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舍曲林作为一种新型驱虫药对抗捻转血矛线虫的毒性、疗效和生物转化。

Sertraline as a new potential anthelmintic against Haemonchus contortus: toxicity, efficacy, and biotransformation.

机构信息

Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05, Hradec Králové, Czech Republic.

Biomedical Research Centre, University Hospital in Hradec Králové, Hradec Králové, Czech Republic.

出版信息

Vet Res. 2021 Dec 11;52(1):143. doi: 10.1186/s13567-021-01012-x.

DOI:10.1186/s13567-021-01012-x
PMID:34895342
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8666012/
Abstract

Haemonchus contortus is a parasitic nematode of ruminants which causes significant losses to many farmers worldwide. Since the drugs currently in use for the treatment of haemonchosis are losing their effectiveness due to the drug-resistance of this nematode, a new or repurposed drug is highly needed. As the antipsychotic drug sertraline (SRT) has been shown to be effective against the parasitic nematodes Trichuris muris, Ancylostoma caninum and Schistosoma mansoni, the aim of the present study was to evaluate the possible effect of SRT on H. contortus. The potential hepatotoxicity of SRT was tested in sheep, a common H. contortus host. In addition, the main metabolic pathways of SRT in H. contortus and the ovine liver were identified. While no effect of SRT on H. contortus egg hatching was observed, SRT was found to significantly decrease the viability of H. contortus adults in drug-sensitive and resistant strains, with its effect comparable to the commonly used anthelmintics levamisole and monepantel. Moreover, SRT in anthelmintically active concentrations showed no toxicity to the ovine liver. Biotransformation of SRT in H. contortus was weak, with most of the drug remaining unmetabolized. Production of the main metabolite hydroxy-SRT did not differ significantly between strains. Other minor metabolites such as SRT-O-glucoside, dihydroxy-SRT, and SRT-ketone were also identified in H. contorts adults. Compared to H. contortus, the ovine liver metabolized SRT more extensively, mainly via desmethylation and glucuronidation. In conclusion, the potency of SRT against H. contortus was proven, and it should be tested further toward possible repurposing.

摘要

捻转血矛线虫是反刍动物的寄生性线虫，它会给全世界许多农民造成重大损失。由于目前用于治疗血矛线虫病的药物由于这种线虫的耐药性而失效，因此非常需要一种新的或重新利用的药物。由于抗精神病药物舍曲林（SRT）已被证明对寄生性线虫秀丽隐杆线虫、犬钩虫和曼氏血吸虫有效，本研究旨在评估 SRT 对捻转血矛线虫的可能作用。SRT 的潜在肝毒性在绵羊中进行了测试，绵羊是捻转血矛线虫的常见宿主。此外，还鉴定了 SRT 在捻转血矛线虫和绵羊肝脏中的主要代谢途径。虽然 SRT 对捻转血矛线虫卵孵化没有影响，但发现 SRT 可显著降低敏感和耐药株捻转血矛线虫成虫的活力，其作用可与常用驱虫药左旋咪唑和莫能菌素相媲美。此外，具有驱虫活性浓度的 SRT 对绵羊肝脏没有毒性。SRT 在捻转血矛线虫中的生物转化较弱，大部分药物未代谢。主代谢物羟基-SRT 的产生在不同菌株之间没有显著差异。在捻转血矛线虫成虫中还鉴定出其他次要代谢物，如 SRT-O-葡萄糖苷、二羟基-SRT 和 SRT-酮。与捻转血矛线虫相比，绵羊肝脏更广泛地代谢 SRT，主要通过去甲基化和葡萄糖醛酸化。总之，SRT 对捻转血矛线虫的效力已得到证明，应进一步测试其可能的再利用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/483c/8666012/b232780ab47c/13567_2021_1012_Fig7_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/483c/8666012/b232780ab47c/13567_2021_1012_Fig7_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/483c/8666012/77dbecb24496/13567_2021_1012_Fig3_HTML.jpg
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