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  • Title: Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents.
    Author: Zhou Z, Ma C, Zhang H, Bi Y, Chen X, Tian H, Xie X, Meng Q, Lewis PJ, Xu J.
    Journal: Eur J Med Chem; 2013 Oct; 68():444-53. PubMed ID: 23994872.
    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.
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