Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos, São Paulo, Brazil.
Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Santo André, São Paulo, Brazil.
Phytother Res. 2021 Sep;35(9):5154-5162. doi: 10.1002/ptr.7184. Epub 2021 Jun 5.
Schistosomiasis is a widespread human parasitic disease currently affecting over 200 million people, particularly in poor communities. Chemotherapy for schistosomiasis relies exclusively on praziquantel (PZQ). Previous studies have shown that licarin A (LIC-A), a dihydrobenzofuran neolignan, exhibited in vitro antiparasitic activity against Schistosoma mansoni adult worms. This study aimed to investigate the potential of LIC-A, isolated as main metabolite from leaves of Nectandra oppositifolia Nees & Mart. (Lauraceae), as an antischistosomal agent orally active in schistosomiasis animal model. PZQ was used as a reference compound. As result, LIC-A showed, at a single dose of 400 mg/kg, to be able to partially cure infected mice (worm burden reductions of ~50%). Parasite eggs, that are responsible for a variety of pathologies and transmission of schistosomiasis, were also moderately inhibited by LIC-A (egg burden reductions of ~50%-60%). Furthermore, it was observed that LIC-A achieved a slight reduction of hepatomegaly and splenomegaly. Collectively, although LIC-A was partially active when administered orally, these results give support for the antiparasitic potential LIC-A as lead compound for novel antischistosomal agent.
血吸虫病是一种广泛存在的人类寄生虫病,目前影响着超过 2 亿人,特别是在贫困社区。血吸虫病的化学疗法完全依赖于吡喹酮(PZQ)。先前的研究表明,二氢苯并呋喃新木脂素利卡林 A(LIC-A)对曼氏血吸虫成虫表现出体外抗寄生虫活性。本研究旨在研究利卡林 A(从 Nees & Mart.(Lauraceae)的 Nectandra oppositifolia Nees & Mart. 的叶子中分离出来的主要代谢物)作为一种抗血吸虫药物的潜力,在血吸虫病动物模型中具有口服活性。吡喹酮被用作参考化合物。结果表明,利卡林 A 在单剂量 400mg/kg 时能够部分治愈感染的小鼠(约减少 50%的蠕虫负荷)。利卡林 A 还适度抑制了寄生虫卵,寄生虫卵是多种病理和血吸虫病传播的原因(约减少 50%-60%的卵负荷)。此外,还观察到利卡林 A 略微减轻了肝脾肿大。总之,尽管利卡林 A 经口服给药时具有部分活性,但这些结果支持了利卡林 A 作为新型抗血吸虫药物的先导化合物的抗寄生虫潜力。