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https://www.readbyqxmd.com/read/29783197/quantification-of-21-antihypertensive-drugs-in-serum-using-uhplc-ms-ms
#1
Per Ole M Gundersen, Arne Helland, Olav Spigset, Solfrid Hegstad
BACKGROUND: Poor drug adherence in hypertensive patients can lead to treatment failure and increased cardiovascular morbidity, as well as increased costs to society. An analytical method based on ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MSMS) was developed and validated for use in routine therapeutic drug monitoring (TDM). The method includes 21 antihypertensive drugs or active metabolites from the groups beta blockers (n=5), calcium antagonists (n=5), angiotensin II receptor antagonists (n=4), angiotensin converting enzyme (ACE) inhibitors (n=3) and diuretics (n = 3), in addition to one α1-selective alpha blocker...
April 28, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29783186/-1-h-nmr-and-uplc-ms-metabolomics-functional-tools-for-exploring-chemotypic-variation-in-sceletium-tortuosum-from-two-provinces-in-south-africa
#2
Jianping Zhao, Ikhlas A Khan, Sandra Combrinck, Maxleene Sandasi, Weiyang Chen, Alvaro M Viljoen
Sceletium tortuosum (Aizoaceae) is widely recognised for the treatment of stress, anxiety and depression, as well as for obsessive compulsive disorders. A comprehensive intraspecies chemotypic variation study, using samples harvested from two distinct regions of South Africa, was done using both proton nuclear magnetic resonance (1 H-NMR) spectroscopy of methanol extracts (N = 145) and ultra performance liquid chromatography-mass spectrometry (UPLC-MS) of acid/base extracts (N = 289). Chemometric analysis of the 1 H-NMR data indicated two main clusters that were region-specific (Northern Cape and Western Cape provinces)...
May 17, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29783185/impact-of-body-mass-index-on-the-efficacy-of-endocrine-therapy-in-patients-with-metastatic-breast-cancer-a-retrospective-two-center-cohort-study
#3
Luwam Zewenghiel, Henrik Lindman, Antonis Valachis
BAKGROUND: The aim of this study was to investigate the impact of body mass index (BMI) on the efficacy of endocrine therapy in postmenopausal women with metastatic hormone receptor breast cancer (HR+BC) as well as to identify if the potential difference in efficacy was associated with Fulvestrant only or both aromatase inhibitors (AIs) and Fulvestrant. METHODS: A consecutive cohort of postmenopausal women with HR+metastatic breast cancer that have received endocrine therapy including Fulvestrant as a metastatic treatment strategy at the Departments of Oncology in Eskilstuna and Uppsala, Sweden, between 2008 and 2016 were identified...
May 18, 2018: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/29783106/prediction-of-the-combined-effects-of-multiple-estrogenic-chemicals-on-mcf-7-human-breast-cancer-cells-and-a-preliminary-molecular-exploration-of-the-estrogenic-proliferative-effects-and-related-gene-expression
#4
Shengwu Yuan, Chao Huang, Xiaoya Ji, Mei Ma, Kaifeng Rao, Zijian Wang
The environmental risks of environmental estrogens (EEs) are often assessed via the same mode of action in the concentration addition (CA) model, neglecting the complex combined mechanisms at the genetic level. In this study, the cell proliferation effects of estrone, 17α-ethinylestradiol, 17β-estradiol, estriol, diethylstilbestrol, estradiol valerate, bisphenol A, 4-tert-octylphenol and 4-nonylphenol were determined individually using the CCK-8 method, and the proliferation effects of a multicomponent mixture of estrogenic chemicals mixed at equipotent concentrations using a fixed-ratio design were studied using estrogen-sensitive MCF-7 cells...
May 18, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29783074/fsh-receptor-binding-inhibitor-restrains-follicular-development-and-possibly-attenuates-carcinogenesis-of-ovarian-cancer-through-down-regulating-expression-levels-of-fshr-and-er%C3%AE-in-normal-ovarian-tissues
#5
Gong Zhuandi, Che Tuanjie, Lai Luju, Ayimuguli Abdiryim, Deng Yingying, Liang Haoqin, Wei Suocheng, Ding Li
OBJECTIVES: The current study aimed to investigate FSH receptor binding inhibitor (FRBI) effects in the expressions of FSH receptor (FSHR) and estrogen receptor-beta (ERβ) in the mice ovaries at the gene and protein levels, also to find the potential efficacy of FRBI on suppressing ovarian cancer through down-regulating over-expression of FSHR and ERβ in the normal ovarian tissues. METHODS: 180 female mice were randomized into six groups (n = 30). Mice of FRBI-1, FRBI-2 and FRBI-3, FRBI-4 were intramuscularly injected with FRBI of 10, 20, 30 and 40 mg/kg, respectively, for five consecutive days...
May 18, 2018: Gene
https://www.readbyqxmd.com/read/29783073/methylation-analysis-of-cmtm3-and-dusp1-gene-promoters-in-high-quality-brush-hair-in-the-yangtze-river-delta-white-goat
#6
Wang Qiang, Haiyan Guo, Yongjun Li, Jianfei Shi, Xiuyuan Yin, Jingwen Qu
The Yangtze River delta white goat is the only goat breed that produces high-quality brush hair, which is specifically used in top-grade writing brushes. Previous studies have indicated that the CMTM3 and DUSP1 genes are involved in the growth and cycle of high-quality brush hair, and these genes are thought to be involved in the formation of high-quality brush hair traits. In this study, we investigated the relationship between methylation of CMTM3 and DUSP1 and such traits. The results indicated that the relative expression levels of the CMTM3 and DUSP1 genes were higher in non-high-quality brush hair than in high-quality brush hair...
May 18, 2018: Gene
https://www.readbyqxmd.com/read/29783035/estrogen-receptor-progesterone-receptor-cd8-expression-in-endometrium-of-women-of-unexplained-infertility
#7
Shilpi Gupta Dixit, Surajit Ghatak, Pratibha Singh, Shilajit Bhattacharya
OBJECTIVE: The present study aimed to investigate the changes of endometrial progesterone and estrogen receptors in luteal phase biopsy specimens of infertile women and find a correlation, if any, between these and CD8+ receptors in the same. METHODS: The study was conducted on luteal phase endometrial biopsy specimens of 30 women of Unexplained Infertility and 15 age matched controls. Paraffin sections were first H & E stained. A standardized immunohistochemical protocol was then used to localize the estrogen, progesterone and CD8+ receptors in these samples that were expressed as percentage positivity...
May 18, 2018: Journal of Gynecology Obstetrics and Human Reproduction
https://www.readbyqxmd.com/read/29782975/roles-of-germline-jak2-activation-mutation-jak2-v625f-in-the-pathology-of-myeloproliferative-neoplasms
#8
Qing-Yun Wu, Meng-Meng Ma, Lin Fu, Yuan-Yuan Zhu, Yang Liu, Jiang Cao, Ping Zhou, Zhen-Yu Li, Ling-Yu Zeng, Feng Li, Xiao-Yun Wang, Kai-Lin Xu
Janus tyrosine kinase 2 (JAK2) mediates downstream signaling of cytokine receptors in all hematological lineages, constitutively active somatic JAK2 mutations play key roles in the pathology of myeloproliferative neoplasms (MPNs). Recently, germline JAK2 mutations are also associated with triple-negative MPNs. A novel germline mutation JAK2 V625F is reported to be involved in a subset of MPNs patients. However, the pathogenesis of this mutation caused MPN is still unclear. In this study, the homology models of JAK2 V625F showed that the newly formed interaction between F625 and Y613 disrupted the JAK2 JH1-JH2 domain interactions was responsible for its activation, when F625 and Y613 interaction was disrupted, its activity significantly decreased...
May 18, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29782964/an-in-vitro-approach-for-prioritization-and-evaluation-of-chemical-effects-on-glucocorticoid-receptor-mediated-adipogenesis
#9
Jessica K Hartman, Tyler Beames, Bethany Parks, Daniel Doheny, Gina Song, Alina Efremenko, Miyoung Yoon, Briana Foley, Chad Deisenroth, Patrick D McMullen, Rebecca A Clewell
Rising obesity rates worldwide have socio-economic ramifications. While genetics, diet, and lack of exercise are major contributors to obesity, environmental factors may enhance susceptibility through disruption of hormone homeostasis and metabolic processes. The obesogen hypothesis contends that chemical exposure early in development may enhance adipocyte differentiation, thereby increasing the number of adipocytes and predisposing for obesity and metabolic disease. We previously developed a primary human adipose stem cell (hASC) assay to evaluate the effect of environmental chemicals on PPARG-dependent adipogenesis...
May 18, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29782961/baclofen-induced-encephalopathy-in-overdose-modeling-of-the-electroencephalographic-effect-concentration-relationships-and-contribution-of-tolerance-in-the-rat
#10
Magali Chartier, Isabelle Malissin, Salma Tannous, Laurence Labat, Patricia Risède, Bruno Mégarbane, Lucie Chevillard
Baclofen, a γ-amino-butyric acid type-B receptor agonist with exponentially increased use at high-dose to facilitate abstinence in chronic alcoholics, is responsible for increasing poisonings. Baclofen overdose may induce severe encephalopathy and electroencephalographic (EEG) abnormalities. Whether prior prolonged baclofen treatment may influence the severity of baclofen-induced encephalopathy in overdose has not been established. We designed a rat study to characterize baclofen-induced encephalopathy, correlate its severity with plasma concentrations and investigate the contribution of tolerance...
May 18, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29782959/targeting-central-%C3%AE-2-receptors-ameliorates-streptozotocin-induced-neuroinflammation-via-inhibition-of-glycogen-synthase-kinase3-pathway-in-mice
#11
Nora O Abdel Rasheed, Nesrine S El-Sayed, Aiman S El-Khatib
Alzheimer's disease (AD) is portrayed by progressive cognitive decline and pathological deposition of amyloid plaques as well as neurofibrillary tangles. Most of AD cases are sporadic, resulting from overlap of various environmental and genetic factors. Intra-cerebroventricular injection of streptozotocin (STZ) leads to insulin resistance brain state accompanied by memory decline, oxidative stress, and neuro-degeneration which mimic the pathologies associated with sporadic Alzheimer's disease (SAD). In the current study, protective effects of formoterol in STZ-induced SAD were studied...
May 18, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29782941/dopamine-and-serotonin-metabolism-associated-with-morphine-reward-and-its-inhibition-with-buspirone-a-study-in-the-rat-striatum
#12
Darakhshan Jabeen Haleem, Shazia Nawaz, Tabinda Salman
Adaptations within the nucleus accumbens (NAc) and caudate nucleus (CN) dopamine neurotransmission are involved in behavioral sensitization and enhanced incentive motivation towards drug paired stimuli which lead to drug addiction. Serotonin (5-hydroxytryptamine; 5-HT) can modulate dopamine neurotransmission to reduce rewarding effects of drugs of abuse. A recent study from our laboratory shows that rewarding effects of morphine are inhibited in rats co-treated with buspirone. To understand the neurochemical mechanism involved in morphine addiction and its inhibition with buspirone, present study determines the effects of buspirone, morphine and their co-administration on the metabolism of serotonin and dopamine in the NAc and CN...
May 18, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29782904/intracellular-s1p-levels-dictates-fate-of-different-regions-of-the-hippocampus-following-transient-global-cerebral-ischemia
#13
Sherif Rashad, Kuniyasu Niizuma, Daisuke Saigusa, Xiaobo Han, Mika Sato-Maeda, Ritsumi Saito, Akira Uruno, Miki Fujimura, Shuntaro Ikawa, Masayuki Yamamoto, Teiji Tominaga
Sphingosine-1-phosphate (S1P) is a sphingolipid molecule produced by the action of sphingosine kinases (SphK) on sphingosine. It possesses various intracellular functions through its interactions with intracellular proteins or via its action on five G-protein-coupled cell membrane receptors. Following transient global cerebral ischaemia (tGCI), only the CA1 subregion of the hippocampus undergoes apoptosis. In this study, we evaluated S1P levels and S1P processing enzyme expression in different hippocampal areas following tGCI in rats...
May 18, 2018: Neuroscience
https://www.readbyqxmd.com/read/29782892/a-glp-1-cck-fusion-peptide-harnesses-the-synergistic-effects-on-metabolism-of-cck-1-and-glp-1-receptor-agonism-in-mice
#14
David C Hornigold, Emma Roth, Victor Howard, Sarah Will, Stephanie Oldham, Matthew P Coghlan, Clemence Blouet, James L Trevaskis
Combination approaches for the treatment of metabolic diseases such as obesity and diabetes are becoming increasingly relevant. Co-administration of a glucagon-like peptide-1 receptor (GLP-1R) agonist with a cholecystokinin receptor-1 (CCKR1) agonist exert synergistic effects on weight loss in obese rodents. Here, we report on the effects of a novel fusion peptide (C2816) comprised of a stabilized GLP-1R agonist, AC3174, and a CCKR1-selective agonist, AC170222. C2816 was constructed such that AC3174 was linked to the N-terminus of AC170222, thus preserving the C-terminal amide of the CCK moiety...
May 18, 2018: Appetite
https://www.readbyqxmd.com/read/29782883/a-new-outlook-on-cholinergic-interneurons-in-parkinson-s-disease-and-l-dopa-induced-dyskinesia
#15
REVIEW
Melissa M Conti, Nicole Chambers, Christopher Bishop
Traditionally, dopamine (DA) and acetylcholine (ACh) striatal systems were considered antagonistic and imbalances or aberrant signaling between these neurotransmitter systems could be detrimental to basal ganglia activity and pursuant motor function, such as in Parkinson's disease (PD) and L-DOPA-induced dyskinesia (LID). Herein, we discuss the involvement of cholinergic interneurons (ChIs) in striatally-mediated movement in a healthy, parkinsonian, and dyskinetic state. ChIs integrate numerous neurotransmitter signals using intrinsic glutamate, serotonin, and DA receptors and convey the appropriate transmission onto nearby muscarinic and nicotinic ACh receptors to produce movement...
May 18, 2018: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29782864/are-dopamine-receptor-and-transporter-changes-in-rett-syndrome-reflected-in-mecp2-deficient-mice
#16
Dean F Wong, Mary E Blue, James R Brašić, Ayon Nandi, Heather Valentine, Kirstie H Stansfield, Olivier Rousset, Genila Bibat, Mary E Yablonski, Michael V Johnston, Albert Gjedde, SakkuBai Naidu
In the present study we tested the claim that the dopaminergic dysfunction of Rett Syndrome (RTT) also occurs in Mecp2-deficient mice that serve as a model of the syndrome. We used positron emission tomography (PET) to image dopamine D2 receptors (D2 R) and transporters (DAT) in women with RTT and in Mecp2-deficient mice, and D1 R and D2 R density was measured in postmortem human tissue by autoradiography. Results showed 1) significantly reduced D2 R density in the striatum of women with RTT compared to control subjects...
May 18, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29782863/analysis-of-mulberry-leaf-components-in-the-treatment-of-diabetes-using-network-pharmacology
#17
Qi Ge, Liang Chen, Min Tang, Shu Zhang, Lu Gao, Shangshang Ma, Lanlan Liu, Ming Kong, Qin Yao, Keping Chen, Fan Feng
Mulberry leaves are one of the most commonly used medicinal and herbaceous traditional Chinese medicines that are currently considered for the treatment of diabetes mellitus and its complications. The alkaloids, flavonoids, and polysaccharides in mulberry leaves impart regulatory effects on blood sugar levels. To identify the hypoglycemia-related active components in mulberry leaves and their targets, the present study conducted gas chromatography-mass spectrometer (GC/MS), which identified 202 components of mulberry leaf, of which 22 components may have significant curative effects on diabetes mellitus and its complications and chronic inflammation...
May 18, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29782857/quaternary-ammonium-salt-of-u50-488h-elicits-protective-effects-against-hypoxic-pulmonary-hypertension
#18
Yaguang Zhou, Xin Tian, Xueying Wang, Yuanbo Wang, Rong Fan, Yuemin Wang, Na Feng, Shumiao Zhang, Haitao Guo, Xiaoming Gu, Min Jia, Wen Yin, Zuoxu Hou, Juan Li, Jianming Pei
The present study aimed to investigate the role of quaternary ammonium salt of U50,488H (Q-U50,488H) in hypoxic pulmonary hypertension (HPH) and underlying mechanisms involved. A HPH animal model was established in rats under hypoxia and the mean pulmonary arterial pressure (mPAP) and right ventricular pressure (RVP) were measured. Relaxation of the pulmonary artery in response to Q-U50,488H was determined. In addition, expression and activity of endothelial nitric oxide (NO) synthase (eNOS) and inducible NO synthase (iNOS) with NO content, Akt expression, total antioxidant capacity (T-AOC), and gp91phox were evaluated...
May 18, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29782852/atp6v1h-regulates-the-growth-and-differentiation-of-bone-marrow-stromal-cells
#19
Lin Li, Shaoqing Yang, Yanli Zhang, Dongrui Ji, Zuolin Jin, Xiaohong Duan
ATP6V1H encodes subunit H of vacuolar ATPase (V-ATPase) and may regulate osteoclastic function. The deficiency of ATP6V1H caused bone loss in human, mouse and zebrafish. In this report, we identified the mechanisms by which ATP6V1H regulates proliferation and differentiation of bone marrow stromal cells (BMSCs). We found that ATP6V1H was expressed in BMSCs, andAtp6v1h+/- BMSCs exhibited the lower proliferation rate, cell cycle arrest and reduced osteogenic differentiation capacity, as well as the increased adipogenic potentials...
May 18, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29782851/glycosylation-of-cblns-attenuates-their-receptor-binding
#20
Yongqi Rong, Parmil K Bansal, Peng Wei, Hong Guo, Kristen Correia, Jennifer Parris, James I Morgan
Cbln1 is the prototype of a family (Cbln1-Cbln4) of secreted glycoproteins and is essential for normal synapse structure and function in cerebellum by bridging presynaptic Nrxn to postsynaptic Grid2. Here we report the effects of glycosylation on the in vitro receptor binding properties of Cblns. Cbln1, 2 and 4 harbor two N-linked glycosylation sites, one at the N-terminus is in a region implicated in Nrxn binding and the second is in the C1q domain, a region involved in Grid2 binding. Mutation (asparagine to glutamine) of the N-terminal site, increased neurexin binding whereas mutation of the C1q site markedly increased Grid2 binding...
May 18, 2018: Brain Research
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