Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, Universidade Estadual de Maringá, Maringá, Paraná, Brazil.
Departamento de Química, Universidade Federal do Amazonas, Manaus, Brazil.
Nat Prod Res. 2021 Nov;35(22):4729-4733. doi: 10.1080/14786419.2020.1715395. Epub 2020 Jan 25.
The search for bioactive compounds against diseases is imperative and the richness of the Amazon provides a large source to be explored. Current therapies for the treatment of parasitic infections have severe side effects and low efficacy, which makes the development of an effective chemotherapy extremely important. In this study, we describe the isolation of styrylpyrone 4-methoxy-6-(11,12-methylenedioxy-trans-styryl)-2-pyrone (SP), from the Amazonian tree species, , the activity against promastigotes, and its pharmacokinetics properties. The results showed morphological and ultrastructural alterations, cell cycle impairment, increased reactive oxygen species production, accumulation of lipid bodies and formation of autophagic vacuoles in SP-treated parasites. studies revealed that the compound has a high drug-score, which is encouraging for further investigation. Our results indicate that SP is a promising drug candidate, which induces alterations in leading to parasite death through cell cycle arrest and autophagy.
寻找针对疾病的生物活性化合物是当务之急，而亚马逊的丰富资源提供了大量有待探索的来源。目前治疗寄生虫感染的疗法具有严重的副作用和低疗效，这使得开发有效的化疗药物变得极为重要。在这项研究中，我们描述了从亚马逊树种 中分离出的苯乙烯基吡喃酮 4-甲氧基-6-(11,12-亚甲基二氧基-反式-苯乙烯基)-2-吡喃酮 (SP)，以及它对 前鞭毛体的活性及其药代动力学特性。结果表明，SP 处理后的寄生虫会发生形态和超微结构改变、细胞周期受损、活性氧产生增加、脂滴积累和自噬空泡形成。 研究表明，该化合物具有高药物评分，这为进一步研究提供了鼓舞。我们的结果表明，SP 是一种很有前途的候选药物，它通过细胞周期停滞和自噬诱导 发生变化，导致寄生虫死亡。
