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来自亚侧枝石蕊(地衣)的松萝酸钾盐:合成、细胞毒性、体外驱虫活性以及对曼氏血吸虫成虫的超微结构分析

Usnic acid potassium salt from Cladonia substellata (Lichen): Synthesis, cytotoxicity and in vitro anthelmintic activity and ultrastructural analysis against adult worms of Schistosoma mansoni.

作者信息

Araújo Hallysson D A, Aires André L, Soares Caroline L R, Brito Thaíse G S, Nascimento Weber M, Martins Mônica C B, Silva Teresinha G, Brayner Fábio A, Alves Luiz C, Silva Nicácio H, Albuquerque Mônica C P A, Lima Vera L M

机构信息

Departamento de Bioquímica, Centro de Biociência, Universidade Federal de Pernambuco, Avenida Prof. Moraes Rego, 1235, Cidade Universitária. CEP 50.670-901, Recife, PE, Brazil.

Departamento de Medicina Tropical, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, Avenida Prof. Moraes Rego, s/n, Cidade Universitária, 50740-600, Recife, PE, Brazil; Laboratório de Imunopatologia Keizo Asami (LIKA), Universidade Federal de Pernambuco, Avenida Prof. Moraes Rego, 1235, Cidade Universitária. CEP 50.670-901, Recife, PE, Brazil.

出版信息

Acta Trop. 2019 Apr;192:1-10. doi: 10.1016/j.actatropica.2018.12.024. Epub 2018 Dec 17.

Abstract

We report for the first time the in vitro effect of Potassium Salt, derived from Usnic Acid (PS-UA), isolated from the lichen Cladonia substellata Vanio, on couples of Schistosoma mansoni. As schistosomicide parameters, we evaluated mortality, motility, cell viability of the worms and tegument changes by scanning electron microscopy (SEM). Exposure to a concentration of 100 μM caused 75% mortality after 3 h. After 6 h, changes in motility in concentrations of 50 and 25 μM are evidenced. After 12 h and 24h, the concentrations of 50 and 100 μM caused 6.25% and 87.5% and 50% and 100% mortality, respectively. PS-UA reduced the cell viability of the worms by 27.36% and 52.82% at concentrations 50 and 100 μM, respectively. Through SEM we observed progressive dose-and time-dependent, alterations such as swelling, blisters, dorsoventral contraction, erosion until disintegration of the tubercles in the tegument of male and female. PS-UA did not alter the viability of human peripheral blood mononuclear cells and showed high selectivity indices (IC > 200 μM). Our results indicate that PS-UA represents a possible candidate for a new anthelmintic drug in the control of schistosomiasis.

摘要

我们首次报告了从地衣亚纲星状石蕊中分离出的扁枝衣酸钾盐(PS-UA)对曼氏血吸虫成虫的体外作用。作为杀血吸虫参数,我们通过扫描电子显微镜(SEM)评估了虫体的死亡率、活力、细胞活力以及体表变化。暴露于100μM的浓度下,3小时后导致75%的死亡率。6小时后,50μM和25μM浓度下的活力变化得到证实。12小时和24小时后,50μM和100μM的浓度分别导致6.25%、87.5%以及50%、100%的死亡率。PS-UA在50μM和100μM浓度下分别使虫体细胞活力降低了27.36%和52.82%。通过扫描电子显微镜,我们观察到了剂量和时间依赖性的渐进变化,如肿胀、水泡、背腹收缩、糜烂,直至雌雄虫体表结节解体。PS-UA并未改变人外周血单核细胞的活力,并显示出高选择性指数(IC>200μM)。我们的结果表明,PS-UA可能是一种用于控制血吸虫病的新型驱虫药物的候选物。

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