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https://www.readbyqxmd.com/read/29332257/kynurenic-acid-and-its-derivatives-are-able-to-modulate-the-adhesion-and-locomotion-of-brain-endothelial-cells
#1
Eszter Lajkó, Bernadett Tuka, Ferenc Fülöp, István Krizbai, József Toldi, Kálmán Magyar, László Vécsei, László Kőhidai
The neuroprotective actions of kynurenic acid (KYNA) and its derivatives in several neurodegenerative disorders [characterized by damage to the cerebral endothelium and to the blood-brain barrier (BBB)] are well established. Cell-extracellular matrix (ECM) adhesion is supposedly involved in recovery of impaired cerebral endothelium integrity (endothelial repair). The present work aimed to investigate the effects of KYNA and its synthetic derivatives on cellular behaviour (e.g. adhesion and locomotion) and on morphology of the GP8 rat brain endothelial cell line, modeling the BBB endothelium...
January 13, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29332251/clinical-pharmacokinetics-and-pharmacodynamics-of-telavancin-compared-with-the-other-glycopeptides
#2
REVIEW
Valentin Al Jalali, Markus Zeitlinger
Telavancin was discovered by modifying the chemical structure of vancomycin and belongs to the group of lipoglycopeptides. It employs its antimicrobial potential through two distinct mechanisms of action: inhibition of bacterial cell wall synthesis and induction of bacterial membrane depolarization and permeabilization. In this article we review the clinically relevant pharmacokinetic and pharmacodynamic data of telavancin. For comparison, the pharmacokinetic and pharmacodynamic data of the other glycopeptides are presented...
January 13, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29332193/melanogenesis-inhibitory-activity-of-components-from-salam-leaf-syzygium-polyanthum-extract
#3
Andriyana Setyawati, Kae Hirabayashi, Kosei Yamauchi, Hiroyuki Hattori, Tohru Mitsunaga, Irmanida Batubara, Rudi Heryanto, Hiroshi Hashimoto, Mitsuyuki Hotta
In order to identify a novel whitening agent, the methanol extract of S. polyanthum leaf was focused on by the screening test using nine Indonesian medicinal plants for the inhibition of melanogenesis and tyrosinase activity in B16 melanoma cells. Three novel compounds [(1) 1-(2,3,5-trihydroxy-4-methylphenyl)hexane-1-one, (2) 1-(2,3,5-trihydroxy methylphenyl)octane-1-one, and (3) (4E)-1-(2,3,5-trihydroxy-4-methylphenyl)decan-1-one and one known compound [(4) 1-(2,3,5-trihydroxy-4-methylphenyl)decan-1-one were isolated from the methanol extract...
January 13, 2018: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29332183/identification-of-n-arylsulfonylpyrimidones-as-anticancer-agents
#4
Santhosh Subramanian, Pulla Reddy Boggu, Jieun Yun, Sang-Hun Jung
For confirming the role of five membered ring of imidazolidinone moiety of N-arylsulfonylimidazolidinones (7) previously reported with highly potent anticancer agent, a series of N-arylsulfonylpyrimidones (10a-g) and N-arylsulfonyltetrahydropyrimidones (11a-e) were prepared and their anti-proliferating activity was measured against human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostate PC-3) using XTT assay. Among them, 1-(1-acetylindolin-5-ylsulfonyl)-4-phenyltetrahydropyrimidin-2(1H)-one (11d, mean GI50 = 3...
January 13, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29332143/conjunction-of-g-quadruplex-and-stem-loop-in-the-5-untranslated-region-of-mouse-hepatocyte-nuclear-factor-4-alpha1-mediates-strong-inhibition-of-protein-expression
#5
Shangdong Guo, Hong Lu
Hepatocyte nuclear factor 4-alpha (HNF4α) is a well-established master regulator of liver development and function. Restoration of HNF4α can treat multiple liver disorders and liver cancers. To date, HNF4α is still "undruggable" due to lack of known activating ligands. Thus, understanding the regulatory mechanism of HNF4α expression may help develop an alternative approach to modulate HNF4α protein levels. G-quadruplexes (G4) are non-canonical stable secondary structures discovered mostly in the promoters of oncogenes...
January 13, 2018: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29332105/the-emergence-of-carbapenem-resistant-klebsiella-pneumoniae-isolates-producing-oxa-48-and-ndm-in-the-southern-asir-province-saudi-arabia
#6
Ibrahim A Al-Zahrani, Bander A Alsiri
To identify the prevalence of carbapenem-resistant Klebsiella pneumoniae (CRKP) and the most common types of cabapenemases among CRKP in the Southern (Asir) province hospitals, Saudi Arabia. Methods: The cross-sectional study was conducted between late April and September in 2015. A total of 54 Klebsiella pneumoniae (K. pneumoniae) isolates with reduced sensitivity to carbapenems were obtained from various clinical specimens of the 2 largest hospitals in the Southern province. Minimum inhibitory concentrations (MICs) of carbapenems were confirmed using E-test...
January 2018: Saudi Medical Journal
https://www.readbyqxmd.com/read/29331916/aerobic-exercise-is-more-effective-than-goal-based-exercise-for-the-treatment-of-cognition-in-parkinson-s-disease
#7
Carolina R A Silveira, Eric A Roy, Brittany N Intzandt, Quincy J Almeida
BACKGROUND: Little is known about how different exercise modalities influence cognition in Parkinson's disease (PD). Moreover, the focus of previous investigations on examining the effects of exercise mainly on executive functions and the exclusion of individuals with cognitive impairment may limit the potential to define exercise as a treatment for cognitive decline in PD. OBJECTIVE: The aim of this study was to compare the effects of aerobic and goal-based exercise on five cognitive domains in cognitively normal and impaired individuals with PD...
January 10, 2018: Brain and Cognition
https://www.readbyqxmd.com/read/29331903/rapid-structure-prediction-by-hplc-esi-msn-of-twenty-five-polyoxypregnane-tetraglycosides-from-dregea-sinensis-with-nmr-confirmation-of-eight-structures
#8
Juan Song, Rongji Dai, Yulin Deng, Fang Lv
Dregea sinensis Hemsl is an important herbal medicine in the Dai nationality of China. Its prominent clinical application has generated interest in the polyoxypregnane glycosides of the plant. This paper describes an extension of previous research on the polyoxypregnane di- and triglycosides of D. sinensis, aiming at identifying related tetraglycosides. On the basis of HPLC-ESI-MSn analysis in positive mode, twenty-five previously undescribed polyoxypregnane tetraglycosides were characterized (regarding molecular masses and fragmentation in MSn) from an ethyl acetate fraction that was not previously investigated...
January 11, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29331846/functional-neuroimaging-in-rasmussen-syndrome
#9
Ichiro Kuki, Kazumi Matsuda, Yuko Kubota, Tetsuhiro Fukuyama, Yukitoshi Takahashi, Yushi Inoue, Haruo Shintaku
PURPOSE: For a diagnosis of Rasmussen syndrome (RS), clinical course together with electroencephalography (EEG) and magnetic resonance imaging (MRI) findings are considered important, but there are few reports on functional neuroimaging. This study investigated cerebral blood flow (CBF)-single photon emission computed tomography (SPECT), central benzodiazepine receptor (BZR)-SPECT, and fluorine-18 fluorodeoxy glucose-positron emission tomography (FDG-PET) in RS patients, and correlated neuroimaging results with MRI and pathological findings...
January 5, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29331845/effect-of-levetiracetam-on-extracellular-amino-acid-levels-in-the-dorsal-hippocampus-of-rats-with-temporal-lobe-epilepsy
#10
Pichardo Macías Luz Adriana, Ramírez Mendiola Blanca Alcira, Contreras García Itzel Jatziri, Zamudio Hernández Sergio Roberto, Chávez Pacheco Juan Luis, Sánchez Huerta Karla Berenice, Mendoza Torreblanca Julieta Griselda
Levetiracetam (LEV) is an anticonvulsant drug with a unique mechanism of action that is not completely understood. However, its activity profile may involve effects on excitatory and/or inhibitory neurotransmission since the primary target of LEV, synaptic vesicle protein 2A, is ubiquitously expressed in all types of synaptic vesicles. Therefore, the objective of the present study was to explore the effect of LEV (300 mg/kg/day for one week, administered via osmotic mini-pumps) on neurotransmitter release and its probable selective effect on extracellular gamma-amino butyric acid (GABA), glutamate (Glu), aspartate (Asp), glutamine (Gln), taurine (Tau) and glycine (Gly) concentrations (using in vivo microdialysis under basal and high-K+ conditions) in the dorsal hippocampus (DH), a region that undergoes major synaptic changes during epilepsy...
January 5, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29331805/synthesis-characterization-and-anticancer-activity-in%C3%A2-vitro-and-in%C3%A2-vivo-evaluation-of-an-iridium-iii-polypyridyl-complex
#11
Qiao-Yan Yi, Dan Wan, Bing Tang, Yang-Jie Wang, Wen-Yao Zhang, Fan Du, Miao He, Yun-Jun Liu
An iridium (III) complex [Ir(ppy)2(BDPIP)]PF6 (Ir-1) was reported to show high anticancer activity and may be used as a potent anticancer drug. In the current study, we designed and synthesized a novel iridium (III) complex and evaluated its potential inhibitory effect on the cancer cell growth in vitro and in vivo. This complex was found to display high cytotoxic activity in vitro and in vivo against A549 cell with a low IC50 value of 3.6 ± 0.3 μM and inhibiting percentage of tumor growth is 63.84% compared with the control...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29331765/5-6-dihydropyrimidine-1-2h-carbothioamides-synthesis-in-vitro-gaba-at-screening-anticonvulsant-activity-and-molecular-modelling-study
#12
Meeta Sahu, Nadeem Siddiqui, Vidushi Sharma, Sharad Wakode
Even after considerable advances in the field of epilepsy treatment, convulsions are inefficiently controlled by standard drug therapy. Herein, a series of pyrimidine-carbothioamide derivatives 4(a-t) was designed as anticonvulsant agents by doing some important structural modifications in well-known anticonvulsant drugs. Two classical animal models were used for the in vivo anticonvulsant screening, maximum electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) models; followed by motor impairment study by rotarod method...
January 2, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29331764/synthesis-small-library-of-hybrid-scaffolds-of-benzothiazole-having-hydrazone-and-evaluation-of-their-%C3%AE-glucuronidase-activity
#13
Muhammad Taha, Mastura Arbin, Norizan Ahmat, Syahrul Imran, Fazal Rahim
Due to the great biological importance of β-glucuronidase inhibitors, here in this study, we have synthesized a library of novel benzothiazole derivatives (1-30), characterized by different spectroscopic methods and evaluated for β-glucuronidase inhibitory potential. Among the series sixteen compounds i.e.1-6, 8, 9, 11, 14, 15, 20-23 and 26 showed outstanding inhibitory potential with IC50 value ranging in between 16.50 ± 0.26 and 59.45 ± 1.12 when compared with standard d-Saccharic acid 1,4-lactone (48...
January 4, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29331763/inhibition-of-isoprenylcysteine-carboxylmethyltransferase-sensitizes-common-chemotherapies-in-cervical-cancer-via-ras-dependent-pathway
#14
Qin Pan, Rong Liu, Hasina Banu, Liang Ma, Hui Li
Isoprenylcysteine carboxylmethyltransferase (Icmt) catalyzes the last step of post-translational protein prenylation, which is essential for the stability and proper functions of many oncogenic proteins, such as Ras. Despite extensive studies on the roles of Icmt in tumor transformation and progression, little is known on the involvement ofIcmt in the development of tumor resistance to chemotherapy. Here we show the upregulation of Icmt as a persistent response to chemotherapy in cervical cancer cells. In-depth functional analysis demonstrated that Icmt inhibition significantly inhibited growth, induced apoptosis and augmented the inhibitory effects of chemotherapy drugs in cervical cancer in cell culture system and xenograft mouse model...
January 10, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29331727/individual-variation-in-working-memory-is-associated-with-fear-extinction-performance
#15
Daniel M Stout, Dean T Acheson, Tyler M Moore, Ruben C Gur, Dewleen G Baker, Mark A Geyer, Victoria B Risbrough
PTSD has been associated consistently with abnormalities in fear acquisition and extinction learning and retention. Fear acquisition refers to learning to discriminate between threat and safety cues. Extinction learning reflects the formation of a new inhibitory-memory that competes with a previously learned threat-related memory. Adjudicating the competition between threat memory and the new inhibitory memory during extinction may rely, in part, on cognitive processes such as working memory (WM). Despite significant shared neural circuits and signaling pathways the relationship between WM, fear acquisition, and extinction is poorly understood...
January 5, 2018: Behaviour Research and Therapy
https://www.readbyqxmd.com/read/29331723/progesterone-arrested-cell-cycle-progression-through-progesterone-receptor-isoform-a-in-pancreatic-neuroendocrine-neoplasm
#16
Samaneh Yazdani, Atsuko Kasajima, Yoshiaki Onodera, Keely May McNamara, Kazue Ise, Yasuhiro Nakamura, Tomoyoshi Tachibana, Fuyuhiko Motoi, Michiaki Unno, Hironobu Sasano
In pancreatic neuroendocrine neoplasms (Pan-NEN) progesterone signaling has been shown to have both inhibitory and stimulatory effects on cell proliferation. The ability of progesterone to inhibit tumor proliferation is of particular interest and is suggested to be mediated through the less abundantly expressed progesterone receptor (PR) isoform A (PRA). To date the mechanistic processes underlying this inhibition of proliferation remain unclear. To examine the mechanism of PRA actions, the human Pan-NEN cell line QGP-1, that endogenously expresses PR isoform B (PRB) without PRA, was transfected with PRA...
January 10, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29331700/effects-of-macrophage-migration-inhibitory-factor-on-cardiac-reperfusion-injury-in-mice-with-depression-induced-by-constant-darkness
#17
Lu-Yuan Tao, Ming-Yuan Huang, Saroj-Thapa, Jiao-Ni Wang, Shao-Ze Wu, Fei He, Kai-Yu Huang, Yang-Jing Xue, Lingwei-Jin, Lian-Ming Liao, Ji-Fei Tang, Kang-Ting Ji
RATIONALE: Depression is associated with coronary artery disease and increases adverse outcomes and mortality in patients with acute myocardial infarction, but the underlying pathophysiological mechanisms remain unclear. OBJECTIVE: To evaluate the effect of macrophage migration inhibitory factor (MIF) on cardiac ischemia-reperfusion (I/R) injury in mice with constant darkness-induced depression. METHODS AND RESULTS: Twenty C57BL/6 mice (8 weeks old, male) were randomly divided into 2 groups: one group was housed in a 12h light/dark cycle environment (LD) and the other in a constant darkness environment (DD)...
December 27, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29331690/effect-of-depressive-symptoms-on-the-evolution-of-neuropsychological-functions-over-the-course-of-adolescence
#18
Mohammad H Afzali, Maeve Oleary-Barrett, Jean R Séguin, Patricia Conrod
INTRODUCTION: Comprehensive understanding of the association between depression and neuropsychological functioning over the course of adolescence requires developmentally sensitive assessment through longitudinal data. The aim of current study is to examine the concurrent and subsequent effects of depressive symptoms on the initial level and evolution of four neuropsychological functioning domains (i.e., spatial working memory, delayed recall memory, perceptual reasoning, and inhibitory control)...
December 22, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29331653/gallic-acid-attenuates-type-i-diabetic-nephropathy-in-rats
#19
Mayuresh Sudamrao Garud, Yogesh Anant Kulkarni
Literatures suggest that TGF-β1 have a central role in the progression of diabetic nephropathy and its down regulation can improve the disease condition. Oxidative stress, generation of advanced glycation end products and activation of renin angiotensin system are the connecting links between hyperglycemia and TGF-β1 over expression. Gallic acid is a phytochemical having wide range of biological activities. Gallic acid is reported to have antioxidant and advanced glycation inhibitory activity. It has also shown inhibitory effects on angiotensin converting enzyme...
January 10, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29331636/cell-wall-damage-and-oxidative-stress-in-candida-albicans-atcc10231-and-aspergillus-niger-caused-by-palladium-nanoparticles
#20
Martha Samira Athie-García, Hilda Amelia Piñón-Castillo, Laila Nayzzel Muñoz-Castellanos, Ana Laura Ulloa-Ogaz, Perla Ivonne Martínez-Varela, Armando Quintero-Ramos, Robert Duran, José Guadalupe Murillo-Ramirez, Erasmo Orrantia-Borunda
In this work the toxic effect of Palladium nanoparticles (PdNPs) was investigated in two eukaryotic cell models, Candida albicans and Aspergillus niger. PdNPs were synthesized by chemical reduction method, obtaining spherical NPs with a primary size ranging from 3 to 15 nm. PdNPs showed a hydrodynamic size of 1548 nm in Lee's minimum media. Minimal inhibitory concentration was determined at 200 and 250 ppm for Candida albicans and Aspergillus niger respectively, revealing a significant cell growth inhibition (ANOVA and tukey analysis, α = 0...
January 10, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
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