期刊
JOURNAL OF NATURAL PRODUCTS
卷 79, 期 4, 页码 721-731出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.5b00641
关键词
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资金
- National Basic Research 973 Program of the People's Republic of China [2012CB722601]
- Major Special Project in Guizhou Province [2013-6006]
- Project of Scientific and Technological Innovation Talent Team Construction in Guizhou Province [2013-4006]
- High-level Innovative Talents Training in Guizhou Province [2015-4027]
The oleanane-type triterpene 18 beta-glycyrrhetinic acid (1) was modified chemically through the introduction of a trihydroxylated A ring and an ester moiety at C-20 to enhance its antibacterial activity. Compounds 22, 23, 25, 28, 29, 31, and 32 showed more potent inhibitory activity against Streptomyces scabies than the positive control, streptomycin. Additionally, the inhibitory activity of the most potent compound, 29, against Bacillus subtilis, Staphylococcus aureus, and methicillin-resistant Staphylococcus aureus was greater than that of the positive controls. The antibacterial mode of action of the active derivatives involved the regulation of the expression of genes associated with peptidoglycans, the respiratory metabolism, and the inherent virulence factors found in bacteria, as determined through a quantitative real-time reverse transcriptase PCR assay.
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