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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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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.
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.
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.
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.
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