Determination of binding parameters of macrolides, lincosamides, and streptogramins to Legionella pneumophila
Fournet, M.P.; Zini, R.; Deforges, L.; Duval, J.; Tillement, J.P.
Journal of Pharmaceutical Sciences 76(2): 153-156
1987
ISSN/ISBN: 0022-3549 PMID: 3572754 DOI: 10.1002/jps.2600760214
Accession: 039780955
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Summary
Parameters of [3H]erythromycin binding to Legionella pneumophila were determined in vitro using both an equilibrium and a kinetic method. Different L. pneumophila serogroups, 1-3, and a virulent strain serogroup, 1, were tested. All strains of bacteria exhibited the same binding pattern, with a dissociation constant of 0.15 microM. Other macrolides, streptogramin B-types, and lincosamides competitively displaced bound erythromycin suggesting that these compounds share common binding sites on the bacteria. Minimum inhibitory concentration (MIC) values for macrolides, streptogramin B-types, and lincosamides were determined with buffered charcoal yeast extract (BCYE) medium. A good correlation (r = 0.994) was found between the corresponding inhibition constants of these antibiotics and their MIC. It was also noted that for lincosamides the microbiological inactivity was associated with a very low bacterium affinity. Thus, it is concluded that binding parameters of these antibiotics reflect their efficacy against L. pneumophila in vitro and may serve as a useful adjunct in developing new compounds.