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.

Základní údaje

Originální název

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

Autoři

PRCHALOVA, Eliska, Martina SÚKUPOVÁ (203 Česká republika, domácí), David MALINAK, Rudolf ANDRYS, Ladislav SIVAK, Vladimir PEKARIK, Adam SKARKA, Jana SVOBODOVA, Lukas PRCHAL, Lukas FRESSER, Zbynek HEGER a Kamil MUSILEK

Vydání

Biomedicine and Pharmacotherapy, Elsevier, 2023, 0753-3322

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

10608 Biochemistry and molecular biology

Stát vydavatele

Francie

Utajení

není předmětem státního či obchodního tajemství

Odkazy

Impakt faktor

Impact factor: 7.500 v roce 2022

Kód RIV

RIV/00216224:14310/23:00133317

Organizační jednotka

Přírodovědecká fakulta

UT WoS

001080945900001

Klíčová slova anglicky

Cholinesterase; Organophosphate; Oxime; BODIPY; Reactivation; Encapsulation

Štítky

Příznaky

Mezinárodní význam, Recenzováno
Změněno: 30. 1. 2024 11:54, Mgr. Marie Šípková, DiS.

Anotace

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.