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Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs
Human helminthiasis affects approximately one in five people in the world and disproportionally affects the poorest and most deprived communities. Human angiostrongyliasis, caused by nematode Angiostrongylus cantonensis, is a neglected emerging disease with escalating importance worldwide. Chemother...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Frontiers Media S.A.
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9255552/ https://www.ncbi.nlm.nih.gov/pubmed/35800438 http://dx.doi.org/10.3389/fphar.2022.901459 |
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author | Roquini, Daniel B. Silva, Gabriel L. Ferreira, Leonardo L. G. Andricopulo, Adriano D. Wilairatana, Polrat De Moraes, Josué |
author_facet | Roquini, Daniel B. Silva, Gabriel L. Ferreira, Leonardo L. G. Andricopulo, Adriano D. Wilairatana, Polrat De Moraes, Josué |
author_sort | Roquini, Daniel B. |
collection | PubMed |
description | Human helminthiasis affects approximately one in five people in the world and disproportionally affects the poorest and most deprived communities. Human angiostrongyliasis, caused by nematode Angiostrongylus cantonensis, is a neglected emerging disease with escalating importance worldwide. Chemotherapy is the main control method for helminthiasis, but the therapeutic arsenal is limited. This study aimed to evaluate the antiparasitic and molecular properties of the major available anthelmintic drugs against A. cantonensis in vitro. The first-stage larvae (L1), isolated from feces of an A. cantonensis-infected rat, were exposed to a set of 12 anthelmintic drugs in vitro. The larvae were monitored, and the concentration- and time-dependent viability alterations were determined. From 12 anthelmintic drugs, six (ivermectin, salamectin, moxidectin, pyrantel pamoate, albendazole and levamisole) were identified to affect the viability of A. cantonensis. The macrocyclic lactones (ivermectin, salamectin, moxidectin) and the imidazothiazole levamisole, were the most effective drugs, with IC(50) ranging from 2.2 to 2.9 µM and a rapid onset of action. Albendazole, the most widely used anthelmintic in humans, had a slower onset of action, but an IC(50) of 11.3 µM was achieved within 24 h. Molecular properties studies suggest that a less lipophilic character and low molecular weight could be favorable for the biological activity of the non-macrocyclic molecules. Collectively, our study revealed that macrocyclic lactones, levamisole, pyrantel pamoate, and albendazole are important anthelmintic agents against A. cantonensis. The results of this in vitro study also suggest that A. cantonensis L1 may be a particularly sensitive and useful model for anthelmintic studies. |
format | Online Article Text |
id | pubmed-9255552 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-92555522022-07-06 Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs Roquini, Daniel B. Silva, Gabriel L. Ferreira, Leonardo L. G. Andricopulo, Adriano D. Wilairatana, Polrat De Moraes, Josué Front Pharmacol Pharmacology Human helminthiasis affects approximately one in five people in the world and disproportionally affects the poorest and most deprived communities. Human angiostrongyliasis, caused by nematode Angiostrongylus cantonensis, is a neglected emerging disease with escalating importance worldwide. Chemotherapy is the main control method for helminthiasis, but the therapeutic arsenal is limited. This study aimed to evaluate the antiparasitic and molecular properties of the major available anthelmintic drugs against A. cantonensis in vitro. The first-stage larvae (L1), isolated from feces of an A. cantonensis-infected rat, were exposed to a set of 12 anthelmintic drugs in vitro. The larvae were monitored, and the concentration- and time-dependent viability alterations were determined. From 12 anthelmintic drugs, six (ivermectin, salamectin, moxidectin, pyrantel pamoate, albendazole and levamisole) were identified to affect the viability of A. cantonensis. The macrocyclic lactones (ivermectin, salamectin, moxidectin) and the imidazothiazole levamisole, were the most effective drugs, with IC(50) ranging from 2.2 to 2.9 µM and a rapid onset of action. Albendazole, the most widely used anthelmintic in humans, had a slower onset of action, but an IC(50) of 11.3 µM was achieved within 24 h. Molecular properties studies suggest that a less lipophilic character and low molecular weight could be favorable for the biological activity of the non-macrocyclic molecules. Collectively, our study revealed that macrocyclic lactones, levamisole, pyrantel pamoate, and albendazole are important anthelmintic agents against A. cantonensis. The results of this in vitro study also suggest that A. cantonensis L1 may be a particularly sensitive and useful model for anthelmintic studies. Frontiers Media S.A. 2022-06-21 /pmc/articles/PMC9255552/ /pubmed/35800438 http://dx.doi.org/10.3389/fphar.2022.901459 Text en Copyright © 2022 Roquini, Silva, Ferreira, Andricopulo, Wilairatana and De Moraes. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Pharmacology Roquini, Daniel B. Silva, Gabriel L. Ferreira, Leonardo L. G. Andricopulo, Adriano D. Wilairatana, Polrat De Moraes, Josué Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title | Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title_full | Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title_fullStr | Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title_full_unstemmed | Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title_short | Susceptibility of Angiostrongylus cantonensis Larvae to Anthelmintic Drugs |
title_sort | susceptibility of angiostrongylus cantonensis larvae to anthelmintic drugs |
topic | Pharmacology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9255552/ https://www.ncbi.nlm.nih.gov/pubmed/35800438 http://dx.doi.org/10.3389/fphar.2022.901459 |
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