Biological activities of 1,1,6-trisubstituted indanes: Beyond magainin 2

Naganori Numao, Yukiko Hirota, Akiyo Iwahori, Shun Ichi Kidokoro, Masanori Sasatsu, Isamu Kondo, Sachiko Itoh, Etsuko Itoh, Tadashi Katoh, Noriko Shimozono, Akiko Yamazaki, Ken Ichi Takao, Susumu Kobayashi

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

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, PM5 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.

Original languageEnglish
Pages (from-to)73-76
Number of pages4
JournalBiological and Pharmaceutical Bulletin
Volume22
Issue number1
DOIs
Publication statusPublished - 1999 Jan
Externally publishedYes

Keywords

  • Antibacterial activity
  • Decarboxylase activity
  • Indane derivative
  • Magainin 2 analog
  • Peptidomimetic
  • S. aureus

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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  • Cite this

    Numao, N., Hirota, Y., Iwahori, A., Kidokoro, S. I., Sasatsu, M., Kondo, I., Itoh, S., Itoh, E., Katoh, T., Shimozono, N., Yamazaki, A., Takao, K. I., & Kobayashi, S. (1999). Biological activities of 1,1,6-trisubstituted indanes: Beyond magainin 2. Biological and Pharmaceutical Bulletin, 22(1), 73-76. https://doi.org/10.1248/bpb.22.73