In vitro assessment for cytotoxicity screening of new antimalarial candidates

Abstract In antimalarial research there are no standard procedures to determine the toxicity of a drug candidate. Among the alternatives available, in vitro cytotoxicity assays are the most widely used to predict toxic effects of future therapeutic products. They have the advantage over the in vivo assays, in that they offer the possibility to restrain the number of experimental variables. The objective of the present study was to compare in vitro cytotoxic methods by testing various compounds currently used to treat malaria against different cell lines. Neutral red (NR) uptake and methylthiazoletetrazolium (MTT) colorimetric in vitro assays were used to determine preliminary toxicity of commercially available antimalarial drugs against tumor and non-tumor cells lines. Toxicity through brine shrimp lethality bioassay and hemolytic activity were also evaluated. Significant differences were observed in the tests measured by NR uptake. The tumor cell lines TOV-21G and HepG2 and non-tumor WI-26VA4 cells showed relatively uniform toxicity results, with TOV-21G being the most sensitive cell tested, presenting the lowest concentration to cause death to 50% of viable cells (CC50) values. The results of this study support the use of TOV-21G, HepG2 and WI-26VA4 cells lines as the choice for cytotoxicity tests to evaluate potential bioactive compounds.

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Main Authors: Espíndola,Mariana Rodrigues, Varotti,Fernando de Pilla, Aguiar,Anna Caroline Campos, Andrade,Silmara Nunes, Rocha,Eliana Maria Mauricio da
Format: Digital revista
Language:English
Published: Universidade de São Paulo, Faculdade de Ciências Farmacêuticas 2022
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100540
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spelling oai:scielo:S1984-825020220001005402022-04-18In vitro assessment for cytotoxicity screening of new antimalarial candidatesEspíndola,Mariana RodriguesVarotti,Fernando de PillaAguiar,Anna Caroline CamposAndrade,Silmara NunesRocha,Eliana Maria Mauricio da Antimalarial Cytotoxicity assay MTT Neutral red Abstract In antimalarial research there are no standard procedures to determine the toxicity of a drug candidate. Among the alternatives available, in vitro cytotoxicity assays are the most widely used to predict toxic effects of future therapeutic products. They have the advantage over the in vivo assays, in that they offer the possibility to restrain the number of experimental variables. The objective of the present study was to compare in vitro cytotoxic methods by testing various compounds currently used to treat malaria against different cell lines. Neutral red (NR) uptake and methylthiazoletetrazolium (MTT) colorimetric in vitro assays were used to determine preliminary toxicity of commercially available antimalarial drugs against tumor and non-tumor cells lines. Toxicity through brine shrimp lethality bioassay and hemolytic activity were also evaluated. Significant differences were observed in the tests measured by NR uptake. The tumor cell lines TOV-21G and HepG2 and non-tumor WI-26VA4 cells showed relatively uniform toxicity results, with TOV-21G being the most sensitive cell tested, presenting the lowest concentration to cause death to 50% of viable cells (CC50) values. The results of this study support the use of TOV-21G, HepG2 and WI-26VA4 cells lines as the choice for cytotoxicity tests to evaluate potential bioactive compounds.info:eu-repo/semantics/openAccessUniversidade de São Paulo, Faculdade de Ciências FarmacêuticasBrazilian Journal of Pharmaceutical Sciences v.58 20222022-01-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100540en10.1590/s2175-97902022e18308
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country Brasil
countrycode BR
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access En linea
databasecode rev-scielo-br
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region America del Sur
libraryname SciELO
language English
format Digital
author Espíndola,Mariana Rodrigues
Varotti,Fernando de Pilla
Aguiar,Anna Caroline Campos
Andrade,Silmara Nunes
Rocha,Eliana Maria Mauricio da
spellingShingle Espíndola,Mariana Rodrigues
Varotti,Fernando de Pilla
Aguiar,Anna Caroline Campos
Andrade,Silmara Nunes
Rocha,Eliana Maria Mauricio da
In vitro assessment for cytotoxicity screening of new antimalarial candidates
author_facet Espíndola,Mariana Rodrigues
Varotti,Fernando de Pilla
Aguiar,Anna Caroline Campos
Andrade,Silmara Nunes
Rocha,Eliana Maria Mauricio da
author_sort Espíndola,Mariana Rodrigues
title In vitro assessment for cytotoxicity screening of new antimalarial candidates
title_short In vitro assessment for cytotoxicity screening of new antimalarial candidates
title_full In vitro assessment for cytotoxicity screening of new antimalarial candidates
title_fullStr In vitro assessment for cytotoxicity screening of new antimalarial candidates
title_full_unstemmed In vitro assessment for cytotoxicity screening of new antimalarial candidates
title_sort in vitro assessment for cytotoxicity screening of new antimalarial candidates
description Abstract In antimalarial research there are no standard procedures to determine the toxicity of a drug candidate. Among the alternatives available, in vitro cytotoxicity assays are the most widely used to predict toxic effects of future therapeutic products. They have the advantage over the in vivo assays, in that they offer the possibility to restrain the number of experimental variables. The objective of the present study was to compare in vitro cytotoxic methods by testing various compounds currently used to treat malaria against different cell lines. Neutral red (NR) uptake and methylthiazoletetrazolium (MTT) colorimetric in vitro assays were used to determine preliminary toxicity of commercially available antimalarial drugs against tumor and non-tumor cells lines. Toxicity through brine shrimp lethality bioassay and hemolytic activity were also evaluated. Significant differences were observed in the tests measured by NR uptake. The tumor cell lines TOV-21G and HepG2 and non-tumor WI-26VA4 cells showed relatively uniform toxicity results, with TOV-21G being the most sensitive cell tested, presenting the lowest concentration to cause death to 50% of viable cells (CC50) values. The results of this study support the use of TOV-21G, HepG2 and WI-26VA4 cells lines as the choice for cytotoxicity tests to evaluate potential bioactive compounds.
publisher Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
publishDate 2022
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100540
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