Indolo[3,2-b]quinoline derivatives suppressed the hemolytic activity of beta-pore forming toxins, aerolysin-like hemolysin produced by aeromonas sobria and alpha-hemolysin produced by staphylococcus aureus

Eizo Takahashi, Chiaki Fujinami, Teruo Kuroda, Yasuo Takeuchi, Shin Ichi Miyoshi, Sakae Arimoto, Tomoe Negishi, Keinosuke Okamoto

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

In an attempt to discover inhibitory compounds against pore-forming toxins, some of the major toxins produced by bacteria, we herein examined the effects of four kinds of indolo[3,2-b]quinoline derivatives on hemolysis induced by the aerolysin-like hemolysin (ALH) of Aeromonas sobria and also by the alphahemolysin of Staphylococcus aureus. The results showed that hemolysis induced by ALH was significantly reduced by every derivative, while that induced by alpha-hemolysis was significantly reduced by three out of the four derivatives. However, the degrees of reduction induced by these derivatives were not uniform. Each derivative exhibited its own activity to inhibit the respective hemolysin. Compounds 1 and 2, which possessed the amino group bonding the naphthalene moiety at the C-11 position of indolo[3,2-b]quinoline, had strong inhibitory effects on the activity of ALH. Compound 4 which consisted of benzofuran and quinoline had strong inhibitory effects on the activity of alpha-hemolysin. These results indicated that the amino group bonding the naphthalene moiety of compounds 1 and 2 assisted in their ability to inhibit ALH activity, while the oxygen atom at the 10 position of compound 4 strengthened its interaction with alpha-hemolysin. These compounds also suppressed the hemolytic activity of the supernatant of A. sobria or A. hydrophila, suggesting that these compounds were effective at the site of infection of these bacteria.

Original languageEnglish
Pages (from-to)114-120
Number of pages7
JournalBiological and Pharmaceutical Bulletin
Volume39
Issue number1
Publication statusPublished - Jan 1 2016

Keywords

  • Aerolysin-like hemolysin
  • Alpha-hemolysin
  • Anti-virulence
  • Indolo[3,2-b]quinoline
  • Pore-forming toxin

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

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