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Index >> Bacterial Cheomotherapy >>Macrolides

Macrolides

Macrolides - The macrolide antibiotics are produced by various species of Streptomyces. They are a group of structurally related compounds containing a large lactone ring of 12-22 atoms. The ring does not contain any nitrogen atoms and has few or no double bonds. One or more sugars are attached to the lactone ring.

Macrolides are active against prokaryotes, but yeasts, Protozoa and animal cells are generally resistant. They bind to a common site on the 50S subunit, and produce conformational changes in the ribosome. Some macrolide-resistant bacterial mutants have 50S subunits with altered affinity for the antibiotics. Examples of macrolides are niddamy­cin, carbomycin, spiramycin III, tylosin and erythromycin.

Niddamycin and carbomycin strongly inhibit transpeptidation. They inhibit the functional attachment of both donor and acceptor substrates to the ribosomes.

Spiramycin III and tylosin moderately inhibit transpeptidation. They inhibit binding to both A and P-sites of the ribosomes.

Erythromycin is a medium spectrum antibiotic which is effective against many gram positive bacteria and a few gram negative organisms. Its action is confined to the 70S prokaryote ribosomes, where it binds to the 50S subunits. Erythromycin bas little or no effect on binding of the acceptor substrates. It interferes with binding of the donor substrates only when they have large peptide moieties.

It is thus a good inhibitor of transpeptidation only with large peptide donors. Erythromycin blocks the  translocation step in which peptidyl-tRNA shifts from the A-site back to the P-site and immobilizes peptidyl tRNA in the A-site. Erythromycin is produced by Streptomyces erythreus, and has a 14-membered lactone ring.

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