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Structure-Activity Relationship (SAR) and in vitro Predictions of Mutagenic and Carcinogenic Activities of Ixodicidal Ethyl-Carbamates
Joint Authors
Angeles, Enrique
Prado-Ochoa, María G.
Strassburger-Madrigal, Maribel
Espinosa-Aguirre, Jesús J.
Velázquez-Sánchez, Ana M.
Vázquez-Valadez, Victor H.
Muñoz-Guzmán, Marco A.
Alba-Hurtado, Fernando
Camacho-Carranza, Rafael
Source
Issue
Vol. 2020, Issue 2020 (31 Dec. 2020), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2020-11-21
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
Ethyl-4-bromophenyl-carbamate (LQM 919) and Ethyl-4-chlorophenyl-carbamate (LQM 996) are compounds that inhibit egg-laying and hatching of tick larvae that are resistant to conventional ixodicides.
The structure-activity relationship (SAR) to get the endpoint predictions of mutagenicity and carcinogenicity of the LQM 919 and LQM 996 was performed and the absence of mutagenicity was confirmed by Ames test.
SAR analysis show no structural alerts indicating the ability of ethyl-carbamates to bind biomolecules or estrogen receptors.
Endpoint of mutagenicity with and without metabolic activation showed that the ethyl-carbamates were negative (p <0.05) for mutagenicity induction in strains TA97, TA98, TA102, TA1535, TA1537 and TA1538 of Salmonella typhimurium.
Pre-incubation with different ethyl-carbamate concentrations did not increase the number of spontaneously reverting colonies; moreover, the compounds did not induce a concentration-dependent increase in the number of reverting colonies in any of the strains used.
This confirmed the absence of mutagenic activity in this test system.
Exogenous metabolic activation did not modify these observations; suggesting that no metabolites with mutagenic activity were present.
The endpoint of carcinogenicity in rats were negative for LQM 919 (p <0.05,) and LQM 996 (p <0.001).
The results of the present study strongly suggest that ethyl-carbamates do not represent a risk for cancer in mammals.
American Psychological Association (APA)
Prado-Ochoa, María G.& Strassburger-Madrigal, Maribel& Camacho-Carranza, Rafael& Espinosa-Aguirre, Jesús J.& Velázquez-Sánchez, Ana M.& Vázquez-Valadez, Victor H.…[et al.]. 2020. Structure-Activity Relationship (SAR) and in vitro Predictions of Mutagenic and Carcinogenic Activities of Ixodicidal Ethyl-Carbamates. BioMed Research International،Vol. 2020, no. 2020, pp.1-8.
https://search.emarefa.net/detail/BIM-1132882
Modern Language Association (MLA)
Prado-Ochoa, María G.…[et al.]. Structure-Activity Relationship (SAR) and in vitro Predictions of Mutagenic and Carcinogenic Activities of Ixodicidal Ethyl-Carbamates. BioMed Research International No. 2020 (2020), pp.1-8.
https://search.emarefa.net/detail/BIM-1132882
American Medical Association (AMA)
Prado-Ochoa, María G.& Strassburger-Madrigal, Maribel& Camacho-Carranza, Rafael& Espinosa-Aguirre, Jesús J.& Velázquez-Sánchez, Ana M.& Vázquez-Valadez, Victor H.…[et al.]. Structure-Activity Relationship (SAR) and in vitro Predictions of Mutagenic and Carcinogenic Activities of Ixodicidal Ethyl-Carbamates. BioMed Research International. 2020. Vol. 2020, no. 2020, pp.1-8.
https://search.emarefa.net/detail/BIM-1132882
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1132882