Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.31 (beta-glucuronidase)
 7,680 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Tilmicosin is a semi-synthetic macrolide antibiotic, currently approved for veterinary use in cattle and swine respiratory disease. As the concentrations of tilmicosin are generally low in swine lung tissue, the interaction of tilmicosin with three types of swine phagocytes (monocyte-macrophages, alveolar macrophages, and neutrophils) was evaluated to provide an understanding of clinical efficacy. After incubation with radiolabelled tilmicosin, uptake was determined and expressed as the ratio of the intracellular (Ci) to the extracellular (Ce) drug concentration (Ci/Ce). Tilmicosin was avidly accumulated by the swine phagocytes (Ci/Ce 48-69 at 4 h incubation) with 51 to 85% localized in the lysosomes. Uptake was dependent on cell viability, temperature and pH, but was not influenced by the metabolic inhibitors, sodium cyanide or potassium fluoride. However, lipopolysaccharide (LPS) exposure increased tilmicosin uptake by the swine phagocytes. In neutrophils, upon removal of extracellular tilmicosin, 60% of the intracellular tilmicosin was effluxed within the first 30 min, but after 4 h of incubation in drug-free medium, 25% remained cell-associated. In contrast, after 4 h of incubation in drug-free medium, 60% and 45% of tilmicosin remained cell-associated, within alveolar macrophages and monocyte-derived macrophages, respectively. Tilmicosin uptake was observed to increase lysosomal enzyme (acid phosphatase, lysozyme and beta-glucuronidase) production. Finally, neutrophils were shown to transport and efflux bioactive tilmicosin in a test system measuring both neutrophil chemotaxis under agarose and a bioassay measuring inhibition of bacterial growth in the presence of antibiotic in agar. These in vitro interactions of tilmicosin with swine phagocytes suggest an integral role in effecting clinical efficacy.
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PMID:Intracellular accumulation, subcellular distribution and efflux of tilmicosin in swine phagocytes. 973 47

Streptolysins S and O from hemolytic streptococci were found to induce mitochondrial swelling and the release of malic dehydrogenase from mitochondria; no other streptococcal products were as active. Mg(++), cyanide, dinitrophenol, bovine serum albumin, and antimycin all inhibited streptolysin-induced mitochondrial swelling; only the latter two agents prevented release of malic dehydrogenase from the particles. The streptolysins also solubilized beta-glucuronidase from the less numerous lysosomes of mitochondrial fractions. Vitamin A induced swelling of mitochondria with release of malic dehydrogenase and, at higher concentrations, release of beta-glucuronidase. In these effects, streptolysin S and vitamin A resembled cysteine and ascorbate, which induced swelling and lysis of mitochondria together with solubilization of enzymes. In contrast, mitochondrial swelling induced by such agents as phosphate, thyroxine, or substrates was not accompanied by release of enzymes. The release of enzymes from particles is suggested as a criterion for distinguishing "lytic" agents from those which induce mitochondrial swelling dependent upon electron transport. It was possible to dissociate effects on mitochondria and lysosomes in these experiments; less streptolysin was necessary to damage lysosomes than mitochondria; the converse was found with vitamin A. Injury to mitochondria resulted from the direct action of these agents, since the lysosomal enzymes released as a consequence of their action were not capable of inducing mitochondrial swelling or release of enzymes under the conditions studied.
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PMID:STUDIES ON LYSOSOMES. IV. SOLUBILIZATION OF ENZYMES DURING MITOCHONDRIAL SWELLING AND DISRUPTION OF LYSOSOMES BY STREPTOLYSIN S AND OTHER HEMOLYTIC AGENTS. 1419 4

The effects of co-administration of a cassava rich diet and alcohol in rats were investigated. The animals were divided into four groups (1) Control, (2) Alcohol, (3) Cassava and (4) Alcohol + Cassava. Consumption of alcohol along with cassava reduced the alcohol induced toxicity which was evidenced by the lower activities of GOT, GPT, GGT, acid phosphatase and alkaline phosphatase in the liver and serum of co-administered group. The pyruvate content in the blood increased while the lactate content, lactate/pyruvate ratio and the activity of LDH decreased in the blood due to co-administration. The blood cyanide content, serum thiocyanate content and the activities of rhodanase and beta-glucuronidase increased on co-administration. The histopathological studies also revealed that co-administration reduced the alcohol induced toxicity.
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PMID:Effect of co-administration of cassava (Manihot esculenta Crantz) rich diet and alcohol in rats. 1527 Mar 68

Enzyme activity changes in reagent and neoplastic glia are examined. In the case of reagent glia, considerably increased ADPase, ATPase and AMPase values have been observed in experimental elective parenchymal necrosis in the rat, in hypertrophic astrocytes from recent plaques in multiple necrosis, in demyelinisation associated with cyanide encephalopathy, and in reagent astrocytes surrounding tumours and arteriosclerosis sites. Depressed ATPase values have been observed in experimental oedema, as compared with increased TPPase in human oedema. BuChE and ChE activity disappears in both oligodendro- and astroglia near old cerebral infarct sites, whereas there is marked BuChE activity peripherally to multiple sclerosis plaques and in areas of phenylpyruvic oligophrenia demyelinisation. In neoplastic glia, ADPase is clearly evident in malignant gliomas, ATPase is related to the extent of the cell body, AMPase is positive in medulloblastoma cell cytoplasm and beta-glucuronidase increases in anaplasia. Above-normal ChE activity has been observed in astrocyte tumors, while BuChE is greater than that of AChE. Phosphorylase reaction is intense in astrocytoma and in glioblastoma giant cells. Phosphoglucomutase values are below-normal in tumours, except in the case of ependymoma, while both phosphohexoisomerase and hexokinase display increased activity in atypical forms.
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PMID:[Histochemical demonstration of glial enzyme activity. II. Reagent and neoplastic glia]. 1734 Aug 8


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