摘要
背景:利什曼病仍然是一个重要的公共卫生问题,表现出环境风险因素,如大规模迁移、城市化和森林砍伐。世卫组织对利什曼病的研究主要侧重于开发新工具,例如诊断测试、药物和疫苗。在药物开发策略中,只有少数化合物有前景,需要在体外和体内临床前试验后进一步研究。 目标:在本次审查中,我们的小组旨在强调 2014 年至 2019 年期间在天然和合成化合物领域所做的最大研究,以及针对利什曼原虫进行体内测试的重新利用药物和新制剂。 方法:在文献检索的基础上,我们使用数据库MEDLINE、PUBMED、CAPES PERIODIC和ELSEVIER来划分每个领域最近5年的研究间隔。 结果:在测试的天然化合物中,大蒜素和一部分马铃薯块茎提取物显示出最有希望的抗利什曼原虫活性。在合成化合物方面,喹啉、冰片酯、百里酚、苯并恶唑和硝基咪唑衍生物表现出令人鼓舞的结果。此外,重新定位的替代方案还涉及与已知药物和单一疗法方案的组合。近年来,新制剂被广泛评估为药物递送系统,例如聚合物结合中的纳米颗粒、胶束和脂质体。 结论:药物再利用和已知药物的新配方是迅速引入利什曼病新治疗方案的有价值的方法。尽管如此,对新合成化合物和新配方的兴趣为新的治疗建议带来了曙光,并且是值得注意的研究方向。
关键词: 利什曼病、合成化合物、天然来源的化合物、再利用、新配方、体内试验。
Current Medicinal Chemistry
Title:An Overview of the Compounds Tested In Vivo for Leishmania spp. of the Last 5 Years
Volume: 28 Issue: 21
关键词: 利什曼病、合成化合物、天然来源的化合物、再利用、新配方、体内试验。
摘要:
Background: Leishmaniasis, a still important public health problem, exhibits environmental risk factors such as massive migrations, urbanization, and deforestation. WHO research for Leishmaniasis is mainly focused on the development of new tools, such as diagnostic tests, drugs, and vaccines. During the drug development strategy, only a few compounds were promising and call for further study after the in vitro and in vivo preclinical tests.
Objective: In this review, our group aimed to highlight the utmost research done during 2014 to 2019 in the fields of natural and synthetic compounds, as well as repurposed drugs and new formulations tested in vivo for Leishmania spp.
Method: Based on the literature search, we used the databases MEDLINE, PUBMED, CAPES PERIODIC and ELSEVIER to delineate an interval of the last 5 years of research on each field.
Results: Among the natural compounds tested, allicin and a fraction of potato tuber extract showed the most promising antileishmanial activity. Concerning synthetic compounds, quinolines, bornyl ester, thymol, benzoxaborole and nitroimidazole derivatives exhibited encouraging results. Moreover, repositioned alternatives involved combinations with known drugs and monotherapy protocols as well. In these years, new formulations were widely assessed as drug delivery systems, such as nanoparticles, micelles and liposomes in polymer conjugations.
Conclusion: Drug repurposing and new formulations of already-known drugs are worthwhile approaches to promptly introduce new treatment schemes to Leishmaniasis. Nevertheless, the interest in new synthetic compounds and new formulations brings light to new treatment proposals and are notable lines of research.
Export Options
About this article
Cite this article as:
An Overview of the Compounds Tested In Vivo for Leishmania spp. of the Last 5 Years, Current Medicinal Chemistry 2021; 28 (21) . https://dx.doi.org/10.2174/0929867327999201116145408
DOI https://dx.doi.org/10.2174/0929867327999201116145408 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements