Abstract
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.
Highlights
Schistosomiasis, caused by the infection with the blood flukes of the genus Schistosoma, is a major neglected parasitic disease in the tropical and subtropical regions [1]
We focus on the role of three major artemisinin derivatives, artemether, artesunate and dihydroartemisinin, in the elimination of schistosomiasis japonica in China
An extended study to evaluate the efficacy of dihydroartemisinin administered at multiple doses or combined with praziquantel showed that the 3-day treatment with dihydroartemisinin at doses of 200, 300, 400 or 600 mg/kg on days 6–8 post-infection reduced total worm burdens of 69.2%, 80.7%, 87.1% and 90.6%, while the same treatment given on days 34–36 achieved total worm burden reductions of 83.8%, 92.9%, 94.1% and 95.3%, respectively; dihydroartemisinin-praziquantel combination administered at the juvenile stage did not appear more effective than treatment with dihydroartemisinin alone, while the combined treatment did not exhibit greater efficacy than that achieved by praziquantel treatment alone
Summary
Schistosomiasis, caused by the infection with the blood flukes of the genus Schistosoma, is a major neglected parasitic disease in the tropical and subtropical regions [1]. Schistosomiasis japonica, caused by the infection with the parasite S. japonicum, is endemic in the People’s Republic of. In China, praziquantel is currently the only market-available chemical used for the treatment of S. japonicum infections, and praziquantel-based chemotherapy, a major part of the national schistosomiasis control program, has been implemented to control the morbidity and reduce the prevalence and intensity of S. japonicum infection for more than 30 years [22,23,24]. The potential development of praziquantel resistance would challenge the elimination of schistosomiasis japonica in China, since praziquantel-based chemotherapy remains highly effective for controlling the morbidity and reducing the prevalence [30]. We focus on the role of three major artemisinin derivatives, artemether, artesunate and dihydroartemisinin, in the elimination of schistosomiasis japonica in China
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