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Jin Wu, Todd Vogel, Xiang Gao, Bin Lin, Charles Kulwin, Jinhui Chen
No FDA approved pharmacological therapy is available that would reduce cell death following traumatic brain injury (TBI). Dexmedetomidine (Dex) is a highly selective agonist of alpha-2 adrenergic receptors and has demonstrated neuroprotective effects in hippocampal slice cultures undergoing direct impact. However, no one has tested whether Dex, in addition to its sedative action, has neuroprotective effects in an animal model of TBI. Thus, in the present study, we investigated the effects of Dex on an animal model of TBI...
March 21, 2018: Scientific Reports
Nageswara Rao Rayala, Rajkumar Kommera, Dayakar Cherupally, Ramalinga Murthy Thampunuri, V Kalivendi Shasi, China Raju Bhimapaka
Series of 4H-chromone-based hydrazones 3a-z, pyrazolecarboxylates 5a-x and pyrazolylmethanones 6a-u were prepared and screened for their anti-proliferative activity on A549, HeLa, DU145 and MDAMB 231 cell lines. The hydrazone compound 3s with a chloro substituent on the chromanone moiety and a methoxy group on the phenyl ring displayed promising activity on A549, HeLa and DU145 cell lines. The compound 5p with a bromo substituent on the chromanone moiety and a methyl group on the phenyl ring displayed potent activity on DU145...
March 2018: Acta Chimica Slovenica
Adrien Lebasnier, Damien Legallois, Boris Bienvenu, Emmanuel Bergot, Cédric Desmonts, Gérard Zalcman, Denis Agostini, Alain Manrique
OBJECTIVE: The identification of cardiac sarcoidosis is challenging as there is no gold standard consensually admitted for its diagnosis. The aim of this study was to evaluate the diagnostic value of the assessment of cardiac dynamic18 F-fluoro-2-deoxyglucose positron emission tomography (18 F-FDG PET/CT) and net influx constant (Ki) in patients suspected of cardiac sarcoidosis. METHODS: Data obtained from 30 biopsy-proven sarcoidosis patients suspected of cardiac sarcoidosis who underwent a 50-min list-mode cardiac dynamic18 F-FDG PET/CT after a 24 h high-fat and low-carbohydrate diet were analyzed...
March 20, 2018: Annals of Nuclear Medicine
Kazuhiro J Fujimoto, Daiki Nema, Masayuki Ninomiya, Mamoru Koketsu, Hidetaka Sadanari, Masaya Takemoto, Tohru Daikoku, Tsugiya Murayama
A novel type of antiviral agent for human cytomegalovirus (HCMV) is required, because the appearance of ganciclovir (GCV) resistant viruses has been reported. Tricin (4',5,7-trihydroxy-3',5'-dimethoxyflavone) has been shown to suppress significantly HCMV replication in human embryonic lung (HEL) fibroblast cells. Recently, we revealed that the action of tricin is different from that of GCV and cyclin-dependent kinase 9 (CDK9) is one of the target proteins of tricin. These results suggested that tricin is considered as a novel type of anti-HCMV agent...
March 17, 2018: Antiviral Research
Nadège Hamon, Malika Kaci, Jean-Pierre Uttaro, Christian Périgaud, Christophe Mathé
The synthesis and the antiviral evaluation of 3'-halo (iodo and fluoro) 5'-norcarbocyclic nucleoside phosphonates is described. No antiviral activity was observed against Zika virus, Dengue virus 2, HSV-1, HSV-2 and Chikungunya virus. In contrast, some of the synthesized compounds are potent inhibitors of the replication of HIV-1, comparatively to (R)-PMPA, with no concomitant cytotoxicity.
March 14, 2018: European Journal of Medicinal Chemistry
Aurélie Fossey-Jouenne, Carine Vergne-Vaxelaire, Anne Zaparucha
Amino alcohols are versatile compounds with a wide range of applications. For instance, they have been used as chiral scaffolds in organic synthesis. Their synthesis by conventional organic chemistry often requires tedious multi-step synthesis processes, with difficult control of the stereochemical outcome. We present a protocol to enzymatically synthetize amino alcohols starting from the readily available L-lysine in 48 h. This protocol combines two chemical reactions that are very difficult to conduct by conventional organic synthesis...
February 16, 2018: Journal of Visualized Experiments: JoVE
Abhilasha Siyag, Tej P Soni, Anil K Gupta, Lalit M Sharma, Naresh Jakhotia, Shantanu Sharma
Plasmacytoma of the skull-base is a rare entity. Differential diagnosis includes chordoma, osteosarcoma, carcinoma nasopharynx, meningioma, metastatic carcinoma, lymphoma, and multiple myeloma. Accurate and precise diagnosis is extremely important for plasmacytoma of the skull-base as its treatment and prognosis is different from other skull-base lesions. A 41-year-old man presented with concerns of headache, diplopia, and left eye strabismus. A magnetic resonance image (MRI) of his brain showed a large expansile mass measuring 51 mm involving the clivus and central skull-base...
January 15, 2018: Curēus
Sonia L Betancourt Cuellar, Diana Palacio, Marcelo F Benveniste, Brett W Carter, Gregory Gladish
Positron emission tomography (PET) computed tomography (CT) with 2-[fluorine-18] fluoro-2-deoxy-d-glucose (FDG) has been established as an effective modality for evaluation of cancer. Interpretations of patterns of physiologic18 F-FDG uptake by the heart is particularly difficult given the wide normal variations of18 F-FDG metabolic activity observed. Atypical patterns of focal or diffuse physiologic cardiac18 F-FDG uptake and post-therapeutic effects after radiation therapy, systemic diseases, or cardiomyopathy may also be confused with malignant disease on18 F-FDG PET/CT...
February 6, 2018: Current Problems in Diagnostic Radiology
Jinbo Yue, Qiuling Shi, Ting Xu, Melenda Jeter, Ting-Yu Chen, Ritsuko Komaki, Daniel R Gomez, Tinsu Pan, Charles S Cleeland, Zhongxing Liao, Xin Shelley Wang
PURPOSE: Clinician ratings of concurrent chemoradiation (CRT)-induced radiation pneumonitis (RP) in patients with non-small cell lung cancer (NSCLC) are based on both imaging and patient-reported lung symptoms. We compared the value of patient-reported outcomes versus normal-lung uptake of18 F-fluoro-2-deoxyglucose in positron emission computed tomography (FDG PET/CT) during the last week of treatment, for indicating the development of grade ≥ 2 RP within 4 months of CRT completion...
March 16, 2018: Quality of Life Research
Thomas F Gamage, Charlotte E Farquhar, Timothy W Lefever, Julie A Marusich, Richard C Kevin, Iain S McGregor, Jenny L Wiley, Brian F Thomas
Synthetic cannabinoids are a class of novel psychoactive substances that exhibit high affinity at the cannabinoid type-1 (CB1) receptor and produce effects similar to those of THC, the primary psychoactive constituent of cannabis. Illicit drug manufacturers are continually circumventing laws banning the sale of synthetic cannabinoids by synthesizing novel structures and doing so with little regard for their potential impact on pharmacological and toxicological effects. Synthetic cannabinoids produce a wide range of effects including cardiotoxicity, seizure activity, and kidney damage and can result in death...
March 16, 2018: Journal of Pharmacology and Experimental Therapeutics
Santosh R Alluri, Patrick J Riss
A variety of substituted non-racemic aziridine-2-carboxylates equivalent to amino acids were prepared and subjected to ring opening reaction by [18F/19F]fluoride. The regio and stereospecific ring opening depends on the substituents on the nitrogen as well as both the carbons of aziridines. The applicability of the methods to afford access to 3-[18F/19F]fluoro amino acids are illustrated.
March 16, 2018: Organic & Biomolecular Chemistry
Kamila Cagliari Zenki, Eduardo Kalinine, Eduardo R Zimmer, Thainá Garbino Dos Santos, Ben Hur Marins Mussulini, Luis Valmor Cruz Portela, Diogo Lösch de Oliveira
Several works have demonstrated that status epilepticus (SE) induced-neurodegeneration appears to involve an overactivation of N-methyl-D-aspartate receptors and treatment with high-affinity NMDAR antagonists is neuroprotective against this brain damage. However, these compounds display undesirable side effects for patients since they block physiological NMDA receptor dependent-activity. In this context, memantine (MN), a well tolerable low-affinity NMDAR channel blocker, will be a promising alternative, since it does not compromise the physiological role of NMDA receptors on synaptic transmission...
March 12, 2018: Neurotoxicology
Beatriz Bernardo-Maestro, Elisa Garrido-Martín, Fernando López-Arbeloa, Joaquín Pérez-Pariente, Luis Gómez-Hortigüela
In an attempt to promote the crystallization of chiral inorganic frameworks, we explore the ability of chiral (1R,2S)-ephedrine and its diastereoisomer (1S,2S)-pseudoephedrine to act as organic building blocks for the crystallization of hybrid organo-inorganic aluminophosphate frameworks in the presence of fluoride. These molecules were selected because of their particular molecular asymmetric structure, which enables a rich supramolecular chemistry and a potential chiral recognition phenomenon during crystallization...
March 15, 2018: Physical Chemistry Chemical Physics: PCCP
A Masarykova, D Scepanovic, P Povinec, P Bires, D Lederleitner, M Pobijakova
OBJECTIVES: To analyse whether the maximum standardized uptake value of the positron emission tomography/computed tomography for radiotherapy planning was useful as a prognostic factor for tumour response and survival of patients with locally advanced non-small cell lung cancer. BACKGROUND: Increased 18F-fluoro-2-deoxyglucose uptake by lung cancer cells, measured as the maximum standardized uptake value, has been reported to predict the biologic aggressiveness of both early and advanced non-small cell lung cancer...
2018: Bratislavské Lekárske Listy
Hongkai Wang, Ziyu Tan, Qiang Zheng, Jing Yu
PURPOSE: Recent researches have demonstrated the value of using 2-deoxy-2-[18 F]fluoro-D-glucose ([18 F]FDG) positron emission tomography (PET) imaging to reveal the hypothyroidism-related damages in local brain regions. However, the influence of hypothyroidism on the entire brain network is barely studied. This study focuses on the application of graph theory on analyzing functional brain networks of the hypothyroidism symptom. PROCEDURES: For both the hypothyroidism and the control groups of Wistar rats, the functional brain networks were constructed by thresholding the glucose metabolism correlation matrices of 58 brain regions...
March 12, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Joan Fledelius, Anne Winther-Larsen, Azza A Khalil, Karin Hjorthaug, Jørgen Frøkiær, Peter Meldgaard
We evaluated whether changes in18 F-Fluoro-D-Glucose (18 F-FDG)-uptake evaluated early during erlotinib treatment predict survival in non-small cell lung cancer (NSCLC) patients. Positron emission tomography (PET)/CT scans from 56 NSCLC patients before and after 7-10 days of erlotinib treatment were analyzed with four different methods: Visual evaluation and percentage change in lean body mass corrected standardized uptake values (SULs): SULpeak , SULmax and total lesion glycolysis (TLG). The semi-quantitative parameters abilities to predict progression free survival (PFS) and overall survival (OS) were compared and we found that percentage change in SULpeak , SULmax and TLG all correlated with PFS and OS with the strongest correlation found for TLG (R=0...
2018: American Journal of Nuclear Medicine and Molecular Imaging
Pengmin Qin, Niall W Duncan, David Yen-Ting Chen, Chi-Jen Chen, Li-Kai Huang, Zirui Huang, Chien-Yuan E Lin, Christine Wiebking, Che-Ming Yang, Georg Northoff, Timothy Lane
Neural activity varies continually from moment to moment. Such temporal variability (TV) has been highlighted as a functionally specific brain property playing a fundamental role in cognition. We sought to investigate the mechanisms involved in TV changes between two basic behavioural states, namely having the eyes open (EO) or eyes closed (EC) in vivo in humans. To these ends we acquired BOLD fMRI, ASL, and [18 F]-fluoro-deoxyglucose PET in a group of healthy participants (n = 15), along with BOLD fMRI and [18 F]-flumazenil PET in a separate group (n = 19)...
March 9, 2018: Neuroscience
Jaime Retamal, Daniel Hurtado, Nicolás Villarroel, Alejandro Bruhn, Guillermo Bugedo, Marcelo Britto Passos Amato, Eduardo Leite Vieira Costa, Göran Hedenstierna, Anders Larsson, João Batista Borges
OBJECTIVE: It is known that ventilator-induced lung injury causes increased pulmonary inflammation. It has been suggested that one of the underlying mechanisms may be strain. The aim of this study was to investigate whether lung regional strain correlates with regional inflammation in a porcine model of acute respiratory distress syndrome. DESIGN: Retrospective analysis of CT images and positron emission tomography images using [F]fluoro-2-deoxy-D-glucose. SETTING: University animal research laboratory...
March 9, 2018: Critical Care Medicine
Song-Lin Zhang, Chang Xiao, Hai-Xing Wan
Cu(iii) trifluoromethyl complexes are proposed as essential intermediates for many copper-promoted trifluoromethylation reactions, but remain elusive and scarcely explored. We report herein the isolation and spectroscopic and X-ray crystallographic characterization of diverse CuIII -CF3 complexes (6-10) with varied coordinating motifs (mono-, bi- or tridentate) and formal charges (neutral or monoanionic) for the ligand L (L is pyridine, 2,4,6-trimethylpyridine, quinol-8-yloxide or 2,6-bis(2'-pyridyl)pyridine)...
March 12, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Patrick A Robertson, Luigi Villani, Uresha L M Dissanayake, Luke F Duncan, Belinda M Abbott, David J D Wilson, Evan G Robertson
The electronic spectra of 2-bromoethylbenzene and its chloro and fluoro analogues have been recorded by resonant two-photon ionisation (R2PI) spectroscopy. Anti and gauche conformers have been assigned by rotational band contour analysis and IR-UV ion depletion spectroscopy in the CH region. Hydrate clusters of the anti conformers have also been observed, allowing the role of halocarbons as hydrogen bond acceptors to be examined in this context. The donor OH stretch of water bound to chlorine is red-shifted by 36 cm-1 , or 39 cm-1 in the case of bromine...
March 12, 2018: Physical Chemistry Chemical Physics: PCCP
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