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
Molecules 2012, 17(6), 6249-6268; doi:10.3390/molecules17066249

Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives

1, 1, 2, 1, 1, 1, 1, 1, 1, 1, 1 and 1,*
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.
Received: 16 April 2012 / Revised: 4 May 2012 / Accepted: 9 May 2012 / Published: 25 May 2012
(This article belongs to the Section Medicinal Chemistry)
Download PDF [915 KB, uploaded 18 June 2014]


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.
Keywords: gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here


[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert