Laboratório de Inovação Tecnológica no Desenvolvimento de Fármacos e Cosméticos, State University of Maringá, Maringa, 87020-900, Brazil.
Cellular Biology Graduate Program, State University of Maringá, Maringa, 87020-900, Brazil.
Sci Rep. 2019 Dec 27;9(1):20080. doi: 10.1038/s41598-019-56647-w.
Yeast cell wall particles isolated from Saccharomyces cerevisiae (scYCWPs) have a rich constitution of β-glucan derived from the cell wall. After removing intracellular contents, β-glucan molecules are readily recognized by dectin-1 receptors, present on the cytoplasmic membrane surface of the mononuclear phagocytic cells and internalized. Leishmania spp. are obligate intracellular parasites; macrophages are its primary host cells. An experimental murine model of visceral leishmaniasis caused by L. infantum was used to evaluate the antileishmanial activity of oral administration of these particles. A low-water soluble thiophene previously studied in vitro against L. infantum was entrapped into scYCWPs to direct it into the host cell, in order to circumvent the typical pharmacokinetic problems of water-insoluble compounds. We found that scYCWPs + T6 reduced the parasitic burden in the liver and spleen. There was an increase in IFN-γ levels related to nitric oxide production, explaining the reduction of the L. infantum burden in the tissue. Histological analysis did not show signals of tissue inflammation and biochemical analysis from plasma did not indicate signals of cytotoxicity after scYCWPs + T6 treatment. These findings suggested that scYCWPs + T6 administered through oral route reduced the parasitic burden without causing toxic effects, satisfying requirements for development of new strategies to treat leishmaniasis.
酵母细胞壁颗粒(Yeast cell wall particles)从酿酒酵母(Saccharomyces cerevisiae)中分离出来,其β-葡聚糖(β-glucan)的组成非常丰富,源自细胞壁。去除细胞内物质后,β-葡聚糖分子很容易被细胞膜表面的单核吞噬细胞上的 dectin-1 受体识别,并被内化。利什曼原虫(Leishmania spp.)是一种必需的细胞内寄生虫;巨噬细胞是其主要宿主细胞。利用利什曼原虫(L. infantum)引起的内脏利什曼病(visceral leishmaniasis)实验性小鼠模型来评估这些颗粒的抗利什曼原虫活性。先前在体外研究过的一种低水溶性噻吩(thiophene)被包裹在 scYCWPs 中,以将其导向宿主细胞,从而避免水不溶性化合物的典型药代动力学问题。我们发现 scYCWPs+T6 降低了肝脏和脾脏中的寄生虫负担。IFN-γ 水平升高与一氧化氮产生有关,这解释了组织中利什曼原虫负担的减少。组织学分析未显示组织炎症信号,血浆生化分析也未显示 scYCWPs+T6 治疗后细胞毒性信号。这些发现表明,scYCWPs+T6 通过口服途径给药可降低寄生虫负担而不会引起毒性作用,满足开发治疗利什曼病的新策略的要求。