TY - JOUR
T1 - Effect of 4-amino-3-nitrobenzoic acid on the expression level of the trans-sialidase gene in Trypanosoma cruzi epimastigotes
AU - Vazquez-Jimenez, Lenci K.
AU - Paz-Gonzalez, Alma D.
AU - Kashif, Muhammad
AU - Juarez-Rendon, Karina J.
AU - Nogueda-Torres, Benjamín
AU - Bocanegra-Garcia, Virgilio
AU - Rivera, Gildardo
N1 - Publisher Copyright:
© 2019 Pakistan Journal of Pharmaceutical Sciences. All rights reserved.
PY - 2019
Y1 - 2019
N2 - Trans-sialidase of Trypanosoma cruzi (TcTS) is a key enzyme in the infection process from parasite to host; therefore, it has been considered an important target for developing new anti-Chagas drugs. Different compounds with trypanocidal activity and/or inhibition of TcTS have been reported; however, some benzoic acid derivatives have shown high enzymatic inhibition but low trypanocidal activity and viceversa. These results show that each compound may possess a different mechanism of action. Based on the above, the compound 4-amino-3-nitrobenzoic acid (16), a potent TcTS inhibitor (77% inhibition in enzymatic assays) was selected to evaluate its effects on the expression level of the TS gene in T. cruzi epimastigotes and determine its involvement in the mechanism of action. Results showed an increase in the expression level of the TcTS gene, which confirmed that compound 16, has a direct effect on TcTS.
AB - Trans-sialidase of Trypanosoma cruzi (TcTS) is a key enzyme in the infection process from parasite to host; therefore, it has been considered an important target for developing new anti-Chagas drugs. Different compounds with trypanocidal activity and/or inhibition of TcTS have been reported; however, some benzoic acid derivatives have shown high enzymatic inhibition but low trypanocidal activity and viceversa. These results show that each compound may possess a different mechanism of action. Based on the above, the compound 4-amino-3-nitrobenzoic acid (16), a potent TcTS inhibitor (77% inhibition in enzymatic assays) was selected to evaluate its effects on the expression level of the TS gene in T. cruzi epimastigotes and determine its involvement in the mechanism of action. Results showed an increase in the expression level of the TcTS gene, which confirmed that compound 16, has a direct effect on TcTS.
KW - Benzoic acid
KW - Chagas disease
KW - Trans-sialidase
KW - Trypanosoma cruzi
UR - http://www.scopus.com/inward/record.url?scp=85066404762&partnerID=8YFLogxK
M3 - Artículo
C2 - 31103978
AN - SCOPUS:85066404762
SN - 1011-601X
VL - 32
SP - 825
EP - 829
JO - Pakistan journal of pharmaceutical sciences
JF - Pakistan journal of pharmaceutical sciences
IS - 2
ER -