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Neila Maria R de Lima, Emerson de O Ferreira, Mara Yone S D Fernandes, Francisco Arnaldo V de Lima, Kelly Rose T Neves, Marta Regina S do Carmo, Geanne M de Andrade
Inflammation plays a pivotal role in the development of ischemic brain damage. Astrocyte activation promotes the production of several proinflammatory mediators, such as TNF-α and iNOS. Eventually, neuronal death occurs, leading to the development of motor and memory deficits in patients. Boldine is the main alkaloid in the leaves and bark of the Peumus boldus Molina, and has anti-inflammatory and antioxidant properties. The aim of this work was to investigate the neuroprotective effect of boldine on neuroinflammation and memory deficits induced by permanent middle cerebral artery occlusion (pMCAO) in mice...
October 19, 2016: Behavioural Pharmacology
Renxun Chen, Nerida Cole, Debarun Dutta, Naresh Kumar, Mark D P Willcox
Lactoferrin and lactoferricin were immobilized on glass surfaces via two linkers, 4-azidobenzoic acid (ABA) or 4-fluoro-3-nitrophenyl azide (FNA). The resulting surfaces were characterized by X-ray photoelectron spectroscopy (XPS) and contact angle measurements. The antimicrobial activity of the surfaces was determined using Pseudomonas aeruginosa and Staphylococcus aureus strains by fluorescence microscopy. Lactoferrin and lactoferricin immobilization was confirmed by XPS showing significant increases (p < 0...
October 19, 2016: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
Rosario Gajardo-Gómez, Valeria C Labra, Carola J Maturana, Kenji F Shoji, Cristian A Santibañez, Juan C Sáez, Christian Giaume, Juan A Orellana
The mechanisms involved in Alzheimer's disease are not completely understood and how astrocytes and their gliotransmission contribute to this neurodegenerative disease remains to be fully elucidated. Previous studies have shown that amyloid-β peptide (Aβ) induces neuronal death by a mechanism that involves the excitotoxic release of ATP and glutamate associated to astroglial hemichannel opening. We have demonstrated that synthetic and endogenous cannabinoids (CBs) reduce the opening of astrocyte Cx43 hemichannels evoked by activated microglia or inflammatory mediators...
October 19, 2016: Glia
Kayako Isohashi, Eku Shimosegawa, Sadahiro Naka, Yasukazu Kanai, Genki Horitsugi, Ikuko Mochida, Keiko Matsunaga, Tadashi Watabe, Hiroki Kato, Mitsuaki Tatsumi, Jun Hatazawa
BACKGROUND: In boron neutron capture therapy (BNCT), positron emission tomography (PET) with 4-borono-2-(18)F-fluoro-phenylalanine (FBPA) is the only method to estimate an accumulation of (10)B to target tumor and surrounding normal tissue after administering (10)B carrier of L-paraboronophenylalanine and to search the indication of BNCT for individual patient. Absolute concentration of (10)B in tumor has been estimated by multiplying (10)B concentration in blood during BNCT by tumor to blood radioactivity (T/B) ratio derived from FBPA PET...
December 2016: EJNMMI Research
D Li, F Liu, T Yang, T Jin, H Zhang, X Luo, M Wang
Intracerebral hemorrhage (ICH) results in a devastating brain disorder with high mortality and poor prognosis and effective therapeutic intervention for the disease remains a challenge at present. The present study investigated the neuroprotective effects of rapamycin on ICH-induced brain damage and the possible involvement of activated microglia. ICH was induced in rats by injection of type IV collagenase into striatum. Different dose of rapamycin was systemically administrated by intraperitoneal injection beginning at 1 h after ICH induction...
September 30, 2016: Cellular and Molecular Biology
Gretchen Bain, Kristen E Shannon, Fei Huang, Janice Darlington, Lance Goulet, Patricia Prodanovich, Gina L Ma, Angelina M Santini, Adam J Stein, Dave Lonergan, Christopher D King, Imelda Calderon, Andiliy Lai, John H Hutchinson, Jilly F Evans
Autotaxin (ATX) is a secreted glycoprotein that converts lysophosphatidylcholine (LPC) to the bioactive phospholipid lysophosphatidic acid (LPA) and is the major enzyme generating circulating LPA. Inhibition of LPA signaling has profound anti-fibrotic effects in multiple organ systems including the lung, kidney, skin and peritoneum. However, other LPA-generating pathways exist and the role of ATX in localized tissue LPA production and fibrosis remains unclear and controversial. In this study, we describe the preclinical pharmacological, pharmacokinetic and pharmacodynamic properties of a novel small-molecule ATX inhibitor [3-((6-chloro-2-cyclopropyl-1-(1-ethyl-1H-pyrazol-4-yl)-7-fluoro-1H-indol-3-yl) thio)-2-fluorobenzoic acid sodium salt] (PAT-505)...
October 17, 2016: Journal of Pharmacology and Experimental Therapeutics
Masahiro Ono, Atsumi Baden, Hiroyuki Okudaira, Masato Kobayashi, Keiichi Kawai, Shuntaro Oka, Hirokatsu Yoshimura
[(18)F]Fluciclovine (trans-1-amino-3-[(18)F]fluorocyclobutanecarboxylic acid; anti-[(18)F]FACBC), a positron emission tomography tracer used for the diagnosis of recurrent prostate cancer, is transported via amino acid transporters (AATs) with high affinity (Km: 97-230 μM). However, the mechanism underlying urinary excretion is unknown. In this study, we investigated the involvement of AATs and drug transporters in renal [(18)F]fluciclovine reuptake. [(14)C]Fluciclovine (trans-1-amino-3-fluoro[1-(14)C]cyclobutanecarboxylic acid) was used because of its long half-life...
October 14, 2016: International Journal of Molecular Sciences
Christopher I McHugh, Jawana M Lawhorn-Crews, Dipenkumar Modi, Kirk A Douglas, Steven K Jones, Thomas J Mangner, Jerry M Collins, Anthony F Shields
BACKGROUND: A principal goal for the use of positron emission tomography (PET) in oncology is for real-time evaluation of tumor response to chemotherapy. Given that many contemporary anti-neoplastic agents function by impairing cellular proliferation, it is of interest to develop imaging modalities to monitor these pathways. Here we examined the effect of capecitabine on the uptake of thymidine analogs used with PET: 3'-deoxy-3'-[(18)F]fluorothymidine ((18)F-FLT), 1-(2'-deoxy-2'-[(18)F]fluoro-β-D-arabinofuranosyl) thymidine ((18)F-FMAU), and 1-(2'-deoxy-2'-[(18)F]fluoro-β-D-arabinofuranosyl) uracil ((18)F-FAU) in patients with advanced cancer...
October 17, 2016: Cancer Imaging: the Official Publication of the International Cancer Imaging Society
Xin-Yue Cheng, Yu-Huan Li, Sheng Tang, Xin Zhang, Yan-Xiang Wang, Sheng-Gang Wang, Jian-Dong Jiang, Ying-Hong Li, Dan-Qing Song
Twenty-eight new 12N-benzenesulfonyl matrinic butane and halogenated 12N-sulfonyl matrinic butane/ethane derivatives were designed, synthesized and evaluated for their anti-coxsakievirus activities against CVB3 taking compound 1 as the lead. SAR analysis indicated the introduction of a fluoro atom on the 1'-position might be helpful for keeping potency. Among them, compound 8a exhibited potential activities against all CVBs with IC50 ranging from 0.69 to 5.14 μM, suggesting a broad-spectrum anti-coxsackievirus B feature...
September 30, 2016: European Journal of Medicinal Chemistry
Brandon A Vara, Jeffrey N Johnston
Preparation of a range of enantioenriched β-fluoro amines (α,β-disubstituted) is described in which the nitrogen and fluorine atoms are attached to sp(3)-hybridized carbons. The key finding is a chiral bifunctional Brønsted acid/base catalyst that can deliver β-amino-α-fluoro nitroalkanes with high enantio- and diastereoselection. A denitration step renders the nitro group "traceless" and delivers secondary, tertiary, or vinyl alkyl fluorides embedded within a vicinal fluoro amine functional group. A synthesis of each possible stereoisomer of a β-fluoro lanicemine illustrates the potential ease with which fluorinated small molecules relevant to neuroscience drug development can be prepared in a stereochemically comprehensive manner...
October 17, 2016: Journal of the American Chemical Society
Yohei Manabe, Marie Yoshimura, Kazuma Sakamaki, Asuka Inoue, Aya Kakinoki, Satoshi Hokari, Mariko Sakanaka, Junken Aoki, Hiroyuki Miyachi, Kazuyuki Furuta, Satoshi Tanaka
Accumulating evidence suggests that activated mast cells are involved in contact hypersensitivity, although the precise mechanisms of their activation are still not completely understood. We investigated the potential of common experimental allergens to induce mast cell activation using murine bone marrow-derived cultured mast cells and rat peritoneal mast cells. Among these allergens, 1-chloro-2,4-dinitrobenzene and 1-fluoro-2,4-dinirobenzene (DNFB) were found to induce degranulation of rat peritoneal mast cells...
October 17, 2016: European Journal of Immunology
Augusto Rivera, Jicli José Rojas, Jaime Ríos-Motta, Michael Bolte
The title fluorinated bis-benzoxazine, C18H18F2N2O2, crystallizes with one half-mol-ecule in the asymmetric unit, which is completed by inversion symmetry. The fused oxazine ring adopts an approximately half-chair conformation. The two benzoxazine rings are oriented anti to one another around the central C-C bond. The dominant inter-molecular inter-action in the crystal structure is a C-H⋯F hydrogen bond between the F atoms and the axial H atoms of the OCH2N methyl-ene group in the oxazine rings of neighbouring mol-ecules...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Miguel Pinto, Indranil Chakraborty, Pradip Mascharak
The title compound, [Ag(qPyr)2]CF3SO3 where qPyr = 1-(quinoline-2-yl-methyl-ene)amino-pyrene, C26H16N2, was synthesized from a reaction of silver tri-fluoro-methane-sulfonate and qPyr in di-chloro-methane-methanol mixed media. In this design, the qPyr ligand was chosen for its characteristic excitation and emission profiles, which could enable the tracking of the silver complex within biological targets. The Ag(I) atom resides in a distorted tetra-hedral N4 coordination sphere. Analysis of the packing pattern revealed significant intra- and inter-molecular π-π stacking inter-actions between the [Ag(qPyr)2](+) cations...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Darcie L Stack, Jason D Masuda
The title compound, C27H38ClN2(+)·C32H12BF24(-), was synthesized by reacting the product formed from a previous reaction between 1,3-bis-(2,6-diiso-propyl-phen-yl)imidazolinium-2-carboxyl-ate (SIPrCO2), and SOCl2, with sodium tetra-kis-[3,5-bis-(tri-fluoro-meth-yl)phen-yl]borate (NaBARF). In the cation, the imidazole ring is in a half-chair conformation and the formerly carbene carbon atom is bonded in a distorted trigonal-planar geometry with N-C-Cl angles of 122.96 (16) and 122.21 (16)° and an N-C-N angle of 114...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Huihua Sun, Wan Lin Yeo, Yee Hwee Lim, Xinying Chew, Derek John Smith, Bo Xue, Kok Ping Chan, Robert C Robinson, Edward G Robins, Huimin Zhao, Ee Lui Ang
Fluorinases offer an environmentally friendly alternative for selective fluorination under mild conditions. However, their diversity is limited in nature and they have yet to be engineered through directed evolution. Herein, we report the directed evolution of the fluorinase FlA1 for improved conversion of the non-native substrate 5'-chloro-5'-deoxyadenosine (5'-ClDA) into 5'-fluoro-5'-deoxyadenosine (5'-FDA). The evolved variants, fah2081 (A279Y) and fah2114 (F213Y, A279L), were successfully applied in the radiosynthesis of 5'-[(18) F]FDA, with overall radiochemical conversion (RCC) more than 3-fold higher than wild-type FlA1...
October 14, 2016: Angewandte Chemie
Stephen W Scheff, Kelly N Roberts
We have previously shown that pycnogenol (PYC) increases antioxidants, decreases oxidative stress, suppresses neuroinflammation and enhances synaptic plasticity following traumatic brain injury (TBI). Here, we investigate the effects of PYC on cognitive function following a controlled cortical impact (CCI). Adult Sprague-Dawley rats received a CCI injury followed by an intraperitoneal injection of PYC (50 or 100mg/kg). Seven days post trauma, subjects were evaluated in a Morris water maze (MWM) and evaluated for changes in lesion volume...
October 11, 2016: Neuroscience Letters
Xin-Xing Zhan, Xin Zhang, Si-Min Dai, Shu-Hui Li, Xu-Zhai Lu, Lin-Long Deng, Su-Yuan Xie, Rong-Bin Huang, Lan-Sun Zheng
Despite being widely used as electron acceptor in polymer solar cells, commercially available PC71BM (phenyl-C71-butyric acid methyl ester) usually has a "random" composition of mixed regioisomers or stereoisomers. Here the PC71BM has been isolated into three typical isomers, α-, β1- and β2-PC71BM, for establishing the isomer-dependent photovoltaic performance on change of ternary composition of α-, β1- and β2-PC71BM. Mixing the isomers in a ratio of α:β1:β2=8:1:1 resulted in the best power conversion efficiency (PCE) of 7...
October 13, 2016: Chemistry: a European Journal
Tahir Ali, Min Ju Kim, Shafiq Ur Rehman, Ashfaq Ahmad, Myeong Ok Kim
Nanomedicine is an emerging research area. In this study, we investigated the neuroprotective efficacy of anthocyanin-loaded polyethylene glycol-gold nanoparticles (PEG-AuNPs) for enhancing the neuroprotective efficacy of anthocyanins in an amyloid beta (Aβ)1-42 mouse model of Alzheimer's disease. We observed that both anthocyanin-loaded PEG-AuNPs and anthocyanins treatment (12 μg/g/day for 14 days) ameliorated memory impairments in the Aβ1-42-injected mice. However, the anthocyanin-loaded PEG-AuNPs were more effective than free anthocyanins...
October 11, 2016: Molecular Neurobiology
Veikko Uahengo, Yan Zhang, Bi Xiong, Pingping Zhao, Ping Cai, Lydia Rhyman, Ponnadurai Ramasami, Kai Hu, Gongzhen Cheng
The 2,2'-dinaphtholazobenzene molecular framework (P) was designed, synthesized and characterized. Its absorption and fluorescence properties revealed that P is a dual sensor for copper ions (Cu(2+)) and fluoride ions (F(-)) in DMSO. The colorimetric activities were clearly visible by naked eye upon the addition of the two ions. Fluorescence quenching and enhancement were observed when Cu(2+) and F(-) ions were added respectively. Density Functional Theory (DFT) calculations were carried out to provide an insight into the interaction of guest ions (Cu(2+) and F(-)) with P, and to explain how the molecular orbitals were affected...
October 11, 2016: Journal of Fluorescence
Pauline W Ondachi, Ana H Castro, Benjamin Sherman, Charles W Luetje, M Imad Damaj, Samuel Wayne Mascarella, Hernán A Navarro, Frank Ivy Carroll
The synthesis, nAChR in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted thiophenyl)deschloroepibatidine analogues (5a-f, 6a-d, and 7a-c) are presented herein. All had subnanomolar affinity at α4β2*-nAChRs. Contrary to lead structure epibatidine, a potent nAChR agonist, all were potent α4β2- and α3β4-AChR antagonists in an in vitro functional assay. In vivo, the compounds were also nAChR antagonists with various degrees of agonist activity. Compounds 5e, 5f, 6a, 6c, 6d, and 7c had no agonist effects in the tail-flick, hot-plate, hypothermia, or spontaneous activity tests whereas 5a-d, 7a and 7b did not have agonist activity in the tail-flick and hot-plate tests but like varenicline, were agonists in the hypothermia and spontaneous activity tests...
October 11, 2016: ACS Chemical Neuroscience
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