Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 23, Issue 11, Pages 4631-4641Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1031-z
Keywords
Pentacyclic triterpenes compounds; 2-Methylene-3-oxo group; Anti-bacteria; Anti-tumor; Apoptosis
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Funding
- National Basic Research 973 Program of China [2012CB722601]
- Major Special Project in Guizhou Province [2013-6006]
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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 alpha,beta-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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