期刊
NATURAL PRODUCT RESEARCH
卷 34, 期 6, 页码 766-772出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2018.1499642
关键词
Triterpenoid derivatives; anti-cancer; anti-hepatic fibrosis; apoptosis; p53-MDM2; docking
资金
- National Nature Science Foundation of China [81703389]
- Education fund item of Liaoning Province [201610163L35]
- Youth development support plan of Shenyang Pharmaceutical University [ZQN2016023]
- E&T modern center for Natural Products of Liaoning Province of China [2008402021]
- Construction of R&D institute of state original new drugs at Benxi of Liaoning Province [2009ZX09301-012-105B]
Oleanolic acid (1), ursolic acid (2), hederagenin (3), betulinol (4), betulinic acid (5), and glycyrrhetinic acid (6) are obtained from acorn/licorice industrial wastes with common triterpenoid structure as a model set for esterification. Eight 3,4,5-methoxybenzoyl triterpenoid derivatives (1a-6a), including four new derivatives (1a, 3a-1, 3a-2, and 3a-3), are synthesized by classical procedures. Their antitumor and anti-hepatic fibrosis activities are evaluated on four human tumor cell lines and t-HSC/Cl-6 cells. Derivative 1a shows maximum antiproliferative effects against all cell lines, especially against tumor cells with IC50 values in the range of 5.32-15.23 mu M, but does not affect the viability of normal cells. The anti-tumor mechanisms of 1a are also investigated by western blot and docking studies. The 3,4,5-methoxybenzoyl triterpenoids offers an intriguing solution for naturally derived antitumor drugs and may be invaluable for further development of cancer therapy.
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