New cyslabdans B and C, potentiators of imipenem activity against methicillin-resistant Staphylococcus aureus produced by Streptomyces sp. K04-0144

Acta Pharmaceutica Sinica B

Yuriko Tokura¹  Nobuhiro Koyama¹  Hiroshi Tomoda¹  Yoko Takahashi² 

[1] Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo 108-8641, Japan;Kitasato Institute for Life Sciences, Kitasato University, Tokyo 108-8641, Japan;

关键词: Cyslabdan;    Actinomycete metabolites;    Imipenem potentiator;    Methicillin-resistant Staphylococcus aureus (MRSA);   

DOI  :  10.1016/j.apsb.2011.10.008

来源: DOAJ

【 摘 要 】

From a further purification study, two new congeners designated cyslabdans B (1) and C (2) were isolated along with previously reported cyslabdan (cyslabdan A (3) in this study) from the culture broth of Streptomyces sp. K04-0144. The structure was elucidated by various spectroscopy including NMR, revealing that 1 and 2 was 18-hydroxy and 1′-methoxy cyslabdan, respectively. Compounds 1 and 2 were found to potentiate imipenem activity against methicillin-resistant Staphylococcus aureus by 123 fold and 533 fold, respectively. Comparison with the activity of compound 3 indicated that the introduction of a hydrophilic group at the dimethyl moiety of the decalin ring was unfavorable for its activity.

【 授权许可】

Unknown