Home About us Contact
|
Home About us Contact | ||
|
|
||
Complexed Form (complexed + form)
Selected AbstractsIncreases in pH and soluble salts influence the effect that additions of organic residues have on concentrations of exchangeable and soil solution aluminiumEUROPEAN JOURNAL OF SOIL SCIENCE, Issue 3 2002M. S. Mokolobate Summary It has been suggested that additions of organic residues to acid soils can ameliorate Al toxicity. For this reason the effects of additions of four organic residues to an acid soil on pH and exchangeable and soil solution Al were investigated. The residues were grass, household compost, filter cake (a waste product from sugar mills) and poultry manure, and they were added at rates equivalent to 10 and 20 t ha,1. Additions of residues increased soil pH measured in KCl (pH(KCl)) and decreased exchangeable Al3+ in the order poultry manure > filter cake > household compost > grass. The mechanism responsible for the increase in pH differed for the different residues. Poultry manure treatment resulted in lower soil pH measured in water (pH(water)) and larger concentrations of total (AlT) and monomeric (Almono) Al in soil solution than did filter cake. This was attributed to a soluble salt effect, originating from the large cation content of poultry manure, displacing exchangeable Al3+ and H+ back into soil solution. The considerably larger concentrations of soluble C in soil solution originating from the poultry manure may also have maintained greater concentrations of Al in soluble complexed form. There was a significant negative correlation (r = ,0.94) between pH(KCl) and exchangeable Al. Concentrations of AlT and Almono in soil solution were not closely related with pH or exchangeable Al. The results suggest that although additions of organic residues can increase soil pH and decrease Al solubility, increases in soluble salt and soluble C concentrations in soil solution can substantially modify these effects. [source] Effects of inflammatory response on in vivo transgene expression by plasmid DNA in miceJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 8 2008Keiko Kako Abstract To examine the effects of inflammatory response to plasmid DNA (pDNA) on transgene expression, serum tumor necrosis factor-, (TNF-,) was measured after intravenous injection of pDNA or calf thymus DNA (CT DNA) in the naked or complexed form with cationic liposomes (lipoplex). pDNA with many CpG motifs induced TNF-, production regardless of the forms. No significant TNF-, production was detected when CT DNA or methylated pDNA was injected. Clodronate liposomes and dexamethasone were used to deplete phagocytes or to inhibit inflammatory responses, respectively. Transient depletion of phagocytes, such as liver Kupffer cells and splenic macrophages, by clodronate liposomes slightly altered the tissue distribution of 32P-pDNA lipoplex, but significantly reduced the TNF-, production and transgene expression. Dexamethasone significantly inhibited the initial transgene expression, but increased the duration of the expression slightly. Use of NF-,B activity-dependent plasmid vector suggested that the inhibition of NF-,B activation is involved in the reduced expression by these treatments. These findings indicate that tissue macrophages are closely involved in the CpG motif-dependent TNF-, production. It is also suggested that TNF-, activates NF-,B and increases transgene expression by pDNA having many NF-,B binding sites, but TNF-, also reduces transgene expression at later time periods, leading to short-term transgene expression. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97: 3074,3083, 2008 [source] Tetrakis(4-pyridyl)porphyrin Supramolecular Complexes with Cyclodextrins in Aqueous SolutionPHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 2 2006Pinalysa Cosma ABSTRACT The formation of inclusion complexes of hydroxypropyl-,-cyclodextrin, heptakis(2,6-di-O-methyl)-,-cyclodextrin and heptakis(2,3,6-tri-O-methyl)-,-cyclodextrin with 5,10,15,20-tetrakis(4-pyridyl)porphyrin (TpyP) has been studied in aqueous buffer solution (phosphate buffer pH = 7 and I = 0.01 M) to give a structural and spectroscopic characterization of a new class of potential sensitizers for photodynamic therapy. The interaction was investigated by a combination of UVNis absorption, fluorescence anisotropy, time-resolved fluorescence and circular dichroism. The experimental results point to the presence of the pigment in water in a monomeric complexed form. The fluorescence anisotropy measurements suggest that TpyP forms 1:1 complexes with heptakis(2,3,6-tri-O-methyl)-,-cyclodextrin and hydroxypropyl-,-cyclodextrin, while 1:2 complexes are obtained with heptakis(2,6-di-O-methyl)-,-cyclodextrin. [source] Overproduction, crystallization and preliminary diffraction data of ADP-ribose pyrophosphatase from Thermus thermophilus HB8ACTA CRYSTALLOGRAPHICA SECTION D, Issue 10 2003Sachiko Yoshiba An ADP-ribose pyrophosphatase from Thermus thermophilus HB8 was overproduced in Escherichia coli and purified. Gel-filtration chromatography showed the protein to be in a dimeric state. This protein catalyses the Mg2+ - or Zn2+ -dependent hydrolysis of ADP-ribose to AMP and ribose-5,-phosphate. It was crystallized in the absence and the presence of ADP-ribose by the hanging-drop vapour-diffusion method. Complete data sets were collected to 1.50,Ĺ resolution from the apo form using synchrotron radiation and to 2.0,Ĺ resolution from the complexed form. Both crystals belong to space group P3121 or P3221 and contain one molecule in the asymmetric unit. [source] Soil-solution speciation of CD as affected by soil characteristics in unpolluted and polluted soilsENVIRONMENTAL TOXICOLOGY & CHEMISTRY, Issue 3 2005Erik Meers Abstract Total metal content by itself is insufficient as a measure to indicate actual environmental risk. Understanding the mobility of heavy metals in the soil and their speciation in the soil solution is of great importance for accurately assessing environmental risks posed by these metals. In a first explorative study, the effects of general soil characteristics on Cd mobility were evaluated and expressed in the form of empirical formulations. The most important factors influencing mobility of Cd proved to be pH and total soil content. This may indicate that current legislation expressing the requirement for soil sanitation in Flanders (Belgium) as a function of total soil content, organic matter, and clay does not successfully reflect actual risks. Current legal frameworks focusing on total content, therefore, should be amended with criteria that are indicative of metal mobility and availability and are based on physicochemical soil properties. In addition, soil-solution speciation was performed using two independent software packages (Visual Minteq 2.23 and Windermere Humic Aqueous model VI [WHAM VI]). Both programs largely were in agreement in concern to Cd speciation in all 29 soils under study. Depending on soil type, free ion and the organically complexed forms were the most abundant species. Additional inorganic soluble species were sulfates and chlorides. Minor species in solution were in the form of nitrates, hydroxides, and carbonates, the relative importance of which was deemed insignificant in comparison to the four major species. [source] Evaluation of gastric toxicity of indomethacin acid, salt form and complexed forms with hydroxypropyl-,-cyclodextrin on Wistar rats: histopathologic analysisFUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 6 2009A.C. Ribeiro-Rama Abstract Indomethacin (IM) is a non-steroidal anti-inflammatory drug which inhibits prostaglandin biosynthesis. It is practically insoluble in water and has the capacity to induce gastric injury. Hydroxypropyl-,-cyclodextrin (HP-,-CD) is an alkylated derivative of ,-CD with the capacity to form inclusion complexes with suitable molecules. IM is considered to form partial inclusion complexes with HP-,-CD by enclosure of the p -chlorobenzoic part of the molecule in the cyclodextrin channel, reducing the adverse effects. The aim of this paper is to evaluate the gastric damage induced by the IM inclusion complex prepared by freeze-drying and spray-drying. A total of 135 Wistar rats weighing 224.4 ± 62.5 g were put into 10 groups. They were allowed free access to water but were maintained fasted for 18 h before the first administration until the end of the experiment. IM acid-form, IM trihydrated-sodium-salt and IM-HP-,-CD spray and freeze-dried, at normal and toxic doses, were administered through gastric cannula once/day for 3 days. Seventy-two hours after the first administration, the animals were sacrificed and the stomachs collected and prepared for morphological study by using the haematoxylin-eosin technique. Lesion indexes (rated 0/4) were developed and the type of injury was scored according to the severity of damage and the incidence of microscopic evidence of harm. Microscopic assessment demonstrated levels of injury with index one on 10,25%. The type of complexation method had different incidence but the same degree. The results show that IM inclusion complexation protects against gastric injury, reducing the incidence and the maximum degree of severity from 4 to 1, with a better performance of the spray-dried complex. [source] Complexation and chiral drug recognition of an amphiphilic phenothiazine derivative with , -cyclodextrinJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2008Andrés Guerrero-Martínez Abstract Promethazine hydrochloride (PTZ) is an amphiphilic drug derived from the phenothiazine structure that possesses a charged aliphatic chain with a chiral carbon. In the presence of , -cyclodextrin (, -CD), this drug undergoes significant changes of its photophysical properties in aqueous solution. Fluorescence spectroscopy measurements show the formation of a 1:1 stoichiometry complex with quantum yield lower than that of the pure PTZ, and two fluorescence lifetimes, which can be assigned to the free and complexed forms of the drug. In addition, 1H NMR spectra, and 2D rotating-frame Overhauser enhancement spectroscopy (ROESY) were used to characterize the drug and the complex, and to determine the effects of the complexation on the aggregation. For the drug binary system, a noncooperative association process is observed, and in the presence of macrocycle, the chemical shifts reveal a chiral resolution of the drug enantiomers, with different stability constants of the complexes. , -CD modifies the aggregation of PTZ in an extension that confirms the formation of a 1:1 complex. ROE enhancements and molecular modeling strategies show the most likely structure of the complex in solution, in which one of the phenyl rings is buried into the CD cavity, with a slight inclusion of the aliphatic part. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:1484,1498, 2008 [source] Re-examining the role of Lys67 in class C ,-lactamase catalysisPROTEIN SCIENCE, Issue 3 2009Yu Chen Abstract Lys67 is essential for the hydrolysis reaction mediated by class C ,-lactamases. Its exact catalytic role lies at the center of several different proposed reaction mechanisms, particularly for the deacylation step, and has been intensely debated. Whereas a conjugate base hypothesis postulates that a neutral Lys67 and Tyr150 act together to deprotonate the deacylating water, previous experiments on the K67R mutants of class C ,-lactamases suggested that the role of Lys67 in deacylation is mainly electrostatic, with only a 2- to 3-fold decrease in the rate of the mutant vs the wild type enzyme. Using the Class C ,-lactamase AmpC, we have reinvestigated the activity of this K67R mutant enzyme, using biochemical and structural studies. Both the rates of acylation and deacylation were affected in the AmpC K67R mutant, with a 61-fold decrease in kcat, the deacylation rate. We have determined the structure of the K67R mutant by X-ray crystallography both in apo and transition state-analog complexed forms, and observed only minimal conformational changes in the catalytic residues relative to the wild type. These results suggest that the arginine side chain is unable to play the same catalytic role as Lys67 in either the acylation or deacylation reactions catalyzed by AmpC. Therefore, the activity of this mutant can not be used to discredit the conjugate base hypothesis as previously concluded, although the reaction catalyzed by the K67R mutant itself likely proceeds by an alternative mechanism. Indeed, a manifold of mechanisms may contribute to hydrolysis in class C ,-lactamases, depending on the enzyme (wt or mutant) and the substrate, explaining why different mutants and substrates seem to support different pathways. For the WT enzyme itself, the conjugate base mechanism may be well favored. [source] | |||||||||||||