首页    期刊浏览 2024年10月06日 星期日
登录注册

文章基本信息

  • 标题:Biological Activities of 1, 1, 6-Trisubstituted Indanes : Beyond Magainin 2
  • 本地全文:下载
  • 作者:Naganori NUMAO ; Yukiko HIROTA ; Akiyo IWAHORI
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1999
  • 卷号:22
  • 期号:1
  • 页码:73-76
  • DOI:10.1248/bpb.22.73
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:MSI-78 is a peptide analog of naturally occurring magainin 2 isolated from the skin of Xenopus laevis. The peptide is known to have one of the strongest antibacterial activities in magainin 2 analogs against methicillin-resistant Staphylococcus aureus (MRSA). To find novel compounds superior to MSI-78, we have further designed, synthesizing 1, 1-di(4-aminobutyl)-6-benzylindane (PM4) and 1, 1-dibenzyl-6-(4-aminobutyl) indane (PM5), and tested their inhibitory ability of the growth of S. aureus. In an in vitro assay, PM4 showed the same antibacterial activity against the bacterium as MSI-78, and non-hemolytic activity against human red blood cells (RBCs) at the MIC (minimum inhibitory concentration )value, in contrast to the latter. On the other hand, PM 5 showed stronger antibacterial activity than MSI-78, but being still accompanied with hemolysis at the MIC value. Otherwise, stronger decarboxylase activity for oxaloacetate was observed in PM5, rather than magainin 2 analogs or Oxaldie 1 as a control peptide, but not in PM4.
  • 关键词:magainin 2 analog;antibacterial activity;decarboxylase activity;peptidomimetic;indane derivative;S. aureus
国家哲学社会科学文献中心版权所有