title: Novel 3-substituted ocotillol-type triterpenoid derivatives as antibacterial candidates.
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.
authors.affiliation: School of Pharmacy, Yantai University, Yantai, 264005, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Bi
authors.forename: Cong
authors.initials: C
authors.lastname: Ma
authors.forename: Hengyuan
authors.initials: H
authors.lastname: Zhang
authors.forename: Zhiwen
authors.initials: Z
authors.lastname: Zhou
authors.forename: Jian
authors.initials: J
authors.lastname: Yang
authors.forename: Zhenlei
authors.initials: Z
authors.lastname: Zhang
authors.forename: Qingguo
authors.initials: Q
authors.lastname: Meng
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Lewis
authors.forename: Jinyi
authors.initials: J
authors.lastname: Xu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001412:Bacillus subtilis / Q000187:drug effects; D004357:Drug Synergism; D036145:Ginsenosides / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D005894:Panax / Q000737:chemistry / Q000378:metabolism; D013211:Staphylococcus aureus / Q000187:drug effects; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D036145:Ginsenosides; D014315:Triterpenes; C524540:ocotillol
keywords: antibacterial activity; ocotillol-type; synergistic effect; triterpenoid saponin