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The Search for Putative Hits in Combating Leishmaniasis: The Contributions of Natural Products Over the Last Decade
Natural Products and Bioprospecting ( IF 4.8 ) Pub Date : 2021-07-14 , DOI: 10.1007/s13659-021-00311-2
Patrick O Sakyi 1, 2 , Richard K Amewu 1 , Robert N O A Devine 2 , Emahi Ismaila 2 , Whelton A Miller 3, 4, 5 , Samuel K Kwofie 6, 7
Affiliation  

Abstract

Despite advancements in the areas of omics and chemoinformatics, potent novel biotherapeutic molecules with new modes of actions are needed for leishmaniasis. The socioeconomic burden of leishmaniasis remains alarming in endemic regions. Currently, reports from existing endemic areas such as Nepal, Iran, Brazil, India, Sudan and Afghanistan, as well as newly affected countries such as Peru, Bolivia and Somalia indicate concerns of chemoresistance to the classical antimonial treatment. As a result, effective antileishmanial agents which are safe and affordable are urgently needed. Natural products from both flora and fauna have contributed immensely to chemotherapeutics and serve as vital sources of new chemical agents. This review focuses on a systematic cross-sectional view of all characterized anti-leishmanial compounds from natural sources over the last decade. Furthermore, IC50/EC50, cytotoxicity and suggested mechanisms of action of some of these natural products are provided. The natural product classification includes alkaloids, terpenes, terpenoids, and phenolics. The plethora of reported mechanisms involve calcium channel inhibition, immunomodulation and apoptosis. Making available enriched data pertaining to bioactivity and mechanisms of natural products complement current efforts geared towards unraveling potent leishmanicides of therapeutic relevance.

Graphic Abstract



中文翻译:

寻找抗击利什曼病的有效药物:过去十年天然产品的贡献

摘要

尽管组学和化学信息学领域取得了进展,但利什曼病仍需要具有新作用模式的有效新型生物治疗分子。在流行地区,利什曼病的社会经济负担仍然令人担忧。目前,来自尼泊尔、伊朗、巴西、印度、苏丹和阿富汗等现有流行地区以及秘鲁、玻利维亚和索马里等新受影响国家的报告表明,人们担心传统锑治疗会产生化学耐药性。因此,迫切需要安全且负担得起的有效抗利什曼病药物。来自动植物群的天然产物对化疗做出了巨大贡献,并成为新化学制剂的重要来源。本综述重点关注过去十年中来自天然来源的所有特征性抗利什曼原虫化合物的系统横截面视图。此外,还提供了其中一些天然产物的IC 50 /EC 50 、细胞毒性和建议的作用机制。天然产物分类包括生物碱、萜烯、萜类化合物和酚类化合物。大量报道的机制涉及钙通道抑制、免疫调节和细胞凋亡。提供有关天然产物的生物活性和机制的丰富数据补充了当前旨在揭示具有治疗相关性的有效利什曼杀剂的努力。

图文摘要

更新日期:2021-07-14
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