摘要
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 antischistosomiasis, 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.
作者
蒋沅岐
董玉洁
周福军
陈金鹏
周钰通
田成旺
陈常青
JIANG Yuan-qi;DONG Yu-jie;ZHOU Fu-jun;CHEN Jin-peng;ZHOU Yu-tong;TIAN Cheng-wang;CHEN Chang-qing(Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;Tianjin Institute of Pharmaceutical Research,Tianjin 300462,China;Tianjin Key Laboratory of Quality Marker of Traditional Medicine,Tianjin 300462,China;State Key Laboratory of Drug Delivery and Pharmacokinetics,Tianjin Institute of Pharmaceutical Research,Tianjin 300462,China)
出处
《中草药》
CAS
CSCD
北大核心
2022年第2期599-608,共10页
Chinese Traditional and Herbal Drugs
基金
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)。
关键词
青蒿素
双氢青蒿素
青蒿琥酯
蒿甲醚
抗疟疾
抗肿瘤
抗炎
安全性
专利申请及保护
artemisinin
dihydroartemisinin
artesunate
artemether
anti-malaria
anti-cancer
anti-inflammatory
safety
patent application and protection
