bluuebunny/crossref_metadata_2025 huggingface dataset:
Potential metabolites of tricyclic neuroleptics and their fluorinated analogues; 3-Hydroxy-, 3-methoxy- and 3-fluoro-10-(4-methylpiperazino)-10,11-dihydrodibenzo[b,f]thiepin
Authors: Protiva Miroslav , Šindelář Karel , Šedivý Zdeněk , Metyšová Jiřina
Published: October 2011

4-Methoxy-2-(phenylthio)benzoic acid (V) was transformed in four steps to the homologous acid IXa which was cyclized to 3-methoxydibenzo[b,f]thiepin-10(11H)-one (Xa). The 3-methoxy derivative III of perathiepin (I) was synthesized via the intermediates XIa and XIIa, and demethylated with boron tribromide to the phenolic compound II. The analogous 3-fluoro derivative IV was synthesized from (4-fluoro-2-iodophenyl)acetic acid (XVII), the preparation of which by several procedures is described. Whereas III has only mild tranquilizing activity, II is more potent than perathiepin (I) in the tests for central depressant and cataleptic effects. The 3-fluoro derivative IV, while lacking the properties of a neuroleptic agent, is highly central depressant and this effect shows some prolongation after oral administration.
Fluorinated neuroleptics of the 10-piperazino-10,11-dihydrodibenzo[b,f]thiepin series; 6-Fluoro derivatives of perathiepin, octoclothepin, doclothepin and some related compounds
Authors: Červená Irena , Metyšová Jiřina , Bártl Václav , Protiva Miroslav
Published: October 2011

The synthesis of a series of 6-fluoro-10-piperazino-10,11-dihydrodibenzo[b,f]thiepins Ic-IIIc, Vc and VIc is described; these compounds are derivatives of the neuroleptic agents perathiepin (Ia), octoclothepin (IIIa), doclothepin (Va) and their hydroxyethyl analogues IIa and VIa in which the metabolic hydroxylation to position 6 was made impossible by blockade. The synthesis used common procedures via the intermediates VII-XVIII. Fluorination in position 6 does not influence much the pharmacological profile of the compounds indicating that hydroxylation in position 6 is only a minor metabolic pathway. The most interesting substance is the 6-fluoro derivative of octoclothepin (IIIc) which is a potent central depressant and neuroleptic agent with some protraction of the sedative effects.
The preparation and characterization of some novel fluorescence labels derived from 7-substituted 2H-1-benzopyrane-2-ones
Authors: Krejčoves Jiří , Drobník Jaroslav , Jokl Jan , Kálal Jaroslav
Published: October 2011

Novel fluorescence compounds derived from 7-substituted 2H-1-benzopyrane-2-ones (coumarins) suitable for fluorescence labelling were prepared and characterized.
Reduction of 2-, 3- and 4-quinolinecarbonitrile and 3- and 4-quinolinecarbonitrile methyl methosulfates with triethylammonium formate
Authors: Ferles Miloslav , Kocián Oldřich
Published: October 2011

Whereas 2-quinolinecarbonitrile (Ia) is not reduced with triethylammonium formate, 3-quinolinecarbonitrile (Ib) affords a mixture of 1,4-dihydro-3-quinolinecarbonitrile (IVb) and 1-formyl-1,2,3,4-tetrahydroquinoline-3-carboxamide (IIa) in addition to the corresponding acid IIb. 4-Quinolinecarbonitrile (Ic) is reduced to 1-formyl-1,2,3,4-tetrahydroquinoline-4-carbonitrile (IId) and 1-formyl-1,2,3,4-tetrahydroquinoline (IIc). Reduction of 3-quinolinecarbonitrile methyl methosulfate (Va) at low temperature leads to 1-methyl-1,4-dihydroquinoline-3-carbonitrile (IVc) whereas at higher temperatures it affords, in addition to IVc, 1-methyl-1,2,3,4-tetrahydroquinoline-3-carboxamide (IIf) and the acid IIg. 4-Quinolinecarbonitrile methyl methosulfate (Vb) gives 1-methyl-1,2,3,4-tetrahydroquinoline-4-carbonitrile (IIh) and 1-methyl-1,2,3,4-tetrahydroquinoline (IIe).
Binding of calcium ions on acid polysaccharides of peach gum and distribution pattern of carboxyl groups in the macromolecule
Authors: Kohn Rudolf , Rosík Jozef , Kubala Jozef , Malovíková Anna
Published: October 2011

The acid polysaccharide of peach gum and its macromolecular products of a gradual degradation by acid hydrolysis were characterized by molecular weight (Mw) and molar ratios of both uronic acids and neutral saccharide units. The single-ion activity coefficient of calcium ions (γCa2+) bound to these acid polysaccharides and to the corresponding aldobiouronic acids was measured and CD spectra of potassium and calcium salts of these compounds were recorded. It was ascertained that Ca2+ ions are bound to carboxyl groups of polysaccharides under study by an electrostatic bond in molecular disperse solutions. The mean distance of the neighboring carboxyl groups b = 0.83 to 1.00 nm, calculated from the measured values γCa2+ indicates a very close arrangement of uronic acid units, which does not undergo alteration with the stepwise degradation of the macromolecule. The obtained results let us conclude that the main chain of the polysaccharide is substituted in longer segments by D-glucuronic acid units and its 4-O-methyl derivative (monomeric side chains), at least at each second D-galactose unit.
The effect of inhomogeneity of the polymer structure on catalytic activity of ion exchangers
Authors: Jeřábek Karel
Published: October 2011

It has been shown that using the dependence of catalytic activity of ion exchangers on the degree of sulphonation one can infer on the structure of their polymeric skeleton. Using condensation of phenol and acetone yielding Bisphenol A as a test reaction we have been able to distinguish up to four fractions of active groups in a series of ion exchangers of the gel and macroreticular type affected to a different extent by the structure of the surrounding polymer mass.
The activity of homogeneous and heterogenized Rh(I) complexes in hydrogenation of alkenes
Authors: Kozák Zdeněk , Čapka Martin
Published: October 2011

Kinetics of liquid phase hydrogenation of alkenes catalysed by homogeneous Rh(I) complexes prepared in situ from di-μ,μ'-chloro-bis/di(cyclooctene)rhodium/ and 3-(triethoxysilyl)propyldiphenylphosphine and by heterogenised analogues anchored to silica have been studied. The reaction was found to be first order in hydrogen, alkene and catalyst. Compared to the soluble complexes, the supported catalyst turned out to be substantially more stable. At 0.3-0.6%Rh concentrations on the support, the activity of the catalyst was not affected by pore size within 4-10 nm region. The supported catalysts prepared by functionalization of the support followed by formation of the Rh complex were more active then their homogeneous analogues.
Reactions of 3-quinolinecarbonitrile and 6-quinolinecarbonitrile with methylmagnesium iodide and phenzlmagnesium bromide.
Authors: Ferles Miloslav , Jančar Pavel , Kocián Oldřich
Published: October 2011

reaction of methylmagnesium iodide with 3-quinolinecarbonitrile gave a product of the 1,4-addition (IIa), whereas that of phenylmagnesium bromide gave products of the 1,2-addition (III) and the 1,4-addition (IIb). 6-Quinolinecarbonitrile (Va) exposed to the two agents gave ketones Vb and Vd, as well as products of the 1,2-addition and the subsequent oxidation (Vc and Ve); with phenyl magnesium bromide one more product was formed, viz. ketone Vf.
Phosphites of some trivalent metals from the first transition series
Authors: Ebert Miroslav , Kavan Ladislav
Published: October 2011

The phosphites M2(HPO3)3 . 7H2O (M = V, Cr), MH3P2O6 . 3 H2O (M = V, Mn) and H3[Cr(HPO3)3 . 10 H2O were studied in the solid phase by means of the thermography, magnetochemistry, and spectroscopy (IR, EPR, electronic reflection) techniques. The EPR spectrum of V2(HPO3)3 . 7H2O at ambient temperature displays hyperfine splitting arising from the nucleus 51V. In the phosphites H3[Cr(HPO3)3] . 10H2O, MnH3P2O6 . 3H2O, and probably also VH3P2O6 . 3H2O, in contrast to the other hithero studied hydrogenphosphites, coordination of the HPO2-3 anions occurs. These anions from which the molecules of the crystal water hydrogen bonds of the energy 40kJ mol-1. The Jorgensen's parameters of the ligand in the tris(phosphito)chromate(III) anion are f = 0.95 and h = 1.50.
Herstelung und Eigenschaften der Verbindung (AsFSeO4)n
Authors: Toužín Jiří , Mitáček Lubomír
Published: October 2011

Aus den, in Abwesenheit eines Lösungsmittels von ca. äquimolaren, Arsentrifluorid und Selentrioxid enthaltenden Reaktionsgemischen scheidet sich nach einigen Tagen Abstehens bei Raumtemperatur eine feste, weiße, kristallinische Substanz mit der Zusammensetzung AsFSeO4 ab. Ihr Entstehen ist an die Bedingung des Entweichens des in der Reaktion sich bildenden Selenonyldifluorids geknüpft. Durch Verlängerung der Reaktionsdauer auf einige Wochen kann aus dem Reaktionsgemisch eine weitere Substanz von gleicher Zusammensetzung, aber mit unterschiedlichen physikalisch-chemischen Eigenschaften gewonnen werden. Aus Ramanspektren beider Verbindungen kann geschlossen werden, daß sie aus linearen Polymermolekülen gebildet sind, in deren Ketten sich mit Hilfe von Sauerstoffbrücken gegenseitig gebundene Arsen- und Selenatome abwechseln. Als Produkte der thermischen Zersetzung beider (AsFSeO4)n-Formen wurden mittels der Ramanspektroskopie Arsentrifluorid, Seleninyldifluorid, sowie Selendioxid und Arsenpentoxid identifiziert.
Reaktion von Antimon(III)-fluorid mit Schwefel- und Selentrioxid
Authors: Toužín Jiří , Mitáček Lubomír
Published: October 2011

Wie die Ramanspektren und die Zusammensetzung der Reaktionsprodukte des Antimon(III)-fluorids mit Schwefeltrioxid im Medium von flüssigem Schwefeldioxid zeigen, entstehen in Abhängigkeit vom gewählten Molverhältnis der Komponenten die Verbindungen F2SbSO3F, FSb(SO3F)3. Wie dur die Untersuchung der Reaktion des Antimon(III)-fluorids mit Selentrioxid in demselben Lösungsmittel mittels Raman- und 19F-NMR-Spektroskopie festgestellt wurde, handelt es sich bei ihren Produkten um Selenonyldifluorid und eine feste kristallische Substanz polymeren Charakters, deren Zusammensetzung durch das verwendete Molverhältnis der Komponenten determiniert wird. Als ihre Baueinheiten wurden die Anionen SeO3F- und SenO3n+12- koordinationsmäßig an die von Antimon- und Fluoratome bildenden Kationen gebunden, bei höherem Selentrioxidgehalt im Reaktionsgemisch wurden auch Sauerstoffatome identifiziert.
Optically active heptamethylenecarbodiimide
Authors: Červinka Otakar , Dudek Václav , Štíhel Zdeněk , Zikmund Jan
Published: October 2011

Heptamethylenecarbodiimide III (n = 7) and undecamethylenecarbodiimide III (n = 11) were prepared. The former was partly resolved into its optical antipodes by chromatographic treatment on a column of partially acetylated cellulose.
Preparation of 9-(β-D-ribofuranosyl)-2-hydroxypurine
Authors: Holý Antonín
Published: October 2011

Reaction of 5-aminocytosine (VI) with ethyl orthoformate afforded 2-hydroxypurine (I) which on acid-catalysed fusion with 1,2,3,5-tetra-O-acetyl-β-D-ribofuranose, followed by methanolysis, gave the 1-ribofuranosyl derivative of I (II). Reaction of the mercuric salt of I with 2,3,5-tri-O-benzoyl-D-ribofuranosyl chloride in toluene in the presence of mercuric bromide, or reaction of the monosodium salt of I with 2,3,5-tri-O-benzoyl-D-ribofuranosyl bromide in acetonitrile, afforded 9-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)-2-hydroxypurine (VII) which was methanolysed to 9-(β-D-ribofuranosyl)-2-hydroxypurine (III). The compound III was prepared also by deamination of 9-(β-D-ribofuranosyl)-2-aminopurine (X) with nitrous acid.
Complexes of germanic acid with mannitol, sorbitol, maltol and with chromotropic and kojic acids
Authors: Mikešová Milena , Bartušek Miloš
Published: October 2011

Formation of complexes of Ge(IV) with chromotropic acid (GeL8-3), with maltol and kojic acid (GeA2(OH)2 and GeA+3) and with mannitol and sorbitol (GeL2(OH)- and GeL2-3) has been studied by the method of potentiometric neutralization titration in diluted aqueous solutions. Equilibrium constants of the reactions of germanic acid with the mentioned reagents have been determined
Determination of the crystal structure of cobalt(II) orthosilicate
Authors: Kratochvíl Bohumil , Podlahová Jana , Hašek Jindřich
Published: October 2011

The crystal structure of Co2SiO4 (olivine structure type) was solved by Patterson and Fourier synthesis and refined by the full matrix least squares method. A final value of the R factor of 0.057 was obtained from 911 independent reflection intensities. The structure symmetry corresponds to space group Pnma with lattice parameters a = 1032.8(3), b = 601.9(2) and c = 478.2(1) pm. The unit cell contains four formula units. The Si-O distance in isolated SiO4 tetrahedra varies from 162.1(3) to 165.9(3) pm. Both cobalt atoms are octahedrally surrounded by oxygen atoms with Co-O distances of 208.0(3)-223.1(2) pm.
Some 6-alkyl derivatives of D-8-ergolin-I-ylacetamide
Authors: Beran Miloš , Křepelka Jiří , Semonský Miroslav
Published: October 2011

D-6-Alkyl-8-cyanomethylergolines-I were converted either by known procedures via the corresponding methyl esters I-III and hydrazides IV-VI to amides VII-IX, or by hydration of the nitrile group under the conditions of ionic pair extraction to amides VIII and X-XIII. In the same system D-6-methyl-8-ergolin-I-ylacetamide (DeprenonR) was prepared from D-6-methyl-8-cyanomethylergoline-I. Amides VII, VIII and XI had a considerably higher prolactin inhibiting activity than Deprenon.
Immbilization on cellulose in bead form after periodate oxidation and reductive alkylation
Authors: Turková Jaroslava , Vajčner Jiří , Vančurová Drahomíra , Štamberg Jiří
Published: October 2011

The covalent binding of trypsin to cellulose beads after periodate oxidation was examined. The degree of cellulose derivatives solubilization is directly related to cellulose oxidation and increases with the increasing pH of the reaction mixture. The quantity of trypsin immobilized was examined as a function of pH, reaction time, and concentration of native trypsin in the reaction mixture during the coupling reaction. The catalytic activity and the stability of the preparations of immobilized trypsin during continuous hydrolysis of low-molecular-weight and high-molecular-weight substrates was assayed.
The dimer (HCl)2: Stationary points on the SCF 4-31G energy hypersurface and the role of entropy in the dimer formation
Authors: Hobza Pavel , Čársky Petr , Zahradník Rudolf
Published: October 2011

Two stationary points have been investigated on the 4-31G SCF energy hypersurface of (HCl)2. It has been shown, in agreement with experiment, that only the quasilinear structure satisfies all criteria required for a real minimum. Small heat of reaction and the crucial role of entropy in the (HCl)2 formation suggest that the dimer (HCl)2, in contrast to (HF)2, represents a true van der Waals molecule. A very small energy difference between the two stationary points (minimum and saddle point) suggests a very high rate of interconversion between two possible structures of the quasilinear form. Common features of and differences between (HCl)2 and (HF)2 are pointed out.
The phase instability and critical point in a liquid mixture of an associating and inert component
Authors: Pouchlý Julius , Sikora Antonín
Published: October 2011

The problem of phase instability in a binary mixture of an associating component with an inert component is analyzed from the standpoint of the theory of association equilibria. It is demonstrated that conditions of the spinodal and critical point for such a binary system are equivalent to those of the spinodal and critical point of a multicomponent mixture consisting of complex species arising by association (including nonassociated molecules). These conditions are formulated so as if species in this mixture did not participate in association and dissociation processes; configurational terms expressing changes in the content of the individual complexes depending on changes in total composition are included implicitly.
Vapour-liquid equilibrium in the methyl tert-butyl ether-n-hexane and methyl tert-butyl ether-toluene systems
Authors: Plura Jiří , Matouš Jaroslav , Novák Josef P. , Šobr Josef
Published: October 2011

Vapour-liquid equilibrium data in binary methyl tert-butyl ether-n-hexane and methyl tert-butyl ether-toluene mixtures were determined experimentally. The data were described thermodynamically by the one-constant Redlich-Kister equation.
The electronic effects in and the oxygen basicity of some oxygen-containing boranes
Authors: Pola Josef , Jakoubková Marie , Chvalovský Václav
Published: October 2011

The oxygen relative basicity of di-n-butylboronous anhydride ((n-C4H9)2B)2O, ethyl di-n-butylboronite (n-C4H9)2BOC2H5 and some orthoborates (RO)3B having electrondonating and electronwithdrawing groups R was measured from the IR spectra of hydrogen bonds of phenol interacting with these compounds in CCl4 and analysed by means of the Taft equation. The substituent electronic effect of (n-C4H9)2B- and (RO)2B-groups attached to the oxygen of the-OR and -OB= moieties has been estimated asa more electronwithdrawing than that of structurally alike R2Z- and (RO)2Z-groups having Z = CH and SiCH3 and is discussed in terms of the vacant 2p orbital of the boron and a weak, if any, mutual polarizability effect of the alkoxy groups in orthoborates. The trimethylsiloxy group in trimethylsilyl borate possesses reduced electronwithdrawing ability compared to that in ((CH3)3SiO)3SiCH3 as a consequence of its great polarizability.
Catalytic activity of cupric oxide in addition reactions of alkyl cyanoacetates with 1-alkenes
Authors: Hájek Milan , Málek Jaroslav
Published: October 2011

In the presence of cupric oxide as the catalyst, ethyl cyanoacetate reacts with 1-alkenes to form 1 : 1 adducts in high yields. The active catalytic component was found to be a soluble copper species generated in the absence of oxygen in 10-3 to 10-5 M concentrations by a partial dissolution of cupric oxide in ethyl cyanoacetate. The homogeneous catalytic reaction proceeds already at temperatures about 80 °C at a fast rate and with high selectivity. Results of inhibition experiments in the presence of α-naphthol and galvinoxyl support strongly the view on a free-radical mechanism of the addition reaction.
Multi-component synthesis of 2-amino-4H-chromenes catalyzed by nano ZnO in water
Authors: Hosseini-Sarvari Mona , Shafiei-Haghighi Sara
Published: October 2011

Naphthalenediols, 1- and 2-naphthols, and phenols in the presence of nano ZnO as catalyst and water as green solvent react with methylenemalononitrile, generated in situ from aldehyde and malononitrile, to yield 2-amino-4H-chromenes.
An efficient synthesis of 4-arylquinolin-2(1H)-ones and 3-alkenyl-4-arylquinolin-2(1H)-one using a Pd/NiFe2O4-catalyzed consecutive Heck reaction
Authors: Borhade Sanjay R. , Waghmode Suresh B.
Published: October 2011

A convenient one-pot method for the synthesis of 4-arylquinolin-2(1H)-ones and 4-arylcoumarins has been described. The successive Heck reaction on substituted 2-iodoaniline and 2-iodophenol catalyzed by a Pd/nickel ferrite catalyst followed by in situ cyclization was the key step. The scope of this methodology was extended to the synthesis of bioactive 3-alkenyl derivatives of 4-arylquinolin-2(1H)-ones.
Theoretical investigation of experimentally determined α-εffects — The role of electronics
Authors: Afzal D. , Fountain K.R.
Published: October 2011

Recent experimental reports involving both α-nucleophiles and normal nucleophiles have reported both the presence and absence of an α-effect. In ester systems, such as dimethylmethylphosphonate (DMMP), a small α-effect is reported, but the reference point is a stationary point of the potential energy surface that must rearrange to acquire the near attack conformation (NAC) necessary for the Sn2 pathway to proceed. The second type of study involves use of highly fluorinated alkoxides as normal nucleophiles and reports no α-effect. This paper employs linear free energy plots in an investigation of electronic effects in methyl formate SN2 reactions, using high-level computations of transition states for determination of energy barriers.
Primate-Inspired Communication Methods for Mobile and Static Sensors and RFID Tags
Authors: Xiao Yang , Zhang Yanping , Liang Xiannuan
Published: October 2011

Although previous bio-inspired models have concentrated on invertebrates, such as ants, mammals, such as primates with higher cognitive function, are valuable for modeling the increasingly complex problems in engineering. Understanding primates’ social and communication systems and applying what is learned from them to engineering domains will likely lead to solutions to a number of problems. Scent-marking is an important behavior among primates and many other mammals. In this article, inspired by primates’ scent-marking activity, we propose and study a collaboration strategy for mobile and static sensors with RFID tags, where mobile sensors can be treated as robots or mobile actuators and can leave information to direct others to find them. Mobile sensors are equipped with RFID tags (or sensors) that can be deployed whenever needed, and RFID tags (or sensors) carry related information for other robots to pick up. We propose several primate-inspired communication mechanisms, including delayed-and-relayed and scent-trail communication among robots. We analytically model and simulate scent-trail communication. We also study a tracking and pursuing scheme of mobile sensors using simulations in terms of robot speeds, searching function, deployment density, turning function, and so on. We assume that robots (mobile sensors or mobile actuators) are capable of deploying/throwing-out sensors/RFID tags.
Circulating GLP-1 and CCK-8 reduce food intake by capsaicin-insensitive, nonvagal mechanisms
Authors: Zhang Jingchuan , Ritter Robert C.
Published: October 2011

Previous reports suggest that glucagon-like peptide (GLP-1), a peptide secreted from the distal small intestine, is an endocrine satiation signal. Nevertheless, there are conflicting reports regarding the site where circulating GLP-1 acts to reduce food intake. To test the hypothesis that vagal afferents are necessary for reduction of food intake by circulating GLP-1, we measured intake of 15% sucrose during intravenous GLP-1 infusion in intact, vagotomized, and capsaicin-treated rats. We also measured sucrose intake during intravenous infusion of cholecystokinin, a peptide known to reduce food intake via abdominal vagal afferents. We found that reduction of intake by GLP-1 was not diminished by capsaicin treatment or vagotomy. In fact, reduction of sucrose intake by our highest GLP-1 dose was enhanced in vagotomized and capsaicin-treated rats. Intravenous GLP-1 induced comparable increases of hindbrain c-Fos immunoreactivity in intact, capsaicin-treated, and vagotomized rats. Plasma concentrations of active GLP-1 in capsaicin-treated rats did not differ from those of controls during the intravenous infusions. Finally, capsaicin treatment was not associated with altered GLP-1R mRNA in the brain, but nodose ganglia GLP-1R mRNA was significantly reduced in capsaicin-treated rats. Although reduction of food intake by intraperitoneal cholecystokinin was abolished in vagotomized and capsaicin-treated rats, reduction of intake by intravenous cholecystokinin was only partially attenuated. These results indicate that vagal or capsaicin-sensitive neurons are not necessary for reduction of food intake by circulating (endocrine) GLP-1, or cholecystokinin. Vagal participation in satiation by these peptides may be limited to paracrine effects exerted near the sites of their secretion.
Transpulmonary lactate shuttle
Authors: Johnson Matthew L. , Emhoff Chi-An W. , Horning Michael A. , Brooks George A.
Published: October 2011

The shuttling of intermediary metabolites such as lactate through the vasculature contributes to the dynamic energy and biosynthetic needs of tissues. Tracer kinetic studies offer a powerful tool to measure the metabolism of substrates like lactate that are simultaneously taken up from and released into the circulation by organs, but in each circulatory passage, the entire cardiac output traverses the pulmonary parenchyma. To determine whether transpulmonary lactate shuttling affects whole-body lactate kinetics in vivo, we examined the effects of a lactate load (via lactate clamp, LC) and epinephrine (Epi) stimulation on transpulmonary lactate kinetics in an anesthetized rat model using a primed-continuous infusion of [U-13C]lactate. Under all conditions studied, control 1.2 (SD 0.7) (Con), LC 1.9 (SD 2.5), and Epi 1.9 (SD 3.5) mg/min net transpulmonary lactate uptake occurred. Compared with Con, a lactate load via LC significantly increased mixed central venous ([v̄]) [1.9 mM (SD 0.5) vs. 4.7 (SD 0.4)] and arterial ([a]) [1.6 mM (SD 0.4) vs. 4.1 (SD 0.6)] lactate concentrations ( P < 0.05). Transpulmonary lactate gradient ([v̄] − [a]) was highest during the lactate clamp condition [0.6 mM (SD 0.7)] and lowest during Epi [0.2 mM (SD 0.5)] stimulation ( P < 0.05). Tracer measured lactate fractional extractions were similar for control, 16.6% (SD 15.3), and lactate clamp, 8.2% (SD 15.3) conditions, but negative during Epi stimulation, −25.3% (SD 45.5) when there occurred a transpulmonary production, the conversion of mixed central venous pyruvate to arterial lactate. Further, isotopic equilibration between L and P occurred following tracer lactate infusion, but depending on compartment (v̄ or a) and physiological stimulus, [L]/[P] concentration and isotopic enrichment ratios ranged widely. We conclude that pulmonary arterial-vein concentration difference measurements across the lungs provide an incomplete, and perhaps misleading picture of parenchymal lactate metabolism, especially during epinephrine stimulation.
Curcumin and enalapril ameliorate renal failure by antagonizing inflammation in ⅚ nephrectomized rats: role of phospholipase and cyclooxygenase
Authors: Ghosh S. S. , Krieg R. , Massey H. D. , Sica D. A. , Fakhry I. , Ghosh S. , Gehr T. W. B.
Published: October 2011

Previously, we showed that curcumin prevents chronic kidney disease (CKD) development in ⅚ nephrectomized (Nx) rats when given within 1 wk after Nx (Ghosh SS, Massey HD, Krieg R, Fazelbhoy ZA, Ghosh S, Sica DA, Fakhry I, Gehr TW. Am J Physiol Renal Physiol 296: F1146–F1157, 2009). To better mimic the scenario for renal disease in humans, we began curcumin and enalapril therapy when proteinuria was already established. We hypothesized that curcumin, by blocking the inflammatory mediators TNF-α and IL-1β, could also reduce cyclooxygenase (COX) and phospholipase expression in the kidney. Nx animals were divided into untreated Nx, curcumin-treated, and enalapril-treated groups. Curcumin (75 mg/kg) and enalapril (10 mg/kg) were administered for 10 wk. Renal dysfunction in the Nx group, as evidenced by elevated blood urea nitrogen, plasma creatinine, proteinuria, segmental sclerosis, and tubular dilatation, was comparably reduced by curcumin and enalapril, with only enalapril significantly lowering blood pressure. Compared with controls, Nx animals had higher plasma/kidney TNF-α and IL-1β, which were reduced by curcumin and enalapril treatment. Nx animals had significantly elevated kidney levels of cytosolic PLA2, calcium-independent intracellular PLA2, COX 1, and COX 2, which were comparably reduced by curcumin and enalapril. Studies in mesangial cells and macrophages were carried out to establish that the in vivo increase in PLA2and COX were mediated by TNF-α and IL-1β and that curcumin, by antagonizing the cytokines, could significantly reduce both PLA2and COX. We conclude that curcumin ameliorates CKD by blocking inflammatory signals even if it is given at a later stage of the disease.
Two hands, one perception: how bimanual haptic information is combined by the brain
Authors: Squeri Valentina , Sciutti Alessandra , Gori Monica , Masia Lorenzo , Sandini Giulio , Konczak Juergen
Published: October 2011

Humans routinely use both of their hands to gather information about shape and texture of objects. Yet, the mechanisms of how the brain combines haptic information from the two hands to achieve a unified percept are unclear. This study systematically measured the haptic precision of humans exploring a virtual curved object contour with one or both hands to understand if the brain integrates haptic information from the two hemispheres. Bayesian perception theory predicts that redundant information from both hands should improve haptic estimates. Thus exploring an object with two hands should yield haptic precision that is superior to unimanual exploration. A bimanual robotic manipulandum passively moved the hands of 20 blindfolded, right-handed adult participants along virtual curved contours. Subjects indicated which contour was more “curved” (forced choice) between two stimuli of different curvature. Contours were explored uni- or bimanually at two orientations (toward or away from the body midline). Respective psychophysical discrimination thresholds were computed. First, subjects showed a tendency for one hand to be more sensitive than the other with most of the subjects exhibiting a left-hand bias. Second, bimanual thresholds were mostly within the range of the corresponding unimanual thresholds and were not predicted by a maximum-likelihood estimation (MLE) model. Third, bimanual curvature perception tended to be biased toward the motorically dominant hand, not toward the haptically more sensitive left hand. Two-handed exploration did not necessarily improve haptic sensitivity. We found no evidence that haptic information from both hands is integrated using a MLE mechanism. Rather, results are indicative of a process of “sensory selection”, where information from the dominant right hand is used, although the left, nondominant hand may yield more precise haptic estimates.
Phasic basal ganglia activity associated with high-gamma oscillation during sleep in a songbird
Authors: Yanagihara Shin , Hessler Neal A.
Published: October 2011

The basal ganglia is thought to be critical for motor control and learning in mammals. In specific basal ganglia regions, gamma frequency oscillations occur during various behavioral states, including sleeping periods. Given the critical role of sleep in regulating vocal plasticity of songbirds, we examined the presence of such oscillations in the basal ganglia. In the song system nucleus Area X, epochs of high-gamma frequency (80–160 Hz) oscillation of local field potential during sleep were associated with phasic increases of neural activity. While birds were awake, activity of the same neurons increased specifically when birds were singing. Furthermore, during sleep there was a clear tendency for phase locking of spikes to these oscillations. Such patterned activity in the sleeping songbird basal ganglia could play a role in off-line processing of song system motor networks.
Immunomodulatory Effects of Anesthetics during Thoracic Surgery
Authors: Mahmoud Khaled , Ammar Amany
Published: October 2011

Background. One-lung ventilation (OLV) during thoracic surgery may induce alveolar cell damage and release of proinflammatory mediators. The current trial was planned to evaluate effect of propofol versus isoflurane anesthesia on alveolar and systemic immune modulation during thoracic surgery.Methods. Fifty adult patients undergoing open thoracic surgery were randomly assigned to receive propofol or isoflurane anesthesia. The primary outcome measures included alveolar and plasma concentrations of interleukin-8(IL-8) and tumour necrosis factor-α(TNF-α), whereas secondary outcome measures were alveolar and plasma concentrations of malondialdehyde (MDA), superoxide dismutase (SOD), and changes in alveolar albumin concentrations and cell numbers.Results. Alveolar and plasma concentrations of IL-8 and TNF-αwere significantly lower in the isoflurane group, whereas alveolar and plasma concentrations of MDA were significantly lower in the propofol group. Alveolar and plasma SOD levels increased significantly in the propofol group whereas they showed no significant change in the isoflurane group. Furthermore, the isoflurane group patients developed significantly lower alveolar albumin concentrations and cell numbers.Conclusion. Isoflurane decreased the inflammatory response associated with OLV during thoracic surgery and may be preferable over propofol in patients with expected high levels of proinflammatory cytokines like cancer patients.
Carbon Nanostructures Production by AC Arc Discharge Plasma Process at Atmospheric Pressure
Authors: Zhao Shenqiang , Hong Ruoyu , Luo Zhi , Lu Haifeng , Yan Biao
Published: October 2011

Carbon nanostructures have received much attention for a wide range of applications. In this paper, we produced carbon nanostructures by decomposition of benzene using AC arc discharge plasma process at atmospheric pressure. Discharge was carried out at a voltage of 380 V, with a current of 6 A–20 A. The products were characterized by scanning electron microscopy (SEM), high-resolution transmission electron microscopy (HRTEM), powder X-ray diffraction (XRD), and Raman spectra. The results show that the products on the inner wall of the reactor and the sand core are nanoparticles with 20–60 nm diameter, and the products on the electrode ends are nanoparticles, agglomerate carbon particles, and multiwalled carbon nanotubes (MWCNTs). The maximum yield content of carbon nanotubes occurs when the arc discharge current is 8 A. Finally, the reaction mechanism was discussed.
T Cells as Vehicles for Cancer Vaccination
Authors: Bear Adham S. , Cruz Conrad R. , Foster Aaron E.
Published: October 2011

The success of cancer vaccines is dependent on the delivery of tumor‐associated antigens (TAAs) within lymphoid tissue in the context of costimulatory molecules and immune stimulatory cytokines. Dendritic cells (DCs) are commonly utilized to elicit antitumor immune responses due to their attractive costimulatory molecule and cytokine expression profile. However, the efficacy of DC‐based vaccines is limited by the poor viability and lymph‐node migration of exogenously generated DCs in vivo. Alternatively, adoptively transferred T cells persist for long periods of time in vivo and readily migrate between the lymphoid and vascular compartments. In addition, T cells may be genetically modified to express both TAA and DC‐activating molecules, suggesting that T cells may be ideal candidates to serve as cellular vehicles for antigen delivery to lymph node‐resident DCs in vivo. This paper discusses the concept of using T cells to induce tumor‐specific immunity for vaccination against cancer.
Exercise Interventions in Children with Cancer: A Review
Authors: Huang Tseng-Tien , Ness Kirsten K.
Published: October 2011

The purpose of this review is to summarize literature that describes the impact of exercise on health and physical function among children during and after treatment for cancer. Relevant studies were identified by entering the following search terms into Pubmed: aerobic training; resistance training; stretching; pediatric; children; AND cancer. Reference lists in retrieved manuscripts were also reviewed to identify additional trials. We include fifteen intervention trials published between 1993 and 2011 that included children younger than age 21 years with cancer diagnoses. Nine included children with an acute lymphoblastic leukemia (ALL) diagnosis, and six children with mixed cancer diagnoses. Generally, interventions tested were either in-hospital supervised exercise training or home based programs designed to promote physical activity. Early evidence from small studies indicates that the effects of exercise include increased cardiopulmonary fitness, improved muscle strength and flexibility, reduced fatigue and improved physical function. Generalizations to the entire childhood cancer and childhood cancer survivor populations are difficult as most of the work has been done in children during treatment for and among survivors of ALL. Additional randomized studies are needed to confirm these benefits in larger populations of children with ALL, and in populations with cancer diagnoses other than ALL.
Observer‐Based Vaccination Strategy for a True Mass Action SEIR Epidemic Model with Potential Estimation of All the Populations
Authors: De la Sen M. , Ibeas A. , Alonso-Quesada S.
Published: October 2011

This paper presents a simple continuous‐time linear vaccination‐based control strategy for a SEIR (susceptible plus infected plus infectious plus removed populations) propagation disease model. The model takes into account the total population amounts as a refrain for the illness transmission since its increase makes more difficult contacts among the susceptible and infected. The control objective is the asymptotically tracking of the removed‐by‐immunity population to the total population while achieving simultaneously the remaining population (i.e., susceptible plus infected plus infectious) to asymptotically converge to zero. A state observer is used to estimate the true various partial populations of the susceptible, infected, infectious, and immune which are assumed to be unknown. The model parameters are also assumed to be, in general, unknown. In this case, the parameters are replaced by available estimates to implement the vaccination action.
Chloroform Extract of Rasagenthi Mezhugu, a Siddha Formulation, as an Evidence-Based Complementary and Alternative Medicine for HPV-Positive Cervical Cancers
Authors: Riyasdeen Anvarbatcha , Periasamy Vaiyapuri S. , Paul Preethy , Alshatwi Ali A. , Akbarsha Mohammad A.
Published: October 2011

Rasagenthi Mezhugu (RGM) is a herbomineral formulation in the Siddha system of traditional medicine and is prescribed in the southern parts of India as a remedy for all kinds of cancers. However, scientific evidence for its therapeutic efficacy in cervical cancer is lacking, and it contains heavy metals. To overcome these limitations, RGM was extracted, and the fractions were tested on HPV-positive cervical cancer cells, ME-180 and SiHa. The extracts, free from the toxic heavy metals, affected the viability of both the cells. The chloroform fraction (cRGM) induced DNA damage and apoptosis. Mitochondria-mediated apoptosis was indicated. Though both the cells responded to the treatment, ME-180 was more responsive. Thus, this study brings up scientific evidence for the efficacy of RGM against the HPV-mediated cervical cancer cells and, if the toxic heavy metals are the limitation in its use, cRGM would be a suitable candidate as evidence-based complementary and alternative medicine for HPV-positive cervical cancers.
Effects of Exposure to Semiconductor Nanoparticles on Aquatic Organisms
Authors: Leigh Kenton , Bouldin Jennifer , Buchanan Roger
Published: October 2011

Because of their unique physical, optical, and mechanical properties, nanomaterials hold great promise in improving on a wide variety of current technologies. Consequently, their use in research and consumer products is increasing rapidly, and contamination of the environment with various nanomaterials seems inevitable. Because surface waters receive pollutants and contaminants from many sources including nanoparticles and act as reservoirs and conduits for many environmental contaminants, understanding the potential impacts of nanoparticles on the organisms within these environments is critical to evaluating their potential toxicity. While there is much to be learned about interactions between nanomaterials and aquatic systems, there have been a number of recent reports of interactions of quantum dots (QDs) with aquatic environments and aquatic organisms. This review is focused on providing a summary of recent work investigating the impacts of quantum dots on aquatic organisms.
Antimicrobial Activity of Single-Walled Carbon Nanotubes Suspended in Different Surfactants
Authors: Dong Lifeng , Henderson Alex , Field Christopher
Published: October 2011

We investigated the antibacterial activity of single-walled carbon nanotubes (SWCNTs) dispersed in surfactant solutions of sodium cholate, sodium dodecylbenzene sulfonate, and sodium dodecyl sulfate. Among the three surfactants, sodium cholate demonstrated the weakest antibacterial activity againstSalmonella enterica,Escherichia coli, andEnterococcus faeciumand thereby was used to disperse bundled SWCNTs in order to study nanotube antibiotic activity. SWCNTs exhibited antibacterial characteristics for bothS. entericaandE. coli. With the increase of nanotube concentrations from 0.3 mg/mL to 1.5 mg/mL, the growth curves had plateaus at lower absorbance values whereas the absorbance value was not obviously affected by the incubation ranging from 5 min to 2 h. Our findings indicate that carbon nanotubes could become an effective alternative to antibiotics in dealing with drug-resistant and multidrug-resistant bacterial strains because of the physical mode of bactericidal action that SWCNTs display.
Immune-Regulatory Mechanisms in Systemic Autoimmune and Rheumatic Diseases
Authors: Takakubo Yuya , Konttinen Yrjö T.
Published: October 2011

Systemic autoimmune and rheumatic diseases (SAIRDs) are thought to develop due to the failure of autoimmune regulation and tolerance. Current therapies, such as biologics, have improved the clinical results of SAIRDs; however, they are not curative treatments. Recently, new discoveries have been made in immune tolerance and inflammation, such as tolerogenic dendritic cells, regulatory T and B cells, Th 17 cells, inflammatory and tolerogenic cytokines, and intracellular signaling pathways. They lay the foundation for the next generation of the therapies beyond the currently used biologic therapies. New drugs should target the core processes involved in disease mechanisms with the aim to attain complete cure combined with safety and low costs compared to the biologic agents. Re-establishment of autoimmune regulation and tolerance in SAIRDs by the end of the current decade should be the final and realistic target.
Molecular Pathways: Osteoclast-Dependent and Osteoclast-Independent Roles of the RANKL/RANK/OPG Pathway in Tumorigenesis and Metastasis
Authors: Dougall William C.
Published: October 2011

Receptor activator of nuclear factor-kappa B ligand (RANKL) is a TNF ligand superfamily member that is essential for the formation, activation, and function of osteoclasts. RANKL functions via its cognate receptor RANK, and it is inhibited by the soluble decoy receptor osteoprotegerin (OPG). In skeletal metastases, the ratio of RANKL to OPG is upregulated, which leads to increased osteoclast-mediated bone destruction. These changes in the bone microenvironment not only compromise the structural integrity of bone, leading to severe clinical morbidities, but have also been implicated in establishment of de novo bone metastasis and the progression of existing skeletal tumors. Evaluation of RANKL inhibitors, including the fully human anti-RANKL antibody denosumab, in patients with cancer has shown reductions in tumor-induced bone resorption activity and successful management of skeletal complications of bone metastases. RANKL also functions as a major paracrine effector of the mitogenic action of progesterone in mouse mammary epithelium, and it has a role in ovarian hormone-dependent expansion and regenerative potential of mammary stem cells. RANKL inhibition attenuates mammary tumorigenesis and pulmonary metastases in mouse models. These data suggest that the contribution of progesterone to increased mammary cancer incidence is mediated, at least in part, by RANKL-dependent changes in the mammary epithelium; RANKL also directly promotes distant metastases. In summary, the antitumor and antimetastatic effects of RANKL inhibition can occur by at least 2 distinct mechanisms, one in the bone via osteoclast-dependent effects, and the second via direct effects on the tumor cells of various origins and/or mammary epithelium. Clin Cancer Res; 18(2); 326–35. ©2011 AACR.
Curcumin Induces the Differentiation of Myeloid-Derived Suppressor Cells and Inhibits Their Interaction with Cancer Cells and Related Tumor Growth
Authors: Tu Shui Ping , Jin Huanyu , Shi Jin Dong , Zhu Li Ming , Suo Ya , Lu Gang , Liu Anna , Wang Timothy C. , Yang Chung S.
Published: October 2011

Myeloid-derived suppressor cells (MDSC) accumulate in the spleen and tumors and contribute to tumor growth, angiogenesis, and progression. In this study, we examined the effects of curcumin on the activation and differentiation of MDSCs, their interaction with human cancer cells, and related tumor growth. Treatment with curcumin in the diet or by intraperitoneal injection significantly inhibited tumorigenicity and tumor growth, decreased the percentages of MDSCs in the spleen, blood, and tumor tissues, reduced interleukin (IL)-6 levels in the serum and tumor tissues in a human gastric cancer xenograft model and a mouse colon cancer allograft model. Curcumin treatment significantly inhibited cell proliferation and colony formation of cancer cells and decreased the secretion of murine IL-6 by MDSCs in a coculture system. Curcumin treatment inhibited the expansion of MDSCs, the activation of Stat3 and NF-κB in MDSCs, and the secretion of IL-6 by MDSCs, when MDSCs were cultured in the presence of IL-1β, or with cancer cell- or myofibroblast-conditioned medium. Furthermore, curcumin treatment polarized MDSCs toward a M1-like phenotype with an increased expression of CCR7 and decreased expression of dectin 1 in vivo and in vitro. Our results show that curcumin inhibits the accumulation of MDSCs and their interaction with cancer cells and induces the differentiation of MDSCs. The induction of MDSC differentiation and inhibition of the interaction of MDSCs with cancer cells are potential strategies for cancer prevention and therapy. Cancer Prev Res; 5(2); 205–15. ©2011 AACR.
Molecular Imaging for Stem Cell Transplantation in Neuroregenerative Medicine
Authors: Sandu Nora , Momen-Heravi Fatemeh , Sadr-Eshkevari Pooyan , Schaller Bernhard
Published: October 2011

Stem cell transplantation is a promising new therapeutic option in different neurological diseases. However, it was not yet possible to translate its potential from animal models to clinical application. One of the main problems of applying stem cell transplantation in clinical medium is the difficulty of detection, localization, and examination of the stem cells in vivo at both cellular and molecular levels. State-of-the-art molecular imaging techniques provide new and better means for noninvasive, repeated, and quantitative tracking of stem cell implant or transplant. From initial deposition to the survival, migration, and differentiation of the transplant/implanted stem cells, current molecular imaging methods allow monitoring of the infused cells in the same live recipient over time. The present review briefly summarizes and compares these molecular imaging methods for cell labeling and imaging in animal models as well as in clinical application and sheds light on consecutive new therapeutic options if appropriate.
Difficulty in Inserting 25- and 23-Gauge Trocar Cannula during Vitrectomy
Authors: Kunikata Hiroshi , Nitta Fumihiko , Meguro Yasuhiko , Aizawa Naoko , Hariya Takehiro , Chiba Naoki , Abe Toshiaki , Nishida Kohji
Published: October 2011

Purpose: To determine the incidence of difficulty in inserting a 25- and 23-gauge trocar cannula (DITC) during 25- or 23-gauge micro-incision vitrectomy surgery (MIVS). Methods: Retrospective, consecutive, interventional case series performed by a single surgeon at a single centre. We defined a DITC as the condition where at least 1 trocar cannula could not be inserted into the vitreous at the beginning of MIVS. The incidence of DITC was calculated from 1,525 eyes, and the pre-operative demographics of the DITC cases were compared to those of the non-DITC cases. Results: The incidence of DITC for all cases was 0.6% (9 of 1,525 eyes). Overall, there were 242 eyes with a retinal detachment (RD), and 8 of the 9 eyes with DITC had an RD with an incidence of 3.3% (8 of 242 RD eyes). Seven of these 8 eyes had a total RD, 4 also had a choroidal detachment, 4 eyes were also myopic (>–8.0 dpt, high myopia), and 6 of the 8 eyes were hypotonic (<8 mm Hg). The DITC cases had larger RDs (p < 0.0001), a higher incidence of choroidal detachment (p < 0.0001), higher myopia (p = 0.0204) and hypotony (p = 0.0003) than the non-DITC eyes with an RD. Conclusions: A large RD, a choroidal detachment, high myopia and hypotony are significant risk factors for DITC. We recommend that MIVS should be performed cautiously for eyes with these risk factors.