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首页> 外文期刊>Parasitology >Efficacy of the cyclooctadepsipeptide PF1022A against Heligmosomoides bakeri in vitro and in vivo
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Efficacy of the cyclooctadepsipeptide PF1022A against Heligmosomoides bakeri in vitro and in vivo

机译：环八肽肽PF1022A在体外和体内对面包酵母的功效

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摘要

The cyclooctadepsipeptide PF1022A derived from the fungus, Mycelia sterilia, is characterized by a broad spectrum of activity against different parasitic gastrointestinal nematodes of livestock. In the present work the anthelmintic activity of PF1022A against Heligmosomoides bakeri, a widely used laboratory model was studied. Albendazole, ivermectin and levamisole served as reference. In vitro, PF1022A showed low activity on embryonation but significantly inhibited egg hatch (10 and 100mug/ml), whereas albendazole (10 and 100mug/ml) revealed statistically significant inhibitions of both embryonation and egg hatch. PF1022A (1-100mug/ml) completely inhibited larval movement at most examination points. Comparable significant anthelmintic activity on the larval stages of H. bakeri was observed with levamisole (48-100%), while slightly lower activities were observed with ivermectin (20-92%) and albendazole (0-87%) at 1-100mug/ml. PF1022A and levamisole significantly inhibited motility and egg release of adult worms, while albendazole and ivermectin failed to demonstrate activity. Significant worm burden reductions were achieved with PF1022A, levamisole and ivermectin in vivo. For example, at 0125 mg/kg PF1022A a worm burden reduction of 91.8% was observed. The use of drug combinations did not further enhance the in vitro and in vivo activity of PF1022A. In conclusion, further investigations are warranted with PF1022A, as the drug is characterized by significant larvicidal and nematocidal activity in vitro and in vivo.
机译：源自真菌菌丝体菌丝体的环八肽肽PF1022A具有针对牲畜的不同寄生性胃肠线虫的广谱活性。在目前的工作中，研究了PF1022A对面包虫Heligmosomoides bakeri的驱虫活性，这是一种广泛使用的实验室模型。阿苯达唑，伊维菌素和左旋咪唑为参考。在体外，PF1022A对胚的活性低，但能显着抑制卵孵化（10和100mug / ml），而阿苯达唑（10和100mug / ml）对胚和卵孵化具有统计学上的显着抑制。 PF1022A（1-100mug / ml）在大多数检查点完全抑制了幼虫的运动。与左旋咪唑（48-100％）相比，在面包虫的幼虫阶段有相当大的驱虫活性，而伊维菌素（20-92％）和阿苯达唑（0-7％）在1-100ug /毫升PF1022A和左旋咪唑显着抑制成虫的蠕动和卵子释放，而阿苯达唑和伊维菌素则没有活性。体内PF1022A，左旋咪唑和伊维菌素可显着降低蠕虫负担。例如，在0125 mg / kg PF1022A处，蠕虫负担减少了91.8％。药物组合的使用并未进一步增强PF1022A的体外和体内活性。总之，由于PF1022A具有体外和体内显着的杀幼虫和杀线虫活性，因此有待进一步研究。

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