title: Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents.
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.
authors.affiliation: State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China.
authors.forename: Zhiwen
authors.initials: Z
authors.lastname: Zhou
authors.forename: Cong
authors.initials: C
authors.lastname: Ma
authors.forename: Hengyuan
authors.initials: H
authors.lastname: Zhang
authors.forename: Yi
authors.initials: Y
authors.lastname: Bi
authors.forename: Xia
authors.initials: X
authors.lastname: Chen
authors.forename: Hua
authors.initials: H
authors.lastname: Tian
authors.forename: Xiaoni
authors.initials: X
authors.lastname: Xie
authors.forename: Qingguo
authors.initials: Q
authors.lastname: Meng
authors.forename: Peter John
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* / Q000633:toxicity; D001419:Bacteria / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D036145:Ginsenosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D057809:HEK293 Cells; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D036145:Ginsenosides; C524540:ocotillol
keywords: Antibacterial activity; Cytotoxicity; Ocotillol; Synergistic effect; Triterpenoid