青蒿素类化合物具有独特的过氧桥结构，对恶性疟疾具有显著的治疗作用，且不易产生耐药性。青蒿素及其衍生物还具有抗血吸虫病、抗肿瘤、抗菌、抗炎、抗病毒、抗纤维化等药理作用。确定了青蒿素的结构，并对其生物合成、化学合成及结构改造进行一系列研究。结构改造得到的双氢青蒿素、青蒿琥酯、蒿甲醚等化合物，有效改善了青蒿素的理化性质和成药性，目前已有复方双氢青蒿素、复方青蒿素、复方蒿甲醚等制剂应用于临床。对近年来青蒿素及其衍生物的结构改造、药理作用、临床应用、安全性、专利申请及保护等的研究进展进行综述，以期为青蒿素及其衍生物的进一步开发利用提供参考。

Artemisinin compounds have unique oxygen bridge structure and have significant therapeutic effect on malaria and are not easy to produce drug resistance. Artemisinin and its derivatives also have a variety of pharmacological activities, such as anti-schistosomiasis, anti-tumor, anti-microbial, anti-inflammatory, anti-virus, anti-fibrosis and so on. Researchers have conducted a series of studies on structure of artemisinin, and determined the structure of artemisinin, and explored its biosynthesis, chemical synthesis and structural modification. After structural modification, researchers have obtained compounds such as dihydroartemisinin, artesunate, artemether, etc., which have effectively improved the physical and chemical properties and medicinal properties of artemisinin. Currently, compound dihydroartemisinin, compound artemisinin, compound artemether, etc are used in clinic. Research progress on structural modification, pharmacological action, clinical application, safety, patent application and protection of artemisinin and its main derivatives are reviewed in this paper in recent years, in order to provide reference for further development and utilization of artemisinin and its derivatives.

R283

国家重大科技专项（2017ZX09101002-001-005）；国家中医药管理局中药国际化基地项目（0610-2040NF020928）