ACTs for schistosomiasis: do they act?
ACTs for schistosomiasis: do they act?
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DOI：
10.1016/s1473-3099(10)70169-9
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发表时间：
2010-09
期刊：
影响因子：
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通讯作者：
J. Utzinger;M. Tanner;J. Keiser
中科院分区：
文献类型：
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作者：
J. Utzinger;M. Tanner;J. Keiser
有证据表明，中国在 2000 多年前就已使用药草青蒿和青蒿的粗提物。 1 事实上，草药医生开出的茶中含有干蒿植物的叶子，用于治疗发烧和其他疾病。 1 然而，青蒿的活性成分直到最近才被发现，并命名为青蒿素，即现在的青蒿素。这一突破性的发现源于20世纪70年代初植物化学家屠呦呦对2000多种中药制剂的筛选。 2 这些发现的真正重要性直到 20 世纪 80 年代中期才被《科学》杂志上的一篇评论所认识，其中包括主要由美国沃尔特·里德陆军研究所生成的验证性数据。青蒿素的主要特点是起效快、寄生虫减少率高、寄生虫阶段特异性广和有效性。 4 由此得出的结论是，青蒿素是迄今为止发现的最有效的抗疟药。 5 尽管如此，青蒿素也有一些缺点，例如由于其半衰期短而导致生物制药特性不佳。因此需要频繁的治疗，这会损害依从性并承担产生耐药性的风险。 4 鉴于这些担忧，为了避免疟疾灾难，领先的疟疾学家在十多年前就强调，基于青蒿素的联合疗法 (ACT) 是前进的方向。 6青蒿素还具有对抗血吸虫病（血吸虫病的病因）的活性。这一发现可以追溯到30年前，而且多年来也没有得到传统医学的认可。 7, 8 深入的实验室研究表明，青蒿素对疟原虫（即血吸虫）幼年期的影响最为严重，而吡喹酮主要杀死成年血吸虫。中国的一系列临床试验表明，反复口服蒿甲醚或青蒿琥酯可预防日本血吸虫感染。 7, 8 在新千年之际，青蒿素的活性
There is evidence that crude extracts of the medicinal herbs Artemisia annua and Artemisia apiacea were used in China more than 2000 years ago. 1 Indeed, herbalists prescribed tea that included dried leaves of the Artemisia plants to treat fever and other ailments. 1 However, the active component of A annua was only identified more recently and named Qinghaosu, now known as artemisinin. This breakthrough discovery made in the early 1970s stemmed from screening more than 2000 Chinese herb preparations by the phytochemist You-You Tu. 2 The true importance of these discoveries was only recognised in the mid-1980s, facilitated by a review in the journal Science3 that included confirmatory data mostly generated by the Walter Reed Army Institute of Research in the USA. Key features of the artemisinins are their rapid onset of action, high parasite reduction ratio, broad parasite stage specificity, and effectiveness. 4 Hence the conclusion that the artemisinins are the most powerful antimalarials discovered so far. 5 Nonetheless, the artemisinins have liabilities, such as suboptimum biopharmaceutical properties due to their short half-lives. Frequent treatments are thus needed, which compromise compliance and bear the risk of resistance development. 4 In view of these concerns, and to avert a malaria disaster, leading malariologists emphasised, more than a decade ago that artemisinin-based combination therapies (ACTs) are the way forward. 6Artemisinins are also active against blood flukes, the cause of schistosomiasis. This discovery dates back 30 years and was also not recognised by conventional medicine for many years. 7, 8 In-depth laboratory investigations showed that juvenile stages of the parasite (ie, schistosomula) were most severely affected by the artemisinins, by contrast with praziquantel, which mainly kills adult schistosomes. A series of clinical trials in China showed that repeated oral artemether or artesunate prevented patent Schistosoma japonicum infections. 7, 8 At the turn of the new millennium, the activity of the artemisinins was