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Molecules 2017, 22(6), 924;

An Overview of Structurally Modified Glycyrrhetinic Acid Derivatives as Antitumor Agents

School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Qing-Wen Zhang
Received: 18 May 2017 / Revised: 31 May 2017 / Accepted: 31 May 2017 / Published: 2 June 2017
(This article belongs to the Special Issue Synthesis and Modification of Natural Product)
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Glycyrrhetinic Acid (GA), a triterpenoid aglycone component of the natural product glycyrrhizinic acid, was found to possess remarkable anti-proliferative and apoptosis-inducing activity in various cancer cell lines. Though GA was not as active as other triterpenes, such as betulinic acid and oleanolic acid, it could trigger apoptosis in tumor cells and it can be obtained easily and cheaply, which has stimulated scientific interest in using GA as a scaffold to synthesize new antitumor agents. The structural modifications of GA reported in recent decades can be divided into four groups, which include structural modifications on ring-A, ring-C, ring-E and multiple ring modifications. The lack of a comprehensive and recent review on this topic prompted us to gather more new information. This overview is dedicated to summarizing and updating the structural modification of GA to improve its antitumor activity published between 2005 and 2016. We reviewed a total of 210 GA derivatives that we encountered and compiled the most active GA derivatives along with their activity profile in different series. Furthermore, the structure activity relationships of these derivatives are briefly discussed. The included information is expected to be of benefit to further studies of structural modifications of GA to enhance its antitumor activity. View Full-Text
Keywords: glycyrrhetinic acid; overview; structural modification; antitumor glycyrrhetinic acid; overview; structural modification; antitumor

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Xu, B.; Wu, G.-R.; Zhang, X.-Y.; Yan, M.-M.; Zhao, R.; Xue, N.-N.; Fang, K.; Wang, H.; Chen, M.; Guo, W.-B.; Wang, P.-L.; Lei, H.-M. An Overview of Structurally Modified Glycyrrhetinic Acid Derivatives as Antitumor Agents. Molecules 2017, 22, 924.

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