Saccharomicins, novel heptadecaglycoside antibiotics produced by Saccharothrix espanaensis:: Antibacterial and mechanistic activities

Saccharomicins, novel heptadecaglycoside antibiotics produced by Saccharothrix espanaensis:: Antibacterial and mechanistic activities
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DOI:
10.1128/aac.44.8.2154-2159.2000
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发表时间:
2000-08-01
影响因子:
4.9
通讯作者:
Greenstein, M
Greenstein, M
中科院分区:
医学2区
文献类型:
--
作者:
Singh, MP;Petersen, PJ;Greenstein, M

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Saccharomicins A and B, two new heptadecaglycoside antibiotics, were isolated front the fermentation broth of the rare actinomycete Saccharothrix espanaensis, They represent a novel class of bactericidal antibiotics that are active both in vitro and in vivo against bacteria and yeast (MICs: Stapylococcus aureus, 128; and yeast, >128 mu g/ml), including multiply resistant strains. Saccharomicins protected mice from lethal challenges by staphylococci (subcutaneous 50% effective dose range of 0.06 to 2.6 mg/kg of body weight, depending on the S. aureus strain). The 50% lethal dose by the subcutaneous route was 16 mg/kg, Mechanistic studies with Escherichia coli imp and Bacillus subtilis suggested complete, nonspecific inhibition of DNA, RNA, and protein biosynthesis within 10 min of drug treatment. Microscopic examination of drug-treated cells also suggested cell ISE;is. These data are consistent with a strong membrane disruptive activity, The antibacterial activities of the saccharomicins against gram-positive bacteria were unaffected by the presence of Ca2+ or Mg2+, but activity against gramnegative bacteria was substantially reduced.