Document Detail

Clarithromycin transport by gingival fibroblasts and epithelial cells.
MedLine Citation:
PMID:  18650552     Owner:  NLM     Status:  MEDLINE    
Macrolide antibiotics penetrate cells, but the mechanism by which this occurs is unclear. The objective of this study was to characterize the mechanisms of clarithromycin uptake by gingival fibroblasts and oral epithelium. Cultured human gingival fibroblasts and SCC-25 cells were incubated with [(3)H]-clarithromycin. We assayed clarithromycin transport by measuring cell-associated radioactivity over time. Fibroblasts and epithelial cells rapidly accumulated clarithromycin, attaining steady-state intracellular concentrations within 15 minutes. Incubation in medium containing 2 mug/mL clarithromycin yielded steady-state intracellular concentrations of 75.8 mug/mL in fibroblasts and 6.6 mug/mL in SCC-25 cells. Clarithromycin transport exhibited Michaelis-Menten kinetics and was inhibited below 37 degrees C. The Michaelis constants for fibro-blasts and SCC-25 cells were 78.4 and 227 mug/mL, respectively, while the maximum transport velocities were 264 and 381 ng/min/10(6) cells, respectively. Thus, both types of cells take up clarithromycin via a concentrative active transport system. By increasing intracellular clarithromycin levels, this system may enhance the effectiveness of clarithromycin against invasive periodontal pathogens.
C-H Chou; J D Walters
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Journal of dental research     Volume:  87     ISSN:  0022-0345     ISO Abbreviation:  J. Dent. Res.     Publication Date:  2008 Aug 
Date Detail:
Created Date:  2008-07-24     Completed Date:  2008-09-18     Revised Date:  2011-09-26    
Medline Journal Info:
Nlm Unique ID:  0354343     Medline TA:  J Dent Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  777-81     Citation Subset:  D; IM    
College of Dentistry, The Ohio State University Health Sciences Center, Columbus, OH 43218-2357, USA.
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MeSH Terms
Anti-Bacterial Agents / pharmacokinetics*
Carcinoma, Squamous Cell
Cell Line, Tumor
Clarithromycin / pharmacokinetics*
Epithelial Cells / metabolism*
Fibroblasts / metabolism*
Gingiva / cytology*,  metabolism
Tongue Neoplasms
Grant Support
Reg. No./Substance:
0/Anti-Bacterial Agents; 81103-11-9/Clarithromycin

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