de Brito Mariana G, Mengarda Ana C, Oliveira George L, Cirino Maria E, Silva Tais C, de Oliveira Rosimeire N, Allegretti Silmara M, de Moraes Josué
Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos, São Paulo, Brazil.
Instituto Federal de Educação, Ciência e Tecnologia de Mato Grosso, Campus Avançado de Guarantã do Norte, Guarantã do Norte, Mato Grosso, Brazil.
Antimicrob Agents Chemother. 2020 Oct 20;64(11). doi: 10.1128/AAC.01372-20.
Praziquantel is currently the only drug available to treat schistosomiasis, a disease of enormous public health significance caused by a blood fluke of the genus Diminazene, a drug approved by the FDA, has been successfully used to treat diseases caused by blood protozoan parasites. In this study, we evaluated the antiparasitic properties of diminazene against and in mice harboring either chronic or early infections. , we monitored phenotypic and tegumental changes as well as the effects of the drug on pairing and egg production. In mice infected with either adult (chronic infection) or immature (early infection) worms, diminazene was administered intraperitoneally (10 to 100 mg/kg of body weight) or by oral gavage (100 to 400 mg/kg), and we studied the influence of the drug on worm burden and egg production. Liver and spleen pathologies and serum aminotransferase levels were also analyzed. , 50% effective concentrations (EC) and EC revealed that diminazene is able to kill both immature and adult parasites, and its effect was time and concentration dependent. In addition, confocal laser scanning microscopy showed morphological alterations in the teguments of schistosomes. In an animal model, the influence of the drug on worm burden, egg production, hepatomegaly, and splenomegaly depended on the dosing regimen applied and the route of administration. Diminazene also caused a significant reduction in aminotransferase levels. Comparatively, diminazene treatment was more effective in chronic infection than in early infection. In tandem, our study revealed that diminazene possesses anthelmintic properties and inhibits liver injury caused by eggs.
吡喹酮是目前唯一可用于治疗血吸虫病的药物,血吸虫病是一种具有重大公共卫生意义的疾病,由日本血吸虫属的一种血吸虫引起。地美硝唑是一种经美国食品药品监督管理局批准的药物,已成功用于治疗由血液原生动物寄生虫引起的疾病。在本研究中,我们评估了地美硝唑对感染慢性或早期血吸虫的小鼠的抗寄生虫特性。我们监测了表型和体表变化以及该药物对配对和产卵的影响。在感染成虫(慢性感染)或未成熟虫体(早期感染)的小鼠中,通过腹腔注射(10至100毫克/千克体重)或灌胃(100至400毫克/千克)给予地美硝唑,我们研究了该药物对虫负荷和产卵的影响。还分析了肝脏和脾脏病理学以及血清转氨酶水平。50%有效浓度(EC)和EC表明,地美硝唑能够杀死未成熟和成虫寄生虫,其效果具有时间和浓度依赖性。此外,共聚焦激光扫描显微镜显示血吸虫体表有形态学改变。在动物模型中,该药物对虫负荷、产卵、肝肿大和脾肿大的影响取决于给药方案和给药途径。地美硝唑还导致转氨酶水平显著降低。相比之下,地美硝唑治疗在慢性感染中比在早期感染中更有效。同时,我们的研究表明,地美硝唑具有驱虫特性,并能抑制由虫卵引起的肝损伤。