April 2009
Volume 50, Issue 13
ARVO Annual Meeting Abstract  |   April 2009
Anti-Inflammatory Activity of Azithromycin as Measured by Its NF-B Inhibitory Activity
Author Affiliations & Notes
  • P. S. Cheung
    InSiteVision, Alameda, California
  • E. C. Si
    InSiteVision, Alameda, California
  • K. Hosseini
    Clinical Affairs,
    InSiteVision, Alameda, California
  • Footnotes
    Commercial Relationships  P.S. Cheung, InSiteVision, E; E.C. Si, InSiteVision, E; K. Hosseini, InSiteVision, E.
  • Footnotes
    Support  None.
Investigative Ophthalmology & Visual Science April 2009, Vol.50, 839. doi:
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      P. S. Cheung, E. C. Si, K. Hosseini; Anti-Inflammatory Activity of Azithromycin as Measured by Its NF-B Inhibitory Activity. Invest. Ophthalmol. Vis. Sci. 2009;50(13):839.

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      © ARVO (1962-2015); The Authors (2016-present)

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Purpose: : Azithromycin has been reported to possess anti-inflammatory and immunosuppressive activities. This study used an activated NF-ΚB assay to assess azithromycin’s anti-inflammatory potency, and compared that to a commonly used anti-inflammatory agent, hydrocortisone.

Methods: : A reporter gene assay employing A549 cells was used to examine the effects of azithromycin and hydrocortisone on TNF- stimulated NF-ΚB activity. By constructing the dose-response curves, the corresponding inhibitory potencies (IC50s) of azithromycin and hydrocortisone were estimated. Dexamethasone was also tested in the assay to compare its NF-ΚB inhibitory activity as related to the glucocorticoid activity.

Results: : All three compounds dose-dependently inhibited TNF- stimulated NF-ΚB activity. IC50 values of azithromycin, hydrocortisone and dexamethasone were 56 µM, 2.6 nM and 0.18 nM, respectively. Hydrocortisone was approximately 4 orders of magnitude more potent than azithromycin while dexamethasone was approximately 14 times as potent as hydrocortisone. The latter approximates the reported glucocorticoid activity ratio between dexamethasone and hydrocortisone.

Conclusions: : In addition to its antibiotic activity, azithromycin also possesses a weak anti-inflammatory activity relative to the glucocorticoids. Since azithromycin can achieve much higher tissue concentration and has a long tissue half-life at clinical doses, this antibiotic might have utility for certain inflammatory ocular surface diseases.

Keywords: inflammation • antibiotics/antifungals/antiparasitics • corticosteroids 

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