Aguiar Anna Caroline Campos, Parisi Julia Risso, Granito Renata Neves, de Sousa Lorena Ramos Freitas, Renno Ana Cláudia Muniz, Gazarini Marcos Leoni
Department of Biosciences, Federal University of São Paulo (UNIFESP), Rua Silva Jardim 136, Santos 11015-020, SP, Brazil.
Special Academic Unit of Chemistry, Federal University of Goiás (UFG/UFCAT), Catalão Regional, Catalão 75704-020, GO, Brazil.
Mar Drugs. 2021 Feb 28;19(3):134. doi: 10.3390/md19030134.
Malaria is an infectious disease caused by protozoan parasites of the genus through the bite of female Anopheles mosquitoes, affecting 228 million people and causing 415 thousand deaths in 2018. Artemisinin-based combination therapies (ACTs) are the most recommended treatment for malaria; however, the emergence of multidrug resistance has unfortunately limited their effects and challenged the field. In this context, the ocean and its rich biodiversity have emerged as a very promising resource of bioactive compounds and secondary metabolites from different marine organisms. This systematic review of the literature focuses on the advances achieved in the search for new antimalarials from marine sponges, which are ancient organisms that developed defense mechanisms in a hostile environment. The principal inclusion criterion for analysis was articles with compounds with IC below 10 µM or 10 µg/mL against culture. The secondary metabolites identified include alkaloids, terpenoids, polyketides endoperoxides and glycosphingolipids. The structural features of active compounds selected in this review may be an interesting scaffold to inspire synthetic development of new antimalarials for selectively targeting parasite cell metabolism.
疟疾是一种由疟原虫属原生动物寄生虫引起的传染病,通过雌性按蚊叮咬传播,2018年感染人数达2.28亿,导致41.5万人死亡。以青蒿素为基础的联合疗法(ACTs)是治疗疟疾最推荐的方法;然而,多药耐药性的出现不幸地限制了它们的效果,并给该领域带来了挑战。在这种背景下,海洋及其丰富的生物多样性已成为来自不同海洋生物的生物活性化合物和次生代谢物的非常有前景的资源。这篇文献系统综述聚焦于从海洋海绵中寻找新型抗疟药所取得的进展,海洋海绵是在恶劣环境中形成防御机制的古老生物。分析的主要纳入标准是针对培养物的化合物IC低于10µM或10µg/mL的文章。鉴定出的次生代谢物包括生物碱、萜类化合物、聚酮过氧化物和糖鞘脂。本综述中所选活性化合物的结构特征可能是一个有趣的支架,以激发新型抗疟药的合成开发,用于选择性靶向寄生虫细胞代谢。