丹参素及其衍生物药理作用机制和应用研究进展

Research Advances in Pharmacological Mechanism and Application of Danshensu and Its Derivatives

关键词:  丹参素  缺血再灌注损伤  PI3K/AKT信号通路  丹参素衍生物

Key words:  Danshensu  ischemia reperfusion injury  PI3K/AKT signal pathway  Danshensu derivative

摘要:

丹参素是中药丹参最重要的水溶性成分之一，在临床中被广泛用于冠心病心绞痛的治疗，研究表明其具有显著的改善微循环、抗内皮损伤、抗氧化、抗炎、抗血小板聚集等药理活性。研究证明丹参素主要是通过激活AKT/ERK1/2/Nrf2信号通路对缺血再灌注（ischemia reperfusion，I/R）损伤起到心脏保护作用。丹参素结构中的酚羟基和α羟基羧酸，阻碍了其进一步的开发和临床应用，因此，开发合成出药理活性更高、稳定性和脂溶性更好的丹参素衍生物成为了近年来的研究热点。本文对近年来丹参素的药理作用、分子机制、衍生物研究以及联合应用的研究进展进行了全面综述，以便对丹参素进行更加全面和深入的了解，为丹参素的临床研究提供参考。

Abstract:

Danshensu(DSS) is one of the most important water-soluble components, has been widely used for the treatment of angina pectoris. Numerous studies have shown that DSS can improve microcirculation and protect endothelial cells from damage, and it has antioxidant, anti-inflammatory, anti-platelet aggregation and other pharmacological activities. The study show that DSS plays a cardiac protective effect on ischemia reperfusion(I/R) injury mainly through the activation of AKT/ERK1/2/Nrf2 signaling pathway. The phenolic hydroxyl group and hydroxy carboxylic acid in DSS structure hinder its further development and clinical application. The development and synthesis of DSS derivatives with higher pharmacological activity, better stability and lipid solubility have become a research hotspot in recent years. In this paper, the advances in pharmacological action, molecular mechanism, derivative research and dosage form application of DSS in recent years were reviewed to make a more comprehensive and in-depth understanding of DSS, in order to provide reference for its application and clinical research.