Department of Chemistry, Ahmadu Bello University, Zaria, Nigeria.
Department of Biochemistry, Umaru Musa Yar'adua University, Katsina, Nigeria.
Int J Antimicrob Agents. 2018 Mar;51(3):311-318. doi: 10.1016/j.ijantimicag.2017.06.010. Epub 2017 Jun 28.
Leishmaniases are endemic diseases in tropical and sub-tropical regions of the world and are considered by the World Health Organization (WHO) to be among the six most important neglected tropical diseases. The current therapeutic arsenal against the disease is associated with a series of chemotherapeutic setbacks. However, since the early 1990s, naturally occurring chalcones with promising antileishmanial effects have been reported, and several other synthetic chalcones and chalcone-hybrid molecules have been confirmed to possess potent activity against various Leishmania species. This paper is a comprehensive review covering the antileishmanial activity of 34 naturally occurring chalcones, 224 synthetic/semisynthetic chalcones and 54 chalcone-hybrid molecules. Several chalcones in the synthetic/semisynthetic category had IC values < 5 µM, with very good selectivity against parasites, and the structure-activity relationships as well as the proposed mechanism of action are discussed. We identified knowledge-gaps with the hope of providing future direction for the discovery of novel antileishmanial drugs from chalcones.
利什曼病是世界热带和亚热带地区的地方病，被世界卫生组织（WHO）认为是六种最重要的被忽视热带病之一。目前针对该疾病的治疗方法与一系列化疗失败有关。然而，自 20 世纪 90 年代初以来，已经报道了具有有前途抗利什曼原虫作用的天然存在的查耳酮，并且已经证实几种其他合成查耳酮和查耳酮杂合分子对各种利什曼原虫具有强大的活性。本文综述了 34 种天然查耳酮、224 种合成/半合成查耳酮和 54 种查耳酮杂合分子的抗利什曼原虫活性。在合成/半合成类别中，有几种查耳酮的 IC 值<5 μM，对寄生虫具有很好的选择性，并且讨论了构效关系以及提出的作用机制。我们确定了知识空白，希望为从查耳酮中发现新型抗利什曼原虫药物提供未来的方向。
