Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents

Zhiwen Zhou, Cong Ma, Hengyuan Zhang, Yi Bi, Xia Chen, Hua Tian, Xiaoni Xie, Qingguo Meng, Peter John Lewis, Jinyi Xu

Research output: Journal article publicationJournal articleAcademic researchpeer-review

29 Citations (Scopus)

Abstract

A novel class of ocotillol-type triterpenoid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against several representative pathogenic bacterial strains. Compounds 20(S)-protopanaxadiol (PPD), 3, 5, 16 and 24 exhibited potent antibacterial activity against Gram-positive bacteria. Compounds 3 and 5 also displayed promising antibacterial activity against a community-associated methicillin-resistant Staphylococcus aureus (CA-MRSA; strain USA300). Furthermore, compounds PPD, 3 and 16 combined with two commercially available antibiotics kanamycin and chloramphenicol showed strong synergistic inhibitory effects at their sub-MIC concentrations against S. aureus USA300 and Bacillus subtilis 168. Additionally, cytotoxic activity assay showed that the compounds tested did not affect cell viability of the human epithelial kidney (HEK-293) and human cervical (HeLa) cells at their MICs.
Original languageEnglish
Pages (from-to)444-453
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume68
DOIs
Publication statusPublished - 1 Jan 2013
Externally publishedYes

Keywords

  • Antibacterial activity
  • Cytotoxicity
  • Ocotillol
  • Synergistic effect
  • Triterpenoid

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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