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https://www.readbyqxmd.com/read/28431455/uhplc-q-tof-ms-ms-based-screening-and-characterization-of-metabolites-of-cnidilin-in-human-liver-microsomes
#1
Lin Yuan, Yuqian Zhang, Man Liao, Yanyan Liu, Changchen Wan, Lantong Zhang
Cnidilin is an active natural furocoumarin ingredient originating from well-known traditional Chinese medicine Radix Angelicae dahuricae. In the present study, an efficient approach was developed for the screening and identification of cnidilin metabolites using ultra-high performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry. In this approach, an on-line data acquisition method multiple mass defect filter (MMDF) combined with dynamic background subtraction was developed to trace all probable metabolites...
April 21, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28431434/bright-light-suppresses-form-deprivation-myopia-development-with-activation-of-dopamine-d1-receptor-signaling-in-the-on-pathway-in-retina
#2
Si Chen, Zhina Zhi, Qingqing Ruan, Qingxia Liu, Fen Li, Fen Wan, Peter S Reinach, Jiangfan Chen, Jia Qu, Xiangtian Zhou
Purpose: To determine whether dopamine receptor D1 (D1R) signaling pathway activation by bright light (BL) in specific retinal neuronal cell types contributes to inhibiting form-deprivation myopia (FDM) in mice. Methods: Mice (3-weeks old) were raised under either normal light (NL: 100-200 lux) or BL (2500-5000 lux) conditions with or without form deprivation. Refraction changes were evaluated with an eccentric infrared photorefractor, and ocular axial components with optical coherence tomography...
April 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28431432/contrast-sensitivity-and-lateral-inhibition-are-enhanced-with-macular-carotenoid-supplementation
#3
James M Stringham, Kevin J O'Brien, Nicole T Stringham
Purpose: Once deposited in the retina, the so-called macular carotenoids lutein (L), zeaxanthin (Z), and mesozeaxanthin (MZ) have been shown to enhance visual performance. The purpose of our study was to investigate whether increasing macular pigment optical density (MPOD) could enhance lateral inhibitory processes, and thereby improve contrast sensitivity (CS). Methods: A total of 59 young (18-25 years), healthy individuals participated in this 1-year, double-masked, placebo-controlled study...
April 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28431421/sevoflurane-posttreatment-attenuates-lung-injury-induced-by-oleic-acid-in-dogs
#4
Guizhi Du, Shurong Wang, Zhuo Li, Jin Liu
BACKGROUND: In animal models, both sevoflurane and propofol protect against acute lung injury (ALI), especially when administered prior to ALI onset. We hypothesized that when compared to propofol, sevoflurane administration after the onset of acute respiratory distress syndrome would mitigate oleic acid (OA)-induced ALI in dogs. METHODS: Dogs were randomly assigned to receive intravenous OA to induce ALI (n = 7 for each OA group) or saline as an OA control (n = 6 for each control)...
May 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28431406/erk-expression-and-its-correlation-with-stat1-in-esophageal-squamous-cell-carcinoma
#5
Hu Wang, Ying Zhang, Hailong Yun, Shubiao Chen, Yelong Chen, Zhaoyong Liu
BACKGROUND: Esophageal squamous cell carcinoma is one of leading causes of cancer-related deaths in Chaoshan region a high-risk region for esophageal cancer. Extracellular regulated protein kinases (ERK) usually play an important role in cell proliferation and differentiation. However, accumulating evidence has shown that the ERK was aberrantly expressed in cancers and correlated with STAT1 depression. RESULTS: The activated ERK downregulates STAT1 expression in ESCC cell lines and U0126 increases expression of STAT1...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431404/upregulation-of-microrna-125b-by-g-csf-promotes-metastasis-in-colorectal-cancer
#6
Xinghua Zhang, Xiao Ma, Huaying An, Changqing Xu, Wenjo Cao, Wei Yuan, Jie Ma
Although there are reports of miR-125b being dysregulated in colorectal cancer (CRC) and associated with CRC progression, little is known about its intrinsic regulatory mechanisms. Here we detected the expression of miR-125b in CRC tissues, subsequently investigated the effect of miR-125b on the proliferation, apoptosis, cell cycle and metastasis on CRC cells. Our results showed that the expression of miR-125b was significantly decreased in CRC tissues comparing to adjacent tissues. However, with the stimulation of Granulocyte colony-stimulating factor (G-CSF), which was highly expressed in CRC tissues, the expression of miR-125b could be improved...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431397/sensitization-of-tamoxifen-resistant-breast-cancer-cells-by-z-ligustilide-through-inhibiting-autophagy-and-accumulating-dna-damages
#7
Hongyi Qi, Zhuyun Jiang, Chengqiang Wang, Yi Yang, Li Li, Hui He, Zanyang Yu
Autophagy plays a pro-survival role in the tamoxifen-resistant breast cancer cells. Herein we found that autophagy was concomitantly induced in tamoxifen-resistant MCF-7 (MCF-7TR5) cells through the dissociation of Bcl-2 from Beclin 1 and subsequent enhancement of interaction among the ATG14-Beclin1-PI3KC3 complex. Moreover, higher level of DNA damage was observed in MCF-7TR5 cells with the decreased BRCA1 and RAD51 level and the increased Ku80 level. Interestingly, Nur77 was selectively degraded by autophagy, which causes the release of Ku80 from the Nur77-Ku80 complex, resulting in the increase of the DNA binding of Ku80 and DNA-PKcs...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431393/loss-of-tpm4-1-leads-to-disruption-of-cell-cell-adhesions-and-invasive-behavior-in-breast-epithelial-cells-via-increased-rac1-signaling
#8
SukYeong Jeong, SunYoung Lim, Galina Schevzov, Peter W Gunning, David M Helfman
Here we report the identification and characterization of a novel high molecular weight isoform of tropomyosin, Tpm4.1, expressed from the human TPM4 gene. Tpm4.1 expression is down-regulated in a subset of breast cancer cells compared with untransformed MCF10A breast epithelial cells and in highly metastatic breast cancer cell lines derived from poorly metastatic MDA-MD-231 cells. In addition, patients with invasive ductal breast carcinoma show decreased TPM4 expression compared with patients with ductal breast carcinoma in situ, and low TPM4 expression is associated with poor prognosis...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431392/characterization-of-aurora-a-and-its-impact-on-the-effect-of-cisplatin-based-chemotherapy-in-patients-with-non-small-cell-lung-cancer
#9
Peng Kuang, Zuhua Chen, JiaYuan Wang, Zhentao Liu, Jingyuan Wang, Jing Gao, Lin Shen
BACKGROUND AND OBJECTIVE: Aurora A, as a member of serine/threonine kinase family and a common characteristic of epithelial cancers, plays a critical role in cell mitosis. However, the clinical significance of Aurora A in non-small cell lung cancer (NSCLC) remains undetermined. METHODS: The expression of Aurora A in NSCLC and paired normal adjacent lung tissues was determined by immunohistochemistry, Western blot, and reverse transcriptase polymerase chain reaction...
April 18, 2017: Translational Oncology
https://www.readbyqxmd.com/read/28431386/tebuconazole-alters-morphological-behavioral-and-neurochemical-parameters-in-larvae-and-adult-zebrafish-danio-rerio
#10
Stefani Altenhofen, Débora Dreher Nabinger, Melissa Talita Wiprich, Talita Carneiro Brandão Pereira, Maurício Reis Bogo, Carla Denise Bonan
In this study, we evaluated the effects of tebuconazole on morphology and exploratory larvae behavior and adult locomotion. Furthermore, we analyzed the effects of this fungicide on AChE activity and gene expression in zebrafish larvae and in the adult zebrafish brain. Tebuconazole (4 mg/L) increased the ocular distance in larvae and reduced the distance travelled, absolute turn angle, line crossing and time outside area in exposed larvae. Moreover, adult zebrafish that were exposed to this fungicide (4 and 6 mg/L) showed a decrease in distance travelled and mean speed when compared to the control group...
April 8, 2017: Chemosphere
https://www.readbyqxmd.com/read/28431381/zeaxanthin-ameliorates-high-glucose-induced-mesangial-cell-apoptosis-through-inhibiting-oxidative-stress-via-activating-akt-signalling-pathway
#11
Changjiang Ying, Lei Chen, Shanshan Wang, Yizhen Mao, Hongwei Ling, Wei Li, Xiaoyan Zhou
Oxidative stress is a critical factor in the pathophysiology of diabetic kidney disease. Previous study shows that hyperglycaemia aggravates renal injury through oxidative stress in diabetic model, and antioxidants have beneficial effect on diabetic kidney disease. However, the role of antioxidants in the progression of diabetic kidney disease is poorly understood. The aim of this study was to clarify whether zeaxanthin, an antioxidant, could ameliorate mesangial cell injury and if so, identify the related mechanism underlying this protective effect...
April 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28431354/first-example-of-peptides-targeting-the-dimer-interface-of-leishmania-infantum-trypanothione-reductase-with-potent-in%C3%A2-vitro-antileishmanial-activity
#12
Marta Ruiz-Santaquiteria, Pedro A Sánchez-Murcia, Miguel A Toro, Héctor de Lucio, Kilian Jesús Gutiérrez, Sonia de Castro, Filipa A C Carneiro, Federico Gago, Antonio Jiménez-Ruiz, María-José Camarasa, Sonsoles Velázquez
A series of 9-mer and 13-mer amide-bridged cyclic peptides derived from the linear prototype Ac-PKIIQSVGIS-Nle-K-Nle-NH2 (Toro et al. ChemBioChem2013) has been designed and synthesized by introduction of the lactam between amino acid side chains that are separated by one helical turn (i, i+4). All of these compounds were tested in vitro as both dimerization and enzyme inhibitors of Leishmania infantum trypanothione reductase (Li-TryR). Three of the 13-mer cyclic peptide derivatives (3, 4 and 6) inhibited the oxidoreductase activity of Li-TryR in the low micromolar range and they also disrupted enzyme dimerization...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431353/discovery-of-potential-anticancer-multi-targeted-ligustrazine-based-cyclohexanone-and-oxime-analogs-overcoming-the-cancer-multidrug-resistance
#13
Gao-Feng Zha, Hua-Li Qin, Bahaa G M Youssif, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja, Ahmed H Abdelazeem, Syed Nasir Abbas Bukhari
The drug research and development nowadays is focusing on multi-target drugs. In the treatment of cancer, therapies using drugs inhibiting one numerous targets signify a novel viewpoint. In comparison with traditional therapy, multi-targeted drugs directly aim cell subpopulations which are involved in progression of tumor. The current study comprises the synthesis of 34 novel ligustrazine-containing α, β-unsaturated carbonyl-based compounds and oximes. The growth of 5 various cancer cell types was strongly inhibited by ligustrazine-containing oximes as revealed by biological evaluation...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431352/degradation-of-sulfamethoxazole-by-uv-uv-h2o2-and-uv-persulfate-pds-formation-of-oxidation-products-and-effect-of-bicarbonate
#14
Yi Yang, Xinglin Lu, Jin Jiang, Jun Ma, Guanqi Liu, Ying Cao, Weili Liu, Juan Li, Suyan Pang, Xiujuan Kong, Congwei Luo
The frequent detection of sulfamethoxazole (SMX) in wastewater and surface waters gives rise of concerns about their ecotoxicological effects and potential risks to induce antibacterial resistant genes. UV/hydrogen peroxide (UV/H2O2) and UV/persulfate (UV/PDS) advanced oxidation processes have been demonstrated to be effective for the elimination of SMX, but there is still a need for a deeper understanding of product formations. In this study, we identified and compared the transformation products of SMX in UV, UV/H2O2 and UV/PDS processes...
March 28, 2017: Water Research
https://www.readbyqxmd.com/read/28431342/discovery-of-tetrahydrocarbazoles-as-dual-perk-and-prb-inhibitors
#15
Mahesh R Kulkarni, Madhav S Mane, Usha Ghosh, Rajiv Sharma, Nitin P Lad, Ankita Srivastava, Asha Kulkarni-Almeida, Prashant S Kharkar, Vijay M Khedkar, Shivaji S Pandit
The extracellular signal-regulated kinase (ERK) is one of the most important molecular targets for cancer that controls diverse cellular processes such as proliferation, survival, differentiation and motility. Similarly, the Rb (retinoblastoma protein) is a tumor suppressor protein and its function is to prevent excessive cell growth by inhibiting cell cycle progression. When the cell is ready to divide, pRb is phosphorylated, becomes inactive and allows cell cycle progression. Herein, we discovered a new series of tetrahydrocarbazoles as dual inhibitors of pERK and pRb phosphorylation...
March 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431339/novel-coumarin-and-quinolinone-based-polycycles-as-cell-division-cycle-25-a-and-c-phosphatases-inhibitors-induce-proliferation-arrest-and-apoptosis-in-cancer-cells
#16
Clemens Zwergel, Brigitte Czepukojc, Emilie Evain-Bana, Zhanjie Xu, Giulia Stazi, Mattia Mori, Alexandros Patsilinakos, Antonello Mai, Bruno Botta, Rino Ragno, Denise Bagrel, Gilbert Kirsch, Peter Meiser, Claus Jacob, Mathias Montenarh, Sergio Valente
Cell division cycle phosphatases CDC25 A, B and C are involved in modulating cell cycle processes and are found overexpressed in a large panel of cancer typology. Here, we describe the development of two novel quinone-polycycle series of CDC25A and C inhibitors on the one hand 1a-k, coumarin-based, and on the other 2a-g, quinolinone-based, which inhibit either enzymes up to a sub-micro molar level and at single-digit micro molar concentrations, respectively. When tested in six different cancer cell lines, compound 2c displayed the highest efficacy to arrest cell viability, showing in almost all cell lines sub-micro molar IC50 values, a profile even better than the reference compound NCS95397...
April 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431330/gas-forming-liposomes-prepared-using-a-liposomal-magnetoporation-method
#17
Jae Min Lee, Dong Sup Kwag, Yu Seok Youn, Eun Seong Lee
In this study, we report a gas-forming drug carrier engineered using the liposomal magnetoporation method. The liposomes that were magnetoporated under a magnetic shear stress possessed an opened lipid bilayer hole. A photosensitizing model drug (chlorin e6: Ce6) and 1H-1H-2H-perfluoro-1-hexene (PFH, as a volatile gas-forming agent) were efficiently loaded into the opened holes of the magnetoporated liposomes. PFH in the liposomes is vaporized at 50°C and can initiate liposome destabilization. The experimental results demonstrated that the liposomes were destabilized at 50°C efficiently released Ce6 and enhanced Ce6-mediated phototoxicity against KB tumor cells...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28431325/bfgf-neutralization-stimulates-vegf-secretion-in-melanoma-b16-cells
#18
Zhiyong Wang, Pei Wei, Junjian Xiang, Hong Wang
Basic fibroblast growth factor (bFGF), which is expressed by most melanoma cells, can stimulate other growth factors secretion. It is well known that bFGF induces VEGF production; however, the influence of bFGF blockade remains uncertain. Here, we investigated the effect of bFGF neutralization on VEGF expression in B16 melanoma cells. We found that bFGF blockade resulting in increased VEGF expression and activated PI3K/AKT and P44/42 MAPK pathways. Moreover, combined inhibition of bFGF and VEGF led to enhanced activity against B16 tumors in vitro and in vivo...
April 17, 2017: Cytokine
https://www.readbyqxmd.com/read/28431315/effects-of-pm2-5-exposure-on-the-notch-signaling-pathway-and-immune-imbalance-in-chronic-obstructive-pulmonary-disease
#19
Xing-Yu Gu, Xu Chu, Xiao-Li Zeng, Hai-Rong Bao, Xiao-Ju Liu
Chronic Obstructive Pulmonary Disease (COPD) is associated with T lymphocytes subset (Th1/Th2, Th17/Treg) imbalance. Notch signaling pathway plays a key role in the development of the adaptive immunity. The immune disorder induced by fine particulate matter (PM2.5) is related to COPD. The aim of this study was to investigate the mechanism by which PM2.5 influences the Notch signaling pathway leading to worsening immune disorder and accelerating COPD development. A COPD mouse model was established by cigarette smoke exposure...
April 18, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28431314/effect-of-metals-on-microcystin-abundance-and-environmental-fate
#20
Guofei Dai, Ningyan Peng, Jiayou Zhong, Ping Yang, Binchun Zou, Hui Chen, Qian Lou, Yuanyuan Fang, Wei Zhang
Metals can react with microcystin (MC), which is released from cyanobacterial blooms through various mechanisms; these reactions may mitigate the environmental and health risks of MCs but may also cause harm to aquatic ecosystems and humans. Several studies were conducted, including laboratory tests, ecological simulations, and a field investigation of Poyang Lake. The laboratory studies showed that Fe(3+), Cu(2+), and Pb(2+) stimulated MC photodegradation under high light intensity at the water-sediment interface, which reduced the MC accumulation in the sediment...
April 18, 2017: Environmental Pollution
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