Anti-inflammatory macrolides

Anti-Inflammatory Macrolides to Manage Chronic Neutrophilic Inflammation... 

The results showed that the compounds studied with more frequency in the aquatic environment, and of which, logically, there is more information, are the antibiotics, analgesics and anti-inflammatories (like diclofenac, ibuprofen, naproxen, acetylsalicylic acid, and paracetamol), as well as the p-blocker atenolol. In the category of antibiotics, several families are included, like the macrolides (erythromycin), the fluoroquinolones (ofloxacin and ciprofloxacin), sulfonamides (sulfamethoxazole), penicillins (amoxicillin), the metronidazol, and trimethoprim. Other therapeutic groups also widely studied and frequently found in the environmental waters are the lipid regulators (gemfibrozil and bezafibrat), antiepileptic carbamaze-pine, and antidepressants (diazepam, fluoxetine, paroxetine) (see Table 3). 

Amsden GW. Anti-inflammatory effects of macrolides -an underappreciated benefit in the treatment of community-acquired respiratory tract infections and chronic inflammatory pulmonary conditions . J An-timicrob Chemother 2005 55(1) 10-21. [Epub 2004 Dec 8]. Review. 

Many macrolides of marine origin have been reported to show other interesting biological properties, such as immunosuppressive [473,474], antifungal [323,475,476], anti-actin [477], and anti-inflammatory activity... 

The macrolide antibiotics (erythromycin, azithromycin, and chn-damycin) exhibit anti-inflammatory properties in patients with acne. 

Furthermore, it has become clear recently that even the subminimum inhibitory concentration of 14-membered ring macrolides has the inhibitory effects of biofilm formation and expression of virulence factors (piocyanin, elastase, proteases) of P. aeruginosa (see following section). Thus, an anti-inflammatory agent such as EM should be used as basic treatment in the therapy of chronic airway infection. 

C. Molecular Mechanisms of the Anti-Inflammatory Actions of Macrolides... 

EM also has a motilin-like stimulating activity on gastrointestinal smooth muscles [39]. Therefore, the inhibitory effect on cytokine expression in human cells summarized here may be a third bioactivity of the macrolide antibiotic. We recently reported that some of these derivatives have inhibitory effect on IL-8 production by human airway epithelial cells [72], These analogues also showed inhibitory action on the activation of NFkB and AP-1 assessed by EMSA (M. Desaki etal., unpublished observations, January 2001). Characterization of the chemical structure responsible for its potential would be important to pursue and further investigation for the molecular mechanism would be necessary for a possible new type of anti-inflammatory agent. 

Anti-inflammatory activities of these 14-membered ring macrolides have not yet been clarified in relation to their structure. To study the structure-activity relationships of macrolides, we examined six macrolides including three new... 

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