Baccharismattogrossis是菊科的一种,已在巴西民间医学中用于治疗几种疾病,包括那些由寄生虫引起的。在目前的工作中,将B.mattogrosis的地上部分的MeOH提取物进行色谱分馏,以提供三种类黄酮:芹菜素(1),槲皮素(2),和山奈酚(3)以及三种绿原酸的混合物:3,4-O-二咖啡酰基奎尼酸(4),3,5-O-二咖啡酰基奎因(5),和4,5-O-二咖啡酰基奎尼酸(6)。在体外测试时,山奈酚(3)表现出对曼氏血吸虫的活性,EC50=81.86μM,而化合物1,2,4-6显示为失活。考虑到这个结果,首次测试了山奈酚(3)对曼氏链球菌感染的体内试验效果。使用单一口服剂量(400mg/kg)的山奈酚(3)对曼氏链球菌感染的小鼠减少了25.5%的蠕虫负担。同样,鸡蛋的数量,它们是血吸虫病的各种病理和传播的原因,在处理的小鼠中减少了28.8%。总的来说,尽管山奈酚(3)在血吸虫病小鼠模型中口服给药时具有部分活性,我们的结果表明,这种化合物可能是,在未来的研究中,以不同的形式管理,如纳米配方。
Baccharis mattogrosensis is a species from Asteraceae which has been used in Brazilian folk medicine to treatment of several illnesses, including those caused by parasites. In the present work, the MeOH extract of aerial parts of B. mattogrosensis was subjected to chromatographic fractionation to afford three flavonoids: apigenin (1), quercetin (2), and
kaempferol (3) as well as a mixture three chlorogenic acids: 3,4-O-dicaffeoylquinic (4), 3,5-O-dicaffeoylquinic (5), and 4,5-O-dicaffeoylquinic (6) acids. When tested in vitro,
kaempferol (3) exhibited activity against Schistosoma mansoni with EC50 = 81.86 μM, whereas compounds 1, 2, 4 - 6 showed to be inactives. Considering this result, the effects of
kaempferol (3) against S. mansoni infection using in vivo assay was tested at first time. Using a single oral dose (400 mg/kg) of
kaempferol (3) to S. mansoni-infected mice reduced the worm burden by 25.5%. Similarly, the number of eggs, which are responsible for a variety of pathologies and transmission of schistosomiasis, was decreased by 28.8% in treated mice. Collectively, although
kaempferol (3) is partially active when administered orally in a mouse model of schistosomiasis, our results suggest that this compound could be, in future studies, administered in different forms, such as nanoformulation.