Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates

Yi Bi, Cong Ma, Hengyuan Zhang, Zhiwen Zhou, Jian Yang, Zhenlei Zhang, Qingguo Meng, Peter J. Lewis, Jinyi Xu

Research output: Journal article publicationJournal articleAcademic researchpeer-review

12 Citations (Scopus)

Abstract

Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 μg/mL against Staphylococcus aureus and 8 μg/mL and 4 μg/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.
Original languageEnglish
Pages (from-to)489-496
Number of pages8
JournalChemical Biology and Drug Design
Volume84
Issue number4
DOIs
Publication statusPublished - 1 Oct 2014
Externally publishedYes

Keywords

  • antibacterial activity
  • ocotillol-type
  • synergistic effect
  • triterpenoid saponin

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

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