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植物源天然产物在新型抗线虫驱虫药物研发中的应用。

Plant-Based Natural Products for the Discovery and Development of Novel Anthelmintics against Nematodes.

机构信息

Department of Biology, KU Leuven, 3000 Leuven, Belgium.

出版信息

Biomolecules. 2020 Mar 9;10(3):426. doi: 10.3390/biom10030426.

Abstract

Intestinal parasitic nematodes infect approximately two billion people worldwide. In the absence of vaccines for human intestinal nematodes, control of infections currently relies mainly on chemotherapy, but resistance is an increasing problem. Thus, there is an urgent need for the discovery and development of new anthelmintic drugs, especially ones with novel mechanisms of action. Medicinal plants hold great promise as a source of effective treatments, including anthelmintic therapy. They have been used traditionally for centuries and are mostly safe (if not, their toxicity is well-known). However, in most medicinal plants the compounds active against nematodes have not been identified thus far. The free-living nematode was demonstrated to be an excellent model system for the discovery of new anthelmintics and for characterizing their mechanism of action or resistance. The compounds discussed in this review are of botanical origin and were published since 2002. Most of them need further studies of their toxicity, mechanisms and structure-activity relationship to assess more fully their potential as drugs.

摘要

肠道寄生线虫感染全世界约 20 亿人。由于目前尚无针对人体肠道线虫的疫苗,感染的控制主要依赖于化疗,但耐药性是一个日益严重的问题。因此,迫切需要发现和开发新的驱虫药物,特别是具有新作用机制的药物。药用植物作为有效的治疗方法(包括驱虫治疗)的来源具有很大的潜力。它们在传统上已经使用了几个世纪,而且大多数是安全的(如果不安全,它们的毒性是众所周知的)。然而,到目前为止,在大多数药用植物中,还没有发现对抗线虫有效的化合物。自由生活的线虫被证明是发现新驱虫剂和描述其作用机制或耐药性的极好模型系统。本综述中讨论的化合物具有植物来源,并且是自 2002 年以来发表的。它们中的大多数需要进一步研究其毒性、机制和构效关系,以更全面地评估它们作为药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1cf3/7175113/f5ec56dc7f36/biomolecules-10-00426-g001.jpg

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