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https://www.readbyqxmd.com/read/27916811/design-synthesis-and-biological-evaluation-of-novel-primaquine-cinnamic-acid-conjugates-of-the-amide-and-acylsemicarbazide-type
#1
Kristina Pavić, Ivana Perković, Petra Gilja, Filip Kozlina, Katja Ester, Marijeta Kralj, Dominique Schols, Dimitra Hadjipavlou-Litina, Eleni Pontiki, Branka Zorc
In this paper design and synthesis of a scaffold comprising primaquine (PQ) motif and cinnamic acid derivatives (CADs) bound directly (compounds 3a-k) or via a spacer (compounds 7a-k) are reported. In the first series of compounds, PQ and various CADs were connected by amide bonds and in the second series by acylsemicarbazide functional groups built from the PQ amino group, CONHNH spacer and the carbonyl group originating from the CADs. PQ-CAD amides 3a-k were prepared by a simple one-step condensation reaction of PQ with a series of CAD chlorides (method A) or benzotriazolides 2 (method B)...
November 28, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27916451/progressive-development-of-endometriosis-and-its-hindrance-by-anti-platelet-treatment-in-mice-with-induced-endometriosis
#2
Qi Zhang, Xishi Liu, Sun-Wei Guo
We have recently shown that platelets drive smooth muscle metaplasia (SMM) and fibrogenesis in endometriosis through epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transdifferentiation (FMT). To see whether this is true in vivo, this prospective, randomized, and serially evaluated mouse investigation was conducted. Endometriosis was induced in female Balb/C mice, which were then randomly divided into two groups: Tanshinone IIA (TAN) and control (CTL) groups. TAN mice were treated with TAN but CTL mice received none...
November 21, 2016: Reproductive Biomedicine Online
https://www.readbyqxmd.com/read/27904990/computer-modeling-in-predicting-the-bioactivity-of-human-5-lipoxygenase-inhibitors
#3
Mengdi Zhang, Zhonghua Xia, Aixia Yan
5-Lipoxygenase (5-LOX) is a key enzyme in the inflammatory path. Inhibitors of 5-LOX are useful for the treatment of diseases like arthritis, cancer, and asthma. We have collected a dataset including 220 human 5-LOX inhibitors for classification. A self-organizing map (SOM), a support vector machine (SVM), and a multilayer perceptron (MLP) algorithm were used to build models with selected descriptors for classifying 5-LOX inhibitors into active and weakly active ones. MACCS fingerprints were used in this model building process...
November 30, 2016: Molecular Diversity
https://www.readbyqxmd.com/read/27903619/interleukin-10-mediated-regenerative-postnatal-tissue-repair-is-dependent-on-regulation-of-hyaluronan-metabolism-via-fibroblast-specific-stat3-signaling
#4
Swathi Balaji, Xinyi Wang, Alice King, Louis D Le, Sukanta S Bhattacharya, Chad M Moles, Manish J Butte, Vinicio A de Jesus Perez, Kenneth W Liechty, Thomas N Wight, Timothy M Crombleholme, Paul L Bollyky, Sundeep G Keswani
The cytokine IL-10 has potent antifibrotic effects in models of adult fibrosis, but the mechanisms of action are unclear. Here, we report a novel finding that IL-10 triggers a signal transducer and activator of transcription 3 (STAT3)-dependent signaling pathway that regulates hyaluronan (HA) metabolism and drives adult fibroblasts to synthesize an HA-rich pericellular matrix, which mimics the fetal regenerative wound healing phenotype with reduced fibrosis. By using cre-lox-mediated novel, inducible, fibroblast-, keratinocyte-, and wound-specific STAT3 knockdown postnatal mice-plus syngeneic fibroblast cell-transplant models-we demonstrate that the regenerative effects of IL-10 in postnatal wounds are dependent on HA synthesis and fibroblast-specific STAT3-dependent signaling...
November 30, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27901042/transplanted-photoreceptor-precursors-transfer-proteins-to-host-photoreceptors-by-a-mechanism-of-cytoplasmic-fusion
#5
Mandeep S Singh, Jasmin Balmer, Alun R Barnard, Sher A Aslam, Daniela Moralli, Catherine M Green, Alona Barnea-Cramer, Isabel Duncan, Robert E MacLaren
Photoreceptor transplantation is a potential future treatment for blindness caused by retinal degeneration. Photoreceptor transplantation restores visual responses in end-stage retinal degeneration, but has also been assessed in non-degenerate retinas. In the latter scenario, subretinal transplantation places donor cells beneath an intact host outer nuclear layer (ONL) containing host photoreceptors. Here we show that host cells are labelled with the donor marker through cytoplasmic transfer-94±4.1% of apparently well-integrated donor cells containing both donor and host markers...
November 30, 2016: Nature Communications
https://www.readbyqxmd.com/read/27899976/low-extracellular-lysyl-oxidase-expression-is-associated-with-poor-prognosis-in-patients-with-prostate-cancer
#6
Wei Zheng, Xuejian Wang, Qiwei Chen, Kun Fang, Lina Wang, Feng Chen, Xiancheng Li, Ziyao Li, Jianbo Wang, Yingxi Liu, Deyong Yang, Xishuang Song
Remodeling of the extracellular matrix (ECM), which is induced by lysyl oxidase (LOX), has been demonstrated to accompany tumor progression; however, the association between LOX expression levels and the malignant behavior of prostate cancer (Pca) remains unclear. The present study aimed to analyze the tumor-associated expression profile of LOX in patients with Pca and to evaluate its potential prognostic value. In the form of a retrospective study, the expression patterns of LOX and collagen I were analyzed in patients with benign prostate hyperplasia and Pca by immunohistochemical examination...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27899483/integrin-linked-kinase-is-necessary-for-the-development-of-diet-induced-hepatic-insulin-resistance
#7
Ashley S Williams, Elijah Trefts, Louise Lantier, Carrie Grueter, Deanna P Bracy, Freyja D James, Ambra Pozzi, Roy Zent, David H Wasserman
The liver extracellular matrix (ECM) expands with high fat (HF) feeding. This finding led us to address whether receptors for the ECM, integrins, are key to the development of diet-induced hepatic insulin resistance. Integrin-linked kinase (ILK) is a downstream integrin signaling molecule involved in multiple hepatic processes including those related to differentiation, wound healing and metabolism. We tested the hypothesis that deletion of ILK in mice on a HF diet would disrupt the ECM-Integrin signaling axis thereby preventing the transformation into the insulin resistant liver...
November 29, 2016: Diabetes
https://www.readbyqxmd.com/read/27893808/common-polymorphisms-in-the-5-lipoxygenase-pathway-and-risk-of-incident-myocardial-infarction-a-danish-case-cohort-study
#8
Anders Gammelmark, Michael S Nielsen, Søren Lundbye-Christensen, Anne Tjønneland, Erik B Schmidt, Kim Overvad
BACKGROUND: The 5-lipoxygenase pathway (5-LOX) has been implicated in the development of cardiovascular disease and studies have suggested that genetic polymorphisms related to key enzymes in this pathway may confer risk of myocardial infarction (MI). This study investigated the association of pre-selected genetic polymorphisms in four candidate genes of 5-LOX (arachidonate 5-lipoxygenase and its activating protein (ALOX-5 and FLAP), leukotriene A4 hydroxylase (LTA4-H) and leukotriene C4 synthase (LTC4-S)) with incident MI...
2016: PloS One
https://www.readbyqxmd.com/read/27893755/quantification-of-arachidonic-acid-and-its-metabolites-in-rat-tissues-by-uhplc-ms-ms-application-for-the-identification-of-potential-biomarkers-of-benign-prostatic-hyperplasia
#9
Qiaoxia Bian, Weihui Wang, Nannan Wang, Yan Peng, Wen Ma, Ronghua Dai
To evaluate the potential relationship between benign prostatic hyperplasia (BPH) and the arachidonic acid (AA) metabolome, a UHPLC-MS/MS method has been developed and validated for simultaneous determination of AA and its cyclooxygenase(COX) and lipoxygenase(LOX) pathway metabolites (15-HETE, 12-HETE, TXA2, 5-HETE, AA, PGI2, PGF2α, 8-HETE, PGD2, PGE2 and LTB4) in rat tissues. The analytes were extracted from tissue samples with a protein precipitation procedure and then separated on a Shim-pack XR-ODSC18 column with 0...
2016: PloS One
https://www.readbyqxmd.com/read/27891092/dihydrotanshinone-i-attenuates-atherosclerosis-in-apoe-deficient-mice-role-of-nox4-nf-%C3%AE%C2%BAb-mediated-lectin-like-oxidized-ldl-receptor-1-lox-1-of-the-endothelium
#10
Wenwen Zhao, Chunxia Li, Hongwei Gao, Qin Wu, Jingshan Shi, Xiuping Chen
Dihydrotanshinone I (DHT) is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases. However, its role in atherosclerosis remains unclear. In this study, the effect of DHT on atherosclerosis were investigated using apolipoprotein E-deficient (ApoE(-/-)) mice and endothelial cells. In lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs), DHT (10 nM) decreased lectin-like ox-LDL receptor-1 (LOX-1) and NADPH oxidase 4 (NOX4) expression, reactive oxygen species (ROS) production, NF-κB nuclear translocation, ox-LDL endocytosis and monocytes adhesion...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27887739/differences-in-the-modulation-of-reactive-species-lipid-bodies-cyclooxygenase-2-5-lipoxygenase-and-ppar-%C3%AE-in-cerebral-malaria-susceptible-and-resistant-mice
#11
Tatiana K S Borges, Érica A R Alves, Henda A R Vasconcelos, Fabiana P Carneiro, André M Nicola, Kelly G Magalhães, Maria Imaculada Muniz-Junqueira
Proinflammatory responses are associated with the severity of cerebral malaria. NO, H2O2, eicosanoid and PPAR-γ are involved in proinflammatory responses, but regulation of these factors is unclear in malaria. This work aimed to compare the expression of eicosanoid-forming-enzymes in cerebral malaria-susceptible CBA and C57BL/6 and -resistant BALB/c mice. Mice were infected with Plasmodium berghei ANKA, and the survival rates and parasitemia curves were assessed. On the sixth day post-infection, cyclooxygenase-2 and 5-lipoxygenase in brain sections were assessed by immunohistochemistry, and, NO, H2O2, lipid bodies, and PPAR-γ expression were assessed in peritoneal macrophages...
November 17, 2016: Immunobiology
https://www.readbyqxmd.com/read/27886056/varietal-dependence-of-glvs-accumulation-and-lox-hpl-pathway-gene-expression-in-four-vitis-vinifera-wine-grapes
#12
Xu Qian, Xiao-Qing Xu, Ke-Ji Yu, Bao-Qing Zhu, Yi-Bin Lan, Chang-Qing Duan, Qiu-Hong Pan
Variety is one of the major factors influencing grape and wine aromatic characteristics. Green leaf volatiles (GLVs), derived from lipoxygenase-hydroperoxides lyase (LOX-HPL) pathway, are important components for the aromatic quality of grapes and wines. However, the varietal difference regarding GLVs accumulation and related gene expression are poorly studied. This work exhibited that the accumulation of various GLVs and the expression of LOX-HPL pathway genes in four Vitis vinifera wine grape cultivars: Syrah, Muscat Tchervine, Gewürztraminer and Chardonnay...
November 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27885502/fading-of-wound-induced-volatile-release-during-populus-tremula-leaf-expansion
#13
Miguel Portillo-Estrada, Taras Kazantsev, Ülo Niinemets
The release of stress-driven volatiles throughout leaf development has been little studied. Therefore, we subjected poplar leaves during their developmental stage (from 2 days to 2 weeks old) to wounding by a single punch hole, and measured online the wound-induced volatile organic compound emissions. Our study shows that the emission of certain volatile compounds fades with increasing leaf age. Among these compounds we found lipoxygenase products (LOX products), acetaldehyde, methyl benzoate, methyl salicylate, and mono- and sesquiterpenes...
November 24, 2016: Journal of Plant Research
https://www.readbyqxmd.com/read/27880719/inhibition-of-5-lipoxygenase-downregulates-stemness-and-kills-prostate-cancer-stem-cells-by-triggering-apoptosis-via-activation-of-c-jun-n-terminal-kinase
#14
Sivalokanathan Sarveswaran, Nadimpalli Varma, Shravan Morisetty, Jagadananda Ghosh
The cancer stem cell (CSC) concept suggests that neoplastic clones are maintained exclusively by a rare group of cells possessed with stem cell properties. CSCs are characterized by features that include self-renewal, pluripotency and tumorigenicity, and are thought to be solely responsible for tumor recurrence and metastasis. A hierarchically organized CSC model is becoming increasingly evident for various types of cancer, including prostate cancer. The CD44 (+), CD133 (+) cell subpopulations were isolated from human prostate tumors which exhibit stem-like properties showing therapeutic-resistance, capacity of self-renewal, and exact recapitulation of the original tumor in vivo...
November 17, 2016: Oncotarget
https://www.readbyqxmd.com/read/27877081/p-selectin-mediated-lox-expression-promotes-insulinoma-growth-in-rip1-tag2-mice-by-increasing-tissue-stiffness
#15
Cuiling Qi, Jialin Li, Simei Guo, Mengshi Li, Yuanyuan Li, Jiangchao Li, Qianqian Zhang, Lingyun Zheng, Xiaodong He, Xiaoming Zheng, Yanli He, Lijing Wang, Bo Wei
P-selectin, a cell adhesion molecule, is an important member of the selectin family. Recent studies have shown that P-selectin deletion inhibits tumor growth in Rip1-Tag2 mice by suppressing platelet accumulation in tumor tissues. This study aimed to evaluate whether and how P-selectin affects tumor stiffness in Rip1-Tag2 mice. To explore the role of P-selectin in tissue stiffness, we demonstrated that tumor progression in Rip1-Tag2 mice was correlated with tissue stiffness using immunofluorescence and histological staining...
2016: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/27876853/collagen-cross-linking-insights-on-the-evolution-of-metazoan-extracellular-matrix
#16
Fernando Rodriguez-Pascual, David Anthony Slatter
Collagens constitute a large family of extracellular matrix (ECM) proteins that play a fundamental role in supporting the structure of various tissues in multicellular animals. The mechanical strength of fibrillar collagens is highly dependent on the formation of covalent cross-links between individual fibrils, a process initiated by the enzymatic action of members of the lysyl oxidase (LOX) family. Fibrillar collagens are present in a wide variety of animals, therefore often being associated with metazoan evolution, where the emergence of an ancestral collagen chain has been proposed to lead to the formation of different clades...
November 23, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27872878/serum-antioxidant-capacity-and-peroxide-level-of-seven-healthy-subjects-after-consumption-of-different-foods
#17
Maura N Laus, Mario Soccio, Michela Alfarano, Antonella Pasqualone, Marcello S Lenucci, Giuseppe Di Miceli, Donato Pastore
This article reports experimental data related to the research article entitled "Different effectiveness of two pastas supplemented with either lipophilic or hydrophilic/phenolic antioxidants in affecting serum as evaluated by the novel Antioxidant/Oxidant Balance approach" (M.N. Laus, M. Soccio, M. Alfarano, A. Pasqualone, M.S. Lenucci, G. Di Miceli, D. Pastore, 2016) [1]. Antioxidant status of blood serum of seven healthy subjects was evaluated during four hours after consumption of two functional pastas, supplemented with either bran oleoresin or bran water extract obtained from durum wheat...
December 2016: Data in Brief
https://www.readbyqxmd.com/read/27871380/an-improved-amperometric-l-lactate-biosensor-based-on-covalent-immobilization-of-microbial-lactate-oxidase-onto-carboxylated-multiwalled-carbon-nanotubes-copper-nanoparticles-polyaniline-modified-pencil-graphite-electrode
#18
Kusum Dagar, C S Pundir
An improved amperometric l-lactate biosensor was constructed based on covalent immobilization of lactate oxidase (LOx) from Pediococcus species onto carboxylated multiwalled carbon nanotubes (cMWCNT)/copper nanoparticles (CuNPs)/polyaniline (PANI) hybrid film electrodeposited on the surface of a pencil graphite electrode (PGE). The enzyme electrode was characterized by cyclic voltammetry (CV), scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy and electrochemical impedance spectroscopy (EIS), while CuNPs synthesized by chemical reduction method, were characterized by transmission electron microscopy (TEM), UV spectrascopy and X-ray diffraction (XRD)...
January 2017: Enzyme and Microbial Technology
https://www.readbyqxmd.com/read/27866534/-dihydrotestosterone-inhibits-foam-cell-formation-via-a-lectin-like-ox-low-density-lipoprotein-receptor-mediated-mechanism-in-j774-1-cell-line
#19
Y Qiu, H D Hu, B Q Hu, X Y Chen, P Y Xu, L Cui, P Li, C Liu, L Li
Objective: To investigate the effect of dihydrotestosterone (DHT) on lectin-like ox- low-density lipoprotein (LDL) receptor(LOX-1)expression and foam cell formation in the female macrophage cell line J774.1. Methods: In cultured J774.1 cells, after pretreated with DHT at concentrations of 1×10(-9) mol/L and 1×10(-8) mol/L, ox-LDL-induced LOX-1 expression and foam cell formation were investigated by quantitative real-time PCR, Western blotting, and oil-red O staining. Results: DHT at concentrations of 1×10(-9) mol/L and 1×10(-8) mol/L inhibited ox-LDL-induced LOX-1 mRNA (2...
November 15, 2016: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/27865451/astrocytic-contributions-to-synaptic-and-learning-abnormalities-in-a-mouse-model-of-fragile-x-syndrome
#20
Jennifer L Hodges, Xinzhu Yu, Anthony Gilmore, Hannah Bennett, Michelle Tjia, James F Perna, Chia-Chien Chen, Xiang Li, Ju Lu, Yi Zuo
BACKGROUND: Fragile X syndrome (FXS) is the most common type of mental retardation attributable to a single-gene mutation. It is caused by FMR1 gene silencing and the consequent loss of its protein product, fragile X mental retardation protein. Fmr1 global knockout (KO) mice recapitulate many behavioral and synaptic phenotypes associated with FXS. Abundant evidence suggests that astrocytes are important contributors to neurological diseases. This study investigates astrocytic contributions to the progression of synaptic abnormalities and learning impairments associated with FXS...
September 13, 2016: Biological Psychiatry
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