Lantabetulic Acid Derivatives Induce G1 Arrest and Apoptosis in Human Prostate Cancer Cells

被引：0
|
作者：
Lin, Kai-Wei [1 ]
Lin, Zih-You [1 ]
Huang, A-Mei [2 ]
Weng, Jing-Ru [3 ]
Yen, Ming-Hong [4 ]
Yang, Shyh-Chyun [1 ]
Lin, Chun-Nan [1 ,3 ]
机构：
[1] Kaohsiung Med Univ, Fac Fragrance & Cosmet, Coll Pharm, Kaohsiung 80708, Taiwan
[2] Kaohsiung Med Univ, Inst Biochem, Coll Med, Kaohsiung, Taiwan
[3] China Med Univ, Sch Med, Dept Biol Sci & Technol, Taichung, Taiwan
[4] Kaohsiung Med Univ, Coll Pharm, Inst Nat Product, Kaohsiung, Taiwan
来源：
ARCHIV DER PHARMAZIE | 2014年 / 347卷 / 01期
关键词：
Apoptosis; Cytotoxicity; G1; arrest; Lantabetulic acid; Synthesis; TRANSITIONAL CARCINOMA; CONSTITUENTS; MITOCHONDRIA; MECHANISM;
D O I：
10.1002/ardp.201300224
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Ten new lantabetulic acid (1) derivatives 2-11 were synthesized and their cytotoxicities against human prostate cancer cells were evaluated. PC3 cells treated with 10M 8 exhibited the most potent G1 phase arrest. In addition, 10M 8 markedly decreased the levels of cyclin E and cdk2 and caused an increase in the p21 and p27 levels, while 20M 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.
引用
收藏
页码：42 / 53
页数：12
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