Anti-inflammatory activity of azithromycin as measured by its NF-kappaB, inhibitory activity.
Growing data suggest that the antibiotic azithromycin mediates anti-inflammatory activity through the inhibition of the transcription factor NF-kappaB. The purpose of this study was to compare azithromycin's anti-inflammatory potency with that of hydrocortisone and dexamethasone as measured in an activated NF-kappaB assay. Dose-response curves and the corresponding inhibitory potencies (IC(50)) of azithromycin, hydrocortisone, and dexamethasone were evaluated in a fluorescence assay using A549 cells. All three compounds inhibited TNFalpha stimulated NF-kappaB activity in a dose-dependent manner. IC(50) values of azithromycin, hydrocortisone and dexamethasone were 56 microM, 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. In relative terms the anti-inflammatory potency of azithromycin was about 4 orders of magnitude weaker than that of hydrocortisone.
Cheung
Paul S
PS
Preclinical Research, InSite Vision, Alameda, California 94501, USA.
Si
Erwin C
EC
Hosseini
Kamran
K
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D017963:Azithromycin / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003907:Dexamethasone / Q000494:pharmacology; D006801:Humans; D006854:Hydrocortisone / Q000494:pharmacology; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D003907:Dexamethasone; D017963:Azithromycin; D006854:Hydrocortisone