Disposition and intracellular activity of azithromycin in human THP-1 acute monocytes

Hall, Iris H.; Schwab, Ute; Ward, E. Stacy; Butts, John D.; Wolford, Eric; Ives, Timothy J.

doi:10.1016/s0924-8579(02)00187-5

Cited by 16 publications

(24 citation statements)

References 29 publications

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“…This suggests that during the process of differentiation, cells acquire some additional characteristics that are involved in the entry of macrolide antibiotics into cells and the accumulation of macrolide antibiotics in cells. Our data are in contrast to those of Hall et al (10). In their studies, the uptake of azithromycin into THP-1 cells was very high even after only 30 min (I/E ratio, nearly 200 with an extracellular concentration of 4 g/ml).…”

Section: Discussioncontrasting

confidence: 99%

Cellular Uptake and Efflux of Azithromycin, Erythromycin, Clarithromycin, Telithromycin, and Cethromycin

Bosnar

Kelnerić

Munić

et al. 2005

Antimicrob Agents Chemother

141

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Macrolide antibiotics have an outstanding ability to concentrate within host cells, particularly phagocytes. In the study described in this paper five different macrolide antibiotics were compared regarding the uptake and release kinetics in human peripheral blood polymorphonuclear neutrophils (PMNs) and three different cell lines, two phagocytic cell lines (RAW 264.7 and THP-1) and an epithelial cell line (MDCK). Based on the results obtained, the substances tested could be clustered into different groups. Azithromycin constituted the first group, characterized by rapid and nonsaturable uptake into phagocytic cells and a high degree of retention in the preloaded cells. The second group included erythromycin and clarithromycin. These two substances do not exhibit cell specificity; consequently, they are taken up to a similar extent and are released by all cell types studied. Ketolides constituted the last group. Their uptake was saturable in cells of monocytic lineage as well as in nondifferentiated cells of myeloid lineage, and they were rapidly released from all the cell lines studied. However, in PMNs, ketolide uptake was not saturable; and unlike telithromycin, cethromycin rapidly egressed from the loaded cells.

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Section: Discussioncontrasting

confidence: 99%

Cellular Uptake and Efflux of Azithromycin, Erythromycin, Clarithromycin, Telithromycin, and Cethromycin

Bosnar

Kelnerić

Munić

et al. 2005

Antimicrob Agents Chemother

141

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“…After 1 h, cells were harvested by centrifugation at 3500 rpm for 6 min, washed once in the appropriate pH medium, and the pooled extracellular media was discarded. 8 The pelleted cells were resuspended in fresh RPMI-1640 with 10% heat-inactivated FCS and -mercaptoethanol adjusted to pH 7.4, 6.8, or 5.0. Samples of the extracellular medium were collected at 0.5, 1, 2, 4, and 8 h, and at each time point, the cells were resuspended in fresh medium.…”

Section: Methodsmentioning

confidence: 99%

“…The extracellular medium was layered onto 150 µl of silicone oil (top layer) and 20 µl of 88% formic acid (bottom layer) and then subjected to velocity-gradient centrifugation. 8,13 Whole cells were trapped in the formic acid layer. The pellet was treated with polyethylene glycol to verify that no extracellular drug remained in the pellet.…”

Section: Methodsmentioning

confidence: 99%

“…Grepafloxacin concentration and its disposition in THP-1 monocytes were determined to compare to that in human PMNs. While the ratio of the intracellular to the extracellular drug concentration (IC/EC) for fluoroquinolone antibiotics in human monocytes has been examined, [7][8][9][10] as well as that for -lactams, macrolides, quinolones, rifampicin, and microcycline, 11 there have been no reports on the effects of pH over a 4-log concentration of grepafloxacin over 48 h and its concentration within subcellular organelles of THP-1 phagocytic cells. Cell culture techniques A human acute monocytic leukemia cell line (THP-1; ATCC TIB-202) was obtained from the American Tissue Culture Collection (Rockville, MD, USA).…”

Section: Introductionmentioning

confidence: 99%

“…These monocytes can be stimulated and do undergo phagocytosis when challenged. 7,8 Suspended THP-1 acute monocytes were grown and maintained in a pH-adjusted growth medium (RPMI-1640; Sigma) with 10% heat-inactivated fetal calf serum (FCS; Sigma), plus 3 ϫ 10 Ϫ5 M -mercaptoethanol and penicillin (100 units/ml)/streptomycin (100 µg/ml) at 37°C in a 5% CO 2 incubator. Cells were fed fresh growth medium 18 h before each study.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Human THP-1 monocyte uptake and cellular disposition of 14C-grepafloxacin

Hall

Schwab

Ward

et al. 2004

Journal of Infection and Chemotherapy

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Nonsurgical therapy of chronic periodontitis with adjunctive systemic azithromycin or amoxicillin/metronidazole

Jentsch

Buchmann²,

Friedrich³

et al. 2015

Clin Oral Invest

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Objectives: To compare the effect of systemic adjunctive use of azithromycin with amoxicillin/metronidazole to scaling and root planing (SRP) in a clinical study. Materials and Methods: Data from 60 individuals with chronic periodontitis were evaluated after full-mouth SRP. Antibiotics were given from the first day of SRP, in the test group (n=29) azithromycin for three days, in the control group (n=31) amoxicillin/metronidazole for seven days. Probing depth (PD), attachment level (AL) and bleeding on probing (BOP) were recorded at baseline and after 3 and 12 months. Gingival crevicular fluid was analyzed for MMP-8 and IL-1beta levels. Subgingival plaque was taken for assessment of the major bacteria associated with periodontitis. Results: In both groups, PD, AL and BOP were significantly reduced (p<0.001). A few significant differences between the groups were found; AL and BOP were significantly better in the test than in the control group at the end of the study (p=0.020 and 0.009). Periodontopathogens were reduced most in the test group. Conclusions: A noninferiority of the treatment with azithromycin in comparison with amoxicillin / metronidazole can be stated. The administration of azithromycin could be an alternative to the use of amoxicillin/metronidazole adjunctive to SRP in patients with moderate or severe chronic periodontitis, however a randomized placebo controlled multicenter study is needed. Clinical Relevance: Application of azithromycin as a single antibiotic for three days might be considered as an additional adjunctive antibiotic to SRP in selected patients.

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Disposition and intracellular activity of azithromycin in human THP-1 acute monocytes

Cited by 16 publications

References 29 publications

Cellular Uptake and Efflux of Azithromycin, Erythromycin, Clarithromycin, Telithromycin, and Cethromycin

Cellular Uptake and Efflux of Azithromycin, Erythromycin, Clarithromycin, Telithromycin, and Cethromycin

Human THP-1 monocyte uptake and cellular disposition of 14C-grepafloxacin

Nonsurgical therapy of chronic periodontitis with adjunctive systemic azithromycin or amoxicillin/metronidazole

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