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.