Enhancement of anti-bacterial and anti-tumor activities of pentacyclic triterpenes by introducing exocyclic α,β-unsaturated ketone moiety in ring A

被引:0
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作者
Li R. Huang
Heng Luo
Xiao S. Yang
Lei Chen
Jian X. Zhang
Dao P. Wang
Xiao J. Hao
机构
[1] Center for Research and Development of Fine Chemicals of Guizhou University,Ministry of Education Key Laboratory of Green Pesticide and Ago
[2] The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Bioengineering
来源
Medicinal Chemistry Research | 2014年 / 23卷
关键词
Pentacyclic triterpenes compounds; 2-Methylene-3-oxo group; Anti-bacteria; Anti-tumor; Apoptosis;
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摘要
Ursolic acid, oleanolic acid, glycyrrhetinic acid, and betulinic acid, the representatives of pentacyclic triterpenes, were modified by introducing 2-methylene-3-oxo group as exocyclic α,β-unsaturated ketone moiety in ring A. The anti-bacterial and anti-tumor activities of these derivatives were assayed by comparing with the parent compounds. Results indicated that pentacyclic triterpenes carrying 2-methylene-3-oxo group in the ring A exhibited a significant improvement in anti-bacterial activity that was limited to Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis. The four derivatives also showed an increased cytotoxicity against leukemia, lung, and breast cancer cell lines in a dose-dependent manner in vitro. U2 and O2 compounds showed strong apoptotic activities to lung carcinoma cell lines. The results for the first time provided scientific evidence for improvement of anti-bacterial and anti-tumor activities of pentacyclic triterpenes using derivatives of these compounds.
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页码:4631 / 4641
页数:10
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