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Vet. Sci. 2018, 5(3), 74;

Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity

Laboratório Integrado de Bioquímica Hatisaburo Masuda, NUPEM-Universidade Federal do Rio de Janeiro campus Macaé and Instituto de Bioquímica Médica, Universidade Federal do Rio de Janeiro, Rio de Janeiro 27971-220, Brazil
Grupo de Química Medicinal, Facultad de Ciencias, Universidad de la República, Montevideo 11400, Uruguay
Laboratorio de Moléculas Bioactivas-CENUR Litoral Norte, Universidad de la República, Paysandú 60000, Uruguay
Centro de Biotecnologia and Faculdade de Veterinária, Universidade Federal do Rio Grande do Sul, Porto Alegre 90040-060, Brazil
Instituto Nacional de Ciência e Tecnologia-Entomologia Molecular, Rio de Janeiro 22290-180, Brazil
Departamento de Bioquímica y Biología Estructural, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, CD México 04510, Mexico
Laboratorio de Química Teórica y Computacional, Facultad de Ciencias, Universidad de la República, Montevideo 11400, Uruguay
Authors to whom correspondence should be addressed.
Received: 28 May 2018 / Revised: 14 August 2018 / Accepted: 20 August 2018 / Published: 23 August 2018
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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. View Full-Text
Keywords: triosephosphate isomerase inhibitors; Rhipicephalus microplus; acaricidal compounds triosephosphate isomerase inhibitors; Rhipicephalus microplus; acaricidal compounds

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Saramago, L.; Gomes, H.; Aguilera, E.; Cerecetto, H.; González, M.; Cabrera, M.; Alzugaray, M.F.; da Silva Vaz Junior, I.; Nunes da Fonseca, R.; Aguirre-López, B.; Cabrera, N.; Pérez-Montfort, R.; Merlino, A.; Moraes, J.; Álvarez, G. Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity. Vet. Sci. 2018, 5, 74.

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