| PRCHALOVA, Eliska, Martina SÚKUPOVÁ, David MALINAK, Rudolf ANDRYS, Ladislav SIVAK, Vladimir PEKARIK, Adam SKARKA, Jana SVOBODOVA, Lukas PRCHAL, Lukas FRESSER, Zbynek HEGER and Kamil MUSILEK. BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS. Biomedicine and Pharmacotherapy. Elsevier, 2023, vol. 167, November, p. 1-11. ISSN 0753-3322. Available from: https://dx.doi.org/10.1016/j.biopha.2023.115490. |
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@article{2367578,
author = {Prchalova, Eliska and Súkupová, Martina and Malinak, David and Andrys, Rudolf and Sivak, Ladislav and Pekarik, Vladimir and Skarka, Adam and Svobodova, Jana and Prchal, Lukas and Fresser, Lukas and Heger, Zbynek and Musilek, Kamil},
article_number = {November},
doi = {http://dx.doi.org/10.1016/j.biopha.2023.115490},
keywords = {Cholinesterase; Organophosphate; Oxime; BODIPY; Reactivation; Encapsulation},
language = {eng},
issn = {0753-3322},
journal = {Biomedicine and Pharmacotherapy},
title = {BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS},
url = {https://www.sciencedirect.com/science/article/pii/S075333222301288X},
volume = {167},
year = {2023}
}
TY - JOUR
ID - 2367578
AU - Prchalova, Eliska - Súkupová, Martina - Malinak, David - Andrys, Rudolf - Sivak, Ladislav - Pekarik, Vladimir - Skarka, Adam - Svobodova, Jana - Prchal, Lukas - Fresser, Lukas - Heger, Zbynek - Musilek, Kamil
PY - 2023
TI - BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS
JF - Biomedicine and Pharmacotherapy
VL - 167
IS - November
SP - 1-11
EP - 1-11
PB - Elsevier
SN - 07533322
KW - Cholinesterase
KW - Organophosphate
KW - Oxime
KW - BODIPY
KW - Reactivation
KW - Encapsulation
UR - https://www.sciencedirect.com/science/article/pii/S075333222301288X
N2 - The BODIPY-labelled oxime reactivator was prepared and used to study its biodistribution into central nervous system. The newly synthesized oxime was found to be weak inhibitor of acetylcholinesterase and strong inhibitor of butyrylcholinesterase. Its reactivation ability for organophosphate inhibited acetylcholinesterase was found similar to a parent oxime. The BODIPY-labelled oxime was further encapsulated into recombinant human Hferritin and evaluated in vitro and in vivo. The oxime or encapsulated oxime were found to be bioaccumulated primarily in liver and kidneys of mice, but some amount was distributed also to the brain, where it was detectable even after 24 h. The BODIPY-labelled oxime encapsulated to human H-ferritin showed better CNS bioaccumulation and tissue retention at 8 and 24 h time points compared to free oxime, although the fluorescence results might be biased due to BODIPY metabolites identified in tissue homogenates. Taken together, the study demonstrates the first utilization of recombinant ferritins for changing the unfavourable pharmacokinetics of oxime reactivators and brings promising results for follow-up studies.
ER -
PRCHALOVA, Eliska, Martina SÚKUPOVÁ, David MALINAK, Rudolf ANDRYS, Ladislav SIVAK, Vladimir PEKARIK, Adam SKARKA, Jana SVOBODOVA, Lukas PRCHAL, Lukas FRESSER, Zbynek HEGER and Kamil MUSILEK. BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS. \textit{Biomedicine and Pharmacotherapy}. Elsevier, 2023, vol.~167, November, p.~1-11. ISSN~0753-3322. Available from: https://dx.doi.org/10.1016/j.biopha.2023.115490.
|
