Novel 3‐Substituted Ocotillol‐Type Triterpenoid Derivatives as Antibacterial Candidates |
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| Authors: | Zhiwen Zhou Jian Yang Zhenlei Zhang Qingguo Meng Peter J Lewis Jinyi Xu |
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| Institution: | 1. State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, , Nanjing, 210009 China;2. School of Pharmacy, Yantai University, , Yantai, 264005 China;3. Biological Sciences, School of Environmental and Life Sciences, University of Newcastle, , Callaghan, NSW, 2308 Australia |
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| 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. |
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| Keywords: | antibacterial activity ocotillol‐type synergistic effect triterpenoid saponin |
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