| Uptake and intracellular activity of ketolide HMR 3647 in human phagocytic and non-phagocytic cells. | |
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MedLine Citation:
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PMID: 11298144 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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OBJECTIVE: To evaluate the uptake of HMR 3647 into human neutrophils (PMNs), human peritoneal macrophages (PMOs) and tissue-cultured cells (epithelial cells and fibroblasts), and to assess the intracellular activity of this drug. METHOD: Cell uptake of HMR 3647 was measured by radiometric assay, as described by Klemper and Styrt. Intracellular activity was determined by incubation for 3 h of PMNs containing bacteria in the presence of HMR 3647. RESULTS: The intracellular concentrations were 130 and 71 times higher than extracellular concentrations in PMNs and PMOs, respectively (extracellular concentrations: 2-25 mg/L). The cellular-to-extracellular concentration ratios (C/E) for tissue-cultured cells were lower than those obtained in phagocytic cells but still greater than 5. The uptake of HMR 3647 was rapid and non-saturable in all cells. HMR 3647 was released slowly from phagocytic cells. HMR 3647 (extracellular concentration: 0.5-10 mg/L) did not significantly reduce the intracellular survival rate of Staphylococcus aureus ATCC 25923 in PMNs. CONCLUSIONS: HMR 3647 reaches intracellular concentrations several times higher than extracellular concentrations within phagocytic and non-phagocytic cells. The slow efflux of this drug from phagocytic cells suggests that these cells may be a vehicle for it, delivering it to sites of infection. |
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Authors:
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Pascual A; S Ballesta; I García; E J Perea |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Clinical microbiology and infection : the official publication of the European Society of Clinical Microbiology and Infectious Diseases Volume: 7 ISSN: 1198-743X ISO Abbreviation: Clin. Microbiol. Infect. Publication Date: 2001 Feb |
Date Detail:
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Created Date: 2001-04-12 Completed Date: 2001-08-09 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9516420 Medline TA: Clin Microbiol Infect Country: France |
Other Details:
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Languages: eng Pagination: 65-9 Citation Subset: IM |
Affiliation:
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Department of Microbiology, School of Medicine, Sevilla, Spain. atomas@cica.es |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Bacterial Agents
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pharmacokinetics*,
pharmacology Cells, Cultured Epithelial Cells / metabolism* Fibroblasts / metabolism* Humans Ketolides* Macrolides* Macrophages, Peritoneal / metabolism Neutrophils / metabolism, microbiology Phagocytes / metabolism* Staphylococcal Infections / microbiology Staphylococcus aureus / drug effects, growth & development |
| Chemical | |
Reg. No./Substance:
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0/Anti-Bacterial Agents; 0/Ketolides; 0/Macrolides; 0/telithromycin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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