A comprehensive assessment of palmatine as anticonvulsant agent - In vivo and in silico studies

Abstrakt

Previously, we demonstrated that palmatine (PALM) – an isoquinoline alkaloid from Berberis sibrica radix, exerted antiseizure activity in the pentylenetetrazole (PTZ)-induced seizure assay in larval zebrafish. The aim of the present study was to more precisely characterize PALM as a potential anticonvulsant drug candidate. A range of zebrafish and mouse seizure/epilepsy models were applied in the investigation. Immunostaining analysis was conducted to assess the changes in mouse brains, while in silico molecular modelling was performed to determine potential targets for PALM. Accordingly, PALM had anticonvulsant effect in ethyl 2-ketopent-4-enoate (EKP)-induced seizure assay in zebrafish larvae as well as in the 6 Hz-induced psychomotor seizure threshold and timed infusion PTZ tests in mice. The protective effect in the EKP-induced seizure assay was confirmed in the local field potential recordings. PALM did not affect seizures in the gabra1a knockout line of zebrafish larvae. In the scn1Lab-/- zebrafish line, pretreatment with PALM potentiated seizure-like behaviour of larvae. Repetitive treatment with PALM, however, did not reduce development of PTZ-induced seizure activity nor prevent the loss of parvalbumin-interneurons in the hippocampus of the PTZ kindled mice. In silico molecular modelling revealed that the noted anticonvulsant effect of PALM in EKP-induced seizure assay might result from its interactions with glutamic acid decarboxylase and/or via AMPA receptor non-competitive antagonism. Our study has demonstrated the anticonvulsant activity of PALM in some experimental models of seizures, including a model of pharmacoresistant seizures induced by EKP. These results indicate that PALM might be a suitable new drug candidate but the precise mechanism of its anticonvulsant activity has to be determined.

Autorzy

Nieoczym Dorota
Nieoczym Dorota
Marszałek-Grabska Marta
Marszałek-Grabska Marta
Kundap Uday
Kundap Uday
Kaczor Agnieszka A.
Kaczor Agnieszka A.
Wróbel Tomasz M.
Wróbel Tomasz M.
Kosheva Natalia
Kosheva Natalia
Abram Michał
Abram Michał
Esquerra Camila V.
Esquerra Camila V.
Samarut Eric
Samarut Eric
Pieróg Mateusz
Pieróg Mateusz
Jakubiec Marcin
Jakubiec Marcin
Kamiński Krzysztof
Kamiński Krzysztof
Gaweł Kinga
Gaweł Kinga
artykuł
BIOMEDICINE & PHARMACOTHERAPY
Angielski
2024
172
116234
otwarte czasopismo
CC BY-NC-ND Uznanie autorstwa-Użycie niekomercyjne-Bez utworów zależnych 4.0
ostateczna wersja opublikowana
w momencie opublikowania
2024-02-06
100
6,9
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