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Sample records for active urea transport

  1. Active urea transport in lower vertebrates and mammals.

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    Bankir, Lise

    2014-01-01

    Some unicellular organisms can take up urea from the surrounding fluids by an uphill pumping mechanism. Several active (energy-dependent) urea transporters (AUTs) have been cloned in these organisms. Functional studies show that active urea transport also occurs in elasmobranchs, amphibians, and mammals. In the two former groups, active urea transport may serve to conserve urea in body fluids in order to balance external high ambient osmolarity or prevent desiccation. In mammals, active urea transport may be associated with the need to either store and/or reuse nitrogen in the case of low nitrogen supply, or to excrete nitrogen efficiently in the case of excess nitrogen intake. There are probably two different families of AUTs, one with a high capacity able to establish only a relatively modest transepithelial concentration difference (renal tubule of some frogs, pars recta of the mammalian kidney, early inner medullary collecting duct in some mammals eating protein-poor diets) and others with a low capacity but able to maintain a high transepithelial concentration difference that has been created by another mechanism or in another organ (elasmobranch gills, ventral skin of some toads, and maybe mammalian urinary bladder). Functional characterization of these transporters shows that some are coupled to sodium (symports or antiports) while others are sodium-independent. In humans, only one genetic anomaly, with a mild phenotype (familial azotemia), is suspected to concern one of these transporters. In spite of abundant functional evidence for such transporters in higher organisms, none have been molecularly identified yet.

  2. Brucella abortus ure2 region contains an acid-activated urea transporter and a nickel transport system

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    García-Lobo Juan M

    2010-04-01

    Full Text Available Abstract Background Urease is a virulence factor that plays a role in the resistance of Brucella to low pH conditions, both in vivo and in vitro. Brucella contains two separate urease gene clusters, ure1 and ure2. Although only ure1 codes for an active urease, ure2 is also transcribed, but its contribution to Brucella biology is unknown. Results Re-examination of the ure2 locus showed that the operon includes five genes downstream of ureABCEFGDT that are orthologs to a nikKMLQO cluster encoding an ECF-type transport system for nickel. ureT and nikO mutants were constructed and analyzed for urease activity and acid resistance. A non-polar ureT mutant was unaffected in urease activity at neutral pH but showed a significantly decreased activity at acidic pH. It also showed a decreased survival rate to pH 2 at low concentration of urea when compared to the wild type. The nikO mutant had decreased urease activity and acid resistance at all urea concentrations tested, and this phenotype could be reverted by the addition of nickel to the growth medium. Conclusions Based on these results, we concluded that the operon ure2 codes for an acid-activated urea transporter and a nickel transporter necessary for the maximal activity of the urease whose structural subunits are encoded exclusively by the genes in the ure1 operon.

  3. Modulation of kidney urea transporter UT-A3 activity by alpha2,6-sialylation.

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    Qian, Xiaoqian; Sands, Jeff M; Song, Xiang; Chen, Guangping

    2016-07-01

    Two urea transporters, UT-A1 and UT-A3, are expressed in the kidney terminal inner medullary collecting duct (IMCD) and are important for the production of concentrated urine. UT-A1, as the largest isoform of all UT-A urea transporters, has gained much attention and been extensively studied; however, the role and the regulation of UT-A3 are less explored. In this study, we investigated UT-A3 regulation by glycosylation modification. A site-directed mutagenesis verified a single glycosylation site in UT-A3 at Asn279. Loss of the glycosylation reduced forskolin-stimulated UT-A3 cell membrane expression and urea transport activity. UT-A3 has two glycosylation forms, 45 and 65 kDa. Using sugar-specific binding lectins, the UT-A3 glycosylation profile was examined. The 45-kDa form was pulled down by lectin concanavalin A (Con A) and Galant husnivalis lectin (GNL), indicating an immature glycan with a high amount of mannose (Man), whereas the 65-kDa form is a mature glycan composed of acetylglucosamine (GlcNAc) and poly-N-acetyllactosame (poly-LacNAc) that was pulled down by wheat germ agglutinin (WGA) and tomato lectin, respectively. Interestingly, the mature form of UT-A3 glycan contains significant amounts of sialic acid. We explored the enzymes responsible for directing UT-A3 sialylation. Sialyltransferase ST6GalI, but not ST3GalIV, catabolizes UT-A3 α2,6-sialylation. Activation of protein kinase C (PKC) by PDB treatment promoted UT-A3 glycan sialylation and membrane surface expression. The PKC inhibitor chelerythrine blocks ST6GalI-induced UT-A3 sialylation. Increased sialylation by ST6GalI increased UT-A3 protein stability and urea transport activity. Collectively, our study reveals a novel mechanism of UT-A3 regulation by ST6GalI-mediated sialylation modification that may play an important role in kidney urea reabsorption and the urinary concentrating mechanism.

  4. Glycoforms of UT-A3 urea transporter with poly-N-acetyllactosamine glycosylation have enhanced transport activity.

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    Su, Hua; Carter, Conner B; Fröhlich, Otto; Cummings, Richard D; Chen, Guangping

    2012-07-15

    Urea transporters UT-A1 and UT-A3 are both expressed in the kidney inner medulla. However, the function of UT-A3 remains unclear. Here, we found that UT-A3, which comprises only the NH(2)-terminal half of UT-A1, has a higher urea transport activity than UT-A1 in the oocyte and that this difference was associated with differences in N-glycosylation. Heterologously expressed UT-A3 is fully glycosylated with two glycoforms of 65 and 45 kDa. By contrast, UT-A1 expressed in HEK293 cells and oocytes exhibits only a 97-kDa glycosylation form. We further found that N-glycans of UT-A3 contain a large amount of poly-N-acetyllactosamine. This highly glycosylated UT-A3 is more stable and is enriched in lipid raft domains on the cell membrane. Kifunensine, an inhibitor of α-mannosidase that inhibits N-glycan processing beyond high-mannose-type N-glycans, significantly reduced UT-A3 urea transport activity. We then examined the native UT-A1 and UT-A3 glycosylation states from kidney inner medulla and found the ratio of 65 to 45 kDa in UT-A3 is higher than that of 117 to 97 kDa in UT-A1. The highly stable expression of highly glycosylated UT-A3 on the cell membrane in kidney inner medulla suggests that UT-A3 may have an important function in urea reabsorption.

  5. Small GTPase Rab14 down-regulates UT-A1 urea transport activity through enhanced clathrin-dependent endocytosis.

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    Su, Hua; Liu, Bingchen; Fröhlich, Otto; Ma, Heping; Sands, Jeff M; Chen, Guangping

    2013-10-01

    The UT-A1 urea transporter plays an important role in the urinary concentration mechanism. However, the molecular mechanisms regarding UT-A1 trafficking, endocytosis, and degradation are still unclear. In this study, we identified the small GTPase Rab14 as a binding partner to the C terminus of UT-A1 in a yeast 2-hybrid assay. Interestingly, UT-A1 binding is preferential for the GDP-bound inactive form of Rab14. Coinjection of Rab14 in Xenopus oocytes results in a decrease of UT-A1 urea transport activity, suggesting that Rab14 acts as a negative regulator of UT-A1. We subsequently found that Rab14 reduces the cell membrane expression of UT-A1, as evidenced by cell surface biotinylation. This effect is blocked by chlorpromazine, an inhibitor of the clathrin-mediated endocytic pathway, but not by filipin, an inhibitor of the caveolin-mediated endocytic pathway. In kidney, Rab14 is mainly expressed in IMCD epithelial cells with a pattern identical to UT-A1 expression. Consistent with its role in participating in clathrin-mediated endocytosis, Rab14 localizes in nonlipid raft microdomains and codistributes with Rab5, a marker of the clathrin-mediated endocytic pathway. Taken together, our study suggests that Rab14, as a novel UT-A1 partner, may have an important regulatory function for UT-A1 urea transport activity in the kidney inner medulla.

  6. Structure-activity analysis of thiourea analogs as inhibitors of UT-A and UT-B urea transporters.

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    Esteva-Font, Cristina; Phuan, Puay-Wah; Lee, Sujin; Su, Tao; Anderson, Marc O; Verkman, A S

    2015-05-01

    Small-molecule inhibitors of urea transporter (UT) proteins in kidney have potential application as novel salt-sparing diuretics. The urea analog dimethylthiourea (DMTU) was recently found to inhibit the UT isoforms UT-A1 (expressed in kidney tubule epithelium) and UT-B (expressed in kidney vasa recta endothelium) with IC50 of 2-3 mM, and was shown to have diuretic action when administered to rats. Here, we measured UT-A1 and UT-B inhibition activity of 36 thiourea analogs, with the goal of identifying more potent and isoform-selective inhibitors, and establishing structure-activity relationships. The analog set systematically explored modifications of substituents on the thiourea including alkyl, heterocycles and phenyl rings, with different steric and electronic features. The analogs had a wide range of inhibition activities and selectivities. The most potent inhibitor, 3-nitrophenyl-thiourea, had an IC50 of ~0.2 mM for inhibition of both UT-A1 and UT-B. Some analogs such as 4-nitrophenyl-thiourea were relatively UT-A1 selective (IC50 1.3 vs. 10 mM), and others such as thioisonicotinamide were UT-B selective (IC50>15 vs. 2.8 mM).

  7. Mathematical modeling of urea transport in the kidney.

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    Layton, Anita T

    2014-01-01

    Mathematical modeling techniques have been useful in providing insights into biological systems, including the kidney. This article considers some of the mathematical models that concern urea transport in the kidney. Modeling simulations have been conducted to investigate, in the context of urea cycling and urine concentration, the effects of hypothetical active urea secretion into pars recta. Simulation results suggest that active urea secretion induces a "urea-selective" improvement in urine concentrating ability. Mathematical models have also been built to study the implications of the highly structured organization of tubules and vessels in the renal medulla on urea sequestration and cycling. The goal of this article is to show how physiological problems can be formulated and studied mathematically, and how such models may provide insights into renal functions.

  8. Comparative transport efficiencies of urea analogues through urea transporter UT-B.

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    Zhao, Dan; Sonawane, N D; Levin, Marc H; Yang, Baoxue

    2007-07-01

    Expression of urea transporter UT-B confers high urea permeability to mammalian erythrocytes. Erythrocyte membranes also permeate various urea analogues, suggesting common transport pathways for urea and structurally similar solutes. In this study, we examined UT-B-facilitated passage of urea analogues and other neutral small solutes by comparing transport properties of wildtype to UT-B-deficient mouse erythrocytes. Stopped-flow light-scattering measurements indicated high UT-B permeability to urea and chemical analogues formamide, acetamide, methylurea, methylformamide, ammonium carbamate, and acrylamide, each with P(s)>5.0 x 10(-6) cm/s at 10 degrees C. UT-B genetic knockout and phloretin treatment of wildtype erythrocytes similarly reduced urea analogue permeabilities. Strong temperature dependencies of formamide, acetamide, acrylamide and butyramide transport across UT-B-null membranes (E(a)>10 kcal/mol) suggested efficient diffusion of these amides across lipid bilayers. Urea analogues dimethylurea, acryalmide, methylurea, thiourea and methylformamide inhibited UT-B-mediated urea transport by >60% in the absence of transmembrane analogue gradients, supporting a pore-blocking mechanism of UT-B inhibition. Differential transport efficiencies of urea and its analogues through UT-B provide insight into chemical interactions between neutral solutes and the UT-B pore.

  9. Phosphorylation of UT-A1 urea transporter at serines 486 and 499 is important for vasopressin-regulated activity and membrane accumulation.

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    Blount, Mitsi A; Mistry, Abinash C; Fröhlich, Otto; Price, S Russ; Chen, Guangping; Sands, Jeff M; Klein, Janet D

    2008-07-01

    The UT-A1 urea transporter plays an important role in the urine concentrating mechanism. Vasopressin (or cAMP) increases urea permeability in perfused terminal inner medullary collecting ducts and increases the abundance of phosphorylated UT-A1, suggesting regulation by phosphorylation. We performed a phosphopeptide analysis that strongly suggested that a PKA consensus site(s) in the central loop region of UT-A1 was/were phosphorylated. Serine 486 was most strongly identified, with other potential sites at serine 499 and threonine 524. Phosphomutation constructs of each residue were made and transiently transfected into LLC-PK1 cells to assay for UT-A1 phosphorylation. The basal level of UT-A1 phosphorylation was unaltered by mutation of these sites. We injected oocytes, assayed [14C]urea flux, and determined that mutation of these sites did not alter basal urea transport activity. Next, we tested the effect of stimulating cAMP production with forskolin. Forskolin increased wild-type UT-A1 and T524A phosphorylation in LLC-PK1 cells and increased urea flux in oocytes. In contrast, the S486A and S499A mutants demonstrated loss of forskolin-stimulated UT-A1 phosphorylation and reduced urea flux. In LLC-PK1 cells, we assessed biotinylated UT-A1. Wild-type UT-A1, S486A, and S499A accumulated in the membrane in response to forskolin. However, in the S486A/S499A double mutant, forskolin-stimulated UT-A1 membrane accumulation and urea flux were totally blocked. We conclude that the phosphorylation of UT-A1 on both serines 486 and 499 is important for activity and that this phosphorylation may be involved in UT-A1 membrane accumulation.

  10. Cortisol-sensitive urea transport across the gill basolateral membrane of the gulf toadfish (Opsanus beta).

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    Rodela, Tamara M; Gilmour, Kathleen M; Walsh, Patrick J; McDonald, M Danielle

    2009-08-01

    Gulf toadfish (Opsanus beta) use a unique pulsatile urea excretion mechanism that allows urea to be voided in large pulses via the periodic insertion or activation of a branchial urea transporter. The precise cellular and subcellular location of the facilitated diffusion mechanism(s) remains unclear. An in vitro basolateral membrane vesicle (BLMV) preparation was used to test the hypothesis that urea movement across the gill basolateral membrane occurs through a cortisol-sensitive carrier-mediated mechanism. Toadfish BLMVs demonstrated two components of urea uptake: a linear element at high external urea concentrations, and a phloretin-sensitive saturable constituent (K(m) = 0.24 mmol/l; V(max) = 6.95 micromol x mg protein(-1) x h(-1)) at low urea concentrations ( 2, further suggestive of carrier-mediated processes. Our data provide evidence that a basolateral urea facilitated transporter accelerates the movement of urea between the plasma and gills to enable the pulsatile excretion of urea. Furthermore, in vivo infusion of cortisol caused a significant 4.3-fold reduction in BLMV urea transport capacity in lab-crowded fish, suggesting that cortisol inhibits the recruitment of urea transporters to the basolateral membrane, which may ultimately affect the size of the urea pulse event in gulf toadfish.

  11. Urea transporters and sweat response to uremia.

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    Keller, Raymond W; Bailey, James L; Wang, Yanhua; Klein, Janet D; Sands, Jeff M

    2016-06-01

    In humans, urea is excreted in sweat, largely through the eccrine sweat gland. The urea concentration in human sweat is elevated when compared to blood urea nitrogen. The sweat urea nitrogen (UN) of patients with end-stage kidney disease (ESRD) is increased when compared with healthy humans. The ability to produce sweat is maintained in the overwhelming majority of ESRD patients. A comprehensive literature review found no reports of sweat UN neither in healthy rodents nor in rodent models of chronic kidney disease (CKD). Therefore, this study measured sweat UN concentrations in healthy and uremic rats. Uninephrectomy followed by renal artery ligation was used to remove 5/6 of renal function. Rats were then fed a high-protein diet to induce uremia. Pilocarpine was used to induce sweating. Sweat droplets were collected under oil. Sweat UN was measured with a urease assay. Serum UN was measured using a fluorescent ortho-pthalaldehyde reaction. Immunohistochemistry (IHC) was accomplished with a horseradish peroxidase and diaminobenzidine technique. Sweat UN in uremic rats was elevated greater than two times compared to healthy pair-fed controls (220 ± 17 and 91 ± 15 mmol/L, respectively). Post hoc analysis showed a significant difference between male and female uremic sweat UN (279 ± 38 and 177 ± 11 mmol/L, respectively.) IHC shows, for the first time, the presence of the urea transporters UT-B and UT-A2 in both healthy and uremic rat cutaneous structures. Future studies will use this model to elucidate how rat sweat UN and other solute excretion is altered by commonly prescribed diuretics.

  12. Functional characterization of the central hydrophilic linker region of the urea transporter UT-A1: cAMP activation and snapin binding.

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    Mistry, Abinash C; Mallick, Rickta; Klein, Janet D; Sands, Jeff M; Fröhlich, Otto

    2010-06-01

    Of the three major protein variants produced by the UT-A gene (UT-A1, UT-A2, and UT-A3) UT-A1 is the largest. It contains UT-A3 as its NH(2)-terminal half and UT-A2 as its COOH-terminal half. When being part of UT-A1, UT-A3 and UT-A2 are joined by a segment, Lp, whose central part, Lc, is not part of UT-A3 or UT-A2 but is present only in UT-A1. Lc contains the phosphorylation sites S486 and S499 that are involved in protein kinase A-dependent activation, as well as the binding site for snapin, a protein involved in soluble N-ethylmaleimide-sensitive fusion protein attachment protein receptor (SNARE)-mediated vesicle trafficking and fusion to the plasma membrane. We attached Lc to UT-A2 and UT-A3 to test how these phosphorylation sites influenced their urea transport activity. Adding Lc to UT-A2 conferred stimulation by cAMP to the cAMP-unresponsive UT-A2, and adding Lc to UT-A3 did not further enhance its already existing cAMP response. These findings suggest that the responsiveness to vasopressin that is observed with UT-A1 can be introduced into the unresponsive UT-A2 variant through the Lc segment that is unique to UT-A1. In UT-A3, however, the Lc segment plays no significant role in its activation by cAMP. In addition, the Lc segment also gave UT-A2 the ability to bind snapin and, in Xenopus oocytes, to be stimulated in its urea transport activity by snapin and syntaxins 3 and 4, in the same way as UT-A1.

  13. Activation of the cAMP/PKA pathway induces UT-A1 urea transporter monoubiquitination and targets it for lysosomal degradation.

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    Su, Hua; Chen, Minguang; Sands, Jeff M; Chen, Guangping

    2013-12-15

    Regulation of urea transporter UT-A1 in the kidney is important for the urinary concentrating mechanism. We previously reported that activation of the cAMP/PKA pathway by forskolin (FSK) leads to UT-A1 ubiquitination, endocytosis, and degradation. In this study, we discovered that FSK-induced UT-A1 ubiquitination is monoubiquitination as judged by immunoblotting with specific ubiquitin antibodies to the different linkages of the ubiquitin chain. UT-A1 monoubiquitination induced by FSK was processed mainly on the cell plasma membrane. Monoubiquitination facilitates UT-A1 endocytosis, and internalized UT-A1 is accumulated in the early endosome. Inhibition of ubiquitination by E1 ubiquitin-activating enzyme inhibitor PYR-41 significantly reduced FSK-induced UT-A1 endocytosis and degradation. Interestingly, FSK-stimulated UT-A1 degradation occurs through a lysosomal protein degradation system. We further found that the PKA phosphorylation sites of UT-A1 at Ser486 and Ser499 are required for FSK-induced UT-A1 monoubiquitination. The physiological significance was confirmed using rat kidney inner medullary collecting duct suspensions, which showed that vasopressin treatment promotes UT-A1 ubiquitination. We conclude that unlike under basal conditions in which UT-A1 is subject to polyubiquitination and proteasome-mediated protein degradation, activation of UT-A1 by FSK induces UT-A1 monoubiquitination and protein lysosomal degradation.

  14. Structure and permeation mechanism of a mammalian urea transporter

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    Levin, Elena J.; Cao, Yu; Enkavi, Giray; Quick, Matthias; Pan, Yaping; Tajkhorshid, Emad; Zhou, Ming (UIUC); (Columbia)

    2012-09-17

    As an adaptation to infrequent access to water, terrestrial mammals produce urine that is hyperosmotic to plasma. To prevent osmotic diuresis by the large quantity of urea generated by protein catabolism, the kidney epithelia contain facilitative urea transporters (UTs) that allow rapid equilibration between the urinary space and the hyperosmotic interstitium. Here we report the first X-ray crystal structure of a mammalian UT, UT-B, at a resolution of 2.36 {angstrom}. UT-B is a homotrimer and each protomer contains a urea conduction pore with a narrow selectivity filter. Structural analyses and molecular dynamics simulations showed that the selectivity filter has two urea binding sites separated by an approximately 5.0 kcal/mol energy barrier. Functional studies showed that the rate of urea conduction in UT-B is increased by hypoosmotic stress, and that the site of osmoregulation coincides with the location of the energy barrier.

  15. Epac regulates UT-A1 to increase urea transport in inner medullary collecting ducts.

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    Wang, Yanhua; Klein, Janet D; Blount, Mitsi A; Martin, Christopher F; Kent, Kimilia J; Pech, Vladimir; Wall, Susan M; Sands, Jeff M

    2009-09-01

    Urea plays a critical role in the concentration of urine, thereby regulating water balance. Vasopressin, acting through cAMP, stimulates urea transport across rat terminal inner medullary collecting ducts (IMCD) by increasing the phosphorylation and accumulation at the apical plasma membrane of UT-A1. In addition to acting through protein kinase A (PKA), cAMP also activates Epac (exchange protein activated by cAMP). In this study, we tested whether the regulation of urea transport and UT-A1 transporter activity involve Epac in rat IMCD. Functional analysis showed that an Epac activator significantly increased urea permeability in isolated, perfused rat terminal IMCD. Similarly, stimulating Epac by adding forskolin and an inhibitor of PKA significantly increased urea permeability. Incubation of rat IMCD suspensions with the Epac activator significantly increased UT-A1 phosphorylation and its accumulation in the plasma membrane. Furthermore, forskolin-stimulated cAMP significantly increased ERK 1/2 phosphorylation, which was not prevented by inhibiting PKA, indicating that Epac mediated this phosphorylation of ERK 1/2. Inhibition of MEK 1/2 phosphorylation decreased the forskolin-stimulated UT-A1 phosphorylation. Taken together, activation of Epac increases urea transport, accumulation of UT-A1 at the plasma membrane, and UT-A1 phosphorylation, the latter of which is mediated by the MEK-ERK pathway.

  16. Urearetics: a small molecule screen yields nanomolar potency inhibitors of urea transporter UT-B.

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    Levin, Marc H; de la Fuente, Ricardo; Verkman, A S

    2007-02-01

    Functional studies in knockout mice indicate a critical role for urea transporters (UTs) in the urinary concentrating mechanism and in renal urea clearance. However, potent and specific urea transport blockers have not been available. Here, we used high-throughput screening to discover high-affinity, small molecule inhibitors of the UT-B urea transporter. A collection of 50,000 diverse, drug-like compounds was screened using a human erythrocyte lysis assay based on UT-B-facilitated acetamide transport. Primary screening yielded approximately 30 UT-B inhibitors belonging to the phenylsulfoxyoxazole, benzenesulfonanilide, phthalazinamine, and aminobenzimidazole chemical classes. Screening of approximately 700 structurally similar analogs gave many active compounds, the most potent of which inhibited UT-B urea transport with an EC50 of approximately 10 nM, and approximately 100% inhibition at higher concentrations. Phenylsulfoxyoxazoles and phthalazinamines also blocked rodent UT-B and had good UT-B vs. UT-A specificity. The UT-B inhibitors did not reduce aquaporin-1 (AQP1)-facilitated water transport. In AQP1-null erythrocytes, "chemical UT-B knockout" by UT-B inhibitors reduced by approximately 3-fold UT-B-mediated water transport, supporting an aqueous pore pathway through UT-B. UT-B inhibitors represent a new class of diuretics, "urearetics," which are predicted to increase renal water and solute clearance in water-retaining states.

  17. Urea Transporter Inhibitors: En Route to New Diuretics

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    Sands, Jeff M.

    2013-01-01

    Summary A selective urea transporter UT-A1 inhibitor would be a novel type of diuretic, likely with less undesirable side-effects than conventional diureticssince it acts on the last portion of the nephron. Esteva-Font et al. (2013) develop suchan inhibitor by using a clever high-throughput screening assay, and document its selectivity. . PMID:24210002

  18. Evolution of urea transporters in vertebrates: adaptation to urea's multiple roles and metabolic sources.

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    LeMoine, Christophe M R; Walsh, Patrick J

    2015-06-01

    In the two decades since the first cloning of the mammalian kidney urea transporter (UT-A), UT genes have been identified in a plethora of organisms, ranging from single-celled bacteria to metazoans. In this review, focusing mainly on vertebrates, we first reiterate the multiple catabolic and anabolic pathways that produce urea, then we reconstruct the phylogenetic history of UTs, and finally we examine the tissue distribution of UTs in selected vertebrate species. Our analysis reveals that from an ancestral UT, three homologues evolved in piscine lineages (UT-A, UT-C and UT-D), followed by a subsequent reduction to a single UT-A in lobe-finned fish and amphibians. A later internal tandem duplication of UT-A occurred in the amniote lineage (UT-A1), followed by a second tandem duplication in mammals to give rise to UT-B. While the expected UT expression is evident in excretory and osmoregulatory tissues in ureotelic taxa, UTs are also expressed ubiquitously in non-ureotelic taxa, and in tissues without a complete ornithine-urea cycle (OUC). We posit that non-OUC production of urea from arginine by arginase, an important pathway to generate ornithine for synthesis of molecules such as polyamines for highly proliferative tissues (e.g. testis, embryos), and neurotransmitters such as glutamate for neural tissues, is an important evolutionary driving force for the expression of UTs in these taxa and tissues.

  19. Transgenic Restoration of Urea Transporter A1 Confers Maximal Urinary Concentration in the Absence of Urea Transporter A3.

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    Klein, Janet D; Wang, Yanhua; Mistry, Abinash; LaRocque, Lauren M; Molina, Patrick A; Rogers, Richard T; Blount, Mitsi A; Sands, Jeff M

    2016-05-01

    Urea has a critical role in urinary concentration. Mice lacking the inner medullary collecting duct (IMCD) urea transporter A1 (UT-A1) and urea transporter A3 (UT-A3) have very low levels of urea permeability and are unable to concentrate urine. To investigate the role of UT-A1 in the concentration of urine, we transgenically expressed UT-A1 in knockout mice lacking UT-A1 and UT-A3 using a construct with a UT-A1 gene that cannot be spliced to produce UT-A3. This construct was inserted behind the original UT-A promoter to yield a mouse expressing only UT-A1 (UT-A1(+/+)/UT-A3(-/-)). Western blot analysis demonstrated UT-A1 in the inner medulla of UT-A1(+/+)/UT-A3(-/-) and wild-type mice, but not in UT-A1/UT-A3 knockout mice, and an absence of UT-A3 in UT-A1(+/+)/UT-A3(-/-) and UT-A1/UT-A3 knockout mice. Immunohistochemistry in UT-A1(+/+)/UT-A3(-/-) mice also showed negative UT-A3 staining in kidney and other tissues and positive UT-A1 staining only in the IMCD. Urea permeability in isolated perfused IMCDs showed basal permeability in the UT-A1(+/+)/UT-A3(-/-) mice was similar to levels in wild-type mice, but vasopressin stimulation of urea permeability in wild-type mice was significantly greater (100% increase) than in UT-A1(+/+)/UT-A3(-/-) mice (8% increase). Notably, basal urine osmolalities in both wild-type and UT-A1(+/+)/UT-A3(-/-) mice increased upon overnight water restriction. We conclude that transgenic expression of UT-A1 restores basal urea permeability to the level in wild-type mice but does not restore vasopressin-stimulated levels of urea permeability. This information suggests that transgenic expression of UT-A1 alone in mice lacking UT-A1 and UT-A3 is sufficient to restore urine-concentrating ability.

  20. Thienoquinolins exert diuresis by strongly inhibiting UT-A urea transporters.

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    Ren, Huiwen; Wang, Yanhua; Xing, Yongning; Ran, Jianhua; Liu, Ming; Lei, Tianluo; Zhou, Hong; Li, Runtao; Sands, Jeff M; Yang, Baoxue

    2014-12-15

    Urea transporters (UT) play an important role in the urine concentration mechanism by mediating intrarenal urea recycling, suggesting that UT inhibitors could have therapeutic use as a novel class of diuretic. Recently, we found a thienoquinolin UT inhibitor, PU-14, that exhibited diuretic activity. The purpose of this study was to identify more potent UT inhibitors that strongly inhibit UT-A isoforms in the inner medullary collecting duct (IMCD). Efficient thienoquinolin UT inhibitors were identified by structure-activity relationship analysis. Urea transport inhibition activity was assayed in perfused rat terminal IMCDs. Diuretic activity of the compound was determined in rats and mice using metabolic cages. The results show that the compound PU-48 exhibited potent UT-A inhibition activity. The inhibition was 69.5% with an IC50 of 0.32 μM. PU-48 significantly inhibited urea transport in perfused rat terminal IMCDs. PU-48 caused significant diuresis in UT-B null mice, which indicates that UT-A is the target of PU-48. The diuresis caused by PU-48 did not change blood Na(+), K(+), or Cl(-) levels or nonurea solute excretion in rats and mice. No toxicity was detected in cells or animals treated with PU-48. The results indicate that thienoquinolin UT inhibitors induce a diuresis by inhibiting UT-A in the IMCD. This suggests that they may have the potential to be developed as a novel class of diuretics with fewer side effects than classical diuretics.

  1. MDM2 E3 ubiquitin ligase mediates UT-A1 urea transporter ubiquitination and degradation.

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    Chen, Guangping; Huang, Haidong; Fröhlich, Otto; Yang, Yuan; Klein, Janet D; Price, S Russ; Sands, Jeff M

    2008-11-01

    UT-A1 is the primary urea transporter in the apical plasma membrane responsible for urea reabsorption in the inner medullary collecting duct. Although the physiological function of UT-A1 has been well established, the molecular mechanisms that regulate its activity are less well understood. Analysis of the UT-A1 amino acid sequence revealed a potential MDM2 E3 ubiquitin ligase-binding motif in the large intracellular loop of UT-A1, suggesting that UT-A1 urea transporter protein may be regulated by the ubiquitin-proteasome pathway. Here, we report that UT-A1 is ubiquitinated and degraded by the proteasome but not the lysosome proteolytic pathway. Inhibition of proteasome activity causes UT-A1 cell surface accumulation and concomitantly increases urea transport activity. UT-A1 interacts directly with MDM2; the binding site is located in the NH2-terminal p53-binding region of MDM2. MDM2 mediates UT-A1 ubiquitination both in vivo and in vitro. Overexpression of MDM2 promotes UT-A1 degradation. The mechanism is likely to be physiologically important as UT-A1 ubiquitination was identified in kidney inner medullary tissue. The ubiquitin-proteasome degradation pathway provides an important novel mechanism for UT-A1 regulation.

  2. Phosphorylation of UT-A1 on serine 486 correlates with membrane accumulation and urea transport activity in both rat IMCDs and cultured cells.

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    Klein, Janet D; Blount, Mitsi A; Fröhlich, Otto; Denson, Chad E; Tan, Xiaoxiao; Sim, Jae H; Martin, Christopher F; Sands, Jeff M

    2010-04-01

    Vasopressin is the primary hormone regulating urine-concentrating ability. Vasopressin phosphorylates the UT-A1 urea transporter in rat inner medullary collecting ducts (IMCDs). To assess the effect of UT-A1 phosphorylation at S486, we developed a phospho-specific antibody to S486-UT-A1 using an 11 amino acid peptide antigen starting from amino acid 482 that bracketed S486 in roughly the center of the sequence. We also developed two stably transfected mIMCD3 cell lines: one expressing wild-type UT-A1 and one expressing a mutated form of UT-A1, S486A/S499A, that is unresponsive to protein kinase A. Forskolin stimulates urea flux in the wild-type UT-A1-mIMCD3 cells but not in the S486A/S499A-UT-A1-mIMCD3 cells. The phospho-S486-UT-A1 antibody identified UT-A1 protein in the wild-type UT-A1-mIMCD3 cells but not in the S486A/S499A-UT-A1-mIMCD3 cells. In rat IMCDs, forskolin increased the abundance of phospho-S486-UT-A1 (measured using the phospho-S486 antibody) and of total UT-A1 phosphorylation (measured by (32)P incorporation). Forskolin also increased the plasma membrane accumulation of phospho-S486-UT-A1 in rat IMCD suspensions, as measured by biotinylation. In rats treated with vasopressin in vivo, the majority of the phospho-S486-UT-A1 appears in the apical plasma membrane. In summary, we developed stably transfected mIMCD3 cell lines expressing UT-A1 and an S486-UT-A1 phospho-specific antibody. We confirmed that vasopressin increases UT-A1 accumulation in the apical plasma membrane and showed that vasopressin phosphorylates UT-A1 at S486 in rat IMCDs and that the S486-phospho-UT-A1 form is primarily detected in the apical plasma membrane.

  3. New Advances in Urea Transporter UT-A1 Membrane Trafficking

    Directory of Open Access Journals (Sweden)

    Guangping Chen

    2013-05-01

    Full Text Available The vasopressin-regulated urea transporter UT-A1, expressed in kidney inner medullary collecting duct (IMCD epithelial cells, plays a critical role in the urinary concentrating mechanisms. As a membrane protein, the function of UT-A1 transport activity relies on its presence in the plasma membrane. Therefore, UT-A1 successfully trafficking to the apical membrane of the polarized epithelial cells is crucial for the regulation of urea transport. This review summarizes the research progress of UT-A1 regulation over the past few years, specifically on the regulation of UT-A1 membrane trafficking by lipid rafts, N-linked glycosylation and a group of accessory proteins.

  4. New advances in urea transporter UT-A1 membrane trafficking.

    Science.gov (United States)

    Chen, Guangping

    2013-05-21

    The vasopressin-regulated urea transporter UT-A1, expressed in kidney inner medullary collecting duct (IMCD) epithelial cells, plays a critical role in the urinary concentrating mechanisms. As a membrane protein, the function of UT-A1 transport activity relies on its presence in the plasma membrane. Therefore, UT-A1 successfully trafficking to the apical membrane of the polarized epithelial cells is crucial for the regulation of urea transport. This review summarizes the research progress of UT-A1 regulation over the past few years, specifically on the regulation of UT-A1 membrane trafficking by lipid rafts, N-linked glycosylation and a group of accessory proteins.

  5. Mice lacking urea transporter UT-B display depression-like behavior.

    Science.gov (United States)

    Li, Xin; Ran, Jianhua; Zhou, Hong; Lei, Tianluo; Zhou, Li; Han, Jingyan; Yang, Baoxue

    2012-02-01

    Urea transporter B is one of urea transporters that selectively transport urea driven by urea gradient across membrane and expressed abundantly in brain. To determine the physiological role of UT-B in brain, UT-B localization, urea concentration, tissue morphology of brain, and behavioral phenotypes were studied in UT-B heterozygous mice via UT-B null mice. UT-B mRNA was expressed in olfactory bulb, cortex, caudate nucleus, hippocampus and hypothalamus of UT-B heterozygous mice. UT-B null mice exhibited depression-like behavior, with urea accumulation, nitric oxide reduction, and selective neuronal nitric oxide synthase level increase in hippocampus. After acute urea loading, the urea level increased, NO production decreased in hippocampus from both types of mice. Moreover, urea level was higher, and NO concentration was lower consistently in UT-B null hippocampus than that in heterozygous hippocampus. In vitro, 25 mM urea inhibited NO production too. Furthermore, UT-B knockout induced a long-lasting notable decrease in regional cerebral blood flow and altered morphology, such as loss of neurons in CA3 region, swelling, and membranous myelin-like structure formation within myelinated and unmyelinated fibers in hippocampus. These results suggest that urea accumulation in the hippocampus induced by UT-B deletion can cause depression-like behavior, which possibly attribute to disturbance in NOS/NO system.

  6. An evaluation of twelve nested models of transperitoneal transport of urea

    DEFF Research Database (Denmark)

    Graff, J; Fugleberg, S; Joffe, P;

    1995-01-01

    Models of transperitoneal urea transport are generally based on the one-compartment assumption, i.e. that the plasma water urea concentration in the peritoneal capillary bed is equal to the plasma water urea concentration in the peripheral veins. The aim of this study was to investigate...... the mechanism(s) of transperitoneal urea transport and to test the one-compartment assumption for urea. A total of 12 nested models were formulated and validated on the basis of experimental results obtained from 23 non-diabetic patients undergoing peritoneal dialysis. The validation procedure demonstrated...... that transperitoneal transport of urea probably involves diffusion, non-lymphatic convection and lymphatic convection. It was furthermore demonstrated that the inclusion of lymphatic convection changes the mass transfer area coefficient considerably. Finally, no deviation from the one-compartment assumption...

  7. A small molecule screen identifies selective inhibitors of urea transporter UT-A.

    Science.gov (United States)

    Esteva-Font, Cristina; Phuan, Puay-Wah; Anderson, Marc O; Verkman, A S

    2013-10-24

    Urea transporter (UT) proteins, including UT-A in kidney tubule epithelia and UT-B in vasa recta microvessels, facilitate urinary concentrating function. A screen for UT-A inhibitors was developed in MDCK cells expressing UT-A1, water channel aquaporin-1, and YFP-H148Q/V163S. An inwardly directed urea gradient produces cell shrinking followed by UT-A1-dependent swelling, which was monitored by YFP-H148Q/V163S fluorescence. Screening of ~90,000 synthetic small molecules yielded four classes of UT-A1 inhibitors with low micromolar half-maximal inhibitory concentration that fully and reversibly inhibited urea transport by a noncompetitive mechanism. Structure-activity analysis of >400 analogs revealed UT-A1-selective and UT-A1/UT-B nonselective inhibitors. Docking computations based on homology models of UT-A1 suggested inhibitor binding sites. UT-A inhibitors may be useful as diuretics ("urearetics") with a mechanism of action that may be effective in fluid-retaining conditions in which conventional salt transport-blocking diuretics have limited efficacy.

  8. Nanomolar potency and metabolically stable inhibitors of kidney urea transporter UT-B.

    Science.gov (United States)

    Anderson, Marc O; Zhang, Jicheng; Liu, Yan; Yao, Chenjuan; Phuan, Puay-Wah; Verkman, A S

    2012-06-28

    Urea transporters, which include UT-B in kidney microvessels, are potential targets for development of drugs with a novel diuretic ('urearetic') mechanism. We recently identified, by high-throughput screening, a triazolothienopyrimidine UT-B inhibitor, 1, that selectively and reversibly inhibited urea transport with IC(50) = 25.1 nM and reduced urinary concentration in mice ( Yao et al. J. Am. Soc. Nephrol. , in press ). Here, we analyzed 273 commercially available analogues of 1 to establish a structure-activity series and synthesized a targeted library of 11 analogues to identify potent, metabolically stable UT-B inhibitors. The best compound, {3-[4-(1,1-difluoroethyl)benzenesulfonyl]thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-yl}thiophen-2-ylmethylamine, 3k, had IC(50) of 23 and 15 nM for inhibition of urea transport by mouse and human UT-B, respectively, and ∼40-fold improved in vitro metabolic stability compared to 1. In mice, 3k accumulated in kidney and urine and reduced maximum urinary concentration. Triazolothienopyrimidines may be useful for therapy of diuretic-refractory edema in heart and liver failure.

  9. How renal cells handle urea.

    Science.gov (United States)

    Bagnasco, S M

    2000-01-01

    The urine concentration process requires an osmolality gradient along the renal cortico-medullary axis, with highest values in the renal papilla. NaCl and urea are the major solutes in the renal inner medulla, concentrations of urea up to 500-600 mM are found in the rat renal papilla. Urea can diffuse across cell membranes and contributes to balance intracellular and extracellular osmotic equilibrium. However, urea has perturbing effects on enzyme activity, and in concentrations above 300 mM is toxic for renal cultured cells. There is increasing evidence that urea can induce cellular responses distinct from those due to NaCl and other non-permeable solutes, including upregulation of immediate-early genes (IEGs). Urea transport by epithelial and endothelial cells is important for intra-medullary urea recycling and preservation of high urea concentration in the inner medulla. Trans-cellular movement of urea in cells expressing urea transporters may influence intracellular levels of this solute and modulate urea-induced signaling pathways. Regulation of urea transporters expression and activity can therefore be viewed as one aspect of cellular adaptation to urea. We have identified tonicity-responsive transcription as one mechanism regulating expression of the urea transporter UT-A. The short-term and long-term effects of variable extracellular urea concentration on the function of renal cells remain still unclear.

  10. Urea transporter proteins as targets for small-molecule diuretics

    Science.gov (United States)

    Esteva-Font, Cristina; Anderson, Marc O.; Verkman, Alan S.

    2016-01-01

    Conventional diuretics such as furosemide and thiazides target salt transporters in kidney tubules, but urea transporters (UTs) have emerged as alternative targets. UTs are a family of transmembrane channels expressed in a variety of mammalian tissues, in particular the kidney. UT knockout mice and humans with UT mutations exhibit reduced maximal urinary osmolality, demonstrating that UTs are necessary for the concentration of urine. Small-molecule screening has identified potent and selective inhibitors of UT-A, the UT protein expressed in renal tubule epithelial cells, and UT-B, the UT protein expressed in vasa recta endothelial cells. Data from UT knockout mice and from rodents administered UT inhibitors support the diuretic action of UT inhibition. The kidney-specific expression of UT-A1, together with high selectivity of the small-molecule inhibitors, means that off-target effects of such small-molecule drugs should be minimal. This Review summarizes the structure, expression and function of UTs, and looks at the evidence supporting the validity of UTs as targets for the development of salt-sparing diuretics with a unique mechanism of action. UT-targeted inhibitors may be useful alone or in combination with conventional diuretics for therapy of various oedemas and hyponatraemias, potentially including those refractory to treatment with current diuretics. PMID:25488859

  11. Differential protein abundance and function of UT-B urea transporters in human colon.

    Science.gov (United States)

    Collins, D; Winter, D C; Hogan, A M; Schirmer, L; Baird, A W; Stewart, G S

    2010-03-01

    Facilitative UT-B urea transporters enable the passage of urea across cell membranes. Gastrointestinal urea transporters are thought to play a significant role in the urea nitrogen salvaging process that occurs between mammalian hosts and their gut bacteria. This study investigated the expression of UT-B urea transporters in different segments of human colon. Immunoblot analysis showed that human colon expressed a 35-kDa glycosylated UT-B protein in the colonic mucosa. The 35-kDa UT-B transporter was predominantly located in plasma membrane-enriched samples (P UT-B transporters were located throughout colonocytes situated in the upper portion of the colonic crypts. Bidirectional trans-epithelial urea transport was significantly greater in the ascending colon than the descending colon (P UT-B protein in different sections of the human colon, strongly correlating to regions that contain the largest populations of intestinal bacteria. This study suggests an important role for UT-B urea transporters in maintaining the symbiotic relationship between humans and their gut bacteria.

  12. The N-terminal 81-aa fragment is critical for UT-A1 urea transporter bioactivity.

    Science.gov (United States)

    Huang, Haidong; Yang, Yuan; Eaton, Douglas C; Sands, Jeff M; Chen, Guangping

    2010-01-01

    The serine protease, furin, is involved in the activation of a number of proteins most notably epithelial sodium channels (ENaC). The urea transporter UT-A1, located in the kidney inner medullary collecting duct (IMCD), is important for urine concentrating ability. UT-A1's amino acid sequence has a consensus furin cleavage site (RSKR) in the N-terminal region. Despite the putative cleavage site, we find that UT-A1, either from the cytosolic or cell surface pool, is not cleaved by furin in CHO cells. This result was further confirmed by an inability of furin to cleave in vitro an (35)S-labeled UT-A1 or the 126 N-terminal UT-A1 fragment. Functionally, mutation of the furin site (R78A, R81A) does not affect UT-A1 urea transport activity. However, deletion of the 81-aa N-terminal portion does not affect UT-A1 cell surface trafficking, but seriously impair UT-A1 urea transport activity. Our results indicate that UT-A1 maturation and activation does not require furin-dependent cleavage. The N-terminal 81-aa fragment is required for proper UT-A1 urea transport activity, but its effect is not through changing UT-A1 membrane trafficking.

  13. Short communication: Assessing urea transport from milk to blood in dairy cows

    NARCIS (Netherlands)

    Spek, J.W.; Dijkstra, J.; Borne, van den J.J.G.C.; Bannink, A.

    2012-01-01

    The concentration of urea in milk (MUC) has emerged as a potentially useful tool to predict urinary N excretion. Various factors may affect the relationship between MUC and urinary N excretion, including transport characteristics of urea from blood to milk and vice versa. The main objective of this

  14. Vasopressin regulation of the renal UT-A3 urea transporter.

    Science.gov (United States)

    Stewart, G S; Thistlethwaite, A; Lees, H; Cooper, G J; Smith, Craig

    2009-03-01

    Facilitative urea transporters in the mammalian kidney play a vital role in the urinary concentrating mechanism. The urea transporters located in the renal inner medullary collecting duct, namely UT-A1 and UT-A3, are acutely regulated by the antidiuretic hormone vasopressin. In this study, we investigated the vasopressin regulation of the basolateral urea transporter UT-A3 using an MDCK-mUT-A3 cell line. Within 10 min, vasopressin stimulates urea flux through UT-A3 transporters already present at the plasma membrane, via a PKA-dependent process. Within 1 h, vasopressin significantly increases UT-A3 localization at the basolateral membrane, causing a further increase in urea transport. While the basic trafficking of UT-A3 to basolateral membranes involves both protein kinase C and calmodulin, its regulation by vasopressin specifically occurs through a casein kinase II-dependent pathway. In conclusion, this study details the effects of vasopressin on UT-A3 urea transporter function and hence its role in regulating urea permeability within the renal inner medullary collecting duct.

  15. The urea carboxylase and allophanate hydrolase activities of urea amidolyase are functionally independent.

    Science.gov (United States)

    Lin, Yi; Boese, Cody J; St Maurice, Martin

    2016-10-01

    Urea amidolyase (UAL) is a multifunctional biotin-dependent enzyme that contributes to both bacterial and fungal pathogenicity by catalyzing the ATP-dependent cleavage of urea into ammonia and CO2 . UAL is comprised of two enzymatic components: urea carboxylase (UC) and allophanate hydrolase (AH). These enzyme activities are encoded on separate but proximally related genes in prokaryotes while, in most fungi, they are encoded by a single gene that produces a fusion enzyme on a single polypeptide chain. It is unclear whether the UC and AH activities are connected through substrate channeling or other forms of direct communication. Here, we use multiple biochemical approaches to demonstrate that there is no substrate channeling or interdomain/intersubunit communication between UC and AH. Neither stable nor transient interactions can be detected between prokaryotic UC and AH and the catalytic efficiencies of UC and AH are independent of one another. Furthermore, an artificial fusion of UC and AH does not significantly alter the AH enzyme activity or catalytic efficiency. These results support the surprising functional independence of AH from UC in both the prokaryotic and fungal UAL enzymes and serve as an important reminder that the evolution of multifunctional enzymes through gene fusion events does not always correlate with enhanced catalytic function.

  16. Short communication: urea transporter protein UT-B in the bovine parotid gland.

    Science.gov (United States)

    Dix, L; Ward, D T; Stewart, G S

    2013-03-01

    Ruminant nutrition relies upon the symbiotic relationship that exists with microbial populations in the rumen. Urea transported across the ruminal epithelia and secreted by the salivary glands is a key source of nitrogen for microbial growth in the rumen. As ruminal urea transport can be mediated by specific UT-B urea transporters, this study investigated whether UT-B urea transporters were also present in the bovine salivary gland. Western blotting experiments detected only small amounts of UT-B protein in whole-cell lysate from the bovine parotid gland. In contrast, strong 32 to 34 and 40 kDa UT-B proteins were detected in parotid plasma membrane-enriched protein, showing the importance of using enriched samples. These signals were also detected in rumen and correspond to bovine UT-B1 and UT-B2 urea transporters, respectively. Further immunolocalization studies identified that these proteins were located in the ductal system of the parotid gland. This study, therefore, confirmed the presence of UT-B urea transporter protein in the bovine parotid salivary gland.

  17. Forskolin stimulation promotes urea transporter UT-A1 ubiquitination, endocytosis, and degradation in MDCK cells.

    Science.gov (United States)

    Su, Hua; Carter, Conner B; Laur, Oskar; Sands, Jeff M; Chen, Guangping

    2012-11-01

    The adenylyl cyclase stimulator forskolin (FSK) stimulates UT-A1 phosphorylation, membrane trafficking, and urea transport activity. Here, we found that FSK stimulation induces UT-A1 ubiquitination in UT-A1 Madin-Darby canine kidney (MDCK) cells. This suggests that phosphorylation by FSK also triggers the protein degradation machinery for UT-A1. UT-A1-MDCK cells were treated with 100 μg/ml cycloheximide to inhibit protein synthesis, with or without 10 μM FSK. Total UT-A1 protein abundance was significantly reduced after FSK treatment, concomitantly ubiquitinated UT-A1 was increased. We then specifically investigated the effect of FSK on UT-A1 expressed on the cell plasma membrane. FSK treatment accelerated UT-A1 removal from the cell plasma membrane by increasing UT-A1 endocytosis as judged by biotinylation/MesNa treatment and confocal microscopy. We further found that inhibition of the clathrin-mediated endocytic pathway, but not the caveolin-mediated endocytic pathway, significantly blocks FSK-stimulated UT-A1 endocytosis. The PKA inhibitor H89 and the proteasome inhibitors MG132 and lactacystin reduced FSK-induced membrane UT-A1 reduction. Our study shows that FSK activates the UT-A1 urea transporter and the activation/phosphorylation subsequently triggers the downregulation of UT-A1, which represents an important mechanism for the cell to return to the basal conditions after vasopressin stimulation.

  18. Effect of Urea on Activity and Conformation of a Glycoprotein

    Institute of Scientific and Technical Information of China (English)

    WEI Xiang; WANG Xiaoyun; ZHOU Bo; ZHOU Haimeng

    2006-01-01

    The changes of the activity and conformation of Aspergillus niger phytase in urea were detected by farultraviolet circular dichroism (CD) spectra, fluorescence spectra, and enzyme activity assays. The results show that no enzyme activity can be detected after phytase is incubated for 10 h in 3.0 mol/L urea, even though at this urea concentration, less than 20% of the tertiary and secondary structures in the native enzyme changed. The inactivation reaction kinetics is found to be a monophasic first-order reaction, but the unfolding is a biphasic process consisting of two first-order reactions. The inactivation rates of the free enzyme and the substrate-enzyme complex are much faster than the conformational changes during urea denaturation. All of the results indicate that, as a glycoprotein, phytase's activity is strongly dependent on its conformational integrity. The phytase active sites seem to be located in a limited region in the molecule and display more conformational fragility and flexibility to denaturants than enzyme molecular structure as a whole.

  19. Ubiquitination regulates the plasma membrane expression of renal UT-A urea transporters.

    Science.gov (United States)

    Stewart, Gavin S; O'Brien, Jennifer H; Smith, Craig P

    2008-07-01

    The renal UT-A urea transporters UT-A1, UT-A2, and UT-A3 are known to play an important role in the urinary concentrating mechanism. The control of the cellular localization of UT-A transporters is therefore vital to overall renal function. In the present study, we have investigated the effect of ubiquitination on UT-A plasma membrane expression in Madin-Darby canine kidney (MDCK) cell lines expressing each of the three renal UT-A transporters. Inhibition of the ubiquitin-proteasome pathway caused an increase in basal transepithelial urea flux across MDCK-rat (r)UT-A1 and MDCK-mouse (m)UT-A2 monolayers (P UT-A transporter expression in the plasma membrane (P UT-A3 expression in the plasma membrane (P UT-A urea transporters, but that this is not the mechanism primarily used by vasopressin to produce its physiological effects.

  20. Urea adsorption by activated carbon prepared from palm kernel shell

    Science.gov (United States)

    Ooi, Chee-Heong; Sim, Yoke-Leng; Yeoh, Fei-Yee

    2017-07-01

    Dialysis treatment is crucial for patients suffer from renal failure. The dialysis system removes the uremic toxin to a safe level in a patient's body. One of the major limitations of the current hemodialysis system is the capability to efficiently remove uremic toxins from patient's body. Nanoporous materials can be applied to improve the treatment. Palm kernel shell (PKS) biomass generated from palm oil mills can be utilized to prepare high quality nanoporous activated carbon (AC) and applied for urea adsorption in the dialysis system. In this study, AC was prepared from PKS via different carbonization temperatures and followed by carbon dioxide gas activation processes. The physical and chemical properties of the samples were studied. The results show that the porous AC with BET surface areas ranging from 541 to 622 m2g-1 and with total pore volumes varying from 0.254 to 0.297 cm3g-1, are formed with different carbonization temperatures. The equilibrium constant for urea adsorption by AC samples carbonized at 400, 500 and 600 °C are 0.091, 0.287 and 0.334, respectively. The increase of carbonization temperatures from 400 to 600 °C resulted in the increase in urea adsorption by AC predominantly due to increase in surface area. The present study reveals the feasibility of preparing AC with good porosity from PKS and potentially applied in urea adsorption application.

  1. Modulation of sheep ruminal urea transport by ammonia and pH.

    Science.gov (United States)

    Lu, Zhongyan; Stumpff, Friederike; Deiner, Carolin; Rosendahl, Julia; Braun, Hannah; Abdoun, Khalid; Aschenbach, Jörg R; Martens, Holger

    2014-09-01

    Ruminal fermentation products such as short-chain fatty acids (SCFA) and CO2 acutely stimulate urea transport across the ruminal epithelium in vivo, whereas ammonia has inhibitory effects. Uptake and signaling pathways remain obscure. The ruminal expression of SLC14a1 (UT-B) was studied using polymerase chain reaction (PCR). The functional short-term effects of ammonia on cytosolic pH (pHi) and ruminal urea transport across native epithelia were investigated using pH-sensitive microelectrodes and via flux measurements in Ussing chambers. Two variants (UT-B1 and UT-B2) could be fully sequenced from ovine ruminal cDNA. Functionally, transport was passive and modulated by luminal pH in the presence of SCFA and CO2, rising in response to luminal acidification to a peak value at pH 5.8 and dropping with further acidification, resulting in a bell-shaped curve. Presence of ammonia reduced the amplitude, but not the shape of the relationship between urea flux and pH, so that urea flux remained maximal at pH 5.8. Effects of ammonia were concentration dependent, with saturation at 5 mmol/l. Clamping the transepithelial potential altered the inhibitory potential of ammonia on urea flux. Ammonia depolarized the apical membrane and acidified pHi, suggesting that, at physiological pH (urea transport. We conclude that transport of urea across the ruminal epithelium involves proteins subject to rapid modulation by manipulations that alter pHi and the cytosolic concentration of NH4 (+). Implications for epithelial and ruminal homeostasis are discussed.

  2. Mechanisms of molecular transport through the urea channel of Helicobacter pylori

    Science.gov (United States)

    McNulty, Reginald; Ulmschneider, Jakob P.; Luecke, Hartmut; Ulmschneider, Martin B.

    2013-12-01

    Helicobacter pylori survival in acidic environments relies on cytoplasmic hydrolysis of gastric urea into ammonia and carbon dioxide, which buffer the pathogen’s periplasm. Urea uptake is greatly enhanced and regulated by HpUreI, a proton-gated inner membrane channel protein essential for gastric survival of H. pylori. The crystal structure of HpUreI describes a static snapshot of the channel with two constriction sites near the center of the bilayer that are too narrow to allow passage of urea or even water. Here we describe the urea transport mechanism at atomic resolution, revealed by unrestrained microsecond equilibrium molecular dynamics simulations of the hexameric channel assembly. Two consecutive constrictions open to allow conduction of urea, which is guided through the channel by interplay between conserved residues that determine proton rejection and solute selectivity. Remarkably, HpUreI conducts water at rates equivalent to aquaporins, which might be essential for efficient transport of urea at small concentration gradients.

  3. Ammonium and urea transporter inventory of the Selaginella and Physcomitrella genomes

    Directory of Open Access Journals (Sweden)

    Roberto eDe Michele

    2012-04-01

    Full Text Available Ammonium and urea are important nitrogen sources for autotrophic organisms. Plant genomes encode several families of specific transporters for these molecules, plus other uptake mechanisms such as aquaporins and ABC transporters. Selaginella and Physcomitrella are representatives of lycophytes and bryophytes, respectively, and the recent completion of their genome sequences provided us with an opportunity for comparative genome studies, with special emphasis on the adaptive processes that accompanied the conquest of dry land and the evolution of a vascular system. Our phylogenetic analysis revealed that the number of genes encoding urea transporters underwent a progressive reduction during evolution, eventually down to a single copy in vascular plants. Conversely, no clear evolutionary pattern was found for ammonium transporters, and their number and distribution in families varies between species. In particular Selaginella, similar to rice, favors the AMT2/MEP family of ammonium transporters over the plant-specific AMT1 type. In comparison, Physcomitrella presents several members belonging to both families.

  4. Ammonium and urea transporter inventory of the selaginella and physcomitrella genomes.

    Science.gov (United States)

    De Michele, Roberto; Loqué, Dominique; Lalonde, Sylvie; Frommer, Wolf B

    2012-01-01

    Ammonium and urea are important nitrogen sources for autotrophic organisms. Plant genomes encode several families of specific transporters for these molecules, plus other uptake mechanisms such as aquaporins and ABC transporters. Selaginella and Physcomitrella are representatives of lycophytes and bryophytes, respectively, and the recent completion of their genome sequences provided us with an opportunity for comparative genome studies, with special emphasis on the adaptive processes that accompanied the conquest of dry land and the evolution of a vascular system. Our phylogenetic analysis revealed that the number of genes encoding urea transporters underwent a progressive reduction during evolution, eventually down to a single copy in vascular plants. Conversely, no clear evolutionary pattern was found for ammonium transporters, and their number and distribution in families varies between species. In particular Selaginella, similar to rice, favors the AMT2/MEP family of ammonium transporters over the plant-specific AMT1 type. In comparison, Physcomitrella presents several members belonging to both families.

  5. Effects of dietary fibre and protein on urea transport across the cecal mucosa of piglets.

    Science.gov (United States)

    Stumpff, F; Lodemann, U; Van Kessel, A G; Pieper, R; Klingspor, S; Wolf, K; Martens, H; Zentek, J; Aschenbach, J R

    2013-12-01

    In ruminants, gastrointestinal recycling of urea is acutely enhanced by fibre-rich diets that lead to high ruminal concentration of short chain fatty acids (SCFA), while high ammonia has inhibitory effects. This study attempted to clarify if urea flux to the porcine cecum is similarly regulated. Thirty-two weaned piglets were fed diets containing protein (P) of poor prececal digestibility and fibre (F) at high (H) or low levels (L) in a 2 × 2 factorial design. After slaughter, cecal content was analyzed and the cecal mucosa incubated in Ussing chambers to measure the effect of pH, SCFA and NH4 (+) on the flux rates of urea, short-circuit current (I sc) and tissue conductance (G t). NH4 (+) significantly enhanced I sc (from 0.5 ± 0.2 to 1.2 ± 0.1 μEq cm(-2) h(-1)). No acute effects of SCFA or ammonia on urea flux were observed. Tissue conductance was significantly lower in the high dietary fibre groups irrespective of the protein content. Only the HP-LF group emerged as different from all others in terms of urea flux (74 ± 6 versus 53 ± 3 nmol cm(-2) h(-1)), associated with higher cecal ammonia concentration and reduced fecal consistency. The data suggest that as in the rumen, uptake of ammonia by the cecum may involve electrogenic transport of the ionic form (NH4 (+)). In contrast to findings in the rumen, neither a high fibre diet nor acute addition of SCFA enhanced urea transport across the pig cecum. Instead, a HP-LF diet had stimulatory effects. A potential role for urea recycling in stabilizing luminal pH is discussed.

  6. The UT-A1 urea transporter interacts with snapin, a SNARE-associated protein.

    Science.gov (United States)

    Mistry, Abinash C; Mallick, Rickta; Fröhlich, Otto; Klein, Janet D; Rehm, Armin; Chen, Guangping; Sands, Jeff M

    2007-10-12

    The UT-A1 urea transporter mediates rapid transepithelial urea transport across the inner medullary collecting duct and plays a major role in the urinary concentrating mechanism. To transport urea, UT-A1 must be present in the plasma membrane. The purpose of this study was to screen for UT-A1-interacting proteins and to study the interactions of one of the identified potential binding partners with UT-A1. Using a yeast two-hybrid screen of a human kidney cDNA library with the UT-A1 intracellular loop (residues 409-594) as bait, we identified snapin, a ubiquitously expressed SNARE-associated protein, as a novel UT-A1 binding partner. Deletion analysis indicated that the C-terminal coiled-coil domain (H2) of snapin is required for UT-A1 interaction. Snapin binds to the intracellular loop of UT-A1 but not to the N- or C-terminal fragments. Glutathione S-transferase pulldown experiments and co-immunoprecipitation studies verified that snapin interacts with native UT-A1, SNAP23, and syntaxin-4 (t-SNARE partners), indicating that UT-A1 participates with the SNARE machinery in rat kidney inner medulla. Confocal microscopic analysis of immunofluorescent UT-A1 and snapin showed co-localization in both the cytoplasm and in the plasma membrane. When we co-injected UT-A1 with snapin cRNA in Xenopus oocytes, urea influx was significantly increased. In the absence of snapin, the influx was decreased when UT-A1 was combined with t-SNARE components syntaxin-4 and SNAP23. We conclude that UT-A1 may be linked to the SNARE machinery via snapin and that this interaction may be functionally and physiologically important for urea transport.

  7. Urea and NaCl regulate UT-A1 urea transporter in opposing directions via TonEBP pathway during osmotic diuresis.

    Science.gov (United States)

    Kim, Yu-Mi; Kim, Wan-Young; Lee, Hyun-Wook; Kim, Jin; Kwon, H Moo; Klein, Janet D; Sands, Jeff M; Kim, Dongun

    2009-01-01

    In our previous studies of varying osmotic diuresis, UT-A1 urea transporter increased when urine and inner medullary (IM) interstitial urea concentration decreased. The purposes of this study were to examine 1) whether IM interstitial tonicity changes with different urine urea concentrations during osmotic dieresis and 2) whether the same result occurs even if the total urinary solute is decreased. Rats were fed a 4% high-salt diet (HSD) or a 5% high-urea diet (HUD) for 2 wk and compared with the control rats fed a regular diet containing 1% NaCl. The urine urea concentration decreased in HSD but increased in HUD. In the IM, UT-A1 and UT-A3 urea transporters, CLC-K1 chloride channel, and tonicity-enhanced binding protein (TonEBP) transcription factor were all increased in HSD and decreased in HUD. Next, rats were fed an 8% low-protein diet (LPD) or a 0.4% low-salt diet (LSD) to decrease the total urinary solute. Urine urea concentration significantly decreased in LPD but significantly increased in LSD. Rats fed the LPD had increased UT-A1 and UT-A3 in the IM base but decreased in the IM tip, resulting in impaired urine concentrating ability. The LSD rats had decreased UT-A1 and UT-A3 in both portions of the IM. CLC-K1 and TonEBP were unchanged by LPD or LSD. We conclude that changes in CLC-K1, UT-A1, UT-A3, and TonEBP play important roles in the renal response to osmotic diuresis in an attempt to minimize changes in plasma osmolality and maintain water homeostasis.

  8. Mature N-linked glycans facilitate UT-A1 urea transporter lipid raft compartmentalization.

    Science.gov (United States)

    Chen, Guangping; Howe, Ashley G; Xu, Gang; Fröhlich, Otto; Klein, Janet D; Sands, Jeff M

    2011-12-01

    The UT-A1 urea transporter is a glycoprotein with two different glycosylated forms of 97 and 117 kDa. In this study, we found the 117-kDa UT-A1 preferentially resides in lipid rafts, suggesting that the glycosylation status may interfere with UT-A1 lipid raft trafficking. This was confirmed by a site-directed mutagenesis study in MDCK cells. The nonglycosylated UT-A1 showed reduced localization in lipid rafts. By using sugar-specific binding lectins, we further found that the UT-A1 in nonlipid rafts contained a high amount of mannose, as detected by concanavalin A, while the UT-A1 in lipid rafts was the mature N-acetylglucosamine-containing form, as detected by wheat germ agglutinin. In the inner medulla (IM) of diabetic rats, the more abundant 117-kDa UT-A1 in lipid rafts was the mature glycosylation form, with high amounts of N-acetylglucosamine and sialic acid. In contrast, in the IM of normal rats, the predominant 97-kDa UT-A1 was the form enriched in mannose. Functionally, inhibition of glycosylation by tunicamycin or elimination of the glycosylation sites by mutation significantly reduced UT-A1 activity in oocytes. Taken together, our study reveals a new role of N-linked glycosylation in regulating UT-A1 activity by promoting UT-A1 trafficking into membrane lipid raft subdomains.

  9. Energetic and molecular water permeation mechanisms of the human red blood cell urea transporter B.

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    Slim Azouzi

    Full Text Available Urea transporter B (UT-B is a passive membrane channel that facilitates highly efficient permeation of urea. In red blood cells (RBC, while the major function of UT-B is to transport urea, it is assumed that this protein is able to conduct water. Here, we have revisited this last issue by studying RBCs and ghosts from human variants with defects of aquaporin 1 (AQP1 or UT-B. We found that UT-B's osmotic water unit permeability (pfunit is similar to that of AQP1. The determination of diffusional permeability coefficient (Pd allowed the calculation of the Pf/Pd ratio, which is consistent with a single-file water transport. Molecular dynamic simulations of water conduction through human UT-B confirmed the experimental finding. From these results, we propose an atomistic description of water-protein interactions involved in this permeation. Inside the UT-B pore, five water molecules were found to form a single-file and move rapidly along a channel by hydrogen bond exchange involving two critical threonines. We further show that the energy barrier for water located in the central region coincides with a water dipole reorientation, which can be related to the proton exclusion observed experimentally. In conclusion, our results indicate that UT-B should be considered as a new member of the water channel family.

  10. Effect of nickel nutrition on yield, urea accumulation and urease enzyme activity of lettuce

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    M. Afyuni

    2011-04-01

    Full Text Available Although nickel (Ni is known as an essential element for higher plants, the biological effects of this nutrient on growth, yield, and N metabolism of some plants, particularly leafy vegetables, is still unknown. Therefore, this study was carried out to investigate the effects of Ni and urea nutrition on the growth and yield of lettuce (Lactuca sativa L. cv. Baker and urea accumulation in plant tissues. In this study, nitrogen was supplied from the source of urea or ammonium nitrate at three levels (5, 10 and 20 mM and Ni was supplied in the form of NiCl2 at two levels (0 and 0.04 µM. The plants were harvested 6 weeks after transplanting and the fresh weight of shoots and roots were determined. The shoots urea concentration and activity of urease enzyme in the leaves were also measured. The results indicated that shoots fresh weight of the urea-fed plants increased with increasing urea concentration in the nutrient solution. Addition of Ni to the nutrient solution significantly promoted the root and shoots fresh weight of urea-fed plants, regardless of N level. Ni nutrition significantly increased the urease activity in the lettuce leaves and as a result, reduced urea accumulation in the shoots and toxicity effects of urea. Therefore, it seems that urea in combination with Ni can successfully be used in production of lettuce in soilless culture systems.

  11. Triazolothienopyrimidine inhibitors of urea transporter UT-B reduce urine concentration.

    Science.gov (United States)

    Yao, Chenjuan; Anderson, Marc O; Zhang, Jicheng; Yang, Baoxue; Phuan, Puay-Wah; Verkman, A S

    2012-07-01

    Urea transport (UT) proteins facilitate the concentration of urine by the kidney, suggesting that inhibition of these proteins could have therapeutic use as a diuretic strategy. We screened 100,000 compounds for UT-B inhibition using an optical assay based on the hypotonic lysis of acetamide-loaded mouse erythrocytes. We identified a class of triazolothienopyrimidine UT-B inhibitors; the most potent compound, UTB(inh)-14, fully and reversibly inhibited urea transport with IC(50) values of 10 nM and 25 nM for human and mouse UT-B, respectively. UTB(inh)-14 competed with urea binding at an intracellular site on the UT-B protein. UTB(inh)-14 exhibited low toxicity and high selectivity for UT-B over UT-A isoforms. After intraperitoneal administration of UTB(inh)-14 in mice to achieve predicted therapeutic concentrations in the kidney, urine osmolality after administration of 1-deamino-8-D-arginine-vasopressin was approximately 700 mosm/kg H(2)O lower in UTB(inh)-14-treated mice than vehicle-treated mice. UTB(inh)-14 also increased urine output and reduced urine osmolality in mice given free access to water. UTB(inh)-14 did not reduce urine osmolality in UT-B knockout mice. In summary, these data provide proof of concept for the potential utility of UT inhibitors to reduce urinary concentration in high-vasopressin, fluid-retaining conditions. The diuretic mechanism of UT inhibitors may complement the action of conventional diuretics, which target sodium transport.

  12. UT-B Urea Transporter Localization in the Bovine Gastrointestinal Tract.

    Science.gov (United States)

    Coyle, J; McDaid, S; Walpole, C; Stewart, Gavin S

    2016-04-01

    Facilitative UT-B urea transporters play an important role in the urea nitrogen salvaging process that occurs in the gastrointestinal tract of mammals, particularly ruminants. Gastrointestinal UT-B transporters have previously been reported in various ruminant species-including cow, sheep and goat. In this present study, UT-B transporter localization was investigated in tissues throughout the bovine gastrointestinal tract. RT-PCR analysis showed that UT-B2 was the predominant UT-B mRNA transcript expressed in dorsal, ventral and cranial ruminal sacs, while alternative UT-B transcripts were present in other gastrointestinal tissues. Immunoblotting analysis detected a strong, glycosylated ~50 kDa UT-B2 protein in all three ruminal sacs. Immunolocalization studies showed that UT-B2 protein was predominantly localized to the plasma membrane of cells in the stratum basale layer of all ruminal sac papillae. In contrast, other UT-B protein staining was detected in the basolateral membranes of the surface epithelial cells lining the abomasum, colon and rectum. Overall, these findings confirm that UT-B2 cellular localization is similar in all ruminal sacs and that other UT-B proteins are located in epithelial cells lining various tissues in the bovine gastrointestinal tract.

  13. Depolymerization of cortical actin inhibits UT-A1 urea transporter endocytosis but promotes forskolin-stimulated membrane trafficking.

    Science.gov (United States)

    Xu, Gang; Su, Hua; Carter, Conner B; Fröhlich, Otto; Chen, Guangping

    2012-04-01

    The cytoskeleton participates in many aspects of transporter protein regulation. In this study, by using yeast two-hybrid screening, we identified the cytoskeletal protein actin as a binding partner with the UT-A1 urea transporter. This suggests that actin plays a role in regulating UT-A1 activity. Actin specifically binds to the carboxyl terminus of UT-A1. A serial mutation study shows that actin binding to UT-A1's carboxyl terminus was abolished when serine 918 was mutated to alanine. In polarized UT-A1-MDCK cells, cortical filamentous (F) actin colocalizes with UT-A1 at the apical membrane and the subapical cytoplasm. In the cell surface, both actin and UT-A1 are distributed in the lipid raft microdomains. Disruption of the F-actin cytoskeleton by latrunculin B resulted in UT-A1 accumulation in the cell membrane as measured by biotinylation. This effect was mainly due to inhibition of UT-A1 endocytosis in both clathrin and caveolin-mediated endocytic pathways. In contrast, actin depolymerization facilitated forskolin-stimulated UT-A1 trafficking to the cell surface. Functionally, depolymerization of actin by latrunculin B significantly increased UT-A1 urea transport activity in an oocyte expression system. Our study shows that cortical F-actin not only serves as a structural protein, but directly interacts with UT-A1 and plays an important role in controlling UT-A1 cell surface expression by affecting both endocytosis and trafficking, therefore regulating UT-A1 bioactivity.

  14. THE INFLUENCE OF PVA.cl.CITRIC ACID/CHITOSAN MEMBRANE HYDROPHICILITY ON THE TRANSPORT OF CREATININE AND UREA

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    Retno Ariadi Lusiana

    2013-12-01

    Full Text Available The influence of cross-linking and membrane hydrophilicity on the transport rate had been studied using a membrane prepared from a mixture of chitosan/PVA cross-linked citric acid (PVA.cl.CA for creatinine and urea transport. The optimum mole ratio of PVA:citric acid as well as the best composition of chitosan:PVA.cl.CA were determined using creatinine transport study. Using the optimum compositions, further study was done using different thickness of the membrane in transporting creatinine, urea and a mixture of 3 species (creatinine, urea and vitamin B12. Membrane characterization was done using FT-IR spectrophotometer, water absorption test, TG/DTG and SEM. The results showed that the optimum composition PVA:citric acid was obtained to be 90:1, having % WU of 113.74% and creatinine transport percentage of 18.16%. Meanwhile, the optimum composition of chitosan:PVA.cl.CA was found at 4:6 ratio having % WU and % transport of 136.67% and 24.26%, respectively. The optimum transport capacity was found for membrane thickness of 50 µm with WU% at 139.61% and the percent transport of creatinine and urea each was 38.93% and 60.36%. The presence vitamin B12 in the solution of is proved to disturb the transport of creatinine and urea through the membrane. Finally, hydrophilicity seemed to give substantial contribution in the transport process as well as the mechanical strength of the membrane.

  15. Diuresis and reduced urinary osmolality in rats produced by small-molecule UT-A-selective urea transport inhibitors.

    Science.gov (United States)

    Esteva-Font, Cristina; Cil, Onur; Phuan, Puay-Wah; Su, Tao; Lee, Sujin; Anderson, Marc O; Verkman, A S

    2014-09-01

    Urea transport (UT) proteins of the UT-A class are expressed in epithelial cells in kidney tubules, where they are required for the formation of a concentrated urine by countercurrent multiplication. Here, using a recently developed high-throughput assay to identify UT-A inhibitors, a screen of 50,000 synthetic small molecules identified UT-A inhibitors of aryl-thiazole, γ-sultambenzosulfonamide, aminocarbonitrile butene, and 4-isoxazolamide chemical classes. Structure-activity analysis identified compounds that inhibited UT-A selectively by a noncompetitive mechanism with IC50 down to ∼1 μM. Molecular modeling identified putative inhibitor binding sites on rat UT-A. To test compound efficacy in rats, formulations and administration procedures were established to give therapeutic inhibitor concentrations in blood and urine. We found that intravenous administration of an indole thiazole or a γ-sultambenzosulfonamide at 20 mg/kg increased urine output by 3-5-fold and reduced urine osmolality by ∼2-fold compared to vehicle control rats, even under conditions of maximum antidiuresis produced by 1-deamino-8-D-arginine vasopressin (DDAVP). The diuresis was reversible and showed urea > salt excretion. The results provide proof of concept for the diuretic action of UT-A-selective inhibitors. UT-A inhibitors are first in their class salt-sparing diuretics with potential clinical indications in volume-overload edemas and high-vasopressin-associated hyponatremias.

  16. Serosal-to-mucosal urea flux across the isolated ruminal epithelium is mediated via urea transporter-B and aquaporins when Holstein calves are abruptly changed to a moderately fermentable diet.

    Science.gov (United States)

    Walpole, M E; Schurmann, B L; Górka, P; Penner, G B; Loewen, M E; Mutsvangwa, T

    2015-02-01

    Urea transport (UT-B) proteins are known to facilitate urea movement across the ruminal epithelium; however, other mechanisms may be involved as well because inhibiting UT-B does not completely abolish urea transport. Of the aquaporins (AQP), which are a family of membrane-spanning proteins that are predominantly involved in the movement of water, AQP-3, AQP-7, and AQP-10 are also permeable to urea, but it is not clear if they contribute to urea transport across the ruminal epithelium. The objectives of this study were to determine (1) the functional roles of AQP and UT-B in the serosal-to-mucosal urea flux (Jsm-urea) across rumen epithelium; and (2) whether functional adaptation occurs in response to increased diet fermentability. Twenty-five Holstein steer calves (n=5) were assigned to a control diet (CON; 91.5% hay and 8.5% vitamin and mineral supplement) or a medium grain diet (MGD; 41.5% barley grain, 50% hay, and 8.5% vitamin and mineral) that was fed for 3, 7, 14, or 21 d. Calves were killed and ruminal epithelium was collected for mounting in Ussing chambers under short-circuit conditions and for analysis of mRNA abundance of UT-B and AQP-3, AQP-7, and AQP-10. To mimic physiologic conditions, the mucosal buffer (pH 6.2) contained no urea, whereas the serosal buffer (pH 7.4) contained 1 mM urea. The fluxes of (14)C-urea (Jsm-urea; 26 kBq/10 mL) and (3)H-mannitol (Jsm-mannitol; 37 kBq/10 mL) were measured, with Jsm-mannitol being used as an indicator of paracellular or hydrophilic movement. Serosal addition of phloretin (1 mM) was used to inhibit UT-B-mediated urea transport, whereas NiCl2 (1 mM) was used to inhibit AQP-mediated urea transport. Across treatments, the addition of phloretin or NiCl2 reduced the Jsm-urea from 116.5 to 54.0 and 89.5 nmol/(cm(2) × h), respectively. When both inhibitors were added simultaneously, Jsm-urea was further reduced to 36.8 nmol/(cm(2) × h). Phloretin-sensitive and NiCl2-sensitive Jsm-urea were not affected by diet. The

  17. CsNIP2;1 is a Plasma Membrane Transporter from Cucumis sativus that Facilitates Urea Uptake When Expressed in Saccharomyces cerevisiae and Arabidopsis thaliana.

    Science.gov (United States)

    Zhang, Lu; Yan, Jiapei; Vatamaniuk, Olena K; Du, Xiangge

    2016-03-01

    Urea is an important source of nitrogen (N) for the growth and development of plants. It occurs naturally in soils, is the major N source in agricultural fertilizers and is an important N metabolite in plants. Therefore, the identification and characterization of urea transporters in higher plants is important for the fundamental understanding of urea-based N nutrition in plants and for designing novel strategies for improving the N-use efficiency of urea based-fertilizers. Progress in this area, however, is hampered due to scarce knowledge of plant urea transporters. From what is known, urea uptake from the soil into plant roots is mediated by two types of transporters: the major intrinsic proteins (MIPs) and the DUR3 orthologs, mediating low- and high-affinity urea transport, respectively. Here we characterized a MIP family member from Cucumis sativus, CsNIP2;1, with regard to its contribution to urea transport. We show that CsNIP2;1 is a plasma membrane transporter that mediates pH-dependent urea uptake when expressed in yeast. We also found that ectopic expression of CsNIP2;1 improves growth of wild-type Arabidopsis thaliana and rescues growth and development of the atdur3-3 mutant on medium with urea as the sole N source. In addition, CsNIP2;1 is transcriptionally up-regulated by N deficiency, urea and NO3 (-). These data and results from the analyses of the pattern of CsNIP2;1 expression in A. thaliana and cucumber suggest that CsNIP2;1 might be involved in multiple steps of urea-based N nutrition, including urea uptake and internal transport during N remobilization throughout seed germination and N delivery to developing tissues.

  18. Clinical aspects of urea cycle dysfunction and altered brain energy metabolism on modulation of glutamate receptors and transporters in acute and chronic hyperammonemia.

    Science.gov (United States)

    Natesan, Vijayakumar; Mani, Renuka; Arumugam, Ramakrishnan

    2016-07-01

    In living organisms, nitrogen arise primarily as ammonia (NH3) and ammonium (NH4(+)), which is a main component of the nucleic acid pool and proteins. Although nitrogen is essential for growth and maintenance in animals, but when the nitrogenous compounds exceeds the normal range which can quickly lead to toxicity and death. Urea cycle is the common pathway for the disposal of excess nitrogen through urea biosynthesis. Hyperammonemia is a consistent finding in many neurological disorders including congenital urea cycle disorders, reye's syndrome and acute liver failure leads to deleterious effects. Hyperammonemia and liver failure results in glutamatergic neurotransmission which contributes to the alteration in the function of the glutamate-nitric oxide-cGMP pathway, modulates the important cerebral process. Even though ammonia is essential for normal functioning of the central nervous system (CNS), in particular high concentrations of ammonia exposure to the brain leads to the alterations of glutamate transport by the transporters. Several glutamate transporters have been recognized in the central nervous system and each has a unique physiological property and distribution. The loss of glutamate transporter activity in brain during acute liver failure and hyperammonemia is allied with increased extracellular brain glutamate concentrations which may be conscientious for the cerebral edema and ultimately cell death.

  19. Salt-sparing diuretic action of a water-soluble urea analog inhibitor of urea transporters UT-A and UT-B in rats.

    Science.gov (United States)

    Cil, Onur; Esteva-Font, Cristina; Tas, Sadik Taskin; Su, Tao; Lee, Sujin; Anderson, Marc O; Ertunc, Mert; Verkman, Alan S

    2015-08-01

    Inhibitors of kidney urea transporter (UT) proteins have potential use as salt-sparing diuretics ('urearetics') with a different mechanism of action than diuretics that target salt transporters. To study UT inhibition in rats, we screened about 10,000 drugs, natural products and urea analogs for inhibition of rat UT-A1. Drug and natural product screening found nicotine, sanguinarine and an indolcarbonylchromenone with IC50 of 10-20 μM. Urea analog screening found methylacetamide and dimethylthiourea (DMTU). DMTU fully and reversibly inhibited rat UT-A1 and UT-B by a noncompetitive mechanism with IC50 of 2-3 mM. Homology modeling and docking computations suggested DMTU binding sites on rat UT-A1. Following a single intraperitoneal injection of 500 mg/kg DMTU, peak plasma concentration was 9 mM with t1/2 of about 10 h, and a urine concentration of 20-40 mM. Rats chronically treated with DMTU had a sustained, reversible reduction in urine osmolality from 1800 to 600 mOsm, a 3-fold increase in urine output, and mild hypokalemia. DMTU did not impair urinary concentrating function in rats on a low protein diet. Compared to furosemide-treated rats, the DMTU-treated rats had greater diuresis and reduced urinary salt loss. In a model of syndrome of inappropriate antidiuretic hormone secretion, DMTU treatment prevented hyponatremia and water retention produced by water-loading in dDAVP-treated rats. Thus, our results establish a rat model of UT inhibition and demonstrate the diuretic efficacy of UT inhibition.

  20. Altered Renal Expression of Relevant Clinical Drug Transporters in Different Models of Acute Uremia in Rats. Role of Urea Levels

    Directory of Open Access Journals (Sweden)

    Anabel Brandoni

    2015-06-01

    Full Text Available Background/Aims: Organic anion transporter 1 (Oat1 and 3 (Oat3 are organic anion transporters that play critical roles in the body disposition of numerous clinically important drugs. We investigated the effects of acute uremia on the renal expression of Oat1 and Oat3 in three in vivo experimental models of acute kidney injury (AKI: induced by ischemia, by ureteral obstruction and by the administration of HgCl2. We also evaluated the influence of urea in the expression of these transporters in proximal tubular cells suspensions. Methods: Membranes were isolated from kidneys of each experimental group and from cell suspensions incubated with different urea concentrations. Oat1 and Oat3 expressions were performed by immunoblotting. Results: A good correlation between uremia and the renal protein expression of Oat1 and Oat3 was observed in vivo. Moreover, the incubation of isolated proximal tubular cells with different concentrations of urea decreases protein expression of Oat1 and Oat3 in plasma membranes in a dose-dependent manner. Conclusion: The more severe the renal failure, the more important is the decrease in protein expression of the transporters in renal membranes where they are functional. The in vitro study demonstrates that urea accounts, at least in part, for the decreased expression of Oat1 and Oat3 in proximal tubule plasma membranes.

  1. Arginase activity, urea, and hydroxyproline concentration are reduced in keratoconus keratocytes.

    Science.gov (United States)

    Stachon, Tanja; Kolev, Krasimir; Flaskó, Zsuzsa; Seitz, Berthold; Langenbucher, Achim; Szentmáry, Nóra

    2017-01-01

    Keratoconus (KC) is a disease characterized by thinning and deformation of the cornea, but its etiology remains unknown. Seventy percent of the corneal stroma consists of collagen, which is composed of three intertwined polypeptide chains with glycine-hydroxyproline-proline repeats along their sequence. Arginase is a cytoplasmatic enzyme and catalyzes the conversion of arginine to urea and ornithine, which serves as a precursor for the endogenous synthesis of proline and hydroxyproline. The purpose of this study was to analyze arginase activity, as well as collagen and urea formation in normal and KC-keratocytes and to determine the impact of urea on keratocyte viability and proliferation in vitro. Primary human keratocytes were isolated by digestion in collagenase (1.0 mg/mL) from surgically removed corneas of eight keratoconus patients and eight normal human corneal buttons and cultured in DMEM/Ham's F12 medium supplemented with 5 % fetal calf serum. Arginase activity and urea concentration were measured in cell-lysates, hydroxyproline concentration in supernatant of cultured keratocytes using colorimetric assay. Cell viability and cell proliferation of cultured keratocytes were assessed after treatment with urea at concentrations up to10 mM for 24 h using assays for metabolic activity and DNA replication. Arginase activity and urea concentration in KC-keratocytes decreased by about 50 % compared to normal keratocytes (p = 0.003 and p = 0.008). Hydroxyproline synthesized by cultured KC-keratocytes was also approximately 50 % less compared to normal keratocytes (p = 0.02) and this difference decreased following treatment with 5.0 or 10.0 mM urea (p = 0.02; 0.03), without any change in cell viability (p > 0.09). However, the urea treatment increased modestly (by 20 %) the proliferation rate of KC-keratocytes (p = 0.04; 0.04; 0.04), without any effect on normal cultured keratocytes (p > 0.09). We identified suppressed arginase

  2. Effects of dietary fibre and protein on urea transport across the cecal mucosa of piglets

    NARCIS (Netherlands)

    Stumpff, F.; Lodemann, U.; Kessel, A.G. van; Pieper, R.; Klingspor, S.; Wolf, K. van der; Martens, H.; Zentek, J.; Aschenbach, J.R.

    2013-01-01

    In ruminants, gastrointestinal recycling of urea is acutely enhanced by fibre-rich diets that lead to high ruminal concentration of short chain fatty acids (SCFA), while high ammonia has inhibitory effects. This study attempted to clarify if urea flux to the porcine cecum is similarly regulated. Thi

  3. Cloning and functional characterization of a second urea transporter from the kidney of the Atlantic stingray, Dasyatis sabina.

    Science.gov (United States)

    Janech, Michael G; Fitzgibbon, Wayne R; Nowak, Mark W; Miller, Donald H; Paul, Richard V; Ploth, David W

    2006-09-01

    The cloning of cDNAs encoding facilitated urea transporters (UTs) from the kidneys of the elasmobranchs indicates that in these fish renal urea reabsorption occurs, at least in part, by passive processes. The previously described elasmobranch urea transporter clones from shark (shUT) and stingray (strUT-1) differ from each other primarily because of the COOH-terminus of the predicted strUT-1 translation product being extended by 51-amino acid residues compared with shUT. Previously, we noted multiple UT transcripts were present in stingray kidney. We hypothesized that a COOH terminally abbreviated UT isoform, homologous to shUT, would also be present in stingray kidney. Therefore, we used 5'/3' rapid amplification of cDNA ends to identify a 3'UTR-variant (strUT-1a) of the cDNA that encodes (strUT-1), as well as three, 3'UTR-variant cDNAs (strUT-2a,b,c) that encode a second phloretin-sensitive, urea transporter (strUT-2). The 5'UTR and the first 1,132 nucleotides of the predicted coding region of the strUT-2 cDNAs are identical to the strUT-1 cDNAs. The remainder of the coding region contains only five novel nucleotides. The strUT-2 cDNAs putatively encode a 379-amino acid protein, the first 377 amino acids identical to strUT-1 plus 2 additional amino acids. We conclude that 1) a second UT isoform is expressed in the Atlantic stingray and that this isoform is similar in size to the UT previously cloned from the kidney of the dogfish shark, and 2) at least five transcripts encoding the 2 stingray UTs are derived from a single gene product through alternative splicing and polyadenylation.

  4. Expression and localization of a UT-B urea transporter in the human bladder.

    Science.gov (United States)

    Walpole, C; Farrell, A; McGrane, A; Stewart, G S

    2014-11-01

    Facilitative UT-B urea transporters have been shown to play an important role in the urinary concentrating mechanism. Recent studies have now suggested a link between UT-B allelic variation and human bladder cancer risk. UT-B1 protein has been previously identified in the bladder of various mammalian species, but not yet in humans. The aim of the present study was to investigate whether any UT-B protein was present in the human bladder. First, RT-PCR results confirmed that UT-B1 was strongly expressed at the RNA level in the human bladder, whereas UT-B2 was only weakly present. Initial Western blot analysis confirmed that a novel UT-B COOH-terminal antibody detected human UT-B proteins. Importantly, this antibody detected a specific 40- to 45-kDa UT-B signal in human bladder protein. Using a peptide-N-glycosidase F enzyme, this bladder UT-B signal was deglycosylated to a core 30-kDa protein, which is smaller than the predicted size for UT-B1 but similar to many proteins reported to be UT-B1. Finally, immunolocalization experiments confirmed that UT-B protein was strongly expressed throughout all urothelium layers except for the apical membrane of the outermost umbrella cells. In conclusion, these data confirm the presence of UT-B protein within the human bladder. Further studies are now required to determine the precise nature, regulation, and physiological role of this UT-B.

  5. Application of a data assimilation method via an ensemble Kalman filter to reactive urea hydrolysis transport modeling

    Energy Technology Data Exchange (ETDEWEB)

    Juxiu Tong; Bill X. Hu; Hai Huang; Luanjin Guo; Jinzhong Yang

    2014-03-01

    With growing importance of water resources in the world, remediations of anthropogenic contaminations due to reactive solute transport become even more important. A good understanding of reactive rate parameters such as kinetic parameters is the key to accurately predicting reactive solute transport processes and designing corresponding remediation schemes. For modeling reactive solute transport, it is very difficult to estimate chemical reaction rate parameters due to complex processes of chemical reactions and limited available data. To find a method to get the reactive rate parameters for the reactive urea hydrolysis transport modeling and obtain more accurate prediction for the chemical concentrations, we developed a data assimilation method based on an ensemble Kalman filter (EnKF) method to calibrate reactive rate parameters for modeling urea hydrolysis transport in a synthetic one-dimensional column at laboratory scale and to update modeling prediction. We applied a constrained EnKF method to pose constraints to the updated reactive rate parameters and the predicted solute concentrations based on their physical meanings after the data assimilation calibration. From the study results we concluded that we could efficiently improve the chemical reactive rate parameters with the data assimilation method via the EnKF, and at the same time we could improve solute concentration prediction. The more data we assimilated, the more accurate the reactive rate parameters and concentration prediction. The filter divergence problem was also solved in this study.

  6. Thiazolopyridone ureas as DNA gyrase B inhibitors: optimization of antitubercular activity and efficacy.

    Science.gov (United States)

    Kale, Ramesh R; Kale, Manoj G; Waterson, David; Raichurkar, Anandkumar; Hameed, Shahul P; Manjunatha, M R; Kishore Reddy, B K; Malolanarasimhan, Krishnan; Shinde, Vikas; Koushik, Krishna; Jena, Lalit Kumar; Menasinakai, Sreenivasaiah; Humnabadkar, Vaishali; Madhavapeddi, Prashanti; Basavarajappa, Halesha; Sharma, Sreevalli; Nandishaiah, Radha; Mahesh Kumar, K N; Ganguly, Samit; Ahuja, Vijaykamal; Gaonkar, Sheshagiri; Naveen Kumar, C N; Ogg, Derek; Boriack-Sjodin, P Ann; Sambandamurthy, Vasan K; de Sousa, Sunita M; Ghorpade, Sandeep R

    2014-02-01

    Scaffold hopping from the thiazolopyridine ureas led to thiazolopyridone ureas with potent antitubercular activity acting through inhibition of DNA GyrB ATPase activity. Structural diversity was introduced, by extension of substituents from the thiazolopyridone N-4 position, to access hydrophobic interactions in the ribose pocket of the ATP binding region of GyrB. Further optimization of hydrogen bond interactions with arginines in site-2 of GyrB active site pocket led to potent inhibition of the enzyme (IC50 2 nM) along with potent cellular activity (MIC=0.1 μM) against Mycobacterium tuberculosis (Mtb). Efficacy was demonstrated in an acute mouse model of tuberculosis on oral administration.

  7. Synthesis and biological activity of substituted urea and thiourea derivatives containing 1,2,4-triazole moiety

    Science.gov (United States)

    A series of novel thiourea and urea derivatives carrying 1,2,4-triazole moiety were synthesized and evaluated for their antifungal and larvicidal activity. Thiourea (1a-e) and urea derivatives (2a-e) were prepared by reacting 4-(aminophenyl)acetic acid with corresponding isothiocyanates and isocyana...

  8. Surface electrocardiogram and action potential in mice lacking urea transporter UT-B.

    Science.gov (United States)

    Meng, Yan; Zhao, Chunyan; Zhang, Xuexin; Zhao, Huashan; Guo, Lirong; Lü, Bin; Zhao, Xuejian; Yang, Baoxue

    2009-05-01

    UT-B is a urea transporter protein expressed in the kidney and in many non-renal tissues including erythrocytes, brain, heart, bladder and the testis. The objective of this study was to determine the phenotype of UT-B deletion in the heart. UT-B expression in the heart was studied in wild-type mice vs UT-B null mice by utilizing RT-PCR and Western blot. A surface electrocardiogram (ECG) recording (lead II) was measured in wild-type mice and UT-B null mice at the ages of 6, 16 and 52 weeks. For the action potential recording, the ventricular myocytes of 16 w mice were isolated and recorded by floating microelectrode method. The sodium current was recorded by the patch clamp technique. RT-PCR and Western blot showed the UT-B expression in the heart of wild-type mice. No UT-B transcript and protein was found in UT-B null mice. The ECG recording showed that the P-R interval was significantly prolonged in UT-B null mice ((43.5 +/- 4.2), (45.5 +/- 6.9) and (43.8 +/- 7.6) ms at ages of 6, 16 and 52 weeks) vs wild-type mice ((38.6 +/- 2.9), (38.7 +/- 5.6) and (38.2 +/- 7.3) ms, PUT-B null mice (52 w old). The amplitude of action potential and V (max) decreased significantly in UT-B null mice ((92.17 +/- 10.56) and (101.89 +/- 9.54) mV/s) vs those in wild-type mice (vs (110.51 +/- 10.38) and (109.53 +/- 10.64) mV/s, PUT-B null mice ((123.83 +/- 11.17) and (195.43 +/- 16.41) ms) vs that in wild-type mice ((108.27 +/- 10.85) and (171.00 +/- 15.53) ms, PUT-B null mice (-8.80 +/- 0.92) nA vs that in wild-type mice ((-5.98 +/- 1.07) nA, PUT-B deletion causes progressive heart block in mice.

  9. Urea and carbamate derivatives of primaquine: synthesis, cytostatic and antioxidant activities.

    Science.gov (United States)

    Simunović, M; Perković, I; Zorc, B; Ester, K; Kralj, M; Hadjipavlou-Litina, D; Pontiki, E

    2009-08-01

    The novel urea primaquine derivatives 3 were prepared by aminolysis of primaquine benzotriazolide 2 with several hydroxyamines and ethylendiamine, while carbamates 4 were synthesized from the same precursor 2 and alcohols. All compounds are fully chemically characterized and evaluated for their cytostatic and antioxidant activities. The most prominent antiproliferative activity was obtained by compounds 3c, 3d, 3g, and 5b (IC(50)=9-40 microM). 1-(5-Hydroxypentyl)-3-[4-(6-methoxy-quinolin-8-ylamino)-pentyl]urea (3c) showed extreme selectivity toward SW 620 colon cancer cells (IC(50)=0.2 microM) and a bit less toward lung cancer cells H 460. Hydroxyurea 3h showed the highest interaction with DPPH. Primaquine twin drug 3g showed very significant inhibition on LOX soybean (IC(50)=62 microM). Almost all the tested derivatives highly inhibited lipid peroxidation, significantly stronger than primaquine phosphate.

  10. Influence of exogenous urea on photosynthetic pigments, (14)CO 2 uptake, and urease activity in Elodea densa-environmental implications.

    Science.gov (United States)

    Maleva, Maria; Borisova, Galina; Chukina, Nadezda; Nekrasova, Galina; Prasad, M N V

    2013-09-01

    This paper analyzes the effect of exogenous urea in increased concentration gradient (0, 100, 500 and 1,000 mg L(-1)) on photosynthetic pigments (measured spectrophotometrically), uptake of (14)CO2 (using radioisotope), and urease activity (by measuring ammonia with Nessler's reagent) in leaves of Elodea densa Planch. We have observed that low concentration of urea (100 mg L(-1)) stimulates the accumulation of photosynthetic pigments and intensifies photosynthesis in E. densa, whereas high concentration (1,000 mg L(-1)) suppresses these processes. Urease activity increased by approximately 2.7 and 8 fold when exogenous urea concentrations were 100 and 500 mg L(-1), respectively. However, exogenous urea in high concentration (1,000 mg L(-1)) decreased urease activity by 1.5 fold compared to the control. The necessity of mitigating urea and other nitrogen-containing compounds (NH3 from urea) in water bodies has been discussed with emphasis on the potential for phytoremediation of urea using common water weed viz. E. densa.

  11. Surface electrocardiogram and action potential in mice lacking urea transporter UT-B

    Institute of Scientific and Technical Information of China (English)

    MENG Yan; ZHAO ChunYan; ZHANG XueXin; ZHAO HuaShan; GUO LiRong; Lü Bin; ZHAO XueJian; YANG BaoXue

    2009-01-01

    UT-B is a urea transporter protein expressed in the kidney and in many non-renal tissues including erythrocytes, brain, heart, bladder and the testis. The objective of this study was to determine the phenotype of UT-B deletion in the heart. UT-B expression in the heart was studied in wild-type mice vs UT-B null mice by utilizing RT-PCR and Western blot. A surface electrocardiogram (ECG) recording (lead Ⅱ) was measured in wild-type mice and UT-B null mice at the ages of 6, 16 and 52 weeks. For the action potential recording, the ventricular myocytes of 16 w mice were isolated and recorded by float-ing microelectrode method. The sodium current was recorded by the patch clamp technique. RT-PCR and Western blot showed the UT-B expression in the heart of wild-type mice. No UT-B transcript and protein was found in UT-B null mice. The ECG recording showed that the P-R interval was significantly prolonged in UT-B null mice ((43.5±4.2), (45.5±6.9) and (43.8±7.6) ms at ages of 6, 16 and 52 weeks) vs wild-type mice ((38.6±2.9), (38.7±5.6) and (38.2±7.3) ms, P<0.05). The atrial ventricular heart block type Ⅱ and Ⅲ only appeared in the aging UT-B null mice (52 w old). The amplitude of action potential and Vmax decreased significantly in UT-B null mice ((92.17±10.56) and (101.89±9.54) mV/s) vs those in wild-type mice (vs (110.51±10.38) and (109.53±10.64) mV/s, P<0.05). The action potential duration at 50% and 90% (APD50 and APD90) was significantly prolonged in UT-B null mice ((123.83±11.17) and (195.43±16.41) ms) vs that in wild-type mice ((108.27±10.85) and (171.00±15.53) ms, P<0.05). The maximal sodium current decreased significantly in UT-B null mice (-8.80±0.92) nA vs that in wild-type mice ((-5.98±1.07) nA, P<0.05). These results provide the first evidence that UT-B deletion causes progressive heart block in mice.

  12. Surface electrocardiogram and action potential in mice lacking urea transporter UT-B

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    UT-B is a urea transporter protein expressed in the kidney and in many non-renal tissues including erythrocytes, brain, heart, bladder and the testis. The objective of this study was to determine the phenotype of UT-B deletion in the heart. UT-B expression in the heart was studied in wild-type mice vs UT-B null mice by utilizing RT-PCR and Western blot. A surface electrocardiogram (ECG) recording (lead II) was measured in wild-type mice and UT-B null mice at the ages of 6, 16 and 52 weeks. For the action potential recording, the ventricular myocytes of 16 w mice were isolated and recorded by floating microelectrode method. The sodium current was recorded by the patch clamp technique. RT-PCR and Western blot showed the UT-B expression in the heart of wild-type mice. No UT-B transcript and protein was found in UT-B null mice. The ECG recording showed that the P-R interval was significantly prolonged in UT-B null mice ((43.5 ± 4.2), (45.5 ± 6.9) and (43.8 ± 7.6) ms at ages of 6, 16 and 52 weeks) vs wild-type mice ((38.6 ± 2.9), (38.7 ± 5.6) and (38.2 ± 7.3) ms, P<0.05). The atrial ventricular heart block type II and III only appeared in the aging UT-B null mice (52 w old). The amplitude of action potential and Vmax decreased significantly in UT-B null mice ((92.17 ± 10.56) and (101.89 ± 9.54) mV/s) vs those in wild-type mice (vs (110.51 ± 10.38) and (109.53 ± 10.64) mV/s, P<0.05). The action potential duration at 50% and 90% (APD50 and APD90) was significantly prolonged in UT-B null mice ((123.83 ± 11.17) and (195.43 ± 16.41) ms) vs that in wild-type mice ((108.27 ± 10.85) and (171.00 ± 15.53) ms, P<0.05). The maximal sodium current decreased significantly in UT-B null mice (-8.80 ± 0.92) nA vs that in wild-type mice ((-5.98 ± 1.07) nA, P<0.05). These results provide the first evidence that UT-B deletion causes progressive heart block in mice.

  13. Design, synthesis and antiproliferative activities of diaryl urea derivatives bearing N-acylhydrazone moiety

    Institute of Scientific and Technical Information of China (English)

    Bei Zhang; Yan Fang Zhao; Xin Zhai; Wei Jie Fan; Jun Ling Ren; Chun Fu Wu; Ping Gong

    2012-01-01

    A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized.All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line (HL-60),human lung adenocarcinoma epithelial cell hne (A549) and human breast cancer cell line (MDA-MB-231) in vitro by standard MTT assay.The pharmacological results indicated that some compounds exhibited promising antitumor activities.Compound lj showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L,0.7 μ mol/L and 0.5 μmol/L,respectively.

  14. α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives.

    Science.gov (United States)

    Popović-Djordjević, Jelena B; Jevtić, Ivana I; Grozdanić, Nadja Dj; Šegan, Sandra B; Zlatović, Mario V; Ivanović, Milovan D; Stanojković, Tatjana P

    2017-12-01

    The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay. The best antitumour activity was achieved with compound 2 (trans-5-phenethyl-1-phenylhexahydro-1H-imidazo[4,5-c]pyridin-2(3H)-one) against MDA-MB-453 human breast cancer cell line (IC50 = 83.41 ± 1.60 µM). Cyclic ureas and carbamates showed promising anti-α-glucosidase activity and should be further tested as potential antidiabetic drugs. The PLS model of preliminary QSAR study indicated that, in planing the future synthesis of more potent compounds, the newly designed should have the substituents capable of polar interactions with receptor sites in various positions, while avoiding the increase of their lipophilicity.

  15. Synthesis, characterization and biological activities of copper(II) complex of 2-Benzimidazolyl-urea and the nitrate salt of 2-Benzimidazolyl-urea

    Science.gov (United States)

    Poyraz, Mehmet; Sari, Musa; Banti, Christina N.; Hadjikakou, Sotiris K.

    2017-10-01

    The synthesis of the complex {[Cu(BZIMU)2](NO3)2} (1) (BZIMU = 2-Benzimidazolyl-urea) is reported here. The complex 1 was characterized by elemental analysis, FT-IR, magnetic susceptibility and molar conductance measurements. The crystal structures of 1 and of the nitrate salt of [(BZIMUH+)(NO3)-] (2) were determined by X-ray diffraction analysis. The copper complex 1 and [(BZIMUH+)(NO3)-] (2) were evaluated for their in vitro cytotoxic activity (cell viability) against human cervix adenocarcinoma (HeLa) and human breast adenocarcinoma (MCF-7) cell line and normal human fetal lung fibroblast cells (MRC-5) with SRB assay.

  16. Caveolin-1 directly interacts with UT-A1 urea transporter: the role of caveolae/lipid rafts in UT-A1 regulation at the cell membrane.

    Science.gov (United States)

    Feng, Xiuyan; Huang, Haidong; Yang, Yuan; Fröhlich, Otto; Klein, Janet D; Sands, Jeff M; Chen, Guangping

    2009-06-01

    The cell plasma membrane contains specialized microdomains called lipid rafts which contain high amounts of sphingolipids and cholesterol. Lipid rafts are involved in a number of membrane protein functions. The urea transporter UT-A1, located in the kidney inner medullary collecting duct (IMCD), is important for urine concentrating ability. In this study, we investigated the possible role of lipid rafts in UT-A1 membrane regulation. Using sucrose gradient cell fractionation, we demonstrated that UT-A1 is concentrated in the caveolae-rich fraction both in stably expressing UT-A1 HEK293 cells and in freshly isolated kidney IMCD suspensions. In these gradients, UT-A1 at the cell plasma membrane is codistributed with caveolin-1, a major component of caveolae. The colocalization of UT-A1 in lipid rafts/caveolae was further confirmed in isolated caveolae from UT-A1-HEK293 cells. The direct association of UT-A1 and caveolin-1 was identified by immunoprecipitation and GST pull-down assay. Examination of internalized UT-A1 in pEGFP-UT-A1 transfected HEK293 cells fluorescent overlap with labeled cholera toxin subunit B, a marker of the caveolae-mediated endocytosis pathway. Disruption of lipid rafts by methyl-beta-cyclodextrin or knocking down caveolin-1 by small-interference RNA resulted in UT-A1 cell membrane accumulation. Functionally, overexpression of caveolin-1 in oocytes decreased UT-A1 urea transport activity and UT-A1 cell surface expression. Our results indicate that lipid rafts/caveolae participate in UT-A1 membrane regulation and this effect is mediated via a direct interaction of caveolin-1 with UT-A1.

  17. The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations.

    Science.gov (United States)

    Dzimbeg, G; Zorc, B; Kralj, M; Ester, K; Pavelić, K; Andrei, G; Snoeck, R; Balzarini, J; De Clercq, E; Mintas, M

    2008-06-01

    The novel urea primaquine derivatives 3a-i were prepared by aminolysis of benzotriazolide 2 with the corresponding amine in the presence or absence of triethylamine. Compound 2 was prepared by acylation of primaquine with 1-benzotriazole carboxylic acid chloride. Among all compounds evaluated, the pyridine derivative 3h exhibited the best cytostatic activities against colon carcinoma, human T-lymphocyte and murine leukemia. However, this compound showed also rather marked cytotoxicity towards human normal fibroblasts. The highest selectivity in the inhibitory effects on human malignant tumor cell lines vs. normal fibroblasts was found for ureas 3c, 3d and 3g. Results of broad antiviral evaluation showed that pyridine and phenethyl derivatives of urea 3h and 3g exhibited some selective inhibition against cytomegalovirus.

  18. Functional characterization of mouse urea transporters UT-A2 and UT-A3 expressed in purified Xenopus laevis oocyte plasma membranes.

    Science.gov (United States)

    Maciver, Bryce; Smith, Craig P; Hill, Warren G; Zeidel, Mark L

    2008-04-01

    Urea is a small solute synthesized by many terrestrial organisms as part of the catabolism of protein. In mammals it is transported across cellular membranes by specific urea transporter (UT) proteins that are the products of two separate, but closely related genes, referred to as UT-A and UT-B. Three major UT-A isoforms are found in the kidney, namely UT-A1, UT-A2, and UT-A3. UT-A2 is found in the thin, descending limb of the loop of Henle, whereas UT-A1 and UT-A3 are concentrated in the inner medullary collecting duct. UT-A2 and UT-A3 effectively represent two halves of the whole UT-A gene and, when joined together by 73 hydrophilic amino acids, constitute UT-A1. A biophysical characterization of mouse UT-A2 and UT-A3 was undertaken by expression in Xenopus laevis oocytes and subsequent preparation of highly enriched plasma membrane vesicles for use in stopped-flow fluorometry. Both isoforms were found to be highly specific for urea, and did not permeate water, ammonia, or other molecules closely related to urea (formamide, acetamide, methylurea, and dimethylurea). Single transporter flux rates of 46,000 +/- 10,000 and 59,000 +/- 15,000 (means +/- SE) urea molecules/s/channel for UT-A2 and UT-A3, respectively, were obtained. Overall, the UT-A2 and UT-A3 isoforms appear to have identical functional kinetics.

  19. Living with urea stress

    Indian Academy of Sciences (India)

    Laishram R Singh; Tanveer Ali Dar; Faizan Ahmad

    2009-06-01

    Intracellular organic osmolytes are present in certain organisms adapted to harsh environments. These osmolytes protect intracellular macromolecules against denaturing environmental stress. In contrast to the usually benign effects of most organic osmolytes, the waste product urea is a well-known perturbant of macromolecules. Although urea is a perturbing solute which inhibits enzyme activity and stability, it is employed by some species as a major osmolyte. The answer to this paradox was believed to be the discovery of protective osmolytes (methylamines). We review the current state of knowledge on the various ways of counteracting the harmful effects of urea in nature and the mechanisms for this. This review ends with the mechanistic idea that cellular salt (KCl/NaCl) plays a crucial role in counteracting the effects of urea, either by inducing required chaperones or methylamines, or by thermodynamic interactions with urea-destabilised proteins. We also propose future opportunities and challenges in the field.

  20. Urea transporters UT-A1 and UT-A3 accumulate in the plasma membrane in response to increased hypertonicity.

    Science.gov (United States)

    Blessing, Nathan W; Blount, Mitsi A; Sands, Jeff M; Martin, Christopher F; Klein, Janet D

    2008-11-01

    The UT-A1 and UT-A3 urea transporters are expressed in the terminal inner medullary collecting duct (IMCD) and play an important role in the production of concentrated urine. We showed that both hyperosmolarity and vasopressin increase urea permeability in perfused rat terminal IMCDs and that UT-A1 and UT-A3 accumulate in the plasma membrane in response to vasopressin. In this study, we investigated whether hyperosmolarity causes UT-A1 and/or UT-A3 to accumulate in the plasma membrane or represents a complimentary stimulatory pathway. Rat IMCD suspensions were incubated in 450 vs. 900 mosM solutions. We biotinylated the IMCD surface proteins, collected, and analyzed them. Membrane accumulation was assessed by Western blotting of the biotinylated protein pool probed with anti-UT-A1 or anti-UT-A3. We studied the effect of NaCl, urea, and sucrose as osmotic agents. Membrane-associated UT-A1 and UT-A3 increased relative to control levels when either NaCl (UT-A1 increased 37 +/- 6%; UT-A3 increased 46 +/- 13%) or sucrose (UT-A1 increased 81 +/- 13%; UT-A3 increased 60 +/- 8%) was used to increase osmolarity. There was no increase in membrane UT-A1 or UT-A3 when urea was added. Analogously, UT-A1 phosphorylation was increased in NaCl- and sucrose- but not in urea-based hyperosmolar solutions. Hypertonicity also increased UT-A3 phosphorylation. We conclude that the increase in the urea permeability in response to hyperosmolarity reflects both UT-A1 and UT-A3 movement to the plasma membrane and may be a direct response to tonicity. Furthermore, this movement is accompanied by, and may require, increased phosphorylation in response to hypertonicity.

  1. Effects of slow-release urea fertilizers on urease activity, microbial biomass, and nematode communities in an aquic brown soil.

    Science.gov (United States)

    Jiao, Xiaoguang; Liang, Wenju; Chen, Lijun; Zhang, Haijun; Li, Qi; Wang, Peng; Wen, Dazhong

    2005-05-01

    A field experiment was carried out at the Shenyang Experimental Station of Ecology (CAS) in order to study the effects of slow-release urea fertilizers high polymer-coated urea (SRU1), SRU1 mixed with dicyandiamide DCD (SRU2), and SRU1 mixed with calcium carbide CaC2 (SRU3) on urease activity, microbial biomass C and N, and nematode communities in an aquic brown soil during the maize growth period. The results demonstrated that the application of slow-release urea fertilizers inhibits soil urease activity and increases the soil NH4+-N content. Soil available N increment could promote its immobilization by microorganisms. Determination of soil microbial biomass N indicated that a combined application of coated urea and nitrification inhibitors increased the soil active N pool. The population of predators/omnivores indicated that treatment with SRU2 could provide enough soil NH4+-N to promote maize growth and increased the food resource for the soil fauna compared with the other treatments.

  2. [Reaction of NO with metal oxides and urea supported on activated carbons at low temperature].

    Science.gov (United States)

    Cui, Hua-Fei; Li, Cai-Ting; Lu, Pei; Peng, Dun-Liang; Guo, Jing; Chen, Ling

    2010-11-01

    The catalysts were prepared by activated carbon fiber (ACF) loaded different contents of NiO and NiO-CeO2, Urea was loaded on the prepared catalysts as reductant. The experiments of selective catalytic reductions (SCR) of NO were carried out from 30 to 120 degrees C. The experiments of SEM, BET and XRD of the samples were also carried out selectively to study the catalysts properties, respectively. The experimental results showed that the loaded mass fraction of NiO could greatly affect the catalytic activity of the catalysts. 10% NiO catalyst activity and activity stability were both higher than that of the others, and it could yield about 50% removal efficiency of NO at 90 degrees C. With the loaded mass increasing, the catalytic activity was obviously decreased. And furthermore, the catalyst of 5% NiO-5% CeO2/ACF had the best catalytic activities on SCR NO and stability among the prepared NiO-CeO2/ACF catalysts, and its NO removal efficiency was over 55% at 110 degrees C. When the loaded mass increased, the similar phenomenon was observed, which was due to the decreasing of specific surface area of the catalysts. The metal oxides, loaded on ACF, were the catalytic centers in this study. Moreover, 5% CeO2-5% NiO/ACF had the highest catalytic activity than 10% CeO2/ACF and 10% NiO/ ACF. Therefore, there should be synergistic effect between CeO2 and NiO. Finally, the catalytic mechanism of SCR on NO at low temperature was discussed.

  3. Copper—Induced Changes in the Urea Uptake and Urease Activity in the Cyanobacteria Anabaena doliolum and Anacystis Nidulans:Interaction With Sulphur Containing Amino Acids

    Institute of Scientific and Technical Information of China (English)

    S.SINGH; B.B.SINGH; 等

    1995-01-01

    Copper-induced changes in the urea uptake and urease activity have been investigated in the cyanobacteria Anabaena doliolum and Anacystis nidulans.Copper,at and above 5μmol/L concentration,inhibited urea uptake and urease activity systems in both the cyanobacteria in a concentration dependent manner,However,the urea uptake and urease activity systems in A.nidulans apeared slightly more tolerant to copper than that of A.doliolum.The inhibitory effect of copeer on urea uptake and urease activity was mitigated by sulphur containing amino acids(cystine and cysteine),however,methionine could not do so,indicating the involvement of sulfhydryl(-SH) groups in the assimilation of urea in cyanobacteria.

  4. New aminoporphyrins bearing urea derivative substituents: synthesis, characterization, antibacterial and antifungal activity

    Directory of Open Access Journals (Sweden)

    Gholamreza Karimipour

    2015-06-01

    Full Text Available This work studied the synthesis of 5,10,15-tris(4-aminophenyl-20-(N,N-dialkyl/diaryl-N-phenylurea porphyrins (P1-P4 with alkyl or aryl groups of Ph, iPr, Et and Me, respectively and also the preparation of their manganese (III and cobalt (II complexes (MnP and CoP. The P1-P4 ligands were characterized by different spectroscopic techniques (1H NMR, FTIR, UV-Vis and elemental analysis, and metalated with Mn and Co acetate salts. The antibacterial and antifungal activities of these compounds in vitro were investigated by agar-disc diffusion method against Escherichia coli (-, Pseudomonas aeruginosa (-, Staphylococcus aureus(+, Bacillus subtilis (+ and Aspergillus oryzae and Candida albicans. Results showed that antibacterial and antifungal activity of the test samples increased with increase of their concentrations and the highest activity was obtained when the concentration of porphyrin compounds was 100 µg/mL. The activity for the porphyrin ligands depended on the nature of the urea derivative substituents and increased in the order P1 > P2 > P3 >P4, which was consistent with the order of their liposolubility. MnP and CoP complexes exhibited much higher antibacterial and antifungal activity than P1-P4ligands. Further, the growth inhibitory effects of these compounds was generally in the order CoP complexes > MnP complexes > P1-P4 ligands. Among these porphyrin compounds, CoP1displayed the highest antibacterial and antifungal activity, especially with a concentration of 100 µg/mL, against all the four tested bacteria and two fungi, and therefore it could be potential to be used as drug.

  5. QSAR modeling of antimalarial activity of urea derivatives using genetic algorithm–multiple linear regressions

    Directory of Open Access Journals (Sweden)

    Abolghasem Beheshti

    2016-05-01

    Full Text Available A quantitative structure–activity relationship (QSAR was performed to analyze antimalarial activities of 68 urea derivatives using multiple linear regressions (MLR. QSAR analyses were performed on the available 68 IC50 oral data based on theoretical molecular descriptors. A suitable set of molecular descriptors were calculated to represent the molecular structures of compounds, such as constitutional, topological, geometrical, electrostatic and quantum-chemical descriptors. The important descriptors were selected with the aid of the genetic algorithm (GA method. The obtained model was validated using leave-one-out (LOO cross-validation; external test set and Y-randomization test. The root mean square errors (RMSE of the training set, and the test set for GA–MLR model were calculated to be 0.314 and 0.486, the square of correlation coefficients (R2 were obtained 0.801 and 0.803, respectively. Results showed that the predictive ability of the model was satisfactory, and it can be used for designing similar group of antimalarial compounds.

  6. Synthesis and antiulcer activity evaluation of conjugates of amino acids with N-aroyl- N, N'-dicyclohexyl urea

    Directory of Open Access Journals (Sweden)

    Subudhi Bharat

    2011-12-01

    Full Text Available Abstract Amino acids are safe molecules with variable efficacy against ulceration. Considering the good antioxidant potential of N-aroyl- N, N'-dicyclohexyl urea and antiulcer activities of amino acids, a series of amino acid conjugates of N-aroyl- N, N'-dicyclohexyl urea was synthesized and the effect against ulceration in albino rats induced by pyloric ligation was screened. All these compounds were found to be safe and active. Reduction of ulcer index was significant for all compounds. Conjugates of methionine and histidine exhibited enhanced antiulcer activity comparable to omeprazole in terms of inhibition of release of gastric juice, hydrochloric acid and neutralization activity. The promising efficacy and safety of these compounds is interesting for further investigation.

  7. Descending thin limb of the intermediate loop expresses both aquaporin 1 and urea transporter A2 in the mouse kidney.

    Science.gov (United States)

    Kim, Wan-Young; Lee, Hyun-Wook; Han, Ki-Hwan; Nam, Sun-Ah; Choi, Arum; Kim, Yong-Kyun; Kim, Jin

    2016-07-01

    A new intermediate type of Henle's loop has been reported that it extends into the inner medulla and turns within the first millimeter beyond the outer medulla. This study aimed to identify the descending thin limb (DTL) of the intermediate loop in the adult C57Bl/6 mouse kidney using aquaporin 1 (AQP1) and urea transporter A2 (UT-A2) antibodies. In the upper part of the inner stripe of the outer medulla (ISOM), AQP1 was expressed strongly in the DTL with type II epithelium of the long loop, but not in type I epithelium of the short loop. The DTL of the intermediate loop exhibited weak AQP1 immunoreactivity. UT-A2 immunoreactivity was not observed in the upper part of any DTL type. AQP1 expression was similar in the upper and middle parts of the ISOM. UT-A2 expression was variable, being expressed strongly in the DTL with type I epithelium of the short loop, but not in type II epithelium of the long loop. In the innermost part of the ISOM, AQP1 was expressed only in type III epithelium of the long loop. UT-A2-positive and UT-A2-negative cells were intermingled in type I epithelium of the intermediate loop, but were not observed in type III epithelium of the long loop. UT-A2-positive DTLs of the intermediate loop extended into the UT-A2/AQP1-negative type I epithelium in the initial part of the inner medulla. These results demonstrate that the DTL of the intermediate loop is composed of type I epithelium and expresses both AQP1 and UT-A2. The functional role of the DTL of the intermediate loop may be distinct from the short or long loops.

  8. New urea and thiourea derivatives of piperazine doped with febuxostat: synthesis and evaluation of anti-TMV and antimicrobial activities.

    Science.gov (United States)

    Krishna Reddy, Reddivari Chenna; Rasheed, Syed; Subba Rao, Devineni; Adam, Shaik; Venkata Rami Reddy, Yellala; Raju, Chamarthi Naga

    2013-01-01

    A series of new 4-(5-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-2-carbonyl)-N-(substituted phenyl)piperazine-1-carboxamides 8(a-e)/carbothioamides 8(f-j) were accomplished for biological interest by the simple addition of active functionalized arylisocyanates 7(a-e)/arylisothiocyanates 7(f-j) with 2-isobutoxy-5-(4-methyl-2-(piperazine-1-carbonyl)thiazol-5-yl)benzonitrile (4). Compound 4 was synthesized in high yields (94%) by the condensation reaction of febuxostat (1) with piperazine using a selective reagent such as propylphosphonic anhydride (T3P). Antiviral activity against Tobacco mosaic virus (TMV) and antimicrobial activity of the synthesized compounds were evaluated. Biological data revealed that 4-nitrophenyl substituted urea 8d, and 3-bromophenyl substituted thiourea 8f exhibited promising antiviral activities. Moreover, 4-fluorophenyl substituted urea 8a, 4-nitrophenyl substituted urea 8d, 3-bromophenyl substituted thiourea 8f, and 2,4-dichlorophenyl substituted thiourea 8j exhibited potent antimicrobial activity.

  9. New insights into urea and glucose handling by the kidney, and the urine concentrating mechanism.

    Science.gov (United States)

    Bankir, Lise; Yang, Baoxue

    2012-06-01

    The mechanism by which urine is concentrated in the mammalian kidney remains incompletely understood. Urea is the dominant urinary osmole in most mammals and may be concentrated a 100-fold above its plasma level in humans and even more in rodents. Several facilitated urea transporters have been cloned. The phenotypes of mice with deletion of the transporters expressed in the kidney have challenged two previously well-accepted paradigms regarding urea and sodium handling in the renal medulla but have provided no alternative explanation for the accumulation of solutes that occurs in the inner medulla. In this review, we present evidence supporting the existence of an active urea secretion in the pars recta of the proximal tubule and explain how it changes our views regarding intrarenal urea handling and UT-A2 function. The transporter responsible for this secretion could be SGLT1, a sodium-glucose cotransporter that also transports urea. Glucagon may have a role in the regulation of this secretion. Further, we describe a possible transfer of osmotic energy from the outer to the inner medulla via an intrarenal Cori cycle converting glucose to lactate and back. Finally, we propose that an active urea transporter, expressed in the urothelium, may continuously reclaim urea that diffuses out of the ureter and bladder. These hypotheses are all based on published findings. They may not all be confirmed later on, but we hope they will stimulate further research in new directions.

  10. Amino substituted nitrogen heterocycle ureas as kinase insert domain containing receptor (KDR inhibitors: Performance of structure–activity relationship approaches

    Directory of Open Access Journals (Sweden)

    Hayriye Yilmaz

    2015-06-01

    Full Text Available A quantitative structure–activity relationship (QSAR study was performed on a set of amino-substituted nitrogen heterocyclic urea derivatives. Two novel approaches were applied: (1 the simplified molecular input-line entry systems (SMILES based optimal descriptors approach; and (2 the fragment-based simplex representation of molecular structure (SiRMS approach. Comparison with the classic scheme of building up the model and balance of correlation (BC for optimal descriptors approach shows that the BC scheme provides more robust predictions than the classic scheme for the considered pIC50 of the heterocyclic urea derivatives. Comparison of the SMILES-based optimal descriptors and SiRMS approaches has confirmed good performance of both techniques in prediction of kinase insert domain containing receptor (KDR inhibitory activity, expressed as a logarithm of inhibitory concentration (pIC50 of studied compounds.

  11. High and Low Affinity Urea Root Uptake: Involvement of NIP5;1.

    Science.gov (United States)

    Yang, Huayiu; Menz, Jochen; Häussermann, Iris; Benz, Martin; Fujiwara, Toru; Ludewig, Uwe

    2015-08-01

    Urea is the most widespread nitrogen (N) fertilizer worldwide and is rapidly degraded in soil to ammonium by urease. Ammonium is either taken up by plant roots or is further processed to nitrate by soil microorganisms. However, urea can be taken up by roots and is further degraded to ammonium by plant urease for assimilation. When urea is supplied under sterile conditions, it acts as a poor N source for seedlings or adult Arabidopsis thaliana plants. Here, the gene expression of young seedlings exposed to urea and ammonium nitrate nutrition was compared. Several primary metabolism and transport genes, including those for nitrate and urea, were differentially expressed in seedlings. However, urease and most major intrinsic proteins were not differentially expressed, with the exception of NIP6;1, a urea-permeable channel, which was repressed. Furthermore, little overlap with the gene expression with ammonium as the sole N source was observed, confirming that pure urea nutrition is not associated with the ammonium toxicity syndrome in seedlings. The direct root uptake of urea was increased under boron deficiency, in both the high and low affinity range. This activity was entirely mediated by the NIP5;1 channel, which was confirmed to transport urea when expressed in oocytes. The uptake of urea in the high and low affinity range was also determined for maize and wheat roots. The urea uptake by maize roots was only about half that of wheat, but was not stimulated by boron deficiency or N deficiency in either species. This analysis identifies novel components of the urea uptake systems in plants, which may become agronomically relevant to urea uptake and utilization, as stabilized urea fertilizers become increasingly popular. © The Author 2015. Published by Oxford University Press on behalf of Japanese Society of Plant Physiologists. All rights reserved. For permissions, please email: journals.permissions@oup.com.

  12. Amino substituted nitrogen heterocycle ureas as kinase insert domain containing receptor (KDR) inhibitors: Performance of structure–activity relationship approaches

    OpenAIRE

    Hayriye Yilmaz; Natalia Sizochenko; Bakhtiyor Rasulev; Andrey Toropov; Yahya Guzel; Viktor Kuz'min; Danuta Leszczynska; Jerzy Leszczynski

    2015-01-01

    A quantitative structure–activity relationship (QSAR) study was performed on a set of amino-substituted nitrogen heterocyclic urea derivatives. Two novel approaches were applied: (1) the simplified molecular input-line entry systems (SMILES) based optimal descriptors approach; and (2) the fragment-based simplex representation of molecular structure (SiRMS) approach. Comparison with the classic scheme of building up the model and balance of correlation (BC) for optimal descriptors approach sho...

  13. Validation of low activity {sup 14}C-urea breath test in diagnosis of ``Helicobacter pylori``in humans

    Energy Technology Data Exchange (ETDEWEB)

    Bielanski, W.; Konturek, S.J.; Dobrzanka, M.J.; Plonka, M.; Sito, E.; Stachura, J. [Uniwersytet Jagiellonski, Cracow (Poland); Hoffman, S.R.; Marshall, B.J. [Tri-Med Specialtis, Charlottenville, VA (United States)

    1996-12-31

    Etiologic role for ``Helicobacter pylori`` (HP) seems to be well established in gastric pathology. The high urease activity of HP can be used to detect this bacterium by non-invasive urea breath tests (UBT). We validated the low activity version of the test in which 37 kBq {sup 14}C-urea is given orally in capsule. With the cut off value {>=} 1.66 Bq (100 DPM) as positive, UBT results correlated highly significant with combined results for invasive methods, i.e. CLO-test + Histology score. The reproducibility of the test was 100%. The results obtained for the breath test performed locally were almost identical with that read at remote laboratory. The data found for fasting and fed states of subjects agreed in 87%. When {sup 14}C-urea was confined in the mouth of both HP positive and HP negative patients UBT showed the presence of urease activity in the mouth cavity. (author). 21 refs, 2 figs, 1 tab.

  14. Urea derivatives enhance the photocatalytic activity of dye-modified titanium dioxide

    OpenAIRE

    Füldner, Stefan; Mitkina, T.; Trottmann, T.; Frimberger, A.; Gruber, Michael; König, Burkhard

    2011-01-01

    Trace amounts of urea derivatives enhance the rate of nitrobenzene N3-sensitized TiO2 photoreduction by catalyzing the proton transfer. The usually required addition of transition metal co-catalysts becomes dispensable for this visible light photocatalysis, facilitating its application in organic synthesis.

  15. Aestivation Induces Changes in the mRNA Expression Levels and Protein Abundance of Two Isoforms of Urea Transporters in the Gills of the African Lungfish, Protopterus annectens

    Science.gov (United States)

    Chng, You R.; Ong, Jasmine L. Y.; Ching, Biyun; Chen, Xiu L.; Hiong, Kum C.; Wong, Wai P.; Chew, Shit F.; Lam, Siew H.; Ip, Yuen K.

    2017-01-01

    The African lungfish, Protopterus annectens, is ammonotelic in water despite being ureogenic. When it aestivates in mucus cocoon on land, ammonia is detoxified to urea. During the maintenance phase of aestivation, urea accumulates in the body, which is subsequently excreted upon arousal. Urea excretion involves urea transporters (UT/Ut). This study aimed to clone and sequence the ut isoforms from the gills of P. annectens, and to test the hypothesis that the mRNA and/or protein expression levels of ut/Ut isoforms could vary in the gills of P. annectens during the induction, maintenance, and arousal phases of aestivation. Two isoforms of ut, ut-a2a and ut-a2b, were obtained from the gills of P. annectens. ut-a2a consisted of 1227 bp and coded for 408 amino acids with an estimated molecular mass of 44.7 kDa, while ut-a2b consisted of 1392 bp and coded for 464 amino acids with an estimated molecular mass of 51.2 kDa. Ut-a2a and Ut-a2b of P. annectens had a closer phylogenetic relationship with Ut/UT of tetrapods than Ut of fishes. While the mRNA expression pattern of ut-a2a and ut-a2b across various tissues of P. annectens differed, the transcript levels of ut-a2a and ut-a2b in the gills were comparable, indicating that they might be equally important for branchial urea excretion during the initial arousal phase of aestivation. During the maintenance phase of aestivation, the transcript level of ut-a2a increased significantly, but the protein abundance of Ut-a2a remained unchanged in the gills of P. annectens. This could be an adaptive feature to prepare for an increase in the production of Ut-a2a upon arousal. Indeed, arousal led to a significant increase in the branchial Ut-a2a protein abundance. Although the transcript level of ut-a2b remained unchanged, there were significant increases in the protein abundance of Ut-a2b in the gills of P. annectens throughout the three phases of aestivation. The increase in the protein abundance of Ut-a2b during the maintenance

  16. Conversion and characterization of activated carbon fiber derived from palm empty fruit bunch waste and its kinetic study on urea adsorption.

    Science.gov (United States)

    Ooi, Chee-Heong; Cheah, Wee-Keat; Sim, Yoke-Leng; Pung, Swee-Yong; Yeoh, Fei-Yee

    2017-07-15

    Urea removal is an important process in household wastewater purification and hemodialysis treatment. The efficiency of the urea removal can be improved by utilizing activated carbon fiber (ACF) for effective urea adsorption. In this study, ACF was prepared from oil palm empty fruit bunch (EFB) fiber via physicochemical activation using sulfuric acid as an activating reagent. Based on the FESEM result, ACF obtained after the carbonization and activation processes demonstrated uniform macropores with thick channel wall. ACF was found better prepared in 1.5:1 acid-to-EFB fiber ratio; where the pore size of ACF was analyzed as 1.2 nm in diameter with a predominant micropore volume of 0.39 cm(3) g(-1) and a BET surface area of 869 m(2) g(-1). The reaction kinetics of urea adsorption by the ACF was found to follow a pseudo-second order kinetic model. The equilibrium amount of urea adsorbed on ACF decreased from 877.907 to 134.098 mg g(-1) as the acid-to-fiber ratio increased from 0.75 to 4. During the adsorption process, the hydroxyl (OH) groups on ACF surface were ionized and became electronegatively charged due to the weak alkalinity of urea solution, causing ionic repulsion towards partially anionic urea. The ionic repulsion force between the electronegatively charged ACF surface and urea molecules became stronger when more OH functional groups appeared on ACF prepared at higher acid impregnation ratio. The results implied that EFB fiber based ACF can be used as an efficient adsorbent for the urea removal process. Copyright © 2017 Elsevier Ltd. All rights reserved.

  17. Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643)

    DEFF Research Database (Denmark)

    Hansen, Rie Schultz; Diness, Thomas Goldin; Christ, Torsten

    2005-01-01

    The cardiac action potential is generated by a concerted action of different ion channels and transporters. Dysfunction of any of these membrane proteins can give rise to cardiac arrhythmias, which is particularly true for the repolarizing potassium channels. We suggest that an increased...... repolarization current could be a new antiarrhythmic principle, because it possibly would attenuate afterdepolarizations, ischemic leak currents, and reentry phenomena. Repolarization of the cardiac myocytes is crucially dependent on the late rapid delayed rectifier current (I(Kr)) conducted by ether......-a-go-go-related gene (ERG) potassium channels. We have developed the diphenylurea compound 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and tested whether this small organic molecule could increase the activity of human ERG (HERG) channels expressed heterologously. In Xenopus laevis oocytes, NS1643...

  18. Internalization of UT-A1 urea transporter is dynamin dependent and mediated by both caveolae- and clathrin-coated pit pathways.

    Science.gov (United States)

    Huang, Haidong; Feng, Xiuyan; Zhuang, Jieqiu; Fröhlich, Otto; Klein, Janet D; Cai, Hui; Sands, Jeff M; Chen, Guangping

    2010-12-01

    Dynamin is a large GTPase involved in several distinct modes of cell endocytosis. In this study, we examined the possible role of dynamin in UT-A1 internalization. The direct relationship of UT-A1 and dynamin was identified by coimmunoprecipitation. UT-A1 has cytosolic NH(2) and COOH termini and a large intracellular loop. Dynamin specifically binds to the intracellular loop of UT-A1, but not the NH(2) and COOH termini. In cell surface biotinylation experiments, coexpression of dynamin and UT-A1 in HEK293 cells resulted in a decrease of UT-A1 cell surface expression. Conversely, cells expressing dynamin mutant K44A, which is deficient in GTP binding, showed an increased accumulation of UT-A1 protein on the cell surface. Cell plasma membrane lipid raft fractionation experiments revealed that blocking endocytosis with dynamin K44A causes UT-A1 protein accumulation in both the lipid raft and nonlipid raft pools, suggesting that both caveolae- and clathrin-mediated mechanisms may be involved in the internalization of UT-A1. This was further supported by 1) small interfering RNA to knock down either caveolin-1 or μ2 reduced UT-A1 internalization in HEK293 cells and 2) inhibition of either the caveolae pathway by methyl-β-cyclodextrin or the clathrin pathway by concanavalin A caused UT-A1 cell membrane accumulation. Functionally, overexpression of dynamin, caveolin, or μ2 decreased UT-A1 urea transport activity and decreased UT-A1 cell surface expression. We conclude that UT-A1 endocytosis is dynamin-dependent and mediated by both caveolae- and clathrin-coated pit pathways.

  19. TEMPERATURE ACTIVATION OF THE UREASE-UREA SYSTEM USING CRUDE AND CRYSTALLINE UREASE.

    Science.gov (United States)

    Sizer, I W

    1939-07-20

    1. The hydrolysis of urea catalyzed by jack bean meal has been followed by determining colorimetrically after Nesslerization the ammonia nitrogen, and volumetrically the carbon dioxide liberated at successive intervals during the reaction. During the early part of hydrolysis the rate of ammonia or carbon dioxide liberation is constant for all the urease solutions which were used. 2. When log rate of NH(3) or CO(2) formation was plotted against 1/T, the points fell along a straight line, the slope of which corresponded to an activation energy of either 8,700 or 11,700 calories per gram mol. Frequently urease, when dissolved in sulfite solution, was characterized by an activation energy of 11,700 below and 8,700 above the critical temperature of about 23 degrees C. At high temperatures the plotted points fell off from the curve due to temperature inactivation. 3. Essentially the same results on temperature activation were obtained with crude jack bean meal, Arlco urease, crystalline urease not recrystallized, and crystalline urease once recrystallized. The temperature characteristic which was obtained depended in part upon the composition of the medium. When dissolved in water, or aqueous solutions of glycerine, KCN, Na(2)S(2)O(2), cystine, Na(2)SO(4), and K(4)Fe(CN)(6), the temperature characteristic or micro of urease is 8,700. On the other hand, when urease is dissolved in solutions of K(3)Fe(CN)(6) or H(2)O(2) the micro value is 11,700. When dissolved in a solution containing Na(2)SO(3) and NaHSO(3) the micro value may be either 8,700 or 11,700 over the whole temperature range, or 11,700 below and 8,700 above 23 degrees C. 4. When crystalline urease is dissolved in varying mixtures of K(4)Fe(CN)(6) and K(3)Fe(CN)(6), the temperature characteristic depends upon the oxidation-reduction potential of the digest. When E(h) is greater than +0.46 volt micro = 11,700, when less than +0.42 volt micro = 8,700, when between +0.42 - +0.46 micro = 11,700 below and 8,700 above

  20. Selective catalytic reduction (SCR) of NO by urea loaded on activated carbon fibre (ACF) and CeO2/ACF at 30 degrees C: the SCR mechanism.

    Science.gov (United States)

    Zeng, Zheng; Lu, Pei; Li, Caiting; Zeng, Guangming; Jiang, Xiao; Zhai, Yunbo; Fan, Xiaopeng

    2012-06-01

    Selective catalytic reduction (SCR) of NO by urea loaded on rayon-based activated carbon fibre (ACF) and CeO2/ACF (CA) was studied at ambient temperature (30 degrees C) to establish a basic scheme for its reduction. Nitric oxide was found to be reduced to N2 with urea deposited on the ACF and CA. When oxygen was present, the greater the amount of loaded urea (20-60%), the greater the NO(x) conversions, which were between 72.03% and 77.30%, whereas the NO(x) conversions were about 50% when oxygen was absent. Moreover, when the urea was loaded on CA, a catalyst containing 40% urea/ACF loaded with 10% CeO2 (UCA4) could yield a NO(x) conversion of about 80% for 24.5 h. Based on the experimental results, the catalytic mechanisms of SCR with and without oxygen are discussed. The enhancing effect of oxygen resulted from the oxidation of NO to NO2, and urea was the main reducing agent in the SCR of loaded catalysts. ACF-C was the catalytic centre in the SCR of NO of ACF, while CeO2 of urea-loaded CA was the catalytic centre.

  1. Effects of dietary nitrogen concentration on messenger RNA expression and protein abundance of urea transporter-B and aquaporins in ruminal papillae from lactating Holstein cows

    DEFF Research Database (Denmark)

    Røjen, Betina Amdisen; Poulsen, Søren Brandt; Theil, Peter Kappel

    2011-01-01

    To test the hypothesis that dietary N concentrations affect gut epithelial urea transport by modifying the expression of urea transporter B (UT-B) and aquaporins (AQP), the mRNA expression and protein abundance of UT-B and AQP3, AQP7, AQP8, and AQP10 were investigated in ruminal papillae from 9...... lactating dairy cows. Ruminal papillae were harvested from cows fed low N (12.9% crude protein) and high N (17.1% crude protein) diets in a crossover design with 21-d periods. The mRNA expression was determined by real-time reverse transcription-PCR and protein abundance by immunoblotting. The mRNA...... expression of UT-B was not affected by dietary treatment, whereas mRNA expression of AQP3, 7, and 10 were greater in the high N compared with the low N fed cows. Using peptide-derived rabbit antibodies to cow AQP3, 7, and 8, immunoblotting revealed bands of approximately 27, 27, and 24 kDa in ruminal...

  2. Bacterial toxins activation of abbreviated urea cycle in porcine cerebral vascular smooth muscle cells.

    Science.gov (United States)

    Mishra, Rajesh G; Tseng, Tzu-Ling; Chen, Mei-Fang; Chen, Po-Yi; Lee, Tony J-F

    2016-12-01

    Nitric oxide (NO) overproduction via induction of inducible nitric oxide synthase (iNOS) is implicated in vasodilatory shock in sepsis, leading to septic encephalopathy and accelerating cerebral ischemic injury. An abbreviated urea-cycle (l-citrulline-l-arginine-NO cycle) has been demonstrated in cerebral perivascular nitrergic nerves and endothelial cells but not in normal cerebral vascular smooth muscle cell (CVSMC). This cycle indicates that argininosuccinate synthase (ASS) catalyzes l-citrulline (l-cit) conversion to form argininosuccinate (AS), and subsequent AS cleavage by argininosuccinate lyase (ASL) forms l-arginine (l-arg), the substrate for NO synthesis. The possibility that ASS enzyme in this cycle was induced in the CVSMC in sepsis was examined. Blood-vessel myography technique was used for measuring porcine isolated basilar arterial tone. NO in cultured CVSMC and in condition mediums were estimated by diaminofluorescein (DAF)-induced fluorescence and Griess reaction, respectively. Immunohistochemical and immunoblotting analyses were used to examine iNOS and ASS induction. l-cit and l-arg, which did not relax endothelium-denuded normal basilar arteries precontracted by U-46619, induced significant vasorelaxation with increased NO production in these arteries and the CVSMCs following 6-hour exposure to 20μg/ml lipopolysaccharide (LPS) or lipoteichoic acid (LTA). Pre-treatment with pyrrolidine dithiocarbamate (PDTC) and salicylate (SAL) (NFκB inhibitors), aminoguanidine (AG, an iNOS inhibitor), and nitro-l-arg (NLA, a non-specific NOS inhibitor) blocked NO synthesis in the CVSMC and attenuated l-cit- and l-arg-induced relaxation of LPS- and LTA-treated arteries. Furthermore, immunohistochemical and immunoblotting studies demonstrated that expression of basal iNOS and ASS in the smooth muscle cell of arterial segments denuded of endothelium and the cultured CVSMCs was significantly increased following 6-hour incubation with LPS or LTA. This increased i

  3. Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors

    Energy Technology Data Exchange (ETDEWEB)

    Pecic, Stevan; Pakhomova, Svetlana; Newcomer, Marcia E.; Morisseau, Christophe; Hammock, Bruce D.; Zhu, Zhengxiang; Rinderspacher, Alison; Deng, Shi-Xian [UCD; (LSU); (Columbia)

    2013-09-27

    A series of potent amide non-urea inhibitors of soluble epoxide hydrolase (sEH) is disclosed. The inhibition of soluble epoxide hydrolase leads to elevated levels of epoxyeicosatrienoic acids (EETs), and thus inhibitors of sEH represent one of a novel approach to the development of vasodilatory and anti-inflammatory drugs. Structure–activities studies guided optimization of a lead compound, identified through high-throughput screening, gave rise to sub-nanomolar inhibitors of human sEH with stability in human liver microsomal assay suitable for preclinical development.

  4. Rhesus glycoprotein and urea transporter genes in rainbow trout embryos are upregulated in response to alkaline water (pH 9.7) but not elevated water ammonia.

    Science.gov (United States)

    Sashaw, Jessica; Nawata, Michele; Thompson, Sarah; Wood, Chris M; Wright, Patricia A

    2010-03-01

    Recent studies have shown that genes for the putative ammonia transporter, Rhesus glycoproteins (Rh) and the facilitated urea transporter (UT) are expressed before hatching in rainbow trout (Oncorhychus mykiss Walbaum) embryos. We tested the hypothesis that Rh and UT gene expressions are regulated in response to environmental conditions that inhibit ammonia excretion during early life stages. Eyed-up embryos (22 days post-fertilization (dpf)) were exposed to control (pH 8.3), high ammonia (1.70 mmol l(-1) NH4HCO3) and high pH (pH 9.7) conditions for 48h. With exposure to high water ammonia, ammonia excretion rates were reversed, tissue ammonia concentration was elevated by 9-fold, but there were no significant changes in mRNA expression relative to control embryos. In contrast, exposure to high water pH had a smaller impact on ammonia excretion rates and tissue ammonia concentrations, whereas mRNA levels for the Rhesus glycoprotein Rhcg2 and urea transporter (UT) were elevated by 3.5- and 5.6-fold, respectively. As well, mRNAs of the genes for H+ATPase and Na+/H+ exchanger (NHE2), associated with NH3 excretion, were also upregulated by 7.2- and 13-fold, respectively, in embryos exposed to alkaline water relative to controls. These results indicate that the Rhcg2, UT and associated transport genes are regulated in rainbow trout embryos, but in contrast to adults, there is no effect of high external ammonia at this stage of development.

  5. Signal focusing through active transport

    Science.gov (United States)

    Godec, Aljaž; Metzler, Ralf

    2015-07-01

    The accuracy of molecular signaling in biological cells and novel diagnostic devices is ultimately limited by the counting noise floor imposed by the thermal diffusion. Motivated by the fact that messenger RNA and vesicle-engulfed signaling molecules transiently bind to molecular motors and are actively transported in biological cells, we show here that the random active delivery of signaling particles to within a typical diffusion distance to the receptor generically reduces the correlation time of the counting noise. Considering a variety of signaling particle sizes from mRNA to vesicles and cell sizes from prokaryotic to eukaryotic cells, we show that the conditions for active focusing—faster and more precise signaling—are indeed compatible with observations in living cells. Our results improve the understanding of molecular cellular signaling and novel diagnostic devices.

  6. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties

    Directory of Open Access Journals (Sweden)

    David E. Wedge

    2013-03-01

    Full Text Available A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives 3a–e and 4a–e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a–e and 2a–e, respectively, in a 130–140 °C oil bath. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1H-NMR and mass spectroscopy. All compounds were evaluated for antifungal activity against plant pathogens, larvicidal and biting deterrent activity against the mosquito Aedes aegypti L. and in vitro cytotoxicity and anti-inflammatory activity against some human cell lines. Phomopis species were the most sensitive fungi to these compounds. Compounds 1b, 1c, 3a and 4e demonstrated selectively good activity against Phomopis obscurans and only 1b and 4e showed a similar level of activity against P. viticola. Compound 3d, with a LD50 value of 67.9 ppm, followed by 1c (LD50 = 118.8 ppm and 3e (LD50 = 165.6 ppm, showed the highest toxicity against Aedes aegypti larvae. Four of these compounds showed biting deterrent activity greater than solvent control, with the highest activity being seen for 1c, with a proportion not biting (PNB value of 0.75, followed by 1e, 2b and 1a. No cytotoxicity was observed against the tested human cancer cell lines. No anti-inflammatory activity was observed against NF-kB dependent transcription induced by phorbol myristate acetate (PMA in human chondrosarcoma cells.

  7. Modeling of Calcite Precipitation Driven by Bacteria-facilitated Urea Hydrolysis in A Flow Column Using A Fully Coupled, Fully Implicit Parallel Reactive Transport Simulator

    Science.gov (United States)

    Guo, L.; Huang, H.; Gaston, D.; Redden, G. D.

    2009-12-01

    One approach for immobilizing subsurface metal contaminants involves stimulating the in situ production of mineral phases that sequester or isolate contaminants. One example is using calcium carbonate to immobilize strontium. The success of such approaches depends on understanding how various processes of flow, transport, reaction and resulting porosity-permeability change couple in subsurface systems. Reactive transport models are often used for such purpose. Current subsurface reactive transport simulators typically involve a de-coupled solution approach, such as operator-splitting, that solves the transport equations for components and batch chemistry sequentially, which has limited applicability for many biogeochemical processes with fast kinetics and strong medium property-reaction interactions. A massively parallel, fully coupled, fully implicit reactive transport simulator has been developed based on a parallel multi-physics object oriented software environment computing framework (MOOSE) developed at the Idaho National Laboratory. Within this simulator, the system of transport and reaction equations is solved simultaneously in a fully coupled manner using the Jacobian Free Newton-Krylov (JFNK) method with preconditioning. The simulator was applied to model reactive transport in a one-dimensional column where conditions that favor calcium carbonate precipitation are generated by urea hydrolysis that is catalyzed by urease enzyme. Simulation results are compared to both laboratory column experiments and those obtained using the reactive transport simulator STOMP in terms of: the spatial and temporal distributions of precipitates and reaction rates and other major species in the reaction system; the changes in porosity and permeability; and the computing efficiency based on wall clock simulation time.

  8. Common folds and transport mechanisms of secondary active transporters.

    Science.gov (United States)

    Shi, Yigong

    2013-01-01

    Secondary active transporters exploit the electrochemical potential of solutes to shuttle specific substrate molecules across biological membranes, usually against their concentration gradient. Transporters of different functional families with little sequence similarity have repeatedly been found to exhibit similar folds, exemplified by the MFS, LeuT, and NhaA folds. Observations of multiple conformational states of the same transporter, represented by the LeuT superfamily members Mhp1, AdiC, vSGLT, and LeuT, led to proposals that structural changes are associated with substrate binding and transport. Despite recent biochemical and structural advances, our understanding of substrate recognition and energy coupling is rather preliminary. This review focuses on the common folds and shared transport mechanisms of secondary active transporters. Available structural information generally supports the alternating access model for substrate transport, with variations and extensions made by emerging structural, biochemical, and computational evidence.

  9. Urea: new questions about an ancient solute.

    Science.gov (United States)

    Bagnasco, S M

    2000-01-01

    Urea recycling and counter-current exchange within the renal tubular, vascular and interstitial compartments help maintain high levels of this solute in the renal medulla, that are crucial for the production of concentrated urine. The role of urea in physiological and pathological conditions is still unclear, although new information is becoming available. Several urea transporters have been identified that mediate facilitated transport of urea across biological membranes in the mammalian kidney, in amphibians, and in elasmobranchs. Evidence that urea transporters may be expressed in other mammalian organs is also beginning to emerge. The mechanisms involved in the regulation of urea transport are incompletely understood. In this respect, the structural and functional characterization of individual transporters is providing the basis to identify specific regulatory factors. Urea can be viewed as a perturbing osmolyte in the renal inner medulla, and the mechanisms of adaptation of renal cells to high concentration of this destabilizing solute are being investigated. Urea-specific signaling pathways have been identified, that could contribute to clarify how cells handle urea.

  10. Passive water and urea permeability of a human Na(+)-glutamate cotransporter expressed in Xenopus oocytes

    DEFF Research Database (Denmark)

    Macaulay, Nanna; Gether, Ulrik; Klærke, Dan Arne

    2002-01-01

    with mannitol. Apparently, the properties of the pore are not uniform along its length. The outer section may accommodate urea and glycerol in an osmotically active form, giving rise to larger water fluxes. The physiological role of EAAT1 for water homeostasis in the central nervous system is discussed....... to the K(0.5) value for glutamate activation of transport. The specific inhibitor DL-threo-beta-benzyloxyaspartate (TBOA) reduced the EAAT1-specific L(p) to 72 %. EAAT1 supported passive fluxes of [(14)C]urea and [(14)C]glycerol. The [(14)C]urea flux was increased in the presence of glutamate. The data...... suggest that the permeability depends on the conformational equilibrium of the EAAT1. At positive potentials and in the presence of Na(+) and glutamate, the pore is enlarged and water and urea penetrate more readily. The L(p) was larger when measured with urea or glycerol as osmolytes as compared...

  11. 1,1-Difluoroethyl-substituted triazolothienopyrimidines as inhibitors of a human urea transport protein (UT-B): new analogs and binding model.

    Science.gov (United States)

    Liu, Y; Esteva-Font, C; Yao, C; Phuan, P W; Verkman, A S; Anderson, M O

    2013-06-01

    The kidney urea transport protein UT-B is an attractive target for the development of small-molecule inhibitors with a novel diuretic ('urearetic') action. Previously, two compounds in the triazolothienopyrimidine scaffold (1a and 1c) were reported as UT-B inhibitors. Compound 1c incorporates a 1,1-difluoroethyl group, which affords improved microsomal stability when compared to the corresponding ethyl-substituted compound 1a. Here, a small focused library (4a-4f) was developed around lead inhibitor 1c to investigate the requirement of an amidine-linked thiophene in the inhibitor scaffold. Two compounds (4a and 4b) with nanomolar inhibitory potency (IC50≈40 nM) were synthesized. Computational docking of lead structure 1c and 4a-4f into a homology model of the UT-B cytoplasmic surface suggested binding with the core heterocycle buried deep into the hydrophobic pore region of the protein.

  12. Political activity for physical activity: health advocacy for active transport

    Directory of Open Access Journals (Sweden)

    Amun Qa-t-a

    2011-05-01

    Full Text Available Abstract Effective health advocacy is a priority for efforts to increase population participation in physical activity. Local councils are an important audience for this advocacy. The aim of the current study was to describe features of advocacy for active transport via submissions to city council annual plans in New Zealand, and the impact of an information sheet to encourage the health sector to be involved in this process. Written submissions to city council's annual consultation process were requested for 16 city councils over the period of three years (2007/08, 2008/09, and 2009/10. Submissions were reviewed and categories of responses were created. An advocacy information sheet encouraging health sector participation and summarising some of the evidence-base related to physical activity, active transport and health was released just prior to the 2009/10 submission time. Over the period of the study, city councils received 47,392 submissions, 17% of which were related to active transport. Most submissions came from city residents, with a small proportion (2% from the health sector. The largest category of submissions was in support of pedestrian and cycling infrastructure, design and maintenance of facilities and additional features to support use of these transport modes. Health arguments featured prominently in justifications for active transport initiatives, including concerns about injury risk, obesity, physical inactivity, personal safety and facilities for people with disabilities. There was evidence that the information sheet was utilised by some health sector submitters (12.5%, providing tentative support for initiatives of this nature. In conclusion, the study provides novel information about the current nature of health advocacy for active transport and informs future advocacy efforts about areas for emphasis, such as health benefits of active transport, and potential alliances with other sectors such as environmental

  13. Political activity for physical activity: health advocacy for active transport.

    Science.gov (United States)

    Richards, Rosalina; Murdoch, Linda; Reeder, Anthony I; Amun, Qa-t-a

    2011-05-29

    Effective health advocacy is a priority for efforts to increase population participation in physical activity. Local councils are an important audience for this advocacy. The aim of the current study was to describe features of advocacy for active transport via submissions to city council annual plans in New Zealand, and the impact of an information sheet to encourage the health sector to be involved in this process. Written submissions to city council's annual consultation process were requested for 16 city councils over the period of three years (2007/08, 2008/09, and 2009/10). Submissions were reviewed and categories of responses were created. An advocacy information sheet encouraging health sector participation and summarising some of the evidence-base related to physical activity, active transport and health was released just prior to the 2009/10 submission time. Over the period of the study, city councils received 47,392 submissions, 17% of which were related to active transport. Most submissions came from city residents, with a small proportion (2%) from the health sector. The largest category of submissions was in support of pedestrian and cycling infrastructure, design and maintenance of facilities and additional features to support use of these transport modes. Health arguments featured prominently in justifications for active transport initiatives, including concerns about injury risk, obesity, physical inactivity, personal safety and facilities for people with disabilities. There was evidence that the information sheet was utilised by some health sector submitters (12.5%), providing tentative support for initiatives of this nature. In conclusion, the study provides novel information about the current nature of health advocacy for active transport and informs future advocacy efforts about areas for emphasis, such as health benefits of active transport, and potential alliances with other sectors such as environmental sustainability, transport and urban

  14. Activity assay of membrane transport proteins

    Institute of Scientific and Technical Information of China (English)

    Hao Xie

    2008-01-01

    Membrane transport proteins are integral membrane proteins and considered as potential drug targets. Activity assay of transport proteins is essential for developing drugs to target these proteins. Major issues related to activity assessment of transport proteins include availability of transporters,transport activity of transporters, and interactions between ligands and transporters. Researchers need to consider the physiological status of proteins (bound in lipid membranes or purified), availability and specificity of substrates, and the purpose of the activity assay (screening, identifying, or comparing substrates and inhibitors) before choosing appropriate assay strategies and techniques. Transport proteins bound in vesicular membranes can be assayed for transporting substrate across membranes by means of uptake assay or entrance counterflow assay. Alternatively, transport proteins can be assayed for interactions with ligands by using techniques such as isothermal titration calorimetry, nuclear magnetic resonance spectroscopy, or surface plasmon resonance. Other methods and techniques such as fluorometry, scintillation proximity assay, electrophysiological assay, or stopped-flow assay could also be used for activity assay of transport proteins. In this paper the major strategies and techniques for activity assessment of membrane transport proteins are reviewed.

  15. H+, Water and Urea Transport in the Inner Medullary Collecting Duct and Their Role in the Prevention and Pathogenesis of Renal Stone Disease

    Science.gov (United States)

    Wall, Susan M.; Klein, Janet D.

    2008-09-01

    The inner medullary collecting duct (IMCD) is the final site within the kidney for the reabsorption of urea, water and electrolytes and for the secretion of H+ before the luminal fluid becomes the final urine. Transporters expressed in the IMCD contribute to the generation of the large ion gradients that exist between the interstitium and the collecting duct lumen. Thus, the luminal fluid within the human IMCD can reach an osmolality of 1200 mOsm/kg H2O and a pH of 4. This ability of the human nephron to concentrate and acidify the urine might predispose to stone formation. However, under treatment conditions that predispose to stone formation, such as during hypercalciuria, the kidney mitigates stone formation by reducing solute concentration by reducing H2O reabsorption. Moreover, the kidney attenuates stone formation by tightly controlling acid-base balance, which prevents the bone loss, hypocitraturia and hypercalciuria observed during metabolic acidosis by augmenting net H+ excretion by tightly regulating H+ transporter function and through luminal buffering, particularly with NH3. This article will review the ion transporters present in the mammalian IMCD and their role in the prevention and in the pathogenesis of renal stone formation.

  16. Design, synthesis, insecticidal activity, and structure-activity relationship (SAR): studies of novel triazone derivatives containing a urea bridge group based on transient receptor potential (TRP) channels.

    Science.gov (United States)

    Yang, Yan; Liu, Yuxiu; Song, Hongjian; Li, Yongqiang; Wang, Qingmin

    2016-11-01

    Numerous compounds containing urea bridge and biurea moieties are used in a variety of fields, especially as drugs and pesticides. To search for novel, environmentally benign and ecologically safe pesticides with unique modes of action, four series of novel triazone analogues containing urea, thiourea, biurea, and thiobiurea bridge, respectively, were designed and synthesized, according to various calcium ion channel inhibitors which act on transient receptor potential protein. Their structures were characterized by [Formula: see text] NMR, [Formula: see text] NMR, and HRMS. The insecticidal activities of the new compounds were obtained. The bioassay results indicated that compounds containing a thiourea bridge and a thiobiurea bridge exhibited excellent insecticidal activities against bean aphid. Specifically, compounds [Formula: see text], [Formula: see text], and [Formula: see text] exhibited 85, 90, and 95 % activities, respectively, at 10 mg/kg. Compounds [Formula: see text] (30 %), [Formula: see text] (35 %), [Formula: see text] (30 %), and [Formula: see text] (40 %) exhibited the approximate aphicidal activity of pymetrozine (30 %) at 5 mg/kg. In addition, some target compounds exhibited insecticidal activities against lepidopteran pests. From a molecular design standpoint, the information obtained in this study could help in the further design of new derivatives with improved insecticidal activities.

  17. Effects of slow-release urea fertilizers on urease activity,microbial biomass, and nematode communities in an aquic brown soil

    Institute of Scientific and Technical Information of China (English)

    JIAO; Xiaoguang; LIANG; Wenju; CHEN; Lijun; ZHANG; Haijun

    2005-01-01

    A field experiment was carried out at the Shenyang Experimental Station of Ecology (CAS) in order to study the effects of slow-release urea fertilizers high polymer-coated urea (SRU1), SRU1 mixed with dicyandiamide DCD (SRU2), and SRU1 mixed with calcium carbide CaC2 (SRU3) on urease activity, microbial biomass C and N, and nematode communities in an aquic brown soil during the maize growth period. The results demonstrated that the application of slow-release urea fertilizers inhibits soil urease activity and increases the soil NH4+-N content.Soil available N increment could promote its immobilization by microorganisms. Determination of soil microbial biomass N indicated that a combined application of coated urea and nitrification inhibitors increased the soil active N pool. The population of predators/omnivores indicated that treatment with SRU2 could provide enough soil NH4+-N to promote maize growth and increased the food resource for the soil fauna compared with the other treatments.

  18. Physiological and transcriptomic aspects of urea uptake and assimilation in Arabidopsis plants.

    Science.gov (United States)

    Mérigout, Patricia; Lelandais, Maud; Bitton, Frédérique; Renou, Jean-Pierre; Briand, Xavier; Meyer, Christian; Daniel-Vedele, Françoise

    2008-07-01

    Urea is the major nitrogen (N) form supplied as fertilizer in agriculture, but it is also an important N metabolite in plants. Urea transport and assimilation were investigated in Arabidopsis (Arabidopsis thaliana). Uptake studies using (15)N-labeled urea demonstrated the capacity of Arabidopsis to absorb urea and that the urea uptake was regulated by the initial N status of the plants. Urea uptake was stimulated by urea but was reduced by the presence of ammonium nitrate in the growth medium. N deficiency in plants did not affect urea uptake. Urea exerted a repressive effect on nitrate influx, whereas urea enhanced ammonium uptake. The use of [(15)N]urea and [(15)N]ammonium tracers allowed us to show that urea and ammonium assimilation pathways were similar. Finally, urea uptake was less efficient than nitrate uptake, and urea grown-plants presented signs of N starvation. We also report the first analysis, to our knowledge, of Arabidopsis gene expression profiling in response to urea. Our transcriptomic approach revealed that nitrate and ammonium transporters were transcriptionally regulated by urea as well as key enzymes of the glutamine synthetase-glutamate synthase pathway. AtDUR3, a high-affinity urea transporter in Arabidopsis, was strongly up-regulated by urea. Moreover, our transcriptomic data suggest that other genes are also involved in urea influx.

  19. From silicon(II)-based dioxygen activation to adducts of elusive dioxasiliranes and sila-ureas stable at room temperature

    Science.gov (United States)

    Xiong, Yun; Yao, Shenglai; Müller, Robert; Kaupp, Martin; Driess, Matthias

    2010-07-01

    Dioxygen activation for the subsequent oxygenation of organic substrates that involves cheap and environmentally friendly chemical elements is at the cutting edge of chemical research. As silicon is a non-toxic and highly oxophilic element, the use of silylenes could be attractive for facile dioxygen activation to give dioxasiliranes with a SiO2-peroxo ring as versatile oxo-transfer reagents. However, the latter are elusive species, and have been generated and studied only in argon matrices at -233 °C. Recently, it was demonstrated that unstable silicon species can be isolated by applying the concept of donor-acceptor stabilization. We now report the first synthesis and crystallographic characterization of dioxasiliranes stabilized by N-heterocyclic carbenes that feature a three-membered SiO2-peroxide ring, isolable at room temperature. Unexpectedly, these can undergo internal oxygen transfer in toluene solution at ambient temperature to give a unique complex of cyclic sila-urea with C=O --> Si=O interaction and the shortest Si=O double-bond distance reported to date.

  20. Urea transformation of wetland microbial communities.

    Science.gov (United States)

    Thorén, Ann-Karin

    2007-02-01

    Transformation of urea to ammonium is an important link in the nitrogen cycle in soil and water. Although microbial nitrogen transformations, such as nitrification and denitrification, are well studied in freshwater sediment and epiphytic biofilm in shallow waters, information about urea transformation in these environments is scarce. In this study, urea transformation of sedimentary, planktonic, and epiphytic microbial communities was quantified and urea transformation of epiphytic biofilms associated with three different common wetland macrophyte species is compared. The microbial communities were collected from a constructed wetland in October 2002 and urea transformation was quantified in the laboratory at in situ temperature (12 degrees C) with the use of the 14C-urea tracer method, which measures the release of 14CO2 as a direct result of urease activity. It was found that the urea transformation was 100 times higher in sediment (12-22 mmol urea-N m(-2) day(-1)) compared with the epiphytic activity on the surfaces of the submerged plant Elodea canadensis (0.1-0.2 mmol urea-N m(-2) day(-1)). The epiphytic activity of leaves of Typha latifolia was lower (0.001-0.03 mmol urea-N m(-2) day(-1)), while urea transformation was negligible in the water column and on the submerged leaves of the emergent plant Phragmites australis. However, because this wetland was dominated by dense beds of the submerged macrophyte E. canadensis, this plant provided a large surface area for epiphytic microbial activity-in the range of 23-33 m2 of plant surfaces per square meter of wetland. Thus, in the wetland system scale at the existing plant distribution and density, the submerged plant community had the potential to transform 2-7 mmol urea-N m(-2) day(-1) and was in the same magnitude as the urea transformation in the sediment.

  1. Engineered nano-magnetic iron oxide-urea-activated carbon nanolayer sorbent for potential removal of uranium (VI) from aqueous solution

    Science.gov (United States)

    Mahmoud, Mohamed E.; Khalifa, Mohamed A.; El Wakeel, Yasser M.; Header, Mennatllah S.; Abdel-Fattah, Tarek M.

    2017-04-01

    A novel magnetic nanosorbent was designed using chemical grafting of nano-magnetite (Nano-Fe3O4) with nanolayer of activated carbon (AC) via urea intermediate for the formation of Nano-Fe3O4-Urea-AC. Characterizing was carried out using FT-IR, SEM, HR-TEM, TGA, point of zero charge (Pzc) and surface area analysis. The designed sorbent maintained its magnetic properties and nanosized structure in the range of 8.7-14.1 nm. The surface area was identified as 389 m2/g based on the BET method. Sorption of uranyl ions from aqueous solutions was studied and evaluated in different experimental conditions. Removal of uranyl ions increased with increasing in pH value and the maximum percentage removal was established at pH 5.0. The removal and sorption processes of uranyl ions by Nano-Fe3O4-Urea-AC sorbent were studied and optimized using the batch technique. The key variables affecting removal of uranyl ions were studied including the effect of the contact time, dosage of Nano-Fe3O4-Urea-AC sorbent, reaction temperature, initial uranyl ions concentration and interfering anions and cations.

  2. The Transport Properties of Activated Carbon Fibers

    Science.gov (United States)

    di Vittorio, S. L.; Dresselhaus, M. S.; Endo, M.; Issi, J-P.; Piraux, L.

    1990-07-01

    The transport properties of activated isotropic pitch-based carbon fibers with surface area 1000 m{sup 2}/g have been investigated. We report preliminary results on the electrical conductivity, the magnetoresistance, the thermal conductivity and the thermopower of these fibers as a function of temperature. Comparisons are made to transport properties of other disordered carbons.

  3. BASIC SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME PHOSPHORCONTATNING ORGANIC COMPOUNDS CONTAINING FRAGMENTS OF UREA AND TRYHLORETILAMID

    Directory of Open Access Journals (Sweden)

    Gushylyk B.

    2013-10-01

    Full Text Available Data about directions of synthesis and use of the phosphororganic compounds in technics, biology and medicine is presented in the paper. Antimicrobial activity of 51 phosphororganic salts and ilides containing urine and threechlor ethylenamide has been studied. Perspective of the development of effective antimicrobial substances has been determined

  4. Insecticidal benzoylphenyl ureas: structure-activity relationships as chitin synthesis inhibitors.

    Science.gov (United States)

    Hajjar, N P; Casida, J E

    1978-06-30

    The 1-benzoyl-3-phenylurea insecticide diflubenzuron is a potent inhibitor for the conversion of (14)C-labeled glucose to (14)C-labeled chitin in isolated abdomens of newly emerged adult milkweed bugs (Oncopeltus fasciatus Dallas). The inhibitory activity of 24 diflubenzuron analogs in this in vitro chitin-synthesizing system is in good agreement with their toxicity to fifth instar nymphs of this species. These insecticides act quickly and directly within the integument to ultimately block the terminal polymerization step in chitin formation.

  5. Synthesis of Urea based Chalcone Derivatives and Evaluate its Biological Activity

    Directory of Open Access Journals (Sweden)

    Arpita Desai

    2016-05-01

    Full Text Available Chalcones have been the center of attraction for researchers from several decades due to nits innumerous therapeutic application, Efforts have been done in my research to synthesized chalcones and their derivatives that further reacts with various substituted aldehyde to give corresponding substituted chalcone derivatives. Now these derivatives on condensation with Guanidine nitrate gives the vast range of phenyl pyrimidine amine Derivatives. Structure elucidation of synthesized compound had been made on the basis of element analysis, 1H NMR Spectra studies. The microbial activity of the synthesized compounds has been studied against the species bacillus subtillis, staphylococcus aureus, Escherichia coli, and salmonella typhi.

  6. Nonisothermal activation: nonlinear transport theory

    NARCIS (Netherlands)

    Dekker, H.; Maassen van den Brink, A.

    1998-01-01

    We present the statistical mechanical foundation of nonisothermal stochastic processes, thereby generalizing Kramers' Fokker-Planck model for thermal activation and providing a microscopic context for Rolf Landauer's original ideas on state-dependent diffusion. By applying projection operator method

  7. Colorimetric detection of urea, urease, and urease inhibitor based on the peroxidase-like activity of gold nanoparticles.

    Science.gov (United States)

    Deng, Hao-Hua; Hong, Guo-Lin; Lin, Feng-Lin; Liu, Ai-Lin; Xia, Xing-Hua; Chen, Wei

    2016-04-07

    Herein, we reported for the first time that gold nanoparticles-catalyzed 3,3',5,5'-tetramethylbenzidine-H2O2 system can serve as an ultrasensitive colorimetric pH indicator. Gold nanoparticles acted as a catalyst and imitated the function of horseradish peroxidase. The absorbance at 450 nm of the yellow-color product in the catalytic reaction exhibited a linear fashion over the pH range of 6.40-6.60. On the basis of this property, we constructed a novel sensing platform for the determination of urea, urease, and urease inhibitor. The limit of detection for urea and urease was 5 μM and 1.8 U/L, respectively. The half-maximal inhibition value IC50 of acetohydroxamic acid was found to be 0.05 mM. Urea in human urine and urease in soil were detected with satisfied results.

  8. [Short-term changes of pH value and Al activity in acid soils after urea fertilization].

    Science.gov (United States)

    Zeng, Qingru; Liao, Bohan; Jiang, Zhaohui; Zhou, Xihong; Tang, Can; Zhong, Ning

    2005-02-01

    Acidic soils are widely distributed in South China, and their acidity is the major environmental stress factor limiting the growth of most crops. It is well known that soil Al solubilized at low pH is a main toxic factor for plant growth. Our study with three acidic soils showed that soil pH increased quickly, while soil exchangeable Al decreased sharply with the increasing concentrations of applied urea. The time-course experiment revealed that the increase of soil pH was short-lived, with a subsequently slow drop after reached its maximum. Urea fertilization caused a drastic change of soil pH during 2-4 weeks of the experimental period. There was a negative relationship between soil pH and soil exchangeable Al. Biological toxicity test demonstrated that applying urea to acidic soils could obviously decrease the aluminum toxicity of maize in a short-term period.

  9. Hereditary urea cycle abnormality

    Science.gov (United States)

    ... vitro so the specific genetic cause is known. Teamwork between parents, the affected child, and doctors can help prevent severe illness. Alternative Names Abnormality of the urea cycle - hereditary; Urea cycle - hereditary abnormality Images Male urinary system Urea cycle References Lichter-Konecki ...

  10. Stable activity of a deubiquitylating enzyme (Usp2-cc) in the presence of high concentrations of urea and its application to purify aggregation-prone peptides.

    Science.gov (United States)

    Shahnawaz, Mohammad; Thapa, Arjun; Park, Il-Seon

    2007-08-03

    Chemical synthesis of long or aggregation-prone peptide has been problematic. Its biological production has an advantage in that point, but it often forms inclusion body which creates difficulties in recovery of targets. As a deubiquitylating enzyme (Usp2-cc) was shown in this study to maintain its activity even in the presence of up to 4M urea, target peptide was purified by a single step of chromatography after overexpression as inclusion body, solubilization in urea and cleavage by the enzyme from the fusion protein consisting of GroES (used for high expression and easy to handle), ubiquitin (as a cleavage site) and target peptide. This system is a convenient tool for production of peptides that are difficult to be chemically synthesized and biologically purified.

  11. Effects of Some Management Practices on Electron Transport System (ETS) Activity in Paddy Soil

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    Electron transport system (ETS)/dehydrogenase activity in a paddy field soil was measured under a variety of incubation conditions using the reduction of 2-(p-iodophenyl-3-(p-nitrophenyl)-5-phenyl tetrazolium chloride (INT) to iodonitrotetrazolium formazan (INTF). The results exhibited a high positive correlation between the ETS activity and the incubation temperature and soil moisture. Dehydrogenase/ETS activity displayed a negative correlation with insecticide concentrations, and the activity affected adversely as the concentration of the insecticide increased. The higher doses, 5 and 10 field rates (1 field rate = 1500 mL ha-1), of insecticide significantly inhibited ETS activity, while lower rates failed to produce any significant reducing effect. Inorganic N (as urea) of concentrations from 0 to 100 μg N g-1 soil showed a positive response to ETS activity. However, at concentrations of 200 and 400μg N g-1, the activity was reduced significantly.

  12. First Cost Calculation Methods for Road Freight Transport Activity

    Directory of Open Access Journals (Sweden)

    Kovács György

    2017-06-01

    Full Text Available The transport activity is one of the most expensive processes in the supply chain. Forwarding and transport companies focuses on the optimization of transportation and the reduction of transport costs.

  13. 缩短1620t/dCO_2气提尿素工艺熔融尿液泵倒运时间%Shortening Transport Time of Melting Urea Liquid Pump in 1620T/D Carbon Dioxide Gas Stripping Urea Process

    Institute of Scientific and Technical Information of China (English)

    肖锡骏

    2012-01-01

    From the daily maintenance of production, through a simple technical improvement, the problem of evaporation system to transport device needed to stop melt urea pump was solved. Through transporting melt urea pump online, the transportation time was shortened, evaporation circulating long time was uret was reduced, consumption of steam and CO2 was decreased, with improved quality pass, reduced production cost. avoided, generation of bi- of product and percent of%从日常生产维护出发,通过技术改造解决了装置需停蒸发系统才能倒运熔融尿液泵的难题,通过在线倒运熔融尿液泵,缩短了倒运时间,避免了蒸发长时间打循环,减少成品缩二脲的生成,降低了蒸汽耗量和CO2耗量,提高了产品质量合格率,降低了生产成本。

  14. Development of novel active transport membrande devices

    Energy Technology Data Exchange (ETDEWEB)

    Laciak, D.V.

    1994-11-01

    Air Products has undertaken a research program to fabricate and evaluate gas separation membranes based upon promising ``active-transport`` (AT) materials recently developed in our laboratories. Active Transport materials are ionic polymers and molten salts which undergo reversible interaction or reaction with ammonia and carbon dioxide. The materials are useful for separating these gases from mixtures with hydrogen. Moreover, AT membranes have the unique property of possessing high permeability towards ammnonia and carbon dioxide but low permeability towards hydrogen and can thus be used to permeate these components from a gas stream while retaining hydrogen at high pressure.

  15. Health Impacts of Active Transportation in Europe.

    Directory of Open Access Journals (Sweden)

    David Rojas-Rueda

    Full Text Available Policies that stimulate active transportation (walking and bicycling have been related to heath benefits. This study aims to assess the potential health risks and benefits of promoting active transportation for commuting populations (age groups 16-64 in six European cities. We conducted a health impact assessment using two scenarios: increased cycling and increased walking. The primary outcome measure was all-cause mortality related to changes in physical activity level, exposure to fine particulate matter air pollution with a diameter <2.5 μm, as well as traffic fatalities in the cities of Barcelona, Basel, Copenhagen, Paris, Prague, and Warsaw. All scenarios produced health benefits in the six cities. An increase in bicycle trips to 35% of all trips (as in Copenhagen produced the highest benefits among the different scenarios analysed in Warsaw 113 (76-163 annual deaths avoided, Prague 61 (29-104, Barcelona 37 (24-56, Paris 37 (18-64 and Basel 5 (3-9. An increase in walking trips to 50% of all trips (as in Paris resulted in 19 (3-42 deaths avoided annually in Warsaw, 11(3-21 in Prague, 6 (4-9 in Basel, 3 (2-6 in Copenhagen and 3 (2-4 in Barcelona. The scenarios would also reduce carbon dioxide emissions in the six cities by 1,139 to 26,423 (metric tonnes per year. Policies to promote active transportation may produce health benefits, but these depend of the existing characteristics of the cities. Increased collaboration between health practitioners, transport specialists and urban planners will help to introduce the health perspective in transport policies and promote active transportation.

  16. Regulators of Slc4 bicarbonate transporter activity

    Directory of Open Access Journals (Sweden)

    Ian M. Thornell

    2015-06-01

    Full Text Available The Slc4 family of transporters is comprised of anion exchangers (AE1-4, Na-coupled bicarbonate transporters (NCBTs including electrogenic Na/bicarbonate cotransporters (NBCe1 and NBCe2, electroneutral Na/bicarbonate cotransporters (NBCn1 and NBCn2, and the electroneutral Na-driven Cl-bicarbonate exchanger (NDCBE, as well as a borate transporter (BTR1. These transporters regulate intracellular pH (pHi and contribute to steady-state pHi, but are also involved in other physiological processes including CO2 carriage by red blood cells and solute secretion/reabsorption across epithelia. Acid-base transporters function as either acid extruders or acid loaders, with the Slc4 proteins moving HCO3– either into or out of cells. According to results from both molecular and functional studies, multiple Slc4 proteins and/or associated splice variants with similar expected effects on pHi are often found in the same tissue or cell. Such apparent redundancy is likely to be physiologically important. In addition to regulating pHi, a HCO3– transporter contributes to a cell’s ability to fine tune the intracellular regulation of the cotransported/exchanged ion(s (e.g., Na+ or Cl–. In addition, functionally similar transporters or splice variants with different regulatory profiles will optimize pH physiology and solute transport under various conditions or within subcellular domains. Such optimization will depend on activated signaling pathways and transporter expression profiles. In this review, we will summarize and discuss both classical and more recently identified regulators of the Slc4 proteins. Some of these regulators include traditional second messengers, lipids, binding proteins, autoregulatory domains, and less conventional regulators. The material presented will provide insight into the diversity and physiological significance of multiple members within the Slc4 gene family.

  17. [Urea formation in the after operational liver].

    Science.gov (United States)

    Savilov, P N

    2016-01-01

    The effect of resection of the left lobe of the liver (LR, 15-20% og the organ weight) on hepatic urea formation was investigated in 84 albino rats. The objects of study were the surgery left (LLP), inoperable middle (MLP) lobe of the liver, blood (aorta, v. hepatica, v. porta) and choledochal bile. They studied the urea content. Arginase activity was examined in liver homogenate. On the day 3 and day 7 after resection reduced arginase activity was detected. LR caused a decrease of urea in v. hepatica, but increased urea content in the arterial blood and v. porta. Increase in bile urea on day 7 it was replaced by a decrease observed on day 14 of the postsurgery period. The concentration of urea in the liver on the 3rd day after LR was below the norm, and on the 7th and 14th day was within it. The results indicate a violation of urea operated by hepatocytes of the liver and extrahepatic activation mechanisms of the formation of urea.

  18. Urea retranslocation from senescing Arabidopsis leaves is promoted by DUR3-mediated urea retrieval from leaf apoplast.

    Science.gov (United States)

    Bohner, Anne; Kojima, Soichi; Hajirezaei, Mohammad; Melzer, Michael; von Wirén, Nicolaus

    2015-02-01

    In plants, urea derives either from root uptake or protein degradation. Although large quantities of urea are released during senescence, urea is mainly seen as a short-lived nitrogen (N) catabolite serving urease-mediated hydrolysis to ammonium. Here, we investigated the roles of DUR3 and of urea in N remobilization. During natural leaf senescence urea concentrations and DUR3 transcript levels showed a parallel increase with senescence markers like ORE1 in a plant age- and leaf age-dependent manner. Deletion of DUR3 decreased urea accumulation in leaves, whereas the fraction of urea lost to the leaf apoplast was enhanced. Under natural and N deficiency-induced senescence DUR3 promoter activity was highest in the vasculature, but was also found in surrounding bundle sheath and mesophyll cells. An analysis of petiole exudates from wild-type leaves revealed that N from urea accounted for >13% of amino acid N. Urea export from senescent leaves further increased in ureG-2 deletion mutants lacking urease activity. In the dur3 ureG double insertion line the absence of DUR3 reduced urea export from leaf petioles. These results indicate that urea can serve as an early metabolic marker for leaf senescence, and that DUR3-mediated urea retrieval contributes to the retranslocation of N from urea during leaf senescence.

  19. Synthesis and Bioactivity of Novel Fluorinated Heteroaromatic Ureas

    Institute of Scientific and Technical Information of China (English)

    Xin Jian SONG; Xiao Hong TAN; Yan Gang WANG

    2006-01-01

    In order to find new urea cytokinins, a series of novel fluorinated heteroaromatic ureas have been designed and synthesized. The crystal structure of 3g was further determined by single crystal X-ray diffraction to obtain the structural feature of this class of urea compounds. The preliminary bioassay showed that some title compounds have good cytokinin activity.

  20. Ammonia and urea permeability of mammalian aquaporins

    DEFF Research Database (Denmark)

    Litman, Thomas; Søgaard, Rikke; Zeuthen, Thomas

    2009-01-01

    The human aquaporins,AQP3,AQP7, AQP8,AQP9, and possibly AQP10, are permeable to ammonia, and AQP7, AQP9, and possibly AQP3, are permeable to urea. In humans, these aquaporins supplement the ammonia transport of the Rhesus (Rh) proteins and the urea transporters (UTs). The mechanism by which...... ammonium is transported by aquaporins is not fully resolved. A comparison of transport equations, models, and experimental data shows that ammonia is transported in its neutral form, NH(3). In the presence of NH(3), the aquaporin stimulates H(+) transport. Consequently, this transport of H(+) is only...... significant at alkaline pH. It is debated whether the H(+) ion passes via the aquaporin or by some external route; the investigation of this problem requires the aquaporin-expressing cell to be voltage-clamped. The ammonia-permeable aquaporins differ from other aquaporins by having a less restrictive aromatic...

  1. Synthesis and pharmacological activity of urea and thiourea derivatives of 4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione.

    Science.gov (United States)

    Struga, Marta; Kossakowski, Jerzy; Kedzierska, Ewa; Fidecka, Sylwia; Stefańska, Joanna

    2007-05-01

    A series of nineteen new thiourea and urea derivatives of 10-isopropyl-8-methyl-4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione, 1-isopropyl-7-methyl-4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione and 1,7,8,9,10-pentamethyl-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5-dione have been prepared and studied by (1)H-NMR. The compound k1a (1-(1,7,8,9,10-pentamethyl-3,5-dioxo-4-aza-tricyclo[5.2.1.0(2,6)]dec-8-en-4-yl)-3-phenyl-urea) was tested for pharmacological activity on animal central nervous system (CNS). The activities of synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells. Antimicrobial activity of the newly obtained derivatives was tested against some Gram-positive and Gram-negative bacteria and fungi of the Candida species.

  2. Synthesis and characterization of new thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[] isoxazole: In vitro Antimicrobial and Antioxidant activity

    Indian Academy of Sciences (India)

    Hasti Sudhamani; S K Thaslim Basha; Nagam Venkateswarlu; Tartte Vijaya; Chamarthi Nagaraju

    2015-10-01

    A new class of antimicrobial and antioxidant agents, based on thiourea and urea derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[] isoxazole were synthesized by adopting a simple and efficient method. Synthesized compounds were characterized by spectral data of IR, 1H, 13C NMR and mass spectra. The compounds were evaluated for their efficacy as antimicrobial and antioxidant agents. A few compounds showed good antibacterial, antifungal and antioxidant activity when compared to standard drugs and thus represent a new class of promising lead compounds.

  3. Facile synthesis of nitrogen-doped graphene via pyrolysis of graphene oxide and urea, and its electrocatalytic activity toward the oxygen-reduction reaction

    Energy Technology Data Exchange (ETDEWEB)

    Lin, Ziyin; Waller, Gordon; Liu, Yan; Liu, Meilin [School of Materials Science and Engineering, Georgia Institube of Technology, Atlanta, Georgia (United States); Wong, Ching-Ping [School of Materials Science and Engineering, Georgia Institube of Technology, Atlanta, Georgia (United States); Department of Electronic Engineering, Chinese University of Hong Kong (China)

    2012-07-15

    Nitrogen-doped graphene (NG) is a promising metal-free catalyst for the oxygen-reduction reaction (ORR). A facile and low-cost synthesis of NG via the pyrolysis of graphene oxide and urea is reported. The N content in NG can be up to 7.86%, with a high percentage of graphitic N({approx}24%), which gives rise to an excellent catalytic activity toward the ORR. (Copyright copyright 2012 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  4. Comparative studies on the mineralization of furfural urea and urea ...

    African Journals Online (AJOL)

    Comparative studies on the mineralization of furfural urea and urea fertilizers in ... conducted to evaluate the effects of furfural urea as a slow release N fertilizer in ... The controlled or slow availability supplies N continuously over an extended ...

  5. Green synthesis, optical properties and catalytic activity of silver nanoparticles in the synthesis of N-monosubstituted ureas in water.

    Science.gov (United States)

    Nasrollahzadeh, Mahmoud; Babaei, Ferydon; Sajadi, S Mohammad; Ehsani, Ali

    2014-11-11

    We report the green synthesis of silver nanoparticles by using Euphorbia condylocarpa M. bieb root extract for the synthesis of N-monosubstituted ureas in water. UV-visible studies show the absorption band at 420 nm due to surface plasmon resonance (SPR) of the silver nanoparticles. This reveals the reduction of silver ions (Ag+) to silver (Ago) which indicates the formation of silver nanoparticles (Ag NPs). This method has the advantages of high yields, simple methodology and easy work up. Copyright © 2014 Elsevier B.V. All rights reserved.

  6. Synthesis of magnetic Pb/Fe304/Si02 and its catalytic activity for propylene carbonate synthesis via urea and 1,2-propylene glycol

    Institute of Scientific and Technical Information of China (English)

    Hualiang AN; Xinqiang ZHAO; Zhiguang JIA; Changcheng WU; Yanji WANG

    2009-01-01

    To facilitate the recovery of Pb/SiO2 catalyst, magnetic Pb/Fe3O4/SiO2 samples were prepared separately by emulsification, sol-gel and incipient impregnation methods. The catalyst samples were characterized by means of X-ray diffraction and N2 adsorption-desorption, and their catalytic activity was investigated in the reaction for synthesizing propylene carbonate from urea and 1,2-propylene glycol. When the gelatin was applied in the preparation of Fe3O4 at 60°C and the pH value was controlled at 4 in the preparation of Fe3O4/SiO2, the Pb/ Fe3O4/SiO2 sample shows good catalytic activity and magnetism. Under the reaction conditions of a reaction temperature of 180°C, reaction time of 2 h, catalyst percentage of 1.7 wt-% and a molar ratio of urea to PG of 1:4, the yield of propylene carbonate attained was 87.7%.

  7. Urea hydrolysis and calcium carbonate reaction fronts

    Science.gov (United States)

    Fox, D. T.; Redden, G. D.; Henriksen, J.; Fujita, Y.; Guo, L.; Huang, H.

    2010-12-01

    The mobility of toxic or radioactive metal contaminants in subsurface environments can be reduced by the formation of mineral precipitates that form co-precipitates with the contaminants or that isolate them from the mobile fluid phase. An engineering challenge is to control the spatial distribution of precipitation reactions with respect to: 1) the location of a contaminant, and 2) where reactants are introduced into the subsurface. One strategy being explored for immobilizing contaminants, such as Sr-90, involves stimulating mineral precipitation by forming carbonate ions and hydroxide via the in situ, microbially mediated hydrolysis of urea. A series of column experiments have been conducted to explore how the construction or design of such an in situ reactant production strategy can affect the temporal and spatial distribution of calcium carbonate precipitation, and how the distribution is coupled to changes in permeability. The columns were constructed with silica gel as the porous media. An interval midway through the column contained an adsorbed urease enzyme in order to simulate a biologically active zone. A series of influent solutions were injected to characterize hydraulic properties of the column (e.g., bromide tracer), profiles of chemical conditions and reaction products as the enzyme catalyzes urea hydrolysis (e.g., pH, ammonia, urea), and changes that occur due to CaCO3 precipitation with the introduction of a calcium+urea solutions. In one experiment, hydraulic conductivity was reduced as precipitate accumulated in a layer within the column that had a higher fraction of fine grained silica gel. Subsequent reduction of permeability and flow (for a constant head condition) resulted in displacement of the hydrolysis and precipitation reaction profiles upstream. In another experiment, which lacked the physical heterogeneity (fine grained layer), the precipitation reaction did not result in loss of permeability or flow velocity and the reaction profile

  8. Anti-HIV activity of HEPT, TIBO, and cyclic urea derivatives: structure-property studies, focused combinatorial library generation, and hits selection using substructural molecular fragments method.

    Science.gov (United States)

    Solov'ev, V P; Varnek, A

    2003-01-01

    Substructural molecular fragments (SMF) method [Solov'ev, V. P.; Varnek, A.; Wipff, G. J. Chem. Inf. Comput. Sci. 2000, 40, 847-858] was applied to assess anti-HIV activity for large data sets for three families of compounds: 1-[2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives, tetrahydroimidazobenzodiazepinone (TIBO) derivatives, and cyclic urea (CU) derivatives. The SMF method uses 49 types of topological descriptors (atom/bond sequences and "augmented atoms") which, being coupled with 3 linear and nonlinear fitting equations, allows the user to generate up to 147 structure-property models. For each family of compounds, the modeling was performed on several training sets followed by the validation calculations where three best fit models were applied. Calculated activities well reproduce available experimental data. On the basis of the "optimal" molecular fragments, the focused combinatorial library containing 252 virtual HEPT derivatives has been generated. Its filtering led to several hits potentially possessing anti-HIV activity.

  9. Use of Several Plant Materials and Chemicals to inhibit Soil Urease Activity and Increase Nitrogen Recovery Rate of Urea by Plant

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Effects of residues of 9 plants, lemon eucalyptus (Eucalyptus citriodora Hook., P1), robust eucalyptus (E. robusta Smith, P2), Nepal camphortree (Cinnamomum glanduliferum (Wall.) Nees, P3), tea (Camellia sinensis (Linn.) O. Ktze. f., P4), oleander (Nerium indicum Mill, P5), rape (Brassica campestris L., P6),Chinese tallow tree (Sapium sebiferum L., P7), tung (Vernicia fordii (Hemsl.), P8), and croton (Croton tiglium L., P9), 7 chemicals, boric acid (C1), borax (C2), oxalic acid (C3), sodium oxalite (C4), sodium dihydrogen phosphate (C6), sodium silicate (C7) and sodium citrate (C8), and a natural organic substance,humic acid (C5), on urease activity of a neutral purple soil and recovery of urea nitrogen by maize were studied through incubation and pot experiments. Hydroquinone (HQ) was applied as the reference inhibitor. After incubation at 37 ℃ for 24 h, 7 inhibitors with higher ability to inhibit urease activity were selected and then incubated for 14 days at 25 ℃. Results of the incubation experiments showed that soil urease activity was greatly inhibited by them, and the inhibition effect followed an order of P2>P4>C3>C2>P3>C1>HQ>P1.The 7 selected materials reduced the accumulative amounts of N released from urea and the maximum urease activity by 11.7%~28.4% and 26.7%~39.7%, respectively, and postponed the N release peak by 2~4 days in the incubation period of 14 days under constant temperature, as compared to the control (no inhibitor).In the pot experiment with the 7 materials at two levels of addition, low (L) and high (H), the C1 (H), C3(H), C1 (L), P4 (L) and C2 (L) treatments could significantly increase the dry weights of the aboveground parts and the total biomass of the maize plants and the apparent recovery rate of urea-N was increased by 6.3%~32.4% as compared to the control (no hibitor).

  10. Effect of a static magnetic field of 7 mT on formaldehyde biodegradation in industrial wastewater from urea-formaldehyde resin production by activated sludge.

    Science.gov (United States)

    Łebkowska, Maria; Narożniak-Rutkowska, Anna; Pajor, Elżbieta

    2013-03-01

    The goal of this study was to assess the efficiency of treating industrial urea-formaldehyde wastewater by activated sludge in a static magnetic field (MF) of 7 mT and the efficiency of treating the wastewater in a bioreactor not exposed to an MF. Exposure to the MF increased formaldehyde (FA) removal from industrial wastewater with an FA concentration of 1600 mg/l by 20%. The MF had also a positive effect on the efficiency of chemical oxygen demand (COD) removal, and bacteria and activated sludge biomass growth, especially when the COD loading increased rapidly. Industrial wastewater may contain up to 13000 mg FA/l. Therefore, its treatment can require the application of more than one method to ensure that the final FA concentration will be within the permissible limit. The application of an MF to enhance the biological processes may be favourable solution to this problem.

  11. Berberine acutely activates the glucose transport activity of GLUT1.

    Science.gov (United States)

    Cok, Alexandra; Plaisier, Christina; Salie, Matthew J; Oram, Daniel S; Chenge, Jude; Louters, Larry L

    2011-07-01

    Berberine, which has a long history of use in Chinese medicine, has recently been shown to have efficacy in the treatment of diabetes. While the hypoglycemic effect of berberine has been clearly documented in animal and cell line models, such as 3T3-L1 adipocytes and L6 myotube cells, the mechanism of action appears complex with data implicating activation of the insulin signaling pathway as well as activation of the exercise or AMP kinase-mediated pathway. There have been no reports of the acute affects of berberine on the transport activity of the insulin-insensitive glucose transporter, GLUT1. Therefore, we examined the acute effects of berberine on glucose uptake in L929 fibroblast cells, a cell line that express only GLUT1. Berberine- activated glucose uptake reaching maximum stimulation of five-fold at >40 μM. Significant activation (P berberine effect was not additive to the maximal stimulation by other known stimulants, azide, methylene blue or glucose deprivation, suggesting shared steps between berberine and these stimulants. Berberine significantly reduced the K(m) of glucose uptake from 6.7 ± 1.9 mM to 0.55 ± 0.08 mM, but had no effect on the V(max) of uptake. Compound C, an inhibitor of AMP kinase, did not affect berberine-stimulated glucose uptake, but inhibitors of downstream kinases partially blocked berberine stimulation. SB203580 (inhibitor of p38 MAP kinase) did not affect submaximal berberine activation, but did lower maximal berberine stimulation by 26%, while PD98059 (inhibitor of ERK kinase) completely blocked submaximal berberine activation and decreased the maximal stimulation by 55%. It appears from this study that a portion of the hypoglycemic effects of berberine can be attributed to its acute activation of the transport activity of GLUT1.

  12. Transport in active systems crowded by obstacles

    Science.gov (United States)

    Huang, Mu-Jie; Schofield, Jeremy; Kapral, Raymond

    2017-02-01

    The reactive and diffusive dynamics of a single chemically powered Janus motor in a crowded medium of moving but passive obstacles is investigated using molecular simulation. It is found that the reaction rate of the catalytic motor reaction decreases in a crowded medium as the volume fraction of obstacles increases as a result of a reduction in the Smoluchowski diffusion-controlled reaction rate coefficient that contributes to the overall reaction rate. A continuum model is constructed and analyzed to interpret the dependence of the steady-state reaction rate observed in simulations on the volume fraction of obstacles in the system. The steady-state concentration fields of reactant and product are shown to be sensitive to the local structure of obstacles around the Janus motor. It is demonstrated that the active motor exhibits enhanced diffusive motion at long times with a diffusion constant that decreases as the volume fraction of crowding species increases. In addition, the dynamical properties of a passive tracer particle in a system containing many active Janus motors is studied to investigate how an active environment influences the transport of non-active species. The diffusivity of a passive tracer particle in an active medium is found to be enhanced in systems with forward-moving Janus motors due to the cooperative dynamics of these motors.

  13. PENGOLAHAN LIMBAH CAIR UREA MENGGUNAKAN PROSES GABUNGAN ACTIVATED MICROALGAE DAN NITRIFIKASI-DENITRIFIKASI AUTOTROFIK: UJI DENGAN RANCANGAN TAGUCHI

    Directory of Open Access Journals (Sweden)

    Indro Sumantri

    2012-05-01

    Full Text Available Proses konvensional untuk mengolah limbah cair industri urea biasanya menggunakan proses alga mikro atau bakteri heterotropik nitrifikasi-denitrifikasi. Proses alga mikro dapat menggunakan berbagai jenis alga mikro. Keuntungannya adalah murah karena hanya memerlukan nutrien Psedikit tetapi tidak dapat digunakan untuk menyusutkan amoniak. Proses nitrifikasi-denitrifikasi bakteri heterotropik memerlukan asupan karbon yang tinggi sehingga pengolahan menjadi mahal. Tujuan saat ini untuk penelitian adalah untuk mempelajari kombinasi yang potensial untuk proses alga mikro jenis tertentu dengan proses nitrifikasi-denitrifikasi ototrofik. Jenis alga mikro yang digunakan dalam proses alga mikro mempunyai kemampuan baik untuk penyusutan amoniak atau tahan dalam konsentrasi amoniak tinggi. Proses nitrifikasi-denitrifikasi ototrofik menggunakan bakteri nitrifikasi/lumpur sebagai biokatalis. Lumpur nitrifikasi awal adalah lumpur aktif kolam aerasi unit pengolahan limbah cair industri partikel board Pengayaan dan pembibitan lumpur nitrifikasi dilakukan dalam konsentrasi amoniak yang tinggi dan kondisi ototrofik. Berdasarkan penelitian, pengayaan dan pembibitan alga mikro yang mempunyai kemampuan untuk penyusutan amoniak dan tahan konsentrasi amoniak yang tinggi mudah. Evaluasi substrat pembatas penghambat amonium terhadap pertumbuhan alga tidak terbukti. Tujuh variabel yang dipilih lewat penapisan adalah : MLSS, waktu tinggal, konsentrasi NH3-N, laju aerasi, kadar CaCO3, nutrien mikro, rasio N:P. Variabel yang berpengaruhadalah konsentrasi NH3-N, laju aerasi, kadar CaCO3.

  14. Acinetobacter baumannii Coordinates Urea Metabolism with Metal Import To Resist Host-Mediated Metal Limitation

    Directory of Open Access Journals (Sweden)

    Lillian J. Juttukonda

    2016-09-01

    Full Text Available During infection, bacterial pathogens must adapt to a nutrient metal-limited environment that is imposed by the host. The innate immune protein calprotectin inhibits bacterial growth in vitro by chelating the divalent metal ions zinc (Zn2+, Zn and manganese (Mn2+, Mn, but pathogenic bacteria are able to cause disease in the presence of this antimicrobial protein in vivo. One such pathogen is Acinetobacter baumannii, a Gram-negative bacterium that causes pneumonia and bloodstream infections that can be complicated by resistance to multiple antibiotics. A. baumannii inhibition by calprotectin is dependent on calprotectin Mn binding, but the mechanisms employed by A. baumannii to overcome Mn limitation have not been identified. This work demonstrates that A. baumannii coordinates transcription of an NRAMP family Mn transporter and a urea carboxylase to resist the antimicrobial activities of calprotectin. This NRAMP family transporter facilitates Mn accumulation and growth of A. baumannii in the presence of calprotectin. A. baumannii is found to utilize urea as a sole nitrogen source, and urea utilization requires the urea carboxylase encoded in an operon with the NRAMP family transporter. Moreover, urea carboxylase activity is essential for calprotectin resistance in A. baumannii. Finally, evidence is provided that this system combats calprotectin in vivo, as deletion of the transporter impairs A. baumannii fitness in a mouse model of pneumonia, and this fitness defect is modulated by the presence of calprotectin. These findings reveal that A. baumannii has evolved mechanisms to subvert host-mediated metal sequestration and they uncover a connection between metal starvation and metabolic stress.

  15. A general method for determining secondary active transporter substrate stoichiometry.

    Science.gov (United States)

    Fitzgerald, Gabriel A; Mulligan, Christopher; Mindell, Joseph A

    2017-01-25

    The number of ions required to drive substrate transport through a secondary active transporter determines the protein's ability to create a substrate gradient, a feature essential to its physiological function, and places fundamental constraints on the transporter's mechanism. Stoichiometry is known for a wide array of mammalian transporters, but, due to a lack of readily available tools, not for most of the prokaryotic transporters for which high-resolution structures are available. Here, we describe a general method for using radiolabeled substrate flux assays to determine coupling stoichiometries of electrogenic secondary active transporters reconstituted in proteoliposomes by measuring transporter equilibrium potentials. We demonstrate the utility of this method by determining the coupling stoichiometry of VcINDY, a bacterial Na(+)-coupled succinate transporter, and further validate it by confirming the coupling stoichiometry of vSGLT, a bacterial sugar transporter. This robust thermodynamic method should be especially useful in probing the mechanisms of transporters with available structures.

  16. Orphan drugs in development for urea cycle disorders: current perspectives

    Directory of Open Access Journals (Sweden)

    Häberle J

    2014-09-01

    Full Text Available Johannes Häberle,1 Shawn E McCandless2 1Division of Metabolism and Children's Research Center, University Children's Hospital Zurich, Zurich, Switzerland; 2Center for Human Genetics, University Hospitals Case Medical Center, and Department of Genetics and Genome Sciences, Case Western Reserve University, Cleveland, OH, USA Abstract: The urea cycle disorders are caused by deficiency of one of the six hepatic enzymes or two transporters involved in detoxification of ammonia. The resulting hyperammonemia causes severe brain injury unless aggressive steps are taken to reduce the accumulation of ammonia, which is thought to be the most toxic metabolite. This review describes the current state of chronic management of urea cycle disorders, focusing on new and emerging therapies. Management strategies include the mainstay of treatment, namely dietary protein restriction and supplementation with l-arginine or l-citrulline. Several currently approved medications utilize and enhance alternative pathways of waste nitrogen excretion (sodium benzoate, sodium phenylacetate, sodium phenylbutyrate in several formulations, and glycerol phenylbutyrate, working through conjugation of the drug to either glycine (in the case of benzoate or glutamine, the products of which are excreted in the urine. Carglumic acid activates the first committed step of conversion of ammonia to urea, carbamoylphosphate synthetase, and thus effectively treats defective synthesis of the endogenous activator, N-acetylglutamate, whether due to genetic defects or biochemical inhibition of the N-acetylglutamate synthase enzyme. Approaches to neuroprotection during episodes of hyperammonemia are discussed, including the use of controlled hypothermia (brain cooling, as well as proposed, but as yet untested, pharmacologic therapies. Finally, cell-based therapies, including liver transplantation, infusion of fresh or cryopreserved hepatocytes, use of stem cells, and new approaches to gene

  17. Characterization of silica particles prepared via urease-catalyzed urea hydrolysis and activity of urease in sol-gel silica matrix

    Energy Technology Data Exchange (ETDEWEB)

    Kato, Katsuya, E-mail: katsuya-kato@aist.go.jp [National Institute of Advanced Industrial Science and Technology (AIST), 2266-98 Anagahora, Shimoshidami, Moriyama-ku, Nagoya 463-8560 (Japan); Nishida, Masakazu [National Institute of Advanced Industrial Science and Technology (AIST), 2266-98 Anagahora, Shimoshidami, Moriyama-ku, Nagoya 463-8560 (Japan); Ito, Kimiyasu; Tomita, Masahiro [Division of Chemistry for Materials, Graduate School of Engineering, Mie University, 1577 Kurimamachiya-cho, Tsu, Mie 514-8570 (Japan)

    2012-12-01

    Highlights: Black-Right-Pointing-Pointer Silica precipitation occurred via urease-catalytic reactions. Black-Right-Pointing-Pointer Higher urease activity for silica synthesis enables mesostructure of silica-urease composites. Black-Right-Pointing-Pointer Urease encapsulating in silica matrix retained high activity. - Abstract: Urease templated precipitation of silica synthesized by sol-gel chemistry produces a composite material allowing high urease activity. This study investigates the structural properties of the composite material that allow for the retention of the urease hydrolysis activity. Scanning (SEM) and transmission (TEM) electron microscopy reveal that the composite has a mesoporous structure composed of closely packed spherical structures {approx}20-50 nm in diameter. Brunauer-Emmett-Teller (BET) analysis revealed that the surface area and pore volume of the composite prepared under the conditions of 50 mM urea and 25 Degree-Sign C is relatively high (324 m{sup 2}/g and 1.0 cm{sup 3}/g). These values are equivalent to those of usual mesoporous silica materials synthesized from the self-assembly of triblock copolymers as organic templates. In addition, after encapsulating in a sol-gel silica matrix, urease retained high activity ({approx}90% of the activity compared with native urease). Our results suggest a new method for synthesizing mesoporous silica materials with highly tunable pore sizes and shapes under mild conditions.

  18. Ethylated Urea - Ether - Modified Urea - Formaldehyde Resins,

    Directory of Open Access Journals (Sweden)

    Mathew Obichukwu EDOGA

    2006-07-01

    Full Text Available First, phenol - formaldehyde (PF and urea - formaldehyde (UFII resins were separately conventionally prepared in our laboratory. Also, UF resin synthesized from the acid modified synthesis procedure was synthesized in a purely acid medium of pH 1.0, FU molar ratio of 1.0 and at 50oC (one-stage acid modified-synthesis procedure. Subsequently, the UF resin II was modified during synthesis by incorporating ethylated urea-ether (EUER (i.e. UFIII and glycerol (GLYC (i.e. UFV cured with and without acid curing agent. The structural and physicochemical analyses of the various resin samples were carried out.The results showed that the unmodified UF resin (UF II synthesized in acid medium of pH 1.0, F/U molar ratio 1.0, and at 50oC, cured in absence of acid curing catalyst, showed features in their spectra which are consistent with a tri-, and/or tetra-substituted urea in the reaction to give a 3 - dimensional network cured UF resin. Modification of the UF resin(UF II with ethylated urea-ether and glycerol to produce UF resins III and respectively V prominently increased the absorbance of methylene and ether groups in the spectra which are consistent with increased hydrophobicity and improved hydrolytic stability. For the conventional UF resin (UF I, the only clear distinction between spectra for the UF resin II and UF resins (III/V is the presence of diminished peaks for methylene groups at 2.2 ppm. The relationship between the logarithmic viscosity of cured PF resin with time showed continuos dependence of viscosity with time during cure up to 70 minutes. Similar trends were shown by UF resins (III/V, cured in absence of acid catalyst. In contrast, the conventional UF resins I and UF IV (i.e. UF II cured with NH4CL showed abrupt discontinuity in viscosity with time just after about 20 minutes of cure.

  19. Integration of a 'proton antenna' facilitates transport activity of the monocarboxylate transporter MCT4.

    Science.gov (United States)

    Noor, Sina Ibne; Pouyssegur, Jacques; Deitmer, Joachim W; Becker, Holger M

    2017-01-01

    Monocarboxylate transporters (MCTs) mediate the proton-coupled transport of high-energy metabolites like lactate and pyruvate and are expressed in nearly every mammalian tissue. We have shown previously that transport activity of MCT4 is enhanced by carbonic anhydrase II (CAII), which has been suggested to function as a 'proton antenna' for the transporter. In the present study, we tested whether creation of an endogenous proton antenna by introduction of a cluster of histidine residues into the C-terminal tail of MCT4 (MCT4-6xHis) could facilitate MCT4 transport activity when heterologously expressed in Xenopus oocytes. Our results show that integration of six histidines into the C-terminal tail does indeed increase transport activity of MCT4 to the same extent as did coexpression of MCT4-WT with CAII. Transport activity of MCT4-6xHis could be further enhanced by coexpression with extracellular CAIV, but not with intracellular CAII. Injection of an antibody against the histidine cluster into MCT4-expressing oocytes decreased transport activity of MCT4-6xHis, while leaving activity of MCT4-WT unaltered. Taken together, these findings suggest that transport activity of the proton-coupled monocarboxylate transporter MCT4 can be facilitated by integration of an endogenous proton antenna into the transporter's C-terminal tail.

  20. Associations between street connectivity and active transportation

    Directory of Open Access Journals (Sweden)

    Pickle Linda W

    2010-04-01

    Full Text Available Abstract Background Past studies of associations between measures of the built environment, particularly street connectivity, and active transportation (AT or leisure walking/bicycling have largely failed to account for spatial autocorrelation of connectivity variables and have seldom examined both the propensity for AT and its duration in a coherent fashion. Such efforts could improve our understanding of the spatial and behavioral aspects of AT. We analyzed spatially identified data from Los Angeles and San Diego Counties collected as part of the 2001 California Health Interview Survey. Results Principal components analysis indicated that ~85% of the variance in nine measures of street connectivity are accounted for by two components representing buffers with short blocks and dense nodes (PRIN1 or buffers with longer blocks that still maintain a grid like structure (PRIN2. PRIN1 and PRIN2 were positively associated with active transportation (AT after adjustment for diverse demographic and health related variables. Propensity and duration of AT were correlated in both Los Angeles (r = 0.14 and San Diego (r = 0.49 at the zip code level. Multivariate analysis could account for the correlation between the two outcomes. After controlling for demography, measures of the built environment and other factors, no spatial autocorrelation remained for propensity to report AT (i.e., report of AT appeared to be independent among neighborhood residents. However, very localized correlation was evident in duration of AT, particularly in San Diego, where the variance of duration, after accounting for spatial autocorrelation, was 5% smaller within small neighborhoods (~0.01 square latitude/longitude degrees = 0.6 mile diameter compared to within larger zip code areas. Thus a finer spatial scale of analysis seems to be more appropriate for explaining variation in connectivity and AT. Conclusions Joint analysis of the propensity and duration of AT behavior and an

  1. Molecular evolution of urea amidolyase and urea carboxylase in fungi

    Directory of Open Access Journals (Sweden)

    Harris Steven D

    2011-03-01

    Full Text Available Abstract Background Urea amidolyase breaks down urea into ammonia and carbon dioxide in a two-step process, while another enzyme, urease, does this in a one step-process. Urea amidolyase has been found only in some fungal species among eukaryotes. It contains two major domains: the amidase and urea carboxylase domains. A shorter form of urea amidolyase is known as urea carboxylase and has no amidase domain. Eukaryotic urea carboxylase has been found only in several fungal species and green algae. In order to elucidate the evolutionary origin of urea amidolyase and urea carboxylase, we studied the distribution of urea amidolyase, urea carboxylase, as well as other proteins including urease, across kingdoms. Results Among the 64 fungal species we examined, only those in two Ascomycota classes (Sordariomycetes and Saccharomycetes had the urea amidolyase sequences. Urea carboxylase was found in many but not all of the species in the phylum Basidiomycota and in the subphylum Pezizomycotina (phylum Ascomycota. It was completely absent from the class Saccharomycetes (phylum Ascomycota; subphylum Saccharomycotina. Four Sordariomycetes species we examined had both the urea carboxylase and the urea amidolyase sequences. Phylogenetic analysis showed that these two enzymes appeared to have gone through independent evolution since their bacterial origin. The amidase domain and the urea carboxylase domain sequences from fungal urea amidolyases clustered strongly together with the amidase and urea carboxylase sequences, respectively, from a small number of beta- and gammaproteobacteria. On the other hand, fungal urea carboxylase proteins clustered together with another copy of urea carboxylases distributed broadly among bacteria. The urease proteins were found in all the fungal species examined except for those of the subphylum Saccharomycotina. Conclusions We conclude that the urea amidolyase genes currently found only in fungi are the results of a horizontal

  2. Experimental study on a room temperature urea-SCR of NO over activated carbon fibre-supported CeO2-CuO.

    Science.gov (United States)

    Jiang, Xiao; Lu, Pei; Li, Caiting; Zeng, Zheng; Zeng, Guangming; Hu, Luping; Mai, Lei; Li, Zhi

    2013-01-01

    In order to establish a desirable method for NO reduction, selective catalytic reduction (SCR) of NO by urea-CeO2/ACF and urea-CeO2-CuO/ACF was carried out at room temperature. The experimental results showed that 10% urea-9% CeO2/ACF could yield the highest NO conversion of 85% among the series of urea-CeO2/ACF prepared. When urea-CeO2-CuO/ACF was compared with urea-CeO2/ACF, it achieved higher NO conversion to a certain degree with the addition of CuO, which was attributed to the synergistic effect between cerium and copper. The effect of the mass ratio of CeO2 and CuO was also observed. The desirable mass ratio of CeO2 and CuO was 1:1, which yielded about 90% NO conversion when ACF was loaded with 10% urea. Furthermore, the influence of O2 concentration and NO concentration was also observed. In this study, NO conversion increased with increasing O2 concentration. In addition, some samples were further characterized by BET, X-ray diffraction, X-ray photoelectron spectroscopy and Fourier transform infrared methods.

  3. Active transport among Czech school-aged children

    Directory of Open Access Journals (Sweden)

    Jan Pavelka

    2012-09-01

    Full Text Available BACKGROUND: Active transport is a very important factor for increasing the level of physical activity in children, which is significant for both their health and positive physical behaviour in adult age. OBJECTIVE: The aim of the study was to establish the proportion of Czech children aged 11 to 15 who select active transport to and from school and, at the same time, describe socio-economic and socio-demographic factors influencing active transport to and from school among children. METHODS: To establish the socio-demographic factors affecting active transport, data of a national representative sample of 11 to 15 year-old elementary school children in the Czech Republic (n = 4,425. Research data collection was performed within an international research study called Health Behaviour in School Aged Children in June 2010. Statistical processing of the results was made using a logistic regression analysis in the statistical programme IBM SPSS v 20. RESULTS: Active transport to and from school is opted for in the Czech Republic by approximately 2/3 of children aged 11 to 15. Differences between genders are not statistically significant; most children opting for active transport are aged 11 (69%. An important factor increasing the probability of active transport as much as 16 times is whether a child's place of residence is in the same municipality as the school. Other factors influencing this choice include BMI, time spent using a computer or a privateroom in a family. A significant factor determining active transport by children is safety; safe road crossing, opportunity to leave a bicycle safely at school, no fear of being assaulted on the way or provision of school lockers where children can leave their items. CONCLUSIONS: Active transport plays an important role in increasing the overall level of physical activity in children. Promotion of active transport should focus on children who spend more time using a computer; attention should also be

  4. Passenger transport and household activity patterns

    DEFF Research Database (Denmark)

    Jørgensen, Kaj

    1997-01-01

    Review of Danish passenger transport patterns and analysis of energy consumption, emissions and safety impacts for selected typical households' travelling......Review of Danish passenger transport patterns and analysis of energy consumption, emissions and safety impacts for selected typical households' travelling...

  5. Air pollution exposure: An activity pattern approach for active transportation

    Science.gov (United States)

    Adams, Matthew D.; Yiannakoulias, Nikolaos; Kanaroglou, Pavlos S.

    2016-09-01

    In this paper, we demonstrate the calculation of personal air pollution exposure during trips made by active transportation using activity patterns without personal monitors. We calculate exposure as the inhaled dose of particulate matter 2.5 μg or smaller. Two modes of active transportation are compared, and they include cycling and walking. Ambient conditions are calculated by combining mobile and stationary monitoring data in an artificial neural network space-time model. The model uses a land use regression framework and has a prediction accuracy of R2 = 0.78. Exposure is calculated at 10 m or shorter intervals during the trips using inhalation rates associated with both modes. The trips are children's routes between home and school. The average dose during morning cycling trips was 2.17 μg, during morning walking trips was 3.19 μg, during afternoon cycling trips was 2.19 μg and during afternoon walking trips was 3.23 μg. The cycling trip dose was significantly lower than the walking trip dose. The air pollution exposure during walking or cycling trips could not be strongly predicted by either the school or household ambient conditions, either individually or in combination. Multiple linear regression models regressing both the household and school ambient conditions against the dose were only able to account for, at most, six percent of the variance in the exposure. This paper demonstrates that incorporating activity patterns when calculating exposure can improve the estimate of exposure compared to its calculation from ambient conditions.

  6. The effects of urea modification and heat treatment on the process of NO2 removal by wood-based activated carbon.

    Science.gov (United States)

    Bashkova, Svetlana; Bandosz, Teresa J

    2009-05-01

    The removal of NO(2) on urea-modified and heat-treated wood-based activated carbons was studied. From the obtained results it was found that these modifications, especially when done at 950 degrees C, have a positive effect on NO(2) adsorption and on the retention of NO (the product of NO(2) reduction by carbon). The presence of moisture in the system enhances the removal of NO(2) but negatively affects the retention of NO. It is possible that the formation of active centers on the carbon surface and some increase in the volume of supermicropores during the high temperature treatment play a significant role in these removal processes. The surface of the carbons was analyzed in terms of the pK(a) distributions. The qualitative and quantitative analyses of the NO(2) adsorption products were carried out by means of FTIR and TA techniques, respectively. The main products found on the carbon surface were the NO(3) and NO(2) species.

  7. Pre-treatment urea breath test results predict the efficacy of Helicobacter pylori eradication therapy in patients with active duodenal ulcers

    Institute of Scientific and Technical Information of China (English)

    Yung-Chih Lai; Jyh-Chin Yang; Shih-Hung Huang

    2004-01-01

    AIM: To evaluate the association of pre-treatment 13C-urea breath test (UBT) results with H pyloridensity and efficacy of eradication therapy in patients with active duodenal ulcers.METHODS: One hundred and seventeen consecutive outpatients with active duodenal ulcer and H pyloriinfection were recruited. H pylori density was histologically graded according to the Sydney system. Each patient received lansoprazole (30 mg b.i.d.), clarithromycin (500 mg b.i.d.) and amoxicillin (1 g b.i.d.) for 1 week. According to pre-treatment UBT values, patients were allocated into low (<16%o),intermediate (16-35%o), and high (>35%o) UBT groups.RESULTS: A significant correlation was found between pre-treatment UBT results andHpyloridensity (P<0.001).H pylorieradication rates were 94.9%, 94.4% and 81.6%in the low, intermediate and high UBT groups, respectively (per protocol analysis, P=0.11). When patients were assigned into two groups (UBT results ≤35%o and >35%o),the eradication rates were 94.7% and 81.6%, respectively (P=0.04).CONCLUSION: The intragastric bacterial load of H pylori can be evaluated by UBT, and high pre-treatment UBT results can predict an adverse outcome of eradication therapy.

  8. Anti-Inflammatory Activity of a Novel Family of Aryl Ureas Compounds in an Endotoxin-Induced Airway Epithelial Cell Injury Model

    Science.gov (United States)

    Cabrera-Benitez, Nuria E.; Pérez-Roth, Eduardo; Casula, Milena; Ramos-Nuez, Ángela; Ríos-Luci, Carla; Rodríguez-Gallego, Carlos; Sologuren, Ithaisa; Jakubkiene, Virginija; Slutsky, Arthur S.; Padrón, José M.; Villar, Jesús

    2012-01-01

    Background Despite our increased understanding of the mechanisms involved in acute lung injury (ALI) and the acute respiratory distress syndrome (ARDS), there is no specific pharmacological treatment of proven benefit. We used a novel screening methodology to examine potential anti-inflammatory effects of a small structure-focused library of synthetic carbamate and urea derivatives in a well established cell model of lipopolysaccharide (LPS)-induced ALI/ARDS. Methodology/Principal Findings After a pilot study to develop an in vitro LPS-induced airway epithelial cell injury model, a library of synthetic carbamate and urea derivates was screened against representative panels of human solid tumor cell lines and bacterial and fungal strains. Molecules that were non-cytotoxic and were inactive in terms of antiproliferative and antimicrobial activities were selected to study the effects on LPS-induced inflammatory response in an in vitro cell culture model using A549 human alveolar and BEAS-2B human bronchial cells. These cells were exposed for 18 h to LPS obtained from Escherichia coli, either alone or in combination with the test compounds. The LPS antagonists rhein and emodin were used as reference compounds. The most active compound (CKT0103) was selected as the lead compound and the impact of CKT0103 on pro-inflammatory IL-6 and IL-8 cytokine levels, expression of toll-like receptor-4 (TLR4) and nuclear factor kappa B inhibitor alpha (IκBα) was measured. CKT0103 significantly inhibited the synthesis and release of IL-6 and IL-8 induced by LPS. This suppression was associated with inhibition of TLR4 up-regulation and IκBα down-regulation. Immunocytochemical staining for TLR4 and IκBα supported these findings. Conclusions/Significance Using a novel screening methodology, we identified a compound – CKT0103 – with potent anti-inflammatory effects. These findings suggest that CKT0103 is a potential target for the treatment of the acute phase of sepsis and

  9. Anti-inflammatory activity of a novel family of aryl ureas compounds in an endotoxin-induced airway epithelial cell injury model.

    Directory of Open Access Journals (Sweden)

    Nuria E Cabrera-Benitez

    Full Text Available BACKGROUND: Despite our increased understanding of the mechanisms involved in acute lung injury (ALI and the acute respiratory distress syndrome (ARDS, there is no specific pharmacological treatment of proven benefit. We used a novel screening methodology to examine potential anti-inflammatory effects of a small structure-focused library of synthetic carbamate and urea derivatives in a well established cell model of lipopolysaccharide (LPS-induced ALI/ARDS. METHODOLOGY/PRINCIPAL FINDINGS: After a pilot study to develop an in vitro LPS-induced airway epithelial cell injury model, a library of synthetic carbamate and urea derivates was screened against representative panels of human solid tumor cell lines and bacterial and fungal strains. Molecules that were non-cytotoxic and were inactive in terms of antiproliferative and antimicrobial activities were selected to study the effects on LPS-induced inflammatory response in an in vitro cell culture model using A549 human alveolar and BEAS-2B human bronchial cells. These cells were exposed for 18 h to LPS obtained from Escherichia coli, either alone or in combination with the test compounds. The LPS antagonists rhein and emodin were used as reference compounds. The most active compound (CKT0103 was selected as the lead compound and the impact of CKT0103 on pro-inflammatory IL-6 and IL-8 cytokine levels, expression of toll-like receptor-4 (TLR4 and nuclear factor kappa B inhibitor alpha (IκBα was measured. CKT0103 significantly inhibited the synthesis and release of IL-6 and IL-8 induced by LPS. This suppression was associated with inhibition of TLR4 up-regulation and IκBα down-regulation. Immunocytochemical staining for TLR4 and IκBα supported these findings. CONCLUSIONS/SIGNIFICANCE: Using a novel screening methodology, we identified a compound - CKT0103 - with potent anti-inflammatory effects. These findings suggest that CKT0103 is a potential target for the treatment of the acute phase of

  10. Superposition of Individual Activities: Urea-Mediated Suppression of Nitrate Uptake in the Dinoflagellate Prorocentrum minimum Revealed at the Population and Single-Cell Levels

    Science.gov (United States)

    Matantseva, Olga; Skarlato, Sergei; Vogts, Angela; Pozdnyakov, Ilya; Liskow, Iris; Schubert, Hendrik; Voss, Maren

    2016-01-01

    Dinoflagellates readily use diverse inorganic and organic compounds as nitrogen sources, which is advantageous in eutrophied coastal areas exposed to high loads of anthropogenic nutrients, e.g., urea, one of the most abundant organic nitrogen substrates in seawater. Cell-to-cell variability in nutritional physiology can further enhance the diversity of metabolic strategies among dinoflagellates of the same species, but it has not been studied in free-living microalgae. We applied stable isotope tracers, isotope ratio mass spectrometry and nanoscale secondary ion mass spectrometry (NanoSIMS) to investigate the response of cultured nitrate-acclimated dinoflagellates Prorocentrum minimum to a sudden input of urea and the effect of urea on the concurrent nitrate uptake at the population and single-cell levels. We demonstrate that inputs of urea lead to suppression of nitrate uptake by P. minimum, and urea uptake exceeds the concurrent uptake of nitrate. Individual dinoflagellate cells within a population display significant heterogeneity in the rates of nutrient uptake and extent of the urea-mediated inhibition of the nitrate uptake, thus forming several groups characterized by different modes of nutrition. We conclude that urea originating from sporadic sources is rapidly utilized by dinoflagellates and can be used in biosynthesis or stored intracellularly depending on the nutrient status; therefore, sudden urea inputs can represent one of the factors triggering or supporting harmful algal blooms. Significant physiological heterogeneity revealed at the single-cell level is likely to play a role in alleviation of intra-population competition for resources and can affect the dynamics of phytoplankton populations and their maintenance in natural environments. PMID:27610101

  11. Pedelecs as a physically active transportation mode.

    Science.gov (United States)

    Peterman, James E; Morris, Kalee L; Kram, Rodger; Byrnes, William C

    2016-08-01

    Pedelecs are bicycles that provide electric assistance only when a rider is pedaling and have become increasingly popular. Our purpose was to quantify usage patterns over 4 weeks of real-world commuting with a pedelec and to determine if pedelec use would improve cardiometabolic risk factors. Twenty sedentary commuters visited the laboratory for baseline physiological measurements [body composition, maximum oxygen consumption ([Formula: see text]), mean arterial blood pressure (MAP), blood lipid profile, and 2-h oral glucose tolerance test (OGTT)]. The following 4 weeks, participants were instructed to commute using a pedelec at least 3 days week(-1) for 40 min day(-1) while wearing a heart rate monitor and a GPS device. Metabolic equivalents (METS) were estimated from heart rate data. Following the intervention, we repeated the physiological measurements. Average total distance and time were 317.9 ± 113.8 km and 15.9 ± 3.4 h, respectively. Participants averaged 4.9 ± 1.2 METS when riding. Four weeks of pedelec commuting significantly improved 2-h post-OGTT glucose (5.53 ± 1.18-5.03 ± 0.91 mmol L(-1), p < 0.05), [Formula: see text] (2.21 ± 0.48-2.39 ± 0.52 L min(-1), p < 0.05), and end of [Formula: see text] test power output (165.1 ± 37.1-189.3 ± 38.2 W, p < 0.05). There were trends for improvements in MAP (84.6 ± 10.5-83.2 ± 9.4 mmHg, p = 0.15) and fat mass (28.6 ± 11.3-28.2 ± 11.4 kg, p = 0.07). Participants rode a pedelec in the real world at a self-selected moderate intensity, which helped them meet physical activity recommendations. Pedelec commuting also resulted in significant improvements in 2-h post-OGTT glucose, [Formula: see text], and power output. Pedelecs are an effective form of active transportation that can improve some cardiometabolic risk factors within only 4 weeks.

  12. Transporting Radioactive Waste: An Engineering Activity. Grades 5-12.

    Science.gov (United States)

    HAZWRAP, The Hazardous Waste Remedial Actions Program.

    This brochure contains an engineering activity for upper elementary, middle school, and high school students that examines the transportation of radioactive waste. The activity is designed to inform students about the existence of radioactive waste and its transportation to disposal sites. Students experiment with methods to contain the waste and…

  13. Short-Term Responses of Soil Respiration and C-Cycle Enzyme Activities to Additions of Biochar and Urea in a Calcareous Soil

    Science.gov (United States)

    Song, Dali; Xi, Xiangyin; Huang, Shaomin; Liang, Guoqing; Sun, Jingwen; Zhou, Wei; Wang, Xiubin

    2016-01-01

    Biochar (BC) addition to soil is a proposed strategy to enhance soil fertility and crop productivity. However, there is limited knowledge regarding responses of soil respiration and C-cycle enzyme activities to BC and nitrogen (N) additions in a calcareous soil. A 56-day incubation experiment was conducted to investigate the combined effects of BC addition rates (0, 0.5, 1.0, 2.5 and 5.0% by mass) and urea (U) application on soil nutrients, soil respiration and C-cycle enzyme activities in a calcareous soil in the North China Plain. Our results showed soil pH values in both U-only and U plus BC treatments significantly decreased within the first 14 days and then stabilized, and CO2emission rate in all U plus BC soils decreased exponentially, while there was no significant difference in the contents of soil total organic carbon (TOC), dissolved organic carbon (DOC), total nitrogen (TN), and C/N ratio in each treatment over time. At each incubation time, soil pH, electrical conductivity (EC), TOC, TN, C/N ratio, DOC and cumulative CO2 emission significantly increased with increasing BC addition rate, while soil potential activities of the four hydrolytic enzymes increased first and then decreased with increasing BC addition rate, with the largest values in the U + 1.0%BC treatment. However, phenol oxidase activity in all U plus BC soils showed a decreasing trend with the increase of BC addition rate. Our results suggest that U plus BC application at a rate of 1% promotes increases in hydrolytic enzymes, does not highly increase C/N and C mineralization, and can improve in soil fertility. PMID:27589265

  14. Short-Term Responses of Soil Respiration and C-Cycle Enzyme Activities to Additions of Biochar and Urea in a Calcareous Soil.

    Science.gov (United States)

    Song, Dali; Xi, Xiangyin; Huang, Shaomin; Liang, Guoqing; Sun, Jingwen; Zhou, Wei; Wang, Xiubin

    2016-01-01

    Biochar (BC) addition to soil is a proposed strategy to enhance soil fertility and crop productivity. However, there is limited knowledge regarding responses of soil respiration and C-cycle enzyme activities to BC and nitrogen (N) additions in a calcareous soil. A 56-day incubation experiment was conducted to investigate the combined effects of BC addition rates (0, 0.5, 1.0, 2.5 and 5.0% by mass) and urea (U) application on soil nutrients, soil respiration and C-cycle enzyme activities in a calcareous soil in the North China Plain. Our results showed soil pH values in both U-only and U plus BC treatments significantly decreased within the first 14 days and then stabilized, and CO2emission rate in all U plus BC soils decreased exponentially, while there was no significant difference in the contents of soil total organic carbon (TOC), dissolved organic carbon (DOC), total nitrogen (TN), and C/N ratio in each treatment over time. At each incubation time, soil pH, electrical conductivity (EC), TOC, TN, C/N ratio, DOC and cumulative CO2 emission significantly increased with increasing BC addition rate, while soil potential activities of the four hydrolytic enzymes increased first and then decreased with increasing BC addition rate, with the largest values in the U + 1.0%BC treatment. However, phenol oxidase activity in all U plus BC soils showed a decreasing trend with the increase of BC addition rate. Our results suggest that U plus BC application at a rate of 1% promotes increases in hydrolytic enzymes, does not highly increase C/N and C mineralization, and can improve in soil fertility.

  15. Pedometer-determined physical activity and active transport in girls

    Directory of Open Access Journals (Sweden)

    Schofield Grant

    2008-01-01

    Full Text Available Abstract Background It is well established that the risk of insufficient physical activity is greater in girls than in boys, especially during the adolescent years. The promotion of active transport (AT to and from school has been posited as a practical and convenient solution for increasing girls' total daily activity. However, there is limited information describing the associations between AT choices and girls' physical activity across a range of age, ethnic, and socioeconomic groups. The objectives of this study were to (1 investigate physical activity patterns in a large multiethnic sample of female children and adolescents, and to (2 estimate the physical activity associated with AT to and from school. Methods A total of 1,513 girls aged 5–16 years wore sealed multiday memory (MDM pedometers for three weekdays and two weekend days. The ethnic composition of this sample was 637 European (42.1%, 272 Pacific Island (18.0%, 207 East Asian (13.7%, 179 Maori (11.8%, 142 South Asian (9.4%, and 76 from other ethnic groups (5%. Pedometer compliance and school-related AT were assessed by questionnaire. Results Mean weekday step counts (12,597 ± 3,630 were higher and less variable than mean weekend steps (9,528 ± 4,407. A consistent decline in daily step counts was observed with age: after adjustment for ethnicity and SES, girls in school years 9–10 achieved 2,469 (weekday and 4,011 (weekend fewer steps than girls in years 1–2. Daily step counts also varied by ethnicity, with Maori girls the most active and South Asian girls the least active. Overall, 44.9% of participants used AT for school-related travel. Girls who used AT to and from school averaged 1,052 more weekday steps than those who did not use AT. However, the increases in steps associated with AT were significant only in older girls (school years 5–10 and in those of Maori or European descent. Conclusion Our data suggest that adolescent-aged girls and girls of Asian descent are

  16. Discovery of bis-aryl urea derivatives as potent and selective Limk inhibitors: Exploring Limk1 activity and Limk1/ROCK2 selectivity through a combined computational study.

    Science.gov (United States)

    Cui, Jiaxin; Ding, Mei; Deng, Wei; Yin, Yan; Wang, Zhonghua; Zhou, Hong; Sun, Guofeng; Jiang, Yu; Feng, Yangbo

    2015-12-01

    Lim kinase (Limk), a proline/serine-rich sequence, can regulate the polymerization of the actin filaments by phosphorylating, and it is found to be highly involved in various human diseases. In this paper, 47 reported Limk1 inhibitors with bis-aryl urea scaffold were used to design potent and selective Limk inhibitors by computational approaches. Firstly, the structure-Limk1 activity relationship models (3D-QSAR) and structure-Limk1/ROCK2 selectivity relationship models (3D-QSSR) were developed and both 3D-QSAR and 3D-QSSR models showed good correlative and predictive abilities. Then, the molecular docking and molecular dynamics (MD) simulations were employed to validate the optimal docking conformation and explore the binding affinities. Finally, five new compounds were designed and all of them exhibited good Limk1 inhibition and Limk1/ROCK2 selectivity after synthesis and biological evaluation, which demonstrated that the obtained information from computational studies were valuable to guide Limk inhibitors' design.

  17. Final report of the safety assessment of Urea.

    Science.gov (United States)

    2005-01-01

    alone or with other agents in treatment of diseased skin. Overall, there are few reports of sensitization among the many clinical studies that report use of Urea in treatment of diseased skin. The Cosmetic Ingredient Review (CIR) Expert Panel determined the data provided in this report to be sufficient to assess the safety of Urea. The Panel did note that Urea can cause uncoiling of DNA, a property used in many DNA studies, but concluded that this in vitro activity is not linked to any in vivo genotoxic activity. Although noting that formulators should be aware that Urea can increase the percutaneous absorption of other chemicals, the CIR Expert Panel concluded that Urea is safe as used in cosmetic products.

  18. Interplay of vacuolar transporters for coupling primary and secondary active transport

    Directory of Open Access Journals (Sweden)

    Michèle Siek

    2016-10-01

    Full Text Available Secondary active transporters are driven by the proton motif force which is generated by primary active transporters such as the vacuolar proton pumps V-ATPase and V-PPase. The vacuole occupies up to 90 % of the mature cell and acidification of the vacuolar lumen is a challenging and energy-consuming task for the plant cell. Therefore, a direct coupling of primary and secondary active transporters is expected to enhance transport efficiency and to reduce energy consumption by transport processes across the tonoplast. This has been addressed by analyzing physical and functional interactions between the V-ATPase and a selection of vacuolar transporters including the primary active proton pump AVP1, the calcium ion/proton exchanger CAX1, the potassium ion/proton symporter KUP5, the sodium ion/proton exchanger NHX1, and the anion/proton exchanger CLC-c. Physical interaction was demonstrated in vivo for the V-ATPase and the secondary active transporters CAX1 and CLC-c, which are responsible for calcium- and anion-accumulation in the vacuole, respectively. Measurements of V-ATPase activity and vacuolar pH revealed a functional interaction of V-ATPase and CAX1, CLC-c that is likely caused by the observed physical interaction. The complex of the V-ATPase further interacts with the nitrate reductase 2, and as a result, nitrate assimilation is directly linked to the energization of vacuolar nitrate accumulation by secondary active anion/proton exchangers.

  19. Transport and biological activities of bile acids.

    Science.gov (United States)

    Zwicker, Brittnee L; Agellon, Luis B

    2013-07-01

    Bile acids have emerged as important biological molecules that support the solubilization of various lipids and lipid-soluble compounds in the gut, and the regulation of gene expression and cellular function. Bile acids are synthesized from cholesterol in the liver and eventually released into the small intestine. The majority of bile acids are recovered in the distal end of the small intestine and then returned to the liver for reuse. The components of the mechanism responsible for the recycling of bile acids within the enterohepatic circulation have been identified whereas the mechanism for intracellular transport is less understood. Recently, the ileal lipid binding protein (ILBP; human gene symbol FABP6) was shown to be needed for the efficient transport of bile acids from the apical side to the basolateral side of enterocytes in the distal intestine. This review presents an overview of the transport of bile acids between the liver and the gut as well as within hepatocytes and enterocytes. A variety of pathologies is associated with the malfunction of the bile acid transport system.

  20. Functional inhibition of urea transporter UT-B enhances endothelial-dependent vasodilatation and lowers blood pressure via L-arginine-endothelial nitric oxide synthase-nitric oxide pathway

    Science.gov (United States)

    Sun, Yi; Lau, Chi-Wai; Jia, Yingli; Li, Yingjie; Wang, Weiling; Ran, Jianhua; Li, Fei; Huang, Yu; Zhou, Hong; Yang, Baoxue

    2016-01-01

    Mammalian urea transporters (UTs), UT-A and UT-B, are best known for their role in urine concentration. UT-B is especially distributed in multiple extrarenal tissues with abundant expression in vascular endothelium, but little is known about its role in vascular function. The present study investigated the physiological significance of UT-B in regulating vasorelaxations and blood pressure. UT-B deletion in mice or treatment with UT-B inhibitor PU-14 in Wistar-Kyoto rats (WKYs) and spontaneous hypertensive rats (SHRs) reduced blood pressure. Acetylcholine-induced vasorelaxation was significantly augmented in aortas from UT-B null mice. PU-14 concentration-dependently produced endothelium-dependent relaxations in thoracic aortas and mesenteric arteries from both mice and rats and the relaxations were abolished by Nω-nitro-L-arginine methyl ester. Both expression and phosphorylation of endothelial nitric oxide synthase (eNOS) were up-regulated and expression of arginase I was down-regulated when UT-B was inhibited both in vivo and in vitro. PU-14 induced endothelium-dependent relaxations to a similar degree in aortas from 12 weeks old SHRs or WKYs. In summary, here we report for the first time that inhibition of UT-B plays an important role in regulating vasorelaxations and blood pressure via up-regulation of L-arginine-eNOS-NO pathway, and it may become another potential therapeutic target for the treatment of hypertension. PMID:26739766

  1. Functional inhibition of urea transporter UT-B enhances endothelial-dependent vasodilatation and lowers blood pressure via L-arginine-endothelial nitric oxide synthase-nitric oxide pathway.

    Science.gov (United States)

    Sun, Yi; Lau, Chi-Wai; Jia, Yingli; Li, Yingjie; Wang, Weiling; Ran, Jianhua; Li, Fei; Huang, Yu; Zhou, Hong; Yang, Baoxue

    2016-01-07

    Mammalian urea transporters (UTs), UT-A and UT-B, are best known for their role in urine concentration. UT-B is especially distributed in multiple extrarenal tissues with abundant expression in vascular endothelium, but little is known about its role in vascular function. The present study investigated the physiological significance of UT-B in regulating vasorelaxations and blood pressure. UT-B deletion in mice or treatment with UT-B inhibitor PU-14 in Wistar-Kyoto rats (WKYs) and spontaneous hypertensive rats (SHRs) reduced blood pressure. Acetylcholine-induced vasorelaxation was significantly augmented in aortas from UT-B null mice. PU-14 concentration-dependently produced endothelium-dependent relaxations in thoracic aortas and mesenteric arteries from both mice and rats and the relaxations were abolished by N(ω)-nitro-L-arginine methyl ester. Both expression and phosphorylation of endothelial nitric oxide synthase (eNOS) were up-regulated and expression of arginase I was down-regulated when UT-B was inhibited both in vivo and in vitro. PU-14 induced endothelium-dependent relaxations to a similar degree in aortas from 12 weeks old SHRs or WKYs. In summary, here we report for the first time that inhibition of UT-B plays an important role in regulating vasorelaxations and blood pressure via up-regulation of L-arginine-eNOS-NO pathway, and it may become another potential therapeutic target for the treatment of hypertension.

  2. Study of active cooling for supersonic transports

    Science.gov (United States)

    Brewer, G. D.; Morris, R. E.

    1975-01-01

    The potential benefits of using the fuel heat sink of hydrogen fueled supersonic transports for cooling large portions of the aircraft wing and fuselage are examined. The heat transfer would be accomplished by using an intermediate fluid such as an ethylene glycol-water solution. Some of the advantages of the system are: (1) reduced costs by using aluminum in place of titanium, (2) reduced cabin heat loads, and (3) more favorable environmental conditions for the aircraft systems. A liquid hydrogen fueled, Mach 2.7 supersonic transport aircraft design was used for the reference uncooled vehicle. The cooled aircraft designs were analyzed to determine their heat sink capability, the extent and location of feasible cooled surfaces, and the coolant passage size and spacing.

  3. TRISNET; a Network of Transportation Information Services and Activities.

    Science.gov (United States)

    Department of Transportation, Washington, DC. Office of the Assistant Secretary for Systems Development and Technology.

    A national Transportation Research Information Services Network (TRISNET) is being developed by the Department of Transportation (DOT) linking libraries, data bases, and retrieval services with DOT information activities. Core services provide switch and referral, indexing and abstracting, online retrieval, and document delivery. (JY)

  4. Sites of pH regulation of the urea channel of Helicobacter pylori.

    Science.gov (United States)

    Weeks, D L; Sachs, G

    2001-06-01

    Helicobacter pylori (Hp) and Streptococcus salivarius (Ss) require intrabacterial urease for acid resistance and express a urea channel, UreI. The presence of UreI was shown to increase urea permeability approximately 300-fold over that of a non-polar ureI deletion mutant. Expression of SsUreI in Xenopus oocytes increased urea uptake pH independently, whereas HpUreI shows an acidic pH dependence, half-maximal at pH 6.0. Mutagenesis of all histidines, aspartates, glutamates and the lysine in the periplasmic domain of HpUreI showed that His-123, His-131, Asp-129, Asp-140, Glu-138 and Lys-132 in the second periplasmic loop (PL2) and His-193 in the C-terminus (Ct) were important for activation of transport. With the exception of a lysine that was shown to substitute for His-193 in HpUreI, these charged amino acids are absent in SsUreI. A chimera in which PL1 of HpUreI was replaced by PL1 of SsUreI retained activity at acidic pH and gained partial activity at neutral pH. Exchange of PL2 inactivated transport, whereas exchange of Ct had no effect. Chimeras, in which either PL1 or PL2 of HpUreI replaced those of SsUreI, retained wild-type transport, but replacement of the Ct or both loops inactivated transport. PL1 appears to be important for restricting transport through HpUreI at neutral pH, whereas protonation of three histidines in PL2 and Ct and the presence of three dicarboxylic amino acids in PL2 appears to be necessary to activate HpUreI at acidic pH.

  5. Schisandrin A and B induce organic anion transporting polypeptide 1B1 transporter activity.

    Science.gov (United States)

    Guo, Cheng-Xian; Deng, Sheng; Yin, Ji-Ye; Liu, Zhao-Qian; Zhang, Wei; Zhou, Hong-Hao

    2015-01-01

    Organic anion transporting polypeptide 1B1 (OATP1B1) is the most important transporter in the organic anion transporting polypeptide family. OATP1B1 plays an important role in the hepatic uptake of many endogenous compounds and xenobiotics, including many clinical drugs. At present, the combinational usage of Chinese traditional herbal medicines and conventional chemical pharmaceuticals may affect the activity of enzymes and transporters activity and cause absorption of their substrates and metabolic changes. In this study, we aimed to investigate the effect of schisandrin A, schisandrin B and tanshinone IIA, which were extracted from medicinal plants, on OATP1B1 activity. HepG2 cells are used as in vitro models for OATP1B1 activity studies. A combination of 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-tertazolium bromide (MTT) assays, real-time RT-PCR, and transporter activity analysis were employed. We found that schisandrin A and B increased OATP1B1 mRNA levels by 1.81-fold (p Schisandrin A of 1 μM and 10 μM and schisandrin B of 10 μM significantly increased the uptake of [3H] estrone-3-sulfate (p schisandrin A and B induced OATP1B1 expression and increased its transporter activity in HepG2 cells.

  6. EPR and photoluminescence properties of Mn{sup 2+}-activated zinc gallate phosphor prepared by urea combustion route and post heat treatment

    Energy Technology Data Exchange (ETDEWEB)

    Singh, Vijay, E-mail: vijayjiin2006@yahoo.com [Mechanical Engineering Department, Chung-Ang University, Seoul 156 756 (Korea, Republic of); Chakradhar, R.P.S. [Glass Technology Lab, Central Glass and Ceramic Research Institute, Kolkata 700032 (India); Rao, J.L. [Department of Physics, Sri Venkateswara University, Tirupati 517502 (India); Kwak, Ho-Young, E-mail: kwakh@cau.ac.kr [Mechanical Engineering Department, Chung-Ang University, Seoul 156 756 (Korea, Republic of)

    2011-08-15

    Mn{sup 2+} activated ZnGa{sub 2}O{sub 4} powder phosphors have been prepared by urea combustion route. Powder X-ray diffraction and scanning electron microscopy (SEM) techniques have been used to characterize the as-prepared and post-treated (900 deg. C, 3 h) phosphors. The morphology shows small particles, voids and pores, with non-uniform shapes and sizes. The EPR spectrum exhibits an intense resonance signal at g{approx}1.985 with a sextet hyperfine structure (hfs) besides a weak broad signal at g{approx}4.05 and a hump near g{approx}2.27. The g{approx}1.985 resonance is due to Mn{sup 2+} ions in an environment close to tetrahedral symmetry. The resonances at g{approx}4.05 and 2.27 are attributed to the rhombic surroundings of the Mn{sup 2+} ions. The spin concentration (N) and the paramagnetic susceptibility ({chi}) are evaluated and discussed. It is observed that the intensity of the resonance signal at g{approx}1.985 increases with decrease in temperature obeying the Boltzmann law. Upon post treatment the intensity of the green emission ({lambda}{sub em}=528 nm,{sup 4}T{sub 1}{yields}{sup 6}A{sub 1} transition of Mn{sup 2+} ions) has been increased to 3.35 times and a red shift has been observed. - Highlights: > The paper deals with the synthesis of ZnGa{sub 2}O{sub 4}:Mn phosphor by an easy combustion method. > Upon post treatment the luminescence intensity of the green emission enhanced by 3.35 times. > EPR results also support such an enhancement in the intensity of the resonance signals.

  7. A general method for determining secondary active transporter substrate stoichiometry

    Science.gov (United States)

    Fitzgerald, Gabriel A; Mulligan, Christopher; Mindell, Joseph A

    2017-01-01

    The number of ions required to drive substrate transport through a secondary active transporter determines the protein’s ability to create a substrate gradient, a feature essential to its physiological function, and places fundamental constraints on the transporter’s mechanism. Stoichiometry is known for a wide array of mammalian transporters, but, due to a lack of readily available tools, not for most of the prokaryotic transporters for which high-resolution structures are available. Here, we describe a general method for using radiolabeled substrate flux assays to determine coupling stoichiometries of electrogenic secondary active transporters reconstituted in proteoliposomes by measuring transporter equilibrium potentials. We demonstrate the utility of this method by determining the coupling stoichiometry of VcINDY, a bacterial Na+-coupled succinate transporter, and further validate it by confirming the coupling stoichiometry of vSGLT, a bacterial sugar transporter. This robust thermodynamic method should be especially useful in probing the mechanisms of transporters with available structures. DOI: http://dx.doi.org/10.7554/eLife.21016.001 PMID:28121290

  8. THE TIME FACTOR IN MARITIME TRANSPORT AND PORT LOGISTICS ACTIVITIES

    Directory of Open Access Journals (Sweden)

    Florin NICOLAE

    2016-06-01

    Full Text Available Execution of the carriage contract requires compliance to all the conditions in it, by all those involved in the transport. Main obligations incumbent upon the vessel, and obviously, to other transporters, who must provide transportation according to deadlines and safety. Contract compliance is certifying transport participants about their seriousness and an appropriate market quotation. Therefore, present work pragmatically sets schematics reference time associated implementation of the carriage contract. Also, are demonstrated relationships established between maritime transport “players” and sequence of activities related to the operation of the vessel in port. The authors propose a set of concepts and terms whose utility is established to solve practical problems in this area of activity.

  9. Curtius rearrangement reactions of 3-(4-azidocarbonyl) phenylsydnone. Synthesis of 4-(sydnon-3-yl) phenyl carbamates, N-aryl-N'-[4-(sydnon-3-yl)] phenyl ureas and their antimicrobial and insecticidal activities

    Indian Academy of Sciences (India)

    P R Latthe; P S Shinge; Bharati V Badami; P B Patil; S N Holihosur

    2006-05-01

    3-[4-(Azidocarbonyl)]phenylsydnone (2) obtained from 3-(4-hydrazinocarbonyl) phenylsydnone (1) on Curtius rearrangement with alcohols, water and amines afforded the corresponding carbamates (3a-h), 4,4'-(sydnone-3-yl) diphenyl urea (4) and 4-(heterocyclyl)phenyl ureas (5a-l). Compounds (5a-l) on one-pot ring conversion yielded the 1,3,4-oxadiazolin-2-one derivatives (6a-l), which on reaction with N2H4 gave the 4-amino-1,2,4-triazolin-3-ones (7a-l). All these compounds exhibited moderate antimicrobial activity against the few microbes tested. The carbamates have been found to be more toxic against fourth instar larvae of Aedes aegypti, in particular, the -butyl derivative (3e).

  10. Effects of a Danish multicomponent physical activity intervention on active school transport

    DEFF Research Database (Denmark)

    Breum, Lars; Toftager, Mette; Ersbøll, Annette K.;

    2014-01-01

    AbstractIntroduction Walking and bicycling to school yields great potential in increasing the physical activity levels of adolescents, but to date very few intervention studies have been evaluated. The aim of this study was to evaluate the effect of a multicomponent school-based physical activity...... activity, active transport and after-school fitness program. Transport mode to school was assessed through a 5-day transportation diary. Results The proportion of active transport was high at baseline (86.0%) and was maintained at the two-year follow-up (87.0%). There was no difference in active travel...

  11. Active Transportation Safety Features around Schools in Canada

    Directory of Open Access Journals (Sweden)

    Bryn Pinkerton

    2013-10-01

    Full Text Available The purpose of this study was to describe the presence and quality of active transportation safety features in Canadian school environments that relate to pedestrian and bicycle safety. Variations in these features and associated traffic concerns as perceived by school administrators were examined by geographic status and school type. The study was based on schools that participated in 2009/2010 Health Behaviour in School-aged Children (HBSC survey. ArcGIS software version 10 and Google Earth were used to assess the presence and quality of ten different active transportation safety features. Findings suggest that there are crosswalks and good sidewalk coverage in the environments surrounding most Canadian schools, but a dearth of bicycle lanes and other traffic calming measures (e.g., speed bumps, traffic chokers. Significant urban/rural inequities exist with a greater prevalence of sidewalk coverage, crosswalks, traffic medians, and speed bumps in urban areas. With the exception of bicycle lanes, the active transportation safety features that were present were generally rated as high quality. Traffic was more of a concern to administrators in urban areas. This study provides novel information about active transportation safety features in Canadian school environments. This information could help guide public health efforts aimed at increasing active transportation levels while simultaneously decreasing active transportation injuries.

  12. Active transportation safety features around schools in Canada.

    Science.gov (United States)

    Pinkerton, Bryn; Rosu, Andrei; Janssen, Ian; Pickett, William

    2013-10-31

    The purpose of this study was to describe the presence and quality of active transportation safety features in Canadian school environments that relate to pedestrian and bicycle safety. Variations in these features and associated traffic concerns as perceived by school administrators were examined by geographic status and school type. The study was based on schools that participated in 2009/2010 Health Behaviour in School-aged Children (HBSC) survey. ArcGIS software version 10 and Google Earth were used to assess the presence and quality of ten different active transportation safety features. Findings suggest that there are crosswalks and good sidewalk coverage in the environments surrounding most Canadian schools, but a dearth of bicycle lanes and other traffic calming measures (e.g., speed bumps, traffic chokers). Significant urban/rural inequities exist with a greater prevalence of sidewalk coverage, crosswalks, traffic medians, and speed bumps in urban areas. With the exception of bicycle lanes, the active transportation safety features that were present were generally rated as high quality. Traffic was more of a concern to administrators in urban areas. This study provides novel information about active transportation safety features in Canadian school environments. This information could help guide public health efforts aimed at increasing active transportation levels while simultaneously decreasing active transportation injuries.

  13. Entropic Ratchet transport of interacting active Brownian particles

    Energy Technology Data Exchange (ETDEWEB)

    Ai, Bao-Quan, E-mail: aibq@hotmail.com [Laboratory of Quantum Engineering and Quantum Materials, School of Physics and Telecommunication Engineering, South China Normal University, 510006 Guangzhou (China); He, Ya-Feng [College of Physics Science and Technology, Hebei University, 071002 Baoding (China); Zhong, Wei-Rong, E-mail: wrzhong@jnu.edu.cn [Department of Physics and Siyuan Laboratory, College of Science and Engineering, Jinan University, 510632 Guangzhou (China)

    2014-11-21

    Directed transport of interacting active (self-propelled) Brownian particles is numerically investigated in confined geometries (entropic barriers). The self-propelled velocity can break thermodynamical equilibrium and induce the directed transport. It is found that the interaction between active particles can greatly affect the ratchet transport. For attractive particles, on increasing the interaction strength, the average velocity first decreases to its minima, then increases, and finally decreases to zero. For repulsive particles, when the interaction is very weak, there exists a critical interaction at which the average velocity is minimal, nearly tends to zero, however, for the strong interaction, the average velocity is independent of the interaction.

  14. Health Impacts of Active Transportation in Europe

    DEFF Research Database (Denmark)

    Rojas-Rueda, David; de Nazelle, Audrey; Andersen, Zorana J

    2016-01-01

    impact assessment using two scenarios: increased cycling and increased walking. The primary outcome measure was all-cause mortality related to changes in physical activity level, exposure to fine particulate matter air pollution with a diameter

  15. Experimental studies on urea degradation in seawater

    Digital Repository Service at National Institute of Oceanography (India)

    Rajendran, A.; Joseph, T.; Reddy, C.V.G.

    The rate of urea degradation in seawater was studied under various conditions and the kinetics of urea degradation was evaluated. Urea decomposition experiments showed that the rates and quantity of ammonium oxidation were slower in the relatively...

  16. Urea enhances the photodynamic efficiency of methylene blue.

    Science.gov (United States)

    Nuñez, Silvia C; Yoshimura, Tania M; Ribeiro, Martha S; Junqueira, Helena C; Maciel, Cleiton; Coutinho-Neto, Maurício D; Baptista, Maurício S

    2015-09-01

    simulations. In 2M-urea solution the atomistic picture revealed a preferential solvation of MB by urea compared with MB dimers while changes in ΔH(dimer) values demonstrated a clear shift favoring MB monomers. Therefore, MB monomers are more stable in urea solutions, which have significantly better photophysics and higher antimicrobial activity. This information can be of use for dental and medical professionals that are using MB based APDT protocols.

  17. Novel urea and bis-urea primaquine derivatives with hydroxyphenyl or halogenphenyl substituents: Synthesis and biological evaluation.

    Science.gov (United States)

    Perković, I; Antunović, M; Marijanović, I; Pavić, K; Ester, K; Kralj, M; Vlainić, J; Kosalec, I; Schols, D; Hadjipavlou-Litina, D; Pontiki, E; Zorc, B

    2016-11-29

    A series of novel compounds 3a-j and 6a-j with primaquine and hydroxyl or halogen substituted benzene moieties bridged by urea or bis-urea functionalities were designed, synthesized and evaluated for biological activity. The title compounds were prepared using benzotriazole as the synthon, through several synthetic steps. 3-[3,5-Bis(trifluoromethyl)phenyl]-1-{4-[(6-methoxyquinolin-8-yl)amino]pentyl}urea (3j) was the most active urea and 1-[({4-[(6-methoxyquinolin-8-yl)amino]pentyl}carbamoyl)amino]-3-[3-(trifluoromethyl)phenyl]urea (6h) the most active bis-urea derivative in antiproliferative screening in vitro against eight tested cancer cell lines. Urea derivatives 3a-g with hydroxy group or one halogen atom showed moderate antiproliferative effects against all the tested cell lines, but stronger activity against breast carcinoma MCF-7 cell line, while trifluoromethyl derivatives 3h-j showed antiproliferative effects against all the tested cell lines in low micromolar range. Finally, bis-ureas with hydroxy and fluoro substituents 6a-d showed extreme selectivity and chloro or bromo derivatives 6e-g high selectivity against MCF-7 cells (IC50 0.1-2.6 μM). p-Fluoro derivative 6d, namely 3-(4-fluorophenyl)-1-[({4-[(6-methoxyquinolin-8-yl)amino]pentyl}carbamoyl)amino]urea, is the most promising compound. Further biological experiments showed that 6d affected cell cycle and induced cell death of MCF-7 cell line. Due to its high activity against MCF-7 cell line (IC50 0.31 μM), extreme selectivity and full agreement with the Lipinski's and Gelovani's rules for prospective small molecular drugs, 6d may be considered as a lead compound in development of breast carcinoma drugs. Urea 3b and almost all bis-ureas showed high antioxidant activity in DPPH assay, but urea derivatives were more active in lipid peroxidation test. Only few compounds exhibited weak inhibition of soybean lipoxygenase. Compound 3j exhibited the strongest antimicrobial activity in susceptibility

  18. Metallic Nickel Hydroxide Nanosheets Give Superior Electrocatalytic Oxidation of Urea for Fuel Cells.

    Science.gov (United States)

    Zhu, Xiaojiao; Dou, Xinyu; Dai, Jun; An, Xingda; Guo, Yuqiao; Zhang, Lidong; Tao, Shi; Zhao, Jiyin; Chu, Wangsheng; Zeng, Xiao Cheng; Wu, Changzheng; Xie, Yi

    2016-09-26

    The direct urea fuel cell (DUFC) is an important but challenging renewable energy production technology, it offers great promise for energy-sustainable developments and mitigating water contamination. However, DUFCs still suffer from the sluggish kinetics of the urea oxidation reaction (UOR) owing to a 6 e(-) transfer process, which poses a severe hindrance to their practical use. Herein, taking β-Ni(OH)2 nanosheets as the proof-of-concept study, we demonstrated a surface-chemistry strategy to achieve metallic Ni(OH)2 nanosheets by engineering their electronic structure, representing a first metallic configuration of transition-metal hydroxides. Surface sulfur incorporation successfully brings synergetic effects of more exposed active sites, good wetting behavior, and effective electron transport, giving rise to greatly enhanced performance for UOR. Metallic nanosheets exhibited a much higher current density, smaller onset potential and stronger durability.

  19. Regional differences in rat conjunctival ion transport activities

    OpenAIRE

    2012-01-01

    Active ion transport and coupled osmotic water flow are essential to maintain ocular surface health. We investigated regional differences in the ion transport activities of the rat conjunctivas and compared these activities with those of cornea and lacrimal gland. The epithelial sodium channel (ENaC), sodium/glucose cotransporter 1 (Slc5a1), transmembrane protein 16 (Tmem16a, b, f, and g), cystic fibrosis transmembrane conductance regulator (Cftr), and mucin (Muc4, 5ac, and 5b) mRNA expressio...

  20. Coupling of Active Motion and Advection Shapes Intracellular Cargo Transport

    CERN Document Server

    Trong, P Khuc; Goldstein, R E; 10.1103/PhysRevLett.109.028104

    2012-01-01

    Intracellular cargo transport can arise from passive diffusion, active motor-driven transport along cytoskeletal filament networks, and passive advection by fluid flows entrained by such motor/cargo motion. Active and advective transport are thus intrinsically coupled as related, yet different representations of the same underlying network structure. A reaction-advection-diffusion system is used here to show that this coupling affects the transport and localization of a passive tracer in a confined geometry. For sufficiently low diffusion, cargo localization to a target zone is optimized either by low reaction kinetics and decoupling of bound and unbound states, or by a mostly disordered cytoskeletal network with only weak directional bias. These generic results may help to rationalize subtle features of cytoskeletal networks, for example as observed for microtubules in fly oocytes.

  1. Sintering as a process of transport of activated volume

    Directory of Open Access Journals (Sweden)

    Nikolić Nataša S.

    2002-01-01

    Full Text Available Starting with the fact that sintering is the consequence of the process of transport of activated volume, it has been shown how the kinetics of the sintering process can be defined. The activated volume was in principle defined as a parameter which describes a system’s deffectivity on an atomic level.

  2. Growth mechanism and photocatalytic activity of self-organized N-doped (BiO)₂CO₃ hierarchical nanosheet microspheres from bismuth citrate and urea.

    Science.gov (United States)

    Dong, Fan; Xiong, Ting; Wang, Rui; Sun, Yanjuan; Jiang, Yanke

    2014-05-14

    Synthesis of nano-/microstructured functional materials with 3D hierarchical microspheres structure has provided new opportunities for optimizing their physical and chemical properties. This work revealed a new growth mechanism of self-organized N-doped (BiO)2CO3 hierarchical microspheres which were fabricated by hydrothermal treatment of bismuth citrate and urea without an additive. Based on time-dependent observation, several evolution processes were believed to account for the formation of the self-organized N-doped (BiO)2CO3 hierarchical microspheres. Initially, crystallized (BiO)4CO3(OH)2 particles were formed during the nucleation and crystallization processes. Subsequently, the intermediate (BiO)4CO3(OH)2 reacted with CO3(2-) to generate (BiO)2CO3 growth nuclei on the surface of the CO2 bubbles which can act as heterogeneous nucleation centers. Next, the (BiO)2CO3 growth nuclei aggregated together after the consumption of CO2 bubbles with the increased concentration of OH(-) and further grew to be nanosheets. The microspheres constructed by small nanosheets further grew with the consumption of small particles. Finally, all (BiO)4CO3(OH)2 transformed to the (BiO)2CO3 phase, accompanied by the doping of N element into the lattice of (BiO)2CO3, and thereby, the well-defined N-doped (BiO)2CO3 hierarchical microspheres were shaped. Depending on the distance between neighboring CO2 bubbles, the resulting microspheres can be linked or dispersed. Besides, the gradual release of CO2 bubbles and CO3(2-) played a crucial role in controlling the nucleation and growth process, resulting in different sizes of microspheres. The fabricated N-doped (BiO)2CO3 hierarchical microspheres displayed admirably efficient and durable photocatalytic activity under both UV and visible light towards removal of NO, which is mainly attributed to the introduction of N element and the special hierarchical structure. This work provides new insights into the controlled synthesis of

  3. Substrate regulation of ascorbate transport activity in astrocytes

    Energy Technology Data Exchange (ETDEWEB)

    Wilson, J.X.; Jaworski, E.M.; Kulaga, A.; Dixon, S.J. (Univ. of Western Ontario, London (Canada))

    1990-10-01

    Astrocytes possess a concentrative L-ascorbate (vitamin C) uptake mechanism involving a Na(+)-dependent L-ascorbate transporter located in the plasma membrane. The present experiments examined the effects of deprivation and supplementation of extracellular L-ascorbate on the activity of this transport system. Initial rates of L-ascorbate uptake were measured by incubating primary cultures of rat astrocytes with L-(14C)ascorbate for 1 min at 37 degrees C. We observed that the apparent maximal rate of uptake (Vmax) increased rapidly (less than 1 h) when cultured cells were deprived of L-ascorbate. In contrast, there was no change in the apparent affinity of the transport system for L-(14C)ascorbate. The increase in Vmax was reversed by addition of L-ascorbate, but not D-isoascorbate, to the medium. The effects of external ascorbate on ascorbate transport activity were specific in that preincubation of cultures with L-ascorbate did not affect uptake of 2-deoxy-D-(3H(G))glucose. We conclude that the astroglial ascorbate transport system is modulated by changes in substrate availability. Regulation of transport activity may play a role in intracellular ascorbate homeostasis by compensating for regional differences and temporal fluctuations in external ascorbate levels.

  4. Presentation and exhibition activities for promoting theexportof transport services

    Directory of Open Access Journals (Sweden)

    Darya Vladimirovna Nesterova

    2012-03-01

    Full Text Available Development of presentation and exhibition activities is considered as an important factor in providing new competitive advantages at the strategic markets for exporting of transportation services. A specific role for exhibition activities as a factor to overcome market failures arose from imperfect information and incomplete markets is displayed. Exhibitions are considered as a true reflection of most market parameters, as a means to get correct information concerning market capacity and its borders, as an instrument to access to new markets. At the firm level presentation and branding activities should be considered as a modern technology (especially it concerns Russian companies which provide to hold up already existed markets and to conquer new ones. Presentation and branding activities are an effective technology to promote company trade-mark, competitive advantages for market demand increasing. Comparative analysis of the main exhibitions on transport and logistics issues is fulfilled on the data basecollected by authors. Data observes geographical distribution of transport exhibition and exhibition facilities development at several regions for the last years. The analyses allow to revealing a geographical structure of the exhibitions and its distribution by type of transport. The most promising and economically favorable exhibition areas for the promotion of Russian transport services are shown.

  5. Advocacy for active transport: advocate and city council perspectives

    Directory of Open Access Journals (Sweden)

    Rosenby Marieah

    2010-01-01

    Full Text Available Abstract Background Effective advocacy is an important part of efforts to increase population participation in physical activity. Research about effective health advocacy is scarce, however, the health sector can learn from the experiences and knowledge of community advocates and those who are on the receiving end of this advocacy. The aim of this study is to explore advocacy for active transport from the perspectives of community advocates and representatives from City councils. Methods Cycling and walking advocates were identified from the local contact list of Cycling Advocates Network and Living Streets Aotearoa. Semi-structured telephone interviews were conducted with cycle and walking advocates from throughout New Zealand. Advocates also nominated a suitable council officer at their local City council to be interviewed. Interviews were recorded and transcribed and categories of responses for each of the questions created. Results Several processes were used by advocates to engage with council staff, including formal council submissions, meetings, stakeholder forums and partnership in running community events promoting active transport. Several other agencies were identified as being influential for active transport, some as potential coalition partners and others as potential adversaries. Barriers to improving conditions for active transport included a lack of funding, a lack of will-power among either council staff or councillors, limited council staff capacity (time or training and a culture of providing infrastructure for motor vehicles instead of people. Several suggestions were made about how the health sector could contribute to advocacy efforts, including encouraging political commitment, engaging the media, communicating the potential health benefits of active transport to the general public and being role models in terms of personal travel mode choice and having workplaces that support participation in active transport

  6. Urea and Ammonia Metabolism and the Control of Renal Nitrogen Excretion.

    Science.gov (United States)

    Weiner, I David; Mitch, William E; Sands, Jeff M

    2015-08-07

    Renal nitrogen metabolism primarily involves urea and ammonia metabolism, and is essential to normal health. Urea is the largest circulating pool of nitrogen, excluding nitrogen in circulating proteins, and its production changes in parallel to the degradation of dietary and endogenous proteins. In addition to serving as a way to excrete nitrogen, urea transport, mediated through specific urea transport proteins, mediates a central role in the urine concentrating mechanism. Renal ammonia excretion, although often considered only in the context of acid-base homeostasis, accounts for approximately 10% of total renal nitrogen excretion under basal conditions, but can increase substantially in a variety of clinical conditions. Because renal ammonia metabolism requires intrarenal ammoniagenesis from glutamine, changes in factors regulating renal ammonia metabolism can have important effects on glutamine in addition to nitrogen balance. This review covers aspects of protein metabolism and the control of the two major molecules involved in renal nitrogen excretion: urea and ammonia. Both urea and ammonia transport can be altered by glucocorticoids and hypokalemia, two conditions that also affect protein metabolism. Clinical conditions associated with altered urine concentrating ability or water homeostasis can result in changes in urea excretion and urea transporters. Clinical conditions associated with altered ammonia excretion can have important effects on nitrogen balance.

  7. Carbonless footprints: promoting health and climate stabilization through active transportation.

    Science.gov (United States)

    Frank, Lawrence D; Greenwald, Michael J; Winkelman, Steve; Chapman, James; Kavage, Sarah

    2010-01-01

    Our objective was to describe how active transportation can help meet health and greenhouse gas emissions goals, and the ability of urban form strategies to impact both issues. In addition, we wanted to assess if there is an inverse relationship between active and motorized forms of travel. A cross-sectional analysis of travel diary data was used to measure relationships among energy (kcal) burned from walking, energy (kcal) burned from motorized transportation, and the ratio of the two (the transport energy index) with regional accessibility and local walkability when adjusting for demographic factors. Multiple linear regression and descriptive statistics were employed to estimate these relationships. Transit accessibility, residential density, and intersection density were positive predictors of walk energy and the energy index and inverse predictors of motorized energy. The land use mix variable was negatively and significantly associated with energy burned from walking and from motorized transportation, with no significant impact on the transport energy index. Because a mixed land use pattern places destinations closer together, it reduces distances and thus energy demands for both walking and driving. The results support the concept, previously untested empirically, that similar urban form strategies can have cobenefits for both physical activity and climate change.

  8. Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.

    Science.gov (United States)

    El-Damasy, Ashraf Kareem; Lee, Ju-Hyeon; Seo, Seon Hee; Cho, Nam-Chul; Pae, Ae Nim; Keum, Gyochang

    2016-06-10

    A new series of benzothiazole amide and urea derivatives tethered with the privileged pyridylamide moiety by ether linkage at the 6-position of benzothiazole (22 final compounds) has been designed and synthesized as potent anticancer sorafenib analogs. A selected group of twelve derivatives was appraised for its antiproliferative activity over a panel of 60 human cancer cell lines at a single dose concentration of 10 μM at National Cancer Institute (NCI, USA). Compounds 4b, 5a, 5b and 5d exhibited promising growth inhibitions and thus were further tested in advanced 5-dose testing assay to determine their GI50 values. The cellular based assay results revealed that 3,5-bis-trifluoromethylphenyl (5b) urea member is the best derivative with superior potency and efficacy compared to sorafenib as well as notable extended spectrum activity covering 57 human cancer cell lines. Kinase screening of compound 5b showed its kinase inhibitory effect against both B-Raf(V600E) and C-Raf. Moreover, the most potent derivatives in cells were investigated for their RAF inhibitory activities, and the results were rationalized with the molecular docking study. Profiling of CYP450 and hERG channel inhibitory effects for the active compounds revealed their low possibilities to exhibit undesirable drug-drug interactions and cardiac side effects.

  9. National Urea Cycle Disorders Foundation

    Science.gov (United States)

    ... triggers undiagnosed fatal urea cycle disorder in Tennessee wife and teacher. Story . More information about bariatric surgery ... with sodium phenylbutyrate may decrease liver dysfunction in patients with ASA. Details "IN TRIBUTE TO HER SON, ...

  10. Transport of active ellipsoidal particles in ratchet potentials

    Energy Technology Data Exchange (ETDEWEB)

    Ai, Bao-Quan, E-mail: aibq@scnu.edu.cn; Wu, Jian-Chun [Laboratory of Quantum Engineering and Quantum Materials, School of Physics and Telecommunication Engineering, South China Normal University, 510006 Guangzhou (China)

    2014-03-07

    Rectified transport of active ellipsoidal particles is numerically investigated in a two-dimensional asymmetric potential. The out-of-equilibrium condition for the active particle is an intrinsic property, which can break thermodynamical equilibrium and induce the directed transport. It is found that the perfect sphere particle can facilitate the rectification, while the needlelike particle destroys the directed transport. There exist optimized values of the parameters (the self-propelled velocity, the torque acting on the body) at which the average velocity takes its maximal value. For the ellipsoidal particle with not large asymmetric parameter, the average velocity decreases with increasing the rotational diffusion rate, while for the needlelike particle (very large asymmetric parameter), the average velocity is a peaked function of the rotational diffusion rate. By introducing a finite load, particles with different shapes (or different self-propelled velocities) will move to the opposite directions, which is able to separate particles of different shapes (or different self-propelled velocities)

  11. Improving long term outcomes in urea cycle disorders-report from the Urea Cycle Disorders Consortium.

    Science.gov (United States)

    Waisbren, Susan E; Gropman, Andrea L; Batshaw, Mark L

    2016-07-01

    The Urea Cycle Disorders Consortium (UCDC) has conducted, beginning in 2006, a longitudinal study (LS) of eight enzyme deficiencies/transporter defects associated with the urea cycle. These include N-acetylglutamate synthase deficiency (NAGSD); Carbamyl phosphate synthetase 1 deficiency (CPS1D); Ornithine transcarbamylase deficiency (OTCD); Argininosuccinate synthetase deficiency (ASSD) (Citrullinemia); Argininosuccinate lyase deficiency (ASLD) (Argininosuccinic aciduria); Arginase deficiency (ARGD, Argininemia); Hyperornithinemia, hyperammonemia, homocitrullinuria (HHH) syndrome (or mitochondrial ornithine transporter 1 deficiency [ORNT1D]); and Citrullinemia type II (mitochondrial aspartate/glutamate carrier deficiency [CITRIN]). There were 678 UCD patients enrolled in 14 sites in the U.S., Canada, and Europe at the writing of this paper. This review summarizes findings of the consortium related to outcome, focusing primarily on neuroimaging findings and neurocognitive function. Neuroimaging studies in late onset OTCD offered evidence that brain injury caused by biochemical dysregulation may impact functional neuroanatomy serving working memory processes, an important component of executive function and regulation. Additionally, there were alteration in white mater microstructure and functional connectivity at rest. Intellectual deficits in OTCD and other urea cycle disorders (UCD) vary. However, when neuropsychological deficits occur, they tend to be more prominent in motor/performance areas on both intelligence tests and other measures. In some disorders, adults performed significantly less well than younger patients. Further longitudinal follow-up will reveal whether this is due to declines throughout life or to improvements in diagnostics (especially newborn screening) and treatments in the younger generation of patients.

  12. Synthesis, Central Nervous System Activity and Structure-Activity Relationships of Novel 1-(1-Alkyl-4-aryl-4,5-dihydro-1H-imidazo-3-substituted Urea Derivatives

    Directory of Open Access Journals (Sweden)

    Elżbieta Szacoń

    2015-02-01

    Full Text Available A series of 10 novel urea derivatives has been synthesized and evaluated for their central nervous system activity. Compounds 3a–3h were prepared in the reaction between the respective 1-alkyl-4-aryl-4,5-dihydro-1H-imidazol-2-amines 1a and 1b and appropriate benzyl-, phenethyl-isocyanate or ethyl 4-isocyanatobenzoate and ethyl isocyanatoacetate 2 in dichloromethane. Derivatives 4c and 4g resulted from the conversion of 3c and 3g into the respective amides due to action of an aqueous ammonia solution. The results obtained in this study, based on literature data suggest a possible involvement of serotonin system and/or the opioid system in the effects of tested compounds, and especially in the effect of compound 3h. The best activity of compound 3h may be primarily attributed to its favourable ADMET properties, i.e., higher lipophilicity (related to lower polar surface area and greater molecular surface, volume and mass than for other compounds and good blood-brain permeation. This compound has also the greatest polarizability and ovality. The HOMO and LUMO energies do not seem to be directly related to activity.

  13. Discovery of enantioselectivity of urea inhibitors of soluble epoxide hydrolase.

    Science.gov (United States)

    Manickam, Manoj; Pillaiyar, Thanigaimalai; Boggu, PullaReddy; Venkateswararao, Eeda; Jalani, Hitesh B; Kim, Nam-Doo; Lee, Seul Ki; Jeon, Jang Su; Kim, Sang Kyum; Jung, Sang-Hun

    2016-07-19

    Soluble epoxide hydrolase (sEH) hydrolyzes epoxyeicosatrienoic acids (EETs) in the metabolic pathway of arachidonic acid and has been considered as an important therapeutic target for chronic diseases such as hypertension, diabetes and inflammation. Although many urea derivatives are known as sEH inhibitors, the enantioselectivity of the inhibitors is not highlighted in spite of the stereoselective hydrolysis of EETs by sEH. In an effort to explore the importance of enantioselectivity in the urea scaffold, a series of enantiomers with the stereocenter adjacent to the urea nitrogen atom were prepared. The selectivity of enantiomers of 1-(α-alkyl-α-phenylmethyl)-3-(3-phenylpropyl)ureas showed wide range differences up to 125 fold with the low IC50 value up to 13 nM. The S-configuration with planar phenyl and small alkyl groups at α-position is crucial for the activity and selectivity. However, restriction of the free rotation of two α-groups with indan-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl moiety abolishes the selectivity between the enantiomers, despite the increase in activity up to 13 nM. The hydrophilic group like sulfonamido group at para position of 3-phenylpropyl motif of 1-(α-alkyl-α-phenylmethyl-3-(3-phenylpropyl)urea improves the activity as well as enantiomeric selectivity. All these ureas are proved to be specific inhibitor of sEH without inhibition against mEH.

  14. Evaporation of urea at atmospheric pressure.

    Science.gov (United States)

    Bernhard, Andreas M; Czekaj, Izabela; Elsener, Martin; Wokaun, Alexander; Kröcher, Oliver

    2011-03-31

    Aqueous urea solution is widely used as reducing agent in the selective catalytic reduction of NO(x) (SCR). Because reports of urea vapor at atmospheric pressure are rare, gaseous urea is usually neglected in computational models used for designing SCR systems. In this study, urea evaporation was investigated under flow reactor conditions, and a Fourier transform infrared (FTIR) spectrum of gaseous urea was recorded at atmospheric pressure for the first time. The spectrum was compared to literature data under vacuum conditions and with theoretical spectra of monomolecular and dimeric urea in the gas phase calculated with the density functional theory (DFT) method. Comparison of the spectra indicates that urea vapor is in the monomolecular form at atmospheric pressure. The measured vapor pressure of urea agrees with the thermodynamic data obtained under vacuum reported in the literature. Our results indicate that considering gaseous urea will improve the computational modeling of urea SCR systems.

  15. Short-Term Treatment with the Urease Inhibitor N-(n-Butyl) Thiophosphoric Triamide (NBPT) Alters Urea Assimilation and Modulates Transcriptional Profiles of Genes Involved in Primary and Secondary Metabolism in Maize Seedlings.

    Science.gov (United States)

    Zanin, Laura; Venuti, Silvia; Tomasi, Nicola; Zamboni, Anita; De Brito Francisco, Rita M; Varanini, Zeno; Pinton, Roberto

    2016-01-01

    To limit nitrogen (N) losses from the soil, it has been suggested to provide urea to crops in conjunction with the urease inhibitor N-(n-butyl) thiophosphoric triamide (NBPT). However, recent studies reported that NBPT affects urea uptake and urease activity in plants. To shed light on these latter aspects, the effects of NBPT were studied analysing transcriptomic and metabolic changes occurring in urea-fed maize seedlings after a short-term exposure to the inhibitor. We provide evidence that NBPT treatment led to a wide reprogramming of plant metabolism. NBPT inhibited the activity of endogenous urease limiting the release and assimilation of ureic-ammonium, with a simultaneous accumulation of urea in plant tissues. Furthermore, NBPT determined changes in the glutamine, glutamate, and asparagine contents. Microarray data indicate that NBPT affects ureic-N assimilation and primary metabolism, such as glycolysis, TCA cycle, and electron transport chain, while activates the phenylalanine/tyrosine-derivative pathway. Moreover, the expression of genes relating to the transport and complexation of divalent metals was strongly modulated by NBPT. Data here presented suggest that when NBPT is provided in conjunction with urea an imbalance between C and N compounds might occur in plant cells. Under this condition, root cells also seem to activate a response to maintain the homeostasis of some micronutrients.

  16. Short-Term Treatment with the Urease Inhibitor N-(n-Butyl) Thiophosphoric Triamide (NBPT) Alters Urea Assimilation and Modulates Transcriptional Profiles of Genes Involved in Primary and Secondary Metabolism in Maize Seedlings

    Science.gov (United States)

    Zanin, Laura; Venuti, Silvia; Tomasi, Nicola; Zamboni, Anita; De Brito Francisco, Rita M.; Varanini, Zeno; Pinton, Roberto

    2016-01-01

    To limit nitrogen (N) losses from the soil, it has been suggested to provide urea to crops in conjunction with the urease inhibitor N-(n-butyl) thiophosphoric triamide (NBPT). However, recent studies reported that NBPT affects urea uptake and urease activity in plants. To shed light on these latter aspects, the effects of NBPT were studied analysing transcriptomic and metabolic changes occurring in urea-fed maize seedlings after a short-term exposure to the inhibitor. We provide evidence that NBPT treatment led to a wide reprogramming of plant metabolism. NBPT inhibited the activity of endogenous urease limiting the release and assimilation of ureic-ammonium, with a simultaneous accumulation of urea in plant tissues. Furthermore, NBPT determined changes in the glutamine, glutamate, and asparagine contents. Microarray data indicate that NBPT affects ureic-N assimilation and primary metabolism, such as glycolysis, TCA cycle, and electron transport chain, while activates the phenylalanine/tyrosine-derivative pathway. Moreover, the expression of genes relating to the transport and complexation of divalent metals was strongly modulated by NBPT. Data here presented suggest that when NBPT is provided in conjunction with urea an imbalance between C and N compounds might occur in plant cells. Under this condition, root cells also seem to activate a response to maintain the homeostasis of some micronutrients. PMID:27446099

  17. Engineering intracellular active transport systems as in vivo biomolecular tools.

    Energy Technology Data Exchange (ETDEWEB)

    Bachand, George David; Carroll-Portillo, Amanda

    2006-11-01

    Active transport systems provide essential functions in terms of cell physiology and metastasis. These systems, however, are also co-opted by invading viruses, enabling directed transport of the virus to and from the cell's nucleus (i.e., the site of virus replication). Based on this concept, fundamentally new approaches for interrogating and manipulating the inner workings of living cells may be achievable by co-opting Nature's active transport systems as an in vivo biomolecular tool. The overall goal of this project was to investigate the ability to engineer kinesin-based transport systems for in vivo applications, specifically the collection of effector proteins (e.g., transcriptional regulators) within single cells. In the first part of this project, a chimeric fusion protein consisting of kinesin and a single chain variable fragment (scFv) of an antibody was successfully produced through a recombinant expression system. The kinesin-scFv retained both catalytic and antigenic functionality, enabling selective capture and transport of target antigens. The incorporation of a rabbit IgG-specific scFv into the kinesin established a generalized system for functionalizing kinesin with a wide range of target-selective antibodies raised in rabbits. The second objective was to develop methods of isolating the intact microtubule network from live cells as a platform for evaluating kinesin-based transport within the cytoskeletal architecture of a cell. Successful isolation of intact microtubule networks from two distinct cell types was demonstrated using glutaraldehyde and methanol fixation methods. This work provides a platform for inferring the ability of kinesin-scFv to function in vivo, and may also serve as a three-dimensional scaffold for evaluating and exploiting kinesin-based transport for nanotechnological applications. Overall, the technology developed in this project represents a first-step in engineering active transport system for in vivo

  18. Berberine acutely activates the glucose transport activity of GLUT1

    OpenAIRE

    Cok, Alexandra; Plaisier, Christina; Salie, Matthew J.; Oram, Daniel S.; Chenge, Jude; Louters, Larry L.

    2011-01-01

    Berberine, which has a long history of use in Chinese medicine, has recently been shown to have efficacy in the treatment of diabetes. While the hypoglycemic effect of berberine has been clearly documented in animal and cell line models, such as 3T3-L1 adipocytes and L6 myotube cells, the mechanism of action appears complex with data implicating activation of the insulin signaling pathway as well as activation of the exercise or AMP kinase-mediated pathway. There have been no reports of the a...

  19. Urea-induced oxidative damage in Elodea densa leaves.

    Science.gov (United States)

    Maleva, Maria; Borisova, Galina; Chukina, Nadezda; Prasad, M N V

    2015-09-01

    Urea being a fertilizer is expected to be less toxic to plants. However, it was found that urea at 100 mg L(-1) caused the oxidative stress in Elodea leaves due to the formation of reactive oxygen species (ROS) and lipid peroxidation that are known to stimulate antioxidant pathway. Urea at a concentration of 500 and 1000 mg L(-1) decreased low-molecular-weight antioxidants. In this case, the antioxidant status of plants was supported by the activity of antioxidant enzymes such as superoxide dismutase and guaiacol peroxidase. A significant increase in the soluble proteins and -SH groups was observed with high concentrations of urea (30-60 % of control). Thus, the increased activity of antioxidant enzymes, low-molecular-weight antioxidants, and induced soluble protein thiols are implicated in plant resistance to oxidative stress imposed by urea. We found that guaiacol peroxidase plays an important role in the removal of the peroxide in Elodea leaves exposed to 1000 mg L(-1)of urea.

  20. Mechanochemical synthesis of thioureas, ureas and guanidines.

    Science.gov (United States)

    Štrukil, Vjekoslav

    2017-01-01

    In this review, the recent progress in the synthesis of ureas, thioureas and guanidines by solid-state mechanochemical ball milling is highlighted. While the literature is abundant on their preparation in conventional solution environment, it was not until the advent of solvent-free manual grinding using a mortar and pestle and automated ball milling that new synthetic opportunities have opened. The mechanochemical approach not only has enabled the quantitative synthesis of (thio)ureas and guanidines without using bulk solvents and the generation of byproducts, but it has also been established as a means to develop "click-type" chemistry for these classes of compounds and the concept of small molecule desymmetrization. Moreover, mechanochemistry has been demonstrated as an effective tool in reaction discovery, with emphasis on the reactivity differences in solution and in the solid state. These three classes of organic compounds share some structural features which are reflected in their physical and chemical properties, important for application as organocatalysts and sensors. On the other hand, the specific and unique nature of each of these functionalities render (thio)ureas and guanidines as the key constituents of pharmaceuticals and other biologically active compounds.

  1. Pore mutations in ammonium transporter AMT1 with increased electrogenic ammonium transport activity.

    Science.gov (United States)

    Loqué, Dominique; Mora, Silvia I; Andrade, Susana L A; Pantoja, Omar; Frommer, Wolf B

    2009-09-11

    AMT/Mep ammonium transporters mediate high affinity ammonium/ammonia uptake in bacteria, fungi, and plants. The Arabidopsis AMT1 proteins mediate uptake of the ionic form of ammonium. AMT transport activity is controlled allosterically via a highly conserved cytosolic C terminus that interacts with neighboring subunits in a trimer. The C terminus is thus capable of modulating the conductivity of the pore. To gain insight into the underlying mechanism, pore mutants suppressing the inhibitory effect of mutations in the C-terminal trans-activation domain were characterized. AMT1;1 carrying the mutation Q57H in transmembrane helix I (TMH I) showed increased ammonium uptake but reduced capacity to take up methylammonium. To explore whether the transport mechanism was altered, the AMT1;1-Q57H mutant was expressed in Xenopus oocytes and analyzed electrophysiologically. AMT1;1-Q57H was characterized by increased ammonium-induced and reduced methylammonium-induced currents. AMT1;1-Q57H possesses a 100x lower affinity for ammonium (K(m)) and a 10-fold higher V(max) as compared with the wild type form. To test whether the trans-regulatory mechanism is conserved in archaeal homologs, AfAmt-2 from Archaeoglobus fulgidus was expressed in yeast. The transport function of AfAmt-2 also depends on trans-activation by the C terminus, and mutations in pore-residues corresponding to Q57H of AMT1;1 suppress nonfunctional AfAmt-2 mutants lacking the activating C terminus. Altogether, our data suggest that bacterial and plant AMTs use a conserved allosteric mechanism to control ammonium flux, potentially using a gating mechanism that limits flux to protect against ammonium toxicity.

  2. Modulation Effects of Curcumin on Erythrocyte Ion-Transporter Activity

    Directory of Open Access Journals (Sweden)

    Prabhakar Singh

    2015-01-01

    Full Text Available Curcumin ((1E,6E-1,7-Bis(4-hydroxy-3-methoxyphenyl-1,6-heptadiene-3,5-dione, the yellow biphenolic pigment isolated from turmeric (Curcuma longa, has various medicinal benefits through antioxidation, anti-inflammation, cardiovascular protection, immunomodulation, enhancing of the apoptotic process, and antiangiogenic property. We explored the effects of curcumin in vitro (10−5 M to 10−8 M and in vivo (340 and 170 mg/kg b.w., oral on Na+/K+ ATPase (NKA, Na+/H+ exchanger (NHE activity, and membrane lipid hydroperoxides (ROOH in control and experimental oxidative stress erythrocytes of Wistar rats. As a result, we found that curcumin potently modulated the membrane transporters activity with protecting membrane lipids against hydro-peroxidation in control as well as oxidatively challenged erythrocytes evidenced by stimulation of NKA, downregulation of NHE, and reduction of ROOH in the membrane. The observed results corroborate membrane transporters activity with susceptibility of erythrocyte membrane towards oxidative damage. Results explain the protective mechanism of curcumin against oxidative stress mediated impairment in ions-transporters activity and health beneficial effects.

  3. The Asymmetric Active Coupler: Stable Nonlinear Supermodes and Directed Transport

    CERN Document Server

    Kominis, Yannis; Flach, Sergej

    2016-01-01

    We consider the asymmetric active coupler (AAC) consisting of two coupled dissimilar waveguides with gain and loss. We show that under generic conditions, not restricted by parity-time symmetry, there exist finite-power, constant-intensity nonlinear supermodes (NS), resulting from the balance between gain, loss, nonlinearity, coupling and dissimilarity. The system is shown to possess nonreciprocal dynamics enabling directed power transport and optical isolation functionality.

  4. NiO nanoparticle-based urea biosensor.

    Science.gov (United States)

    Tyagi, Manisha; Tomar, Monika; Gupta, Vinay

    2013-03-15

    NiO nanoparticles (NiO-NPs) have been exploited successfully for the fabrication of a urea biosensor. A thin film of NiO nanoparticles deposited on an indium tin oxide (ITO) coated glass substrate serves as an efficient matrix for the immobilisation of urease (Ur), the specific enzyme for urea detection. The prepared bioelectrode (Ur/NiO-NP/ITO/glass) is utilised for urea sensing using cyclic voltammetry and UV-visible spectroscopy. NiO nanoparticles act as electro-catalytic species that are based on the shuttling of electrons between Ni(2+) and Ni(3+) in the octahedral site and result in an enhanced electrochemical current response. The prepared bioelectrode (Ur/NiO-NPs/ITO/glass) exhibits a high sensitivity of 21.3 μA/(mM (*) cm(2)) and a good linearity in a wide range (0.83-16.65 Mm) of urea concentrations with fast response time of 5s. The low value of the Michaelis-Menten constant (K(m)=0.34 mM) indicates the high affinity of Ur towards the analyte (urea). The high catalytic activity, along with the redox behaviour of NiO-NPs, makes it an efficient matrix for the realisation of a urea biosensor.

  5. Activation of CFTR-mediated Cl- Transport by Magnolin

    Institute of Scientific and Technical Information of China (English)

    JIN Ling-ling; LIU Xin; SUN Yan; LIN Sen; ZHOU Na; XU Li-na; YU BO; HOU Shu-guang; YANG Hong

    2008-01-01

    Magnolin is a herbal compound from Magnolia biondii Pamp.It possesses numerous biological activities.Cystic fibrosis transmembrane conductance regulator(CFTR)is all epithelial chloride channel that plays a key role in the fluid secretion of various exocrine organs.In the present study,the activation of CFTR-mediated chloride transport by magnolin is indentified and characterized.In CFTR stably trailsfected FRT cells.magnolin increases CFTR Cl- currents in a concentration-dependent manner.The activation of magnolin on CFTR is rapid,reversible,and cAMP-dependent.Magnolin does not elevate cellular cAMP level.indicating that it activates CFTR by direct binding and interaction with CFTR protein.Magnolin selectively activates wildtype CFTR rather than mutant CFTIL Magnolin may present a novel class of therapeutic lead compound for the treatment of diseases associated with reduced CFTR function such as keratoconjunctivitis sicca,idiopathic chronic pancreatiti,and chromc constipation.

  6. Imaging Renal Urea Handling in Rats at Millimeter Resolution using Hyperpolarized Magnetic Resonance Relaxometry

    Science.gov (United States)

    Reed, Galen D.; von Morze, Cornelius; Verkman, Alan S.; Koelsch, Bertram L.; Chaumeil, Myriam M.; Lustig, Michael; Ronen, Sabrina M.; Bok, Robert A.; Sands, Jeff M.; Larson, Peder E. Z.; Wang, Zhen J.; Larsen, Jan Henrik Ardenkjær; Kurhanewicz, John; Vigneron, Daniel B.

    2016-01-01

    In vivo spin spin relaxation time (T2) heterogeneity of hyperpolarized [13C,15N2]urea in the rat kidney was investigated. Selective quenching of the vascular hyperpolarized 13C signal with a macromolecular relaxation agent revealed that a long-T2 component of the [13C,15N2]urea signal originated from the renal extravascular space, thus allowing the vascular and renal filtrate contrast agent pools of the [13C,15N2]urea to be distinguished via multi-exponential analysis. The T2 response to induced diuresis and antidiuresis was performed with two imaging agents: hyperpolarized [13C,15N2]urea and a control agent hyperpolarized bis-1,1-(hydroxymethyl)-1-13C-cyclopropane-2H8. Large T2 increases in the inner-medullar and papilla were observed with the former agent and not the latter during antidiuresis. Therefore, [13C,15N2]urea relaxometry is sensitive to two steps of the renal urea handling process: glomerular filtration and the inner-medullary urea transporter (UT)-A1 and UT-A3 mediated urea concentrating process. Simple motion correction and subspace denoising algorithms are presented to aid in the multi exponential data analysis. Furthermore, a T2-edited, ultra long echo time sequence was developed for sub-2 mm3 resolution 3D encoding of urea by exploiting relaxation differences in the vascular and filtrate pools. PMID:27570835

  7. Substituted urea derivatives: a potent class of antidepressant agents.

    Science.gov (United States)

    Perveen, Shahnaz; Mustafa, Sana; Khan, Muhammad A; Dar, Ahsana; Khan, Khalid M; Voelter, Wolfgang

    2012-05-01

    A series of fourteen (14) N-nitrophenyl-N'-(alkyl/aryl)urea and symmetrical 1,3-disubstituted urea derivatives were synthesized and evaluated for their antidepressant activity in mice. Among them, N-(4-nitrophenyl)-N'-(1'-phenylethyl)urea (1), demonstrated profound antidepressant property as reflected by significant reduction in the immobility time (89.83%), whereas compounds 2-6 showed activity values between 36 to 59% which were also larger than the standard phenelzine. Compounds 7-9 were less effective in reducing the immobility period of mice 26.20 to 31.01%). This variable magnitude of antidepressant activity appears to be related to the position of the nitro group to the parent molecules 1, 2, and 8. Compound 1 with the nitro group at para position showed to be the most effective antidepressant. However, the activity declined, if the nitro is attached to ortho and meta positions.

  8. Urea production in long-term cultures of adult rat hepatocytes.

    Science.gov (United States)

    Sierra-Santoyo, A; López, M L; Hernández, A; Mendoza-Figueroa, T

    1994-04-01

    To study the functionality of the urea cycle in long-term cultures of adult rat hepatocytes, urea production and the activity of two urea cycle enzymes were measured in hepatocytes cultured on 3T3 cells for 15 days. Urea production was also measured in cultures maintained with medium containing either 0.4 mm arginine or 0.4 mm ornithine and in cultures exposed to different concentrations of NH(4)Cl, an in vivo inducer of urea production. In hepatocytes seeded on 3T3 cells, urea production decreased gradually to 50% of the initial value after 15 days. Urea production was similar in 3T3-hepatocyte cultures maintained for 11 days with medium containing ornithine or arginine. Hepatocytes exposed for 24 hr to 1, 3 and 5 mm NH(4)Cl showed an average increase in urea production of 25, 50 and 69%, respectively, above that of unexposed cultures over 15 days. Ornithine transcarbamylase (OTC) activity decreased by 84% after 5 days in culture and remained constant thereafter, while arginase activity remained constant over 15 days. In contrast, in hepatocytes seeded on plastic substratum, urea production decreased to 24% of the initial value after 8 days in culture. OTC and arginase activities also decreased to 13 and 10% of their initial values after 8 days in culture. These results show that 3T3-hepatocyte cultures from adult rats produce urea from ornithine and/or arginine for at least 15 days and respond to an inducer of urea production as in vivo. They also show that these cultures have decreasing and constant levels of OTC and arginase activities, respectively, owing probably to an adaptative response dependent on substrate concentrations and hormonal regulation. These findings also suggest that 3T3-hepatocyte cultures are a suitable in vitro system to study urea production, its regulation by substrates and hormones and its alteration by drugs and toxic chemicals.

  9. Associations between built environment and active transport in Danish adolescents

    DEFF Research Database (Denmark)

    Breum, Lars

    Introduction: Active commuting to school in Denmark is common but differentiates between schools. What is the association between the surrounding school environment assessed with a three component index and active commuting in adolescents? Methods: Materials: The study material consists of 1348...... adolescents (11-13 years) attending 5th or 6th grade in 14 different schools in Region Southern Denmark. Measures: - 5-day commuting diary. Mode of transport was reported from home to school and return (walk, bike, car, bus, train and other). - Web based questionnaire to asses perceived safety of bike route...

  10. Green synthesis of CuO nanoparticles by aqueous extract of Gundelia tournefortii and evaluation of their catalytic activity for the synthesis of N-monosubstituted ureas and reduction of 4-nitrophenol.

    Science.gov (United States)

    Nasrollahzadeh, Mahmoud; Maham, Mehdi; Sajadi, S Mohammad

    2015-10-01

    A facile, efficient and environmentally-friendly protocol has been developed for the green synthesis of CuO nanoparticles (NPs) by aqueous extract of Gundelia tournefortii as a mild, renewable and non-toxic reducing agent. CuO NPs were characterized by SEM, TEM, XRD, EDS, FT-IR and UV-vis spectroscopy. More importantly, the green synthesized CuO NPs presented excellent catalytic activity for reduction of 4-nitrophenol and synthesis of N-monosubstituted ureas via hydration of cyanamides with the aid of acetaldoxime as an effective water surrogate in ethanol as a green solvent. The catalyst was easily separated and the recovered catalyst was reused many times without any significant loss of the catalytic activity. Copyright © 2015 Elsevier Inc. All rights reserved.

  11. Morphological and functional characteristics of the kidney of cartilaginous fishes: with special reference to urea reabsorption.

    Science.gov (United States)

    Hyodo, Susumu; Kakumura, Keigo; Takagi, Wataru; Hasegawa, Kumi; Yamaguchi, Yoko

    2014-12-15

    For adaptation to high-salinity marine environments, cartilaginous fishes (sharks, skates, rays, and chimaeras) adopt a unique urea-based osmoregulation strategy. Their kidneys reabsorb nearly all filtered urea from the primary urine, and this is an essential component of urea retention in their body fluid. Anatomical investigations have revealed the extraordinarily elaborate nephron system in the kidney of cartilaginous fishes, e.g., the four-loop configuration of each nephron, the occurrence of distinct sinus and bundle zones, and the sac-like peritubular sheath in the bundle zone, in which the nephron segments are arranged in a countercurrent fashion. These anatomical and morphological characteristics have been considered to be important for urea reabsorption; however, a mechanism for urea reabsorption is still largely unknown. This review focuses on recent progress in the identification and mapping of various pumps, channels, and transporters on the nephron segments in the kidney of cartilaginous fishes. The molecules include urea transporters, Na(+)/K(+)-ATPase, Na(+)-K(+)-Cl(-) cotransporters, and aquaporins, which most probably all contribute to the urea reabsorption process. Although research is still in progress, a possible model for urea reabsorption in the kidney of cartilaginous fishes is discussed based on the anatomical features of nephron segments and vascular systems and on the results of molecular mapping. The molecular anatomical approach thus provides a powerful tool for understanding the physiological processes that take place in the highly elaborate kidney of cartilaginous fishes.

  12. Examining Changes in Radioxenon Isotope Activity Ratios during Subsurface Transport

    Science.gov (United States)

    Annewandter, Robert

    2014-05-01

    The Non-Proliferation Experiment (NPE) has demonstrated and modelled the usefulness of barometric pumping induced gas transport and subsequent soil gas sampling during On-Site inspections. Generally, gas transport has been widely studied with different numerical codes. However, gas transport of radioxenons and radioiodines in the post-detonation regime and their possible fractionation is still neglected in the open peer-reviewed literature. Atmospheric concentrations of the radioxenons Xe-135, Xe-133m, Xe-133 and Xe-131m can be used to discriminate between civilian releases (nuclear power plants or medical isotope facilities), and nuclear explosion sources. It is based on the multiple isotopic activity ratio method. Yet it is not clear whether subsurface migration of the radionuclides, with eventual release into the atmosphere, can affect the activity ratios due to fractionation. Fractionation can be caused by different mass diffusivities due to mass differences between the radionuclides. Cyclical changes in atmospheric pressure can drive subsurface gas transport. This barometric pumping phenomenon causes an oscillatoric flow in upward trending fractures or highly conductive faults which, combined with diffusion into the porous matrix, leads to a net transport of gaseous components - a so-called ratcheting effect. We use a general purpose reservoir simulator (Complex System Modelling Platform, CSMP++) which is recognized by the oil industry as leading in Discrete Fracture-Matrix (DFM) simulations. It has been applied in a range of fields such as deep geothermal systems, three-phase black oil simulations, fracture propagation in fractured, porous media, and Navier-Stokes pore-scale modelling among others. It is specifically designed to account for structurally complex geologic situation of fractured, porous media. Parabolic differential equations are solved by a continuous Galerkin finite-element method, hyperbolic differential equations by a complementary finite

  13. Differences in associations between active transportation and built environmental exposures when expressed using different components of individual activity spaces.

    Science.gov (United States)

    van Heeswijck, Torbjorn; Paquet, Catherine; Kestens, Yan; Thierry, Benoit; Morency, Catherine; Daniel, Mark

    2015-05-01

    This study assessed relationships between built environmental exposures measured within components of individual activity spaces (i.e., travel origins, destinations and paths in-between), and use of active transportation in a metropolitan setting. Individuals (n=37,165) were categorised as using active or sedentary transportation based on travel survey data. Generalised Estimating Equations analysis was used to test relationships with active transportation. Strength and significance of relationships between exposures and active transportation varied for different components of the activity space. Associations were strongest when including travel paths in expression of the built environment. Land use mix and greenness were negatively related to active transportation.

  14. Modelling of electron transport and of sawtooth activity in tokamaks

    Energy Technology Data Exchange (ETDEWEB)

    Angioni, C

    2001-10-01

    Transport phenomena in tokamak plasmas strongly limit the particle and energy confinement and represent a crucial obstacle to controlled thermonuclear fusion. Within the vast framework of transport studies, three topics have been tackled in the present thesis: first, the computation of neoclassical transport coefficients for general axisymmetric equilibria and arbitrary collisionality regime; second, the analysis of the electron temperature behaviour and transport modelling of plasma discharges in the Tokamak a configuration Variable (TCV); third, the modelling and simulation of the sawtooth activity with different plasma heating conditions. The work dedicated to neoclassical theory has been undertaken in order to first analytically identify a set of equations suited for implementation in existing Fokker-Planck codes. Modifications of these codes enabled us to compute the neoclassical transport coefficients considering different realistic magnetic equilibrium configurations and covering a large range of variation of three key parameters: aspect ratio, collisionality, and effective charge number. A comparison of the numerical results with an analytical limit has permitted the identification of two expressions for the trapped particle fraction, capable of encapsulating the geometrical effects and thus enabling each transport coefficient to be fitted with a single analytical function. This has allowed us to provide simple analytical formulae for all the neoclassical transport coefficients valid for arbitrary aspect ratio and collisionality in general realistic geometry. This work is particularly useful for a correct evaluation of the neoclassical contribution in tokamak scenarios with large bootstrap cur- rent fraction, or improved confinement regimes with low anomalous transport and for the determination of the plasma current density profile, since the plasma conductivity is usually assumed neoclassical. These results have been included in the plasma transport code

  15. Curcumin directly inhibits the transport activity of GLUT1.

    Science.gov (United States)

    Gunnink, Leesha K; Alabi, Ola D; Kuiper, Benjamin D; Gunnink, Stephen M; Schuiteman, Sam J; Strohbehn, Lauren E; Hamilton, Kathryn E; Wrobel, Kathryn E; Louters, Larry L

    2016-06-01

    Curcumin, a major ingredient in turmeric, has a long history of medicinal applications in a wide array of maladies including treatment for diabetes and cancer. Seemingly counterintuitive to the documented hypoglycemic effects of curcumin, however, a recent report indicates that curcumin directly inhibits glucose uptake in adipocytes. The major glucose transporter in adipocytes is GLUT4. Therefore, this study investigates the effects of curcumin in cell lines where the major transporter is GLUT1. We report that curcumin has an immediate inhibitory effect on basal glucose uptake in L929 fibroblast cells with a maximum inhibition of 80% achieved at 75 μM curcumin. Curcumin also blocks activation of glucose uptake by azide, glucose deprivation, hydroxylamine, or phenylarsine oxide. Inhibition does not increase with exposure time and the inhibitory effects reverse within an hour. Inhibition does not appear to involve a reaction between curcumin and the thiol side chain of a cysteine residue since neither prior treatment of cells with iodoacetamide nor curcumin with cysteine alters curcumin's inhibitory effects. Curcumin is a mixed inhibitor reducing the Vmax of 2DG transport by about half with little effect on the Km. The inhibitory effects of curcumin are not additive to the effects of cytochalasin B and 75 μM curcumin actually reduces specific cytochalasin B binding by 80%. Taken together, the data suggest that curcumin binds directly to GLUT1 at a site that overlaps with the cytochalasin B binding site and thereby inhibits glucose transport. A direct inhibition of GLUT proteins in intestinal epithelial cells would likely reduce absorption of dietary glucose and contribute to a hypoglycemic effect of curcumin. Also, inhibition of GLUT1 activity might compromise cancer cells that overexpress GLUT1 and be another possible mechanism for the documented anticancer effects of curcumin. Copyright © 2016. Published by Elsevier B.V.

  16. Evaluation of the physical activity biography: sport and transport.

    Science.gov (United States)

    Rogen, Sandra; Hofmann, Peter; Bauernhofer, Thomas; Müller, Wolfram

    2014-05-01

    Beside the genetic disposition, physical activity (PA) is one of the major health factors and can play a large role in the prevention and therapy of many diseases (cardiovascular diseases, cancer, obesity-related diseases etc.). In contrast to the genetic disposition, PA can be deliberately influenced by lifestyle. Therefore, it is of high importance to assess PA patterns. In order to assess PA reliably and validly, a new questionnaire (Physical Activity Biography, PAB) was created. The PAB assesses recreational PA (sport and transport) and enables to distinguish between endurance intensity levels and considers strength and high speed activity patterns throughout life. This study aims to evaluate the PAB by means of item analysis, retest-reliability and validity (criteria were physical fitness assessed by the questionnaire FFB-mot and by exercise tests). 141 participants answered the PAB. For deriving retest-reliability, 81 participants completed the PAB after a retest-interval of one month again. 55 participated in exercise tests and answered the FFB-mot to determine construct validity. Retest-reliability (ICC) above 0.7 was found for most items. For the items assessing recent PA, the criteria of convergent and discriminant validity were given. Despite the complexity of the question under study, the results fulfilled the expectations concerning reliability and validity. The PAB enables to assess the amount of sport and locomotion a person has accomplished during different life time frames and, because of the protective effects of PA on various diseases, may become an important tool for risk assessment. Key pointsThe risk of chronic diseases depends largely on physical activity biography.A new questionnaire (PAB) assessing recent and lifetime physical activity was created.The PAB assesses physical activity during sports and transport.The results of the evaluation of the PAB fulfilled the expectations.The PAB enables to determine a person's amount of recreational

  17. Metabolic Induction of Lactic Acid Bacteria for Urea Removal

    Institute of Scientific and Technical Information of China (English)

    ZHANG Su-ai; BAI Yu; LI Dong-xia; CHEN Bo-li; SONG Cun-jiang; QIAO Ming-qiang; KONG De-ling; YU Yao-ting

    2009-01-01

    Objective:This study aims to induce nonpathogenic bacteria for urea removal as a potential treatment in renal failure. Methods:Lactococus lactis MG1363 was induced by repeated exposure to urea-rich culture media, the ability to remove urea from the media was evaluated. The effect of gastroenteric environment, such as low pH, bile salt and antiagonistic properties were investigated.The antimicrobial activities on pathogenic E.coli and S.aureus in the intestinal tract and the antibiotic tolerance of the induced bacteria were also studied.Results: Induced bacteria of 50 generations could decrease the urea level from 40.01 mg/dL to 32.99 mg/dL after 24 h. The bacteria could grow after treatment at pH3.0 for 2 h and in 0.1% bile salt for 6 h, and the urea removal activity was retained in such simulated gastroenteric environment. The removal of urea was significantly enhanced to 35.8% by addition of Ni2+ to the culture medium at neutral pH. It was also found that the induced bacteria could inhibit the growth of E.coli and S.aureus, and tolerate ampicillin,gentamicin,roxithromycin,tetracycline and cefradine. The safety tests were performed by feeding normal rats with either Lactococus lactis MG1363 or induced Lactococus lactis MG1363. The two materials did not cause any changes in blood cells, blood biochemical indexes and body weight. Conclusion: These results suggest that the induced Lactococus lactis MG1363 has the potential as an oral therapy for the removal of urea in patients with renal failure.

  18. 40 CFR 721.9928 - Urea, tetraethyl-.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Urea, tetraethyl-. 721.9928 Section... Substances § 721.9928 Urea, tetraethyl-. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as urea, tetraethyl- (PMN P-94-1017; CAS No. 1187-03-7)...

  19. 40 CFR 721.9892 - Alkylated urea.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Alkylated urea. 721.9892 Section 721... Alkylated urea. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as an alkylated urea (PMN P-93-1649) is subject to reporting under...

  20. Dopamine Transporter Activity Is Modulated by α-Synuclein.

    Science.gov (United States)

    Butler, Brittany; Saha, Kaustuv; Rana, Tanu; Becker, Jonas P; Sambo, Danielle; Davari, Paran; Goodwin, J Shawn; Khoshbouei, Habibeh

    2015-12-04

    The duration and strength of the dopaminergic signal are regulated by the dopamine transporter (DAT). Drug addiction and neurodegenerative and neuropsychiatric diseases have all been associated with altered DAT activity. The membrane localization and the activity of DAT are regulated by a number of intracellular proteins. α-Synuclein, a protein partner of DAT, is implicated in neurodegenerative disease and drug addiction. Little is known about the regulatory mechanisms of the interaction between DAT and α-synuclein, the cellular location of this interaction, and the functional consequences of this interaction on the basal, amphetamine-induced DAT-mediated dopamine efflux, and membrane microdomain distribution of the transporter. Here, we found that the majority of DAT·α-synuclein protein complexes are found at the plasma membrane of dopaminergic neurons or mammalian cells and that the amphetamine-mediated increase in DAT activity enhances the association of these proteins at the plasma membrane. Further examination of the interaction of DAT and α-synuclein revealed a transient interaction between these two proteins at the plasma membrane. Additionally, we found DAT-induced membrane depolarization enhances plasma membrane localization of α-synuclein, which in turn increases dopamine efflux and enhances DAT localization in cholesterol-rich membrane microdomains.

  1. Artemisinin inhibits chloroplast electron transport activity: mode of action.

    Directory of Open Access Journals (Sweden)

    Adyasha Bharati

    Full Text Available Artemisinin, a secondary metabolite produced in Artemisia plant species, besides having antimalarial properties is also phytotoxic. Although, the phytotoxic activity of the compound has been long recognized, no information is available on the mechanism of action of the compound on photosynthetic activity of the plant. In this report, we have evaluated the effect of artemisinin on photoelectron transport activity of chloroplast thylakoid membrane. The inhibitory effect of the compound, under in vitro condition, was pronounced in loosely and fully coupled thylakoids; being strong in the former. The extent of inhibition was drastically reduced in the presence of uncouplers like ammonium chloride or gramicidin; a characteristic feature described for energy transfer inhibitors. The compound, on the other hand, when applied to plants (in vivo, behaved as a potent inhibitor of photosynthetic electron transport. The major site of its action was identified to be the Q(B; the secondary quinone moiety of photosystemII complex. Analysis of photoreduction kinetics of para-benzoquinone and duroquinone suggest that the inhibition leads to formation of low pool of plastoquinol, which becomes limiting for electron flow through photosystemI. Further it was ascertained that the in vivo inhibitory effect appeared as a consequence of the formation of an unidentified artemisinin-metabolite rather than by the interaction of the compound per se. The putative metabolite of artemisinin is highly reactive in instituting the inhibition of photosynthetic electron flow eventually reducing the plant growth.

  2. Promoting physical activity and reducing climate change : Opportunities to replace short car trips with active transportation

    NARCIS (Netherlands)

    Maibach, E.; Steg, L.; Anable, J.

    2009-01-01

    Automobile use is a significant contributor to climate change, local air pollution, pedestrian injuries and deaths, declines in physical activity and obesity. A significant proportion of car use is for short trips that can relatively easily be taken with active transportation options - walking or

  3. CFD Model of Water Droplet Transport for ISS Hygiene Activity

    Science.gov (United States)

    Son, Chang H.

    2011-01-01

    The goal of the study is to assess the impacts of free water propagation in the Waste and Hygiene Compartment (WHC). Free water can be generated inside the WHC in small quantities due to crew hygiene activity. To mitigate potential impact of free water in Node 3 cabin the WHC doorway is enclosed by a waterproof bump-out, Kabin, with openings at the top and bottom. At the overhead side of the rack, there is a screen that prevents large drops of water from exiting. However, as the avionics fan in the WHC causes airflow toward the deck side of the rack, small quantities of free water may exit at the bottom of the Kabin. A Computational Fluid Dynamics (CFD) analysis of Node 3 cabin airflow made possible to identify the paths of water transport. The Node 3 airflow was computed for several ventilation scenarios. To simulate the droplet transport the Lagrangian discrete phase approach was used. Various initial droplet distributions were considered in the study. The droplet diameter was varied in the range of 2-20 mm. The results of the computations showed that most of the drops fall to the rack surface not far from the WHC curtain. The probability of the droplet transport to the adjacent rack surface with electronic equipment was predicted.

  4. Oscillations and multiple steady states in active membrane transport models.

    Science.gov (United States)

    Vieira, F M; Bisch, P M

    1994-01-01

    The dynamic behavior of some non-linear extensions of the six-state alternating access model for active membrane transport is investigated. We use stoichio-metric network analysis to study the stability of steady states. The bifurcation analysis has been done through standard numerical methods. For the usual six-state model we have proved that there is only one steady state, which is globally asymptotically stable. When we added an autocatalytic step we found self-oscillations. For the competition between a monomer cycle and a dimer cycle, with steps of dimer formation, we have also found self-oscillations. We have also studied models involving the formation of a complex with other molecules. The addition of two steps for formation of a complex of the monomer with another molecule does not alter either the number or the stability of steady states of the basic six-state model. The model which combines the formation of a complex with an autocatalytic step shows both self-oscillations and multiple steady states. The results lead us to conclude that oscillations could be produced by active membrane transport systems if the transport cycle contains a sufficiently large number of steps (six in the present case) and is coupled to at least one autocatalytic reaction,. Oscillations are also predicted when the monomer cycle is coupled to a dimer cycle. In fact, the autocatalytic reaction can be seen as a simplification of the model involving competition between monomer and dimer cycles, which seems to be a more realistic description of biological systems. A self-regulation mechanism of the pumps, related to the multiple stationary states, is expected only for a combined effect of autocatalysis and formation of complexes with other molecules. Within the six-state model this model also leads to oscillation.

  5. Assessing Barriers and Motivators for Use of a Trail for Active Transportation in a College Town

    OpenAIRE

    FitzPatrick, Timothy Michael

    2017-01-01

    A high amount of the US population is not physically active, contributing to rates of heart disease and obesity. One strategy to increase physical activity is to use more active transportation, defined as walking or biking for transit. Besides increasing physical activity levels, active transportation can provide other benefits such as decreased air pollution from cars. College campuses provide opportunities for active transportation as most residences are close to campus. Therefore, we exami...

  6. Socioeconomic and regional differences in active transportation in Brazil

    Directory of Open Access Journals (Sweden)

    Thiago Hérick de Sá

    2016-01-01

    Full Text Available ABSTRACT OBJECTIVE To present national estimates regarding walking or cycling for commuting in Brazil and in 10 metropolitan regions. METHODS By using data from the Health section of 2008’s Pesquisa Nacional por Amostra de Domicílio (Brazil’s National Household Sample Survey, we estimated how often employed people walk or cycle to work, disaggregating our results by sex, age range, education level, household monthly income per capita, urban or rural address, metropolitan regions, and macro-regions in Brazil. Furthermore, we estimated the distribution of this same frequency according to quintiles of household monthly income per capita in each metropolitan region of the country. RESULTS A third of the employed men and women walk or cycle from home to work in Brazil. For both sexes, this share decreases as income and education levels rise, and it is higher among younger individuals, especially among those living in rural areas and in the Northeast region of the country. Depending on the metropolitan region, the practice of active transportation is two to five times more frequent among low-income individuals than among high-income individuals. CONCLUSIONS Walking or cycling to work in Brazil is most frequent among low-income individuals and the ones living in less economically developed areas. Active transportation evaluation in Brazil provides important information for public health and urban mobility policy-making

  7. Coupled ATPase-adenylate kinase activity in ABC transporters

    Science.gov (United States)

    Kaur, Hundeep; Lakatos-Karoly, Andrea; Vogel, Ramona; Nöll, Anne; Tampé, Robert; Glaubitz, Clemens

    2016-01-01

    ATP-binding cassette (ABC) transporters, a superfamily of integral membrane proteins, catalyse the translocation of substrates across the cellular membrane by ATP hydrolysis. Here we demonstrate by nucleotide turnover and binding studies based on 31P solid-state NMR spectroscopy that the ABC exporter and lipid A flippase MsbA can couple ATP hydrolysis to an adenylate kinase activity, where ADP is converted into AMP and ATP. Single-point mutations reveal that both ATPase and adenylate kinase mechanisms are associated with the same conserved motifs of the nucleotide-binding domain. Based on these results, we propose a model for the coupled ATPase-adenylate kinase mechanism, involving the canonical and an additional nucleotide-binding site. We extend these findings to other prokaryotic ABC exporters, namely LmrA and TmrAB, suggesting that the coupled activities are a general feature of ABC exporters. PMID:28004795

  8. Autotrophic ammonia oxidation at low pH through urea hydrolysis.

    Science.gov (United States)

    Burton, S A; Prosser, J I

    2001-07-01

    Ammonia oxidation in laboratory liquid batch cultures of autotrophic ammonia oxidizers rarely occurs at pH values less than 7, due to ionization of ammonia and the requirement for ammonium transport rather than diffusion of ammonia. Nevertheless, there is strong evidence for autotrophic nitrification in acid soils, which may be carried out by ammonia oxidizers capable of using urea as a source of ammonia. To determine the mechanism of urea-linked ammonia oxidation, a ureolytic autotrophic ammonia oxidizer, Nitrosospira sp. strain NPAV, was grown in liquid batch culture at a range of pH values with either ammonium or urea as the sole nitrogen source. Growth and nitrite production from ammonium did not occur at pH values below 7. Growth on urea occurred at pH values in the range 4 to 7.5 but ceased when urea hydrolysis was complete, even though ammonia, released during urea hydrolysis, remained in the medium. The results support a mechanism whereby urea enters the cells by diffusion and intracellular urea hydrolysis and ammonia oxidation occur independently of extracellular pH in the range 4 to 7.5. A proportion of the ammonia produced during this process diffuses from the cell and is not subsequently available for growth if the extracellular pH is less than 7. Ureolysis therefore provides a mechanism for nitrification in acid soils, but a proportion of the ammonium produced is likely to be released from the cell and may be used by other soil organisms.

  9. Adult active transport in the Netherlands: an analysis of its contribution to physical activity requirements.

    Directory of Open Access Journals (Sweden)

    Elliot Fishman

    Full Text Available Modern, urban lifestyles have engineered physical activity out of everyday life and this presents a major threat to human health. The Netherlands is a world leader in active travel, particularly cycling, but little research has sought to quantify the cumulative amount of physical activity through everyday walking and cycling.Using data collected as part of the Dutch National Travel Survey (2010 - 2012, this paper determines the degree to which Dutch walking and cycling contributes to meeting minimum level of physical activity of 150 minutes of moderate intensity aerobic activity throughout the week. The sample includes 74,465 individuals who recorded at least some travel on the day surveyed. As physical activity benefits are cumulative, all walking and cycling trips are analysed, including those to and from public transport. These trips are then converted into an established measure of physical activity intensity, known as metabolic equivalents of tasks. Multivariate Tobit regression models were performed on a range of socio-demographic, transport resources, urban form and meteorological characteristics.The results reveal that Dutch men and women participate in 24 and 28 minutes of daily physical activity through walking and cycling, which is 41% and 55% more than the minimum recommended level. It should be noted however that some 57% of the entire sample failed to record any walking or cycling, and an investigation of this particular group serves as an important topic of future research. Active transport was positively related with age, income, bicycle ownership, urban density and air temperature. Car ownership had a strong negative relationship with physically active travel.The results of this analysis demonstrate the significance of active transport to counter the emerging issue of sedentary lifestyle disease. The Dutch experience provides other countries with a highly relevant case study in the creation of environments and cultures that

  10. Hydrotropic Solubilization by Urea Derivatives: A Molecular Dynamics Simulation Study

    Directory of Open Access Journals (Sweden)

    Yong Cui

    2013-01-01

    Full Text Available Hydrotropy is a phenomenon where the presence of a large quantity of one solute enhances the solubility of another solute. The mechanism of this phenomenon remains a topic of debate. This study employed molecular dynamics simulation to investigate the hydrotropic mechanism of a series of urea derivatives, that is, urea (UR, methylurea (MU, ethylurea (EU, and butylurea (BU. A poorly water-soluble compound, nifedipine (NF, was used as the model solute that was solubilized. Structural, dynamic, and energetic changes upon equilibration were analyzed to supply insights to the solubilization mechanism. The study demonstrated that NF and urea derivatives underwent significant nonstoichiometric molecular aggregation in the aqueous solution, a result consistent with the self-aggregation of urea derivatives under the same conditions. The analysis of hydrogen bonding and energy changes revealed that the aggregation was driven by the partial restoration of normal water structure. The energetic data also suggested that the promoted solubilization of NF is favored in the presence of urea derivatives. While the solutes aggregated to a varying degree, the systems were still in single-phase liquid state as attested by their active dynamics.

  11. Estudio histopatológico de hígado y riñón de caninos y su relación con las concentraciones de urea, creatinina, proteínas, enzimas (ALT y SAP en sangre premortem y en humor acuoso a las 0 y 24 horas postmortem Histopathological study of canine liver and kidney and their relationship with blood and postmortem aqueous humour samples concentrations of urea, creatinine, proteins and enzymes activities (ALT and SAP

    Directory of Open Access Journals (Sweden)

    C. GALLARDO

    2003-01-01

    and ALT and SAP plasmatic activity. Thirty one animals were used in this study. They did not have clinical history of hepatic or renal diseases. Plasma samples were obtained before euthanasia. A sample of aqueous humor was obtained from the right eye of each dog just after euthanasia and a similar sample was obtained 24 hours later from the left eye. Urea, creatinine and protein concentrations and plasmatic activity of ALT and SAP were determined and samples of liver and kidney were obtained at postmortem and preserved in formaline (10%. Histophatological findings were characterized according to the following scale: none (0, mild (I, moderate (II, marked (III and severe (IV. The results showed that all dogs have some degree of renal and hepatic damage (R.D.L. and H.D.L. respectively. Glomerulonephritis and interstitial nephritis were found in 100% and 88% of cases, respectively. Histophatological findings of circulatory type were the main changes found in the liver (100%, characterized mainly by diffuse congestion (63.3%. The values of urea, creatinine and proteins concentration and ALT and SAP activity were higher in plasma than in aqueous humour, but there was not a correlation between them, with exception of urea (c = 0.99. In addition, there was not a significant correlation between histophatological findings and plasmatic values studied

  12. An Efficient and Green Procedure for the Knoevenagel Condensation Catalyzed by Urea

    Institute of Scientific and Technical Information of China (English)

    孙崎; 史兰香; 葛泽梅; 程铁明; 李润涛

    2005-01-01

    An efficient and green procedure for the urea catalyzed Knoevenagel condensation was developed. In the presence of a catalytic ammount of urea, stoichiometric aldehyde and active methylene compound reacted under sol-vent-free conditions at 100℃ for 5-60 min to give nearly quantitative yield of product.

  13. Body Composition, Physical Activity and Active Transportation in Adolescents of Metropolitan Region of Curitiba, Brazil

    Directory of Open Access Journals (Sweden)

    Leandra Ulbrict

    2014-06-01

    Full Text Available Background: Physical activity is a part of a healthy lifestyle, however sed entary habits are currently prevalent among adolescents which impacts rates of overweight and obesity in this group. This study aims to describe the relationship of physical activity with the use of active transportation to school (ATS and its relationshi p with body composition in adolescents. Materials and Methods: Information about physical activity, sedentary behavior and active transportation were collected through two survey instruments, one completed by a responsible parent/guardian and other by the adolescent. Body composition was assessed by dual - energy x - ray absorptiometry (DXA. Excess body fat was defined as ≥ 25% in male and ≥ 30% among female adolescents. Less than 60 minutes of moderate to vigorous daily physical activity defined one as sede ntary and greater than 2 hours of screen time per day was defined as excessive. Results: The prevalence of excess body fat was 46.5%. Only 24.7% of the sample performed recommended amounts of physical activity and 92.3% engaged in excess screen time. Appro ximately one - fifth of our sample (19.2% used ATS. The main barriers to active transport were traffic, distance and safety. Those that used ATS had lower body fat and fewer hours of sedentary behavior.

  14. Variability and seasonality of active transportation in USA: evidence from the 2001 NHTS

    Directory of Open Access Journals (Sweden)

    Bingham C Raymond

    2011-09-01

    Full Text Available Abstract Background Active transportation including walking and bicycling is an important source of physical activity. Promoting active transportation is a challenge for the fields of public health and transportation. Descriptive data on the predictors of active transportation, including seasonal patterns in active transportation in the US as a whole, is needed to inform interventions and policies. Methods This study analyzed monthly variation in active transportation for the US using National Household Travel Survey 2001 data. For each age group of children, adolescents, adults and elderly, logistic regression models were used to identify predictors of the odds of active transportation including gender, race/ethnicity, household income level, geographical region, urbanization level, and month. Results The probability of engaging in active transportation was generally higher for children and adolescents than for adults and the elderly. Active transportation was greater in the lower income groups (except in the elderly, was lower in the South than in other regions of the US, and was greater in areas with higher urbanization. The percentage of people using active transportation exhibited clear seasonal patterns: high during summer months and low during winter months. Children and adolescents were more sensitive to seasonality than other age groups. Women, non-Caucasians, persons with lower household income, who resided in the Midwest or Northeast, and who lived in more urbanized areas had greater seasonal variation. Conclusions These descriptive results suggest that interventions and policies that target the promotion of active transportation need to consider socio-demographic factors and seasonality.

  15. Active transport and obesity prevention - A transportation sector obesity impact scoping review and assessment for Melbourne, Australia.

    Science.gov (United States)

    Brown, V; Moodie, M; Mantilla Herrera, A M; Veerman, J L; Carter, R

    2017-03-01

    Given the alarming prevalence of obesity worldwide and the need for interventions to halt the growing epidemic, more evidence on the role and impact of transport interventions for obesity prevention is required. This study conducts a scoping review of the current evidence of association between modes of transport (motor vehicle, walking, cycling and public transport) and obesity-related outcomes. Eleven reviews and thirty-three primary studies exploring associations between transport behaviours and obesity were identified. Cohort simulation Markov modelling was used to estimate the effects of body mass index (BMI) change on health outcomes and health care costs of diseases causally related to obesity in the Melbourne, Australia population. Results suggest that evidence for an obesity effect of transport behaviours is inconclusive (29% of published studies reported expected associations, 33% mixed associations), and any potential BMI effect is likely to be relatively small. Hypothetical scenario analyses suggest that active transport interventions may contribute small but significant obesity-related health benefits across populations (approximately 65 health adjusted life years gained per year). Therefore active transport interventions that are low cost and targeted to those most amenable to modal switch are the most likely to be effective and cost-effective from an obesity prevention perspective. The uncertain but potentially significant opportunity for health benefits warrants the collection of more and better quality evidence to fully understand the potential relationships between transport behaviours and obesity. Such evidence would contribute to the obesity prevention dialogue and inform policy across the transportation, health and environmental sectors.

  16. Urea Hydrolysis Rate in Soil Toposequences as Influenced by pH, Carbon, Nitrogen, and Soluble Metals.

    Science.gov (United States)

    Fisher, Kristin A; Meisinger, John J; James, Bruce R

    2016-01-01

    A simultaneous increase in the use of urea fertilizer and the incidence of harmful algal blooms worldwide has generated interest in potential loss pathways of urea from agricultural areas. The objective of this research was to study the rate of urea hydrolysis in soil profile toposequences sampled from the Coastal Plain (CP) and Piedmont (PM) regions of Maryland to understand native urea hydrolysis rates (UHRs) as well as the controls governing urea hydrolysis both across a landscape and with depth in the soil profile. A pH-adjustment experiment was conducted to explore the relationship between pH and urea hydrolysis because of the importance of pH to both agronomic productivity and microbial communities. Soils were sampled from both A and B horizons along transects containing an agricultural field (AG), a grassed field border (GB), and a perennially vegetated zone adjacent to surface water. On average, the A-horizon UHRs were eight times greater than corresponding B-horizon rates, and within the CP, the riparian zone (RZ) soils hydrolyzed urea faster than the agricultural soils. The pH adjustment of these soils indicated the importance of organic-matter-related factors (C, N, extractable metals) in determining UHR. These results suggest that organic-matter-rich RZ soils may be valuable in mitigating losses of urea from neighboring fields. Additional field-scale urea hydrolysis studies would be valuable to corroborate the mechanisms described herein and to explore the conditions affecting the fate and transport of urea in agroecosystems.

  17. Thermally activated charge transport in microbial protein nanowires.

    Science.gov (United States)

    Lampa-Pastirk, Sanela; Veazey, Joshua P; Walsh, Kathleen A; Feliciano, Gustavo T; Steidl, Rebecca J; Tessmer, Stuart H; Reguera, Gemma

    2016-03-24

    The bacterium Geobacter sulfurreducens requires the expression of conductive protein filaments or pili to respire extracellular electron acceptors such as iron oxides and uranium and to wire electroactive biofilms, but the contribution of the protein fiber to charge transport has remained elusive. Here we demonstrate efficient long-range charge transport along individual pili purified free of metal and redox organic cofactors at rates high enough to satisfy the respiratory rates of the cell. Carrier characteristics were within the orders reported for organic semiconductors (mobility) and inorganic nanowires (concentration), and resistivity was within the lower ranges reported for moderately doped silicon nanowires. However, the pilus conductance and the carrier mobility decreased when one of the tyrosines of the predicted axial multistep hopping path was replaced with an alanine. Furthermore, low temperature scanning tunneling microscopy demonstrated the thermal dependence of the differential conductance at the low voltages that operate in biological systems. The results thus provide evidence for thermally activated multistep hopping as the mechanism that allows Geobacter pili to function as protein nanowires between the cell and extracellular electron acceptors.

  18. Hypoxia inhibits colonic ion transport via activation of AMP kinase.

    LENUS (Irish Health Repository)

    Collins, Danielle

    2012-02-01

    BACKGROUND AND AIMS: Mucosal hypoxia is a common endpoint for many pathological processes including ischemic colitis, colonic obstruction and anastomotic failure. Previous studies suggest that hypoxia modulates colonic mucosal function through inhibition of chloride secretion. However, the molecular mechanisms underlying this observation are poorly understood. AMP-activated protein kinase (AMPK) is a metabolic energy regulator found in a wide variety of cells and has been linked to cystic fibrosis transmembrane conductance regulator (CFTR) mediated chloride secretion in several different tissues. We hypothesized that AMPK mediates many of the acute effects of hypoxia on human and rat colonic electrolyte transport. METHODS: The fluorescent chloride indicator dye N-(ethoxycarbonylmethyl)-6-methoxyquinolinium bromide was used to measure changes in intracellular chloride concentrations in isolated single rat colonic crypts. Ussing chamber experiments in human colonic mucosa were conducted to evaluate net epithelial ion transport. RESULTS: This study demonstrates that acute hypoxia inhibits electrogenic chloride secretion via AMPK mediated inhibition of CFTR. Pre-treatment of tissues with the AMPK inhibitor 6-[4-(2-piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo [1,5-a] pyrimidine (compound C) in part reversed the effects of acute hypoxia on chloride secretion. CONCLUSION: We therefore suggest that AMPK is a key component of the adaptive cellular response to mucosal hypoxia in the colon. Furthermore, AMPK may represent a potential therapeutic target in diseased states or in prevention of ischemic intestinal injury.

  19. Measuring the performance of multi-agency programmatic permits for Washington State Department of Transportation activities

    OpenAIRE

    2005-01-01

    In 2001, the Washington State Legislature established the Transportation Permit Efficiency and Accountability Committee (TPEAC) to identify measures to streamline permit procedures for transportation activities and improve environmental outcomes. A programmatic subcommittee was created to develop a multi-agency approach for developing programmatic permits that would cover 60 to 70 percent of Washington State Department of Transportation (WSDOT) activities (mostly maintenance and preservation ...

  20. Reliability and validity of the transport and physical activity questionnaire (TPAQ for assessing physical activity behaviour.

    Directory of Open Access Journals (Sweden)

    Emma J Adams

    Full Text Available BACKGROUND: No current validated survey instrument allows a comprehensive assessment of both physical activity and travel behaviours for use in interdisciplinary research on walking and cycling. This study reports on the test-retest reliability and validity of physical activity measures in the transport and physical activity questionnaire (TPAQ. METHODS: The TPAQ assesses time spent in different domains of physical activity and using different modes of transport for five journey purposes. Test-retest reliability of eight physical activity summary variables was assessed using intra-class correlation coefficients (ICC and Kappa scores for continuous and categorical variables respectively. In a separate study, the validity of three survey-reported physical activity summary variables was assessed by computing Spearman correlation coefficients using accelerometer-derived reference measures. The Bland-Altman technique was used to determine the absolute validity of survey-reported time spent in moderate-to-vigorous physical activity (MVPA. RESULTS: In the reliability study, ICC for time spent in different domains of physical activity ranged from fair to substantial for walking for transport (ICC = 0.59, cycling for transport (ICC = 0.61, walking for recreation (ICC = 0.48, cycling for recreation (ICC = 0.35, moderate leisure-time physical activity (ICC = 0.47, vigorous leisure-time physical activity (ICC = 0.63, and total physical activity (ICC = 0.56. The proportion of participants estimated to meet physical activity guidelines showed acceptable reliability (k = 0.60. In the validity study, comparison of survey-reported and accelerometer-derived time spent in physical activity showed strong agreement for vigorous physical activity (r = 0.72, p<0.001, fair but non-significant agreement for moderate physical activity (r = 0.24, p = 0.09 and fair agreement for MVPA (r = 0.27, p = 0.05. Bland

  1. Understanding strategy of nitrate and urea assimilation in a Chinese strain of Aureococcus anophagefferens through RNA-seq analysis.

    Directory of Open Access Journals (Sweden)

    Hong-Po Dong

    Full Text Available Aureococcus anophagefferens is a harmful alga that dominates plankton communities during brown tides in North America, Africa, and Asia. Here, RNA-seq technology was used to profile the transcriptome of a Chinese strain of A. anophagefferens that was grown on urea, nitrate, and a mixture of urea and nitrate, and that was under N-replete, limited and recovery conditions to understand the molecular mechanisms that underlie nitrate and urea utilization. The number of differentially expressed genes between urea-grown and mixture N-grown cells were much less than those between urea-grown and nitrate-grown cells. Compared with nitrate-grown cells, mixture N-grown cells contained much lower levels of transcripts encoding proteins that are involved in nitrate transport and assimilation. Together with profiles of nutrient changes in media, these results suggest that A. anophagefferens primarily feeds on urea instead of nitrate when urea and nitrate co-exist. Furthermore, we noted that transcripts upregulated by nitrate and N-limitation included those encoding proteins involved in amino acid and nucleotide transport, degradation of amides and cyanates, and nitrate assimilation pathway. The data suggest that A. anophagefferens possesses an ability to utilize a variety of dissolved organic nitrogen. Moreover, transcripts for synthesis of proteins, glutamate-derived amino acids, spermines and sterols were upregulated by urea. Transcripts encoding key enzymes that are involved in the ornithine-urea and TCA cycles were differentially regulated by urea and nitrogen concentration, which suggests that the OUC may be linked to the TCA cycle and involved in reallocation of intracellular carbon and nitrogen. These genes regulated by urea may be crucial for the rapid proliferation of A. anophagefferens when urea is provided as the N source.

  2. Safety and Health Perceptions in Work-related Transport Activities in Ghanaian Industries

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    Charles Atombo

    2017-06-01

    Conclusion: OSH culture is not fully complied in industries transport activities. This study, therefore, supports the use of safety seminars and training sessions for industry workers responsible for transport operations for better integration of safety standards.

  3. The urease inhibitor NBPT negatively affects DUR3-mediated uptake and assimilation of urea in maize roots

    Directory of Open Access Journals (Sweden)

    Laura eZanin

    2015-11-01

    Full Text Available Despite the widespread use of urease inhibitors in agriculture, little information is available on their effect on nitrogen uptake and assimilation. Aim of this work was to study, at physiological and transcriptional level, the effects of NBPT on urea nutrition in hydroponically grown maize plants. Presence of NBPT in the nutrient solution limited the capacity of plants to utilize urea as a N-source; this was shown by a decrease in urea uptake rate and 15N accumulation. Noteworthy, these negative effects were evident only when plants were fed with urea, as NBPT did not alter 15N accumulation in nitrate-fed plants. NBPT also impaired the growth of Arabidopsis plants when urea was used as N-source, while having no effect on plants grown with nitrate or ammonium.This response was related, at least in part, to a direct effect of NBPT on the high affinity urea transport system. Impact of NBPT on urea uptake was further evaluated using lines of Arabidopsis overexpressing ZmDUR3 and dur3-knockout; results suggest that not only transport but also urea assimilation could be compromised by the inhibitor. This hypothesis was reinforced by an over-accumulation of urea and a decrease in ammonium concentration in NBPT-treated plants. Furthermore, transcriptional analyses showed that in maize roots NBPT treatment severely impaired the expression of genes involved in the cytosolic pathway of ureic-N assimilation and ammonium transport. NBPT also limited the expression of a gene coding for a transcription factor highly induced by urea and possibly playing a crucial role in the regulation of its acquisition.This work provides evidence that NBPT can heavily interfere with urea nutrition in maize plants, limiting influx as well as the following assimilation pathway.

  4. The Urease Inhibitor NBPT Negatively Affects DUR3-mediated Uptake and Assimilation of Urea in Maize Roots.

    Science.gov (United States)

    Zanin, Laura; Tomasi, Nicola; Zamboni, Anita; Varanini, Zeno; Pinton, Roberto

    2015-01-01

    Despite the widespread use of urease inhibitors in agriculture, little information is available on their effect on nitrogen (N) uptake and assimilation. Aim of this work was to study, at physiological and transcriptional level, the effects of N-(n-butyl) thiophosphoric triamide (NBPT) on urea nutrition in hydroponically grown maize plants. Presence of NBPT in the nutrient solution limited the capacity of plants to utilize urea as a N-source; this was shown by a decrease in urea uptake rate and (15)N accumulation. Noteworthy, these negative effects were evident only when plants were fed with urea, as NBPT did not alter (15)N accumulation in nitrate-fed plants. NBPT also impaired the growth of Arabidopsis plants when urea was used as N-source, while having no effect on plants grown with nitrate or ammonium. This response was related, at least in part, to a direct effect of NBPT on the high affinity urea transport system. Impact of NBPT on urea uptake was further evaluated using lines of Arabidopsis overexpressing ZmDUR3 and dur3-knockout; results suggest that not only transport but also urea assimilation could be compromised by the inhibitor. This hypothesis was reinforced by an over-accumulation of urea and a decrease in ammonium concentration in NBPT-treated plants. Furthermore, transcriptional analyses showed that in maize roots NBPT treatment severely impaired the expression of genes involved in the cytosolic pathway of ureic-N assimilation and ammonium transport. NBPT also limited the expression of a gene coding for a transcription factor highly induced by urea and possibly playing a crucial role in the regulation of its acquisition. This work provides evidence that NBPT can heavily interfere with urea nutrition in maize plants, limiting influx as well as the following assimilation pathway.

  5. Urea-induced Inactivation and Unfolding of Recombinant Phospholipid Hydroperoxide Glutathione Peroxidase from Oryza sativa

    Institute of Scientific and Technical Information of China (English)

    WANG Feng; ZHOU Hui-ping; KONG Bao-hua; FAN Jing-hua; CHEN Hai-ru; LIU Jin-yuan

    2007-01-01

    Phospholipid hydroperoxide glutathione peroxidase is an antioxidant enzyme that has the highest capability of reducing membrane-bound hydroperoxy lipids as compared to free organic and inorganic hydroperoxides amongst the glutathione peroxidases. In this study, urea-induced effects on the inactivation and unfolding of a recombinant phospholipid hydroperoxide glutathione peroxidase(PHGPx) from Oryza sativa were investigated by means of circular dichroism and fluorescence spectroscopy. With the increase of urea concentration, the residual activity of OsPHGPx decreasea correspondingly. When the urea concentration is above 5.0 mol/L, there was no residual activity. In addition,the observed changes in intrinsic tryptophan fluorescence, the binding of the hydrophobic fluorescence probe ANS,and the far UV CD describe a common dependence on the concentration of urea suggesting that the conformational features of the native OsPHGPx are lost in a highly cooperative single transition. The unfolding process comprises of three zones: the native base-line zone between 0 and 2.5 mol/L urea, the transition zone between 2.5 and 5.5 mol/L urea, and the denatured base-line zone above 5.5 mol/L urea. The transition zone has a midpoint at about 4.0 mol/L urea.

  6. 21 CFR 184.1923 - Urea.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Urea. 184.1923 Section 184.1923 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN... Substances Affirmed as GRAS § 184.1923 Urea. (a) Urea (CO(NH2)2, CAS Reg. No. 57-13-6) is the diamide...

  7. Discovery and Optimization of Piperidyl-1,2,3-Triazole Ureas as Potent, Selective, and In Vivo-Active Inhibitors of Alpha/Beta-Hydrolase Domain Containing 6 (ABHD6)

    Science.gov (United States)

    Hsu, Ku-Lung; Tsuboi, Katsunori; Chang, Jae Won; Whitby, Landon R.; Speers, Anna E.; Pugh, Holly; Cravatt, Benjamin F.

    2014-01-01

    Alpha/beta-hydrolase domain containing 6 (ABHD6) is a transmembrane serine hydrolase that hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to regulate certain forms of cannabinoid receptor-dependent signaling in the nervous system. The full spectrum of ABHD6 metabolic activities and functions is currently unknown and would benefit from selective, in vivo-active inhibitors. Here, we report the development and characterization of an advanced series of irreversible (2-substituted)-piperidyl-1,2,3-triazole urea inhibitors of ABHD6, including compounds KT182 and KT203, which show exceptional potency and selectivity in cells (< 5 nM) and, at equivalent doses in mice (1 mg kg-1), served as systemic and peripherally-restricted ABHD6 inhibitors, respectively. We also describe an orally-bioavailable ABHD6 inhibitor KT185 that displays excellent selectivity against other brain and liver serine hydrolases in vivo. We thus describe several chemical probes for biological studies of ABHD6, including brain-penetrant and peripherally-restricted inhibitors that should prove of value for interrogating ABHD6 function in animal models. PMID:24152295

  8. The Influence of Urban Land-Use and Public Transport Facilities on Active Commuting in Wellington, New Zealand: Active Transport Forecasting Using the WILUTE Model

    Directory of Open Access Journals (Sweden)

    Joreintje Dingena Mackenbach

    2016-03-01

    Full Text Available Physical activity has numerous physical and mental health benefits, and active commuting (walking or cycling to work can help meet physical activity recommendations. This study investigated socioeconomic differences in active commuting, and assessed the impact of urban land-use and public transport policies on active commuting in the Wellington region in New Zealand. We combined data from the New Zealand Household Travel Survey and GIS data on land-use and public transport facilities with the Wellington Integrated Land-Use, Transportation and Environment (WILUTE model, and forecasted changes in active commuter trips associated with changes in the built environment. Results indicated high income individuals were more likely to commute actively than individuals on low income. Several land-use and transportation factors were associated with active commuting and results from the modelling showed a potential increase in active commuting following an increase in bus frequency and parking fees. In conclusion, regional level policies stimulating environmental factors that directly or indirectly affect active commuting may be a promising strategy to increase population level physical activity. Access to, and frequency of, public transport in the neighbourhood can act as a facilitator for a more active lifestyle among its residents without negatively affecting disadvantaged groups.

  9. Urea and its formation in coelacanth liver.

    Science.gov (United States)

    Brown, G W; Brown, S G

    1967-02-01

    Urea occurs in liver of the coelacanth Latimeria chalumnae to the extent of about 1.7 percent by weight. It was determined quantitatively by reaction with 1-phenyl-1,2-propanedione-2-oxime (Archibald reagent) and by measurement of ammonia released upon treatment with urease. Arginase and ornithine carbamoyltransferase, enzymes instrumental in the formation of urea in typical ureotelic vertebrates, occur in homogenates of coelacanth liver. Formed in part by the ornithine-urea cycle, urea may have an osmoregulatory function in the coelacanth as it has in elasmobranchs.

  10. 控释尿素与普通尿素配施对水稻氮代谢关键酶活性及产质量的影响%Effects of Combined Application of Controlled Release Urea and Common Urea on Activities of Key Enzymes Related with Nitrogen Metabolism, Yield and Quality of Rice

    Institute of Scientific and Technical Information of China (English)

    杜君; 孙克刚; 雷利君; 和爱玲; 张运红; 孙克振

    2016-01-01

    为了探明控释尿素对提高水稻氮肥利用率和产量、改善水稻品质的作用机制,通过田间试验,研究了控释尿素与普通尿素配施[处理1为对照(不施氮肥,CK),处理2为100%普通尿素,处理3为40%控释尿素+60%普通尿素,处理4为60%控释尿素+40%普通尿素,处理5为100%控释尿素]对水稻氮代谢关键酶活性、氮肥利用率以及产质量的影响。结果表明,与100%普通尿素相比,施用控释尿素能显著提高水稻齐穗期和乳熟期叶片中的硝酸还原酶活性,特别是乳熟期最为明显;总体能显著增强水稻齐穗期和乳熟期叶片谷氨酰胺合成酶活性、齐穗期至蜡熟期谷氨酰胺转化酶活性,其增强效果在齐穗期最为明显;能显著提高乳熟期和蜡熟期叶片的蛋白水解酶活性;总体能显著增强水稻齐穗期至蜡熟期籽粒中的谷氨酰胺合成酶和谷氨酰胺转化酶活性;能显著提高水稻产量及氮肥利用率,提高幅度分别为16.0%~21.4%和30.7%~48.5%;并能显著增加籽粒蛋白质含量。上述指标均以处理4增强效果最为明显。%In oder to verify the mechanism of controlled release urea( CRU) on increasing nitrogen use ef-ficiency, yield and improving rice quality, field experiments were conducted to study the effects of com-bined application of CRU and common urea( CU) on activities of key enzymes related with nitrogen me-tabolism and nitrogen use efficiency as well as yield and quality of rice with four treatments( treatment 1 without nitrogen fertilizer( CK) , treatment 2 with 100%CU,treatment 3 with 40%CRU+60%CU,treat-ment 4 with 60%CRU+40%CU,treatment 5 with 100%CRU) . The results showed that compared with 100%CU, the application of CRU could significantly improve nitrate reductase ( NR) activities of rice leaves at full heading stage and milk stage, especially at milk stage;as a whole, CRU could significantly improve glutamine synthetase activities of rice leaves at full heading

  11. Uterine activity, sperm transport, and the role of boar stimuli around insemination in sows

    NARCIS (Netherlands)

    Langendijk, P.; Soede, N.M.; Kemp, B.

    2005-01-01

    This paper describes changes in spontaneous myometrial activity around estrus, factors that affect myometrial activity, and the possible role of uterine contractions in the process of (artificial) insemination, sperm transport and fertilization. Myometrial activity in the sow increases during estrus

  12. Evaluation of the Physical Activity Biography: Sport and Transport

    Directory of Open Access Journals (Sweden)

    Sandra Rogen

    2014-06-01

    Full Text Available Beside the genetic disposition, physical activity (PA is one of the major health factors and can play a large role in the prevention and therapy of many diseases (cardiovascular diseases, cancer, obesity-related diseases etc.. In contrast to the genetic disposition, PA can be deliberately influenced by lifestyle. Therefore, it is of high importance to assess PA patterns. In order to assess PA reliably and validly, a new questionnaire (Physical Activity Biography, PAB was created. The PAB assesses recreational PA (sport and transport and enables to distinguish between endurance intensity levels and considers strength and high speed activity patterns throughout life. This study aims to evaluate the PAB by means of item analysis, retest-reliability and validity (criteria were physical fitness assessed by the questionnaire FFB-mot and by exercise tests. 141 participants answered the PAB. For deriving retest-reliability, 81 participants completed the PAB after a retest-interval of one month again. 55 participated in exercise tests and answered the FFB-mot to determine construct validity. Retest-reliability (ICC above 0.7 was found for most items. For the items assessing recent PA, the criteria of convergent and discriminant validity were given. Despite the complexity of the question under study, the results fulfilled the expectations concerning reliability and validity. The PAB enables to assess the amount of sport and locomotion a person has accomplished during different life time frames and, because of the protective effects of PA on various diseases, may become an important tool for risk assessment.

  13. Adolescents who engage in active school transport are also more active in other contexts

    DEFF Research Database (Denmark)

    Stewart, Tom; Duncan, Scott; Schipperijn, Jasper

    2017-01-01

    and travel behaviours across time- and space-classified domains. METHODS: A total of 196 adolescents wore a Global Positioning System receiver and an accelerometer for 7 days. All data were classified into one of four domains: home, school, transport, or leisure. Generalized linear mixed models were used......BACKGROUND: Although active school travel (AST) is important for increasing moderate-to-vigorous physical activity (MVPA), it is unclear how AST is related to context-specific physical activity and non-school travel. This study investigated how school travel is related to physical activity...... to compare domain-specific PA and non-school trips between active and passive school travellers. RESULTS: Active travellers accumulated 13 and 14 more min of MVPA on weekdays and weekend days, respectively. They also spent 15min less time in vehicular travel during non-school trips, and accrued an additional...

  14. The Association between Access to Public Transportation and Self-Reported Active Commuting

    Directory of Open Access Journals (Sweden)

    Sune Djurhuus

    2014-12-01

    Full Text Available Active commuting provides routine-based regular physical activity which can reduce the risk of chronic diseases. Using public transportation involves some walking or cycling to a transit stop, transfers and a walk to the end location and users of public transportation have been found to accumulate more moderate physical activity than non-users. Understanding how public transportation characteristics are associated with active transportation is thus important from a public health perspective. This study examines the associations between objective measures of access to public transportation and self-reported active commuting. Self-reported time spent either walking or cycling commuting each day and the distance to workplace were obtained for adults aged 16 to 65 in the Danish National Health Survey 2010 (n = 28,928. Access to public transportation measures were computed by combining GIS-based road network distances from home address to public transit stops an integrating their service level. Multilevel logistic regression was used to examine the association between access to public transportation measures and active commuting. Distance to bus stop, density of bus stops, and number of transport modes were all positively associated with being an active commuter and with meeting recommendations of physical activity. No significant association was found between bus services at the nearest stop and active commuting. The results highlight the importance of including detailed measurements of access to public transit in order to identify the characteristics that facilitate the use of public transportation and active commuting.

  15. BicaudalD actively regulates microtubule motor activity in lipid droplet transport.

    Directory of Open Access Journals (Sweden)

    Kristoffer S Larsen

    Full Text Available BACKGROUND: A great deal of sub-cellular organelle positioning, and essentially all minus-ended organelle transport, depends on cytoplasmic dynein, but how dynein's function is regulated is not well understood. BicD is established to play a critical role in mediating dynein function-loss of BicD results in improperly localized nuclei, mRNA particles, and a dispersed Golgi apparatus-however exactly what BicD's role is remains unknown. Nonetheless, it is widely believed that BicD may act to tether dynein to cargos. Here we use a combination of biophysical and biochemical studies to investigate BicD's role in lipid droplet transport during Drosophila embryogenesis. METHODOLOGY/PRINCIPAL FINDINGS: Functional loss of BicD impairs the embryo's ability to control the net direction of droplet transport; the developmentally controlled reversal in transport is eliminated. We find that minimal BicD expression (near-BicD(null decreases the average run length of both plus and minus end directed microtubule (MT based transport. A point mutation affecting the BicD N-terminus has very similar effects on transport during cellularization (phase II, but in phase III (gastrulation motion actually appears better than in the wild-type. CONCLUSIONS/SIGNIFICANCE: In contrast to a simple static tethering model of BicD function, or a role only in initial dynein recruitment to the cargo, our data uncovers a new dynamic role for BicD in actively regulating transport. Lipid droplets move bi-directionally, and our investigations demonstrate that BicD plays a critical-and temporally changing-role in balancing the relative contributions of plus-end and minus-end motors to control the net direction of transport. Our results suggest that while BicD might contribute to recruitment of dynein to the cargo it is not absolutely required for such dynein localization, and it clearly contributes to regulation, helping activation/inactivation of the motors.

  16. Regulation of dopamine transporter activity by carboxypeptidase E

    Directory of Open Access Journals (Sweden)

    Zhang Heping

    2009-05-01

    Full Text Available Abstract Background The dopamine transporter (DAT plays a critical role in terminating the action of dopamine by rapid reuptake into the presynaptic neuron. Previous studies have revealed that the DAT carboxyl terminus (DAT-CT can directly interact with other cellular proteins and regulate DAT function and trafficking. Results Here, we have identified that carboxypeptidase E (CPE, a prohormone processing exopeptidase and sorting receptor for the regulated secretory pathway, interacts with the DAT-CT and affects DAT function. Mammalian cell lines coexpressing CPE and DAT exhibited increased DAT-mediated dopamine uptake activity compared to cells expressing DAT alone. Moreover, coexpression of an interfering DAT-CT minigene inhibited the effects of CPE on DAT. Functional changes caused by CPE could be attributed to enhanced DAT expression and subsequent increase in DAT cell surface localization, due to decreased DAT degradation. In addition, CPE association could reduce the phosphorylation state of DAT on serine residues, potentially leading to reduced internalization, thus stabilizing plasmalemmal DAT localization. Conclusion Taken together, our results reveal a novel role for CPE in the regulation of DAT trafficking and DAT-mediated DA uptake, which may provide a novel target in the treatment of dopamine-governed diseases such as drug addiction and obesity.

  17. Crystal structure, spectral property, antimicrobial activity and DFT calculation of N-(coumarin-3-yl)-N‧-(2-amino-5-phenyl-1,3,4-thiadiazol-2-yl) urea

    Science.gov (United States)

    Zhang, Hong-Song; Zhang, Kong-Yan; Chen, Li-Chuan; Li, Yao-Xin; Chai, Lan-Qin

    2017-10-01

    N-(coumarin-3-yl)-N‧-(2-amino-5-phenyl-1,3,4-thiadiazol-2-yl) urea was synthesized and characterized by elemental analysis, IR, 1H NMR, 13C NMR, UV-Vis and emission spectroscopy, as well as by single-crystal X-ray diffraction. X-ray crystallographic analyses have indicated that the crystal structure consists of two dimethyl sulfoxide (DMSO) solvent molecules and the structural geometry of DMSO is a trigonal pyramid in shape. In the crystal structure, a self-assembling two-dimensional (2-D) layer supramolecular architecture is formed through intermolecular hydrogen bonds, Cdbnd O···π (thiadiazole ring) and π···π stacking interactions. The geometry of the compound has been optimized by the DFT method and the results are compared with the X-ray diffraction data. The electronic transitions and spectral features of the compound were carried out by using DFT/B3LYP method. In addition, the antimicrobial activity was also studied, and the highest occupied molecular orbital (HOMO), lowest unoccupied molecular orbital (LUMO), and HOMO-LUMO gap were also calculated.

  18. Lamprey parasitism of sharks and teleosts: high capacity urea excretion in an extant vertebrate relic.

    Science.gov (United States)

    Wilkie, Michael P; Turnbull, Steven; Bird, Jonathan; Wang, Yuxiang S; Claude, Jaime F; Youson, John H

    2004-08-01

    We observed 10 sea lampreys (Petromyzon marinus) parasitizing basking sharks (Cetorhinus maximus), the world's second largest fish, in the Bay of Fundy. Due to the high concentrations of urea in the blood and tissues of ureosmotic elasmobranchs, we hypothesized that sea lampreys would have mechanisms to eliminate co-ingested urea while feeding on basking sharks. Post-removal urea excretion rates (J(Urea)) in two lampreys, removed from separate sharks by divers, were initially 450 ( approximately 9000 micromol N kg-1 h-1) and 75 times ( approximately 1500 micromol N kg-1 h-1) greater than basal (non-feeding) rates ( approximately 20 micromol N kg-1 h-1). In contrast, J(Urea) increased by 15-fold after parasitic lampreys were removed from non-ureosmotic rainbow trout (Oncorhynchus mykiss). Since activities of the ornithine urea cycle (OUC) enzymes, carbamoyl phosphate synthetase III (CPSase III) and ornithine carbamoyl transferase (OCT) were relatively low in liver and below detection in intestine and muscle, it is unlikely that the excreted urea arose from de novo urea synthesis. Measurements of arginase activity suggested that hydrolysis of dietary arginine made a minor contribution to J(Urea.). Post-feeding ammonia excretion rates (J(Amm)) were 15- to 25-fold greater than basal rates in lampreys removed from both basking sharks and rainbow trout, suggesting that parasitic lampreys have a high capacity to deaminate amino acids. We conclude that the sea lamprey's ability to penetrate the dermal denticle armor of sharks, to rapidly excrete large volumes of urea and a high capacity to deaminate amino acids, represent adaptations that have contributed to the evolutionary success of these phylogenetically ancient vertebrates.

  19. Phosphorylation regulates NCC stability and transporter activity in vivo.

    Science.gov (United States)

    Yang, Sung-Sen; Fang, Yu-Wei; Tseng, Min-Hua; Chu, Pei-Yi; Yu, I-Shing; Wu, Han-Chung; Lin, Shu-Wha; Chau, Tom; Uchida, Shinichi; Sasaki, Sei; Lin, Yuh-Feng; Sytwu, Huey-Kang; Lin, Shih-Hua

    2013-10-01

    A T60M mutation in the thiazide-sensitive sodium chloride cotransporter (NCC) is common in patients with Gitelman's syndrome (GS). This mutation prevents Ste20-related proline and alanine-rich kinase (SPAK)/oxidative stress responsive kinase-1 (OSR1)-mediated phosphorylation of NCC and alters NCC transporter activity in vitro. Here, we examined the physiologic effects of NCC phosphorylation in vivo using a novel Ncc T58M (human T60M) knock-in mouse model. Ncc(T58M/T58M) mice exhibited typical features of GS with a blunted response to thiazide diuretics. Despite expressing normal levels of Ncc mRNA, these mice had lower levels of total Ncc and p-Ncc protein that did not change with a low-salt diet that increased p-Spak. In contrast to wild-type Ncc, which localized to the apical membrane of distal convoluted tubule cells, T58M Ncc localized primarily to the cytosolic region and caused an increase in late distal convoluted tubule volume. In MDCK cells, exogenous expression of phosphorylation-defective NCC mutants reduced total protein expression levels and membrane stability. Furthermore, our analysis found diminished total urine NCC excretion in a cohort of GS patients with homozygous NCC T60M mutations. When Wnk4(D561A/+) mice, a model of pseudohypoaldosteronism type II expressing an activated Spak/Osr1-Ncc, were crossed with Ncc(T58M/T58M) mice, total Ncc and p-Ncc protein levels decreased and the GS phenotype persisted over the hypertensive phenotype. Overall, these data suggest that SPAK-mediated phosphorylation of NCC at T60 regulates NCC stability and function, and defective phosphorylation at this residue corrects the phenotype of pseudohypoaldosteronism type II.

  20. Individual, Social, and Environmental Correlates of Active Transportation Patterns in French Women

    Directory of Open Access Journals (Sweden)

    Camille Perchoux

    2017-01-01

    Full Text Available The objectives were (1 to define physical activity (PA and sedentary behaviors (SB patterns in daily life contexts (work, leisure, and transportation in French working women from NutriNet-Santé web-cohort and (2 to identify pattern(s of active transportation and their individual, social, and environmental correlates. 23,432 participants completed two questionnaires to evaluate PA and SB in daily life contexts and individual representations of residential neighborhood and transportation modes. Hierarchical cluster analysis was performed which identified 6 distinct movement behavior patterns: (i active occupation, high sedentary leisure, (ii sedentary occupation, low leisure, (iii sedentary transportation, (iv sedentary occupation and leisure, (v active transportation, and (vi active leisure. Multinomial logistic regressions were performed to identify correlates of the “active transportation” cluster. The perceived environmental characteristics positively associated with “active transportation” included “high availability of destinations around home,” “presence of bicycle paths,” and “low traffic.” A “positive image of walking/cycling,” the “individual feeling of being physically active,” and a “high use of active transport modes by relatives/friends” were positively related to “active transportation,” identified as a unique pattern regarding individual and environmental correlates. Identification of PA and SB context-specific patterns will help to understand movement behaviors’ complexity and to design interventions to promote active transportation in specific subgroups.

  1. 1-ethyl-3-(6-methylphenanthridine-8-il) urea modulates TLR3/9 activation and induces selective pro-inflammatory cytokine expression in vitro.

    Science.gov (United States)

    Teofilović, Natalija Knežević; Bihi, Mahjoub; Stojković, Marijana Radić; Tumir, Lidija M; Ester, Katja; Kralj, Marijeta; Majhen, Dragomira; Oršolić, Nada; Lepur, Adriana; Vrbanec, Damir; Markotić, Alemka; Dembić, Zlatko; Weber, Alexander N R; Piantanida, Ivo; Vugrek, Oliver; Diken, Mustafa; Knežević, Jelena

    2017-04-01

    We have previously demonstrated the nucleic acid binding capacity of phenanthridine derivatives (PHTs). Because nucleic acids are potent inducers of innate immune response through Toll-like receptors (TLRs), and because PTHs bear a structural resemblance to commonly used synthetic ligands for TLR7/8, we hypothesized that PHTs could modulate/activate immune response. We found that compound M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs and inhibits TLR3/9 activation in different cellular systems (PBMCs, HEK293 and THP-1 cell lines). Copyright © 2017 Elsevier Ltd. All rights reserved.

  2. Urea synthesis in patients with chronic pancreatitis

    DEFF Research Database (Denmark)

    Hamberg, Ole; Sonne, J; Larsen, S

    2001-01-01

    Up-regulation of urea synthesis by amino acids and dietary protein intake may be impaired in patients with chronic pancreatitis (CP) due to the reduced glucagon secretion. Conversely, urea synthesis may be increased as a result of the chronic inflammation. The aims of the study were to determine...

  3. Evaluation of Urea-motility-indole medium for recognition and differentiation of Salmonella and Shigella species in stool cultures.

    OpenAIRE

    Rosa Fraile, M; Vega Aleman, D; Fernandez Gutierrez, C

    1980-01-01

    A semisolid urea-motility-indole medium designed for detection in Enterobacteriaceae of urease activity, motility, and indole production in one tube was prepared and evaluated. The formulation of the medium was similar to that of Christensen urea agar, but the agar concentration was 0.2%, and 1% tryptone was added. Results with 687 strains of Enterobacteriaceae were the same as those obtained with standard test media (98% overall agreement). The urea-motility-indole medium was also used in co...

  4. Urea degradation rates by size-fractionated plankton populations in a temperate estuary

    Science.gov (United States)

    Savidge, G.; Johnston, J. P.

    1987-04-01

    The distribution of the rates of remineralisation and assimilation of labelled urea by bacteria was determined in a temperate estuary in winter and related to the activities of planktonic populations separated by filtration into a large fraction (LF > 3 μm) and small fractions (SF urea concentrations, whereas corresponding relationships between the LF in situ and urea concentrations were inconsistent. A series of comparable artificial dilution experiments demonstrated consistent effects of salinity on rates of urea remineralisation with opposing relationships observed for the LF and SF. However interpretation of the data obtained from the in situ samples in relation to those obtained experimentally indicated only minimal control of the in situ rates of urea remineralisation by salinity, thus confirming the greater influence on these rates of the ambient urea concentrations. Remineralisation activity was approximately an order of magnitude greater than the assimilation activity with no clear trends being shown between assimilation rates and environmental variables. Highest ambient concentrations of urea were consistently recorded adjacent to the freshwater inflow.

  5. Reduction in slow intercompartmental clearance of urea during dialysis

    Energy Technology Data Exchange (ETDEWEB)

    Bowsher, D.J.; Krejcie, T.C.; Avram, M.J.; Chow, M.J.; Del Greco, F.; Atkinson, A.J. Jr.

    1985-04-01

    The kinetics of urea and inulin were analyzed in five anesthetized dogs during sequential 2-hour periods before, during, and after hemodialysis. The distribution of both compounds after simultaneous intravenous injection was characterized by three-compartment models, and the total volumes of urea (0.66 +/- 0.05 L/kg) and inulin (0.19 +/- 0.01 L/kg) distribution were similar to expected values for total body water and extravascular space, respectively. Intercompartmental clearances calculated before dialysis were used to estimate blood flows to the fast and slow equilibrating compartments. In agreement with previous results, the sum of these flows was similar to cardiac output, averaging 101% of cardiac output measured before dialysis (range 72% to 135%). Dialysis was accompanied by reductions in the slow intercompartmental clearances of urea (81%) and inulin (47%), which reflected a 90% attenuation in blood flow supplying the slow equilibrating compartments. This was estimated to result in a 10% average reduction in the efficiency with which urea was removed by dialysis (range 2.0% to 16.4%). Mean arterial pressure fell by less than 5% during dialysis, but total peripheral resistance increased by 47% and cardiac output fell by 35%. In the postdialysis period, total peripheral resistance and cardiac output returned toward predialysis values, but blood flow to the slow equilibrating peripheral compartment was still reduced by 80%. These changes parallel activation of the renin-angiotensin system, but further studies are required to establish causality.

  6. Transcriptomic analysis highlights reciprocal interactions of urea and nitrate for nitrogen acquisition by maize roots.

    Science.gov (United States)

    Zanin, Laura; Zamboni, Anita; Monte, Rossella; Tomasi, Nicola; Varanini, Zeno; Cesco, Stefano; Pinton, Roberto

    2015-03-01

    Even though urea and nitrate are the two major nitrogen (N) forms applied as fertilizers in agriculture and occur concomitantly in soils, the reciprocal influence of these two N sources on the mechanisms of their acquisition are poorly understood. Therefore, molecular and physiological aspects of urea and nitrate uptake were investigated in maize (Zea mays), a crop plant consuming high amounts of N. In roots, urea uptake was stimulated by the presence of urea in the external solution, indicating the presence of an inducible transport system. On the other hand, the presence of nitrate depressed the induction of urea uptake and, at the same time, the induction of nitrate uptake was depressed by the presence of urea. The expression of about 60,000 transcripts of maize in roots was monitored by microarray analyses and the transcriptional patterns of those genes involved in nitrogen acquisition were analyzed by real-time reverse transcription-PCR (RT-PCR). In comparison with the treatment without added N, the exposure of maize roots to urea modulated the expression of only very few genes, such as asparagine synthase. On the other hand, the concomitant presence of urea and nitrate enhanced the overexpression of genes involved in nitrate transport (NRT2) and assimilation (nitrate and nitrite reductase, glutamine synthetase 2), and a specific response of 41 transcripts was determined, including glutamine synthetase 1-5, glutamine oxoglutarate aminotransferase, shikimate kinase and arogenate dehydrogenase. Also based on the real-time RT-PCR analysis, the transcriptional modulation induced by both sources might determine an increase in N metabolism promoting a more efficient assimilation of the N that is taken up.

  7. Urea Synthesis Plant - Process Water Treatment

    Directory of Open Access Journals (Sweden)

    Matijašević, Lj.

    2007-09-01

    Full Text Available After the years of operation of Petrokemija d. d. from Kutina it has been recognized that the technology of urea production can be improved at several points, including wastewater treatment.The wastewater treatment area is a part of the urea plant, Urea 2 of Petrokemija d. d., Kutina. The plant has been in operation since 1983 based on the licensed Stamicarbon CO2 stripping process. So far there have been no major process improvements in terms of utility savings. This part of the plant releases into the environment almost 800 t per day of superfluous wastewater polluted with small, however significant, amounts of urea and ammonium. As such, this wastewater cannot be used in any other segment of urea production. The aim of this paper is to improve the current process from the economical and ecological point of view with ultimate goal of implementing the results obtained.

  8. A double-blind comparison of two creams containing urea as the active ingredient. Assessment of efficacy and side-effects by non-invasive techniques and a clinical scoring scheme.

    Science.gov (United States)

    Serup, J

    1992-01-01

    From a group of 72 healthy individuals, 47 with evidence of dry skin according to measurements by non-invasive techniques were enrolled for a 3-week study with double-blind and randomized treatment of one forearm, using either 3% urea cream (HTH lotion 'light') or 10% urea cream (HTH lotion 'Original'). The contralateral forearm served as an untreated control. Two volunteers had to be excluded because measurements of skin surface lipids gave evidence of vehicle components on the skin surface at the time of final evaluations. Evaluations took place not less than 12 h after the last application. According to questionnaire replies, the two creams were equally effective. This was confirmed by "blind" evaluation of the skin hydration state by a dermatologist, measurements of electrical capacitance and conductance indicating epidermal and skin surface hydration, and by D-Squame tape assessments including optical transmission of tapes with stratum corneum and scales from adhering skin, as well as visual scoring of the tapes. The methods showed a high degree of correlation, i.a. a definite relation between increase in electrical hydration parameters, reduced scaling according to the D-Squame tape evaluations, and clinical improvement of dryness. In skin treated with 10% urea cream the transepidermal water loss (TEWL) decreased, indicating an improved water barrier function. Skin colour measurement according to the CIE colour system showed that skin treated with the 3% urea cream turned in the direction of yellow, and there was generally a tendency for the brightness to decrease. Thus, the 3% urea cream gave the skin a more golden colour. There was no change in redness with any of the creams. Neither data from the questionnaire, the clinical examination, nor results of TEWL and colour measurements indicated any local irritant effect of urea causing water barrier damage or inflammation. In conclusion, the 3% and 10% urea creams were both found efficient, resulting in

  9. Effects of surfactants and thermodynamic activity of model active ingredient on transport over plant leaf cuticle.

    Science.gov (United States)

    Fagerström, Anton; Kocherbitov, Vitaly; Ruzgas, Tautgirdas; Westbye, Peter; Bergström, Karin; Engblom, Johan

    2013-03-01

    The main objective of this study was to investigate the mechanism of molecular transport across the cuticle of Clivia leaves. In vitro diffusion methodology was used to investigate the transport of a systemic fungicide, tebuconazole, over a model silicone membrane, enzymatically isolated cuticle membranes, and dermatomed leaves. It was shown that dermatomed leaves may replace enzymatically isolated cuticles. Furthermore, the effects of two surfactants, C(10)EO(7) and C(8)G(1.6), on the fungicide transport were investigated. Tebuconazole cuticle permeation was described using Fick's first law of diffusion, expressed by the thermodynamic activity of the solute in the membrane. A new method for calculation of diffusion coefficients in the membrane is proposed. To access the thermodynamic activity of the fungicide in the membranes, sorption isotherms of tebuconazole in the membrane materials studied were recorded. The thermodynamic activity of the fungicide in aqueous solutions was calculated from solubility data. For that purpose, the effect of surfactants on tebuconazole solubility was studied. The results show that addition of surfactants allows for higher concentrations of tebuconazole available for penetration. Nonetheless, at a fixed fungicide thermodynamic activity, all formulations produced the same flux over the silicone membrane independently on the fungicide concentration. This shows that the driving force across non-responding membranes is the gradient of thermodynamic activity, rather than the gradient of the fungicide concentration. In case of leaves, surfactants induced the same quantitative increase in both flux and diffusion coefficient of solute in the cuticle, while the cuticle-water partition coefficient was unaffected.

  10. Socioeconomic and regional differences in active transportation in Brazil.

    Science.gov (United States)

    Sá, Thiago Hérick de; Pereira, Rafael Henrique Moraes; Duran, Ana Clara; Monteiro, Carlos Augusto

    2016-06-27

    To present national estimates regarding walking or cycling for commuting in Brazil and in 10 metropolitan regions. By using data from the Health section of 2008's Pesquisa Nacional por Amostra de Domicílio (Brazil's National Household Sample Survey), we estimated how often employed people walk or cycle to work, disaggregating our results by sex, age range, education level, household monthly income per capita, urban or rural address, metropolitan regions, and macro-regions in Brazil. Furthermore, we estimated the distribution of this same frequency according to quintiles of household monthly income per capita in each metropolitan region of the country. A third of the employed men and women walk or cycle from home to work in Brazil. For both sexes, this share decreases as income and education levels rise, and it is higher among younger individuals, especially among those living in rural areas and in the Northeast region of the country. Depending on the metropolitan region, the practice of active transportation is two to five times more frequent among low-income individuals than among high-income individuals. Walking or cycling to work in Brazil is most frequent among low-income individuals and the ones living in less economically developed areas. Active transportation evaluation in Brazil provides important information for public health and urban mobility policy-making. Apresentar estimativas nacionais sobre o deslocamento a pé ou de bicicleta no trajeto casa-trabalho no Brasil e em 10 de suas regiões metropolitanas. Utilizando dados do Suplemento sobre Saúde da Pesquisa Nacional por Amostra de Domicílios de 2008, estimamos a frequência de pessoas empregadas que se deslocam a pé ou de bicicleta no trajeto casa-trabalho estratificada por sexo, e segundo faixa etária, escolaridade, renda domiciliar per capita, residência em área urbana ou rural, regiões metropolitanas e macrorregiões do país. Adicionalmente, estimamos a distribuição da mesma frequ

  11. Pyridine-3-carboxamide-6-yl-ureas as novel inhibitors of bacterial DNA gyrase: structure based design, synthesis, SAR and antimicrobial activity.

    Science.gov (United States)

    Yule, Ian A; Czaplewski, Lloyd G; Pommier, Stephanie; Davies, David T; Narramore, Sarah K; Fishwick, Colin W G

    2014-10-30

    The development of antibacterial drugs based on novel chemotypes is essential to the future management of serious drug resistant infections. We herein report the design, synthesis and SAR of a novel series of N-ethylurea inhibitors based on a pyridine-3-carboxamide scaffold targeting the ATPase sub-unit of DNA gyrase. Consideration of structural aspects of the GyrB ATPase site has aided the development of this series resulting in derivatives that demonstrate excellent enzyme inhibitory activity coupled to potent Gram positive antibacterial efficacy.

  12. Ammonia volatilization from coated urea forms

    Directory of Open Access Journals (Sweden)

    Carlos Antonio Costa do Nascimento

    2013-08-01

    Full Text Available Nitrogen fertilization is a major component of the cost of agricultural production, due to the high cost and low efficiency of fertilizers. In the case of urea, the low efficiency is mainly due to losses by volatilization, which are more pronounced in cultivation systems in which plant residues are left on the soil. The objective of this work was to compare the influence of urea coated with sulfur or boric acid and copper sulfate with conventional N fertilizers on N volatilization losses in sugar cane harvested after stubble burning. The sources urea, sulfur-coated urea, urea coated with boric acid and copper sulfate, as well as nitrate and ammonium sulfate, were tested at amounts containing N rates of 120 kg ha-1 N. The integration of new technologies in urea fertilization can reduce N losses by volatilization. These losses were most reduced when using nitrate and ammonium sulfate. The application of a readily acidified substance (boric acid to urea was more efficient in reducing volatilization losses and nutrient removal by sugar cane than that of a substance with gradual acidification (elemental sulfur.

  13. What Moves Them? Active Transport among Inhabitants of Dutch Deprived Districts

    Directory of Open Access Journals (Sweden)

    Carla Saris

    2013-01-01

    Full Text Available Background. Active modes of transport like walking and cycling have been shown to be valuable contributions to daily physical activity. The current study investigates associations between personal and neighbourhood environmental characteristics and active transport among inhabitants of Dutch deprived districts. Method. Questionnaires about health, neighbourhoods, and physical activity behaviour were completed by 742 adults. Data was analysed by means of multivariate linear regression analyses. Results. Being younger, female, and migrant and having a normal weight were associated with more walking for active transport. Being younger, male, and native Dutch and having a normal weight were associated with more cycling for active transport. Neighbourhood characteristics were generally not correlated with active transport. Stratified analyses, based on significant person-environment interactions, showed that migrants and women walked more when cars did not exceed maximum speed in nearby streets and that younger people walked more when speed of traffic in nearby streets was perceived as low. Among migrants, more cycling was associated with the perceived attractiveness of the neighbourhood surroundings. Discussion and Conclusion. Results indicated that among inhabitants of Dutch deprived districts, personal characteristics were associated with active transport, whereas neighbourhood environmental characteristics were generally not associated with active transport. Nevertheless, interaction effects showed differences among subgroups that should be considered in intervention development.

  14. Antibacterial kaolinite/urea/chlorhexidine nanocomposites: Experiment and molecular modelling

    Energy Technology Data Exchange (ETDEWEB)

    Holešová, Sylva, E-mail: sylva.holesova@vsb.cz [Nanotechnology Centre, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); IT4Innovations Centre of Excellence, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); Valášková, Marta; Hlaváč, Dominik [Nanotechnology Centre, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); IT4Innovations Centre of Excellence, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); Madejová, Jana [Institute of Inorganic Chemistry, SAS, Dúbravská cesta 9, SK-845 36 Bratislava (Slovakia); Samlíková, Magda; Tokarský, Jonáš [Nanotechnology Centre, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); IT4Innovations Centre of Excellence, VŠB – Technical University of Ostrava, 17.listopadu 15/2172, CZ-708 33 Ostrava, Poruba (Czech Republic); Pazdziora, Erich [Institute of Public Health Ostrava, Centre of Clinical Laboratories, Partyzánské náměstí 7, CZ-702 00 Ostrava (Czech Republic)

    2014-06-01

    Clay minerals are commonly used materials in pharmaceutical production both as inorganic carriers or active agents. The purpose of this study is the preparation and characterization of clay/antibacterial drug hybrids which can be further included in drug delivery systems for treatment oral infections. Novel nanocomposites with antibacterial properties were successfully prepared by ion exchange reaction from two types of kaolinite/urea intercalates and chlorhexidine diacetate. Intercalation compounds of kaolinite were prepared by reaction with solid urea in the absence of solvents (dry method) as well as with urea aqueous solution (wet method). The antibacterial activity of two prepared samples against Enterococcus faecalis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa was evaluated by finding the minimum inhibitory concentration (MIC). Antibacterial studies of both samples showed the lowest MIC values (0.01%, w/v) after 1 day against E. faecalis, E. coli and S. aureus. A slightly worse antibacterial activity was observed against P. aeruginosa (MIC 0.12%, w/v) after 1 day. Since samples showed very good antibacterial activity, especially after 1 day of action, this means that these samples can be used as long-acting antibacterial materials. Prepared samples were characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The experimental data are supported by results of molecular modelling.

  15. Antibacterial kaolinite/urea/chlorhexidine nanocomposites: Experiment and molecular modelling

    Science.gov (United States)

    Holešová, Sylva; Valášková, Marta; Hlaváč, Dominik; Madejová, Jana; Samlíková, Magda; Tokarský, Jonáš; Pazdziora, Erich

    2014-06-01

    Clay minerals are commonly used materials in pharmaceutical production both as inorganic carriers or active agents. The purpose of this study is the preparation and characterization of clay/antibacterial drug hybrids which can be further included in drug delivery systems for treatment oral infections. Novel nanocomposites with antibacterial properties were successfully prepared by ion exchange reaction from two types of kaolinite/urea intercalates and chlorhexidine diacetate. Intercalation compounds of kaolinite were prepared by reaction with solid urea in the absence of solvents (dry method) as well as with urea aqueous solution (wet method). The antibacterial activity of two prepared samples against Enterococcus faecalis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa was evaluated by finding the minimum inhibitory concentration (MIC). Antibacterial studies of both samples showed the lowest MIC values (0.01%, w/v) after 1 day against E. faecalis, E. coli and S. aureus. A slightly worse antibacterial activity was observed against P. aeruginosa (MIC 0.12%, w/v) after 1 day. Since samples showed very good antibacterial activity, especially after 1 day of action, this means that these samples can be used as long-acting antibacterial materials. Prepared samples were characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The experimental data are supported by results of molecular modelling.

  16. Urea-containing peptide boronic acids as potent proteasome inhibitors.

    Science.gov (United States)

    Han, Li-Qiang; Yuan, Xia; Wu, Xing-Yu; Li, Ri-Dong; Xu, Bo; Cheng, Qing; Liu, Zhen-Ming; Zhou, Tian-Yan; An, Hao-Yun; Wang, Xin; Cheng, Tie-Ming; Ge, Ze-Mei; Cui, Jing-Rong; Li, Run-Tao

    2017-01-05

    A novel class of urea-containing peptide boronic acids as proteasome inhibitors was designed by introducing a urea scaffold to replace an amido bond. Compounds were synthesized and their antitumor activities were evaluated. After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor. Compared with Bortezomib, I-14 showed higher potency against the chymotrypsin-like activity of human 20S proteasome (IC50 < 1 pM), similar potency against four different cancer cell lines (IC50 < 10 nM), and better pharmacokinetic profile. Furthermore, I-14 significantly inhibited tumor growth in Bel7404 mouse xenograft model. The excellent proteasome inhibition by I-14 was rationalized through docking and molecular dynamics studies. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  17. Glutamate transporter activity promotes enhanced Na+/K+-ATPase-mediated extracellular K+ management during neuronal activity

    DEFF Research Database (Denmark)

    Larsen, Brian Roland; Holm, Rikke; Vilsen, Bente;

    2016-01-01

    , in addition, Na+/K+-ATPase-mediated K+ clearance could be governed by astrocytic [Na+]i. During most neuronal activity, glutamate is released in the synaptic cleft and is re-absorbed by astrocytic Na+-coupled glutamate transporters, thereby elevating [Na+]i. It thus remains unresolved whether the different Na...... constellations in Xenopus oocytes and determined their apparent Na+ affinity in intact oocytes and isolated membranes. The Na+/K+-ATPase was not fully saturated at basal astrocytic [Na+]i, irrespective of isoform constellation, although the β1 subunit conferred lower apparent Na+ affinity to the α1 and α2...

  18. The Association between Access to Public Transportation and Self-Reported Active Commuting

    DEFF Research Database (Denmark)

    Djurhuus, Sune; Hansen, Henning S; Aadahl, Mette

    2014-01-01

    more moderate physical activity than non-users. Understanding how public transportation characteristics are associated with active transportation is thus important from a public health perspective. This study examines the associations between objective measures of access to public transportation...... and self-reported active commuting. Self-reported time spent either walking or cycling commuting each day and the distance to workplace were obtained for adults aged 16 to 65 in the Danish National Health Survey 2010 (n = 28,928). Access to public transportation measures were computed by combining GIS......-based road network distances from home address to public transit stops an integrating their service level. Multilevel logistic regression was used to examine the association between access to public transportation measures and active commuting. Distance to bus stop, density of bus stops, and number...

  19. [Degradation of urea and ethyl carbamate in Chinese Rice wine by recombinant acid urease].

    Science.gov (United States)

    Zhou, Jianli; Kang, Zhen; Liu, Qingtao; Du, Guocheng; Chen, Jian

    2016-01-01

    Ethyl carbamate (EC) as a potential carcinogen commonly exists in traditional fermented foods. It is important eliminate urea that is the precursors of EC in many fermented foods, including Chinese Rice wine. On the basis of achieving high-level overexpression of food-grade ethanol-resistant acid urease, we studied the hydrolysis of urea and EC with the recombinant acid urease. Recombinant acid urease showed degraded urea in both the simulated system with ethanol and Chinese Rice wine (60 mg/L of urea was completely degraded within 25 h), indicating that the recombinant enzyme is suitable for the elimination of urea in Chinese Rice wine. Although recombinant acid urease also has degradation catalytic activity on EC, no obvious degradation of EC was observed. Further investigation results showed that the Km value for urea and EC of the recombinant acid urease was 0.7147 mmol/L and 41.32 mmol/L, respectively. The results provided theoretical foundation for realizing simultaneous degradation of urea and EC.

  20. Release Kinetics of Urea from Polymer Coated Urea and Its Relationship with Coating Penetrability

    Institute of Scientific and Technical Information of China (English)

    ZHANG Hai-jun; WU Zhi-jie; CHEN Li-jun; LIANG Wen-ju

    2003-01-01

    Four kinds of polymer coated urea (PCU) were put in distilled water at 30C to determine the variation of coating penetrability and give a precise description of the urea release kinetics. The urea release from PCU could be divided into four stages: lag stage, swell stage, steady stage and decay stage. The release rate coefficient K, a measure of coating penetrability, was linearly increased at swell stage, but almost not variable at steady stage. At decay stage, the relation of K to time t could be described by the equation K= mtn-1(where m and n are the coefficients). When n>1, the coating penetrability was gradually increased, and the urea release from PCU was accelerated; when n=1, the coating penetrability was steady, and the urea release from PCU obeyed the first-order kinetics; and when n<1, the coating penetrability was gradually decreased,and the urea release from PCU was delayed, resulting in a significant "tailing effect".

  1. Urea and deuterium mixtures at high pressures

    Energy Technology Data Exchange (ETDEWEB)

    Donnelly, M., E-mail: m.donnelly-2@sms.ed.ac.uk; Husband, R. J.; Frantzana, A. D.; Loveday, J. S. [Centre for Science at Extreme Conditions and School of Physics and Astronomy, The University of Edinburgh, Erskine Williamson Building, Peter Guthrie Tait Road, The King’s Buildings, Edinburgh EH9 3FD (United Kingdom); Bull, C. L. [ISIS, Rutherford Appleton Laboratory, Oxford Harwell, Didcot OX11 0QX (United Kingdom); Klotz, S. [IMPMC, CNRS UMR 7590, Université P and M Curie, 4 Place Jussieu, 75252 Paris (France)

    2015-03-28

    Urea, like many network forming compounds, has long been known to form inclusion (guest-host) compounds. Unlike other network formers like water, urea is not known to form such inclusion compounds with simple molecules like hydrogen. Such compounds if they existed would be of interest both for the fundamental insight they provide into molecular bonding and as potential gas storage systems. Urea has been proposed as a potential hydrogen storage material [T. A. Strobel et al., Chem. Phys. Lett. 478, 97 (2009)]. Here, we report the results of high-pressure neutron diffraction studies of urea and D{sub 2} mixtures that indicate no inclusion compound forms up to 3.7 GPa.

  2. Surface modified silicon nanochannel for urea sensing

    CERN Document Server

    Chen, Yu; Hong, Mi; Erramilli, Shyamsunder; Mohanty, Pritiraj

    2008-01-01

    Silicon nanowires have been surface functionalized with the enzyme urease for biosensor applications to detect and quantify urea concentration. The device is nanofabricated from a silicon on insulator (SOI) wafer with a top down lithography approach. The differential conductance of silicon nanowires can be tuned for optimum performance using the source drain bias voltage, and is sensitive to urea at low concentration. The experimental results show a linear relationship between surface potential change and urea concentration in the range of 0.1 to 0.68 mM. The sensitivity of our devices shows high reproducibility with time and different measurement conditions. The nanowire urea biosensor offers the possibility of high quality, reusable enzyme sensor array integration with silicon based circuits.

  3. High nonlinear optical anisotropy of urea nanofibers

    Science.gov (United States)

    Isakov, D.; de Matos Gomes, E.; Belsley, M.; Almeida, B.; Martins, A.; Neves, N.; Reis, R.

    2010-07-01

    Nanofibers consisting of the optically nonlinear organic molecule urea embedded in both poly(ethylene oxide) (PEO) and poly(vinyl alcohol) (PVA) polymers were produced by the electrospinning technique. The second-harmonic generation produced by aligned fiber mats of these materials displays a strong dependence on the polarization of the incident light. In PVA-urea nanofibers the effectiveness in generating of the second-harmonic light is as high as that of a pure urea powder with an average grain size of 110 μm. The results suggest that single crystalline urea nanofibers were achieved with a long-range crystalline order extending into the range of 2-4 μm with PVA as the host polymer.

  4. Green urea synthesis catalyzed by hematite nanowires in magnetic field

    Science.gov (United States)

    Yahya, Noorhana; Qureshi, Saima; Rehman, Zia ur; Alqasem, Bilal; Fai Kait, Chong

    2017-04-01

    The catalytic activity of hematite (α-Fe2O3) nanowires under the influence of magnetic field on urea synthesis is considered green. The adsorption and subsequent dissociative reaction of hydrogen, nitrogen and carbon dioxide gases on the α-Fe2O3 (111) nanowires were investigated using the density functional theory (DFT) method. The average adsorption energy is -4.12 kcal/mole at different sites. The adsorption of gases resulted in a difference in density and net spin of electrons from 68 to 120 and 0-21 respectively. In addition, it induces magnetic moment value of 36.33 μB, which confirms the enhanced magnetic behaviour of hematite. α-Fe2O3 nanowires (NWs) synthesized by heating iron wire in a box furnace at (750-800) °C and as synthesized α-Fe2O3 nanoparticles (NPs) were received to use as a catalyst in the magnetic reaction of urea synthesis. X-ray Diffractometer (XRD) confirms the peaks of rhombohedral structure of α-Fe2O3 and Raman spectrum analyses confirms the α-Fe2O3 peaks at 410 cm-1, 500 cm-1 and 616 cm-1. The needle-like shape of hematite nanowires with length ranging from 16-25) μm and diameter from 74 to 145 nm confirmed by Field emission scanning electron microscopy (FESEM). The magnetic properties of the nanowires exhibited different levels of saturation magnetization, for α-Fe2O3 perpendicularly aligned direction (13.18 emu/g) and random direction (10.73 emu/g). Urea synthesis was done under magnetic field ranges from 0.0 to 2.5 T. The activation energy of α-Fe2O3 NWs for urea production is lower than NPs in the range of 0-1 T, whereas it is reversed for higher magnetic induction values. Fourier transform infrared spectroscopy (FTIR) confirmed the formation of urea at the peaks of 1690-1600 cm-1. This green urea employing magnetically induced method could be a contender to the Haber-Bosch process currently used by the current industry which utilizes high temperature and high pressure.

  5. Detection of Interstellar Urea with Carma

    Science.gov (United States)

    Kuo, H.-L.; Snyder, L. E.; Friedel, D. N.; Looney, L. W.; McCall, B. J.; Remijan, A. J.; Lovas, F. J.; Hollis, J. M.

    2010-06-01

    Urea, a molecule discovered in human urine by H. M. Rouelle in 1773, has a significant role in prebiotic chemistry. Previous BIMA observations have suggested that interstellar urea [(NH_2)_2CO] is a compact hot core molecule such as other large molecules, e.g. methyl formate and acetic acid (2009, 64th OSU Symposium On Molecular Spectroscopy, WI05). We have conducted an extensive search for urea toward the high mass hot molecular core Sgr B2(N-LMH) using CARMA and the IRAM 30 m. Because the spectral lines of heavy molecules like urea tend to be weak and hot cores display lines from a wide range of molecules, a major problem in identifying urea lines is confusion with lines of other molecules. Therefore, it is necessary to detect a number of urea lines and apply sophisticated statistical tests before having confidence in an identification. The 1 mm resolution of CARMA enables favorable coupling of the source size and synthesized beam size, which was found to be essential for the detection of weak signals. The 2.5^"×2^" synthesized beam of CARMA significantly resolves out the contamination by extended emission and reveals the eight weak urea lines that were previously blended with nearby transitions. Our analysis indicates that these lines are likely to be urea since the resulting observed line frequencies are coincident with a set of overlapping connecting urea lines, and the observed line intensities are consistent with the expected line strengths of urea. In addition, we have developed a new statistical approach to examine the spatial correlation between the observed lines by applying the Student T-test to the high resolution channel maps obtained from CARMA. The T-test shows similar spatial distributions from all eight candidate lines, suggesting a common molecular origin, urea. Our T-test method could have a broad impact on the next generation of arrays, such as ALMA, because the new arrays will require a method to systematically determine the credibility of

  6. Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells

    Directory of Open Access Journals (Sweden)

    Elodie Jouan

    2016-12-01

    Full Text Available Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter expression, activity and regulation in human hepatoma HuH-7 cells, in order to determine the potential relevance of these cells for drug transport assays. HuH-7 cells displayed notable multidrug resistance-associated protein (MRP activity, presumed to reflect expression of various hepatic MRPs, including MRP2. By contrast, they failed to display functional activities of the uptake transporters sodium taurocholate co-transporting polypeptide (NTCP, organic anion-transporting polypeptides (OATPs and organic cation transporter 1 (OCT1, and of the canalicular transporters P-glycoprotein and breast cancer resistance protein (BCRP. Concomitantly, mRNA expressions of various sinusoidal and canalicular hepatic drug transporters were not detected (NTCP, OATP1B1, organic anion transporter 2 (OAT2, OCT1 and bile salt export pump or were found to be lower (OATP1B3, OATP2B1, multidrug and toxin extrusion protein 1, BCRP and MRP3 in hepatoma HuH-7 cells than those found in human hepatocytes, whereas other transporters such as OAT7, MRP4 and MRP5 were up-regulated. HuH-7 cells additionally exhibited farnesoid X receptor (FXR- and nuclear factor erythroid 2-related factor 2 (Nrf2-related up-regulation of some transporters. Such data indicate that HuH-7 cells, although expressing rather poorly some main hepatic drug transporters, may be useful for investigating interactions of drugs with MRPs, notably MRP2, and for studying FXR- or Nrf2-mediated gene regulation.

  7. Effects of plasma total ammonia content and pH on urea excretion in Nile tilapia.

    Science.gov (United States)

    McKenzie, D J; Piraccini, G; Felskie, A; Romano, P; Bronzi, P; Bolis, C L

    1999-01-01

    Nile tilapia (Oreochromis niloticus) were infused with ammonium salts, acid, and base to investigate the effects of changes in arterial plasma total ammonia content (Tamm) and pH (pHa) on plasma urea-nitrogen (urea-N) levels and urea-N excretory fluxes (Jurea-N). The tilapia did not possess a functional hepatic ornithine urea-cycle (no significant carbamyl phosphate synthetase III activity). Infused substances were dissolved in a saline vehicle and injected twice (5 mL kg-1), the first infusion to "prime" the animal and promote a more marked response to the second infusion, given 2.5 h later. The results reported are those of the second infusion. Infusion of 200 mM NH4Cl increased Tamm, reduced pHa, and increased plasma urea-N and Jurea-N. Two hundred mM NH4HCO3 increased Tamm and arterial plasma total CO2 content (TaCO2), reduced pHa, and increased Jurea-N. Fifty mM HCl reduced pHa but had no effects on urea dynamics. Fifty mM NaOH increased pHa, plasma urea-N levels, and Jurea-N. Two hundred mM NaHCO3 increased pHa, TaCO2, plasma urea-N levels, and Jurea-N. Infusion of the saline vehicle was without effect. The results indicate that ammonia loading and plasma alkalosis both stimulate urea excretion in uricolytic fish. The responses to hyperammonemia or alkalosis were not modified when combined with elevated plasma bicarbonate levels.

  8. Theoretical and NMR experimental insights on urea, thiourea and diindolyurea as fluoride carriers

    Science.gov (United States)

    Mendonça, João Guilherme P.; Silla, Josué M.; Andrade, Laize A. F.; Fernandes, Sergio A.; Cormanich, Rodrigo A.; Freitas, Matheus P.

    2016-06-01

    Urea and thiourea derivatives are widely known as anion transporters. The pristine urea and thiourea compounds were theoretically and spectroscopically evaluated as fluoride ligands, since transportation of F- is involved in many biochemical processes and this anion is suitable to be analyzed through NMR. Conformational changes induced by anions can be useful to probe ligand-anion complexation, but urea and thiourea do not undergo conformational isomerization. Thus, diindolylurea (DIU) was computationally investigated to search for its conformational preferences upon complexation with fluoride. Overall, the NMR proton signal for urea and thiourea moved downfield and broadened upon addition of one equivalent of fluoride anion in DMSO solution, indicating complexation. The 19F signal for the thiourea-F- mixture also shifted relative to the anion source. However, a J(N)H,F coupling constant was not observed, probably because of entropy and bulk solvation effects. In addition, the conformational preference of DIU changed drastically after simulated complexation with fluoride, in agreement with previous studies with other anions. This confirms the potential of urea derivatives as fluoride carriers.

  9. A fully resolved active musculo-mechanical model for esophageal transport

    CERN Document Server

    Kou, Wenjun; Griffith, Boyce E; Pandolfino, John E; Kahrilas, Peter J; Patankar, Neelesh A

    2015-01-01

    Esophageal transport is a physiological process that mechanically transports an ingested food bolus from the pharynx to the stomach via the esophagus, a multi-layered muscular tube. This process involves interactions between the bolus, the esophagus, and the neurally coordinated activation of the esophageal muscles. In this work, we use an immersed boundary (IB) approach to simulate peristaltic transport in the esophagus. The bolus is treated as a viscous fluid that is actively transported by the muscular esophagus, which is modeled as an actively contracting, fiber-reinforced tube. A simplified version of our model is verified by comparison to an analytic solution to the tube dilation problem. Three different complex models of the multi-layered esophagus, which differ in their activation patterns and the layouts of the mucosal layers, are then extensively tested. To our knowledge, these simulations are the first of their kind to incorporate the bolus, the multi-layered esophagus tube, and muscle activation i...

  10. Canine amino acid transport system Xc(-): cDNA sequence, distribution and cystine transport activity in lens epithelial cells.

    Science.gov (United States)

    Maruo, Takuya; Kanemaki, Nobuyuki; Onda, Ken; Sato, Reiichiro; Ichihara, Nobuteru; Ochiai, Hideharu

    2014-04-01

    The cystine transport activity of a lens epithelial cell line originated from a canine mature cataract was investigated. The distinct cystine transport activity was observed, which was inhibited to 28% by extracellular 1 mM glutamate. The cDNA sequences of canine cysteine/glutamate exchanger (xCT) and 4F2hc were determined. The predicted amino acid sequences were 527 and 533 amino acid polypeptides, respectively. The amino acid sequences of canine xCT and 4F2hc showed high similarities (>80%) to those of humans. The expression of xCT in lens epithelial cell line was confirmed by western blot analysis. RT-PCR analysis revealed high level expression only in the brain, and it was below the detectable level in other tissues.

  11. Multimotor transport in a system of active and inactive kinesin-1 motors.

    Science.gov (United States)

    Scharrel, Lara; Ma, Rui; Schneider, René; Jülicher, Frank; Diez, Stefan

    2014-07-15

    Long-range directional transport in cells is facilitated by microtubule-based motor proteins. One example is transport in a nerve cell, where small groups of motor proteins, such as kinesins and cytoplasmic dynein, work together to ensure the supply and clearance of cellular material along the axon. Defects in axonal transport have been linked to Alzheimer's and other neurodegenerative diseases. However, it is not known in detail how multimotor-based cargo transport is impaired if a fraction of the motors are defective. To mimic impaired multimotor transport in vitro, we performed gliding motility assays with varying fractions of active kinesin-1 motors and inactive kinesin-1 motor mutants. We found that impaired transport manifests in multiple motility regimes: 1), a fast-motility regime characterized by gliding at velocities close to the single-molecule velocity of the active motors; 2), a slow-motility regime characterized by gliding at close-to zero velocity or full stopping; and 3), a regime in which fast and slow motilities coexist. Notably, the transition from the fast to the slow regime occurred sharply at a threshold fraction of active motors. Based on single-motor parameters, we developed a stochastic model and a mean-field theoretical description that explain our experimental findings. Our results demonstrate that impaired multimotor transport mostly occurs in an either/or fashion: depending on the ratio of active to inactive motors, transport is either performed at close to full speed or is out of action.

  12. UREA BREATH TEST – ITS ROLE IN DIAGNOSTICS

    Directory of Open Access Journals (Sweden)

    Joško Osredkar

    2004-01-01

    Full Text Available Background. Each year many patients visit their physicians complaining of digestive symptoms, most commonly functional dyspepsia (»indigestion« or gastroesophageal reflux (»heartburn«. However, many patients with abdominal discomfort are actually suffering from gastric or duodenal ulcers that are commonly caused by H. pylori and thus are curable. Clearing the infection usually heals the ulcer and prevents relapse, so an accurate diagnosis is important. There are several options for diagnosing H. pylori infection: serology to detect antibodies against the bacterium; endoscopic biopsy for urease testing (H. pylori produce a urease that breaks down urea to ammonia and carbon dioxide; histology with special stains; or culture. Unfortunately, these procedures are invasive, expensive and not always accurate. Serological tests require a blood sample and tell only that a patient has been exposed to H. pylori at some time in the past, but not whether the patient is currently infected. Endoscopy and biopsy can detect current infection — the CLO test urease test allows rapid detection of H. pylori in gastric biopsy specimens — but endoscopy and biopsy are unpleasant medical procedures.Recently, noninvasive, sensitive, specific, easy to perform and patient’s well accepted methods had been developed known as urea breath test (UBT. When an infected person swallows a dose of urea labeled with an isotope of carbon — carbon-13 (13C or carbon-14 (14C – H. pylori in the gastric mucosa break down the labeled urea to form ammonia and labeled carbon dioxide. The carbon dioxide is absorbed into the bloodstream and excreted via the lungs. The patient then exhales into a device that measures the level of carbon dioxide. The urea breath test is specific for H. pylori (it detects only urease-producing bacteria, it is sensitive (the labeled urea reaches a large area of the stomach and thus reflects total gastric urease activity and the results can be

  13. Liquid chromatographic determination of urea in water-soluble urea-formaldehyde fertilizer products and in aqueous urea solutions: collaborative study.

    Science.gov (United States)

    Hojjatie, Michael M; Abrams, Dean E; Parham, Thomas M; Balthrop, J; Beine, R; Dickinson, V; Hartshorn, J; Herald, S; Latimer, G; Padmore, J; Pleasants, S; Riter, K; Roser, R; Schmunck, G; Sensmeier, R; Smith, V; Taylor, L; Volgas, G

    2004-01-01

    Water soluble urea-formaldehyde (UF) fertilizers, manufactured by complex reaction of urea and formaldehyde, typically contain varying amounts of unreacted urea. A liquid chromatography method for the analysis of urea in these products, and in aqueous urea solutions, was collaboratively studied. An amine chromatography column was used to separate the unreacted urea from numerous UF reaction products present in these liquid fertilizers. Unreacted urea was determined by using external urea standards with UV detection at 195 nm. The standards and test samples were prepared in the mobile phase of 85% (v/v) acetonitrile in water. Ten laboratories analyzed 5 different UF-based commercial products containing unreacted urea in the range of 6 to 17% by weight, and 5 different concentrations of urea in water equivalent to commercial products of that nature. The aqueous urea solutions contained 2-20% urea (w/w). The range of s(R) values for the 5 UF-based commercial fertilizers was 0.49-1.02 and the %RSD(R) was 1.94-6.14. The s(R) range for the 5 urea solutions was 0.10 to 0.79 and the %RSD(R) range was 2.54 to 4.88. The average recovery of urea from the aqueous urea solutions was 96-103%. Therefore, this method is capable of monitoring urea nitrogen manufacturers' label claims and total nitrogen claims in those cases where urea is the sole source of plant food nitrogen. Based on the collaborative study data, the authors recommend this method be approved for AOAC Official First Action status.

  14. Individual public transportation accessibility is positively associated with self-reported active commuting

    Directory of Open Access Journals (Sweden)

    Sune eDjurhuus

    2014-11-01

    Full Text Available Background: Active commuters have lower risk of chronic disease. Understanding which of the, to some extent, modifiable characteristics of public transportation that facilitate its use is thus important in a public health perspective. The aim of the study was to examine the association between individual public transportation accessibility and self-reported active commuting, and whether the associations varied with commute distance, age and gender. Methods: 28,928 commuters in the Capital Region of Denmark reported self-reported time spent either walking or cycling to work or study each day and the distance to work or study. Data were obtained from the Danish National Health Survey collected in February to April 2010. Individual accessibility by public transportation was calculated using a multimodal network in a GIS. Multilevel logistic regression was used to analyze the association between accessibility, expressed as access area, and being an active commuter.Results: Public transport accessibility area based on all stops within walking and cycling distance was positively associated with being an active commuter. Distance to work, age and gender modified the associations. Residing within 10 km commuting distance and in areas of high accessibility was associated with being an active commuter and meeting the recommendations of physical activity. For the respondents above 29 years, Individual public transportation accessibility was positively associated with being an active commuter. Women having high accessibility had significantly higher odds of being an active commuter compared to having a low accessibility. For men the associations were insignificant.Conclusions: This study extends the knowledge about the driving forces of using public transportation for commuting by examining the individual public transportation accessibility. Findings suggest that transportation accessibility supports active commuting and planning of improved public transit

  15. Inhibition of Human Drug Transporter Activities by the Pyrethroid Pesticides Allethrin and Tetramethrin.

    Science.gov (United States)

    Chedik, Lisa; Bruyere, Arnaud; Le Vee, Marc; Stieger, Bruno; Denizot, Claire; Parmentier, Yannick; Potin, Sophie; Fardel, Olivier

    2017-01-01

    Pyrethroids are widely-used chemical insecticides, to which humans are commonly exposed, and known to alter functional expression of drug metabolizing enzymes. Limited data have additionally suggested that drug transporters, that constitute key-actors of the drug detoxification system, may also be targeted by pyrethroids. The present study was therefore designed to analyze the potential regulatory effects of these pesticides towards activities of main ATP-binding cassette (ABC) and solute carrier (SLC) drug transporters, using transporter-overexpressing cells. The pyrethroids allethrin and tetramethrin were found to inhibit various ABC and SLC drug transporters, including multidrug resistance-associated protein (MRP) 2, breast cancer resistance protein (BCRP), organic anion transporter polypeptide (OATP) 1B1, organic anion transporter (OAT) 3, multidrug and toxin extrusion transporter (MATE) 1, organic cation transporter (OCT) 1 and OCT2, with IC50 values however ranging from 2.6 μM (OCT1 inhibition by allethrin) to 77.6 μM (OAT3 inhibition by tetramethrin) and thus much higher than pyrethroid concentrations (in the nM range) reached in environmentally pyrethroid-exposed humans. By contrast, allethrin and tetramethrin cis-stimulated OATP2B1 activity and failed to alter activities of OATP1B3, OAT1 and MATE2-K, whereas P-glycoprotein activity was additionally moderately inhibited. Twelve other pyrethoids used at 100 μM did not block activities of the various investigated transporters, or only moderately inhibited some of them (inhibition by less than 50%). In silico analysis of structure-activity relationships next revealed that molecular parameters, including molecular weight and lipophilicity, are associated with transporter inhibition by allethrin/tetramethrin and successfully predicted transporter inhibition by the pyrethroids imiprothrin and prallethrin. Taken together, these data fully demonstrated that two pyrethoids, i.e., allethrin and tetramethrin, can

  16. Inhibition of Human Drug Transporter Activities by the Pyrethroid Pesticides Allethrin and Tetramethrin

    Science.gov (United States)

    Chedik, Lisa; Bruyere, Arnaud; Le Vee, Marc; Stieger, Bruno; Denizot, Claire; Parmentier, Yannick; Potin, Sophie; Fardel, Olivier

    2017-01-01

    Pyrethroids are widely-used chemical insecticides, to which humans are commonly exposed, and known to alter functional expression of drug metabolizing enzymes. Limited data have additionally suggested that drug transporters, that constitute key-actors of the drug detoxification system, may also be targeted by pyrethroids. The present study was therefore designed to analyze the potential regulatory effects of these pesticides towards activities of main ATP-binding cassette (ABC) and solute carrier (SLC) drug transporters, using transporter-overexpressing cells. The pyrethroids allethrin and tetramethrin were found to inhibit various ABC and SLC drug transporters, including multidrug resistance-associated protein (MRP) 2, breast cancer resistance protein (BCRP), organic anion transporter polypeptide (OATP) 1B1, organic anion transporter (OAT) 3, multidrug and toxin extrusion transporter (MATE) 1, organic cation transporter (OCT) 1 and OCT2, with IC50 values however ranging from 2.6 μM (OCT1 inhibition by allethrin) to 77.6 μM (OAT3 inhibition by tetramethrin) and thus much higher than pyrethroid concentrations (in the nM range) reached in environmentally pyrethroid-exposed humans. By contrast, allethrin and tetramethrin cis-stimulated OATP2B1 activity and failed to alter activities of OATP1B3, OAT1 and MATE2-K, whereas P-glycoprotein activity was additionally moderately inhibited. Twelve other pyrethoids used at 100 μM did not block activities of the various investigated transporters, or only moderately inhibited some of them (inhibition by less than 50%). In silico analysis of structure-activity relationships next revealed that molecular parameters, including molecular weight and lipophilicity, are associated with transporter inhibition by allethrin/tetramethrin and successfully predicted transporter inhibition by the pyrethroids imiprothrin and prallethrin. Taken together, these data fully demonstrated that two pyrethoids, i.e., allethrin and tetramethrin, can

  17. Predictive model for segmented poly(urea

    Directory of Open Access Journals (Sweden)

    Frankl P.

    2012-08-01

    Full Text Available Segmented poly(urea has been shown to be of significant benefit in protecting vehicles from blast and impact and there have been several experimental studies to determine the mechanisms by which this protective function might occur. One suggested route is by mechanical activation of the glass transition. In order to enable design of protective structures using this material a constitutive model and equation of state are needed for numerical simulation hydrocodes. Determination of such a predictive model may also help elucidate the beneficial mechanisms that occur in polyurea during high rate loading. The tool deployed to do this has been Group Interaction Modelling (GIM – a mean field technique that has been shown to predict the mechanical and physical properties of polymers from their structure alone. The structure of polyurea has been used to characterise the parameters in the GIM scheme without recourse to experimental data and the equation of state and constitutive model predicts response over a wide range of temperatures and strain rates. The shock Hugoniot has been predicted and validated against existing data. Mechanical response in tensile tests has also been predicted and validated.

  18. Are characteristics of the school district associated with active transportation to school in Danish adolescents?

    DEFF Research Database (Denmark)

    Stock, Christiane; Bloomfield, Kim; Ejstrud, Bo;

    2012-01-01

    BACKGROUND: This study sought to determine the influence of individual factors on active transportation to school among Danish seventh graders and whether school district factors are associated with such behaviour independently of individual factors. METHODS: Mixed effects logistic regression...

  19. Dopamine Transporter Genotype Conveys Familial Risk of Attention-Deficit/Hyperactivity Disorder through Striatal Activation

    Science.gov (United States)

    Durston, Sarah; Fossella, John A.; Mulder, Martijn J.; Casey B. J.; Ziermans, Tim B.; Vessaz, M. Nathalie; Van Engeland, Herman

    2008-01-01

    The study examines the effect of the dopamine transporter (DAT1) genotype in attention-deficit/hyperactivity disorder (ADHD). The results confirm that DAT1 translates the genetic risk of ADHD through striatal activation.

  20. Dopamine Transporter Genotype Conveys Familial Risk of Attention-Deficit/Hyperactivity Disorder through Striatal Activation

    Science.gov (United States)

    Durston, Sarah; Fossella, John A.; Mulder, Martijn J.; Casey B. J.; Ziermans, Tim B.; Vessaz, M. Nathalie; Van Engeland, Herman

    2008-01-01

    The study examines the effect of the dopamine transporter (DAT1) genotype in attention-deficit/hyperactivity disorder (ADHD). The results confirm that DAT1 translates the genetic risk of ADHD through striatal activation.

  1. 76 FR 73020 - Agency Information Collection (Request for Transportation Expense Reimbursement): Activity Under...

    Science.gov (United States)

    2011-11-28

    ... unable to pursue training or employment without travel assistance. An agency may not conduct or sponsor... From the Federal Register Online via the Government Publishing Office DEPARTMENT OF VETERANS AFFAIRS Agency Information Collection (Request for Transportation Expense Reimbursement): Activity...

  2. OPTIMIZATION METHOD AND SOFTWARE FOR FUEL COST REDUCTION IN CASE OF ROAD TRANSPORT ACTIVITY

    Directory of Open Access Journals (Sweden)

    György Kovács

    2017-06-01

    Full Text Available The transport activity is one of the most expensive processes in the supply chain and the fuel cost is the highest cost among the cost components of transportation. The goal of the research is to optimize the transport costs in case of a given transport task both by the selecting the optimal petrol station and by determining the optimal amount of the refilled fuel. Recently, in practice, these two decisions have not been made centrally at the forwarding company, but they depend on the individual decision of the driver. The aim of this study is to elaborate a precise and reliable mathematical method for selecting the optimal refuelling stations and determining the optimal amount of the refilled fuel to fulfil the transport demands. Based on the elaborated model, new decision-supporting software is developed for the economical fulfilment of transport trips.

  3. Ciprofloxacin Is Actively Transported across Bronchial Lung Epithelial Cells Using a Calu-3 Air Interface Cell Model

    Science.gov (United States)

    Ong, Hui Xin; Traini, Daniela; Bebawy, Mary

    2013-01-01

    Ciprofloxacin is a well-established broad-spectrum fluoroquinolone antibiotic that penetrates well into the lung tissues; still, the mechanisms of its transepithelial transport are unknown. The contributions of specific transporters, including multidrug efflux transporters, organic cation transporters, and organic anion-transporting polypeptide transporters, to the uptake of ciprofloxacin were investigated in vitro using an air interface bronchial epithelial model. Our results demonstrate that ciprofloxacin is subject to predominantly active influx and a slight efflux component. PMID:23507281

  4. Borreliacidal activity of Borrelia metal transporter A (BmtA binding small molecules by manganese transport inhibition

    Directory of Open Access Journals (Sweden)

    Wagh D

    2015-02-01

    Full Text Available Dhananjay Wagh,* Venkata Raveendra Pothineni,* Mohammed Inayathullah, Song Liu, Kwang-Min Kim, Jayakumar Rajadas Biomaterials and Advanced Drug Delivery Laboratory, Stanford Cardiovascular Pharmacology Division, Cardiovascular Institute, Stanford University School of Medicine, Palo Alto, CA, USA *These authors contributed equally to this work  Abstract: Borrelia burgdorferi, the causative agent of Lyme disease, utilizes manganese (Mn for its various metabolic needs. We hypothesized that blocking Mn transporter could be a possible approach to inhibit metabolic activity of this pathogen and eliminate the infection. We used a combination of in silico protein structure prediction together with molecular docking to target the Borrelia metal transporter A (BmtA, a single known Mn transporter in Borrelia and screened libraries of FDA approved compounds that could potentially bind to the predicted BmtA structure with high affinity. Tricyclic antihistamines such as loratadine, desloratadine, and 3-hydroxydesloratadine as well as yohimbine and tadalafil demonstrated a tight binding to the in silico folded BmtA transporter. We, then, tested borreliacidal activity and dose response of the shortlisted compounds from this screen using a series of in vitro assays. Amongst the probed compounds, desloratadine exhibited potent borreliacidal activity in vitro at and above 78 µg/mL (250 µM. Borrelia treated with lethal doses of desloratadine exhibited a significant loss of intracellular Mn specifically and a severe structural damage to the bacterial cell wall. Our results support the possibility of developing a novel, targeted therapy to treat Lyme disease by targeting specific metabolic needs of Borrelia.  Keywords: Lyme disease, BmtA, Borrelia burgdorferi, desloratadine, Bac Titer-Glo assay

  5. Diagnosis of Transport Activity as a Component of the Enterprise Logistical System

    Directory of Open Access Journals (Sweden)

    Skrynkovskyy Ruslan M.

    2016-05-01

    Full Text Available The article reveals the essence of the concept of “diagnosis of the enterprise transport activity”, by which there should be meant a process of evaluating the state of movement (transportation, carrying of freight (material resources, work in process or finished products by one type of transport facilities or their combination in accordance with the applied transport system and trends of its changes as well as determining the future prospects on the basis of sound management decisions in order to ensure a successful operation and development of the enterprise in the competitive environment. It has been found that the key business-indicators of the diagnosis system of transport activity as a component of the enterprise logistical system are: the coefficient of timeliness of freight transportation (delivery; coefficient of completeness of transportation; coefficient of freight safety conditions; coefficient of efficiency of freight transportation; coefficient of complexity of servicing freight owners; coefficient of satisfaction of freight owners’ demand, coefficient of readiness to operation of transport facilities per working day; coefficient of using vehicle kilometers travelled; coefficient of extensity of transport facility packing.

  6. Active patterning and asymmetric transport in a model actomyosin network

    Science.gov (United States)

    Wang, Shenshen; Wolynes, Peter G.

    2013-12-01

    Cytoskeletal networks, which are essentially motor-filament assemblies, play a major role in many developmental processes involving structural remodeling and shape changes. These are achieved by nonequilibrium self-organization processes that generate functional patterns and drive intracellular transport. We construct a minimal physical model that incorporates the coupling between nonlinear elastic responses of individual filaments and force-dependent motor action. By performing stochastic simulations we show that the interplay of motor processes, described as driving anti-correlated motion of the network vertices, and the network connectivity, which determines the percolation character of the structure, can indeed capture the dynamical and structural cooperativity which gives rise to diverse patterns observed experimentally. The buckling instability of individual filaments is found to play a key role in localizing collapse events due to local force imbalance. Motor-driven buckling-induced node aggregation provides a dynamic mechanism that stabilizes the two-dimensional patterns below the apparent static percolation limit. Coordinated motor action is also shown to suppress random thermal noise on large time scales, the two-dimensional configuration that the system starts with thus remaining planar during the structural development. By carrying out similar simulations on a three-dimensional anchored network, we find that the myosin-driven isotropic contraction of a well-connected actin network, when combined with mechanical anchoring that confers directionality to the collective motion, may represent a novel mechanism of intracellular transport, as revealed by chromosome translocation in the starfish oocyte.

  7. Study of supported bilayer lipid membranes for use in chemo-electric energy conversion via active proton transport

    Science.gov (United States)

    Sarles, Stephen A.; Sundaresan, Vishnu B.; Leo, Donald J.

    2007-09-01

    Bilayer lipid membranes (BLMs) have been studied extensively due to functional and structural similarities to cell membranes, fostering research to understand ion-channel protein functions, measure bilayer mechanical properties, and identify self-assembly mechanisms. BLMs have traditionally been formed across single pores in substrates such as PTFE (Teflon). The incorporation of ion-channel proteins into the lipid bilayer enables the selective transfer of ions and fluid through the BLM. Processes of this nature have led to the measurement of ion current flowing across the lipid membrane and have been used to develop sensors that signal the presence of a particular reactant (glucose, urea, penicillin), improve drug recognition in cells, and develop materials capable of creating chemical energy from light. Recent research at Virginia Tech has shown that the incorporation of proton transporters in a supported BLM formed across an array of pores can convert chemical energy available in the adenosine triphosphate (ATP) into electricity. Experimental results from this work show that the system-named Biocell-is capable of developing 2µW/cm2 of membrane area with 15μl of ATPase. Efforts to increase the power output and conversion efficiency of this process while moving toward a packaged device present a unique engineering problem. The bilayer, as host to the active proton transporters, must therefore be formed evenly across a porous substrate, remain stable and yet fluid-like for protein interaction, and exhibit a large seal resistance. This article presents the ongoing work to characterize the Biocell using impedance analysis. Electrical impedance spectroscopy (EIS) is used to study the effect of adding ATPase proteins to POPS:POPE bilayer lipid membranes and correlate structural changes evident in the impedance data to the energy-conversion capability of various partial and whole Biocell assemblies. The specific membrane resistance of a pure BLM drops from 40-120k

  8. Webcams, crowdsourcing, and enhanced crosswalks: Developing a novel method to analyze active transportation

    Directory of Open Access Journals (Sweden)

    J. Aaron eHipp

    2016-05-01

    Full Text Available Introduction: Active transportation opportunities and infrastructure are an important component of a community’s design, livability, and health. Features of the built environment influence active transportation, but objective study of the natural experiment effects of built environment improvements on active transportation is challenging. The purpose of this study was to develop and present a novel method of active transportation research using webcams and crowdsourcing, and to determine if crosswalk enhancement was associated with changes in active transportation rates, including across a variety of weather conditions. Methods: 20,529 publicly available webcam images from two street intersections in Washington, D.C., were used to examine the impact of an improved crosswalk on active transportation. A crowdsource, Amazon Mechanical Turk, annotated image data. Temperature data was collected from the National Oceanic and Atmospheric Administration, and precipitation data was annotated from images by trained research assistants. Results: Summary analyses demonstrated slight, bi-directional differences in the percent of images with pedestrians and bicyclists captured before and after the enhancement of the crosswalks. Chi-square analyses revealed these changes were not significant. In general, pedestrian presence increased in images captured during moderate temperatures compared to images captured during hot or cold temperatures. Chi-square analyses indicated the crosswalk improvement may have encouraged walking and biking in uncomfortable outdoor conditions (p<0.5. Conclusion: The methods employed provide an objective, cost-effective alternative to traditional means of examining the effects of built environment changes on active transportation. The use of webcams to collect active transportation data has applications for community policymakers, planners, and health professionals. Future research will work to validate this method in a variety of

  9. Synthesis and Characterization of Branched Poly(ester urea)s with Different Branch Density

    Science.gov (United States)

    Yu, Jiayi; Becker, Matthew

    2015-03-01

    A new class of L-phenylalanine-based poly(ester urea)s (PEU) was developed that possess tunable mechanical properties, water uptake ability and degradation rates. Our preliminary data has shown that 1,6-hexanediol L - phenylalanine-based poly(ester urea)s possesses an elastic modulus nearly double that of poly(lactic acid). My work details the synthesis of a series of L - phenylalanine-based poly(ester urea)s possessing a variation in diol chain length and in branch density and shows how these subtle structural differences influence the mechanical properties and in vitro biodegradation rates. The elastic moduli span a range of values that overlap with several currently clinically available degradable polymers. Increasingly the diol chain lengths increases the amount of flexible segment in the chemical structure, which results in reduced elastic modulus values and increased values of elongation at break. Increasing the amount of branch monomer incorporated into the system reduces the molecular entanglement, which also results in decreased elastic modulus values and increased values of elongation at break. The L - phenylalanine-based poly(ester urea)s also exhibited a diol length dependent degradation process that varied between 1-5 % over 16 weeks. Compared with PLLA, PEUs degrade more quickly and the rate can be tuned by changing the diol chain length. PEUs absorb more water and the water uptake ability can be tuned by changing the branch density. This work was supported by Akron Functional Materials Center.

  10. Standardization of the TRUE Test imidazolidinyl urea and diazolidinyl urea patches

    DEFF Research Database (Denmark)

    Agner, T; Andersen, Klaus Ejner; Björkner, B;

    2001-01-01

    The preservatives imidazolidinyl urea (IMID, Germall 115) and diazolidinyl urea (DU, Germall II) are commonly used in cosmetic products and are well-known sensitizers. The aim of the present study was to establish the optimal patch test concentration in hydrophilic dried-in vehicle (TRUE Test...

  11. Standardization of the TRUE Test imidazolidinyl urea and diazolidinyl urea patches

    DEFF Research Database (Denmark)

    Agner, T; Andersen, Klaus Ejner; Björkner, B

    2001-01-01

    The preservatives imidazolidinyl urea (IMID, Germall 115) and diazolidinyl urea (DU, Germall II) are commonly used in cosmetic products and are well-known sensitizers. The aim of the present study was to establish the optimal patch test concentration in hydrophilic dried-in vehicle (TRUE Test...

  12. Stress-Induced CDK5 Activation Disrupts Axonal Transport via Lis1/Ndel1/Dynein

    Directory of Open Access Journals (Sweden)

    Eva Klinman

    2015-07-01

    Full Text Available Axonal transport is essential for neuronal function, and defects in transport are associated with multiple neurodegenerative diseases. Aberrant cyclin-dependent kinase 5 (CDK5 activity, driven by the stress-induced activator p25, also is observed in these diseases. Here we show that elevated CDK5 activity increases the frequency of nonprocessive events for a range of organelles, including lysosomes, autophagosomes, mitochondria, and signaling endosomes. Transport disruption induced by aberrant CDK5 activation depends on the Lis1/Ndel1 complex, which directly regulates dynein activity. CDK5 phosphorylation of Ndel1 favors a high affinity Lis1/Ndel/dynein complex that blocks the ATP-dependent release of dynein from microtubules, inhibiting processive motility of dynein-driven cargo. Similar transport defects observed in neurons from a mouse model of amyotrophic lateral sclerosis are rescued by CDK5 inhibition. Together, these studies identify CDK5 as a Lis1/Ndel1-dependent regulator of transport in stressed neurons, and suggest that dysregulated CDK5 activity contributes to the transport deficits observed during neurodegeneration.

  13. Activity-Based Costing Application in an Urban Mass Transport Company

    Directory of Open Access Journals (Sweden)

    Popesko Boris

    2011-12-01

    Full Text Available The purpose of this paper is to provide a basic overview of the application of Activity-Based Costing in an urban mass transport company which operates land public transport via buses and trolleys within the city. The case study was conducted using the Activity-Based Methodology in order to calculate the true cost of individual operations and to measure the profitability of particular transport lines. The case study analysis showed the possible effects of the application of the Activity-Based Costing for an urban mass transport company as well as the limitations of using the ABC methodology in the service industry. With regards to the application of the ABC methodology, the primary limitation of the accuracy of the conclusions is the quality of the non-financial information which had to be gathered throughout the implementation process. A basic limitation of the accurate data acquisition is the nature of the fare system of the transport company which does not allow the identification of the route that is taken by an individual passenger. The study illustrates the technique of ABC in urban mass transport and provides a real company example of information outputs of the ABC system. The users indicated that, the ABC model is very useful for profitability reporting and profit management. Also, the paper shows specific application of the Activity-Based Methodology in conditions of urban mass transport companies with regional specifics.

  14. Amperometric urea biosensors based on sulfonated graphene/polyaniline nanocomposite

    Science.gov (United States)

    Das, Gautam; Yoon, Hyon Hee

    2015-01-01

    An electrochemical biosensor based on sulfonated graphene/polyaniline nanocomposite was developed for urea analysis. Oxidative polymerization of aniline in the presence of sulfonated graphene oxide was carried out by electrochemical methods in an aqueous environment. The structural properties of the nanocomposite were characterized by Fourier-transform infrared, Raman spectroscopy, X-ray photoelectron spectroscopy, and scanning electron microscopy techniques. The urease enzyme-immobilized sulfonated graphene/polyaniline nanocomposite film showed impressive performance in the electroanalytical detection of urea with a detection limit of 0.050 mM and a sensitivity of 0.85 (μA · cm−2·mM−1. The biosensor achieved a broad linear range of detection (0.12–12.3 mM) with a notable response time of approximately 5 seconds. Moreover, the fabricated biosensor retained 81% of its initial activity (based on sensitivity) after 15 days of storage at 4°C. The ease of fabrication coupled with the low cost and good electrochemical performance of this system holds potential for the development of solid-state biosensors for urea detection. PMID:26346240

  15. Amperometric urea biosensors based on sulfonated graphene/polyaniline nanocomposite

    Directory of Open Access Journals (Sweden)

    Das G

    2015-08-01

    Full Text Available Gautam Das, Hyon Hee Yoon Department of Chemical and Biological Engineering, Gachon University, Seongnam, Gyeonggi-do, South Korea Abstract: An electrochemical biosensor based on sulfonated graphene/polyaniline nanocomposite was developed for urea analysis. Oxidative polymerization of aniline in the presence of sulfonated graphene oxide was carried out by electrochemical methods in an aqueous environment. The structural properties of the nanocomposite were characterized by Fourier-transform infrared, Raman spectroscopy, X-ray photoelectron spectroscopy, and scanning electron microscopy techniques. The urease enzyme-immobilized sulfonated graphene/polyaniline nanocomposite film showed impressive performance in the electroanalytical detection of urea with a detection limit of 0.050 mM and a sensitivity of 0.85 µA·cm-2·mM-1. The biosensor achieved a broad linear range of detection (0.12–12.3 mM with a notable response time of approximately 5 seconds. Moreover, the fabricated biosensor retained 81% of its initial activity (based on sensitivity after 15 days of storage at 4°C. The ease of fabrication coupled with the low cost and good electrochemical performance of this system holds potential for the development of solid-state biosensors for urea detection. Keywords: electrochemical deposition, sulfonated graphene oxide, urease

  16. Amperometric urea biosensors based on sulfonated graphene/polyaniline nanocomposite.

    Science.gov (United States)

    Das, Gautam; Yoon, Hyon Hee

    2015-01-01

    An electrochemical biosensor based on sulfonated graphene/polyaniline nanocomposite was developed for urea analysis. Oxidative polymerization of aniline in the presence of sulfonated graphene oxide was carried out by electrochemical methods in an aqueous environment. The structural properties of the nanocomposite were characterized by Fourier-transform infrared, Raman spectroscopy, X-ray photoelectron spectroscopy, and scanning electron microscopy techniques. The urease enzyme-immobilized sulfonated graphene/polyaniline nanocomposite film showed impressive performance in the electroanalytical detection of urea with a detection limit of 0.050 mM and a sensitivity of 0.85 (μA · cm(-2)·mM(-1). The biosensor achieved a broad linear range of detection (0.12-12.3 mM) with a notable response time of approximately 5 seconds. Moreover, the fabricated biosensor retained 81% of its initial activity (based on sensitivity) after 15 days of storage at 4°C. The ease of fabrication coupled with the low cost and good electrochemical performance of this system holds potential for the development of solid-state biosensors for urea detection.

  17. Synthesis of dimethyl carbonate from urea and methanol

    Energy Technology Data Exchange (ETDEWEB)

    Polyakov, M.; Kalevaru, V.N.; Martin, A. [Rostock Univ. (Germany). Leibniz Institute for Catalysis; Mueller, K.; Arlt, W. [Erlangen-Nuernberg Univ. (Germany); Strautmann, J.; Kruse, D. [Evonik Industries AG, Marl (Germany). Creavis Technologies and Innovation

    2012-07-01

    Alcoholation of urea with methanol to produce dimethyl carbonate (DMC) is an interesting approach from both the ecological and economical points of view because the urea synthesis usually occurs by the direct use of carbon dioxide. Literature survey reveals that metal oxide catalysts for instance MgO, ZnO, etc. or polyphosphoric acids are mostly used as catalysts for this reaction. In this contribution, we describe the application of ZnO, MgO, CaO, TiO{sub 2}, ZrO{sub 2} or Al{sub 2}O{sub 3} catalysts for the above mentioned reaction. The catalytic activity of different metal oxides towards DMC synthesis was checked and additionally a comparison of achieved conversions with that of predictions made by thermodynamic calculations was also carried out. The achieved conversions are in good agreement with those of calculated ones. The test results reveal that the reaction pressure and temperature have a strong influence on the formation of DMC. Higher reaction pressure improved the yield of DMC. Among different catalysts investigated, ZnO displayed the best performance. The conversion of urea in most cases is close to 100 % and methyl carbamate MC is the major product of the reaction. A part of MC is subsequently converted to DMC, which however depends upon the reaction conditions applied and nature of catalyst used. From the best case, a DMC yield of ca. 8 % could be successfully achieved over ZnO catalyst. (orig.)

  18. Effect of urea on degradation of terbuthylazine in soil.

    Science.gov (United States)

    Caracciolo, Anna Barra; Giuliano, Giuseppe; Grenni, Paola; Cremisini, Carlo; Ciccoli, Roberto; Ubaldi, Carla

    2005-05-01

    Pesticide and nitrate contamination of soil and groundwater from agriculture is an environmental and public health concern worldwide. The herbicide terbuthylazine (CBET) has replaced atrazine in Italy and in many other countries because the use of the latter has been banned because of its adverse environmental impacts. Unlike atrazine, knowledge about the fate of CBET in soil is still not extensive, especially regarding its transformation products, but recent monitoring data show its occurrence and that of its main metabolite, desethyl-terbuthylazine (CBAT), in groundwater above the limit of 0.1 microg/L established by European Union Directive and Italian legislation. The objective of this work was to investigate if the presence of the fertilizer urea affects CBET degradation in the soil. Laboratory CBET degradation experiments in the presence/absence of urea were performed with microbiologically active soil and sterilized soil. Terbuthylazine degradation rates under the different experimental conditions were assessed, and the formation, degradation, and transformation of the metabolite CBAT were also studied. Terbuthylazine degradation was affected by the presence of urea, in terms both of a higher disappearance time of 50% of the initial concentration and of a lower amount of CBAT formed. These findings have practical implications for the real-life assessment of the environmental fate of triazine herbicides in agricultural areas since these herbicides are frequently applied to soils receiving ureic fertilizers.

  19. Synthesis and Biological Activity of N,N’-Bis(4-nitropheoyl) urea%4,4′-二硝基二苯脲合成工艺研究

    Institute of Scientific and Technical Information of China (English)

    薛月圆; 苏畅; 刘新民

    2015-01-01

    N,N’-Bis(4-nitrophenyl)urea is prepared by reacting p-nitroaniline with urea in the presence of distilled water as solvent at refluxing temperature .Its structure is elucidated with IR and the optimal synthesis con-ditions are established .As the results indicate , under the optimal ratio of materials ( p-nitroaniline : urea : con-centrated hydrochloric acid =1.00 :1.00 :1.25), under reflux for 7h, the production rate can reach 68.7%.%以蒸馏水为溶剂、浓盐酸作催化剂、对硝基苯胺与尿素为原料合成了4,4′-二硝基二苯脲.采用IR对其结构进行了表征,并确定了最佳合成条件.结果表明,在最佳原料配比:对硝基苯胺∶尿素∶浓盐酸(摩尔比)=1.00∶1.00∶1.25条件下回流7h,产率可达68.7%.

  20. Urea coated with oxidized charcoal reduces ammonia volatilization

    Directory of Open Access Journals (Sweden)

    Diogo Mendes de Paiva

    2012-08-01

    Full Text Available Urea is the most consumed nitrogen fertilizer in the world. However, its agronomic and economic efficiency is reduced by the volatilization of NH3, which can reach 78 % of the applied nitrogen. The coating of urea granules with acidic compounds obtained by charcoal oxidation has the potential to reduce the volatilization, due to the acidic character, the high buffering capacity and CEC. This work aimed to evaluate the effect of HNO3-oxidized carbon on the control of NH3 volatilization. These compounds were obtained by oxidation of Eucalyptus grandis charcoal, produced at charring temperatures of 350 and 450 ºC, with 4.5 mol L-1 HNO3. The charcoal was oxidized by solubilization in acidic or alkaline medium, similar to the procedure of soil organic matter fractionation (CHox350 and CHox450. CHox was characterized by C, H, O, N contents and their respective atomic relations, by the ratio E4 (absorbance 465 nm by E6 (absorbance 665 nm, and by active acidity and total acidity (CEC. The inhibitory effect of CHox on the urease activity of Canavalia ensiformis was assessed in vitro. The NH3 volatilization from urea was evaluated with and without coating of oxidized charcoal (U-CHox350 or U-CHox450 in a closed system with continuous air flow. The pH of both CHox was near 2.0, but the total acidity of CHox350 was higher, 72 % of which was attributed to carboxylic groups. The variation in the ionization constants of CHox350 was also greater. The low E4/E6 ratios characterize the high stability of the compounds in CHox. CHox did not inhibit the urease activity in vitro, although the maximum volatilization peak from U-CHox450 and U-CHox350 occurred 24 h after that observed for uncoated urea. The lowest volatilization rate was observed for U-CHox350 as well as a 43 % lower total amount of NH3 volatilized than from uncoated urea.

  1. Can simulations quantitatively predict peptide transfer free energies to urea solutions? Thermodynamic concepts and force field limitations.

    Science.gov (United States)

    Horinek, Dominik; Netz, Roland R

    2011-06-16

    Many proteins denature when they are transferred to concentrated urea solutions. Three mechanisms for urea's denaturing ability have been proposed: (i) direct binding to polar parts of the protein surface, (ii) direct binding to nonpolar parts of the protein surface, and (iii) an indirect effect mediated by modifications of the bulk water properties. The disentanglement of these three processes has been the goal of many experimental and computational studies, yet there is no final agreement on the relative importance of the three contributions. The separation of the two direct mechanisms, albeit conceptually clear, is difficult in experimental studies and in simulations depends subtly on how the discrimination between polar and nonpolar groups is accomplished. Indirect effects, embodied in the change of solution activity as urea is added, are rarely monitored in urea/peptide simulations and thus have remained elusive in numerical studies. In this paper we establish a rigorous separation of all three contributions to the solvation thermodynamics of stretched peptide chains. We contrast this scenario with two commonly used model systems: the air/water interface and the interface between water and a hydrophobic alkane self-assembled monolayer. Together with bulk thermodynamic properties of urea/water mixed solvents, a complete thermodynamic description of the urea/water/peptide system is obtained: urea avoids the air/water interface but readily adsorbs at the oil-water interface and at hydrophobic as well as hydrophilic peptide chains, in accordance with experimental results. Simple thermodynamic arguments show that the indirect contribution to urea's denaturing capability is negligibly small, although urea strongly changes the water bulk properties as judged by the number of hydrogen bonds formed. Urea's tendency to bind to proteins is correctly reproduced with several force field combinations, but the quantitative binding strength as well as the relative importance

  2. Photoluminescence of urea- and urea/rhodamine B-capped TiO{sub 2} nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Gonzalo-Juan, I., E-mail: gonzalo@materials.tu-darmstadt.de; Macé, L.; Tengeler, S.; Mosallem, A.; Nicoloso, N.; Riedel, R.

    2016-07-01

    Urea- and rhodamine B (RhB)-capped TiO{sub 2} nanoparticles (NPs) have been prepared by solvothermal synthesis and characterized by HRTEM, XRD, FTIR, XPS, optical absorption and photoemission. The urea and urea/RhB ligands are capped to the surface of the TiO{sub 2} NPs for the first time through carbamate bonding. The band gap of TiO{sub 2} is slightly reduced from 3.1 eV to 3.0 eV in the urea capped TiO{sub 2} NPs (TU) and 2.9 eV for the NPs capped with urea/RhB (TUR). The generation of new trapping states in TU and TUR at the conduction band edges (surface oxygen vacancies) has been confirmed by the Urbach law providing tail state energies of 180 meV and 270 meV, respectively. These tail states are considered to be responsible for the strong reduction of the photoluminescence at ≈400 nm and the increased emission at ≈600 nm in TU and TUR. The findings suggest that urea- and RhB-capped TiO{sub 2} NPs could have potential applications as photocatalysts, opto-electronic devices, sensors, biological labels and anti-bacterial agents. - Highlights: • Urea- and urea/rhodamine B (RhB)-capped TiO{sub 2} nanoparticles preparation. • Characterization of optical properties of urea- and urea/rhodamine B (RhB)-capped TiO{sub 2} nanoparticles. • The recombination of electrons and holes is significantly reduced in the capped TiO{sub 2} nanoparticles, in comparison with TiO{sub 2}.

  3. Profile of sodium phenylbutyrate granules for the treatment of urea-cycle disorders: patient perspectives.

    Science.gov (United States)

    Peña-Quintana, Luis; Llarena, Marta; Reyes-Suárez, Desiderio; Aldámiz-Echevarria, Luis

    2017-01-01

    Urea-cycle disorders are a group of rare hereditary metabolic diseases characterized by deficiencies of one of the enzymes and transporters involved in the urea cycle, which is necessary for the removal of nitrogen produced from protein breakdown. These hereditary metabolic diseases are characterized by hyperammonemia and life-threatening hyperammonemic crises. Pharmacological treatment of urea-cycle disorders involves alternative nitrogen-scavenging pathways. Sodium benzoate combines with glycine and phenylacetate/phenylbutyrate with glutamine, forming, respectively, hippuric acid and phenylacetylglutamine, which are eliminated in the urine. Among the ammonia-scavenging drugs, sodium phenylbutyrate is a well-known long-term treatment of urea-cycle disorders. It has been used since 1987 as an investigational new drug, and was approved for marketing in the US in 1996 and the EU in 1999. However, sodium phenylbutyrate has an aversive odor and taste, which may compromise patients' compliance, and many patients have reported difficulty in taking this drug. Sodium phenylbutyrate granules are a new tasteless and odor-free formulation of sodium phenylbutyrate, which is indicated in the treatment of urea-cycle disorders. This recently developed taste-masked formulation of sodium phenylbutyrate granules was designed to overcome the considerable issues that taste has on adherence to therapy. Several studies have reported the clinical experience of patients with urea-cycle disorders treated with this new tasteless formulation of sodium phenylbutyrate. Analysis of the data indicated that this taste-masked formulation of sodium phenylbutyrate granules improved quality of life for urea-cycle disorder patients. Furthermore, a postmarketing report on the use of the product has confirmed the previous observations of improved compliance, efficacy, and safety with this taste-masked formulation of sodium phenylbutyrate.

  4. Active transportation to school in Canadian youth: should injury be a concern?

    Science.gov (United States)

    Gropp, Kathleen; Janssen, Ian; Pickett, William

    2013-02-01

    Active transportation to school provides a means for youth to incorporate physical activity into their daily routines, and this has obvious benefits for child health. Studies of active transportation have rarely focused on the negative health effects in terms of injury. This cross-sectional study is based on the 2009/10 Canadian Health Behaviour in School-Aged Children survey. A sample of children aged 11-15 years (n=20 076) was studied. Multi-level logistic regression was used to examine associations between walking or bicycling to school and related injury. Regular active transportation to school at larger distances (approximately >1.6 km; 1.0 miles) was associated with higher relative odds of active transportation injury (OR: 1.52; 95% CI 1.08 to 2.15), with a suggestion of a dose-response relationship between longer travel distances and injury (p=0.02). Physical activity interventions for youth should encourage participation in active transportation to school, while also recognising the potential for unintentional injury.

  5. Activated human CD4 T cells express transporters for both cysteine and cystine

    DEFF Research Database (Denmark)

    Levring, Trine Bøegh; Hansen, Ann Kathrine; Nielsen, Bodil Lisbeth;

    2012-01-01

    Because naïve T cells are unable to import cystine due to the absence of cystine transporters, it has been suggested that T cell activation is dependent on cysteine generated by antigen presenting cells. The aim of this study was to determine at which phases during T cell activation exogenous...... cystine/cysteine is required and how T cells meet this requirement. We found that early activation of T cells is independent of exogenous cystine/cysteine, whereas T cell proliferation is strictly dependent of uptake of exogenous cystine/cysteine. Naïve T cells express no or very low levels of both...... cystine and cysteine transporters. However, we found that these transporters become strongly up-regulated during T cell activation and provide activated T cells with the required amount of cystine/cysteine needed for T cell proliferation. Thus, T cells are equipped with mechanisms that allow T cell...

  6. Demand-responsive public transportation re-scheduling for adjusting to the joint leisure activity demand

    Directory of Open Access Journals (Sweden)

    Konstantinos Gkiotsalitis

    2016-10-01

    Full Text Available Fixed daily trips such as trips to work/school have fixed departure/arrival times and destination points. The recurrent nature of fixed activities facilitates individuals on making more well-informed decisions about the transport mode selection. On the contrary, selecting a transportation mode for non-recurrent leisure trips, which can account for up to 60% of trips in some cities (Transport for London, 2014, is a more complex task due to the fact that individuals have little knowledge about the alternative modal options. In this paper, we try to improve the operations of demand-responsive public transportation systems by increasing their service quality and their ridership related to joint-leisure-trips via timetable rescheduling. First, we model the public transport service re-scheduling problem considering operational regulations and the quality of service. Then, a sequential heuristic method is introduced for re-scheduling the timetables of demand-responsive public transport modes in near-real time and accommodating the joint leisure activity demand without deteriorating the quality of service. The public transport re-scheduling for increasing the joint leisure activity ridership was tested in a case study using user-generated data from social media in Stockholm and the General Transit Feed Specification (GTFS data from Sweden focusing especially on central bus lines 1 and 4.

  7. Active transmembrane drug transport in microgravity: a validation study using an ABC transporter model [v1; ref status: indexed, http://f1000r.es/41n

    Directory of Open Access Journals (Sweden)

    Sergi Vaquer

    2014-08-01

    Full Text Available Abstract Microgravity has been shown to influence the expression of ABC (ATP-Binding Cassette transporters in bacteria, fungi and mammals, but also to modify the activity of certain cellular components with structural and functional similarities to ABC transporters. Changes in activity of ABC transporters could lead to important metabolic disorders and undesired pharmacological effects during spaceflights. However, no current means exist to study the functionality of these transporters in microgravity. To this end, a Vesicular Transport Assay® (Solvo Biotechnology, Hungary was adapted to evaluate multi-drug resistance-associated protein 2 (MRP2 trans-membrane estradiol-17-β-glucuronide (E17βG transport activity, when activated by adenosine-tri-phosphate (ATP during parabolic flights. Simple diffusion, ATP-independent transport and benzbromarone inhibition were also evaluated. A high accuracy engineering system was designed to perform, monitor and synchronize all procedures. Samples were analysed using a validated high sensitivity drug detection protocol. Experiments were performed in microgravity during parabolic flights, and compared to 1g on ground results using identical equipment and procedures in all cases. Our results revealed that sufficient equipment accuracy and analytical sensitivity were reached to detect transport activity in both gravitational conditions. Additionally, transport activity levels of on ground samples were within commercial transport standards, proving the validity of the methods and equipment used. MRP2 net transport activity was significantly reduced in microgravity, so was signal detected in simple diffusion samples. Ultra-structural changes induced by gravitational stress upon vesicle membranes or transporters could explain the current results, although alternative explanations are possible. Further research is needed to provide a conclusive answer in this regard. Nevertheless, the present validated technology

  8. Removal of urea in a wearable dialysis device: a reappraisal of electro-oxidation.

    Science.gov (United States)

    Wester, Maarten; Simonis, Frank; Lachkar, Nadia; Wodzig, Will K; Meuwissen, Frank J; Kooman, Jeroen P; Boer, Walther H; Joles, Jaap A; Gerritsen, Karin G

    2014-12-01

    A major challenge for a wearable dialysis device is removal of urea, as urea is difficult to adsorb while daily production is very high. Electro-oxidation (EO) seems attractive because electrodes are durable, small, and inexpensive. We studied the efficacy of urea oxidation, generation of chlorine by-products, and their removal by activated carbon (AC). EO units were designed. Three electrode materials (platinum, ruthenium oxide, and graphite) were compared in single pass experiments using urea in saline solution. Chlorine removal by AC in series with EO by graphite electrodes was tested. Finally, urea-spiked bovine blood was dialyzed and dialysate was recirculated in a dialysate circuit with AC in series with an EO unit containing graphite electrodes. Platinum electrodes degraded more urea (21 ± 2 mmol/h) than ruthenium oxide (13 ± 2 mmol/h) or graphite electrodes (13 ± 1 mmol/h). Chlorine generation was much lower with graphite (13 ± 4 mg/h) than with platinum (231 ± 22 mg/h) or ruthenium oxide electrodes (129 ± 12 mg/h). Platinum and ruthenium oxide electrodes released platinum (4.1 [3.9-8.1] umol/h) and ruthenium (83 [77-107] nmol/h), respectively. AC potently reduced dialysate chlorine levels to Urea was removed from blood by EO at constant rate (9.5 ± 1.0 mmol/h). EO by graphite electrodes combined with AC shows promising urea removal and chlorine release complying with Association for the Advancement of Medical Instrumentation standards, and may be worth further exploring for dialysate regeneration in a wearable system.

  9. High-level expression and characterization of recombinant acid urease for enzymatic degradation of urea in rice wine.

    Science.gov (United States)

    Yang, Yuqing; Kang, Zhen; Zhou, Jianli; Chen, Jian; Du, Guocheng

    2015-01-01

    Ethylcarbamate, a carcinogenic compound, is formed from urea and ethanol in rice wine, and enzymatic elimination of urea is always attractive. In the present work, we amplified the acid urease gene cluster ureABCEFGD from Lactobacillus reuteri CICC6124 and constructed robust Lactococcus lactis cell factories for the production of acid urease. The titer of the recombinant acid urease was increased from 1,550 to 11,560 U/L by optimization of the cultivation process. Meanwhile, the enzyme showed satisfied properties toward urea elimination in the rice wine model system. By incubating the enzyme (50 U/L) at 20 °C for 60 h, about 95.8% of urea in rice wine was removed. Interestingly, this acid urease also exhibited activity toward ethylcarbamate. The results demonstrated that this recombinant acid urease has great potential in the elimination of urea in rice wine.

  10. Salt potentiates methylamine counteraction system to offset the deleterious effects of urea on protein stability and function.

    Directory of Open Access Journals (Sweden)

    Safikur Rahman

    Full Text Available Cellular methylamines are osmolytes (low molecular weight organic compounds believed to offset the urea's harmful effects on the stability and function of proteins in mammalian kidney and marine invertebrates. Although urea and methylamines are found at 2:1 molar ratio in tissues, their opposing effects on protein structure and function have been questioned on several grounds including failure to counteraction or partial counteraction. Here we investigated the possible involvement of cellular salt, NaCl, in urea-methylamine counteraction on protein stability and function. We found that NaCl mediates methylamine counteracting system from no or partial counteraction to complete counteraction of urea's effect on protein stability and function. These conclusions were drawn from the systematic thermodynamic stability and functional activity measurements of lysozyme and RNase-A. Our results revealed that salts might be involved in protein interaction with charged osmolytes and hence in the urea-methylamine counteraction.

  11. The Kinetics of Urea in the Body after Liver Resection in the Experiment

    Directory of Open Access Journals (Sweden)

    P. N. Savilov

    2016-01-01

    Full Text Available Purpose. To study urea kinetics in the body after liver resection in the experiment.Material and Methods. Experiments were carried out on 45 white female rats weighing between 180 g and 220 g. Liver resection (LR was performed under ester anesthesia, wherein 15—20% of the organ weight was removed. Urea content was studied in biological fluids (arterial blood, venous — v.porta, v.hepatica, v.renalis — blood, choledochal bile, urine, and tissues of visceral organs (the thyroid gland, lungs, heart, liver, kidneys, spleen, stomach, intestine on days 3, 7, and 14 after LR. Results. LR, while reducing the urea content in the v. hepatica blood, does not lead to similar changes in the arterial blood. This is accompanied by increased urea reabsorption in kidneys and higher v.porta blood urea content, which, depending on the postoperative time, results either from reduced urea excretion into the small intestine lumen or from its greater production by enterocytes followed by metabolite intake into the portal blood flow. The urea intake from hepatocytes into the hepatic bile ducts did not change on day 3 after LR; however, it increased on day 7 and slowed down on day 14. LR caused no changes in the gastric tissues urea content; never theless, it led to its increased content in the duodenal and colonic tissues. Without affecting the cardiac muscleurea content, LR entailed its increase in the lungs and thyroid gland on postoperative days 3, 7, and 14. At the background of absence of similar changes in the arterial blood data indicates promotion of urea production by the cells of these organs or metabolite retention therein.Conclusions. LR not only changes urea kinetics in the portal system organs, but also activates extrahepatic mechanisms aimed at preventing development of the arterial blood urea deficit because of its abnormal intake from the resected organ into the central blood flow.

  12. Imaging Renal Urea Handling in Rats at Millimeter Resolution using Hyperpolarized Magnetic Resonance Relaxometry

    CERN Document Server

    Reed, Galen D; Verkman, Alan S; Koelsch, Bertram L; Chaumeil, Myriam M; Lustig, Michael; Ronen, Sabrina M; Sands, Jeff M; Larson, Peder E Z; Wang, Zhen J; Larsen, Jan Henrik Ardenkjær; Vigneron, Daniel B

    2015-01-01

    \\textit{In vivo} spin spin relaxation time ($T_2$) heterogeneity of hyperpolarized \\textsuperscript{13}C urea in the rat kidney was investigated. Selective quenching of the vascular hyperpolarized \\textsuperscript{13}C signal with a macromolecular relaxation agent revealed that a long-$T_2$ component of the \\textsuperscript{13}C urea signal originated from the renal extravascular space, thus allowing the vascular and renal filtrate contrast agent pools of the \\textsuperscript{13}C urea to be distinguished via multi-exponential analysis. The $T_2$ response to induced diuresis and antidiuresis was performed with two imaging agents: hyperpolarized \\textsuperscript{13}C urea and a control agent hyperpolarized bis-1,1-(hydroxymethyl)-1-\\textsuperscript{13}C-cyclopropane-$^2\\textrm{H}_8$. Large $T_2$ increases in the inner-medullar and papilla were observed with the former agent and not the latter during antidiuresis suggesting that $T_2$ relaxometry may be used to monitor the inner-medullary urea transporter (UT)-...

  13. Elevated osmolytes in rainbow smelt: the effects of urea, glycerol and trimethylamine oxide on muscle contractile properties.

    Science.gov (United States)

    Coughlin, David J; Long, Gabrielle M; Gezzi, Nicole L; Modi, Parth M; Woluko, Kossivi N

    2016-04-01

    Rainbow smelt, Osmerus mordax, experience a wide range of temperatures in their native habitat. In response to cold, smelt express anti-freeze proteins and the osmolytes glycerol, trimethylamine N-oxide (TMAO) and urea to avoid freezing. The physiological influences of these osmolytes are not well understood. Urea destabilizes proteins, while TMAO counteracts the protein-destabilizing forces of urea. The influence of glycerol on muscle function has not been explored. We examined the effects of urea, glycerol and TMAO through muscle mechanics experiments with treatments of the three osmolytes at physiological concentrations. Experiments were carried out at 10°C. The contractile properties of fast-twitch muscle bundles were determined in physiological saline and in the presence of 50 mmol l(-1)urea, 50 mmol l(-1)TMAO and/or 200 mmol l(-1)glycerol in saline. Muscle exposed to urea and glycerol produced less force and displayed slower contractile properties. However, treatment with TMAO led to higher force and faster relaxation by muscle bundles. TMAO increased power production during cyclical activity, while urea and glycerol led to reduced oscillatory power output. When muscle bundles were exposed to a combination of the three osmolytes, they displayed little change in contraction kinetics relative to control, although power output under lower oscillatory conditions was enhanced while maximum power output was reduced. The results suggest that maintenance of muscle function in winter smelt requires a balanced combination of urea, glycerol and TMAO.

  14. Effect of urea and nickel on growth, physiological traits and total nitrogen concentration of lettuce in hydroponic culture

    Directory of Open Access Journals (Sweden)

    H. Nazari Mamaqani

    2016-02-01

    Full Text Available Nitrate fertilizers are common source of nitrogen (N in nutrient solutions. Substitution of urea with nitrate could reduce this dependence. Also, nickel (Ni is essential for activation of urease in plants fed with urea. For this aim, a factorial experiment was conducted in a completely randomized design with four replicates. Urea in five levels (0, 25, 50, 75 and 100 mg/L and Ni in two levels (0 and 2 mg/L were used for lettuce (Lactuca sativa cv. Siyahoo in hydroponics. The results showed that the highest fresh and dry weight of leaves and stem were obtained in 50 mg/L urea treatment. Leaf area was reduced in treatments having more than 25 mg/L urea concentration. The highest chlorophyll index and maximal quantum yield of PS II photochemistry efficiency (Fv/Fm were obtained in 100 and 75 mg/L urea, respectively. Total nitrogen concentration of leaves was increased significantly with increasing urea concentration; plants treated with 100 mg/L urea had the highest total nitrogen concentration. Nickel application reduced yield and physiological traits of lettuce; while it had no significant effect on total nitrogen concentration.

  15. Regulation of human hepatic drug transporter activity and expression by diesel exhaust particle extract.

    Directory of Open Access Journals (Sweden)

    Marc Le Vee

    Full Text Available Diesel exhaust particles (DEPs are common environmental air pollutants primarily affecting the lung. DEPs or chemicals adsorbed on DEPs also exert extra-pulmonary effects, including alteration of hepatic drug detoxifying enzyme expression. The present study was designed to determine whether organic DEP extract (DEPe may target hepatic drug transporters that contribute in a major way to drug detoxification. Using primary human hepatocytes and transporter-overexpressing cells, DEPe was first shown to strongly inhibit activities of the sinusoidal solute carrier (SLC uptake transporters organic anion-transporting polypeptides (OATP 1B1, 1B3 and 2B1 and of the canalicular ATP-binding cassette (ABC efflux pump multidrug resistance-associated protein 2, with IC50 values ranging from approximately 1 to 20 μg/mL and relevant to environmental exposure situations. By contrast, 25 μg/mL DEPe failed to alter activities of the SLC transporter organic cation transporter (OCT 1 and of the ABC efflux pumps P-glycoprotein and bile salt export pump (BSEP, whereas it only moderately inhibited those of sodium taurocholate co-transporting polypeptide and of breast cancer resistance protein (BCRP. Treatment by 25 μg/mL DEPe was next demonstrated to induce expression of BCRP at both mRNA and protein level in cultured human hepatic cells, whereas it concomitantly repressed mRNA expression of various transporters, including OATP1B3, OATP2B1, OCT1 and BSEP. Such changes in transporter expression were found to be highly correlated to those caused by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, a reference activator of the aryl hydrocarbon receptor (AhR pathway. This suggests that DEPe, which is enriched in known ligands of AhR like polycyclic aromatic hydrocarbons, alters drug transporter expression via activation of the AhR cascade. Taken together, these data established human hepatic transporters as targets of organic chemicals containing in DEPs, which may contribute

  16. Transport of Optically Active Particles from the Surface Mixed Layer

    Science.gov (United States)

    2005-09-30

    aragonite in the form of abundant coccoliths and coccospheres, and occasional forams, pteropods and larval gastropods . The δ18O signature of the 2003... APPLICATIONS These experiments were designed to identify the major loss terms of optically-active particles. This indeed was accomplished. Such

  17. The effects of urea and n-propanol on collagen denaturation: using DSC, circular dicroism and viscosity

    Energy Technology Data Exchange (ETDEWEB)

    Usha, R.; Ramasami, T

    2004-01-30

    The effect of urea and n-propanol on circular dichroism (CD) and viscosity of purified type1 collagen solution at various temperatures and differential scanning calorimetry (DSC) of rat-tail tendon (RTT) collagen fibre have been studied. CD reveals a spectrum with a positive peak at around 220 nm and a negative peak at 200 nm characteristics of collagen triple helix. The molar ellipticity decreases as the concentration of urea increases up to particular concentration (collagen solution treated with 265 {mu}M of urea) and after that it increases (collagen solution treated with 500 {mu}M of urea). There is a linear decrease in molar ellipticity as the concentration of n-propanol increases. Denaturation temperature of urea and n-propanol treated with purified collagen solution has been studied using viscosity method. Additives such as urea and n-propanol decrease the thermal stability of collagen triple helix in solution and in RTT collagen fibre. Thermal helix to coil transition of urea and n-propanol treated collagen depends on the degree of hydration and the concentration of these additives. Thermodynamic parameters such as the peak temperature, enthalpy of activation, and energy of activation for collagen-gelatin transition for native, urea and n-propanol treated RTT collagen fibre has been calculated using DSC. The change in the thermodynamic parameters has been observed for native, urea and n-propanol treated RTT collagen fibres. The experimental results show that the change in the water structure, dehydration and desolvation induced by different additives such as urea and n-propanol on RTT may vary with the type of denaturation.

  18. Activity transport models for PWR primary circuits; PWR-ydinvoimalaitoksen primaeaeripiirin aktiivisuuskulkeutumismallit

    Energy Technology Data Exchange (ETDEWEB)

    Tanner, V.; Rosenberg, R. [VTT Chemical Technology, Otaniemi (Finland)

    1995-03-01

    The corrosion products activated in the primary circuit form a major source of occupational radiation dose in the PWR reactors. Transport of corrosion activity is a complex process including chemistry, reactor physics, thermodynamics and hydrodynamics. All the mechanisms involved are not known and there is no comprehensive theory for the process, so experimental test loops and plant data are very important in research efforts. Several activity transport modelling attempts have been made to improve the water chemistry control and to minimise corrosion in PWR`s. In this research report some of these models are reviewed with special emphasis on models designed for Soviet VVER type reactors. (51 refs., 16 figs., 4 tabs.).

  19. Glycerol and urea can be used to increase skin permeability in reduced hydration conditions.

    Science.gov (United States)

    Björklund, Sebastian; Engblom, Johan; Thuresson, Krister; Sparr, Emma

    2013-12-18

    The natural moisturizing factor (NMF) is a group of hygroscopic molecules that is naturally present in skin and protects from severe drying. Glycerol and urea are two examples of NMF components that are also used in skin care applications. In the present study, we investigate the influence of glycerol and urea on the permeability of a model drug (metronidazole, Mz) across excised pig skin membranes at different hydrating conditions. The degree of skin hydration is regulated by the gradient in water activity across the membrane, which in turn depends on the water activity of the formulation in contact with the skin membrane. Here, we determine the water activity of all formulations employed using an isothermal calorimetric method. Thus, the gradient in water activity is controlled by a novel experimental set-up with well-defined boundary conditions on both sides of the skin membrane. The results demonstrate that glycerol and urea can retain high steady state flux of Mz across skin membranes at dehydrating conditions, which otherwise would decrease the permeability due to dehydration. X-ray diffraction measurements are performed to give insight into the effects of glycerol and urea on SC molecular organization. The novel steady state flux results can be related to the observation that water, glycerol, and urea all affect the structural features of the SC molecular components in a similar manner.

  20. Prolactin increases hepatic Na+/taurocholate co-transport activity and messenger RNA post partum.

    Science.gov (United States)

    Ganguly, T C; Liu, Y; Hyde, J F; Hagenbuch, B; Meier, P J; Vore, M

    1994-01-01

    We have shown that Na+/taurocholate co-transport activity is decreased in pregnancy, but rebounds post partum relative to non-pregnant controls, and that activity can be increased by treatment with ovine prolactin [Ganguly, Hyde and Vore (1993) J. Pharmacol. Exp. Ther. 267, 82-87]. To determine the basis for these effects, Na+/taurocholate co-transport was determined in purified basolateral liver plasma-membrane (bLPM) vesicles and compared with steady-state mRNA levels encoding the Na+/taurocholate-co-transporting polypeptide (Ntcp) in non-pregnant controls, pregnant rats (19-20 days pregnant), rats post partum (48 h post partum) and rats post partum treated with bromocriptine to inhibit prolactin secretion. Na+/taurocholate co-transport activity (nmol/5 s per mg of protein) in bLPM was decreased from 10.4 +/- 1.8 in non-pregnant controls to 7.9 +/- 0.6 in bLPM in pregnant rats, but rebounded to 17.5 +/- 1.3 post partum; treatment of rats post partum with bromocriptine to inhibit prolactin secretion decreased activity to 14.1 +/- 0.9. Northern and slot-blot analyses revealed similar changes in mRNA for Ntcp, so that a positive correlation was observed between Na+/taurocholate co-transport activity and Ntcp mRNA. Furthermore, treatment of ovariectomized rats with ovine prolactin increased Ntcp mRNA 10-fold compared with solvent-treated controls, consistent with the 2-fold increase in Vmax, for Na+/taurocholate co-transport in isolated hepatocytes. These data are the first to demonstrate endogenous physiological regulation by prolactin of Ntcp mRNA in parallel with Na+/taurocholate co-transport activity. Images Figure 2 PMID:7945260

  1. Polystyrene nanoparticles activate ion transport in human airway epithelial cells

    Directory of Open Access Journals (Sweden)

    McCarthy J

    2011-06-01

    Full Text Available J McCarthy1, X Gong2, D Nahirney2, M Duszyk2, MW Radomski11School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, Dublin, Ireland; 2Department of Physiology, University of Alberta, Edmonton, Alberta, CanadaBackground: Over the last decade, nanotechnology has provided researchers with new nanometer materials, such as nanoparticles, which have the potential to provide new therapies for many lung diseases. In this study, we investigated the acute effects of polystyrene nanoparticles on epithelial ion channel function.Methods: Human submucosal Calu-3 cells that express cystic fibrosis transmembrane conductance regulator (CFTR and baby hamster kidney cells engineered to express the wild-type CFTR gene were used to investigate the actions of negatively charged 20 nm polystyrene nanoparticles on short-circuit current in Calu-3 cells by Ussing chamber and single CFTR Cl- channels alone and in the presence of known CFTR channel activators by using baby hamster kidney cell patches.Results: Polystyrene nanoparticles caused sustained, repeatable, and concentration-dependent increases in short-circuit current. In turn, these short-circuit current responses were found to be biphasic in nature, ie, an initial peak followed by a plateau. EC50 values for peak and plateau short-circuit current responses were 1457 and 315.5 ng/mL, respectively. Short-circuit current was inhibited by diphenylamine-2-carboxylate, a CFTR Cl- channel blocker. Polystyrene nanoparticles activated basolateral K+ channels and affected Cl- and HCO3- secretion. The mechanism of short-circuit current activation by polystyrene nanoparticles was found to be largely dependent on calcium-dependent and cyclic nucleotide-dependent phosphorylation of CFTR Cl- channels. Recordings from isolated inside-out patches using baby hamster kidney cells confirmed the direct activation of CFTR Cl- channels by the nanoparticles.Conclusion: This is the first study to identify

  2. Stability of urea in solution and pharmaceutical preparations.

    Science.gov (United States)

    Panyachariwat, Nattakan; Steckel, Hartwig

    2014-01-01

    The stability of urea in solution and pharmaceutical preparations was analyzed as a function of temperature (25°-60°C), pH (3.11-9.67), and initial urea concentration (2.5%-20%). This study was undertaken to (i) obtain more extensive, quantitative information relative to the degradation of urea in both aqueous and non-aqueous solutions and in pharmaceutical preparations, and (ii) test the effects of initial urea concentration, pH, buffer, and temperature values on urea degradation. The stability analysis shows that urea is more stable at the pH range of 4-8 and the stability of urea decreases by increase in temperature for all pH values. Within the experimental range of temperature and initial urea concentration values, the lowest urea degradation was found with lactate buffer pH 6.0. The urea decomposition rate in solution and pharmaceutical preparations shows the dependence of the initial urea concentrations. At higher initial urea concentrations, the rate of degradation is a decreasing function with time. This suggests that the reverse reaction is a factor in the degradation of concentrated urea solution. For non-aqueous solvents, isopropanol showed the best effort in retarding the decomposition of urea. Since the losses in urea is directly influenced by its stability at a given temperature and pH, the stability analysis of urea by the proposed model can be used to prevent the loss and optimize the operating condition for urea-containing pharmaceutical preparations.

  3. Role of urea on recombinant Apo A-I stability and its utilization in anion exchange chromatography.

    Science.gov (United States)

    Angarita, Monica; Arosio, Paolo; Müller-Späth, Thomas; Baur, Daniel; Falkenstein, Roberto; Kuhne, Wolfgang; Morbidelli, Massimo

    2014-08-08

    Apolipoprotein A-I (Apo A-I) is an important lipid-binding protein involved in the transport and metabolism of cholesterol. High protein purity, in particular with respect to endotoxins is required for therapeutic applications. The use of urea during the purification process of recombinant Apo A-I produced in Escherichia coli has been suggested so as to provide high endotoxin clearance. In this work, we show that urea can be used as a sole modifier during the ion exchange chromatographic purification of Apo A-I and we investigate the molecular mechanism of elution by correlating the effect of urea on self-association, conformation and adsorption equilibrium properties of a modified model Apo A-I. In the absence of urea the protein was found to be present as a population of oligomers represented mainly by trimers, hexamers and nonamers. The addition of urea induced oligomer dissociation and protein structure unfolding. We correlated the changes in protein association and conformation with variations of the adsorption equilibrium of the protein on a strong anion exchanger. It was confirmed that the adsorption isotherms, described by a Langmuir model, were dependent on both protein and urea concentrations. Monomers, observed at low urea concentration (0.5M), were characterized by larger binding affinity and adsorption capacity compared to both protein oligomers (0M) and unfolded monomers (2-8M). The reduction of both the binding strength and maximum adsorption capacity at urea concentrations larger than 0.5M explains the ability of urea of inducing elution of the protein from the ion exchange resin. The dissociation of the protein complexes occurring during the elution could likely be the origin of the effective clearance of endotoxins originally trapped inside the oligomers.

  4. Hydroponics versus field lysimeter studies of urea, ammonium and nitrate uptake by oilseed rape (Brassica napus L.).

    Science.gov (United States)

    Arkoun, Mustapha; Sarda, Xavier; Jannin, Laëtitia; Laîné, Philippe; Etienne, Philippe; Garcia-Mina, José-Maria; Yvin, Jean-Claude; Ourry, Alain

    2012-09-01

    N-fertilizer use efficiencies are affected by their chemical composition and suffer from potential N-losses by volatilization. In a field lysimeter experiment, (15)N-labelled fertilizers were used to follow N uptake by Brassica napus L. and assess N-losses by volatilization. Use of urea with NBPT (urease inhibitor) showed the best efficiency with the lowest N losses (8% of N applied compared with 25% with urea alone). Plants receiving ammonium sulphate, had similar yield achieved through a better N mobilization from vegetative tissues to the seeds, despite a lower N uptake resulting from a higher volatilization (43% of applied N). Amounts of (15)N in the plant were also higher when plants were fertilized with ammonium nitrate but N-losses reached 23% of applied N. In parallel, hydroponic experiments showed a deleterious effect of ammonium and urea on the growth of oilseed rape. This was alleviated by the nitrate supply, which was preferentially taken up. B. napus was also characterized by a very low potential for urea uptake. BnDUR3 and BnAMT1, encoding urea and ammonium transporters, were up-regulated by urea, suggesting that urea-grown plants suffered from nitrogen deficiency. The results also suggested a role for nitrate as a signal for the expression of BnDUR3, in addition to its role as a major nutrient. Overall, the results of the hydroponic study showed that urea itself does not contribute significantly to the N nutrition of oilseed rape. Moreover, it may contribute indirectly since a better use efficiency for urea fertilizer, which was further increased by the application of a urease inhibitor, was observed in the lysimeter study.

  5. Mechanism of active transport: free energy dissipation and free energy transduction.

    OpenAIRE

    Tanford, C

    1982-01-01

    The thermodynamic pathway for "chemiosmotic" free energy transduction in active transport is discussed with an ATP-driven Ca2+ pump as an illustrative example. Two innovations are made in the analysis. (i) Free energy dissipated as heat is rigorously excluded from overall free energy bookkeeping by focusing on the dynamic equilibrium state of the chemiosmotic process. (ii) Separate chemical potential terms for free energy donor and transported ions are used to keep track of the thermodynamic ...

  6. Functional materials from self-assembled bis-urea macrocycles.

    Science.gov (United States)

    Shimizu, Linda S; Salpage, Sahan R; Korous, Arthur A

    2014-07-15

    CONSPECTUS: This Account highlights the work from our laboratories on bis-urea macrocycles constructed from two C-shaped spacers and two urea groups. These simple molecular units assembled with high fidelity into columnar structures guided by the three-centered urea hydrogen bonding motif and aryl stacking interactions. Individual columns are aligned and closely packed together to afford functional and homogeneous microporous crystals. This approach allows for precise and rational control over the dimensions of the columnar structure simply by changing the small molecular unit. When the macrocyclic unit lacks a cavity, columnar assembly gives strong pillars. Strong pillars with external functional groups such as basic lone pairs can expand like clays to accept guests between the pillars. Macrocycles that contain sizable interior cavities assemble into porous molecular crystals with aligned, well-defined columnar pores that are accessible to gases and guests. Herein, we examine the optimal design of the macrocyclic unit that leads to columnar assembly in high fidelity and probe the feasibility of incorporating a second functional group within the macrocycles. The porous molecular crystals prepared through the self-assembly of bis-urea macrocycles display surface areas similar to zeolites but lower than MOFs. Their simple one-dimensional channels are well-suited for studying binding, investigating transport, diffusion and exchange, and monitoring the effects of encapsulation on reaction mechanism and product distribution. Guests that complement the size, shape, and polarity of the channels can be absorbed into these porous crystals with repeatable stoichiometry to form solid host-guest complexes. Heating or extraction with an organic solvent enables desorption or removal of the guest and subsequent recovery of the solid host. Further, these porous crystals can be used as containers for the selective [2 + 2] cycloadditions of small enones such as 2-cyclohexenone or 3

  7. Glucose elevates NITRATE TRANSPORTER2.1 protein levels and nitrate transport activity independently of its HEXOKINASE1-mediated stimulation of NITRATE TRANSPORTER2.1 expression.

    Science.gov (United States)

    de Jong, Femke; Thodey, Kate; Lejay, Laurence V; Bevan, Michael W

    2014-01-01

    Mineral nutrient uptake and assimilation is closely coordinated with the production of photosynthate to supply nutrients for growth. In Arabidopsis (Arabidopsis thaliana), nitrate uptake from the soil is mediated by genes encoding high- and low-affinity transporters that are transcriptionally regulated by both nitrate and photosynthate availability. In this study, we have studied the interactions of nitrate and glucose (Glc) on gene expression, nitrate transport, and growth using glucose-insensitive2-1 (gin2-1), which is defective in sugar responses. We confirm and extend previous work by showing that HEXOKINASE1-mediated oxidative pentose phosphate pathway (OPPP) metabolism is required for Glc-mediated NITRATE TRANSPORTER2.1 (NRT2.1) expression. Treatment with pyruvate and shikimate, two products derived from intermediates of the OPPP that are destined for amino acid production, restores wild-type levels of NRT2.1 expression, suggesting that metabolites derived from OPPP metabolism can, together with Glc, directly stimulate high levels of NRT2.1 expression. Nitrate-mediated NRT2.1 expression is not influenced by gin2-1, showing that Glc does not influence NRT2.1 expression through nitrate-mediated mechanisms. We also show that Glc stimulates NRT2.1 protein levels and transport activity independently of its HEXOKINASE1-mediated stimulation of NRT2.1 expression, demonstrating another possible posttranscriptional mechanism influencing nitrate uptake. In gin2-1 plants, nitrate-responsive biomass growth was strongly reduced, showing that the supply of OPPP metabolites is essential for assimilating nitrate for growth.

  8. Facile Synthesis of Ureas in Ionic Liquid

    Institute of Scientific and Technical Information of China (English)

    Wei Xing QIAN; Feng Yang JU; Yong Min ZHANG; Wei Liang BAO

    2004-01-01

    The reaction of isocyanates with aliphatic and aromatic amines in the 1-n-butyl-3- methylimidazolium tetrafluoroborate (bmimBF4) ionic liquid in good to excellent yields is described. Due to its insolubility, the desired urea solids could be recovered by simple filtration from the ionic liquid after reaction.

  9. Urea Decomposition Method to Synthesize Hydrotalcites

    Institute of Scientific and Technical Information of China (English)

    Piao Ping YANG; Jian Feng YU; Tong Hao WU; Guo Zong LIU; Tae Sun CHANG; Dong Koo LEE; Deug Hee CHO

    2004-01-01

    The urea decomposition property at high temperature has been used to control the pH value in the synthesis of layer compounds. The hydrotalcites of Mg-Al and Ni-Al with high crystallinity were synthesized by using this property.

  10. Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model.

    Science.gov (United States)

    Li, Guo-Bo; Ma, Shuang; Yang, Ling-Ling; Ji, Sen; Fang, Zhen; Zhang, Guo; Wang, Li-Jiao; Zhong, Jie-Min; Xiong, Yu; Wang, Jiang-Hong; Huang, Shen-Zhen; Li, Lin-Li; Xiang, Rong; Niu, Dawen; Chen, Ying-Chun; Yang, Sheng-Yong

    2016-09-22

    Psoriasis is a chronic T-cell-mediated autoimmune disease, and FMS-like tyrosine kinase 3 (FLT3) has been considered as a potential molecular target for the treatment of psoriasis. In this investigation, structural optimization was performed on a lead compound, 1-(4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea (1), which showed a moderate inhibitory activity againt FLT3. A series of pyrazolo[3,4-d]pyrimidine derivatives were synthesized, and structure-activity relationship analysis led to the discovery of a number of potent FLT3 inhibitors. One of the most active compounds, 1-(4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)-3-fluorophenyl)-3-(5-tert-butylisoxazol-3-yl)urea (18b), was then chosen for in-depth antipsoriasis studies because this compound displayed the highest potency in a preliminary antipsoriasis test. Compound 18b exhibited significant antipsoriatic effects in the K14-VEGF transgenic mouse model of psoriasis, and no recurrence was found 15 days later after the last administration. Detailed mechanisms of action of compound 18b were also investigated. Collectively, compound 18b could be a potential drug candidate for psoriasis treatment.

  11. Packaging design criteria (onsite) project W-520 immobilized low-activity waste transportation system

    Energy Technology Data Exchange (ETDEWEB)

    BOEHNKE, W.M.

    2001-10-16

    A plan is currently in place to process the high-level radioactive wastes that resulted from uranium and plutonium recovery operations from Spent Nuclear Fuel at the Hanford Site, Richland, Washington. Currently, millions of gallons of high-level radioactive waste in the form of liquids, sludges, and saltcake are stored in many large underground tanks onsite. This waste will be processed and separated into high-level and low-activity fractions. Both fractions will then be vitrified (i.e., blended with molten borosilicate glass) in order to encapsulate the toxic radionuclides. The immobilized low-activity waste (ILAW) glass will be poured into LAW canisters, allowed to cool and harden to solid form, sealed by welding, and then transported to a double-lined trench in the 200 East Area for permanent disposal. This document presents the packaging design criteria (PDC) for an onsite LAW transportation system, which includes the ILAW canister, ILAW package, and transport vehicle and defines normal and accident conditions. This PDC provides the basis for the ILAW onsite transportation system design and fabrication and establishes the transportation safety criteria that the design will be evaluated against in the Package Specific Safety Document (PSSD). It provides the criteria for the ILAW canister, cask and transport vehicles and defines normal and accident conditions. The LAW transportation system is designed to transport stabilized waste from the vitrification facility to the ILAW disposal facility developed by Project W-520. All ILAW transport will take place within the 200 East Area (all within the Hanford Site).

  12. Metal dispersion and transportational activities using food crops as biomonitors.

    Science.gov (United States)

    Ward, N I; Savage, J M

    1994-05-23

    The multielement (Al, Ca, Cd, Ce, Cr, Cu, Fe, Mg, Mn, Ni, Pb, Si, and Zn) levels of various common vegetables (bean, broccoli, cabbage, cauliflower, lettuce, marrow, onion, parsnip, spinach, sprouts, sweet corn, and tomato); fruits (grape and strawberry); herbs (garlic, lemon balm, marjoram, mint, rosemary and tarragon); local pasture species and surface soils collected from a commercial garden centre located within a distance of 30 m of the London Orbital Motorway (M25) is presented. Comparative values are given from a background area, namely a domestic garden located in the North Yorkshire Dales National Park area. Analysis was undertaken by inductively coupled plasma optical emission spectrometry (ICP-OES) and inductively coupled plasma-source mass spectrometry (ICP-MS) with quality control assessment using four international biological reference materials; BCR:CRM 62 Olive Leaves, NIST 1575 Pine Needles, NIST 1573 Tomato Leaves, and NIST 1572 Citrus Leaves. Inter-analytical method comparison is given using two methods of ICP-MS; namely conventional pneumatic nebulisation of sample solution, and direct solids analysis by laser ablation; and neutron activation analysis methods (NAA). For the elements listed there is a good precision obtained by ICP-MS and NAA. In particular levels of herbs > vegetables > cereals > fruits. Measured values are in good agreement with reported literature values. The lowest Pb values are for marrow, lettuce, tomato and sweet corn samples (approximately 0.001-0.021 microgram/g). 'Green' leaf material levels were approximately 0.02-0.10 microgram/g (i.e. sprouts and cabbage). Root vegetables contain higher levels, approximately 0.02-0.125 microgram/g (especially carrot), reflecting possible metal uptake from soil. The highest vegetable Pb values are for leek and onion (approximately 0.35 microgram/g). Background values are also provided for nineteen elements (Al, As, B, Ba, Br, Cd, Co, Cr, Cu, Fe, Li, Mn, Mo, Ni, Rb, Se, Sr, V, and Zn

  13. Control of ammonia and urea emissions from urea manufacturing facilities of Petrochemical Industries Company (PIC), Kuwait.

    Science.gov (United States)

    Khan, A R; Al-Awadi, L; Al-Rashidi, M S

    2016-06-01

    Petrochemical Industries Company (PIC) in Kuwait has mitigated the pollution problem of ammonia and urea dust by replacing the melting and prilling units of finished-product urea prills with an environmentally friendly granulation process. PIC has financed a research project conducted by the Coastal and Air Pollution Program's research staff at the Kuwait Institute for Scientific Research to assess the impact of pollution control strategies implemented to maintain a healthy productive environment in and around the manufacturing premises. The project was completed in three phases: the first phase included the pollution monitoring of the melting and prilling units in full operation, the second phase covered the complete shutdown period where production was halted completely and granulation units were installed, and the last phase encompassed the current modified status with granulation units in full operation. There was substantial decrease in ammonia emissions, about 72%, and a 52.7% decrease in urea emissions with the present upgrading of old melting and prilling units to a state-of-the-art technology "granulation process" for a final finished product. The other pollutants, sulfur dioxide (SO2), nitrogen oxides (NOx), and volatile organic compounds (VOCs), have not shown any significant change, as the present modification has not affected the sources of these pollutants. Petrochemical Industries Company (PIC) in Kuwait has ammonia urea industries, and there were complaints about ammonia and urea dust pollution. PIC has resolved this problem by replacing "melting and prilling unit" of final product urea prills by more environmentally friendly "granulation unit." Environmental Pollution and Climate Program has been assigned the duty of assessing the outcome of this change and how that influenced ammonia and urea dust emissions from the urea manufacturing plant.

  14. Neuronal Activity and Glutamate Uptake Decrease Mitochondrial Mobility in Astrocytes and Position Mitochondria Near Glutamate Transporters

    Science.gov (United States)

    Jackson, Joshua G.; O'Donnell, John C.; Takano, Hajime; Coulter, Douglas A.

    2014-01-01

    Within neurons, mitochondria are nonuniformly distributed and are retained at sites of high activity and metabolic demand. Glutamate transport and the concomitant activation of the Na+/K+-ATPase represent a substantial energetic demand on astrocytes. We hypothesized that mitochondrial mobility within astrocytic processes might be regulated by neuronal activity and glutamate transport. We imaged organotypic hippocampal slice cultures of rat, in which astrocytes maintain their highly branched morphologies and express glutamate transporters. Using time-lapse confocal microscopy, the mobility of mitochondria within individual astrocytic processes and neuronal dendrites was tracked. Within neurons, a greater percentage of mitochondria were mobile than in astrocytes. Furthermore, they moved faster and farther than in astrocytes. Inhibiting neuronal activity with tetrodotoxin (TTX) increased the percentage of mobile mitochondria in astrocytes. Mitochondrial movement in astrocytes was inhibited by vinblastine and cytochalasin D, demonstrating that this mobility depends on both the microtubule and actin cytoskeletons. Inhibition of glutamate transport tripled the percentage of mobile mitochondria in astrocytes. Conversely, application of the transporter substrate d-aspartate reversed the TTX-induced increase in the percentage of mobile mitochondria. Inhibition of reversed Na+/Ca2+ exchange also increased the percentage of mitochondria that were mobile. Last, we demonstrated that neuronal activity increases the probability that mitochondria appose GLT-1 particles within astrocyte processes, without changing the proximity of GLT-1 particles to VGLUT1. These results imply that neuronal activity and the resulting clearance of glutamate by astrocytes regulate the movement of astrocytic mitochondria and suggest a mechanism by which glutamate transporters might retain mitochondria at sites of glutamate uptake. PMID:24478345

  15. Active transport improves the precision of linear long distance molecular signalling

    Science.gov (United States)

    Godec, Aljaž; Metzler, Ralf

    2016-09-01

    Molecular signalling in living cells occurs at low copy numbers and is thereby inherently limited by the noise imposed by thermal diffusion. The precision at which biochemical receptors can count signalling molecules is intimately related to the noise correlation time. In addition to passive thermal diffusion, messenger RNA and vesicle-engulfed signalling molecules can transiently bind to molecular motors and are actively transported across biological cells. Active transport is most beneficial when trafficking occurs over large distances, for instance up to the order of 1 metre in neurons. Here we explain how intermittent active transport allows for faster equilibration upon a change in concentration triggered by biochemical stimuli. Moreover, we show how intermittent active excursions induce qualitative changes in the noise in effectively one-dimensional systems such as dendrites. Thereby they allow for significantly improved signalling precision in the sense of a smaller relative deviation in the concentration read-out by the receptor. On the basis of linear response theory we derive the exact mean field precision limit for counting actively transported molecules. We explain how intermittent active excursions disrupt the recurrence in the molecular motion, thereby facilitating improved signalling accuracy. Our results provide a deeper understanding of how recurrence affects molecular signalling precision in biological cells and novel medical-diagnostic devices.

  16. Influence of excipients on drug absorption via modulation of intestinal transporters activity

    Directory of Open Access Journals (Sweden)

    Hetal P Thakkar

    2015-01-01

    Full Text Available One of the major factors affecting oral drug bioavailability is the activity of intestinal transport proteins, particularly for the drugs that undergo absorption by active transport mechanism. Many of the active pharmacological agents and the excipients used in their formulation are reported to modulate the activity of these transporters thereby either enhancing or decreasing the drug absorption and its systemic availability. These excipients are considered pharmacologically "inert" and have been used since years in pharmaceutical formulations. Appreciable interest is developing on the data demonstrating the role of excipients in altering the drug absorption across the intestine. Careful selection of the excipients thus is very important. A correctly chosen excipient can enhance the drug bioavailability and thus its therapeutic efficacy without increasing its dose. For locally acting drugs having systemic side effects, a proper excipient could lead to a decrease in its systemic absorption, thus reducing its side effects. This review focuses on the current findings of the excipients identified to modulate the activity of transporters, their mechanism of modulating the transporter′s activity and various formulation strategies using these excipients to enhance drug absorption.

  17. The transports in the French Plutonium Industry. A high risk activity

    Energy Technology Data Exchange (ETDEWEB)

    NONE

    2003-02-01

    This study throws light on the scale of transport of plutonium in France nuclear industry, an activity involving quantities of high risk materials often unknown to the public. The study is a significantly extended update of the one carried out by WISE-Paris in 1995 for the Plutonium Forum. It was motivated by important developments in the French plutonium industry and the publication of numerous data concerning transport activities since 1995. The 2003 study presents, in particular, all of the flows of plutonium crossing France every year, as well as analysis of the risks associated with this particular transport activity. Putting these data into perspective in terms of a rapidly and permanently changing political and industrial context, and a description of the regulatory framework within which shipments of plutonium take place, serve as a guide and source of reference to help readers better understand the issues. The importance of transport in the plutonium ''chain'', i.e. the stages corresponding to various industrial processes, is often under-estimated, even by the nuclear industry itself. Transport is, in fact, the activity which involves the greatest quantities of plutonium in the entire nuclear chain. Plutonium, produced during the fission reactions in the cores of nuclear reactors, is transported, contained in the irradiated fuel, to the facilities at La Hague where reprocessing separates it from the other radioactive components of the spent fuel. Part of the plutonium, now isolated in powder form, is then shipped to one of the three plants able to produce the fuel known as MOX. These are located at Cadarache and Marcoule, in France, and at Dessel in Belgium. Once in the MOX form, this plutonium has to be re-transported to reactor sites to be used. Once irradiated, the spent MOX will return to the La Hague installations to be stored for an unknown period; the plutonium contained in the spent MOX is not, at present, destined to be re

  18. The rationale for alternative fertilization: Equilibrium isotherm, kinetics and mass transfer analysis for urea-nitrogen adsorption from cow urine

    Directory of Open Access Journals (Sweden)

    M. Ganesapillai

    2015-12-01

    Full Text Available In an effort to minimize the loss of urea-N through volatilization and concurrently recover urea in a usable form from cow urine, adsorption experiments using bamboo-based activated carbon were performed. Batch studies were undertaken to evaluate the effect of initial concentration, sorption time and temperature on the variation in urea uptake capacity of the prepared carbon. Equilibrium data were tested against various isotherms, kinetics and mass transfer models. The Langmuir monolayer sorption was found to be 146.12 mg.g−1 with nearly 90% urea recovery attained. The process was found to be reversible as seen through regeneration experiments. Thermodynamic parameters indicated that urea sorption was physical, spontaneous and exothermic in nature. Kinetic studies revealed that the rate of urea uptake was limited by both surface adsorption and intra-particle diffusion. It was concluded that the mass transfer of urea molecules over the activated carbon was governed by film diffusion at all concentrations examined.

  19. Synthesis, Characterization, and Sensitivity Analysis of Urea Nitrate (UN)

    Science.gov (United States)

    2015-04-01

    ARL-TR-7250 ● APR 2015 US Army Research Laboratory Synthesis, Characterization, and Sensitivity Analysis of Urea Nitrate (UN...Characterization, and Sensitivity Analysis of Urea Nitrate (UN) by William M Sherrill Weapons and Materials Research Directorate...Characterization, and Sensitivity Analysis of Urea Nitrate (UN) 5a. CONTRACT NUMBER 5b. GRANT NUMBER 5c. PROGRAM ELEMENT NUMBER 6. AUTHOR(S

  20. 21 CFR 176.320 - Sodium nitrate-urea complex.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Sodium nitrate-urea complex. 176.320 Section 176... Substances for Use Only as Components of Paper and Paperboard § 176.320 Sodium nitrate-urea complex. Sodium nitrate-urea complex may be safely used as a component of articles intended for use in...

  1. 76 FR 15339 - Solid Urea From Russia and Ukraine

    Science.gov (United States)

    2011-03-21

    ... COMMISSION Solid Urea From Russia and Ukraine AGENCY: United States International Trade Commission. ACTION... orders on solid urea from Russia and Ukraine. SUMMARY: The Commission hereby gives notice that it will...)) to determine whether revocation of the antidumping duty orders on solid urea from Russia and...

  2. 76 FR 77015 - Solid Urea From Russia and Ukraine

    Science.gov (United States)

    2011-12-09

    ... COMMISSION Solid Urea From Russia and Ukraine Determination On the basis of the record \\1\\ developed in the... antidumping duty orders on solid urea from Russia and Ukraine would be likely to lead to continuation or... 2011), entitled Solid Urea from Russia and Ukraine: Investigation Nos. 731-TA- 340-E and 340-H...

  3. Hydrogen peroxide stimulates the active transport of serotonin into human platelets

    Energy Technology Data Exchange (ETDEWEB)

    Bosin, T.R. (Indiana Univ., Bloomington (United States))

    1991-03-11

    The effect of hydrogen peroxide on the active transport of serotonin (5-HT) by human platelets was investigated. Platelets were exposed to either a single dose of H{sub 2}O{sub 2} or to H{sub 2}O{sub 2} generated by the glucose/glucose oxidase or xanthine/xanthine oxidase enzyme systems. H{sub 2}{sub 2} produced a rapid, dose-dependent and time-dependent increase in 5-HT transport which was maximal after a 2 min incubation and decreased with continued incubation. Catalase completely prevented H{sub 2}O{sub 2}-induced stimulation and fluoxetine totally blocked 5-HT uptake into stimulated platelets. The glucose/glucose oxidase and the xanthine/xanthine oxidase generating systems produced a similar response to that of H{sub 2}O{sub 2}. In the xanthine/xanthine oxidase system, superoxide dismutase failed to alter the stimulation, while catalase effectively prevented the response. The kinetics of 5-HT transport indicated that H{sub 2}O{sub 2} treatment did not alter the K{sub m} of 5-HT transport but significantly increased the maximal rate of 5-HT transport. These data demonstrated that exposure of human platelets to H{sub 2}O{sub 2} resulted in a stimulation of the active transport of 5-HT and suggested that H{sub 2}O{sub 2} may function to regulate this process.

  4. Pancreatic lipase activity in overnight effluent predicts high transport status in peritoneal dialysis patients.

    Science.gov (United States)

    Idei, Mayumi; Tabe, Yoko; Hamada, Chieko; Miyake, Kazunori; Takemura, Hiroyuki; Io, Hiroaki; Wakita, Mitsuru; Horii, Takashi; Tomino, Yasuhiko; Ohsaka, Akimichi; Miida, Takashi

    2016-11-01

    Long-term peritoneal dialysis (PD) causes peritoneal morphological and functional changes, resulting in high transport status featuring increased peritoneal permeability. High transport status is diagnosed by peritoneal equilibration test (PET), a reliable but time-consuming method. We identifed a reliable biomarker in peritoneal effluent to predict high transport status in PD patients. We collected peritoneal effluent and serum from 33 PD patients and measured common laboratory test parameters. High transport status was determined by PET if the dialysate/plasma ratio of creatinine at 4h dwell (D/P Cr 4h) was ≥0.81. There were significant correlations between D/P Cr 4h and some laboratory parameters in overnight effluent (pancreatic lipase activity, r=0.65, povernight effluent was identified as an independent predictor of high transport status even after adjusting for age, PD duration, and glomerular filtration rate [OR=1.43 (95% CI: 1.11-1.83), p=0.005]. The pancreatic lipase activity in overnight effluent is an independent predictor of high transport status in PD patients. Copyright © 2016 Elsevier B.V. All rights reserved.

  5. Penentuan Rute Pengiriman Pupuk Urea Bersubsidi di Karanganyar

    Directory of Open Access Journals (Sweden)

    Yusuf Priyandari

    2011-01-01

    Full Text Available This paper develops a vehicle routing problem (VRP model for determining the routes in urea fertilizer distribution from a depot to retailers. The distribution is done in work days which uses trucks, each truck can serve more than one route (multiple trips, and each retailer has a time window. The vehicle routing model is built in a mixed integer linear programming (MILP and the objective function is minimizing total transportation cost. The distances from the distributor to retailers and inter-retailers do not use Euclidian approach but the road network on a digital map in order to make the route solution is more realistic. Historical distribution data was used to test the model. The result shows that the model can minimize the cost about 2.28% which is compared to the original routes.

  6. 1-(4-氯苯基)-3-三唑脲的合成及其植物生长调节活性%Synthesis and Plant Growth-Regulating Activity of 1-(4-Chlorphenyl)-3-Triyl Urea

    Institute of Scientific and Technical Information of China (English)

    冯桂荣; 王磊; 刘征原

    2015-01-01

    1-(4-chlorphenyl)-3-triyl urea was synthesized by addition reaction of 3-amino-1, 2, 4-triazole and aromatic isocyanate, which was produced by triphosgene with phenylamine, and was characterized by UV and IR. According to the tests of plant growth regulating activity, 1-(4-chlorphenyl)-3-triyl urea, on ten milligram of per liter had the better activity of plant growth regulator on the monocotyledon corn and the dicotyledon soybean.%利用固体光气法合成了4-氯苯基异氰酸酯,再进一步与3-氨基-1,2,4-三氮唑发生亲核加成反应合成了1-(4-氯苯基)-3-(1H-1,2,4-三氮唑-3-基)脲,目标产物结构用IR、UV进行了表征。植物生长调节活性测试表明,1-(4-氯苯基)-3-(1H-1,2,4-三氮唑-3-基)脲浓度为10 mg·L-1时对单子叶植物玉米和双子叶植物黄豆的生长具有较好的生长调节活性。

  7. An overview on the potential of natural products as ureas

    Directory of Open Access Journals (Sweden)

    Luzia V. Modolo

    2015-01-01

    Full Text Available Ureases, enzymes that catalyze urea hydrolysis, have received considerable attention for their impact on living organisms’ health and life quality. On the one hand, the persistence of urease activity in human and animal cells can be the cause of some diseases and pathogen infections. On the other hand, food production can be negatively affected by ureases of soil microbiota that, in turn, lead to losses of nitrogenous nutrients in fields supplemented with urea as fertilizer. In this context, nature has proven to be a rich resource of natural products bearing a variety of scaffolds that decrease the ureolytic activity of ureases from different organisms. Therefore, this work compiles the state-of-the-art researches focused on the potential of plant natural products (present in extracts or as pure compounds as urease inhibitors of clinical and/or agricultural interests. Emphasis is given to ureases of Helicobacter pylori, Canavalia ensiformis and soil microbiota although the active site of this class of hydrolases is conserved among living organisms.

  8. Effect of arsenite on urea production by long-term cultures of adult rat hepatocytes.

    Science.gov (United States)

    Sierra-Santoyo, A; Hernández, A; López, M L; Mendoza-Figueroa, T

    1996-01-01

    Urea cycle is a hepatic metabolic pathway involving five enzymes and several intermediary metabolites and can be altered by different chemicals. To investigate the effect of arsenic, an ubiquitous hepatotoxic agent, on urea production we exposed long-term cultures of adult rat hepatocytes, which produce urea, to 1.33 and 6.67 microM arsenite for 2 weeks. In cultures exposed to 6.67 microM, urea production decreased 60-70% and cellular arginase activity decreased 30, 70 and 85% after 4, 7 and 14 days of exposure, respectively. The arginase activity released to the medium increased significantly after 4, 7 and 14 days, with a maximum value after 7 days of exposure that was 27-fold higher than that of the untreated controls. The total arginase activity also decreased 35, 52 and 82% after 4, 7 and 14 days of exposure and protein content decreased 57 and 65% after 7 and 14 days of exposure, respectively. Exposure to 6.67 microM arsenite also produced accumulation of intracytoplasmic lipid droplets, vacuolizations and enlargement of the intercellular spaces. On the other hand, exposure of hepatocytes to 1.33 microM arsenite caused an initial decrease of 20% in urea production, did not change cellular, released and total arginase activity and cellular protein content and produced accumulation of intracytoplasmic lipid droplets. These results show that long-term exposure of cultured rat hepatocytes to 6.67 microM arsenite decreases urea production, cellular and total arginase activity and protein content and increases the release of arginase into the culture medium. These alterations could be useful markers of hepatotoxicity in in vitro assays.

  9. Active intracellular transport in metastatic cells studied by spatial light interference microscopy.

    Science.gov (United States)

    Ceballos, Silvia; Kandel, Mikhail; Sridharan, Shamira; Majeed, Hassaan; Monroy, Freddy; Popescu, Gabriel

    2015-01-01

    Spatiotemporal patterns of intracellular transport are very difficult to quantify and, consequently, continue to be insufficiently understood. While it is well documented that mass trafficking inside living cells consists of both random and deterministic motions, quantitative data over broad spatiotemporal scales are lacking. We studied the intracellular transport in live cells using spatial light interference microscopy, a high spatiotemporal resolution quantitative phase imaging tool. The results indicate that in the cytoplasm, the intracellular transport is mainly active (directed, deterministic), while inside the nucleus it is both active and passive (diffusive, random). Furthermore, we studied the behavior of the two-dimensional mass density over 30 h in HeLa cells and focused on the active component. We determined the standard deviation of the velocity distribution at the point of cell division for each cell and compared the standard deviation velocity inside the cytoplasm and the nucleus. We found that the velocity distribution in the cytoplasm is consistently broader than in the nucleus, suggesting mechanisms for faster transport in the cytosol versus the nucleus. Future studies will focus on improving phase measurements by applying a fluorescent tag to understand how particular proteins are transported inside the cell.

  10. Unassisted refolding of urea-denatured arginine kinase from shrimp Feneropenaeus chinensis: evidence for two equilibrium intermediates in the refolding pathway.

    Science.gov (United States)

    Pan, Ji-Cheng; Yu, Zhenhang; Su, Xiao-Yang; Sun, Ye-Qing; Rao, Xue-Ming; Zhou, Hai-Meng

    2004-07-01

    The refolding process and the equilibrium intermediates of urea-denatured arginine kinase (AK) were investigated by 1-anilino-8-naphthalenesulfonate (ANS) intrinsic fluorescence, far-UV circular dichroism (CD), size-exclusion chromatography (SEC), and enzymatic activity. In dilute denaturant, two equilibrium refolding intermediates (I and N') were discovered, and a refolding scheme of urea-denatured AK was proposed. During the refolding of urea-denatured AK, the fluorescence intensity increased remarkably, accompanied by a significant blue shift of the emission maximum and a pronounced increase in molar ellipticity of CD at 222 nm. The first folding intermediate (I) was inactive in urea solution ranging between 2.4 and 3.0 M. The second (N') existed between a 0.4- and 0.8-M urea solution, with slightly increased activity. Neither the blue shift emission maximum nor the molar ellipticity of CD at 222 nm showed significant changes in these two regions. The two intermediates were characterized by monitoring the ANS binding ability in various residual urea solutions, and two peaks of the emission intensity were observed in urea solutions of 0.6 and 2.8 M, respectively. The SEC results indicated that a distribution coefficient (K(D)) platform existed in urea solutions ranging between 2.4 and 3.0 M urea, suggesting that there was a similarly apparent protein profile and size in the urea solution region. The refolding kinetics showed that the urea-denatured AK was in two-phase refolding. Proline isomerization occurred in the unfolding process of AK, which blocked the slow phase of refolding. These results suggested that the refolding process of urea-denatured AK contained at the least two equilibrium refolding intermediates.

  11. The effect of urea on microstructures of Ni3S2 on nickel foam and its hydrogen evolution reaction

    Science.gov (United States)

    Jinlong, Lv; Tongxiang, Liang

    2016-11-01

    The effects of urea concentration on microstructures of Ni3S2formed on nickel foam and its hydrogen evolution reaction were investigated. The Ni3S2 nanosheets with porous structure were formed on nickel foam during hydrothermal process due to low urea concentration. While high urea concentration facilitated the forming of Ni3S2 nanotube arrays. The resulting Ni3S2 nanotube arrays exhibited higher catalytic activity than Ni3S2nanosheets for hydrogen evolution reaction. This was mainly attributed to a fact that Ni3S2 nanotube arrays facilitated diffusion of electrolyte for hydrogen evolution reaction.

  12. Viscometric study of lysozyme solution with sugar and urea at various temperatures

    Directory of Open Access Journals (Sweden)

    Jamal Akhter Siddique

    2016-11-01

    at temperatures (293.15, 303.15, 313.13 and 323.15 K at various concentrations of glucose, maltose and urea. Change in entropy (ΔH, enthalpy (ΔS and free energy of activation (ΔG have also been evaluated for these systems. Value of B-coefficient of d (− glucose, maltose and urea has also been calculated from viscosity data in aqueous lysozyme solution. Viscosity B-coefficients of glucose and maltose in aqueous lysozyme solution are positive while that of the urea–lysozyme water system it is negative due to the structure breaking effect of urea. The values of entropy of activation are negative due to attainment of transition state for viscous flow, which is accompanied by bond formation and increase in order.

  13. Central Hemodynamics and Oxygen Transport in Various Activation of Patients Operated On Under Extracorporeal Circulation

    Directory of Open Access Journals (Sweden)

    Ye. V. Dzybinskaya

    2009-01-01

    Full Text Available Objective: to study central hemodynamics, the determinants of myocardial oxygen balance, and the parameters of oxygen transport in various activation of patients after surgery under extracorporeal circulation. Subjects and methods. Thirty-four patients aged 57.8±2.5 years who had coronary heart disease were divided into 2 groups: 1 those with late activation (artificial ventilation time 157±9 min and 2 those with immediate activation (artificial ventilation time 33±6 min. Group 2 patients were, if required, given fentanyl, midazolam, or myorelaxants. Results. During activation, there were no intergroup differences in the mean levels of the major parameters of cardiac pump function, in the determinants of coronary blood flow (coronary perfusion gradients and myocardial oxygen demand (the product of heart rate by systolic blood pressure, and in the parameters of oxygen transport, including arterial lactatemia. After tracheal extubation, the left ventricular pump coefficient was increased considerably (up to 3.8±0.2 and 4.4±0.2 gm/mm Hg/m2 in Groups 1 and 2, respectively; p<0.05 with minimum inotropic support (dopamine and/or dobutamine being used at 2.7±0.3 and 2.4±0.3 mg/kg/min, respectively. In both groups, there were no close correlations between the indices of oxygen delivery and consumption at all stages of the study, which was indicative of no transport-dependent oxygen uptake. Conclusion. When the early activation protocol was followed up, the maximum acceleration of early activation, including that using specific antagonists of anesthetics, has no negative impact on central hemodynamics, the determinants of myocardial oxygen balance and transport in patients operated on under extracorporeal circulation. Key words: early activation, surgery under extracorporeal circulation, tracheal extubation in the operating-room, central hemodynamics, oxygen transport.

  14. A fully resolved active musculo-mechanical model for esophageal transport

    Science.gov (United States)

    Kou, Wenjun; Bhalla, Amneet Pal Singh; Griffith, Boyce E.; Pandolfino, John E.; Kahrilas, Peter J.; Patankar, Neelesh A.

    2015-10-01

    Esophageal transport is a physiological process that mechanically transports an ingested food bolus from the pharynx to the stomach via the esophagus, a multi-layered muscular tube. This process involves interactions between the bolus, the esophagus, and the neurally coordinated activation of the esophageal muscles. In this work, we use an immersed boundary (IB) approach to simulate peristaltic transport in the esophagus. The bolus is treated as a viscous fluid that is actively transported by the muscular esophagus, and the esophagus is modeled as an actively contracting, fiber-reinforced tube. Before considering the full model of the esophagus, however, we first consider a standard benchmark problem of flow past a cylinder. Next a simplified version of our model is verified by comparison to an analytic solution to the tube dilation problem. Finally, three different complex models of the multi-layered esophagus, which differ in their activation patterns and the layouts of the mucosal layers, are extensively tested. To our knowledge, these simulations are the first of their kind to incorporate the bolus, the multi-layered esophagus tube, and muscle activation into an integrated model. Consistent with experimental observations, our simulations capture the pressure peak generated by the muscle activation pulse that travels along the bolus tail. These fully resolved simulations provide new insights into roles of the mucosal layers during bolus transport. In addition, the information on pressure and the kinematics of the esophageal wall resulting from the coordination of muscle activation is provided, which may help relate clinical data from manometry and ultrasound images to the underlying esophageal motor function.

  15. Individual public transportation accessibility is positively associated with self-reported active commuting

    DEFF Research Database (Denmark)

    Djurhuus, Sune; Hansen, Henning Sten; Aadahl, Mette;

    2014-01-01

    BACKGROUND: Active commuters have lower risk of chronic disease. Understanding which of the, to some extent, modifiable characteristics of public transportation that facilitate its use is thus important in a public health perspective. The aim of the study was to examine the association between...... individual public transportation accessibility and self-reported active commuting, and whether the associations varied with commute distance, age, and gender. METHODS: Twenty-eight thousand nine hundred twenty-eight commuters in The Capital Region of Denmark reported self-reported time spent either walking...... or cycling to work or study each day and the distance to work or study. Data were obtained from the Danish National Health Survey collected in February to April 2010. Individual accessibility by public transportation was calculated using a multi-modal network in a GIS. Multilevel logistic regression was used...

  16. Mathematical modeling of the intracellular protein dynamics: the importance of active transport along microtubules.

    Science.gov (United States)

    Szymańska, Zuzanna; Parisot, Martin; Lachowicz, Mirosław

    2014-12-21

    In this paper we propose a mathematical model of protein and mRNA transport inside a cell. The spatio-temporal model takes into account the active transport along microtubules in the cytoplasm as well as diffusion and is able to reproduce the oscillatory changes in protein concentration observed in many experimental data. In the model the protein and the mRNA interact with each other that allows us to classify the model as a simple gene regulatory network. The proposed model is generic and may be adapted to specific signaling pathways. On the basis of numerical simulations, we formulate a new hypothesis that the oscillatory dynamics is allowed by the mRNA active transport along microtubules from the nucleus to distant locations.

  17. Reconsidering the Lack of Urea Toxicity in Dialysis Patients.

    Science.gov (United States)

    Massy, Ziad A; Pietrement, Christine; Touré, Fatouma

    2016-09-01

    Urea is an old uremic toxin which has been used for many years as a global biomarker of CKD severity and dialysis adequacy. Old studies were not in favor of its role as a causal factor in the pathogenesis of complications associated with the uremic state. However, recent experimental and clinical evidence is compatible with both direct and indirect toxicity of urea, particularly via the deleterious actions of urea-derived carbamylated molecules. Further studies are clearly needed to explore the potential relevance of urea-related CKD complications for patient management, in particular the place of new therapeutic strategies to prevent urea toxicity.

  18. Children's route choice during active transportation to school : difference between shortest and actual route

    NARCIS (Netherlands)

    Dessing, D.; Vries, S.I. (Sanne); Hegeman, G.; Mechelen, W. van; Pierik, F.H.

    2016-01-01

    Background: The purpose of this study is to increase our understanding of environmental correlates that are associated with route choice during active transportation to school (ATS) by comparing characteristics of actual walking and cycling routes between home and school with the shortest possible r

  19. The Association Between the Physical Environment of Primary Schools and Active School Transport

    NARCIS (Netherlands)

    Kann, D.H.H. van; Kremers, S.P.J.; Gubbels, J.S.; Bartelink, N.H.M.; Vries, S.I. de; Vries, N.K. de; Jansen, M.W.J.

    2015-01-01

    This study examined the relationship between the physical environment characteristics of primary schools and active school transport among 3,438 5- to 12-year-old primary school children in the Netherlands. The environmental characteristics were categorized into four theory-based clusters (function,

  20. En-route mechanical activation of viscous oil and oil products transported in railroad tank cars

    Directory of Open Access Journals (Sweden)

    Yerlan MYRZAKHMETOV

    2012-01-01

    Full Text Available The authors of this document are aiming to substantiate the advantages of en-route mechanical activation technology as aids for railroad transportation of viscous oil and oil products in tank cars. The conceptual design implies the use of momentum generated by brake action. This document also contains preliminary data of laboratory research confirming the validity of the developed concept.

  1. Inhibition of Activity of GABA Transporter GAT1 by δ-Opioid Receptor

    Directory of Open Access Journals (Sweden)

    Lu Pu

    2012-01-01

    Full Text Available Analgesia is a well-documented effect of acupuncture. A critical role in pain sensation plays the nervous system, including the GABAergic system and opioid receptor (OR activation. Here we investigated regulation of GABA transporter GAT1 by δOR in rats and in Xenopus oocytes. Synaptosomes of brain from rats chronically exposed to opiates exhibited reduced GABA uptake, indicating that GABA transport might be regulated by opioid receptors. For further investigation we have expressed GAT1 of mouse brain together with mouse δOR and μOR in Xenopus oocytes. The function of GAT1 was analyzed in terms of Na+-dependent [3H]GABA uptake as well as GAT1-mediated currents. Coexpression of δOR led to reduced number of fully functional GAT1 transporters, reduced substrate translocation, and GAT1-mediated current. Activation of δOR further reduced the rate of GABA uptake as well as GAT1-mediated current. Coexpression of μOR, as well as μOR activation, affected neither the number of transporters, nor rate of GABA uptake, nor GAT1-mediated current. Inhibition of GAT1-mediated current by activation of δOR was confirmed in whole-cell patch-clamp experiments on rat brain slices of periaqueductal gray. We conclude that inhibition of GAT1 function will strengthen the inhibitory action of the GABAergic system and hence may contribute to acupuncture-induced analgesia.

  2. Statement of work for the immobilized low-activity waste transportation system -- Project W-465

    Energy Technology Data Exchange (ETDEWEB)

    Mouette, P.

    1998-06-19

    The objective of this Statement of Work (SOW) is to present the scope, the deliverables, the organization, the technical and schedule expectations for the development of a Package Design Criteria (PDC), cost and schedule estimate for the acquisition of a transportation system for the Immobilized Low-Activity Waste (ILAW).

  3. Potential Activity of Subglacial Microbiota Transported to Anoxic River Delta Sediments

    DEFF Research Database (Denmark)

    Cameron, Karen A.; Stibal, Marek; Olsen, Nikoline S.

    2017-01-01

    The Watson River drains a portion of the SW Greenland ice sheet, transporting microbial communities from subglacial environments to a delta at the head of Søndre Strømfjord. This study investigates the potential activity and community shifts of glacial microbiota deposited and buried under layers...

  4. Nitrogen excretion and expression of urea cycle enzymes in the atlantic cod (Gadus morhua l.): a comparison of early life stages with adults

    Science.gov (United States)

    Chadwick; Wright

    1999-10-01

    For many years, the urea cycle was considered to be relatively unimportant in the life history of most teleost fishes. In previous studies, we were surprised to find that newly hatched freshwater rainbow trout embryos had relatively high activities of the key urea cycle enzyme, carbamoyl phosphate synthetase III (CPSase III), and other enzymes in the pathway, whereas adult trout had much lower or non-detectable activities. The present study tested the hypothesis that urea cycle enzyme expression is unique to early stages of rainbow trout. In marine Atlantic cod (Gadus morhua) embryos, CPSase III, ornithine transcarbamoylase (OTCase), glutamine synthetase (GSase) and arginase activities were all expressed prior to hatching. Urea excretion was detected shortly after fertilization and rates were high relative to those of ammonia excretion (50-100 % of total nitrogen excreted as urea nitrogen; total=ammonia+urea). Urea concentration was relatively constant in embryos, but ammonia concentration increased by about fourfold during embryogenesis. Two populations of cod embryos were studied (from Newfoundland and New Brunswick), and significant differences in enzyme activities and excretion rates were detected between the two populations. In adult cod, CPSase III was not detectable in liver, white muscle, intestine and kidney tissues, but OTCase, GSase and arginase were present. Adult cod excreted about 17 % of nitrogenous waste as urea. Taken together, these data indicate that early urea cycle enzyme expression is not unique to rainbow trout but is also a feature of Atlantic cod development, and possibly other teleosts. The relatively high urea excretion rates underline the importance of urea as the primary nitrogen excretory product in Atlantic cod during early embryogenesis.

  5. Site-Specific Description of the Enhanced Recognition Between Electrogenerated Nitrobenzene Anions and Dihomooxacalix[4]arene Bidentate Ureas.

    Science.gov (United States)

    Martínez-González, Eduardo; Armendáriz-Vidales, Georgina; Ascenso, José R; Marcos, Paula M; Frontana, Carlos

    2015-05-01

    Electron transfer controlled hydrogen bonding was studied for a series of nitrobenzene derivative radical anions, working as large guest anions, and substituted ureas, including dihomooxacalix[4]arene bidentate urea derivatives, in order to estimate binding constants (Kb) for the hydrogen-bonding process. Results showed enhanced Kb values for the interaction with phenyl-substituted bidentate urea, which is significantly larger than for the remaining compounds, e.g., in the case of 4-methoxynitrobenzene a 28-fold larger Kb value was obtained for the urea bearing a phenyl (Kb ∼ 6888) vs tert-butyl (Kb ∼ 247) moieties. The respective nucleophilic and electrophilic characters of the participant anion radical and urea hosts were parametrized with global and local electrodonating (ω(-)) and electroaccepting (ω(+)) powers, derived from DFT calculations. ω(-) data were useful for describing trends in structure–activity relationships when comparing nitrobenzene radical anions. However, ω(+) for the host urea structures lead to unreliable explanations of the experimental data. For the latter case, local descriptors ωk(+)(r) were estimated for the atoms within the urea region in the hosts [∑kωk(+)(r)]. By compiling all the theoretical and experimental data, a Kb-predictive contour plot was built considering ω(-) for the studied anion radicals and ∑kωk(+)(r) which affords good estimations.

  6. Development of a multiphysics model to characterize the responsive behavior of urea-sensitive hydrogel as biosensor.

    Science.gov (United States)

    Goh, K B; Li, Hua; Lam, K Y

    2017-05-15

    A remarkable feature of biomaterials is their ability to deform in response to certain external bio-stimuli. Here, a novel biochemo-electro-mechanical model is developed for the numerical characterization of the urea-sensitive hydrogel in response to the external stimulus of urea. The urea sensitivity of the hydrogel is usually characterized by the states of ionization and denaturation of the immobilized urease, as such the model includes the effect of the fixed charge groups and temperature coupled with pH on the activity of the urease. Therefore, a novel rate of reaction equation is proposed to characterize the hydrolysis of urea that accounts for both the ionization and denaturation states of the urease subject to the environmental conditions. After examination with the published experimental data, it is thus confirmed that the model can characterize well the responsive behavior of the urea-sensitive hydrogel subject to the urea stimulus, including the distribution patterns of the electrical potential and pH of the hydrogel. The results point to an innovative means for generating electrical power via the enzyme-induced pH and electrical potential gradients, when the hydrogel comes in contact with the urea-rich solution, such as human urine.

  7. Cargo-towing synthetic nanomachines: towards active transport in microchip devices.

    Science.gov (United States)

    Wang, Joseph

    2012-05-08

    This review article discusses the use of synthetic catalytic nano motors for cargo manipulations and for developing miniaturized lab-on-chip systems based on autonomous transport. The ability of using chemically-powered artificial nanomotors to capture, transport and release therapeutic payloads or nanostructured biomaterials represents one of the next major prospects for nanomotor development. The increased cargo-towing force of such self-propelled nanomotors, along with their precise motion control within microchannel networks, versatility and facile functionalization, pave the way to new integrated functional lab-on-a-chip powered by active transport and perform a series of tasks. Such use of cargo-towing artificial nanomotors has been inspired by on-chip kinesin molecular shuttles. Functionalized nano/microscale motors can thus be used to pick a selected nano/microscale chemical or biological payload target at the right place, transport and deliver them to a target location in a timely manner. Key challenges for using synthetic nanomachines for driving transport processes along microchannel networks are discussed, including loading and unloading of cargo and precise motion control, along with recent examples of related cargo manipulation processes and guided transport in lab-on-a-chip formats. The exciting research area of cargo-carrying catalytic man-made nanomachines is expected to grow rapidly, to lead to new lab-on-a-chip formats and to provide a wide range of future microchip opportunities.

  8. Characteristics of Wheat-Maize Yield and Soil Organic Carbon/Nitrogen Mineralization in Cinnamon Soil with Application of Different Activation Humic Acid-Urea%不同活化处理腐植酸-尿素对褐土小麦-玉米产量及有机碳氮矿化的影响

    Institute of Scientific and Technical Information of China (English)

    刘艳丽; 丁方军; 谷端银; 吴钦泉; 张民; 李成亮

    2015-01-01

    腐植酸-尿素是一种新型有机无机肥料,不同活化方式对其肥效的发挥具有重要作用.本研究利用田间定位试验和室内培养试验,设计不施肥处理(CK)、无机肥处理(U)、腐植酸-尿素直接掺混处理(U+HA1)、腐植酸-尿素硫化活化处理(U+HA2)、腐植酸-尿素硫化加超声波处理(U+HA3),在褐土上研究不同活化处理腐植酸-尿素肥料对小麦-玉米产量和土壤有机碳氮矿化的影响.结果表明:施用腐植酸-尿素显著提高小麦-玉米产量,小麦、玉米产量分别比U处理增产15%~28%、8%~10%,比CK处理增产63%~81%、55%~57%.U+HA3处理比U+HA1和U+HA2处理具有更强的增产效果.土壤养分在不同施肥处理间存在差异,土壤NO3--N含量的变化趋势为U+HA1、U+HA3>U+HA2>U>CK.土壤NH4-N含量在不同处理间与NO3--N含量具有相似的趋势,其中U+HA1处理土壤NH4+-N含量较其他两种腐植酸-尿素处理有显著的降低.施肥处理提高了土壤有效磷、速效钾含量,但是腐殖酸-尿素处理与U处理的影响未见差异.腐殖酸-尿素处理对土壤有机碳含量未产生显著影响,但提高了土壤有机碳的矿化速率与累积矿化量,其中U+HA3处理比U+HA1和U+HA2处理效果明显.土壤有机碳的累积矿化量与作物总产量、土壤速效氮、有效磷、速效钾含量具有显著的正相关关系.与CK处理相比,腐植酸的添加对土壤有机氮矿化比率影响不显著,但U处理土壤有机氮矿化比率显著提高.通过本研究验证腐植酸-尿素肥料比无机肥料具有更强的提高土壤生产力和肥力的作用,硫化超声波活化处理效果比其他两种活化处理效果显著.硫化超声波活化处理腐植酸-尿素肥料是值得推广的新型肥料,对丰富肥料资源具有重要作用.%Humic acid-urea is one of the novel inorganic-organic fertilizers.Different activation approaches to humic acids play important roles in the

  9. Milk Urea Dynamics during its Transformation into Yogurt

    Directory of Open Access Journals (Sweden)

    Cornelia Vintila

    2011-10-01

    Full Text Available The purpose of our work was to evaluate in what measure milk urea concentration stays in processed yogurt and in what measure urea dose influences its quality. We added known amounts of urea into milk destined to yogurt processing in order to obtain probes with concentrations from 0,5 to 28 mg/ 100 ml milk. Obtained results lead us to the conclusion that milk urea decreases dramatically until the finishing of the process of milk coagulation and its transformation into yogurt. All probes which contained higher amounts of urea than 6 mg/ 100 ml milk, urea totally disappeared from yogurt before 48 hours of keeping. Milk coagulation time and its transformation to yogurt is reduced proportional with urea concentration in milk.

  10. Determination of urea kinetics by isotope dilution with [C-13]urea and gas chromatography isotope ratio mass spectrometry (GC-IRMS) analysis

    NARCIS (Netherlands)

    Kloppenburg, Wybe; Wolthers, BG; Stellaard, F; Elzinga, H; Tepper, T; deJong, PE; Huisman, RM

    1997-01-01

    1. Stable urea isotopes can be used to study urea kinetics in humans, The use of stable urea isotopes far studying urea kinetic parameters in humans on a large scale is hampered by the high costs of the labelled material, We devised a urea dilution for measurement of the distribution volume, product

  11. Suppression of adenosine-activated chloride transport by ethanol in airway epithelia.

    Directory of Open Access Journals (Sweden)

    Sammeta V Raju

    Full Text Available Alcohol abuse is associated with increased lung infections. Molecular understanding of the underlying mechanisms is not complete. Airway epithelial ion transport regulates the homeostasis of airway surface liquid, essential for airway mucosal immunity and lung host defense. Here, air-liquid interface cultures of Calu-3 epithelial cells were basolaterally exposed to physiologically relevant concentrations of ethanol (0, 25, 50 and 100 mM for 24 hours and adenosine-stimulated ion transport was measured by Ussing chamber. The ethanol exposure reduced the epithelial short-circuit currents (I(SC in a dose-dependent manner. The ion currents activated by adenosine were chloride conductance mediated by cystic fibrosis transmembrane conductance regulator (CFTR, a cAMP-activated chloride channel. Alloxazine, a specific inhibitor for A(2B adenosine receptor (A(2BAR, largely abolished the adenosine-stimulated chloride transport, suggesting that A(2BAR is a major receptor responsible for regulating the chloride transport of the cells. Ethanol significantly reduced intracellular cAMP production upon adenosine stimulation. Moreover, ethanol-suppression of the chloride secretion was able to be restored by cAMP analogs or by inhibitors to block cAMP degradation. These results imply that ethanol exposure dysregulates CFTR-mediated chloride transport in airways by suppression of adenosine-A(2BAR-cAMP signaling pathway, which might contribute to alcohol-associated lung infections.

  12. Riluzole and gabapentinoids activate glutamate transporters to facilitate glutamate-induced glutamate release from cultured astrocytes

    OpenAIRE

    Yoshizumi, Masaru; Eisenach, James C.; Hayashida, Ken-ichiro

    2011-01-01

    We have recently demonstrated that the glutamate transporter activator riluzole paradoxically enhanced glutamate-induced glutamate release from cultured astrocytes. We further showed that both riluzole and the α2δ subunit ligand gabapentin activated descending inhibition in rats by increasing glutamate receptor signaling in the locus coeruleus and hypothesized that these drugs share common mechanisms to enhance glutamate release from astrocytes. In the present study, we examined the effects o...

  13. Quantum crystallographic charge density of urea

    OpenAIRE

    Wall, Michael E.

    2015-01-01

    Standard X-ray crystallography methods use free-atom models to calculate mean unit-cell charge densities. Real molecules, however, have shared charge that is not captured accurately using free-atom models. To address this limitation, a charge density model of crystalline urea was calculated using high-level quantum theory and was refined against publicly available ultra-high-resolution experimental Bragg data, including the effects of atomic displacement parameters. The resulting quantum crys...

  14. Analysis of urea distribution volume in hemodialysis.

    Science.gov (United States)

    Maduell, F; Sigüenza, F; Caridad, A; Miralles, F; Serrato, F

    1994-01-01

    According to the urea kinetic model it is considered that the urea distribution volume (V) is that of body water, and that it is distributed in only one compartment. Since the V value is different to measure, it is normal to use 58% of body weight, in spite of the fact that it may range from 35 to 75%. In this study, we have calculated the value of V by using an accurate method based on the total elimination of urea from the dialysate. We have studied the V, and also whether the different dialysis characteristics modify it. Thirty-five patients were included in this study, 19 men and 16 women, under a chronic hemodialysis programme. The dialysate was collected in a graduated tank, and the concentration of urea in plasma and in dialysate were determined every hour. Every patient received six dialysis sessions, changing the blood flow (250 or 350 ml/min), the ultrafiltration (0.5 or 1.5 l/h), membrane (cuprophane or polyacrylonitrile) and/or buffer (bicarbonate or acetate). At the end of the hemodialysis session, the V value ranged from 43 to 72% of body weight; nevertheless, this value was practically constant in every patient. The V value gradually increased throughout the dialysis session, 42.1 +/- 6.9% of body weight in the first hour, 50.7 +/- 7.5% in the second hour and 55.7 +/- 7.9% at the end of the dialysis session. The change of blood flow, ultrafiltration, membrane or buffer did not alter the results. The V value was significantly higher in men in comparison with women, 60.0 +/- 6.6% vs. 50.5 +/- 5.9% of body weight (p < 0.001).

  15. Neutron transport calculation for Activation Evaluation for Decommissioning of PET cyclotron Facility

    Science.gov (United States)

    Nobuhara, Fumiyoshi; Kuroyanagi, Makoto; Masumoto, Kazuyoshi; Nakamura, Hajime; Toyoda, Akihiro; Takahashi, Katsuhiko

    2017-09-01

    In order to evaluate the state of activation in a cyclotron facility used for the radioisotope production of PET diagnostics, we measured the neutron flux by using gold foils and TLDs. Then, the spatial distribution of neutrons and induced activity inside the cyclotron vault were simulated with the Monte Calro calculation code for neutron transport and DCHAIN-SP for activation calculation. The calculated results are in good agreement with measured values within factor 3. Therefore, the adaption of the advanced evaluation procedure for activation level is proved to be important for the planning of decommissioning of these facilities.

  16. Inactivation and unfolding of protein tyrosine phosphatase from Thermus thermophilus HB27 during urea and guanidine hydrochloride denaturation.

    Directory of Open Access Journals (Sweden)

    Yejing Wang

    Full Text Available The effects of urea and guanidine hydrochloride (GdnHCl on the activity, conformation and unfolding process of protein tyrosine phosphatase (PTPase, a thermostable low molecular weight protein from Thermus thermophilus HB27, have been studied. Enzymatic activity assays showed both urea and GdnHCl resulted in the inactivation of PTPase in a concentration and time-dependent manner. Inactivation kinetics analysis suggested that the inactivation of PTPase induced by urea and GdnHCl were both monophasic and reversible processes, and the effects of urea and GdnHCl on PTPase were similar to that of mixed-type reversible inhibitors. Far-ultraviolet (UV circular dichroism (CD, Tryptophan and 1-anilinonaphthalene -8-sulfonic acid (ANS fluorescence spectral analyses indicated the existence of a partially active and an inactive molten globule-like intermediate during the unfolding processes induced by urea and GdnHCl, respectively. Based on the sequence alignment and the homolog Tt1001 protein structure, we discussed the possible conformational transitions of PTPase induced by urea and GdnHCl and compared the conformations of these unfolding intermediates with the transient states in bovine PTPase and its complex structures in detail. Our results may be able to provide some valuable clues to reveal the relationship between the structure and enzymatic activity, and the unfolding pathway and mechanism of PTPase.

  17. Supply chain and innovation activity in transport related enterprises in Eastern Poland

    Directory of Open Access Journals (Sweden)

    Giuseppe Ioppolo

    2016-12-01

    Full Text Available  Background: One of the development strategies uses R&D activity as the main source of innovation, which is often carried out in cooperation with other units, but in particular in the supply chain, and therefore applies to cooperation between enterprises and their customers and suppliers. The aim of the study was to identify the variable determinants of the impact of the character of relationships among enterprises and their suppliers and customers on their innovative performance, within regional industrial systems and to define the constraints for a model regional structure of innovation network tailored to the needs of Poland and its regions. Methods: 167 enterprises belonging to the transport sector and operating in the area of Eastern Poland took part. In order to determine the impact of relationships with suppliers and customers on innovation activity, models based on probability analysis - probit models - were used. Results: It can be clearly stated that the cooperation of industrial enterprises in the transport sector with customers and suppliers activates innovation activity and its specified attributes. However, the probability varies depending on the test variable adopted. Conclusions: The cooperation with suppliers and customers is the cognitive aspect in the development of innovation activity in industrial enterprises representing the transport-related sector. Such cooperation has a stimulating effect on expenditures on innovation activity and on the implementation of innovative solutions in the field of technological innovation (products and processes.  

  18. Activated human CD4+ T cells express transporters for both cysteine and cystine.

    Science.gov (United States)

    Levring, Trine Bøegh; Hansen, Ann Kathrine; Nielsen, Bodil Lisbeth; Kongsbak, Martin; von Essen, Marina Rode; Woetmann, Anders; Odum, Niels; Bonefeld, Charlotte Menné; Geisler, Carsten

    2012-01-01

    Because naïve T cells are unable to import cystine due to the absence of cystine transporters, it has been suggested that T cell activation is dependent on cysteine generated by antigen presenting cells. The aim of this study was to determine at which phases during T cell activation exogenous cystine/cysteine is required and how T cells meet this requirement. We found that early activation of T cells is independent of exogenous cystine/cysteine, whereas T cell proliferation is strictly dependent of uptake of exogenous cystine/cysteine. Naïve T cells express no or very low levels of both cystine and cysteine transporters. However, we found that these transporters become strongly up-regulated during T cell activation and provide activated T cells with the required amount of cystine/cysteine needed for T cell proliferation. Thus, T cells are equipped with mechanisms that allow T cell activation and proliferation independently of cysteine generated by antigen presenting cells.

  19. Urea Induced Denaturation of Pre-Q1 Riboswitch

    Science.gov (United States)

    Yoon, Jeseong; Thirumalai, Devarajan; Hyeon, Changbong

    2013-01-01

    Urea, a polar molecule with a large dipole moment, not only destabilizes the folded RNA structures, but can also enhance the folding rates of large ribozymes. Unlike the mechanism of urea-induced unfolding of proteins, which is well understood, the action of urea on RNA has barely been explored. We performed extensive all atom molecular dynamics (MD) simulations to determine the molecular underpinnings of urea-induced RNA denaturation. Urea displays its denaturing power in both secondary and tertiary motifs of the riboswitch (RS) structure. Our simulations reveal that the denaturation of RNA structures is mainly driven by the hydrogen bonds and stacking interactions of urea with the bases. Through detailed studies of the simulation trajectories, we found that geminate pairs between urea and bases due to hydrogen bonds and stacks persist only ~ (0.1-1) ns, which suggests that urea-base interaction is highly dynamic. Most importantly, the early stage of base pair disruption is triggered by penetration of water molecules into the hydrophobic domain between the RNA bases. The infiltration of water into the narrow space between base pairs is critical in increasing the accessibility of urea to transiently disrupted bases, thus allowing urea to displace inter base hydrogen bonds. This mechanism, water-induced disruption of base-pairs resulting in the formation of a "wet" destabilized RNA followed by solvation by urea, is the exact opposite of the two-stage denaturation of proteins by urea. In the latter case, initial urea penetration creates a dry-globule, which is subsequently solvated by water penetration leading to global protein unfolding. Our work shows that the ability to interact with both water and polar, non-polar components of nucleotides makes urea a powerful chemical denaturant for nucleic acids.

  20. Promoting better health through public transit use : another step towards active, sustainable transportation

    Energy Technology Data Exchange (ETDEWEB)

    Noxon, G. [Noxon Associates Ltd., Ottawa, ON (Canada)

    2001-07-01

    A study was conducted on behalf of the Canadian Urban Transit Association and the Federation of Canadian Municipalities, aimed at determining the contribution of public transit to public health in Canada. Health and transportation are linked together in their impact on air quality, climate change and safety, to name a few. The author defined sustainable transportation, limited growth, modal shift and modal efficiency. The benefits to be derived from sustainable transportation include health, with the emphasis being placed on urban transportation. Transportation in Toronto causes 90 per cent of carbon dioxide emissions, 83 per cent of nitrogen oxide emissions, and 60 per cent of sulphur dioxide emissions. Air quality is vastly improved and pollution reduced through the use of public transit. Alternative fuels, such as clean diesel, natural gas and biomass pollute a lot less. The use of auto and urban travel represent major sources of greenhouse gases and have an effect on global climate change. Some of the measures being considered involve the use of fare technologies, tax-exempt transit benefits, pricing strategies, service improvements, vehicle/fuel technologies. Road safety has improved but vehicle accidents still represent the major cause of death among young people. Canadians are not active enough, and physical activity is critical to good health. It was recommended that walking and cycling be used for short trips. Health also improves with income and social standing. Low income families end up spending more on transportation than they do on food. Some of the challenges facing equity in access to public transit are route elimination, fare increases, and paratransit demand. More research is needed to better address public transit contribution to public health, especially air quality, climate change, safety, physical activity (multimodal lifestyles and trips) and equity of access. figs.

  1. Discovery of nitroaryl urea derivatives with antiproliferative properties.

    Science.gov (United States)

    Wróbel, Tomasz M; Kiełbus, Michał; Kaczor, Agnieszka A; Kryštof, Vladimír; Karczmarzyk, Zbigniew; Wysocki, Waldemar; Fruziński, Andrzej; Król, Sylwia K; Grabarska, Aneta; Stepulak, Andrzej; Matosiuk, Dariusz

    2016-08-01

    A series of urea derivatives bearing nitroaryl moiety has been synthesized and assayed for their potential antiproliferative activities. Some of the tested compounds displayed activity in RK33 laryngeal cancer cells and TE671 rhabdomyosarcoma cells while being generally less toxic to healthy HSF human fibroblasts cells. One compound was demonstrated to be a moderate CDK2 inhibitor with IC50 = 14.3 µM. Its structure was solved by an X-ray crystallography and molecular modelling was performed to determine structure-activity relationship. Obtained compounds constitute novel structures and generally demonstrated greater cytotoxicity in comparison to cisplatin. This study offers new structural motifs with potential for further development.

  2. Altering the structure and properties of iron oxide nanoparticles and graphene oxide/iron oxide composites by urea

    Energy Technology Data Exchange (ETDEWEB)

    Naghdi, Samira [Physics department, Bu-Ali Sina University, 65174 Hamedan (Iran, Islamic Republic of); Department of Mechanical Engineering, College of Engineering, Kyung Hee University, 446-701 Yongin (Korea, Republic of); Rhee, Kyong Yop, E-mail: rheeky@khu.ac.kr [Department of Mechanical Engineering, College of Engineering, Kyung Hee University, 446-701 Yongin (Korea, Republic of); Jaleh, Babak [Physics department, Bu-Ali Sina University, 65174 Hamedan (Iran, Islamic Republic of); Park, Soo Jin [Chemistry, Colloge of Natural Science, Inha University, 402-751 Incheon (Korea, Republic of)

    2016-02-28

    Graphical abstract: - Highlights: • Iron oxide (Fe{sub 2}O{sub 3}) nanoparticles were directly grown on graphene oxide (GO) using a facile microwave assistant method. • The effect of urea concentration on Fe{sub 2}O{sub 3} nanoparticles and GO/Fe{sub 2}O{sub 3} composite was examined. • Increasing urea concentration altered the morphology and decreased the particle size. • The increased concentration of urea induced a larger surface area with more active sites in the Fe{sub 2}O{sub 3} nanoparticles. • The increase in urea concentration led to decreased thermal stability of the Fe{sub 2}O{sub 3} nanoparticles. - Abstract: Iron oxide (Fe{sub 2}O{sub 3}) nanoparticles were grown on graphene oxide (GO) using a simple microwave-assisted method. The effects of urea concentration on Fe{sub 2}O{sub 3} nanoparticles and GO/Fe{sub 2}O{sub 3} composite were examined. The as-prepared samples were characterized using X-ray powder diffraction, Raman spectroscopy, and transmission electron microscopy. The Fe{sub 2}O{sub 3} nanoparticles were uniformly developed on GO sheets. The results showed that urea affects both Fe{sub 2}O{sub 3} morphology and particle size. In the absence of urea, the Fe{sub 2}O{sub 3} nanostructures exhibited a rod-like morphology. However, increasing urea concentration altered the morphology and decreased the particle size. The Raman results of GO/Fe{sub 2}O{sub 3} showed that the intensity ratio of D band to G band (I{sub D}/I{sub G}) was decreased by addition of urea, indicating that urea can preserve the GO sheets during synthesis of the composite from exposing more defects. The surface area and thermal stability of GO/Fe{sub 2}O{sub 3} and Fe{sub 2}O{sub 3} were compared using the Brunauer–Emmett–Teller method and thermal gravimetric analysis, respectively. The results showed that the increased concentration of urea induced a larger surface area with more active sites in the Fe{sub 2}O{sub 3} nanoparticles. However, the increase in urea

  3. The Chinese soft-shelled turtle, Pelodiscus sinensis, decreases nitrogenous excretion, reduces urea synthesis and suppresses ammonia production during emersion.

    Science.gov (United States)

    Ip, Yuen K; Lee, Serene M L; Wong, Wai P; Chew, Shit F

    2013-05-01

    The objective of this study was to examine the effects of 6 days of emersion on nitrogen metabolism and excretion in the Chinese soft-shelled turtle, Pelodiscus sinensis. Despite having a soft shell with a cutaneous surface that is known to be water permeable, P. sinensis lost only ~2% of body mass and was able to maintain its hematocrit and plasma osmolality, [Na(+)] and [Cl(-)] during 6 days of emersion. During emersion, it ameliorated water loss by reducing urine output, which led to a reduction (by 29-76%) in ammonia excretion. In comparison, there was a more prominent reduction (by 82-99%) in urea excretion during emersion due to a lack of water to flush the buccopharyngeal epithelium, which is known to be the major route of urea excretion. Consequently, emersion resulted in an apparent shift from ureotely to ammonotely in P. sinensis. Although urea concentration increased in several tissues, the excess urea accumulated could only account for 13-22% of the deficit in urea excretion. Hence, it can be concluded that a decrease (~80%) in urea synthesis occurred in P. sinensis during the 6 days of emersion. Indeed, emersion led to significant decreases in the activity of some ornithine-urea cycle enzymes (argininosuccinate synthetase/argininosuccinate lyase and arginase) from the liver of P. sinensis. As a decrease in urea synthesis occurred without the accumulation of ammonia and total free amino acids, it can be deduced that ammonia production through amino acid catabolism was suppressed with a proportional reduction in proteolysis in P. sinensis during emersion. Indeed, calculated results revealed that there could be a prominent decrease (~88%) in ammonia production in turtles after 6 days of emersion. In summary, despite being ureogenic and ureotelic in water, P. sinensis adopted a reduction in ammonia production, instead of increased urea synthesis, as the major strategy to ameliorate ammonia toxicity and problems associated with dehydration during

  4. Genetic and chemical reductions in protein phosphatase activity alter auxin transport, gravity response, and lateral root growth

    Science.gov (United States)

    Rashotte, A. M.; DeLong, A.; Muday, G. K.; Brown, C. S. (Principal Investigator)

    2001-01-01

    Auxin transport is required for important growth and developmental processes in plants, including gravity response and lateral root growth. Several lines of evidence suggest that reversible protein phosphorylation regulates auxin transport. Arabidopsis rcn1 mutant seedlings exhibit reduced protein phosphatase 2A activity and defects in differential cell elongation. Here we report that reduced phosphatase activity alters auxin transport and dependent physiological processes in the seedling root. Root basipetal transport was increased in rcn1 or phosphatase inhibitor-treated seedlings but showed normal sensitivity to the auxin transport inhibitor naphthylphthalamic acid (NPA). Phosphatase inhibition reduced root gravity response and delayed the establishment of differential auxin-induced gene expression across a gravity-stimulated root tip. An NPA treatment that reduced basipetal transport in rcn1 and cantharidin-treated wild-type plants also restored a normal gravity response and asymmetric auxin-induced gene expression, indicating that increased basipetal auxin transport impedes gravitropism. Increased auxin transport in rcn1 or phosphatase inhibitor-treated seedlings did not require the AGR1/EIR1/PIN2/WAV6 or AUX1 gene products. In contrast to basipetal transport, root acropetal transport was normal in phosphatase-inhibited seedlings in the absence of NPA, although it showed reduced NPA sensitivity. Lateral root growth also exhibited reduced NPA sensitivity in rcn1 seedlings, consistent with acropetal transport controlling lateral root growth. These results support the role of protein phosphorylation in regulating auxin transport and suggest that the acropetal and basipetal auxin transport streams are differentially regulated.

  5. Synthesis of propylene carbonate from urea and 1,2-propanediol

    Institute of Scientific and Technical Information of China (English)

    Zhi Wen Gao; Shou Feng Wang; Chun Gu Xia

    2009-01-01

    The production of propylene carbonate(PC)from urea and 1,2-propanediol(PG)was investigated in a batch process.The catalytic performances of zinc chloride and magnesium chloride were investigated for this reaction system.The influences of various operation conditions on the PC yield were explored.In this work,MgCl2 and ZnCl2 showed the excellent catalytic activity toward PC synthesis,and the yields of propylene carbonate reached 96.5% and 92.4%,respectively.The optimum reaction conditions were as follows:ethanol/urea molar ratio of 4,catalyst concentration of 1.5%,reaction temperature of 160 ℃,reaction time of 3 h,respectively.The route from urea and 1,2-propanediol shows advantages,such as mild reaction condition and safe operation.The catalytic system is environmentally benign.

  6. A Facile, Choline Chloride/Urea Catalyzed Solid Phase Synthesis of Coumarins via Knoevenagel Condensation

    Directory of Open Access Journals (Sweden)

    Hosanagara N. Harishkumar

    2011-01-01

    Full Text Available The influence of choline chloride/urea ionic liquid in solid phase on the Knoevenagel condensation is demonstrated. The active methylene compounds such as meldrum’s acid, diethylmalonate, ethyl cyanoacetate, dimethylmalonate, were efficiently condensed with various salicylaldehydes in presence of choline chloride/urea ionic liquid without using any solvents or additional catalyst. The reaction is remarkably facile because of the air and water stability of the catalyst, and needs no special precautions. The reactions were completed within 1hr with excellent yields (95%. The products formed were sufficiently pure, and can be easily recovered. The use of ionic liquid choline chloride/urea in solid phase offered several significant advantages such as low cost, greater selectivity and easy isolation of products.

  7. A theoretical study on the water-mediated asynchronous addition between urea and formaldehyde

    Institute of Scientific and Technical Information of China (English)

    Tao-Hong Li; Xiao-Guang Xie; Guan-Ben Du

    2013-01-01

    The reaction between urea and formaldehyde in water solution was theoretically investigated by using B3LYP and MP2 methods,It was found that the addition of the nitrogen atom in urea to the carbonyl group in formaldehyde precedes the proton transfer and the proton migration from water to the carbonyl group occurs before the proton abstraction from the nitrogen,With one or two water molecules involved in the TS,the activation energy barrier is lowered compared to the TS of the mechanism with no water participation.The energy change along the reaction coordinate clearly shows that a zwitterionic-like intermediate does not exist on the PES.The reaction between urea and formaldehyde occurs in a concerted mechanism but with asynchronous characters.This is different from the stepwise mechanism recently found for the amination reactions of formaldehyde.

  8. Comparison between conformational change and inactivation rates of aminoacylase during denaturation in urea solutions

    Institute of Scientific and Technical Information of China (English)

    王洪睿; 王希成; 张彤; 周海梦

    1995-01-01

    The kinetic method of the substrate reaction in the presence of mactivator previously described by Tsou has been applied to the determination of inactivation rates of aminoacylase during denaturation in urea solutions. The protective effect of substrate on the inactivation of aminoacylase by urea has been investigated. Simultaneously, the comparison between conformational change and inactivation rates of enzyme in the urea solutions of different concentrations has been studied. Results obtained show that the inactivation rate constants of the enzyme are larger than the rate constants of conformational changes. The present results show that the active site of metal enzyme-aminoacylase is also located in a limited and flexible region of the molecule that is more sensitive to denaturants than the enzyme as a whole.

  9. Myoelectrical activity and transport of unfertilized ova in the oviduct of the mouse in vitro.

    Science.gov (United States)

    Talo, A

    1980-09-01

    The relationship of myoelectrical activity to locations and movements of eggs was analysed in 12 mouse oviducts in vitro. When the eggs were in the ampulla the ampullary activity did not spread through the ampullary-isthmic junction (AIJ), and a narrow region of activity of lower frequency separated the ampullary and isthmic activities. When the eggs were in the isthmus the activity beginning on the isthmic side of the AIJ spread towards the uterus for progressively longer distances. Eggs were near or at the front of the plateau formed by this activity. A separate activity arising in one or more areas of the uterine side of the plateau often spread in the ovarian direction, thus opposing movements of eggs and fluid in the uterine direction. Transport of unfertilized eggs appears to be regulated by a small number of relatively stable pacemakers in the mouse oviduct.

  10. Ratchet transport of an active-passive mixture chain in confined structures

    Science.gov (United States)

    Lu, Shi-cai; Ou, Ya-li; Ai, Bao-quan

    2017-09-01

    Rectified transport of the active-passive mixture chain is numerically investigated in periodic confined structures. Due to the out-of-equilibrium property of active particles in the chain, the whole chain can be rectified. It is found that the interaction between particles can significantly affect the rectified transport. When all particles in the chain are active, the directed velocity decreases monotonously with increasing the interaction strength. When the particles are mixture, on increasing the interaction strength, the directed velocity firstly decreases to its minimal value, then increases to its maximal value, and finally decreases to zero. In addition, there exist optimal parameters (self-propelled velocity, the natural length of the spring) at which the average velocity is maximal.

  11. Measurement of multiple drug resistance transporter activity in putative cancer stem/progenitor cells.

    Science.gov (United States)

    Donnenberg, Vera S; Meyer, E Michael; Donnenberg, Albert D

    2009-01-01

    Multiple drug resistance, mediated by the expression and activity of ABC-transporters, is a major obstacle to antineoplastic therapy. Normal tissue stem cells and their malignant counterparts share MDR transporter activity as a major mechanism of self-protection. Although MDR activity is upregulated in response to substrate chemotherapeutic agents, it is also constitutively expressed on both normal tissue stem cells and a subset of tumor cells prior to the initiation of therapy, representing a built-in obstacle to therapeutic ratio. Constitutive and induced MDR activity can be detected in cellular subsets of disaggregated tissues, using the fluorescent substrates Rhodamine 123 and Hoechst 33342 for ABCB1 (also known as P-gp and MDR1) and ABCG2 (BCRP1). In this chapter, we will describe the complete procedure for the detection of MDR activity, including: (1) Preparing single-cell suspensions from tumor and normal tissue specimens; (2) An efficient method to perform cell surface marker staining on large numbers of cells; (3) Flow cytometer setup and controls; (4) Simultaneous measurement of Hoechst 33342 and Rhodamine123 transport; and (5) Data acquisition and analysis.

  12. Na+- and Cl−-coupled active transport of carnitine by the amino acid transporter ATB0,+ from mouse colon expressed in HRPE cells and Xenopus oocytes

    Science.gov (United States)

    Nakanishi, Takeo; Hatanaka, Takahiro; Huang, Wei; Prasad, Puttur D; Leibach, Frederick H; Ganapathy, Malliga E; Ganapathy, Vadivel

    2001-01-01

    ATB0,+ is an amino acid transporter energized by transmembrane gradients of Na+ and Cl− and membrane potential. We cloned this transporter from mouse colon and expressed the clone functionally in mammalian (human retinal pigment epithelial, HRPE) cells and Xenopus laevis oocytes to investigate the interaction of carnitine and its acyl esters with the transporter. When expressed in mammalian cells, the cloned ATB0,+ was able to transport carnitine, propionylcarnitine and acetylcarnitine. The transport process was Na+ and Cl− dependent and inhibitable by the amino acid substrates of the transporter. The Michaelis constant for carnitine was 0.83 ± 0.08 mm and the Hill coefficient for Na+ activation was 1.6 ± 0.1. When expressed in Xenopus laevis oocytes, the cloned ATB0,+ was able to induce inward currents in the presence of carnitine and propionylcarnitine under voltage-clamped conditions. There was no detectable current in the presence of acetylcarnitine. Carnitine-induced currents were obligatorily dependent on the presence of Na+ and Cl−. The currents were saturable with carnitine and the Michaelis constant was 1.8 ± 0.4 mm. The analysis of Na+- and Cl−-activation kinetics revealed that 2 Na+ and 1 Cl− were involved in the transport of carnitine via the transporter. These studies describe the identification of a novel function for the amino acid transporter ATB0,+. Since this transporter is expressed in the intestinal tract, lung and mammary gland, it is likely to play a significant role in the handling of carnitine in these tissues. A Na+-dependent transport system for carnitine has already been described. This transporter, known as OCTN2 (novel organic cation transporter 2), is expressed in most tissues and transports carnitine with high affinity. It is energized, however, only by a Na+ gradient and membrane potential. In contrast, ATB0,+ is a low-affinity transporter for carnitine, but exhibits much higher concentrative capacity than OCTN2 because

  13. Variations in active transport behavior among different neighborhoods and across adult life stages

    DEFF Research Database (Denmark)

    Christiansen, Lars Breum; Madsen, Thomas; Schipperijn, Jasper;

    2014-01-01

    OBJECTIVE: Built environment characteristics are closely related to transport behavior, but observed variations could be due to residents own choice of neighborhood called residential self-selection. The aim of this study was to investigate differences in neighborhood walkability and residential...... self-selection across life stages in relation to active transport behavior. METHODS: The IPEN walkability index, which consists of four built environment characteristics, was used to define 16 high and low walkable neighborhoods in Aarhus, Denmark (250.000 inhabitants). Transport behavior was assessed...... using the IPAQ questionnaire. Life stages were categorized in three groups according to age and parental status. A factor analysis was conducted to investigate patterns of self-selection. Multivariable logistic regression analyses were carried out to evaluate the association between walkability...

  14. Light-activated amino acid transport in Halobacterium halobium envelope vesicles

    Science.gov (United States)

    Macdonald, R. E.; Lanyi, J. K.

    1977-01-01

    Vesicles prepared from Halobacterium halobium cell envelopes accumulate amino acids in response to light-induced electrical and chemical gradients. Nineteen of 20 commonly occurring amino acids have been shown to be actively accumulated by these vesicles in response to illumination or in response to an artificially created Na+ gradient. On the basis of shared common carriers the transport systems can be divided into eight classes, each responsible for the transport of one or several amino acids: arginine, lysine, histidine; asparagine, glutamine; alanine, glycine, threonine, serine; leucine, valine, isoleucine, methionine; phenylalanine, tyrosine, tryptophan; aspartate; glutamate; proline. Available evidence suggests that these carriers are symmetrical in that amino acids can be transported equally well in both directions across the vesicle membranes. A tentative working model to account for these observations is presented.

  15. Estimating active transportation behaviors to support health impact assessment in the United States

    Directory of Open Access Journals (Sweden)

    Theodore J Mansfield

    2016-05-01

    Full Text Available Health impact assessment (HIA has been promoted as a means to encourage transportation and city planners to incorporate health considerations into their decision-making. Ideally, HIAs would include quantitative estimates of the population health effects of alternative planning scenarios, such as scenarios with and without infrastructure to support walking and cycling. However, the lack of baseline estimates of time spent walking or biking for transportation (together known as active transportation, which are critically related to health, often prevents planners from developing such quantitative estimates. To address this gap, we use data from the 2009 US National Household Travel Survey to develop a statistical model that estimates baseline time spent walking and biking as a function of the type of transportation used to commute to work along with demographic and built environment variables. We validate the model using survey data from the Raleigh-Durham-Chapel Hill, NC, metropolitan area. We illustrate how the validated model could be used to support transportation-related HIAs by estimating the potential health benefits of built environment modifications that support walking and cycling. Our statistical model estimates that on average, individuals who commute on foot spend an additional 19.8 (95% CI 16.9–23.2 minutes per day walking compared to automobile commuters. Public transit riders walk an additional 5.0 (95% CI 3.5–6.4 minutes per day compared to automobile commuters. Bicycle commuters cycle for an additional 28.0 (95% CI 17.5–38.1 minutes per day compared to automobile commuters. The statistical model was able to predict observed transportation physical activity in the Raleigh-Durham-Chapel Hill region to within 0.5 MET-hours per day (equivalent to about 9 minutes of daily walking time for 83% of observations. Across the Raleigh-Durham-Chapel Hill region, an estimated 38 (95% CI 15–59 premature deaths potentially could be

  16. Estimating Active Transportation Behaviors to Support Health Impact Assessment in the United States.

    Science.gov (United States)

    Mansfield, Theodore J; Gibson, Jacqueline MacDonald

    2016-01-01

    Health impact assessment (HIA) has been promoted as a means to encourage transportation and city planners to incorporate health considerations into their decision-making. Ideally, HIAs would include quantitative estimates of the population health effects of alternative planning scenarios, such as scenarios with and without infrastructure to support walking and cycling. However, the lack of baseline estimates of time spent walking or biking for transportation (together known as "active transportation"), which are critically related to health, often prevents planners from developing such quantitative estimates. To address this gap, we use data from the 2009 US National Household Travel Survey to develop a statistical model that estimates baseline time spent walking and biking as a function of the type of transportation used to commute to work along with demographic and built environment variables. We validate the model using survey data from the Raleigh-Durham-Chapel Hill, NC, USA, metropolitan area. We illustrate how the validated model could be used to support transportation-related HIAs by estimating the potential health benefits of built environment modifications that support walking and cycling. Our statistical model estimates that on average, individuals who commute on foot spend an additional 19.8 (95% CI 16.9-23.2) minutes per day walking compared to automobile commuters. Public transit riders walk an additional 5.0 (95% CI 3.5-6.4) minutes per day compared to automobile commuters. Bicycle commuters cycle for an additional 28.0 (95% CI 17.5-38.1) minutes per day compared to automobile commuters. The statistical model was able to predict observed transportation physical activity in the Raleigh-Durham-Chapel Hill region to within 0.5 MET-hours per day (equivalent to about 9 min of daily walking time) for 83% of observations. Across the Raleigh-Durham-Chapel Hill region, an estimated 38 (95% CI 15-59) premature deaths potentially could be avoided if the entire

  17. Benzotropolone moiety in theaflavins is responsiblefor inhibitingpeptide-transport and activating AMP-activated protein kinase in Caco-2 cells

    Directory of Open Access Journals (Sweden)

    Ha-Young Park

    2013-05-01

    Full Text Available ABSTRACTObjective:In the small intestine, peptide transporter 1 (PEPT1 plays a role in the transport of di- and tri-peptides. Recently, we found that theaflavins (TFs, dimeric catechins, inhibitedthe transport of di-peptides across Caco-2 monolayersby suppressingthe expression of PEPT1 through AMP-activated protein kinase (AMPK activation. In this study, we investigated the structural requirement of theaflavinsfor the effect, and the mechanism(sunderling theaflavin-induced AMPK activation.Methods:Theaflavin-3’-O-gallate (TF3’G was used forthis study, since it possessed the most potent inhibition power for peptide-transport among theaflavins. Absorption ability was measured with Caco-2 cell monolayers treated with or without 20 M sample (TF3’G or its related compounds in an Ussing Chamber. The amountof Gly-Sar (a model of PEPT1-transporing peptide transportat fixed time-pointsto 60min wasdeterminedby fluorescent naphthalene-2,3-dicarboxaldehyde-derivatized assay(Ex/Em: 405 nm/460 nm. The apparent permeability coefficient(Papp wasused to evaluate the permeability. Expression of PEPT1 protein in Caco-2 cells treated with or without 20 M TF3’G in the presence or absence of inhibitor (10 μM compound C as AMPK inhibitor or 25 μMSTO-609 as CaMKK inhibitor wasevaluated by Western blot.Results:The Pappvalue of Gly-Sar significantly (P<0.05 decreasedin 20 μM purprogallin-treated Caco-2 cellsas well asin TF3’G-treated cells, together with the reduction of PEPT1 expression, while their monomeric catechins did not show any Pappreduction. In TF3’G-treated Caco-2 cells, the recovery of the reduced PEPT1 expression was found by 10 μM compound C,but not STO-609.Conclusion:The study demonstrated that the benzotropolone moiety in theaflavins was a crucial structural requirement for exerting the inhibition of intestinal peptide-transport,and the suppression of PEPT1 expression by theaflavins would be caused by activating LKB1/AMPK pathway

  18. Altered nitrogen balance and decreased urea excretion in male rats fed cafeteria diet are related to arginine availability.

    Science.gov (United States)

    Sabater, David; Agnelli, Silvia; Arriarán, Sofía; Fernández-López, José-Antonio; Romero, María del Mar; Alemany, Marià; Remesar, Xavier

    2014-01-01

    Hyperlipidic diets limit glucose oxidation and favor amino acid preservation, hampering the elimination of excess dietary nitrogen and the catabolic utilization of amino acids. We analyzed whether reduced urea excretion was a consequence of higher NO x ; (nitrite, nitrate, and other derivatives) availability caused by increased nitric oxide production in metabolic syndrome. Rats fed a cafeteria diet for 30 days had a higher intake and accumulation of amino acid nitrogen and lower urea excretion. There were no differences in plasma nitrate or nitrite. NO(x) and creatinine excretion accounted for only a small part of total nitrogen excretion. Rats fed a cafeteria diet had higher plasma levels of glutamine, serine, threonine, glycine, and ornithine when compared with controls, whereas arginine was lower. Liver carbamoyl-phosphate synthetase I activity was higher in cafeteria diet-fed rats, but arginase I was lower. The high carbamoyl-phosphate synthetase activity and ornithine levels suggest activation of the urea cycle in cafeteria diet-fed rats, but low arginine levels point to a block in the urea cycle between ornithine and arginine, thereby preventing the elimination of excess nitrogen as urea. The ultimate consequence of this paradoxical block in the urea cycle seems to be the limitation of arginine production and/or availability.

  19. Determination of urea content in urea cream by centrifugal partition chromatography

    Directory of Open Access Journals (Sweden)

    Ying-Qun Wang

    2016-04-01

    Full Text Available The objective of this study is to establish a centrifugal partition chromatography (CPC method for determination of the urea ingredient in urea cream. The mechanism of this method is that urea is determined by UV detector at 430 nm after being extracted from the cream and derivatized on line via Ehrlich reaction in rotor of CPC, where the reaction products dissolve in the mobile phase and the cream matrix retains in the stationary phase. The mixed solvent consisting of n-hexane, methanol, hydrochloric acid and p-dimethylaminobenzaldehyde with a ratio of 1000 mL:1000 mL:18 mL:2.0 g is used for solvent system of CPC. The CPC method proposed offers good precision and convenience without complex sample pretreatment processes.

  20. New benzimidazole-2-urea derivates as tubulin inhibitors.

    Science.gov (United States)

    Wang, Wenna; Kong, Dexin; Cheng, Huimin; Tan, Li; Zhang, Zhang; Zhuang, Xiaoxi; Long, Huoyou; Zhou, Yang; Xu, Yong; Yang, Xiaohong; Ding, Ke

    2014-09-01

    Emerging drug resistance and other drawbacks limit tubulin inhibitors' therapeutic applications and developing novel tubulin inhibitors still attracts intensive efforts. We describe the discovery and structure-activity relationship study of a series of benzimidazole-2-urea derivatives as novel β tubulin inhibitors. The representative compound 6o potently suppressed the proliferation of a panel of human cancer cells (NCI-H460, Colo205, K562, A431, HepG2, Hela, MDA-MB-435S) with IC50 values of 0.040, 0.050, 0.006, 0.026, 1.774, 0.452 and 0.052 μM, respectively. Compound 6o obviously inhibited NCI-H460 spindles formation and induced cell cycle arrest at G2/M phase at 0.10 μM. Computational study suggested that 6o interacts with β tubulin in a novel binding mode. Our results suggested that benzimidazole-2-urea derivatives might be promising tubulin inhibitors with novel binding mode for further development.

  1. A Urea Potentiometric Biosensor Based on a Thiophene Copolymer

    Directory of Open Access Journals (Sweden)

    Cheng-Yuan (Kevin Lai

    2017-03-01

    Full Text Available A potentiometric enzyme biosensor is a convenient detector for quantification of urea concentrations in industrial processes, or for monitoring patients with diabetes, kidney damage or liver malfunction. In this work, poly(3-hexylthiophene-co-3-thiopheneacetic acid (P(3HT-co-3TAA was chemically synthesized, characterized and spin-coated onto conductive indium tin oxide (ITO glass electrodes. Urease (Urs was covalently attached to the smooth surface of this copolymer via carbodiimide coupling. The electrochemical behavior and stability of the modified Urs/P(3HT-co-3TAA/ITO glass electrode were investigated by cyclic voltammetry, and the bound enzyme activity was confirmed by spectrophotometry. Potentiometric response studies indicated that this electrode could determine the concentration of urea in aqueous solutions, with a quasi-Nernstian response up to about 5 mM. No attempt was made to optimize the response speed; full equilibration occurred after 10 min, but the half-time for response was typically <1 min.

  2. Orthotopic Liver Transplantation for Urea Cycle Enzyme Deficiency

    Science.gov (United States)

    Todo, Satoru; Starzl, Thomas E.; Tzakis, Andreas; Benkov, Keith J.; Kalousek, Frantisek; Saheki, Takeyori; Tanikawa, Kyuichi; Fenton, Wayne A.

    2010-01-01

    Hyperammonemia, abnormalities in plasma amino acids and abnormalities of standard liver functions were corrected by orthotopic liver transplantation in a 14-day-old boy with carbamyl phosphate synthetase-I deficiency and in a 35-yr-old man with argininosuccinic acid synthetase deficiency. The first patient had high plasma glutamine levels and no measureable citrulline, whereas citrulline values were markedly increased in Patient 2. Enzyme analysis of the original livers showed undetectable activity of carbamyl phosphate synthetase-I in Patient 1 and arginosuccinic acid synthetase in Patient 2. Both patients were comatose before surgery. Intellectual recovery of patient 1 has been slightly retarded because of a brain abscess caused by Aspergillus infection after surgery. Both patients are well at 34 and 40 mo, respectively, after surgery. Our experience has shown that orthotopic liver transplantation corrects the life-threatening metabolic abnormalities caused by deficiencies in the urea cycle enzymes carbamyl phosphate synthetase-I and arginosuccinic acid synthetase. Seven other patients–six with ornithine transcarbamylase deficiency and another with carbamyl phosphate synthetase-I deficiency–are known to have been treated elsewhere with liver transplantation 1½ yr or longer ago. Four of these seven recipients also are well, with follow-ups of 1½ to 5 yr. Thus liver transplantation corrects the metabolic abnormalities of three of the six urea cycle enzyme deficiencies, and presumably would correct all. PMID:1544622

  3. Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.

    Science.gov (United States)

    Panchaud, Philippe; Bruyère, Thierry; Blumstein, Anne-Catherine; Bur, Daniel; Chambovey, Alain; Ertel, Eric A; Gude, Markus; Hubschwerlen, Christian; Jacob, Loïc; Kimmerlin, Thierry; Pfeifer, Thomas; Prade, Lars; Seiler, Peter; Ritz, Daniel; Rueedi, Georg

    2017-05-11

    Our strategy to combat resistant bacteria consisted of targeting the GyrB/ParE ATP-binding sites located on bacterial DNA gyrase and topoisomerase IV and not utilized by marketed antibiotics. Screening around the minimal ethyl urea binding motif led to the identification of isoquinoline ethyl urea 13 as a promising starting point for fragment evolution. The optimization was guided by structure-based design and focused on antibacterial activity in vitro and in vivo, culminating in the discovery of unprecedented substituents able to interact with conserved residues within the ATP-binding site. A detailed characterization of the lead compound highlighted the potential for treatment of the problematic fluoroquinolone-resistant MRSA, VRE, and S. pneumoniae, and the possibility to offer patients an intravenous-to-oral switch therapy was supported by the identification of a suitable prodrug concept. Eventually, hERG K-channel block was identified as the main limitation of this chemical series, and efforts toward its minimization are reported.

  4. Influence of milk urea concentration on fractional urea disappearance rate from milk to blood plasma in dairy cows.

    Science.gov (United States)

    Spek, J W; Dijkstra, J; Bannink, A

    2016-05-01

    The relationship between milk urea nitrogen (MUN; mg of N/dL) and urinary N excretion is affected, among others, by diurnal dynamics in MUN, which in turn is largely influenced by feed intake pattern and characteristics of urea transfer from blood plasma to milk and vice versa. This study aimed to obtain insight in urea transfer characteristics within the mammary gland and from the mammary gland to blood plasma in dairy cows at various concentrations of plasma urea nitrogen (PUN; mg of N/dL) and MUN. Urea transfer from milk to blood plasma and urea transfer within the mammary gland itself was evaluated in a 4×4 Latin square design using 4 lactating multiparous Holstein-Friesian cows (milk production of 39.8±4.70kg/d and 90±3.9 d in milk). Treatments consisted of 4 primed continuous intravenous urea infusions of 0, 5, 10, and 15g of urea/h. Boluses of [(15)N(15)N]urea were injected in cistern milk at 20, 60, and 100 min before the 1700h milking. Milk was collected in portions of approximately 2 L at the 1700h milking. Milk samples were analyzed for urea and enrichment of (15)N-urea. Results from one cow were discarded because of leakage of milk from the teats after injection of boluses of [(15)N(15)N]urea. Increasing urea infusion rate linearly increased PUN from 11.4 (0g of urea/h) to 25.9mg/dL (15g of urea/h) and MUN from 10.3 (0g of urea/h) to 23.5 (15g of urea/h) mg of N/dL. The percentage of injected [(15)N(15)N]urea recovered from milk at the time of injection was not affected by urea infusion rate and varied between 65.1 and 73.0%, indicating that a substantial portion of injected [(15)N(15)N]urea was not accounted for by collected milk. The estimated fractional disappearance rate of (15)N-urea from milk to blood (Kurea; per hour) linearly increased from 0.429 (0g of urea/h) to 0.641 per hour (15g of urea/h). Cistern injected [(15)N(15)N]urea diffused within 20 min after injection toward alveoli milk. Calculations with the average Kurea estimated in this

  5. Modulation of LAT1 (SLC7A5) transporter activity and stability by membrane cholesterol

    Science.gov (United States)

    Dickens, David; Chiduza, George N.; Wright, Gareth S. A.; Pirmohamed, Munir; Antonyuk, Svetlana V.; Hasnain, S. Samar

    2017-01-01

    LAT1 (SLC7A5) is a transporter for both the uptake of large neutral amino acids and a number of pharmaceutical drugs. It is expressed in numerous cell types including T-cells, cancer cells and brain endothelial cells. However, mechanistic knowledge of how it functions and its interactions with lipids are unknown or limited due to inability of obtaining stable purified protein in sufficient quantities. Our data show that depleting cellular cholesterol reduced the Vmax but not the Km of the LAT1 mediated uptake of a model substrate into cells (L-DOPA). A soluble cholesterol analogue was required for the stable purification of the LAT1 with its chaperon CD98 (4F2hc,SLC3A2) and that this stabilised complex retained the ability to interact with a substrate. We propose cholesterol interacts with the conserved regions in the LAT1 transporter that have been shown to bind to cholesterol/CHS in Drosophila melanogaster dopamine transporter. In conclusion, LAT1 is modulated by cholesterol impacting on its stability and transporter activity. This novel finding has implications for other SLC7 family members and additional eukaryotic transporters that contain the LeuT fold. PMID:28272458

  6. Symplasmic networks in secondary vascular tissues: parenchyma distribution and activity supporting long-distance transport.

    Science.gov (United States)

    Spicer, Rachel

    2014-04-01

    Stems that develop secondary vascular tissue (i.e. xylem and phloem derived from the vascular cambium) have unique demands on transport owing to their mass and longevity. Transport of water and assimilates must occur over long distances, while the increasing physical separation of xylem and phloem requires radial transport. Developing secondary tissue is itself a strong sink positioned between xylem and phloem along the entire length of the stem, and the integrity of these transport tissues must be maintained and protected for years if not decades. Parenchyma cells form an interconnected three-dimensional lattice throughout secondary xylem and phloem and perform critical roles in all of these tasks, yet our understanding of their physiology, the nature of their symplasmic connections, and their activity at the symplast-apoplast interface is very limited. This review highlights key historical work as well as current research on the structure and function of parenchyma in secondary vascular tissue in the hopes of spurring renewed interest in this area, which has important implications for whole-plant transport processes and resource partitioning.

  7. Community Vision and Interagency Alignment: A Community Planning Process to Promote Active Transportation.

    Science.gov (United States)

    DeGregory, Sarah Timmins; Chaudhury, Nupur; Kennedy, Patrick; Noyes, Philip; Maybank, Aletha

    2016-04-01

    In 2010, the Brooklyn Active Transportation Community Planning Initiative launched in 2 New York City neighborhoods. Over a 2-year planning period, residents participated in surveys, school and community forums, neighborhood street assessments, and activation events-activities that highlighted the need for safer streets locally. Consensus among residents and key multisectoral stakeholders, including city agencies and community-based organizations, was garnered in support of a planned expansion of bicycling infrastructure. The process of building on community assets and applying a collective impact approach yielded changes in the built environment, attracted new partners and resources, and helped to restore a sense of power among residents.

  8. Fluoride and urea chewing gums in an intra-oral experimental caries model

    NARCIS (Netherlands)

    Sjogren, K; Ruben, J; Lingstrom, P; Lundberg, AB; Birkhed, D

    2002-01-01

    The aim of the present investigation was to evaluate the effect of sugar-free chewing gums containing fluoride (F) and urea in an intra-oral experimental caries model. Placebo chewing gums (without any active ingredient) and no gum served as controls. Fifteen subjects participated in a cross-over, s

  9. IL-6 has no acute effect on the regulation of urea synthesis in vivo in rats

    DEFF Research Database (Denmark)

    Thomsen, Karen L; Aagaard, Niels K; Grønbæk, Henning

    2011-01-01

    Clinical or experimentally induced, active inflammation up-regulates the in vivo capacity of urea synthesis (CUNS), which promotes nitrogen removal from the body and metabolic catabolism. We have shown that tumor necrosis factor a (TNF-a) up-regulates CUNS and increases interleukin 6 expression (IL...

  10. N-Heterocyclic Carbene-Palladium Complex Catalyzed Oxidative Carbonylation of Amines to Ureas

    Institute of Scientific and Technical Information of China (English)

    ZHENG,Shu-Zhan; PENG,Xin-Gao; LIU,Jian-Ming; SUN,Wei; XIA,Chun-Gu

    2007-01-01

    Palladium carbene shows high efficiency without any promoter on oxidative carbonylation of amines to ureas and a new type of palladium carbene complex containing both an aniline and an NHC ligands was found to be the active species for the reaction.

  11. Criterion distances and correlates of active transportation to school in Belgian older adolescents

    Directory of Open Access Journals (Sweden)

    De Bourdeaudhuij Ilse

    2010-12-01

    Full Text Available Abstract Background Since physical activity levels in older adolescents have the potential to be increased by stimulating active transportation to school (ATS, the most important correlates of ATS should be determined before developing interventions, especially in those adolescents for whom the distance to school is feasible for active commuting. The main aims of this study were to determine criterion distances for ATS in Belgian older adolescents, to examine multidimensional correlates of ATS in adolescents living within a feasible distance from school and to investigate the associations of ATS with total physical activity and with other physical activities besides ATS. Methods In total, 1281 older adolescents (17-18 years from 20 general secondary schools in East- and West-Flanders completed a questionnaire on physical activity behaviors, demographic factors and psychosocial and physical environmental correlates of physical activity. Distance to school was objectively measured using Routenet online route planner. Results In total, 58.4% of the participants commuted actively to school. The criterion distance for ATS could be set at eight kilometers for cycling and two kilometers for walking. For those adolescents living within a feasible distance for ATS, gender, smoking status, walkability of the neighborhood and social modeling were associated with transportation mode choice. ATS was positively associated with total physical activity, but not significantly related to min/week of other physical activities. Conclusions For older adolescents living within eight kilometers of their school, interventions taking into account the correlates found to be related to ATS could possibly be effective to enhance ATS and to increase total physical activity levels. In the context of the overall physical activity decline in adolescence, also interventions targeting physical activity behaviors of adolescents living further away from school might be needed, but

  12. Variation of milk urea in dairy cattle : a study on factors that affect the relationship between urea concentration in milk and urea excretion in urine

    NARCIS (Netherlands)

    Spek, J.W.

    2013-01-01

    The aim of this thesis was to increase the applicability of milk urea nitrogen concentration (MUN) as a predictor of urinary urea nitrogen excretion (UUN) by identifying and quantifying factors that can explain variation in MUN that is not related to UUN. A literature study was conducted in order to

  13. The contribution of SNAT1 to system A amino acid transporter activity in human placental trophoblast

    Energy Technology Data Exchange (ETDEWEB)

    Desforges, M., E-mail: michelle.desforges@manchester.ac.uk [Maternal and Fetal Health Research Centre, Developmental Biomedicine, School of Medicine, Manchester Academic Health Sciences Centre, University of Manchester, St. Mary' s Hospital, Level 5-Research, Oxford Road, Manchester M13 9WL (United Kingdom); Greenwood, S.L.; Glazier, J.D.; Westwood, M.; Sibley, C.P. [Maternal and Fetal Health Research Centre, Developmental Biomedicine, School of Medicine, Manchester Academic Health Sciences Centre, University of Manchester, St. Mary' s Hospital, Level 5-Research, Oxford Road, Manchester M13 9WL (United Kingdom)

    2010-07-16

    Research highlights: {yields} mRNA levels for SNAT1 are higher than other system A subtype mRNAs in primary human cytotrophoblast. {yields} SNAT1 knockdown in cytotrophoblast cells significantly reduces system A activity. {yields} SNAT1 is a key contributor to system A-mediated amino acid transport in human placenta. -- Abstract: System A-mediated amino acid transport across the placenta is important for the supply of neutral amino acids needed for fetal growth. All three system A subtypes (SNAT1, 2, and 4) are expressed in human placental trophoblast suggesting there is an important biological role for each. Placental system A activity increases as pregnancy progresses, coinciding with increased fetal nutrient demands. We have previously shown SNAT4-mediated system A activity is higher in first trimester than at term, suggesting that SNAT1 and/or SNAT2 are responsible for the increased system A activity later in gestation. However, the relative contribution of each subtype to transporter activity in trophoblast at term has yet to be evaluated. The purpose of this study was to identify the predominant subtype of system A in cytotrophoblast cells isolated from term placenta, maintained in culture for 66 h, by: (1) measuring mRNA expression of the three subtypes and determining the Michaelis-Menten constants for uptake of the system A-specific substrate, {sup 14}C-MeAIB, (2) investigating the contribution of SNAT1 to total system A activity using siRNA. Results: mRNA expression was highest for the SNAT1 subtype of system A. Kinetic analysis of {sup 14}C-MeAIB uptake revealed two distinct transport systems; system 1: K{sub m} = 0.38 {+-} 0.12 mM, V{sub max} = 27.8 {+-} 9.0 pmol/mg protein/20 min, which resembles that reported for SNAT1 and SNAT2 in other cell types, and system 2: K{sub m} = 45.4 {+-} 25.0 mM, V{sub max} = 1190 {+-} 291 pmol/mg protein/20 min, which potentially represents SNAT4. Successful knockdown of SNAT1 mRNA using target-specific si

  14. Sediment transport in an active erodible channel bend of Brahmaputra river

    Indian Academy of Sciences (India)

    Tapas Karmaker; Y Ramprasad; Subashisa Dutta

    2010-12-01

    Spatial variation of sediment transport in an alluvial sand-bed river bend needs to be understood with its influencing factors such as bank erosion, secondary current formation, land spur and bed-material characteristics. In this study, detailed hydrographic surveys with Acoustic Doppler Current Profiler (ADCP) were conducted at an active erodible river bend to measure suspended load, velocity, bathymetric profile and characteristics of the bed material. Study indicates the presence of multi-thread flow in the channel bend. Local variation of sediment transport is primarily controlled by active bank erosion, land spur and sand bar formation. Vertical distribution of suspended sediment concentration follows a power function with normalized depth. Average bed-material concentration at the reach level is computed from observed sediment profiles, and is compared against various sediment transport functions. Results show that the sediment transport function suggested by Yang gives better predictions for this reach. Transverse bed slopes at critical survey transects were computed from the bathymetric data and evaluated with analytical approaches. Out of three analytical approaches used, Odgaard’s approach estimates the bed slopes fairly close to the observed one. These two functions are suitable in the Brahmaputra river for further morphological studies.

  15. Quantification of ionic transport within thermally-activated batteries using electron probe micro-analysis

    Science.gov (United States)

    Humplik, Thomas; Stirrup, Emily K.; Grillet, Anne M.; Grant, Richard P.; Allen, Ashley N.; Wesolowski, Daniel E.; Roberts, Christine C.

    2016-07-01

    The transient transport of electrolytes in thermally-activated batteries is studied using electron probe micro-analysis (EPMA), demonstrating the robust capability of EPMA as a useful tool for studying and quantifying mass transport within porous materials, particularly in difficult environments where classical flow measurements are challenging. By tracking the mobility of bromine and potassium ions from the electrolyte stored within the separator into the lithium silicon anode and iron disulfide cathode, we are able to quantify the transport mechanisms and physical properties of the electrodes including permeability and tortuosity. Due to the micron to submicron scale porous structure of the initially dry anode, a fast capillary pressure driven flow is observed into the anode from which we are able to set a lower bound on the permeability of 10-1 mDarcy. The transport into the cathode is diffusion-limited because the cathode originally contained some electrolyte before activation. Using a transient one-dimensional diffusion model, we estimate the tortuosity of the cathode electrode to be 2.8 ± 0.8.

  16. A fully resolved fluid-structure-muscle-activation model for esophageal transport

    Science.gov (United States)

    Kou, Wenjun; Bhalla, Amneet P. S.; Griffith, Boyce E.; Johnson, Mark; Patankar, Neelesh A.

    2013-11-01

    Esophageal transport is a mechanical and physiological process that transfers the ingested food bolus from the pharynx to the stomach through a multi-layered esophageal tube. The process involves interactions between the bolus, esophageal wall composed of mucosal, circular muscle (CM) and longitudinal muscle (LM) layers, and neurally coordinated muscle activation including CM contraction and LM shortening. In this work, we present a 3D fully-resolved model of esophageal transport based on the immersed boundary method. The model describes the bolus as a Newtonian fluid, the esophageal wall as a multi-layered elastic tube represented by springs and beams, and the muscle activation as a traveling wave of sequential actuation/relaxation of muscle fibers, represented by springs with dynamic rest lengths. Results on intraluminal pressure profile and bolus shape will be shown, which are qualitatively consistent with experimental observations. Effects of activating CM contraction only, LM shortening only or both, for the bolus transport, are studied. A comparison among them can help to identify the role of each type of muscle activation. The support of grant R01 DK56033 and R01 DK079902 from NIH is gratefully acknowledged.

  17. Effect of feed forage particle size and dietary urea on excretion of phosphorus in lactating dairy cows

    DEFF Research Database (Denmark)

    Puggaard, Liselotte; Lund, Peter; Sehested, Jakob

    2013-01-01

    Thirty six multiparous Danish Holstein cows, 222 days from calving with a standard deviation (±) of 102 days, 627±7 kg of body weight, and 32±3 kg/d energy corrected milk were used to investigate the effect of forage particle size (FPS) and dietary urea supplementation on excretion of phosphorus (P......) in feces and urine when cows were fed P below requirement. Dietary P content was 2.5 g P/kg DM in all treatments. Treatments (CONTROL, SHORT and LOW-N) were all based on the same content of forage ingredients but varied in FPS and dietary urea content. In CONTROL and SHORT rumen degradable protein...... was optimized according to the Nordic protein evaluation system by supplementing dietary urea, whereas urea was excluded in LOW-N in order to obtain a supply of rumen degradable protein below requirements. It was hypothesized that dietary factors that reduce saliva secretion via reduced chewing activity...

  18. Urea's effect on the ribonuclease A catalytic efficiency: a kinetic, 1H NMR and molecular orbital study.

    Science.gov (United States)

    Almarza, Jorge; Rincón, Luis; Bahsas, Alí; Pinto, María Angela; Brito, Francisco

    2013-02-01

    Understanding of protein-urea interactions is one of the greatest challenges to modern structural protein chemistry. Based in enzyme kinetics experiments and (1)H NMR spectroscopic analysis we proposed that urea, at low concentrations, directly interacts with the protonated histidines of the active center of RNase A, following a simple model of competitive inhibition. These results were supported by theoretical analysis based on the frontier molecular orbital theory and suggest that urea might establish a favorable interaction with the cationic amino acids. Our experimental evidence and theoretical analysis indicate that the initials steps of the molecular mechanism of Urea-RNase A interaction passes through the establishment of a three center four electron adduct. Also, our results would explain the observed disruption of the (1)H NMR signals corresponding to H12 and H119 (involved in catalysis) of the RNase A studied in the presence of urea. Our interaction model of urea-amino acids (cationic) can be extended to explain the inactivation of other enzymes with cationic amino acids at the active site.

  19. Optical enzyme sensor for urea determination via immobilized pH indicator and urease onto transparent membranes.

    Science.gov (United States)

    Krysteva, Milka; Al Hallak, Mohamed

    2003-07-01

    Transparent triacetylcellulose membranes with immobilized pH indicator (neutral red) as well as with simultaneously immobilized urease and neutral red were used as optical sensors for determination of urea concentrations in model solutions. Decomposition of urea with the enzyme urease is accompanied by evolution of ammonia. This leads to the changes of the neutral red absorption, which is proportional to the substrate (urea) within certain concentration limits in model solution. As a result of the investigation, standard curves were plotted for determination of urea over the range of 1 to 500 mM using immobilized indicator and free urease. Simultaneous immobilization of indicator and urease permitted determination of urea in the interval 50 to 500 mM. The membrane used contained 0.169 U urease activity on an area of 1.7 cm2. The standard curves were plotted using the linear region of the kinetic curves for the corresponding substrate concentrations. A possible scheme of the interaction between the activated triacetylcellulose membrane and the indicator and enzyme is proposed. The membranes obtained are suitable for repeated ecological applications where urea is to be determined.

  20. Optical Enzyme Sensor for Urea Determination via Immobilized pH Indicator and Urease onto Transparent Membranes

    Directory of Open Access Journals (Sweden)

    Milka Krysteva

    2003-01-01

    Full Text Available Transparent triacetylcellulose membranes with immobilized pH indicator (neutral red as well as with simultaneously immobilized urease and neutral red were used as optical sensors for determination of urea concentrations in model solutions. Decomposition of urea with the enzyme urease is accompanied by evolution of ammonia. This leads to the changes of the neutral red absorption, which is proportional to the substrate (urea within certain concentration limits in model solution. As a result of the investigation, standard curves were plotted for determination of urea over the range of 1 to 500 mM using immobilized indicator and free urease. Simultaneous immobilization of indicator and urease permitted determination of urea in the interval 50 to 500 mM. The membrane used contained 0.169 U urease activity on an area of 1.7 cm2. The standard curves were plotted using the linear region of the kinetic curves for the corresponding substrate concentrations. A possible scheme of the interaction between the activated triacetylcellulose membrane and the indicator and enzyme is proposed. The membranes obtained are suitable for repeated ecological applications where urea is to be determined.

  1. Home transport and wastage: environmentally relevant household activities in the life cycle of food.

    Science.gov (United States)

    Sonesson, Ulf; Anteson, Frida; Davis, Jennifer; Sjödén, Per-Olow

    2005-06-01

    In environmental systems analysis of food production systems, the consumer phase (home transport, cooking, storing, and wastage) is an important contributor to the total life-cycle environmental impact. However, households are the least investigated part of the food chain. Information gathering about households involves difficulties; the number of households is large, and food-related activities are embedded in other household activities. In cooperation between researchers from environmental systems analysis and consumer research, Swedish households were surveyed by questionnaire, diary, and interviews. Data on home transport of food and wastage were collected. The average weekly driving distance was 28 to 63 km per household, depending on how trips made in conjunction with other errands are allocated. The wastage of prepared food ranged between 0 and 34% for different food categories, and wastage from storing between 0 and 164% (more food was discarded, e.g. by cleaning out a cupboard, than consumed). In both cases dairy products scored highest.

  2. Experimental thermal transport evolution of silane activated nano-clay reinforced styrene butadiene elastomeric nanocomposites

    Science.gov (United States)

    Iqbal, S. S.; Iqbal, N.; Jamil, T.; Bashir, A.; Shahid, M.

    2016-08-01

    In this study, silane activated nanoclay was reinforced in styrene butadiene rubber (SBR) to enhance the thermal resistance/stability and mechanical properties of SBR. silane activated nanoclay with variant concentrations was impregnated in the rubber matrix to fabricate polymer nanocomposites under control processing conditions. Experimental thermal transport, thermal oxidation, phase transition study, and mechanical properties of the nanocomposite specimens were carried out. Thermal insulation, thermal stability, and heat flow response were remarkably enhanced with the addition of nanokaolinite in the polymer matrix. Phase transition temperatures, their corresponding enthalpies, tensile strength, elastic modulus, elongation at break and hardness of the rubber composites were positively influenced with the filler incorporation into the host matrix. The Even dispersion of nanoreinforcements, morphological and compositional analyses of the thermal transport tested specimens were performed using scanning electron microscopy and energy dispersive spectroscopy, respectively.

  3. Dynamic defect correlations dominate activated electronic transport in SrTiO3

    Science.gov (United States)

    Snijders, Paul C.; Şen, Cengiz; McConnell, Michael P.; Ma, Ying-Zhong; May, Andrew F.; Herklotz, Andreas; Wong, Anthony T.; Ward, T. Zac

    2016-07-01

    Strontium titanate (SrTiO3, STO) is a critically important material for the study of emergent electronic phases in complex oxides, as well as for the development of applications based on their heterostructures. Despite the large body of knowledge on STO, there are still many uncertainties regarding the role of defects in the properties of STO, including their influence on ferroelectricity in bulk STO and ferromagnetism in STO-based heterostructures. We present a detailed analysis of the decay of persistent photoconductivity in STO single crystals with defect concentrations that are relatively low but significantly affect their electronic properties. The results show that photo-activated electron transport cannot be described by a superposition of the properties due to independent point defects as current models suggest but is, instead, governed by defect complexes that interact through dynamic correlations. These results emphasize the importance of defect correlations for activated electronic transport properties of semiconducting and insulating perovskite oxides.

  4. Nanoscale charge transport in cytochrome c3/DNA network: Comparative studies between redox-active molecules

    Science.gov (United States)

    Yamaguchi, Harumasa; Che, Dock-Chil; Hirano, Yoshiaki; Suzuki, Masayuki; Higuchi, Yoshiki; Matsumoto, Takuya

    2015-09-01

    The redox-active molecule of a cytochrome c3/DNA network exhibits nonlinear current-voltage (I-V) characteristics with a threshold bias voltage at low temperature and zero-bias conductance at room temperature. I-V curves for the cytochrome c3/DNA network are well matched with the Coulomb blockade network model. Comparative studies of the Mn12 cluster, cytochrome c, and cytochrome c3, which have a wide variety of redox potentials, indicate no difference in charge transport, which suggests that the conduction mechanism is not directly related to the redox states. The charge transport mechanism has been discussed in terms of the newly-formed electronic energy states near the Fermi level, induced by the ionic interaction between redox-active molecules with the DNA network.

  5. Impact of travel mode shift and trip distance on active and non-active transportation in the São Paulo Metropolitan Area in Brazil

    Directory of Open Access Journals (Sweden)

    Thiago Hérick de Sá

    2015-01-01

    Conclusion: Transport and urban planning policies to reduce individual motorized trips and the number of long trips might produce important health benefits, both by increasing population levels of active transportation and reducing the non-active and the total time of daily trips.

  6. Interactions of ( sup 3 H)amphetamine with rat brain synaptosomes. II. Active transport

    Energy Technology Data Exchange (ETDEWEB)

    Zaczek, R.; Culp, S.; De Souza, E.B. (Addiction Research Center, Baltimore, MD (USA))

    1991-05-01

    The accumulation of 5 nM d-({sup 3}H)amphetamine (d-({sup 3}H)AMPH) into rat brain synaptosomes was examined using physiological buffer conditions. The accumulation of d-({sup 3}H)AMPH into striatal synaptosomes was saturable, of high affinity, ouabain-sensitive and temperature-dependent, suggesting an active transport phenomenon. Eadee-Hofstee analysis of striatal d-({sup 3}H)AMPH transport (AMT) saturation isotherms indicated an apparent Km of 97 nM and a Vmax of 3.0 fmol/mg tissue/min. Lesion of the striatal dopaminergic innervation led to equivalent decreases of ({sup 3}H) dopamine (DA) transport and AMT, indicating that AMT occurs in DA terminals. Furthermore, AMT was not evident in cerebral cortex, a brain region with a paucity of DA terminals. In competition studies, AMT was stereospecific; d-AMPH (IC50 = 60 nM) was an 8-fold more potent inhibitor of the transport than its I-isomer (IC50 = 466 nM). DA(IC50 = 257 nM), DA uptake blockers and substrates were found to be potent inhibitors of AMT: GBR12909 IC50 = 5 nM; methamphetamine IC50 = 48 nM; methylphenidate IC50 = 53 nM; and cocaine IC50 = 172 nM. In contrast, serotonin was relatively weak in inhibiting AMT (IC50 = 7.9 microM). There was a highly significant (P less than .001; slope = 1.2) linear correlation between the AMT-inhibiting potencies of AMPH analogs and their potencies in stimulating locomotor activity in rodents. AMT may be important in the low dose effects of AMPH such as increased locomotor activity in rodents and stimulant activity in man. Differences between AMT and d-({sup 3}H)AMPH sequestration described earlier, as well as their possible relevance to behavioral and neurochemical sequelae of AMPH administration are also discussed.

  7. System Studies on Active Thermal Protection of a Hypersonic Suborbital Passenger Transport Vehicle

    OpenAIRE

    Schwanekamp, Tobias; Meyer, Frank; Reimer, Thomas; Petkov, Ivaylo; Tröltzsch, Anke; Siggel, Martin

    2014-01-01

    Aerodynamic heating is a critical design aspect for the development of reusable hypersonic transport and reentry vehicles. The reliability in terms of thermal resistance is one of the major driving factors with respect to the design margins, the mass balance and finally the total costs of a configuration. Potential designs of active cooling systems for critical regions such as the vehicle nose and leading edges are presented as well as preliminary approaches for their impact on the total mass...

  8. By your own two feet: factors associated with active transportation in Canada.

    Science.gov (United States)

    Butler, Gregory P; Orpana, Heather M; Wiens, Alexander J

    2007-01-01

    The purpose of this study is to examine socio-demographic, geographic and physical activity correlates of walking and cycling for non-leisure purposes, i.e., to work, school, or errands, in Canada. Cross-sectional data from the Canadian Community Health Survey (CCHS) 2003 (n = 127,610) were analyzed using logistic regression to identify factors associated with active transportation. The dependent variables were walking 6+ hours per week and any cycling per week. Independent variables were based on age; marital, education, working and immigrant status; income; geographic location; smoking; and other physical activity. Age and income were associated with both walking and cycling, as was geographic location and other physical activity. The results demonstrated that, while similar, walking and cycling are associated with different factors, and that socio-demographic, geographic and health behaviour variables must be taken into consideration when modelling these transportation modes. Although walking and cycling are relatively easy means to incorporate physical activity in daily life, these results suggest that it is the young and the physically active who engage in them. This research points to a need to address barriers among those who could benefit the most from increased use of both modes of travel.

  9. Structure of the proton-gated urea channel from the gastric pathogen Helicobacter pylori.

    Science.gov (United States)

    Strugatsky, David; McNulty, Reginald; Munson, Keith; Chen, Chiung-Kuang; Soltis, S Michael; Sachs, George; Luecke, Hartmut

    2013-01-10

    Half the world's population is chronically infected with Helicobacter pylori, causing gastritis, gastric ulcers and an increased incidence of gastric adenocarcinoma. Its proton-gated inner-membrane urea channel, HpUreI, is essential for survival in the acidic environment of the stomach. The channel is closed at neutral pH and opens at acidic pH to allow the rapid access of urea to cytoplasmic urease. Urease produces NH(3) and CO(2), neutralizing entering protons and thus buffering the periplasm to a pH of roughly 6.1 even in gastric juice at a pH below 2.0. Here we report the structure of HpUreI, revealing six protomers assembled in a hexameric ring surrounding a central bilayer plug of ordered lipids. Each protomer encloses a channel formed by a twisted bundle of six transmembrane helices. The bundle defines a previously unobserved fold comprising a two-helix hairpin motif repeated three times around the central axis of the channel, without the inverted repeat of mammalian-type urea transporters. Both the channel and the protomer interface contain residues conserved in the AmiS/UreI superfamily, suggesting the preservation of channel architecture and oligomeric state in this superfamily. Predominantly aromatic or aliphatic side chains line the entire channel and define two consecutive constriction sites in the middle of the channel. Mutation of Trp 153 in the cytoplasmic constriction site to Ala or Phe decreases the selectivity for urea in comparison with thiourea, suggesting that solute interaction with Trp 153 contributes specificity. The previously unobserved hexameric channel structure described here provides a new model for the permeation of urea and other small amide solutes in prokaryotes and archaea.

  10. Association of serotonin transporter promoter regulatory region polymorphism and cerebral activity to visual presentation of food.

    Science.gov (United States)

    Kaurijoki, Salla; Kuikka, Jyrki T; Niskanen, Eini; Carlson, Synnöve; Pietiläinen, Kirsi H; Pesonen, Ullamari; Kaprio, Jaakko M; Rissanen, Aila; Tiihonen, Jari; Karhunen, Leila

    2008-07-01

    Recent functional magnetic resonance imaging (fMRI) studies have revealed links between genetic polymorphisms and cognitive and behavioural processes. Serotonin is a classical neurotransmitter of central nervous system, and it is connected to the control of appetite and satiety. In this study, the relationship between the functional variation in the serotonin transporter gene and the activity in the left posterior cingulate cortex (PCC), a brain area activated by visual food stimuli was explored. Thirty subjects underwent serial fMRI studies and provided DNA for genetic analyses. Subjects homozygous for the long allele exhibited greater left PCC activity in the comparison food > non-food compared with individuals heterozygous or homozygous for the short allele. The association between genotype and activation was linear, the subjects with two copies of the long allele variant having the strongest activation. These results demonstrate the possible genetically driven variation in the response of the left PCC to visual presentation of food in humans.

  11. Mixing it up: Corals take an active role in mass transport

    Science.gov (United States)

    Fernandez, Vicente; Shapiro, Orr; Brumley, Douglas; Garren, Melissa; Guasto, Jeffrey; Kramarski-Winter, Esti; Vardi, Assaf; Stocker, Roman

    2014-11-01

    The growth and health of reef-building corals are limited by corals' ability to exchange nutrients and oxygen with the surrounding, sometimes quiescent, seawater. Mass transport in coral systems has long been considered to occur passively as a result of molecular diffusion and the ambient fluid flow over the coral. Through a combination of microscale visualization experiments and numerical modeling, we demonstrate instead that motile cilia densely covering the coral surface - previously thought to serve cleaning and feeding purposes- actively stir the coral boundary layer by generating persistent vortices above the coral surface. This active mixing was observed over a variety of corals with differing surface geometries. We have quantified the contribution of ciliary surface vortices to mass transport, finding oxygen flux enhancements of 2 to 3 orders of magnitude under environmentally relevant ambient flow conditions. These results reveal a new, active role of the coral animal in regulating its mass transport by engineering its local hydrodynamic environment, an ability that may have an important role in the evolutionary success of reef corals.

  12. Schools, Air Pollution, and Active T