A synthetic gamma-lactone group with beta-lactamase inhibitory and sporulation initiation effects.
Previous studies showed that some lactones have beta-lactamase inhibitory or antibacterial effects, others--like A-factor (a gamma-butyrolactone) and its derivatives--stimulate sporulation in Streptomyces griseus strains. Our experiments were aimed at exploring whether synthetic gamma-lactones had such effects. None of the seven gamma-lactones studied showed antibacterial activity, but two of them inhibited beta-lactamases isolated from various bacteria. These two gamma-lactones did not reduce colony formation of murine bone marrow cells in vitro, indicating that they were not toxic to proliferating mammalian cells. Four gamma-lactones, including the two inhibiting beta-lactamase, stimulated sporulation in the non-sporulating S. griseus bald 7 mutant. Further studies of gamma-lactones as potential inhibitors of beta-lactamase seem to be warranted.
Gál
Z
Z
Department of Pharmacology, University of Debrecen, Hungary. gal@king.pharmacol.dote.hu
Koncz
A
A
Szabó
I
I
Deák
E
E
Benkö
I
I
Barabás
G
G
Hernádi
F
F
Kovács
P
P
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001854:Bone Marrow Cells / Q000166:cytology / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D003114:Colony-Forming Units Assay; D004305:Dose-Response Relationship, Drug; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D013171:Spores, Bacterial / Q000187:drug effects; D013305:Streptomyces griseus / Q000187:drug effects*; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D007783:Lactones; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams