{"title":"二芳基二羰基苷和伊维菌素对肝吸虫的杀卵活性:混合治疗策略的新候选方案。","authors":"Irineu Romero-Neto , Thayany Magalhães de Almeida , Tay Zugman , Leandro Piovan , Marcelo Beltrão Molento","doi":"10.1016/j.actatropica.2024.107363","DOIUrl":null,"url":null,"abstract":"<div><p>Fasciolosis is a food and waterborne disease caused by <em>Fasciola</em> spp., representing a global health burden to various hosts, including humans and other animals. This study investigates the <em>in vitro</em> activity of tellurium- and selenium-containing diaryl dichalcogenides: diacetal ditelluride (LQ07), diacetal diselenide (LQ62), and diacetyl diselenide (LQ68) alone and in combination with ivermectin (IVM) against eggs of <em>Fasciola hepatica</em>. The eggs were exposed for 12 h with each organochalcogen (OC) (0.1 - 2 mmol <span>l</span><sup>-1</sup>) and IVM (0.01 - 2 mmol <span>l</span><sup>-1</sup>) following an incubation of 15 days, allowing embryonation. The inhibitory concentration of 50 % (IC<sub>50</sub>) of each OC or IVM was tested with the IC<sub>10</sub>, IC<sub>30</sub>, and IC<sub>50</sub> of IVM or each OC, respectively. LQ07, LQ62, and LQ68, as well as IVM, demonstrated a concentration-dependent ovicidal activity. The peak ovicidal activity of 99.74 % was achieved when IVM was tested at 2.0 mmol <span>l</span><sup>-1</sup>. LQ62 and LQ68 demonstrated greater ovicidal activity, having an IC<sub>50</sub> < 0.32 mmol <span>l</span><sup>-1</sup> being 6.25-fold more toxic than IVM alone. The percentage of dead eggs was significantly higher in the IVM group (early mortality), as Se-containing OCs led to the (miracidia) embryonation of the eggs with no hatching (late mortality). Blending Se-containing OCs and IVM showed an additive effect of up to 27 % against <em>F. hepatica</em> eggs. The present data contribute to the potential use of blending-based therapeutic strategies to combat <em>F. hepatica</em> infections in eradication programs worldwide. The combinations may also act against multidrug-resistant strains, reinstating drug-based parasite control.</p></div>","PeriodicalId":7240,"journal":{"name":"Acta tropica","volume":null,"pages":null},"PeriodicalIF":2.1000,"publicationDate":"2024-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Ovicidal activity of diaryl dichalcogenides and ivermectin on Fasciola hepatica: A novel candidate for a blending-based therapeutic strategy\",\"authors\":\"Irineu Romero-Neto , Thayany Magalhães de Almeida , Tay Zugman , Leandro Piovan , Marcelo Beltrão Molento\",\"doi\":\"10.1016/j.actatropica.2024.107363\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Fasciolosis is a food and waterborne disease caused by <em>Fasciola</em> spp., representing a global health burden to various hosts, including humans and other animals. This study investigates the <em>in vitro</em> activity of tellurium- and selenium-containing diaryl dichalcogenides: diacetal ditelluride (LQ07), diacetal diselenide (LQ62), and diacetyl diselenide (LQ68) alone and in combination with ivermectin (IVM) against eggs of <em>Fasciola hepatica</em>. The eggs were exposed for 12 h with each organochalcogen (OC) (0.1 - 2 mmol <span>l</span><sup>-1</sup>) and IVM (0.01 - 2 mmol <span>l</span><sup>-1</sup>) following an incubation of 15 days, allowing embryonation. The inhibitory concentration of 50 % (IC<sub>50</sub>) of each OC or IVM was tested with the IC<sub>10</sub>, IC<sub>30</sub>, and IC<sub>50</sub> of IVM or each OC, respectively. LQ07, LQ62, and LQ68, as well as IVM, demonstrated a concentration-dependent ovicidal activity. The peak ovicidal activity of 99.74 % was achieved when IVM was tested at 2.0 mmol <span>l</span><sup>-1</sup>. LQ62 and LQ68 demonstrated greater ovicidal activity, having an IC<sub>50</sub> < 0.32 mmol <span>l</span><sup>-1</sup> being 6.25-fold more toxic than IVM alone. The percentage of dead eggs was significantly higher in the IVM group (early mortality), as Se-containing OCs led to the (miracidia) embryonation of the eggs with no hatching (late mortality). Blending Se-containing OCs and IVM showed an additive effect of up to 27 % against <em>F. hepatica</em> eggs. The present data contribute to the potential use of blending-based therapeutic strategies to combat <em>F. hepatica</em> infections in eradication programs worldwide. The combinations may also act against multidrug-resistant strains, reinstating drug-based parasite control.</p></div>\",\"PeriodicalId\":7240,\"journal\":{\"name\":\"Acta tropica\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.1000,\"publicationDate\":\"2024-08-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Acta tropica\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0001706X24002456\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PARASITOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Acta tropica","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0001706X24002456","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PARASITOLOGY","Score":null,"Total":0}
Ovicidal activity of diaryl dichalcogenides and ivermectin on Fasciola hepatica: A novel candidate for a blending-based therapeutic strategy
Fasciolosis is a food and waterborne disease caused by Fasciola spp., representing a global health burden to various hosts, including humans and other animals. This study investigates the in vitro activity of tellurium- and selenium-containing diaryl dichalcogenides: diacetal ditelluride (LQ07), diacetal diselenide (LQ62), and diacetyl diselenide (LQ68) alone and in combination with ivermectin (IVM) against eggs of Fasciola hepatica. The eggs were exposed for 12 h with each organochalcogen (OC) (0.1 - 2 mmol l-1) and IVM (0.01 - 2 mmol l-1) following an incubation of 15 days, allowing embryonation. The inhibitory concentration of 50 % (IC50) of each OC or IVM was tested with the IC10, IC30, and IC50 of IVM or each OC, respectively. LQ07, LQ62, and LQ68, as well as IVM, demonstrated a concentration-dependent ovicidal activity. The peak ovicidal activity of 99.74 % was achieved when IVM was tested at 2.0 mmol l-1. LQ62 and LQ68 demonstrated greater ovicidal activity, having an IC50 < 0.32 mmol l-1 being 6.25-fold more toxic than IVM alone. The percentage of dead eggs was significantly higher in the IVM group (early mortality), as Se-containing OCs led to the (miracidia) embryonation of the eggs with no hatching (late mortality). Blending Se-containing OCs and IVM showed an additive effect of up to 27 % against F. hepatica eggs. The present data contribute to the potential use of blending-based therapeutic strategies to combat F. hepatica infections in eradication programs worldwide. The combinations may also act against multidrug-resistant strains, reinstating drug-based parasite control.
期刊介绍:
Acta Tropica, is an international journal on infectious diseases that covers public health sciences and biomedical research with particular emphasis on topics relevant to human and animal health in the tropics and the subtropics.