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首页> 外文期刊>Parasitology >The anthelmintic efficacy of plant-derived cysteine proteinases against the rodent gastrointestinal nematode, Heligmosomoides polygyrus, in vivo.
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The anthelmintic efficacy of plant-derived cysteine proteinases against the rodent gastrointestinal nematode, Heligmosomoides polygyrus, in vivo.

机译：在体内，植物来源的半胱氨酸蛋白酶对啮齿类胃肠道线虫多螺旋藻的驱虫效果。

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Gastrointestinal (GI) nematodes are important disease-causing organisms, controlled primarily through treatment with synthetic drugs, but the efficacy of these drugs has declined due to widespread resistance, and hence new drugs, with different modes of action, are required. Some medicinal plants, used traditionally for the treatment of worm infections, contain cysteine proteinases known to damage worms irreversibly in vitro. Here we (i) confirm that papaya latex has marked efficacy in vivo against the rodent gastrointestinal nematode, Heligmosomoides polygyrus, (ii) demonstrate the dose-dependent nature of the activity (>90% reduction in egg output and 80% reduction in worm burden at the highest active enzyme concentration of 133 nmol), (iii) establish unequivocally that it is the cysteine proteinases that are the active principles in vivo (complete inhibition of enzyme activity when pre-incubated with the cysteine proteinase-specific inhibitor, E-64) and (iv) show that activity is confined to worms that are in the intestinal lumen. The mechanism of action was distinct from all current synthetic anthelmintics, and was the same as that in vitro, with the enzymes attacking and digesting the protective cuticle. Treatment had no detectable side-effects on immune cell numbers in the mucosa (there was no difference in the numbers of mast cells and goblet cells between the treated groups) and mucosal architecture (length of intestinal villi). Only the infected and untreated mice had much shorter villi than the other 3 groups, which was a consequence of infection and not treatment. Plant-derived cysteine proteinases are therefore prime candidates for development as novel drugs for the treatment of GI nematode infections.
机译：胃肠道（GI）线虫是重要的致病生物，主要通过合成药物治疗来控制，但是由于广泛的耐药性，这些药物的功效已经下降，因此需要具有不同作用方式的新药物。一些传统上用于治疗蠕虫感染的药用植物都含有半胱氨酸蛋白酶，已知该酶在体外会不可逆地破坏蠕虫。在这里，我们（i）确认木瓜乳胶在体内对啮齿类胃肠道线虫多螺旋藻具有显着功效，（ii）证明了该活性的剂量依赖性（卵产量减少90％以上，蠕虫负担减少80％以上）在最高活性酶浓度为133 nmol时）（iii）明确地确定半胱氨酸蛋白酶是体内的活性成分（与半胱氨酸蛋白酶特异性抑制剂E-64预孵育后完全抑制了酶的活性）和（iv）表明活动仅限于肠腔中的蠕虫。作用机理不同于目前所有的合成驱虫药，并且与体外的驱虫酶相同，其酶攻击并消化了保护性表皮。治疗对粘膜中免疫细胞数目（治疗组之间肥大细胞和杯状细胞数目没有差异）和粘膜结构（肠绒毛长度）没有可检测到的副作用。只有感染和未经治疗的小鼠的绒毛比其他3组要短得多，这是感染而不是治疗的结果。因此，植物来源的半胱氨酸蛋白酶是开发用于治疗胃肠道线虫感染的新药的主要候选药物。

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