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. 1990 Feb;34(2):277–280. doi: 10.1128/aac.34.2.277

Uptake and intracellular activity of an optically active ofloxacin isomer in human neutrophils and tissue culture cells.

A Pascual 1, I Garcia 1, E J Perea 1
PMCID: PMC171573  PMID: 2327777

Abstract

The penetration of an optically active ofloxacin isomer [(-)-ofloxacin] into human neutrophils and different tissue culture cells (HEp-2, McCoy, MDCK, and Vero) was studied and compared with that of ofloxacin by a fluorometric assay. The cellular-to-extracellular-concentration ratios (C/E) of (-)-ofloxacin were always higher than 6, significantly greater than those of ofloxacin at extracellular concentrations of 5 and 10 mg/liter. The penetration of (-)-ofloxacin and ofloxacin was doubled when neutrophils were stimulated by phorbol myristate acetate but not affected after ingestion of opsonized Staphylococcus aureus. The C/E ratios of (-)-ofloxacin and ofloxacin for different tissue culture epithelial cells and fibroblasts were lower than those of neutrophils but still higher than 2. Both compounds produced a significant reduction in viable intraphagocytic S. aureus during 3 h of exposure to antimicrobial agents. We conclude that (-)-ofloxacin appears to reach higher intracellular concentrations than ofloxacin, remaining active inside the neutrophils.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Brown K. N., Percival A. Penetration of antimicrobials into tissue culture cells and leucocytes. Scand J Infect Dis Suppl. 1978;(14):251–260. [PubMed] [Google Scholar]
  2. Chadwick P. R., Mellersh A. R. The use of a tissue culture model to assess the penetration of antibiotics into epithelial cells. J Antimicrob Chemother. 1987 Feb;19(2):211–220. doi: 10.1093/jac/19.2.211. [DOI] [PubMed] [Google Scholar]
  3. Easmon C. S., Crane J. P., Blowers A. Effect of ciprofloxacin on intracellular organisms: in-vitro and in-vivo studies. J Antimicrob Chemother. 1986 Nov;18 (Suppl 500):43–48. doi: 10.1093/jac/18.supplement_d.43. [DOI] [PubMed] [Google Scholar]
  4. Easmon C. S., Crane J. P. Uptake of ciprofloxacin by macrophages. J Clin Pathol. 1985 Apr;38(4):442–444. doi: 10.1136/jcp.38.4.442. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Hand W. L., King-Thompson N. L. Contrasts between phagocyte antibiotic uptake and subsequent intracellular bactericidal activity. Antimicrob Agents Chemother. 1986 Jan;29(1):135–140. doi: 10.1128/aac.29.1.135. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Hayakawa I., Atarashi S., Yokohama S., Imamura M., Sakano K., Furukawa M. Synthesis and antibacterial activities of optically active ofloxacin. Antimicrob Agents Chemother. 1986 Jan;29(1):163–164. doi: 10.1128/aac.29.1.163. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Imamura M., Shibamura S., Hayakawa I., Osada Y. Inhibition of DNA gyrase by optically active ofloxacin. Antimicrob Agents Chemother. 1987 Feb;31(2):325–327. doi: 10.1128/aac.31.2.325. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Klempner M. S., Styrt B. Clindamycin uptake by human neutrophils. J Infect Dis. 1981 Nov;144(5):472–479. doi: 10.1093/infdis/144.5.472. [DOI] [PubMed] [Google Scholar]
  9. Koga H. High-performance liquid chromatography measurement of antimicrobial concentrations in polymorphonuclear leukocytes. Antimicrob Agents Chemother. 1987 Dec;31(12):1904–1908. doi: 10.1128/aac.31.12.1904. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Maridonneau-Parini I., Tringale S. M., Tauber A. I. Identification of distinct activation pathways of the human neutrophil NADPH-oxidase. J Immunol. 1986 Nov 1;137(9):2925–2929. [PubMed] [Google Scholar]
  11. Milatovic D. Intraphagocytic activity of ciprofloxacin and CI 934. Eur J Clin Microbiol. 1986 Dec;5(6):659–660. doi: 10.1007/BF02013293. [DOI] [PubMed] [Google Scholar]
  12. Pascual A., Garcia I., Perea E. J. Fluorometric measurement of ofloxacin uptake by human polymorphonuclear leukocytes. Antimicrob Agents Chemother. 1989 May;33(5):653–656. doi: 10.1128/aac.33.5.653. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Pascual A., Martínez-Martínez L., Perea E. J. Effect of ciprofloxacin and ofloxacin on human polymorphonuclear leukocyte activity against staphylococci. Chemotherapy. 1989;35(1):17–22. doi: 10.1159/000238631. [DOI] [PubMed] [Google Scholar]
  14. Pascual A., Tsukayama D., Kovarik J., Gekker G., Peterson P. Uptake and activity of rifapentine in human peritoneal macrophages and polymorphonuclear leukocytes. Eur J Clin Microbiol. 1987 Apr;6(2):152–157. doi: 10.1007/BF02018197. [DOI] [PubMed] [Google Scholar]
  15. Peterson P. K., Verhoef J., Schmeling D., Quie P. G. Kinetics of phagocytosis and bacterial killing by human polymorphonuclear leukocytes and monocytes. J Infect Dis. 1977 Oct;136(4):502–509. doi: 10.1093/infdis/136.4.502. [DOI] [PubMed] [Google Scholar]
  16. Sato K., Matsuura Y., Inoue M., Une T., Osada Y., Ogawa H., Mitsuhashi S. In vitro and in vivo activity of DL-8280, a new oxazine derivative. Antimicrob Agents Chemother. 1982 Oct;22(4):548–553. doi: 10.1128/aac.22.4.548. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Wallenstein S., Zucker C. L., Fleiss J. L. Some statistical methods useful in circulation research. Circ Res. 1980 Jul;47(1):1–9. doi: 10.1161/01.res.47.1.1. [DOI] [PubMed] [Google Scholar]

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