Cioli Donato, Pica-Mattoccia Livia, Basso Annalisa, Guidi Alessandra
Institute of Cell Biology and Neurobiology, National Research Council, Rome, Italy.
Mol Biochem Parasitol. 2014 Jun;195(1):23-9. doi: 10.1016/j.molbiopara.2014.06.002. Epub 2014 Jun 21.
Since no vaccine exists against schistosomiasis and the molluscs acting as intermediate hosts are not easy to attack, chemotherapy is the main approach for schistosomiasis control. Praziquantel is currently the only available antischistosomal drug and it is distributed mainly through mass administration programs to millions of people every year. A number of positive features make praziquantel an excellent drug, especially with regard to safety, efficacy, cost and ease of distribution. A major flaw is its lack of efficacy against the immature stages of the parasite. In view of its massive and repeated use on large numbers of individuals, the development of drug resistance is a much feared possibility. The mechanism of action of praziquantel is still unclear, a fact that does not favor the development of derivatives or alternatives. A large number of compounds have been tested as potential antischistosomal agents. Some of them are promising, but none so far represents a suitable substitute or adjunct to praziquantel. The research of new antischistosomal compounds is an imperative and urgent matter.
由于目前尚无针对血吸虫病的疫苗，且作为中间宿主的软体动物不易控制，化疗是控制血吸虫病的主要方法。吡喹酮是目前唯一可用的抗血吸虫药物，主要通过大规模给药计划每年分发给数百万人。吡喹酮具有许多积极特性，使其成为一种优秀的药物，特别是在安全性、有效性、成本和易于分发方面。一个主要缺陷是它对寄生虫未成熟阶段缺乏疗效。鉴于其在大量个体中的大量和重复使用，耐药性的发展是一个令人非常担忧的可能性。吡喹酮的作用机制仍不清楚，这一事实不利于衍生物或替代品的开发。大量化合物已作为潜在的抗血吸虫药物进行了测试。其中一些有前景，但迄今为止没有一种能作为吡喹酮的合适替代品或辅助药物。新型抗血吸虫化合物的研究是当务之急。
