BODIPY-labelled acetylcholinesterase reactivators can be
encapsulated into ferritin nanovehicles for enhanced
bioavailability in the CNS

J 2023

BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS

PRCHALOVA, Eliska, Martina SÚKUPOVÁ, David MALINAK, Rudolf ANDRYS, Ladislav SIVAK et. al.

Basic information

Original name

BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS

Authors

PRCHALOVA, Eliska, Martina SÚKUPOVÁ (203 Czech Republic, belonging to the institution), David MALINAK, Rudolf ANDRYS, Ladislav SIVAK, Vladimir PEKARIK, Adam SKARKA, Jana SVOBODOVA, Lukas PRCHAL, Lukas FRESSER, Zbynek HEGER and Kamil MUSILEK

Edition

Biomedicine and Pharmacotherapy, Elsevier, 2023, 0753-3322

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

10608 Biochemistry and molecular biology

Country of publisher

France

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

Impact factor

Impact factor: 7.500 in 2022

RIV identification code

RIV/00216224:14310/23:00133317

Organization unit

Faculty of Science

DOI

http://dx.doi.org/10.1016/j.biopha.2023.115490

UT WoS

001080945900001

Keywords in English

Cholinesterase; Organophosphate; Oxime; BODIPY; Reactivation; Encapsulation

Abstract

V originále

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.

Citovat

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.

@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.

Detailed Information on Publication Record