2. Academic Validation
  3. Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents

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

  • Eur J Med Chem. 2013 Oct:68:444-53. doi: 10.1016/j.ejmech.2013.07.041.
Zhiwen Zhou 1,  Cong Ma,  Hengyuan Zhang,  Yi Bi,  Xia Chen,  Hua Tian,  Xiaoni Xie,  Qingguo Meng,  Peter John Lewis,  Jinyi Xu
Affiliations

Affiliation

  • 1 State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China.
PMID: 23994872 DOI: 10.1016/j.ejmech.2013.07.041
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.

Keywords

Antibacterial activity; Cytotoxicity; Ocotillol; Synergistic effect; Triterpenoid.

Figures