Pereira Vinícius R D, Junior Ismael J Alves, da Silveira Lígia S, Geraldo Reinaldo B, de F Pinto Priscila, Teixeira Fernanda S, Salvadori Maria C, Silva Marcos P, Alves Lara A, Capriles Priscila V S Z, das C Almeida Ayla, Coimbra Elaine S, Pinto Pedro L S, Couri Mara R C, de Moraes Josué, Da Silva Filho Ademar A
Faculdade de Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, R. José Lourenço Kelmer s/n, Campus Universitário, 36036-900, Juiz de Fora, MG, Brazil.
Departamento de Química, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, Brazil.
Chem Biodivers. 2018 Dec;15(12):e1800398. doi: 10.1002/cbdv.201800398. Epub 2018 Dec 10.
In this study, we evaluated the in vitro and in vivo schistosomicidal activities of chalcones against Schistosoma mansoni worms. In vitro assays revealed that chalcones 1 and 3 were the most active compounds, without affecting significantly mammalian cells. Confocal laser scanning microscopy and scanning electron microscopy studies revealed reduction on the numbers of tubercles and morphological alterations in the tegument of S. mansoni worms after in vitro incubation with chalcones 1 and 3. In a mouse model of schistosomiasis, the oral treatment (400 mg/kg) with chalcone 1 or 3 significantly caused a total worm burden reduction in mice. Chalcone 1 showed significant inhibition of the S. mansoni ATP diphosphohydrolase activity, which was corroborated by molecular docking studies. The results suggested that chalcones could be explored as lead compounds with antischistosomal properties.
在本研究中，我们评估了查耳酮对曼氏血吸虫的体外和体内杀血吸虫活性。体外试验表明，查耳酮1和3是活性最强的化合物，且对哺乳动物细胞无显著影响。共聚焦激光扫描显微镜和扫描电子显微镜研究显示，用查耳酮1和3进行体外孵育后，曼氏血吸虫虫体上的结节数量减少，其体表出现形态学改变。在血吸虫病小鼠模型中，用查耳酮1或3进行口服治疗（400 mg/kg）可显著降低小鼠体内的虫体总负荷。查耳酮1对曼氏血吸虫ATP二磷酸水解酶活性有显著抑制作用，分子对接研究证实了这一点。结果表明，查耳酮可作为具有抗血吸虫特性的先导化合物进行研究。
