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Arch Pharm (Weinheim). 2014 Jan;347(1):42-53. doi: 10.1002/ardp.201300224. Epub 2013 Nov 18.

Lantabetulic acid derivatives induce G1 arrest and apoptosis in human prostate cancer cells.

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Faculty of Fragrance and Cosmetics, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.


Ten new lantabetulic acid (1) derivatives 2-11 were synthesized and their cytotoxicities against human prostate cancer cells were evaluated. PC3 cells treated with 10 μM 8 exhibited the most potent G1 phase arrest. In addition, 10 μM 8 markedly decreased the levels of cyclin E and cdk2 and caused an increase in the p21 and p27 levels, while 20 μM 8 mainly led to cell death through the apoptotic pathway, which correlated with an increase in reactive oxygen species levels, decreased expression levels of Bcl-2 and caspase-8, the induction of mitochondrial changes, and decreased levels of cytochrome c in mitochondria. The dual action of 8 could provide a new approach for the development of chemotherapeutic drugs.


Apoptosis; Cytotoxicity; G1 arrest; Lantabetulic acid; Synthesis

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