Effect of antibiotic amphotericin b combinations with selected 1,3,4-thiadiazole derivatives on RPTECS in an in vitro model

Abstrakt

4-(5-methyl-1,3,4-thiadiazole-2-yl) benzene-1,3-diol (C1) and 4-[5-(naphthalen-1-ylmethyl)-1,3,4-thiadiazol-2-yl] benzene1,3-diol (NTBD) are representative derivatives of the thiadiazole group, with a high antimycotic potential and minimal toxicity against normal human fibroblast cells. The present study has proved its ability to synergize with the antifungal activity of AmB. The aim of this work was to evaluate the cytotoxic effects of C1 or NTBD, alone or in combination with AmB, on human renal proximal tubule epithelial cells (RPTECs) in vitro. Cell viability was assessed with the MTT assay. Flow cytometry and spectrofluorimetric techniques were used to assess the type of cell death and production of reactive oxygen species (ROS), respectively. The ELISA assay was performed to measure the caspase-2, -3, and -9 activity. ATR-FTIR spectroscopy was used to evaluate biomolecular changes in RPTECs induced by the tested formulas. The combinations of C1/NTBD and AmB did not exert a strong inhibitory effect on the viability/growth of kidney cells, as evidenced by the negligible changes in the apoptotic/necrotic rate and caspase activity, compared to the control cells. Both NTBD and C1 displayed stronger anti-oxidant activity when combined with AmB. The relatively low nephrotoxicity of the thiadiazole derivative combinations and the protective activity against AmB-induced oxidative stress may indicate their potential use in the therapy of fungal infections.

Autorzy

Agnieszka Dróżdż
Agnieszka Dróżdż
Adrianna Sławińska-Brych
Adrianna Sławińska-Brych
Dominika Kubera
Dominika Kubera
Magdalena Kimsa-Dudek
Magdalena Kimsa-Dudek
Jolanta Adamska
Jolanta Adamska
Celina Kruszniewska-Rajs
Celina Kruszniewska-Rajs
Dariusz Karcz
Dariusz Karcz
Wojciech Dąbrowski
Wojciech Dąbrowski
Andrzej Stepulak
Andrzej Stepulak
artykuł
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Angielski
2022
23
23
15260
otwarte czasopismo
CC BY 4.0 Uznanie autorstwa 4.0
ostateczna wersja opublikowana
w momencie opublikowania
2022-12-03
140
5,6
0
1