Liu Yi-Xin, Wu Wei, Liang Yue-Jin, Jie Zu-Liang, Wang Hui, Wang Wei, Huang Yi-Xin
Jiangsu Institute of Parasitic Diseases, 117 Yangxiang, Meiyuan, Wuxi 214064, China.
Department of Microbiology and Immunology, The University of Texas Medical Branch, 301 University Blvd, Galveston, TX 77555, USA.
Molecules. 2014 Sep 19;19(9):15058-74. doi: 10.3390/molecules190915058.
Artemisinin (qinghaosu), extracted from the Chinese herb Artemisia annua L. in 1972, and its three major derivatives--artemether, artesunate and dihydroartemisinin--were firstly identified as antimalarials and found active against all species of the malaria parasite. Since the early 1980s, artemisinin and its derivatives have been found efficacious against Schistosoma spp., notably larval parasites, and artemisinin derivatives have played a critical role in the prevention and treatment of human schistosomiasis in China. Currently, China is moving towards the progress of schistosomiasis elimination. However, the potential development of praziquantel resistance may pose a great threat to the progress of elimination of schistosomiasis japonica in China. Fortunately, these three major artemisinin derivatives also exhibit actions against adult parasites, and reduced sensitivity to artemether, artesunate and dihydroartemisinin has been detected in praziquantel-resistant S. japonicum. In this review, we describe the application of artemisinin derivatives in the prevention and treatment of schistosomiasis japonica in China, so as to provide tools for the global agenda of schistosomiasis elimination. In addition to antimalarial and antischistosomal actions, they also show activities against other parasites and multiple cancers. Artemisinin derivatives, as old drugs identified firstly as antimalarials, continue to create new stories.
青蒿素(青蒿素)于1972年从中国草药黄花蒿中提取,其三种主要衍生物——蒿甲醚、青蒿琥酯和双氢青蒿素——首先被确定为抗疟药物,并被发现对所有疟原虫物种均有活性。自20世纪80年代初以来,青蒿素及其衍生物已被发现对血吸虫有效,尤其是幼虫寄生虫,青蒿素衍生物在中国人体血吸虫病的预防和治疗中发挥了关键作用。目前,中国正朝着消除血吸虫病的目标迈进。然而,吡喹酮耐药性的潜在发展可能对中国日本血吸虫病消除进程构成巨大威胁。幸运的是,这三种主要的青蒿素衍生物也对成虫寄生虫有作用,并且在吡喹酮耐药的日本血吸虫中已检测到对蒿甲醚、青蒿琥酯和双氢青蒿素的敏感性降低。在这篇综述中,我们描述了青蒿素衍生物在中国日本血吸虫病预防和治疗中的应用,以便为全球消除血吸虫病议程提供工具。除了抗疟和抗血吸虫作用外,它们还对其他寄生虫和多种癌症显示出活性。青蒿素衍生物作为首先被确定为抗疟药物的老药,不断创造新的故事。