淫羊藿素衍生物的结构修饰及活性研究进展

Advance on the structural modification and activities of icaritin derivative

淫羊藿苷可以通过增加免疫细胞来提高免疫细胞分泌淋巴因子,从而提高人体免疫力。然而,淫羊藿苷不能通过血脑屏障,这限制了其在中枢神经系统方面的临床应用。近年来,淫羊藿苷的苷元淫羊藿素的药理作用研究受到广泛关注。淫羊藿素不仅可以提高免疫力,改善记忆力,通过激活Wnt/β-catenin信号通路来抑制β-catenin磷酸化,从而抑制β-淀粉样蛋白所致的大鼠肾上腺嗜铬细胞瘤细胞株的神经毒性作用,其对于中枢神经系统还有镇痛作用。它对治疗阿尔兹海默症方面还具有显著的疗效。针对这些新的药理作用和用途,药物学家对淫羊藿素进行了多种结构修饰,如增加溶解度和生物利用度等来增强其生物活性,希望使其在临床上得以广泛应用。本文就淫羊藿素类衍生物的结构改造及其生物活性进行综述,以期为以后寻找具有开发前景的淫羊藿素类衍生物提供依据。

Icariin can increase the number of immune cells and improve immune system by increasing the secretion of lymphokines by immune cells.However,icariin limits its clinical application to the central nervous system because it does not cross the blood-brain barrier.In recent years,studies on the pharmacological effects of icaritin have received extensive attention.Icaritin not only improved immunity and memory,but also had analgesic effects on the central nervous system;inhibited β-catenin phosphorylation by activating the Wnt/β-catenin signaling pathway and inhibits β-amyloid-induced rats neurotoxicity of adrenal pheochromocytoma cell line.Especially,icaritin played an important role in the treatment of Alzheimer′s disease.In response to these new pharmacological effects and uses,pharmacists havd made various structural modifications to icariin,such as increasing solubility and bioavailability to enhance its biological activity,etc.,hoping to make it widely used in clinical practice.In this paper,the structural modification and biological activity of icaritin derivatives were reviewed in order to provide a basis for the future development of icaritin derivatives.