Next Article in Journal
α-Glucosidase Inhibitory Constituents from Acanthopanax senticosus Harm Leaves
Previous Article in Journal
Antiatherogenic Properties of Acetone Extract of Alpinia zerumbet Seeds
Article

Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives

1
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China
2
School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China
*
Author to whom correspondence should be addressed.
Molecules 2012, 17(6), 6249-6268; https://doi.org/10.3390/molecules17066249
Received: 16 April 2012 / Revised: 4 May 2012 / Accepted: 9 May 2012 / Published: 25 May 2012
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity
Show Figures

Graphical abstract

MDPI and ACS Style

Chen, T.; Zhang, R.-H.; He, S.-C.; Xu, Q.-Y.; Ma, L.; Wang, G.-C.; Qiu, N.; Peng, F.; Chen, J.-Y.; Qiu, J.-X.; Peng, A.-H.; Chen, L.-J. Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives. Molecules 2012, 17, 6249-6268. https://doi.org/10.3390/molecules17066249

AMA Style

Chen T, Zhang R-H, He S-C, Xu Q-Y, Ma L, Wang G-C, Qiu N, Peng F, Chen J-Y, Qiu J-X, Peng A-H, Chen L-J. Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives. Molecules. 2012; 17(6):6249-6268. https://doi.org/10.3390/molecules17066249

Chicago/Turabian Style

Chen, Tao, Rong-Hong Zhang, Shi-Chao He, Qin-Yuan Xu, Liang Ma, Guang-Cheng Wang, Neng Qiu, Fei Peng, Jin-Ying Chen, Jing-Xiang Qiu, Ai-Hua Peng, and Li-Juan Chen. 2012. "Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives" Molecules 17, no. 6: 6249-6268. https://doi.org/10.3390/molecules17066249

Find Other Styles

Article Access Map by Country/Region

1
Only visits after 24 November 2015 are recorded.
Back to TopTop