穿心莲内酯为爵床科植物穿心莲的重要天然活性成分之一,穿心莲内酯及其衍生物具有抗炎、抗病毒、抗肿瘤、抗HIV、保肝活性以及α-葡萄糖苷酶抑制等活性,由于其广泛的药理活性而备受研究者关注。该文对穿心莲内酯衍生物的合成进行综述,并简述其相关的药理活性报道。 Andrographolide is one of the important natural active ingredients of Orchidaceae, which contains anti-inflammatory, antiviral, anti-tumor, anti-HIV, hepatoprotective and α-glucosidase inhibitory activities. Due to its wide range of pharmacological activities, researchers are concerned about it. This article reviews the synthesis of andrographolide derivatives and briefly reports on its related pharmacological activity.