School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China.
International Healthcare Innovation Institute (Jiangmen), Jiangmen, 529020, China.
Mini Rev Med Chem. 2020;20(5):396-407. doi: 10.2174/1389557519666191015202723.
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.
鞣花酸是从桃金娘科（Myrsinaceae）植物石榴（Embelia ribes （Burm. f.））中分离出来的一种天然对苯醌，它含有两个羰基、一个亚甲氧基和两个羟基。以鞣花酸为先导化合物，已报道了一百多种衍生物。鞣花酸以其能够拮抗 X 连锁凋亡抑制蛋白（XIAP）的能力而闻名，其 IC50 值为 4.1 μM。鞣花酸及其衍生物在治疗各种癌症方面的潜力已得到广泛研究。此外，这些化合物还具有多种其他生物学作用：抗菌、抗氧化、镇痛、抗炎、抗焦虑和抗生育活性。本文综述了鞣花酸及其衍生物的合成和生物学活性的最新进展。还讨论了它们的细胞作用机制以及在新药研发中的前景。
