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药物在血吸虫病治疗方面的演变:回顾过去,改善未来。

The evolution of drugs on schistosoma treatment: looking to the past to improve the future.

机构信息

Laboratório de Imunomodulação e novas abordagens terapêuticas (LINAT), Universidade Federal de Pernambuco(UFPE), Brazil.

出版信息

Mini Rev Med Chem. 2013 Apr;13(4):493-508. doi: 10.2174/1389557511313040003.

Abstract

Schistosomiasis is a devastating worldwide widespread tropical disease that currently affects more than 230 million people, making it an issue of great socioeconomic and public health importance. Unfortunatelly there is a single drug for the treatment of all forms of schistosomiasis, praziquantel, which was introduced in therapy in 1980. The article goes by antimony compounds, emetine, hydantoin, nitrofurans, lucanthone, hycanthone, oxamniquine derivatives and organophosphates until it finally gets to praziquantel derivatives. The intent of this review is to provide a panorama of drugs that were and are being used in human chemotherapy looking to the past to improve rational design drugs in the future. Not only clinical used compounds will be shown but also synthesized and tested compounds in vitro and in vivo in animal models which haven't yet to be used in humans. Prospects for drug discovery and vaccines to be used in the treatment and prevention of schistosomiasis, clinical trials, concerns about the resistance/decreased effectiveness of the treatment, and patent database will also be discussed. At the end of the review the reader will notice that much has been done but much still needs to be done yet.

摘要

血吸虫病是一种具有毁灭性的、广泛流行于全球的热带病,目前影响着超过 2.3 亿人,因此成为一个具有重大社会经济和公共卫生意义的问题。不幸的是,目前仅有一种药物可用于治疗所有形式的血吸虫病,即吡喹酮,它于 1980 年被引入治疗。这篇文章还提到了一些其他的药物,如锑化合物、吐根碱、海因酮、硝基呋喃类、硝呋太尔、六氯对二甲苯、羟氯喹衍生物和有机磷酸酯,直到最后才提到吡喹酮衍生物。本文的目的是提供一个过去和现在用于人体化疗的药物全景图,以期从过去的经验中为未来合理设计药物提供参考。本文不仅展示了临床使用的化合物,还展示了在体外和动物模型中合成和测试的化合物,这些化合物尚未在人类中使用。本文还讨论了血吸虫病治疗和预防用药物发现和疫苗的前景、临床试验、对治疗耐药性/效果降低的担忧,以及专利数据库。在综述的最后,读者会注意到,虽然已经做了很多工作,但仍有许多工作需要去做。

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