Synthesis and Biological Activity of Embelin and its Derivatives: An Overview

Author(s): Zhaojun Sheng*, Siyuan Ge, Min Gao, Rongchao Jian, Xiaole Chen, Xuetao Xu, Dongli Li, Kun Zhang, Wen-Hua Chen*

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 20 , Issue 5 , 2020


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Abstract:

Embelin is a naturally occurring para-benzoquinone isolated from Embelia ribes (Burm. f.) of the Myrsinaceae family, and contains two carbonyl groups, a methine group and two hydroxyl groups. With embelin as the lead compound, more than one hundred derivatives have been reported. Embelin is well known for its ability to antagonize the X-linked inhibitor of apoptosis protein (XIAP) with an IC50 value of 4.1 μM. The potential of embelin and its derivatives in the treatment of various cancers has been extensively studied. In addition, these compounds display a variety of other biological effects: antimicrobial, antioxidant, analgesic, anti-inflammatory, anxiolytic and antifertility activity. This paper reviews the recent progress in the synthesis and biological activity of embelin and its derivatives. Their cellular mechanisms of action and prospects in the research and development of new drugs are also discussed.

Keywords: Embelin, anticancer, anti-inflammatory activity, benzoquinone, XIAP antagonist, natural product

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Article Details

VOLUME: 20
ISSUE: 5
Year: 2020
Published on: 24 April, 2020
Page: [396 - 407]
Pages: 12
DOI: 10.2174/1389557519666191015202723
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