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@article{1775941,
author = {Jakubek, Milan and Masařík, Michal and Briza, Tomas and Kaplanek, Robert and Vesela, Katerina and Abramenko, Nikita and Martasek, Pavel},
article_location = {Basel},
article_number = {2},
doi = {http://dx.doi.org/10.3390/pr9020383},
keywords = {protoporphyrinogen oxidase; inhibitors; herbicides},
language = {eng},
issn = {2227-9717},
journal = {Processes},
title = {PPO-Inhibiting Herbicides and Structurally Relevant Schiff Bases: Evaluation of Inhibitory Activities against Human Protoporphyrinogen Oxidase},
url = {https://www.mdpi.com/2227-9717/9/2/383},
volume = {9},
year = {2021}
}
TY - JOUR
ID - 1775941
AU - Jakubek, Milan - Masařík, Michal - Briza, Tomas - Kaplanek, Robert - Vesela, Katerina - Abramenko, Nikita - Martasek, Pavel
PY - 2021
TI - PPO-Inhibiting Herbicides and Structurally Relevant Schiff Bases: Evaluation of Inhibitory Activities against Human Protoporphyrinogen Oxidase
JF - Processes
VL - 9
IS - 2
SP - 1-16
EP - 1-16
PB - MDPI
SN - 22279717
KW - protoporphyrinogen oxidase
KW - inhibitors
KW - herbicides
UR - https://www.mdpi.com/2227-9717/9/2/383
N2 - The study of human protoporphyrinogen oxidase (hPPO) inhibition can contribute significantly to a better understanding of some pathogeneses (e.g., porphyria, herbicide exposure) and the development of anticancer agents. Therefore, we prepared new potential inhibitors with Schiff base structural motifs (2-hydroxybenzaldehyde-based Schiff bases 9-13 and chromanone derivatives 17-19) as structurally relevant to PPO herbicides. The inhibitory activities (represented by the half maximal inhibitory concentration (IC50) values) and enzymatic interactions (represented by the hPPO melting temperatures) of these synthetic compounds and commercial PPO herbicides used against hPPO were studied by a protoporphyrin IX fluorescence assay. In the case of PPO herbicides, significant hPPO inhibition and changes in melting temperature were observed for oxyfluorten, oxadiazon, lactofen, butafenacil, saflufenacil, oxadiargyl, chlornitrofen, and especially fomesafen. Nevertheless, the prepared compounds did not display significant inhibitory activity or changes in the hPPO melting temperature. However, a designed model of hPPO inhibitors based on the determined IC50 values and a docking study (by using AutoDock) found important parts of the herbicide structural motif for hPPO inhibition. This model could be used to better predict PPO herbicidal toxicity and improve the design of synthetic inhibitors.
ER -
JAKUBEK, Milan, Michal MASAŘÍK, Tomas BRIZA, Robert KAPLANEK, Katerina VESELA, Nikita ABRAMENKO a Pavel MARTASEK. PPO-Inhibiting Herbicides and Structurally Relevant Schiff Bases: Evaluation of Inhibitory Activities against Human Protoporphyrinogen Oxidase. \textit{Processes}. Basel: MDPI, 2021, roč.~9, č.~2, s.~1-16. ISSN~2227-9717. Dostupné z: https://dx.doi.org/10.3390/pr9020383.
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