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

页码：42 / 53

页数：12

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