Novel 3‐Substituted Ocotillol‐Type Triterpenoid Derivatives as Antibacterial Candidates. (20th May 2014)

• Record Type: Journal Article
• Authors: Bi, Yi; Ma, Cong; Zhang, Hengyuan; Zhou, Zhiwen; Yang, Jian; Zhang, Zhenlei; Meng, Qingguo; Lewis, Peter J.; Xu, Jinyi
• Is Part Of: Chemical biology & drug design. Volume 84:Number 4(2014:Oct.)
• Page Start: 489
• Page End: 496
• Publication Date: 2014-05-20
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12337
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12337-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>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 <italic>Panax ginseng</italic> and their antibacterial activity against several representative bacteria were evaluated. Compounds <bold>5</bold> and <bold>11</bold> exhibited excellent antibacterial activity with MIC values of 1 <italic>μ</italic>g/mL against <italic>Staphylococcus aureus</italic> and 8 <italic>μ</italic>g/mL and 4 <italic>μ</italic>g/mL against <italic>Bacillus subtilis</italic>, respectively. Furthermore, when compounds <bold>5</bold> and <bold>11</bold> were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub‐MIC levels against <italic>S. aureus</italic> USA300 and <italic>B. subtilis</italic> 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound <bold>11</bold> against <italic>B. subtilis</italic> 168.</p> </abstract>