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91.
92.
Dahiya S Chuttani K Khar RK Saluja D Mishra AK Chopra M 《Metallomics : integrated biometal science》2009,1(5):409-417
Development of target-specific diagnostic radiopharmaceuticals has always been a challenging task. For this purpose, design and development of the imaging-friendly variant of a potent antibiotic could aid in treatment planning and follow-up of patients with hard-to-diagnose bacterial infections. Fluoroquinolone analogues were synthesized taking the lead from Ciprofloxacin (the broad spectrum antibiotic) molecule. The idea of modifying fluoroquinolones, and subsequently labeling them, was to preserve their capacity to bind bacteria and thereby enable the compound to specifically target those microorganisms. Three compounds were thus synthesized as derivatives of Ciprofloxacin. The fluoroquinolone analogues were labeled with (99m)Tc by using (99m)Tc pertechnetate with high labeling efficiency for all the formulations. The complexes formed by chelation of (99m)Tc with our synthesized fluoroquinolone analogues showed good in vitro serum stability. The blood clearance study performed in New Zealand White rabbits exhibited a curve indicating the initial fast phase in which radiocomplexed drugs cleared from blood very quickly followed by a slow phase. The in vivo evaluation showed that fluoroquinolone-based radiopharmaceuticals bind to the bacteria present at the site of infection, which results in the retention of the agent at sites of active bacterial infection. The biodistribution data and the scintigrams demonstrated that Staphylococcus aureus bacteria in animal infection models took up the radiopharmaceutical formulations, confirming our hypothesis that (99m)Tc fluoroquinolone derivatives might be useful as diagnostic agents for targeted delivery in bacterial infections. 相似文献
93.
Stereochemistry of Gd3+ and Mn2+ interactions with D-gluconamide derivatives by 13C NMR spectroscopy
Kilian Dill Marsha E. Daman Elaine Decoster Jean M. Lacombe André A. Pavia 《Inorganica chimica acta》1985,106(4):203-208
Natural abundance 13C nuclear magnetic resonance spectroscopy (13C NMR) was used to study the mode of binding of Gd3+ and Mn2+ to the polyol portion of several synthetic D-gluconamides. The results indicate that Gd3+ forms a single, unique binding structure requiring three oxygen atoms. The binding of Mn2+ to the polyol portion of these compounds appears to be nonspecific. The carbohydrate containing model compounds studied may be used to design new metal-ion chelating agents. 相似文献
94.
95.
Rohit Saluja Rashmi Saini Kalyan Mitra Virendra K. Bajpai Madhu Dikshit 《Cell and tissue research》2010,340(2):381-388
The involvement of nitric oxide (NO) as both pro and anti-inflammatory agent in allergic, airway inflammatory, and asthmatic
diseases and the active participation of eosinophils in such ailments have been previously suggested. NO modulates eosinophil
number, migration and their survival. The microenvironment of NO synthase (NOS) in subcellular organelles determines its rate
and efficiency of catalysis, which in turn influences NO generation at distinct intracellular locales. The present study was
undertaken to assess the intracellular distribution of NOS isoforms by transmission electron microscopy followed by morphometric
analysis in human and rat eosinophils. Rat eosinophils were explored in parallel, and since they are widely used as model
systems to mimic human diseases, a comparative study on NOS localization patterns might provide useful information in deciphering
NO role in diverse aspects of eosinophil-related inflammatory ailments. The results demonstrated predominance of neuronal
NOS (nNOS) in the eosinophilic granules and even distribution of inducible NOS (iNOS) and nNOS in the cytoplasm and nucleus
of human eosinophils. In rat eosinophils, however, iNOS was mainly localized in the eosinophilic granules and nucleus, while
nNOS was distributed evenly in cytoplasm and nucleus. Distribution of endothelial NOS (eNOS) in eosinophils was scanty. Differences
in NOS isoforms and their localization in human and rat cells might have implications in differential mode of catalysis and
functional contribution to eosinophil physiology and pathology, warranting detailed investigations. The present study highlights
species-specific differences in the relative abundance and distribution pattern of NOS isoforms in rat and human eosinophils,
which should be considered cautiously in interpreting the rat data to humans. 相似文献
96.
Hietaranta AJ Singh VP Bhagat L van Acker GJ Song AM Mykoniatis A Steer ML Saluja AK 《The Journal of biological chemistry》2001,276(22):18742-18747
97.
Daman Abel Harris Frederick Biwas Suman Wallace James Phoenix David A. 《Molecular and cellular biochemistry》2001,223(1-2):159-163
The protease, mcalpain, has been implicated in a number of pathological conditions. The enzyme is a calciumdependent heterodimer whose activity appears to be modulated by membrane interaction involving a segment, TAMRIL, located in domain V of the protein's small subunit. Based on a sequence analysis of mcalpain, using DWIH and hydrophobic moment plot based methodologies, we have shown that this segment may contribute to a lipid interactive, oblique orientated, helical region. Our results could form a basis for future studies on the postulated lipid modulation of mcalpain activity. 相似文献
98.
99.
R E Powers A K Saluja M J Houlihan M L Steer 《Biochemical and biophysical research communications》1985,131(1):284-288
Dispersed mouse pancreatic acini prelabelled with (3H)-myoinositol generated (3H)-inositol trisphosphate (3H-IP3), (3H)-IP2 and (3H)-IP1 in response to both cholinergic and cholecystokinin analogues. The generation of (3H)-IP3 was very rapid, reaching a maximal value within 5 seconds following hormone stimulation. Stimulation with 10(-3)M carbachol increased (3H)-IP3 to a value which was 13 times that found in unstimulated acini. These results indicate that the mechanism of stimulus-secretion coupling in mouse pancreatic acini may proceed by a mechanism similar to many other systems, including rat pancreatic acini. This sequence includes hormone-stimulated phosphatidylinositol turnover and Ca2+ mobilization, i.e. secretagogue-stimulated generation of IP3 which induces the subsequent release of intracellular Ca2+. These observations differ from those recently reported by Hokin-Neaverson and Sadeghian (J. Biol. Chem. 259: 1346, 1984), in which no hormone stimulated IP3 generation was detected in mouse pancreatic acini. 相似文献
100.
Three monoclonal antibodies to avian lipoprotein lipase have been isolated by fusing spleen cells from immunized BALB/c mice with myeloma P3X-63 Ag 8. The antibodies were detected by their ability to bind immobilized lipoprotein lipase in enzyme-linked immunosorbent assay (ELISA) and by immunoprecipitation of purified enzyme in the presence of second (rabbit anti-mouse) antibodies. Two of these antibodies, CAL1-7 and CAL1-11, inhibited catalytic activity, whereas with CAL1-2 interaction with lipoprotein lipase could be demonstrated only in ELISA and in Western blot assays following denaturation of the enzyme with sodium dodecyl sulfate. An immunoadsorbent column was prepared by coupling immunopurified CAL1-11 to Sepharose-4B. When acetone powder extracts of adipose tissue were applied on the column, 70% of the catalytic activity bound to the matrix. Effective elution was achieved with 1.8 M NaCl, 40% glycerol, 5% acetone, 20 mM Chaps (3[(3-cholamidopropyl)dimethylammonio]propanesulfonate), 0.5 mM EDTA, 1 mM phosphate (pH 6.5). After concentration of the active fractions on a heparin-Sepharose 4B column, the purified enzyme was obtained with an overall recovery of 25%. Sodium dodecyl sulfate polyacrylamide gel electrophoresis demonstrates that the preparation is homogeneous with a major band at Mr 60900. Thus, avian adipose lipoprotein lipase has been purified by a one-step immunoaffinity followed by a concentrating step on heparin-Sepharose 4B. 相似文献