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Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity

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Title: Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity
Authors: Luiz Saramago, Helga Gomes, Elena Aguilera, Hugo Cerecetto, Mercedes González, Mauricio Cabrera, Maria Fernanda Alzugaray, Itabajara da Silva Vaz Junior, Rodrigo Nunes da Fonseca, Beatriz Aguirre-López, Nallely Cabrera, Ruy Pérez-Montfort, Alicia Merlino, Jorge Moraes, Guzmán Álvarez
Source: Veterinary Sciences, Vol 5, Iss 3, p 74 (2018)
Publisher Information: MDPI AG, 2018.
Publication Year: 2018
Collection: LCC:Veterinary medicine
Subject Terms: triosephosphate isomerase inhibitors, Rhipicephalus microplus, acaricidal compounds, Veterinary medicine, SF600-1100
More Details: The cattle tick Rhipicephalus microplus is one of the most important ectoparasites causing significant economic losses for the cattle industry. The major tool of control is reducing the number of ticks, applying acaricides in cattle. However, overuse has led to selection of resistant populations of R. microplus to most of these products, some even to more than one active principle. Thus, exploration for new molecules with acaricidal activity in R. microplus has become necessary. Triosephosphate isomerase (TIM) is an essential enzyme in R. microplus metabolism and could be an interesting target for the development of new methods for tick control. In this work, we screened 227 compounds, from our in-house chemo-library, against TIM from R. microplus. Four compounds (50, 98, 14, and 161) selectively inhibited this enzyme with IC50 values between 25 and 50 μM. They were also able to diminish cellular viability of BME26 embryonic cells by more than 50% at 50 μM. A molecular docking study showed that the compounds bind in different regions of the protein; compound 14 interacts with the dimer interface. Furthermore, compound 14 affected the survival of partially engorged females, fed artificially, using the capillary technique. This molecule is simple, easy to produce, and important biological data—including toxicological information—are available for it. Our results imply a promising role for compound 14 as a prototype for development of a new acaricidal involving selective TIM inhibition.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 2306-7381
Relation: http://www.mdpi.com/2306-7381/5/3/74; https://doaj.org/toc/2306-7381
DOI: 10.3390/vetsci5030074
Access URL: https://doaj.org/article/b3ba876d496047d1888629821e215b46
Accession Number: edsdoj.b3ba876d496047d1888629821e215b46
Database: Directory of Open Access Journals
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  Data: Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity
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  Data: <searchLink fieldCode="AR" term="%22Luiz+Saramago%22">Luiz Saramago</searchLink><br /><searchLink fieldCode="AR" term="%22Helga+Gomes%22">Helga Gomes</searchLink><br /><searchLink fieldCode="AR" term="%22Elena+Aguilera%22">Elena Aguilera</searchLink><br /><searchLink fieldCode="AR" term="%22Hugo+Cerecetto%22">Hugo Cerecetto</searchLink><br /><searchLink fieldCode="AR" term="%22Mercedes+González%22">Mercedes González</searchLink><br /><searchLink fieldCode="AR" term="%22Mauricio+Cabrera%22">Mauricio Cabrera</searchLink><br /><searchLink fieldCode="AR" term="%22Maria+Fernanda+Alzugaray%22">Maria Fernanda Alzugaray</searchLink><br /><searchLink fieldCode="AR" term="%22Itabajara+da+Silva+Vaz+Junior%22">Itabajara da Silva Vaz Junior</searchLink><br /><searchLink fieldCode="AR" term="%22Rodrigo+Nunes+da+Fonseca%22">Rodrigo Nunes da Fonseca</searchLink><br /><searchLink fieldCode="AR" term="%22Beatriz+Aguirre-López%22">Beatriz Aguirre-López</searchLink><br /><searchLink fieldCode="AR" term="%22Nallely+Cabrera%22">Nallely Cabrera</searchLink><br /><searchLink fieldCode="AR" term="%22Ruy+Pérez-Montfort%22">Ruy Pérez-Montfort</searchLink><br /><searchLink fieldCode="AR" term="%22Alicia+Merlino%22">Alicia Merlino</searchLink><br /><searchLink fieldCode="AR" term="%22Jorge+Moraes%22">Jorge Moraes</searchLink><br /><searchLink fieldCode="AR" term="%22Guzmán+Álvarez%22">Guzmán Álvarez</searchLink>
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  Data: Veterinary Sciences, Vol 5, Iss 3, p 74 (2018)
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  Data: MDPI AG, 2018.
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  Data: LCC:Veterinary medicine
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  Data: <searchLink fieldCode="DE" term="%22triosephosphate+isomerase+inhibitors%22">triosephosphate isomerase inhibitors</searchLink><br /><searchLink fieldCode="DE" term="%22Rhipicephalus+microplus%22">Rhipicephalus microplus</searchLink><br /><searchLink fieldCode="DE" term="%22acaricidal+compounds%22">acaricidal compounds</searchLink><br /><searchLink fieldCode="DE" term="%22Veterinary+medicine%22">Veterinary medicine</searchLink><br /><searchLink fieldCode="DE" term="%22SF600-1100%22">SF600-1100</searchLink>
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  Data: The cattle tick Rhipicephalus microplus is one of the most important ectoparasites causing significant economic losses for the cattle industry. The major tool of control is reducing the number of ticks, applying acaricides in cattle. However, overuse has led to selection of resistant populations of R. microplus to most of these products, some even to more than one active principle. Thus, exploration for new molecules with acaricidal activity in R. microplus has become necessary. Triosephosphate isomerase (TIM) is an essential enzyme in R. microplus metabolism and could be an interesting target for the development of new methods for tick control. In this work, we screened 227 compounds, from our in-house chemo-library, against TIM from R. microplus. Four compounds (50, 98, 14, and 161) selectively inhibited this enzyme with IC50 values between 25 and 50 μM. They were also able to diminish cellular viability of BME26 embryonic cells by more than 50% at 50 μM. A molecular docking study showed that the compounds bind in different regions of the protein; compound 14 interacts with the dimer interface. Furthermore, compound 14 affected the survival of partially engorged females, fed artificially, using the capillary technique. This molecule is simple, easy to produce, and important biological data—including toxicological information—are available for it. Our results imply a promising role for compound 14 as a prototype for development of a new acaricidal involving selective TIM inhibition.
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  Data: http://www.mdpi.com/2306-7381/5/3/74; https://doaj.org/toc/2306-7381
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  Data: 10.3390/vetsci5030074
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        Value: 10.3390/vetsci5030074
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      – Text: English
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        StartPage: 74
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      – SubjectFull: triosephosphate isomerase inhibitors
        Type: general
      – SubjectFull: Rhipicephalus microplus
        Type: general
      – SubjectFull: acaricidal compounds
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      – SubjectFull: Veterinary medicine
        Type: general
      – SubjectFull: SF600-1100
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      – TitleFull: Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity
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