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https://www.readbyqxmd.com/read/29786911/esipt-modulated-emission-of-lanthanide-complexes-different-energy-transfer-pathway-and-multi-responses
#1
Si-Si Sun, Zheng Wang, Xiang Wen Wu, Jian-Hua Zhang, Chao-Jie Li, Shao-Yun Yin, Ling Chen, Mei Pan, Cheng-Yong Su
Two series of isostructural lanthanide coordination complexes, namely, LIFM-42(Ln), Ln = Eu, Tb, Gd, and LIFM-43(Ln), Ln = Er, Yb) were synthesized through the self-assembly of an ESIPT (excited-state intramolecular proton transfer) ligand, H2hpi2cf (5-(2-(5-fluoro-2-hydroxyphenyl)-4,5-bis(4-fluorophenyl)-1H-imidazol-1-yl)isophthalic acid) with different lanthanide ions. In the coordination structures linked by the ligands and oxo-bridged LnIII2 clusters (for LIFM-42(Ln) series) or isolated LnIII ions (for LIFM-43(Ln) series), the ESIPT ligand can serve as both the host and antenna for protecting and sensitizing the photoluminescence (PL) of LnIII ions...
May 22, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29786852/evolution-of-lobar-abnormalities-of-cerebral-glucose-metabolism-in-41-children-with-drug-resistant-epilepsy
#2
Tuhina Govil-Dalela, Ajay Kumar, Michael E Behen, Harry T Chugani, Csaba Juhász
OBJECTIVE: We analyzed long-term changes of lobar glucose metabolic abnormalities in relation to clinical seizure variables and development in a large group of children with medically refractory epilepsy. METHODS: Forty-one children (25 males) with drug-resistant epilepsy had a baseline positron emission tomography (PET) scan at a median age of 4.7 years; the scans were repeated after a median of 4.3 years. Children with progressive neurological disorders or space-occupying lesion-related epilepsy and those who had undergone epilepsy surgery were excluded...
May 22, 2018: Epilepsia
https://www.readbyqxmd.com/read/29785630/calcium-channels-rho-kinase-protein-kinase-c-and-phospholipase-c-pathways-mediate-mercury-chloride-induced-myometrial-contractions-in-rats
#3
Swati Koli, Atul Prakash, Soumen Choudhury, Rajesh Mandil, Satish K Garg
Adverse effects of mercury on female reproduction are reported; however, its effect on myogenic activity of uterus and mechanism thereof is obscure. Present study was undertaken to unravel the mechanistic pathways of mercuric chloride (HgCl2 )-induced myometrial contraction in rats. Isometric tension in myometrial strips of rats following in vitro exposure to HgCl2 was recorded using data acquisition system-based physiograph. HgCl2 produced concentration-dependent (10 nM-100 μM) uterotonic effect which was significantly (p < 0...
May 21, 2018: Biological Trace Element Research
https://www.readbyqxmd.com/read/29779163/discovering-simple-phenylboronic-acid-and-benzoxaborole-derivatives-for-experimental-oncology-phase-cycle-specific-inducers-of-apoptosis-in-a2780-ovarian-cancer-cells
#4
Mateusz Psurski, Agnieszka Łupicka-Słowik, Agnieszka Adamczyk-Woźniak, Joanna Wietrzyk, Andrzej Sporzyński
Objective The aim of the study was to evaluate the antiproliferative potential of simple phenylboronic acid and benzoxaborole derivatives as well as to provide preliminary insight into their mode of action in cancer cells in vitro. Methods The antiproliferative activity was assessed in five diverse cancer cell lines via the SRB method (sulforhodamine B) or MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method after 72 h of treatment. Further studies of the mechanism of action consisted of the influence of the compounds on cell cycle progression and apoptosis induction, which was assessed by flow cytometry, caspase-3 enzymatic activity, fluorescence microscopy and western blot analysis...
May 19, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29778441/hypoxic-postconditioning-enhances-functional-recovery-following-endothelin-1-induced-middle-cerebral-artery-occlusion-in-conscious-rats
#5
Hong L Nguyen, Alexander M Ruhoff, Thomas Fath, Nicole M Jones
Stroke is a leading cause of death and a major contributor to neurological disability in adults. Tissue plasminogen activator is the only approved treatment. However, due to its narrow therapeutic window, <5% of patients receive treatment. Recently, hypoxic postconditioning (HPC) was shown to reduce stroke induced-injury in mice, but the mechanisms and functional outcomes are still unknown. In the current study, male Sprague Dawley rats were subjected to endothelin-1 induced stroke. HPC (8% O2 , 1 h/d for 5d) or normoxia treatments were started 24 h after stroke...
May 17, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29776597/the-role-of-fdg-pet-in-detecting-rejection-after-liver-transplantation
#6
Ashley M Watson, Neal Bhutiani, Prejesh Philips, Eric G Davis, Mary Eng, Robert M Cannon, Christopher M Jones
BACKGROUND: The activation and increased metabolic activity of T cells in acute cellular rejection could allow fluoro-2-deoxyglucose positron emission tomography to be utilized for detection of acute cellular rejection. The objective of this study was to evaluate the effectiveness of fluoro-2-deoxyglucose positron emission tomography in detecting acute cellular rejection in the clinical setting. METHODS: Fluoro-2-deoxyglucose positron emission tomography studies were performed on 88 orthotopic liver transplant patients at 7 and 17 days postoperatively (first positron emission tomography and second positron emission tomography, respectively)...
May 15, 2018: Surgery
https://www.readbyqxmd.com/read/29775538/discovery-of-potent-and-centrally-active-6-substituted-5-fluoro-1-3-dihydro-oxazine-%C3%AE-secretase-bace1-inhibitors-via-active-conformation-stabilization
#7
Kenji Nakahara, Kouki Fuchino, Kazuo Komano, Naoya Asada, Genta Tadano, Tsuyoshi Hasegawa, Takahiko Yamamoto, Yusuke Sako, Masayoshi Ogawa, Chie Unemura, Motoko Hosono, Hisanori Ito, Gaku Sakaguchi, Shigeru Ando, Shuichi Ohnishi, Yasuto Kido, Tamio Fukushima, Deborah Dhuyvetter, Herman Borghys, Harrie J M Gijsen, Yoshinori Yamano, Yasuyoshi Iso, Ken-Ichi Kusakabe
β-Secretase (BACE1) has an essential role in the production of amyloid β peptides that accumulate in patients with Alzheimer's disease (AD). Thus, inhibition of BACE1 is considered to be a disease-modifying approach for the treatment of AD. Our hit-to-lead efforts led to a cellular potent 1,3-dihydro-oxazine 6, which however inhibited hERG and showed high P-gp efflux. The close analog of 5-fluoro-oxazine 8 reduced P-gp efflux; further introduction of electron withdrawing groups at the 6-position improved potency and also mitigated P-gp efflux and hERG inhibition...
May 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29774744/tetrafluorobenzo-fused-bodipy-a-platform-for-regioselective-synthesis-of-bodipy-dye-derivatives
#8
Andrea Savoldelli, Qianli Meng, Roberto Paolesse, Frank R Fronczek, Kevin Malcolm Smith, M Graça Henriques Vicente
A novel route for the synthesis of unsymmetrical benzo-fused BODIPYs is reported using 4,5,6,7-tetrafluoroisoindole as a precursor. The reactivity of the asymmetric 3,5-dibromo benzo-fused BODIPY was investigated under nucleophilic substitution and Pd(0)-catalyzed cross-coupling reaction conditions. In addition to the 3,5-bromines, one α-fluoro group on the benzo-fused ring can also be functionalized, and an unusual homocoupling with formation of a bisBODIPY was observed. This new class of fluorinated BODIPYs could find various applications in medicine and materials...
May 18, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29772244/gender-difference-in-the-effect-of-progesterone-on-neonatal-hypoxic-ischemic-brain-injury-in-mouse
#9
Shuyu Dong, Qian Zhang, Delian Kong, Chao Zhou, Jie Zhou, Jingjing Han, Yan Zhou, Guoliang Jin, Xiaodong Hua, Jun Wang, Fang Hua
This study was to investigate the effects of progesterone (PROG) on neonatal hypoxic/ischemic (NHI) brain injury, the differences in effects between genders, and the underlying mechanisms. NHI brain injury was established in both male and female neonatal mice induced by occlusion of the left common carotid artery followed by hypoxia. The mice were treated with PROG or vehicle. Fluoro-Jade B staining (F-JB), long term behavior testing, and brain magnetic resonance image (MRI) were applied to evaluate neuronal death, neurological function, and brain damage...
May 14, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29771717/prognostic-predictive-value-of-preoperative-intratumoral-2-deoxy-2-18f-fluoro-d-glucose-uptake-heterogeneity-in-patients-with-high-grade-serous-ovarian-cancer
#10
Shuai Liu, Zheng Feng, Zhaoxia Jiang, Hao Wen, Junyan Xu, Herong Pan, Yu Deng, Lei Zhang, Xingzhu Ju, Xiaojun Chen, Xiaohua Wu
OBJECTIVE: This study aimed to explore the clinical and prognostic significance of pretreatment positron-emission tomography/computed tomography (PET/CT) parameters, especially 2-deoxy-2-(F)fluoro-D-glucose-based heterogeneity, in high-grade serous ovarian cancer (HGSC). MATERIALS AND METHODS: We retrospectively investigated 56 patients with HGSC who underwent PET/CT before primary surgery at our hospital between January 2010 and June 2015. None of these patients received neoadjuvant chemotherapy...
May 16, 2018: Nuclear Medicine Communications
https://www.readbyqxmd.com/read/29771302/physical-linkage-of-estrogen-receptor-%C3%AE-and-aromatase-in-rat-oligocrine-and-endocrine-actions-of-cns-produced-estrogens
#11
Emiliya M Storman, Nai-Jiang Liu, Martin W Wessendorf, Alan R Gintzler
Rapid-signaling membrane estrogen receptors and aromatase are present throughout the central nervous system (CNS), enabling acute regulation of CNS estrogenic signaling. We previously reported that spinal membrane aromatase (mAro) and membrane estrogen receptor α (mERα) oligomerize (1). Since their organizational relationship would likely influence functions of locally produced estrogens, we quantified the mAro and mERα that are physically associated and non-associated in two functionally different regions of rat CNS - spinal cord, which has predominantly neural functionalities, and hypothalamus, which has both neural and endocrine capabilities...
May 15, 2018: Endocrinology
https://www.readbyqxmd.com/read/29769797/protective-effects-of-erigeron-breviscapus-hand-mazz-ebhm-extract-in-retinal-neurodegeneration-models
#12
Jingyuan Zhu, Li Chen, Yun Qi, Jing Feng, Li Zhu, Yujing Bai, Huijuan Wu
Purpose: To investigate the neuroprotective effects of scutellarin, an active component of the multifunctional traditional Chinese herb Erigeron breviscapus (vant.) Hand.-Mazz. (EBHM), which has been used as a neuroprotective therapy for cerebrovascular diseases. We performed the experiments using in vitro and in vivo models of retinal neurodegeneration. Methods: In the in vitro experiments, we exposed BV-2 cells to low oxygen levels in an incubator for 24 and 48 h to generate hypoxia models...
2018: Molecular Vision
https://www.readbyqxmd.com/read/29768881/lipophilic-prodrug-of-floxuridine-loaded-into-solid-lipid-nanoparticles-in-vitro-cytotoxicity-studies-on-different-human-cancer-cell-lines
#13
Daniela Chirio, Elena Peira, Luigi Battaglia, Benedetta Ferrara, Alessandro Barge, Simona Sapino, Susanna Giordano, Chiara Dianzani, Marina Gallarate
Floxuridine is a very effective drug with high potency in the treatment of various tumors but its utility is limited by its low efficiency of cellular uptake. In order to improve the floxuridine efficiency of cellular uptake, lipophilic prodrug of floxuridine (3',5'-distearoyl-5-fluoro-2'-deoxyuridine) was synthetized and loaded into behenic acid nanoparticles produced by fatty acid coacervation technique. Generally, spherical shaped SLN with mean diameters below 300 nm were obtained. Distearoyl-floxuridine was loaded in SLN with high entrapment efficiency (from 70...
January 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29766661/structure-based-design-of-a-eukaryote-selective-antiprotozoal-fluorinated-aminoglycoside
#14
Hiroki Kanazawa, Oscar M Saavedra, Juan Pablo Maianti, Simon A Young, Luis Izquierdo, Terry K Smith, Stephen Hanessian, Jiro Kondo
Aminoglycosides (AG) are antibiotics that lower the accuracy of protein synthesis by targeting a highly-conserved RNA helix of the ribosomal A-site. The discovery of AGs that selectively target the eukaryotic ribosome, but lack activity in prokaryotes, are promising as antiprotozoals for the treatment of neglected tropical diseases, and as therapies to read-through point-mutation genetic diseases. However, a single nucleobase change A1408G in the eukaryotic A-site leads to negligible affinity for most AGs. Herein we report the synthesis of 6'-fluoro sisomicin, the first 6'-fluorinated aminoglycoside, which specifically interacts with the protozoal cytoplasmic rRNA A-site, but not the bacterial A-site, as evidenced by X-ray co-crystal structures...
May 15, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29765765/cs-tf-2-n-a-second-polymorph-with-a-layered-structure
#15
Jared T Stritzinger, Janelle E Droessler, Brian L Scott, George S Goff
The structural determination of the ionic liquid, caesium bis-[(tri-fluoro-meth-yl)sulfon-yl]imide or poly[[μ4 -bis-[(tri-fluoro-meth-yl)sulfon-yl]imido]caesium(I)], Cs[N(SO2 CF3 )2 ] or Cs[Tf2 N], reveals a second polymorph that also crystallizes in a layer structure possessing monoclinic P 21 / c symmetry at 120 K instead of C 2/ c for the known polymorph [Xue et al. (2002 ▸). Solid State Sci. 4 , 1535-1545]. The caesium ions in the cationic layers are coordinated by the sulfonyl groups of the bis-triflimide mol-ecules from anion layers while the tri-fluoro-methyl groups are oriented in the opposite direction, forming a non-polar surface separating the layers...
April 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29765759/crystal-structures-of-5-12-dimethyl-1-4-8-11-tetra-aza-cyclo-tetra-decane-cobalt-iii-mono-phenyl-acetyl-ide-and-bis-phenyl-acetyl-ide
#16
Benjamin M Oxley, Brandon Mash, Matthias Zeller, Susannah Banziger, Tong Ren
Reported in this contribution are the synthesis and crystal structures of new mono- and bis-phenyl-acetyl-ides based on CoIII (DMC) (DMC is 5,12-dimethyl-1,4,8,11-tetra-aza-cyclo-tetra-deca-ne). Chlorido-(5,12-dimethyl-1,4,8,11-tetra-aza-cyclo-tetra-deca-ne)(phenyl-ethyn-yl)cobalt(III) chloride-aceto-nitrile-methanol (1/1/1), [Co(C8 H5 )Cl(C12 H28 N4 )]Cl·CH3 CN·CH3 OH, 1 , and (5,12-dimethyl-1,4,8,11-tetra-aza-cyclo-tetra-deca-ne)bis-(phenyl-ethyn-yl)cobalt(III) tri-fluoro-methane-sulfonate-di-chloro-methane (2/1), [Co(C8 H5 )2 (C12 H28 N4 )]2 (CF3 SO3 )2 ·CH2 Cl2 , 2 , were prepared under weak-base conditions in satisfactory yields...
April 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29765751/crystal-structures-of-two-new-3-2-chloro-eth-yl-r-2-c-6-diarylpiperidin-4-ones
#17
K Rajkumar, S Sivakumar, R Arulraj, Manpreet Kaur, Jerry P Jasinski, A Manimekalai, A Thiruvalluvar
The syntheses and crystal structures of 3-(2-chloro-eth-yl)- r -2, c -6-di-phenyl-piperidin-4-one, C19 H20 ClNO, (I), and 3-(2-chloro-eth-yl)- r -2, c -6-bis-(4-fluoro-phen-yl)piperidin-4-one, C19 H18 ClF2 NO, (II), are described. The piperidone ring adopts a chair conformation in (I), whereas a slightly distorted chair conformation is formed in (II). The dihedral angle between the mean plane of the phenyl rings is 59.1 (1)° in (I) and 76.1 (1)° in (II). The crystal packing features weak inter-molecular N-H⋯O hydrogen bonds in each structure...
April 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29765738/crystal-structure-and-hirshfeld-analysis-of-trans-bis-5-fluoro-indoline-2-3-dione-3-oximato-%C3%AE%C2%BA-2-o-2-n-3-trans-bis-pyridine-%C3%AE%C2%BA-n-copper-ii
#18
Ana Paula Lopes de Melo, Leandro Bresolin, Bianca Barreto Martins, Vanessa Carratu Gervini, Adriano Bof de Oliveira
The reaction in methanol of CuII acetate monohydrate with 5-fluoro-isatin 3-oxime deprotonated with KOH in a 1:2 molar ratio and recrystallization from pyridine yielded the title compound, [Cu(C8 H4 FN2 O2 )2 (C5 H5 N)2 ]. In the centrosymmetric complex, the anionic form of the isatin oxime acts as a κ2 N , O donor, building five-membered metallarings. The CuII cation is sixfold coordinated in a slightly distorted octa-hedral environment by two trans , equatorial, anionic isatin derivatives and two trans pyridine ligands in axial positions...
April 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29765728/different-mol-ecular-conformations-in-the-crystal-structures-of-three-5-nitro-imidazolyl-derivatives
#19
Luis F B Osorio, Samir A Carvalho, Edson F da Silva, Carlos A M Fraga, Solange M S V Wardell, Bruce F Milne, James L Wardell, William T A Harrison
The crystal structures of ( E )-1-methyl-5-nitro-1 H -imidazole-2-carbaldehyde O -benzyl-oxime, C12 H12 N4 O3 , (I), ( E )-1-methyl-5-nitro-1 H -imidazole-2-carb-alde-hyde O -(4-fluoro-benz-yl) oxime, C12 H11 FN4 O3 , (II), and ( E )-1-methyl-5-nitro-1 H -imidazole-2-carbaldehyde O -(4-bromo-benz-yl) oxime, C12 H11 BrN4 O3 , (III), are described. The dihedral angle between the ring systems in (I) is 49.66 (5)° and the linking Nm -C-C=N (m = methyl-ated) bond shows an anti conformation [torsion angle = 175...
March 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29765724/crystal-structures-of-two-2-3-diaryl-2-3-di-hydro-4-h-1-3-benzo-thia-zin-4-ones
#20
Hemant P Yennawar, Michaela J Buchwalter, Baylee K Colburn, Lee J Silverberg
The syntheses and crystal structures of 2,3-bis-[3-(tri-fluoro-meth-yl)phen-yl]-2,3-di-hydro-4 H -1,3-benzo-thia-zin-4-one (di- m -CF3 ; C22 H13 F6 NOS) ( 1 ) and 2,3-bis-(4-methyl-phen-yl)-2,3-di-hydro-4 H -1,3-benzo-thia-zin-4-one (di- p -CH3 ; C22 H19 NOS) ( 2 ) are reported. Each structure is racemic: the asymmetric unit of 2 consists of two mol-ecules. In both 1 and 2 , the six-membered 1,3-thia-zine ring is close to an envelope conformation with the chiral C atom forming the flap. In 1 , the 2-aryl group is pseudo-equatorial, while in 2 it is pseudo-axial...
March 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
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