Vol.52 No.7 July 2004
Novel action of macrolide antibiotics
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato Univeristy, and the Kitasato Institute, 5-9-1 Shirokane, Minato-ku, Tokyo, Japan
Abstract
Macrolide antibiotics are classified by the size of the macrocyclic lactone ring of aglycone as 12-, 14-, or 16-membered ring macrolides. A number of macrolide antibiotics, such as erythromycin (EM), oleandomycin, leucomycin, spiramycin, josamycin, midecamycin and their derivatives, have been used extensively in human medicine, especially against a wide range of gram-positive bacteria. They have seen only limited activity, however against most gram-negative bacteria. Some are active against Legionella pneumophila, Rickettia strains, Spirochaeta, large viruses, protozoa, Toxoplasma, and Mycoplasma. Recently, macrolide antibiotics have showen some novel action. First, EM showed dramatic gastrointestinal motor-stimulating activity, and the genetic name "motilide" was proposed for a series of macrolides having motilin-agonistic activity. Second, the prognosis of diffuse panbronchiolitis (DPB), an incurable chronic inflammatory airway disease, improved significantly by treatment with long-term, low-dose EM. Such therapeutic efficacy is assumed to be due to antiinflammatory or immunomodulatory activity by macrolide antibiotics. Third, macrolide antibiotics showed the modulation of bacterial functions such as the inhibition of biofilm formation and the inhibition of the expression of virulence factors at sub-MIC concentrations.
Key word
macrolides, novel actions, anti-infectious drug, Pseudomonas aeruginosa, anti-inflammatory
Received
May 14, 2004
Accepted
June 15, 2004
Jpn. J. Chemother. 52 (7): 367-370, 2004