Efficacy of ursolic acid against Echinococcus granulosus in vitro and in a murine infection model.
Efficacy of ursolic acid against Echinococcus granulosus in vitro and in a murine infection model.
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熊果酸在体外和小鼠感染模型中对抗细粒棘球绦虫的功效
DOI：
10.1186/s13071-018-2628-8
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发表时间：
2018-01-24
影响因子：
3.2
通讯作者：
Cao J
中科院分区：
文献类型：
--
作者：
Yin J;Liu C;Shen Y;Zhang H;Cao J
囊型包虫病是一个全球性的公共卫生问题；然而，目前世卫组织推荐用于治疗囊型包虫病的药物(阿苯达唑和甲苯达唑)疗效有限。因此，需要新的药物为本病的治疗提供更多的选择。体外实验测定了熊果酸(UA)对细粒棘球绦虫原头节、生殖细胞和后鞭毛虫的驱虫作用。研究了尿酸对细粒棘球绦虫二次感染小鼠的体内疗效。并用电子显微镜观察UA所致的相应超微结构损伤。在体外，40 g/ml的UA对原头节的杀伤率为45.95%± 5.30%，10~40μg/ml的UA对90%以上的生发细胞的生长有抑制作用，10、20和40μg/ml的UA处理7天后对后鞭毛虫也有同样的作用，实验结束时超过50%的后鞭毛虫失去完整性。在体内，口服200和100 mg/kg的UA可显著减轻小鼠的后鞭毛虫重量(分别为39.5%和38.3%)。此外，体外用UA处理的寄生虫还观察到超微结构的损伤，如生发细胞形态的改变、空泡和脂肪颗粒的形成，而体内的后生孢子虫也观察到生发层与层状层的分离。UA在体内外对细粒棘球绦虫均有一定的杀灭活性，提示UA可能是一种潜在的抗包虫病药物。
Cystic echinococcosis is a global public health problem; however, the drugs (albendazole and mebendazole) currently recommended by WHO for its treatment, have limited efficacy. Therefore, novel drugs are required to provide more choices for the treatment of this disease. The anthelmintic effects of ursolic acid (UA) were tested on Echinococcus granulosus protoscoleces, germinal cells and metacestodes in vitro. The in vivo efficacy of UA was investigated in mice following secondary infection with E. granulosus. Furthermore, the corresponding ultrastructural damage induced by UA was evaluated by electron microscopy. In vitro, 45.95 ± 5.30% of protoscoleces were killed by UA at 40 μg/ml, while the growth of more than 90% of germinal cells was inhibited by UA at 10 to 40 μg/ml. The same effect was observed in metacestodes 7 days after treatment with UA at 10, 20 and 40 μg/ml, and more than 50% of metacestodes showed loss of integrity at the end of the experiment. In vivo, metacestode weight was significantly reduced following oral administration of UA at 200 and 100 mg/kg (39.5 and 38.3%, respectively). Additionally, ultrastructural damage, such as alternations in germinal cell morphology and formation of vacuoles and lipid granules were observed in parasites treated with UA in vitro, while detachment of the germinal layer from the laminated layer was also seen in metacestodes in vivo. UA was demonstrated to exert parasiticidal activity against E. granulosus in vitro and in vivo, thus implicating UA as a potential anti-echinococcosis agent.
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影响因子：
2.7
作者：
Klug DM;Gelb MH;Pollastri MP
通讯作者：
Pollastri MP
影响因子：
4.7
作者：
Fragkouli, Apostolia;Papatheodoropoulos, Costas;Tzinia, Athina K.
通讯作者：
Tzinia, Athina K.
影响因子：
4
作者：
Gelmedin, Verena;Spiliotis, Markus;Brehm, Klaus
通讯作者：
Brehm, Klaus
影响因子：
4.9
作者：
Celeste Nicolao, Maria;Celina Elissondo, Maria;Cumino, Andrea C.
通讯作者：
Cumino, Andrea C.
影响因子：
--
作者：
Qian Z;Wang X;Song Z;Zhang H;Zhou S;Zhao J;Wang H
通讯作者：
Wang H