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犬弓首蛔虫 P-糖蛋白药物转运体的库。

Repertoire of P-glycoprotein drug transporters in the zoonotic nematode Toxocara canis.

机构信息

Department of Veterinary Pathology, College of Veterinary Medicine, Iowa State University, Ames, IA, USA.

Department of Diagnostic Medicine and Pathobiology, College of Veterinary Medicine, Kansas State University, 1800 Denison Ave, Manhattan, KS, USA.

出版信息

Sci Rep. 2023 Mar 27;13(1):4971. doi: 10.1038/s41598-023-31556-1.

Abstract

Toxocara canis has a complex lifecycle including larval stages in the somatic tissue of dogs that tolerate macrocyclic lactones. In this study, we investigated T. canis permeability glycoproteins (P-gps, ABCB1) with a putative role in drug tolerance. Motility experiments demonstrated that while ivermectin failed to abrogate larval movement, the combination of ivermectin and the P-gp inhibitor verapamil induced larval paralysis. Whole organism assays revealed functional P-gp activity in larvae which were capable of effluxing the P-gp substrate Hoechst 33342 (H33342). Further investigation of H33342 efflux demonstrated a unique rank order of potency for known mammalian P-gp inhibitors, suggesting that one or more of the T. canis transporters has nematode-specific pharmacological properties. Analysis of the T. canis draft genome resulted in the identification of 13 annotated P-gp genes, enabling revision of predicted gene names and identification of putative paralogs. Quantitative PCR was used to measure P-gp mRNA expression in adult worms, hatched larvae, and somatic larvae. At least 10 of the predicted genes were expressed in adults and hatched larvae, and at least 8 were expressed in somatic larvae. However, treatment of larvae with macrocyclic lactones failed to significantly increase P-gp expression as measured by qPCR. Further studies are needed to understand the role of individual P-gps with possible contributions to macrocyclic lactone tolerance in T. canis.

摘要

犬弓首蛔虫具有复杂的生命周期,包括在能耐受大环内酯类药物的犬体组织中的幼虫期。在本研究中,我们研究了具有潜在药物耐受性作用的犬弓首蛔虫渗透糖蛋白(P-gp,ABCB1)。运动实验表明,伊维菌素未能阻止幼虫运动,而伊维菌素和 P-糖蛋白抑制剂维拉帕米的联合使用则诱导幼虫瘫痪。全虫实验显示幼虫具有 P-糖蛋白活性,能够外排 P-糖蛋白底物 Hoechst 33342(H33342)。对 H33342 外排的进一步研究表明,已知的哺乳动物 P-糖蛋白抑制剂具有独特的效力顺序,这表明一种或多种犬弓首蛔虫转运蛋白具有线虫特异性的药理学特性。对犬弓首蛔虫草案基因组的分析导致了 13 个注释的 P-糖蛋白基因的鉴定,从而能够修订预测的基因名称并鉴定可能的同源基因。实时定量 PCR 用于测量成虫、孵化幼虫和体节幼虫中的 P-糖蛋白 mRNA 表达。至少 10 个预测基因在成虫和孵化幼虫中表达,至少 8 个在体节幼虫中表达。然而,用大环内酯类药物处理幼虫未能如 qPCR 所测量的那样显著增加 P-糖蛋白的表达。需要进一步的研究来了解单个 P-糖蛋白的作用,这可能对犬弓首蛔虫对大环内酯类药物的耐受性有贡献。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2548/10042841/f724e6f087a4/41598_2023_31556_Fig1_HTML.jpg

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