingwang Ye
Vacuum freeze-drying is an important food-processing technology for valid retention of nutrients and bioactive compounds. Cronobacter sakazakii has been reported to be associated with severe infections in neonates through consumption of contaminated powdered infant formula. In this study, effects of vacuum freeze-drying treatment for 12, 24, and 36 h on inactivation of C. sakazakii with different initial inoculum levels in sterile water, tryptic soy broth (TSB), skim milk, and whole milk were determined. Results indicated that the lethality rate of C...
January 11, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28088403/ginkgo-fruit-extract-as-an-additive-to-modify-rumen-microbiota-and-fermentation-and-to-mitigate-methane-production
#15
S Oh, R Shintani, S Koike, Y Kobayashi
Ginkgo fruit, an unused byproduct of the ginkgo nut industry, contains antimicrobial compounds known as anacardic acids. Two major cultivars of ginkgo, Kyuju (K) and Tokuro (T), were evaluated for their potential as a feed additive for ruminants. In batch culture, we incubated a mixture of hay and concentrate in diluted rumen fluid with or without 1.6% (fruit equivalent) ginkgo fruit extract. We conducted another series of batch culture studies to determine the dose response of fermentation. We also conducted continuous culture using the rumen simulation technique (RUSITEC) with cultivar K and carried out a pure culture study to monitor the sensitivity of 17 representative rumen bacterial species to ginkgo extract and component phenolics...
January 11, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28088387/sirt2-mediated-antitumour-effects-of-shikonin-on-metastatic-colorectal-cancer
#16
Li-Li Zhang, Lin Zhan, Yong-Dong Jin, Zhen-Li Min, Can Wei, Qiang Wang, Ya-Jun Chen, Qing-Ming Wu, Xia-Min Hu, Qiong Yuan
SIRT2 is involved in the development of a variety of cancers. Shikonin is a natural compound that is known to have antitumour effects. This study aims to assess the effects of shikonin on the development and metastatic progression of colorectal cancer (CRC) through regulation of SIRT2 expression and whether this effect is related to the phosphorylation of extracellular signal-regulated kinases (ERKs). The results demonstrated that SIRT2 is downregulated in CRC biopsy samples (n = 31) compared with the adjacent non-cancerous tissues (ANCT, n = 26)...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088385/flavonoid-derivative-fla-cn-inhibited-adipocyte-differentiation-via-activating-ampk-and-up-regulating-microrna-27-in-3t3-l1-cells
#17
Chun-Chun Gan, Tian-Wen Ni, Yang Yu, Nan Qin, Ying Chen, Mei-Na Jin, Hong-Quan Duan
Fla-CN (3-O-[(E)-4-(4-cyanophenyl)-2-oxobut-3-en-1-yl] kaempferol) is a semi-synthesized flavonoid derivative of tiliroside which exhibited anti-diabetic effect in vivo. Our previous study revealed the role of Fla-CN in anti-obesity and anti-diabetes in vivo, but the underlying mechanism remained to be addressed. The present study aimed to investigate the mechanism of anti-adipogenesis in vitro. Fla-CN markedly inhibited intracellular lipid accumulation in a dose-dependent manner, and the inhibitory effect was mainly limited to the early stage of adipocyte differentiation in vitro...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088384/the-signalling-mechanisms-of-a-novel-mitochondrial-complex-i-inhibitor-prevent-lipid-accumulation-and-attenuate-tnf-%C3%AE-induced-insulin-resistance-in-vitro
#18
Siobhán Leonard, Laura M Tobin, John B C Findlay
RTC-1 has recently been identified as a member of a new class of anti-diabetic compounds acting through the inhibition of complex I of the mitochondrial respiratory chain (NADH:ubiquinone oxidoreductase) to improve glucose handling and inhibit weight gain in mice fed a high-fat diet (HFD). The exact mechanism by which the reduced activity of NADH:ubiquinone oxidoreductase, in response to RTC-1, promotes these improved metabolic parameters remains to be established. Through extensive in vitro analysis, new molecular insights into these downstream signalling pathways have been obtained...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088359/argentation-chromatography-coupled-to-ultrahigh-resolution-mass-spectrometry-for-the-separation-of-a-heavy-crude-oil
#19
Lilla Molnárné Guricza, Wolfgang Schrader
Simplification of highly complex mixtures such as crude oil by using chromatographic methods makes it possible to get more detailed information about the composition of the analyte. Separation by argentation chromatography can be achieved based on the interaction of different strength between the silver ions (Ag(+)) immobilized through a spacer on the silica gel surface and the π-bonds of the analytes. Heavy crude oils contain compounds with a high number of heteroatoms (N, O, S) and a high degree of unsaturation thus making them the perfect analyte for argentation chromatography...
December 30, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28088354/uncovering-oxysterol-binding-protein-osbp-as-a-target-of-the-anti-enteroviral-compound-ttp-8307
#20
Lucian Albulescu, Joëlle Bigay, Bishyajit Biswas, Marion Weber-Boyvat, Cristina M Dorobantu, Leen Delang, Hilde M van der Schaar, Young-Sik Jung, Johan Neyts, Vesa M Olkkonen, Frank J M van Kuppeveld, Jeroen R P M Strating
The genus Enterovirus (e.g. poliovirus, coxsackievirus, rhinovirus) of the Picornaviridae family of positive-strand RNA viruses includes many important pathogens linked to a range of acute and chronic diseases for which no approved antiviral therapy is available. Targeting a step in the life cycle that is highly conserved provides an attractive strategy for developing broad-range inhibitors of enterovirus infection. A step that is currently explored as a target for the development of antivirals is the formation of replication organelles, which support replication of the viral genome...
January 11, 2017: Antiviral Research
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