Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.6.1 (sulfatase)
3,205 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A method has been developed to quantify three lidocaine metabolites, N-ethylglycyl-2,6-xylidide (MEGX), glycyl-2,6-xylidide (GX), and 4-hydroxy-2,6-xylidine (4-OH-XY), and their conjugates in pooled human urine using enzymic hydrolysis. The commonly used enzymes, pure beta-glucuronidase, sulfatase, and a mixture of the two, were tested for their efficiencies in hydrolyzing the conjugates. Initially, it was found that 4-OH-XY was highly unstable after it was released from conjugates by beta-glucuronidase and the enzyme mixture. This problem was corrected by purging the sample with nitrogen prior to incubation. It has been determined that 4-OH-XY is present in human urine exclusively as its glucuronide. The percentage of MEGX in free and in conjugated forms (glucuronide, sulfate, and others) are 44.9 +/- 6.8, 16.6 +/- 4.5, 6.6 +/- 1.8, and 31.9 +/- 4.4, respectively. GX was present mostly in the free form (90.6 +/- 10.5%).
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PMID:Quantification of three lidocaine metabolites and their conjugates. 236 19

A reversed-phase high-performance liquid chromatographic method is described, which allows the simultaneous quantification of propranolol and 4-hydroxypropranolol enantiomers in human plasma. After extraction from plasma (pH 10.5) using ethyl acetate, the enantiomers are derivatized with R-(+)-phenylethylisocyanate as chiral derivatization reagent and triethylamine as basic catalyst in chloroform. Ascorbic acid is used to prevent 4-hydroxypropranolol from oxidation during the extraction. Chromatographic separation on ODS columns and fluorescence detection (228 nm/greater than 340 nm) allows sensitive quantitation of all derivatives. Incubation of the plasma samples with beta-glucuronidase/arylsulfatase and the use of the specific beta-glucuronidase inhibitor saccharo-1,4-lactone allows the quantitation of both the sulfate and glucuronide conjugates of the enantiomers. The method was applied to human plasma samples from a subject after administration of 60 mg racemic propranolol three times daily.
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PMID:Simultaneous determination of propranolol and 4-hydroxypropranolol enantiomers after chiral derivatization using reversed-phase high-performance liquid chromatography. 238 82

Urinary metabolites and biological half-life of chlorpyrifos (O, O-diethyl-O-3,5,6-trichloro-2-pyridinyl phosphorothioate) were investigated. Male Wistar rats weighing 200 g were intraperitoneally injected with chlorpyrifos at a level of 0.2 mmol/kg body weight. Both chlorpyrifos and 3,5,6-trichloro-2-pyridinol (TCP) levels in blood showed maximum values at 5 h post-injection, and then decreased rapidly. Biological half-lives of the blood chlorpyrifos and TCP were estimated to 8.15 and 24.66 h, respectively. Urine was collected for 96 h post-injection and hydrolyzed with 4 N HCl or beta-glucuronidase with sulfatase, and TCP released was determined. Urinary excretion levels of the acid hydrolysis-released TCP and the enzyme hydrolysis-released TCP accounted for 86 and 54% of chlorpyrifos administered, respectively. Urinary excretion levels of alkylphosphate for 96 h post-injection were analyzed. The excretion levels of diethylthiophosphate (DETP) and diethylphosphate (DEP) accounted for 45 and 15% of chlorpyrifos administered, respectively. These results indicate that 1) about half of the chlorpyrifos administered was directly hydrolyzed to DETP and TCP, 2) 10 to 20% was hydrolyzed to DEP and TCP after the oxidation to chlorpyrifos oxon, and 3) about 30% was dealkylated to TCP-phosphate after the oxidation.
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PMID:[Metabolism and urinary excretion of chlorpyrifos in rats]. 247 31

Interleukin-1 (IL-1) plays a major role in the response to infection, inflammation, and immunological challenge. Eosinophils participate in the host response to parasitic infection and allergic and hypersensitivity diseases. The role of IL-1 in these disease states has not been extensively explored. We have reported that purified human monocyte derived IL-1 (mIL-1), a mixture of the two IL-1 forms but predominantly consisting of IL-1 beta, modulates eosinophil oxidative metabolism and enzyme secretion. Although the two major species of IL-1 (IL-1 alpha and IL-1 beta) have identical specific activities on T cells, we now report the selective effects of human recombinant IL-1 (hrIL-1) alpha and hrIL-1 beta on eosinophil function. Whereas hrIL-1 beta caused a significant increase in arylsulfatase secretion (235.4 +/- 29% of resting secretion, P less than or equal to .01) and beta-glucuronidase secretion (135.8 +/- 9.6% of resting secretion, P less than or equal to .02) similar to our experience with mIL-1, hrIL-1 alpha had no effect on enzyme secretion. However, a mixture of hrIL-1 alpha and hrIL-1 beta reproduced the ability of mIL-1 to inhibit the oxidative response to suboptimal doses of phorbol myristate acetate (PMA). When eosinophils were separated into subpopulations by density gradients, we found that eosinophil responses to IL-1 differed among the populations. These results suggest that eosinophil subpopulations respond selectively to each form of IL-1.
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PMID:Differential effects of interleukin-1 alpha and interleukin-1 beta on human peripheral blood eosinophils. 254 Aug 58

Platelet-activating factor (PAF) is a highly active mediator which has been implicated in allergic inflammation and bronchial asthma, possibly by interacting with eosinophils. We have examined the effect of PAF on activation of purified human eosinophils as measured by degranulation (eosinophil peroxidase, eosinophil cationic protein, arylsulfatase B, beta-glucuronidase, and alkaline phosphatase) and oxidative metabolism (superoxide anion production). PAF induced enzyme release at concentrations ranging from 1 pM to 10 microM in a rapid (t1/2 5 to 8 min), Ca2+-dependent and noncytotoxic manner from both the specific and small granules, whereas its biologic precursor and metabolite, lyso-PAF, had no effect. For all enzymes, maximal enzyme release occurred at 100 nM PAF with a mean ED50 value of 1.47 +/- 0.4 nM. At this concentration the mean percentage of total enzyme release by PAF from specific granules was 20.3 +/- 1.6% (17.9% for eosinophil peroxidase, 20.6% for beta-glucuronidase, 22.4% for alkaline phosphatase) and 28.8 +/- 2.2% from small granules (arylsulfatase B). Calcium ionophore A23187, PMA, and opsonized zymosan also induced eosinophil degranulation but their peak effect after 10-min incubation with maximal release 14.7%, 12.9%, or 14.1%, respectively, was lower when compared with PAF. Incubation of eosinophils with the PAF-antagonist WEB 2086 led to a parallel shift of the dose-response curve to the right, indicating a competitive antagonism. PAF also caused generation of superoxide anions by human eosinophils but this occurred at higher concentrations of PAF (1 microM to 30 microM) with an ED50 of 8.4 +/- 0.9 microM. Again, this effect was competitively inhibited by WEB 2086. These studies demonstrate that PAF activates human eosinophils to release granule constituents and generate superoxide anions. Since both PAF and eosinophil products are associated with pathogenesis of bronchial asthma our findings may be of particular pathophysiologic relevance.
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PMID:Stimulation of degranulation from human eosinophils by platelet-activating factor. 254 Nov 98

The enzymes sulfatase and beta-glucuronidase from Helix pomatia were simultaneously immobilized on aminopropyl control pore glass. Once immobilized, these enzymes retained activity under varied conditions of pH, organic solvent, and temperature. To hydrolyze the sulfate and glucuronide conjugates of xenobiotics, the immobilized enzymes were either added directly to incubation mixtures for qualitative in vitro studies or packed in a short stainless steel column and placed in an HPLC system for quantitative studies. By incorporating specific inhibitors (D-saccharic acid-1,4-lactone to inhibit beta-glucuronidase or phosphate ions to inhibit sulfatase) into the incubation mixture or into the HPLC mobile phases, selective hydrolysis of either sulfate or glucuronide conjugates was achieved. Upon removal of the inhibitors from the incubation mixtures or from the mobile phases, original enzyme activity was restored. The utility of immobilized enzymes was demonstrated for quantitative analysis of sulfate and glucuronide conjugates of fenoldopam, where the liberation of the catechol aglycone moiety was necessary for electrochemical detection.
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PMID:Immobilized sulfatase:beta-glucuronidase enzymes for the qualitative and quantitative analysis of drug conjugates. 256 76

The metabolism of an orally administered, 10-mg single dose of the antianxiety drug buspirone was studied in the rat. Samples of bile and urine were collected for 6 hr and were treated with beta-glucuronidase/arylsulfatase. The deconjugated metabolites were isolated and purified by HPLC. Structural analysis was carried out by combined gas chromatography/electron impact mass spectrometry as their trimethylsilyl derivatives and by 1H-NMR spectroscopy. Structures of the metabolites were further confirmed by co-elution on HPLC with authentic standards when possible. In addition to the already known metabolites 5-hydroxy-buspirone and 1-pyrimidinylpiperazine, seven major metabolites were unambiguously identified together with unchanged drug. Ten minor metabolites were partially characterized. Hydroxylation alpha to the glutaramidyl carbon at the 6'-position on the bicyclo ring system, hydroxylation on the pyrimidine aromatic ring, and N-dealkylation of the butyl side chain were observed as major routes of metabolism. Minor routes of metabolism observed were: 3'-hydroxylation on the bicyclo ring system and formation of the methylated catechol derivatives. The identified metabolites accounted for greater than 90% of the total metabolites excreted in the rat bile and urine samples.
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PMID:Metabolism of the antianxiety drug buspirone in the rat. 257 98

The metabolism of an oral dose (20 mg) of the antianxiety drug buspirone labeled with 14C/15N was studied in human subjects. 15N was incorporated in the molecule to facilitate structural characterization of the metabolites by mass spectrometry. Urine samples were collected at intervals up to 24 hr and analyzed for radioactivity. Cumulative urinary excretion accounted for 50% of the dose in 24 hr. The urine was hydrolyzed with beta-glucuronidase/arylsulfatase and the deconjugated metabolites were isolated and purified by HPLC. The purified metabolites were identified by GC/MS, 1H-NMR, and comparison with authentic standards when available. Seven metabolites of buspirone were identified unambiguously, together with unchanged drug. Hydroxylation alpha to the glutarimidyl carbonyl at the 6'-position on the spiro ring system, hydroxylation at the 5-position on the pyrimidine ring, and N-dealkylation of the butyl-substituted side chain were major routes of metabolism. The identified metabolites accounted for 88% of the total radioactivity in the urine. A scheme for metabolism of buspirone in human subjects has been proposed.
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PMID:Metabolism of the antianxiety drug buspirone in human subjects. 257 99

Examining the relationships among indicators of the acute inflammatory response in gingival crevicular fluid (GCF) and specific bacterial species in subgingival plaque may provide indications of which bacterial species or groups of species may be associated with potentially destructive host-derived processes. Here we report on the relationship of the subgingival plaque flora to the activity of mammalian forms of the enzymes beta-glucuronidase (beta G), lactate dehydrogenase (LDH), and arylsulfatase (AS) in GCF from a total of 54 4-6 mm periodontal sites from 13 periodontitis patients. Sites were scored for probing depth (PD) and bleeding on probing, and GCF was collected using filter paper strips inserted into the sulcus for 30 s, eluted in buffer and assayed for enzyme activity. 1 week later, the patients were again evaluated for PD and bleeding, and subgingival plaque was removed with a curette oriented toward the pocket epithelium. Plaque samples were examined by darkfield microscopy and cultured anaerobically on selective and non-selective media. Various groups of bacteria, including species of black pigmenting Bacteroides (BPB), Fusobacterium sp., Capnocytophaga sp, Streptococcus sanguis, and total facultative organisms were enumerated. Relationships among the enzymes and bacterial groups expressed as colony-forming unit (CFU) counts or as a % of the total cultivable flora were assessed by Spearman correlation analysis. beta G levels were significantly correlated with populations of spirochetes, B. intermedius, B. gingivalis, and total lactose negative BPB's. Correlation between beta G and F. nucleatum sp. or Capnocytophaga sp. approached but did not reach statistically significant levels. In contrast, LDH activity showed a significant positive correlation with levels of B. gingivalis and total lactose negative BPB's. AS levels were significantly correlated only with B. gingivalis. beta G and LDH showed a significant negative correlation with levels of coccoid forms. Thus, beta G, an acid hydrolase which can serve as a marker for primary granule release from polymorphonuclear leukocytes, was most closely correlated with the micro-organisms found in other studies to be associated with chronic adult periodontitis.
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PMID:Relationship of subgingival plaque flora to lysosomal and cytoplasmic enzyme activity in gingival crevicular fluid. 265 65

Cigarette smokers have been reported to void urine which is more mutagenic, as measured in the Ames bacterial mutation assay, than urine voided by non-smokers. Condensate from the mainstream smoke of a cigarette which heats, but does not burn tobacco (test cigarette) showed no evidence of mutagenicity in a battery of in vitro genotoxicity assays under conditions in which condensate from the mainstream smoke of cigarettes that burn tobacco was mutagenic. The objective of this study was to determine whether the absence of mutagenic activity observed in the in vitro assays would be reflected in the urine of smokers of the test cigarette. 72 subjects (31 smokers and 41 non-smokers) were enrolled in a 6-week study, with the smokers randomly divided into 2 groups. The study was designed as a double crossover, with each smoker smoking both test (tobacco-heating) and reference (tobacco-burning) cigarettes. This design allowed each smoker to serve as his or her own control while at the same time allowing comparisons between groups of non-smokers and smokers of both test and reference cigarettes. 24-h urine samples were collected twice a week and concentrated using XAD-2 resin. Urine concentrates were tested in Ames bacterial strains TA98 and TA100, with and without metabolic activation and with and without beta-glucuronidase/aryl sulfatase. Individuals who smoked the test cigarette voided urine which was significantly less mutagenic than that voided when they smoked reference cigarettes. The mutagenicity of urine from smokers who smoked the test cigarette and non-smokers did not differ under any of the assay conditions used in this study.
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PMID:Human urine mutagenicity study comparing cigarettes which burn or only heat tobacco. 273 80


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