Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives

被引：16

作者：

Chen, Tao ^{[1
]}

Zhang, Rong-Hong ^{[1
]}

He, Shi-Chao ^{[2
]}

Xu, Qin-Yuan ^{[1
]}

Ma, Liang ^{[1
]}

Wang, Guang-Cheng ^{[1
]}

Qiu, Neng ^{[1
]}

Peng, Fei ^{[1
]}

Chen, Jin-Ying ^{[1
]}

Qiu, Jing-Xiang ^{[1
]}

Peng, Ai-Hua ^{[1
]}

Chen, Li-Juan ^{[1
]}

机构：

[1] Sichuan Univ, State Key Lab Biotherapy, W China Hosp, W China Med Sch, Chengdu 610041, Sichuan, Peoples R China

[2] Sichuan Univ, Sch Chem Engn, Chengdu 610065, Sichuan, Peoples R China

来源：

MOLECULES | 2012年 / 17卷 / 06期

关键词：

gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity; IN-VITRO; STRUCTURAL MODIFICATION; INHIBITS ANGIOGENESIS; ENDOTHELIAL-CELLS; GROWTH; ZEBRAFISH; PERSPECTIVES; MIGRATION; RECEPTOR; ANALOGS;

D O I：

10.3390/molecules17066249

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Gambogic acid (GA) is in a phase II clinical trial as an antitumor and antiangiogenesis agent. In this study, 36 GA derivatives were synthesized and screened in a zebrafish model to evaluate their antiangiogenic activity and toxicity. Derivatives 4, 32, 35, 36 effectively suppressed the formation of newly grown blood vessels and showed lower toxicities than GA as evaluated by zebrafish heart rates and mortalities. They also exhibited more potent migration and HUVEC tube formation inhibiting activities than GA. Among them, 36 was the most potent one, suggesting that it may serve as a potential new antiangiogenesis candidate with low toxicity. Additionally, 36 showed comparable antiproliferative activity to HUVECs and five tumor cell lines but low cytotoxicity to LO2 cells.

引用

页码：6249 / 6268

页数：20

共 25 条

[1]

How to create the vascular tree? (Latest) help from the zebrafish [J].