Institute of Pharmacy & Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang 421001, China.
Institute of Chemistry & Chemical Engineering, University of South China, Hengyang 421001, China.
Mini Rev Med Chem. 2019;19(7):555-568. doi: 10.2174/1389557518666180424094821.
Chrysin is a natural product of a flavonoid compound. Chemically, chrysin consists of two phenyl rings (A and B) and a heterocyclic ring (C). Biologically, chrysin exerts many different physiological activities. In recent years, with the in-depth development for more active drugs, the synthesis and biological activities of chrysin derivatives have been well studied. Besides, structure-activity relationship of chrysin revealed that the chemical construction meets the critical chemical structural necessities of flavonoids for numerous pharmacological activities. It is generally believed that modified chrysin could be more potent than unmodified chrysin. Different modification in the rings of chrysin could possess various degrees of biological activities. This review aims to summarize the mechanism for the activities of chrysin and its derivatives in different rings. We also explored the relationship between biological function and structure-activity of substituted chrysin derivatives with different functional groups. The influence of chrysin derivatives on the proliferation and apoptosis of cancer cells is also investigated. Development of novel drugs based on the biological functions of chrysin could better improve clinical outcomes of affected population, especially for tumor patients and diabetic patients.
白杨素是一种黄酮类化合物的天然产物。从化学角度来看，白杨素由两个苯环（A 和 B）和一个杂环（C）组成。从生物学角度来看，白杨素有许多不同的生理活性。近年来，随着对更具活性药物的深入开发，对白杨素衍生物的合成和生物活性进行了很好的研究。此外，白杨素的构效关系表明，其化学结构满足了黄酮类化合物发挥多种药理活性的关键化学结构要求。一般认为，修饰后的白杨素可能比未修饰的白杨素有更强的活性。白杨素环上的不同修饰可以具有不同程度的生物活性。本综述旨在总结白杨素及其衍生物在不同环上的活性机制。我们还探讨了不同取代基的取代白杨素衍生物的生物功能与构效关系。研究了白杨素衍生物对癌细胞增殖和凋亡的影响。基于白杨素的生物学功能开发新型药物，可以更好地改善受影响人群的临床结局，特别是肿瘤患者和糖尿病患者。
