linezolid and butenolide

Activity-guided fractionations of the tunicate Pseudodistoma antinboja yielded four new compounds of the cadiolide class (cadiolides J-M, 1, 3-5) along with a known one (cadiolide H, 2). The structures were defined by spectroscopic methods including X-ray crystallographic analysis. These compounds were evaluated for their antibacterial activity and exhibited potent antibacterial activity against all of the drug resistant strains tested with MICs comparable to those of marketed drugs such as vancomycin and linezolid.

Topics: 4-Butyrolactone; Animals; Anti-Bacterial Agents; Dose-Response Relationship, Drug; Drug Resistance, Bacterial; Gram-Positive Bacteria; Microbial Sensitivity Tests; Molecular Structure; Republic of Korea; Structure-Activity Relationship; Urochordata

Six new (1, 2, and 5-8) and three known (3, 4, and 9) butenolide metabolites were isolated from the tunicate Pseudodistoma antinboja by activity-guided fractionations. The structures were elucidated by combined NMR and MS spectroscopic methods. These compounds were evaluated for their antibacterial activity, and most of them exhibited moderate to significant activity that selectively targeted Gram-positive strains and did not exhibit cytotoxicity in the MTT assay at 100 μM. Cadiolides 5-9 in particular exhibited significant antibacterial activity that was comparable to or even better than those of marketed drugs such as vancomycin and linezolid against all of the drug-resistant strains tested.

Topics: 4-Butyrolactone; Acetamides; Animals; Anti-Bacterial Agents; Drug Resistance, Bacterial; Gram-Positive Bacteria; Linezolid; Marine Biology; Microbial Sensitivity Tests; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Oxazolidinones; Republic of Korea; Urochordata; Vancomycin