bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of some heterocyclic imides and azomethine derivatives under solvent free condition and their anti‐inflammatory activity evaluation
Authors: Sondhi Sham M. , Rani Reshma , Diwvedi Amarendra Dhar , Roy Partha 
Published: November 2009

Abstract
magnified image Condensation of various mono amines with various diacids gave heterocyclic imide derivatives and condensation of amines with various aldehydes gave azomethine derivatives in good yields under solvent free condition. Structures assigned to imide and azomethine derivatives are fully supported by spectral data. All these compounds were screened for anti‐inflammatory activity at a dose of 50 mg/kg p.o. Compound 8a (6‐((tetrahydrofuran‐2‐yl)methyl)‐6H‐pyrrolo[3,4]pyrazine‐5,7‐dione) exhibited anti‐inflammatory activity comparable to standard drug phenyl butazone which showed 37% activity at 50 mg/kg p.o. J. Heterocyclic Chem., 46, 1369, (2009).
Synthesis and antimicrobial activity of new tetrahydro‐naphthalene‐thiazolidinedione and thiohydantoine derivatives
Authors: Ates‐Alagoz Zeynep , Altanlar Nurten , Buyukbingol Erdem 
Published: November 2009

Abstract
magnified image As part of an ongoing program aimed at recognizing novel antioxidant, antimicrobial, and anticancer molecules, herein we report the synthesis and biological evaluation of imidazolidin‐4‐one and thiazolidine‐2,4‐dione derivatives as antimicrobial agents. These compounds were prepared from 5,5,8,8‐tetramethyl‐5,6,7,8‐tetrahydro‐naphthalen‐2‐carboxaldehyde and 3‐substituted phenacyl‐2,4‐thiazolidinediones using Knoevenagel reaction. The structures of compounds were confirmed by 1H NMR, mass spectral data, and elemental analyses. The molecules were evaluated for in vitro antimicrobial activity against methicillin‐resistant Staphylococcus aureus (MRSA) (standard), methicillin‐resistant Staphylococcus aureus (isolated), Staphylococcus aureus (SA), Escherichia coli (EC), Bacillus subtilis (BS), and Candida albicans (CA). Compounds 3a, 3b, 3c, 3d, 3e, 3f, 3g and compound 4 showed equal and/or greater antimicrobial activity against MRSA and EC than ampicillin and sultamicillin. J. Heterocyclic Chem., (2009)
(4,4‐Difluoro‐4‐bora‐3a,4a,‐diaza‐s‐indacen‐3‐yl)acetaldehyde: Synthesis and chemical properties
Authors: Shandura Mykola P. , Yakubovskyi Viktor P. , Kovtun Yuriy P. 
Published: November 2009

Abstract
magnified image A reaction of 3,5‐dimethylborondipyrromethene 3 with the DMF dimethylacetal gives rise to monoenamine 4. The latter is converted to the corresponding aldehyde 5. A considerable contribution of the enolic form of the aldehyde allows preparing numerous 3‐vinyl substituted borondipyrromethenes and some heterocyclic derivatives. A reaction of the aldehyde 5 with tertiary aliphatic amines and the consecutive Hofmann‐type decomposition of the intermediary quaternary salt give rise to the corresponding dialkylaminovinyl derivatives. J. Heterocyclic Chem., (2009).
Facile, efficient, and eco‐friendly synthesis of benzo[b]pyran‐2‐imines over MgO and transformation to the coumarin derivatives
Authors: Valizadeh Hassan , Fakhari Ashraf 
Published: November 2009

Abstract
magnified image Room temperature synthesis of benzo[b]pyran‐2‐imine derivatives via the Knoevenagel condensation of malononitrile and cyanoacetates with salicylaldehyde derivatives over MgO and their transformation to the known coumarins is described. The satisfactory results were obtained with good yields, short reaction time, and simplicity in the experimental procedure. J. Heterocyclic Chem., (2009).
Application of 3‐methylthiopyrido[4,3‐e]‐1,4,2‐dithiazine 1,1‐dioxide to the synthesis of novel series of 4H‐pyrido[4,3‐e]‐1,2,4‐thiadiazine derivatives with potential biological activity
Authors: Brzozowski Zdzisław , Sławiński Jarosław , Kędzia Anna , Kwapisz Ewa , Gdaniec Maria 
Published: November 2009

Abstract
magnified image Two series of 4H‐pyrido[4,3‐e]‐1,2,4‐thiadiazine derivatives 3, 4, 5 and 7, 8, 9, 10, 11, 12 were synthesized by the reactions of 3‐methylthiopyrido[4,3‐e]‐1,4,2‐dithiazine 1,1‐dioxide 1 with 2‐or 6‐hydrazinoazines and 2‐aminophenols or 2‐aminothiophenol, respectively. Aminolysis of 8 (R = Me, Y = O) afforded the corresponding 3‐(R‐amino)‐4‐(2‐hydroxy‐5‐methylphenyl)‐4H‐pyrido[4,3‐e]‐1,2,4‐thiadiazine 1,1‐dioxides 13, 14, 15, 16, 17, 18. The structures of these compounds were confirmed on the basis of elemental analysis, spectral data, and X‐ray crystallography. Compounds 3, 4, 5, 7, 8, 9, 10, 12, 13, 14, 15, and 17, 18 were screened in vitro for antibacterial activity. Moreover, preliminary in vitro anticancer assay was performed for compounds 3, 7, 10, 11, 12, 13, and 17, 18 at the National Cancer Institute (Bethesda, MD) at a single dose (10 μM) in the full NCI 60 cell panel. J. Heterocyclic Chem., (2009).
An evaluation of paper chromatography for measuring the levels of radiochemical impurities in 99mTc Medronate Injection
Authors: Millar Alistair M. , O'Brien Lesley M. , Beattie Lynn A. , Craig Fiona 
Published: November 2009

AbstractBackground: The European Pharmacopoeia specifies Instant Thin‐Layer Chromatography Silica Gel (ITLC‐SG) as the stationary phase for measuring radiochemical impurities in 99mTc Medronate. The Pall Corporation has stopped manufacturing ITLC‐SG. Aim: To investigate chromatography papers as alternatives to ITLC‐SG. Experimental: The resolution of the main 99mTc Medronate and impurity peaks were compared on five Whatman papers (1CHR, 31ET, 3MM, 4CHR and 54SFC) using the pharmacopoeial mobile phases: methyl ethyl ketone for detecting 99mTc pertechnetate impurity and sodium acetate solution (136 g/l) for detecting hydrolysed reduced and colloidal 99mTc impurities. The effects of three sample spot treatments (wet, hot dried and air dried) on the distribution of the radiochemical impurities were compared. The levels of radiochemical impurities measured in samples of 99mTc Medronate were compared. Results: The highest resolutions were obtained with 1CHR, 4CHR and 54SFC. Sample spot drying resulted in the measurement of artifactually high levels of 99mTc pertechnetate impurity. When analysing 99mTc Medronate, erroneously high levels of colloidal and 99mTc pertechnetate impurities were measured with 1CHR and 4CHR. Conclusions: 54SFC paper is a suitable alternative to ITLC‐SG for measuring radiochemical impurities in 99mTc Medronate. The sample spot should be wet when the paper strip is placed in the chromatography tank. Copyright © 2009 John Wiley & Sons, Ltd.
Differing in vitro survival dependency of mouse and rat NG2+ oligodendroglial progenitor cells
Authors: Horiuchi Makoto , Lindsten Tullia , Pleasure David , Itoh Takayuki 
Published: November 2009

AbstractNG2 chondroitin sulfate proteoglycan is a surface marker of oligodendroglial progenitor cells (OPCs) in various species. In contrast to well‐studied rat OPCs, however, we found that purified mouse NG2 surface positive cells (NG2+ cells) require additional activation of cyclic AMP (cAMP) signaling for survival in a medium containing 30% B104 neuroblastoma conditioned medium supplemented with fibroblast growth factor‐2 (B104CM+FGF2), whereas B104CM+FGF2 alone is sufficient for survival and selective proliferation of rat OPCs. After induction of in vitro differentiation, more than 90% of mouse NG2+ cells became O4‐positive, and a majority expressed myelin basic protein by 5 day of differentiation, which confirmed the identity of isolated mouse NG2+ cells as OPCs. In comparison to rat OPCs, mouse OPCs in B104CM+FGF2 were less motile, and demonstrated lower basal phosphorylation levels of ERK1/2 and cAMP response element‐binding protein (CREB) and a higher incidence of apoptosis mediated by the intrinsic pathway. Transient up‐regulation of cAMP‐CREB signaling partially inhibited apoptosis of mouse OPCs independently of the ERK pathway. This study demonstrates a difference in trophic requirements between mouse and rat OPCs, with an essential role for cAMP signaling to preserve viability of mouse OPCs. © 2009 Wiley‐Liss, Inc.
Description of distributed features of the nestin‐containing cells in brains of adult mice: A potential source of neural precursor cells
Authors: Xu Renshi , Wu Chengsi , Tao Yuhui , Yi Juan , Yang Yunzhu , Yang Rongwei , Zhang Xiong , Zhang Yuhu , Liu Rugao 
Published: November 2009

AbstractThe distribution of neural precursor cells (NPCs) in adult mice brain has so far not been described. Therefore, we investigated the distribution of NPCs by analyzing the nestin‐containing cells (NCCs) in distinct brain regions of adult nestin second‐intron enhancer‐controlled LacZ reporter transgenic mice through LacZ staining. Results showed that NCCs existed in various regions of adult mouse brain. In cerebellum, the greatest number of NCCs existed in cortex of the simple lobule, followed by cortex of the cerebellar lobule. In olfactory bulb, NCCs were most numerous in the granular cell layer, followed by the mitral cell layer and the internal plexiform, glomerular, and external plexiform layers. In brain nuclei (nu), NCCs were most numerous in the marginal nu, followed by the brainstem and diencephalon nu. NCCs in sensory nu of brainstem were more numerous than in motor nu, and NCCs in the dorsal of sensory nu were more numerous than in the ventral part. In brain ventricle systems, NCCs were largely distributed in the center of and external to the lateral ventricle, the inferior part of the third ventricle, the dorsal and inferior parts of the fourth ventricle, and the gray matter around the cerebral aqueduct. NCCs in the left vs. right brain were not significantly different. These data collectively indicate that NCCs were extensively distributed in the cerebellum and olfactory bulb, the partial nu of the marginal system, the partial brain nu adjacent to brain ventricle systems, the subependymal zone, and the cerebral cortex around the marginal lobe and were a potential source of NPCs. © 2009 Wiley‐Liss, Inc.
CCAAT/enhancer binding protein delta in microglial activation
Authors: Ejarque‐Ortiz Aroa , Gresa‐Arribas Núria , Straccia Marco , Mancera Pilar , Solà Carme , Tusell Josep Maria , Serratosa Joan , Saura Josep 
Published: November 2009

AbstractThe transcription factor CCAAT/enhancer binding protein δ (C/EBPδ) regulates transcription of genes that play important roles in glial activation. Previous studies have shown the astroglial expression of C/EBPδ but the microglial expression of C/EBPδ remains virtually unexplored, with the exception of two microarray studies. In this report, using murine primary cultures and BV2 cells we clearly demonstrate that C/EBPδ is expressed by microglia and it is upregulated in microglial activation. Lipopolysaccharide upregulates C/EBPδ both in microglia and in astrocytes. This effect is time‐dependent, with a maximum effect at 3 hr at mRNA level and at 4–8 hr at protein level, and concentration‐dependent, with a maximum effect at 100 ng/mL. The lipopolysaccharide‐induced C/EBPδ upregulation in BV2 microglia is mimicked by agonists of the toll‐like receptors 2, 3 and 9 and can be prevented by an inhibitor of extracellular signal‐regulated kinase activation. C/EBPδ from activated BV2 microglia binds to the cyclooxygenase‐2 promoter and forms complexes with C/EBPβ isoforms. These results point to C/EBPδ as a putative key regulator of proinflammatory gene expression in microglial activation. © 2009 Wiley‐Liss, Inc.
Low levels of citrin (SLC25A13) expression in adult mouse brain restricted to neuronal clusters
Authors: Contreras Laura , Urbieta Almudena , Kobayashi Keiko , Saheki Takeyori , Satrústegui Jorgina 
Published: November 2009

AbstractThe mitochondrial aspartate‐glutamate carriers (AGC) aralar (SLC25A12) and citrin (SLC25A13) are components of the malate aspartate shuttle (MAS), a major intracellular pathway to transfer reducing equivalents from NADH to the mitochondrial matrix. Aralar is the main AGC isoform present in the adult brain, and it is expressed mainly in neurons. To search for the other AGC isoform, citrin, in brain glial cells, we used a citrin knockout mouse in which the lacZ gene was inserted into the citrin locus as reporter gene. In agreement with the low citrin levels known to be present in the adult mouse brain, β‐galactosidase expression was very low. Surprisingly, unlike the case with astroglial cultures that express citrin, no β‐galactosidase was found in brain glial cells. It was confined to neuronal cells within discrete neuronal clusters. Double‐immunolabelling experiments showed that β‐galactosidase colocalized not with glial cell markers but with the pan‐neuronal marker NeuN. The deep cerebellar nuclei and a few midbrain nuclei (reticular tegmental pontine nuclei; magnocellular red nuclei) were the regions where β‐galactosidase expression was highest, and it was up‐regulated in fasted mice, as was also the case for liver β‐galactosidase. The results support the notion that glial cells have much lower AGC levels and MAS activity than neurons. © 2009 Wiley‐Liss, Inc.
Tau hyperphosphorylation and axonal damage induced by N,N‐diethyldithiocarbamate (DEDTC) treatment along late postnatal development is followed by a rescue during adulthood
Authors: Utrera Juana , Junyent Felix , de Lemos Luisa , Pallàs Merce , Camins Antoni , Romero Rafael , Auladell Carme 
Published: November 2009

AbstractAxonal degeneration has been described as the pathological hallmark of peripheral neuropathies induced by DEDTC. In addition, axonal damage has also been observed in the brain of mice treated daily with DEDTC along postnatal development, though with this experimental model there was observed to be axonal recovery after treatment, during the adulthood. To focus on this axonal dynamic activity, damage‐recovery, a key axonal protein, the microtubule associated protein tau, was analyzed in this DEDTC model. Tau is a phosphoprotein and its dynamic site‐specific phosphorylation is essential for its proper function; in fact, high levels are correlated with cell dysfunction. Furthermore, the levels of tau phosphorylation are associated with dynamic microtubules during periods of high plasticity. Thus, phosphorylated tau at two sites of phosphorylation, Ser199 and Ser396, were evaluated during the second week of postnatal development and throughout adulthood. The results obtained by Western blot made it evident that the levels of p‐tau Ser199 and p‐tau Ser396 were higher in treated mice than in controls. Interestingly, by immunohistochemistry there was shown to be an increase in p‐tau‐immunolabeling in neuronal soma together with axonal tract alterations in treated animals with respect to controls, and the analyses of GSK3β and cdk5 revealed an increase in its activity in DEDTC‐treated animals. Nevertheless, in the adult a general decline in p‐tau was observed together with a rescue of axonal tract. All these data support the idea that the axonal damage induced by DEDTC treatment along postnatal development is followed by an axonal rescue during adulthood. © 2009 Wiley‐Liss, Inc.
Peptides derived from the solvent‐exposed loops 3 and 4 of BDNF bind TrkB and p75NTR receptors and stimulate neurite outgrowth and survival
Authors: Fobian Kristina , Owczarek Sylwia , Budtz Christian , Bock Elisabeth , Berezin Vladimir , Pedersen Martin V. 
Published: November 2009

AbstractBrain‐derived neurotrophic factor (BDNF) is critically involved in modeling the developing nervous system and is an important regulator of a variety of crucial functions in the mature CNS. BDNF exerts its action through interactions with two transmembrane receptors, either separately or in concert. BDNF has been implicated in several neurological disorders, and irregularities in BDNF function may have severe consequences. Administration of BDNF as a drug has thus far yielded few practicable results, and the potential side effects when using a multifunctional protein are substantial. In an effort to produce more specific compounds without side effects, small peptides mimicking protein function have been developed. The present study characterized two mimetic peptides, Betrofin 3 and Betrofin 4, derived from the BDNF sequence. Both Betrofins bound the cognate BDNF receptors, TrkB and p75NTR, and induced neurite outgrowth and enhanced neuronal survival, probably by inducing signaling through tha Akt and MAPK pathways. Distinct, charged residues within the Betrofin sequences were identified as important for generating the neuritogenic response, which was also inhibited when BDNF was added together with either Betrofin, indicating partial agonistic effects of the peptides. Thus, two peptides derived from BDNF induced neurite outgrowth and enhanced neuronal survival, probably through binding to BDNF receptors. © 2009 Wiley‐Liss, Inc.
Sonic hedgehog (SHH) promotes the differentiation of mouse cochlear neural progenitors via the Math1–Brn3.1 signaling pathway in vitro
Authors: Hu Xiaohua , Huang Jianmin , Feng Ling , Fukudome Shinji , Hamajima Yuki , Lin Jizhen 
Published: November 2009

AbstractSonic hedgehog (SHH) is essential for the development of the cochlear duct that harbors the organ of Corti. However, little is known about the molecular signaling pathway through which SHH promotes the development of the organ of Corti, especially cochlear sensory epithelial cells. In this study, we demonstrated that SHH contributes to the differentiation of cochlear neural progenitors (CNPs), which are derived from the postnatal day 1 organ of Corti in mice. Addition of SHH to CNPs increased the formation of epithelial cell islands, simultaneously activated the expression of Math1 that is a transcription factor for the initial differentiation of auditory hair cells. The increased expression of Math1 then regulated the promoter activity of Brn3.1, another transcription factor that controls the further differentiation and survival of auditory hair cells. Taken together, our data suggest that SHH plays an important role in the promotion of auditory hair cell differentiation via the Math1‐Brn3.1 signaling pathway. © 2009 Wiley‐Liss, Inc.
Maternal caffeine intake during gestation and lactation down‐regulates adenosine A1receptor in rat brain from mothers and neonates
Authors: Lorenzo A.M. , León D. , Castillo C.A. , Ruiz M.A. , Albasanz J.L. , Martín M. 
Published: November 2009

AbstractEven though caffeine can be excreted in breast milk, few studies have analyzed the effect of maternal caffeine consumption during lactation on neonatal brain. In the present work pregnant rats were treated daily with 1 g/L of caffeine in their drinking water during pregnancy and/or lactation and the effect on adenosine A1receptor in brains from both lactating mothers and 15 days‐old neonates was assayed using radioligand binding and real time PCR assays. Mothers receiving caffeine during gestational period developed motor activation in gestational days 8–10 which was associated with a significant decrease of total adenosine A1receptor number (84%). A similar decrease was detected in mothers treated with caffeine during lactation (76%) and throughout gestation and lactation (73%); this was accompanied by a significant decrease in mRNA level coding adenosine A1receptor (28%). In male neonates, adenosine A1receptor was also decreased after chronic caffeine exposure during gestation (80%), lactation (76%) and gestation plus lactation (80%). In female neonates, adenosine A1receptor tended to decrease in response to caffeine exposure although no significant variations were found. No variation in the level of mRNA coding adenosine A1receptor was detected in neonates in any case. Concerning adenosine A2Areceptor, radioligand binding assays revealed that this receptor remains unaltered in maternal and neonatal brain in response to caffeine exposure. However, caffeine consumption during gestation and lactation evoked a significant decrease in mRNA level coding A2Areceptor (32%) in mothers' brain. © 2009 Wiley‐Liss, Inc.
Promoting directional axon growth from neural progenitors grafted into the injured spinal cord
Authors: Bonner Joseph F. , Blesch Armin , Neuhuber Birgit , Fischer Itzhak 
Published: November 2009

AbstractSpinal cord injury (SCI) is a devastating condition characterized by disruption of axonal connections, failure of axonal regeneration, and loss of motor and sensory function. The therapeutic promise of neural stem cells has been focused on cell replacement, but many obstacles remain in obtaining neuronal integration following transplantation into the injured CNS. This study investigated the neurotransmitter identity and axonal growth potential of neural progenitors following grafting into adult rats with a dorsal column lesion. We found that using a combination of neuronal and glial restricted progenitors (NRP and GRP) produced graft‐derived glutamatergic and GABAergic neurons within the injury site, with minimal axonal extension. Administration of brain‐derived neurotrophic factor (BDNF) with the graft promoted modest axonal growth from grafted cells. In contrast, injecting a lentiviral vector expressing BDNF rostral into the injured area generated a neurotrophin gradient and promoted directional growth of axons for up to 9 mm. Animals injected with BDNF lentivirus (at 2.5 and 5.0 mm) showed significantly more axons and significantly longer axons than control animals injected with GFP lentivirus. However, only the 5.0‐mm‐BDNF group showed a preference for extension in the rostral direction. We concluded that NRP/GRP grafts can be used to produce excitatory and inhibitory neurons, and neurotrophin gradients can guide axonal growth from graft‐derived neurons toward putative targets. Together they can serve as a building block for neuronal cell replacement of local circuits and formation of neuronal relays. © 2009 Wiley‐Liss, Inc.
Balance dysfunction resulting from acute inner ear energy failure is caused primarily by vestibular hair cell damage
Authors: Mizutari Kunio , Fujioka Masato , Nakagawa Susumu , Fujii Masato , Ogawa Kaoru , Matsunaga Tatsuo 
Published: November 2009

AbstractInner ear energy failure is associated with disorders such as inner ear ischemia. Recently, we used the mitochondrial toxin 3‐nitropropionic acid (3‐NP) to establish an animal model of inner ear energy failure that presents with auditory dysfunction. Here we investigated the mechanisms underlying balance disorders in the 3‐NP animal model. Spontaneous nystagmus peaked 6 hr after treatment with either 300 mM or 500 mM 3‐NP. The nystagmus attenuated gradually and disappeared 3 days after 3‐NP treatment. A caloric test using ice water was performed to evaluate residual vestibular function 7 days after 3‐NP treatment. The response to caloric stimulation was reduced to ∼40% of the response of the untreated ear following 300 mM 3‐NP and was undetectable following 500 mM 3‐NP. Structural changes in the peripheral vestibular organs were analyzed by light and electron microscopy. Severe loss of stereocilia was observed following 500 mM 3‐NP, whereas disorganized and mildly reduced stereocilia were observed following 300 mM 3‐NP. There was severe loss and degeneration of vestibular hair cells following 500 mM 3‐NP but only slight loss and degeneration of hair cells following 300 mM 3‐NP. These results indicate that acute inner ear energy failure causes balance dysfunction mainly by damaging hair cells in the vestibule, which is distinct from the mechanism underlying auditory disorders. © 2009 Wiley‐Liss, Inc.