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Polyfunctionalized α-phenyl-tert-butyl(benzyl)nitrones : multifunctional antioxidants for stroke treatment
ID
Diez-Iriepa, Daniel
(
Avtor
),
ID
Knez, Damijan
(
Avtor
),
ID
Gobec, Stanislav
(
Avtor
),
ID
Iriepa, Isabel
(
Avtor
),
ID
de los Ríos, Cristóbal
(
Avtor
),
ID
Bravo, Isaac
(
Avtor
),
ID
López-Muñoz, Francisco
(
Avtor
),
ID
Marco-Contelles, José
(
Avtor
),
ID
Hadjipavlou-Litina, Dimitra
(
Avtor
)
URL - Izvorni URL, za dostop obiščite
https://www.mdpi.com/2076-3921/11/9/1735
PDF - Predstavitvena datoteka,
prenos
(2,12 MB)
MD5: C64216B59CE76F4B43F6B07297438AE4
Galerija slik
Izvleček
Nowadays, most stroke patients are treated exclusively with recombinant tissue plasminogen activator, a drug with serious side effects and limited therapeutic window. For this reason, and because of the known effects of oxidative stress on stroke, a more tolerable and efficient therapy for stroke is being sought that focuses on the control and scavenging of highly toxic reactive oxygen species by appropriate small molecules, such as nitrones with antioxidant properties. In this context, herein we report here the synthesis, antioxidant, and neuroprotective properties of twelve novel polyfunctionalized α-phenyl-tert-butyl(benzyl)nitrones. The antioxidant capacity of these nitrones was investigated by various assays, including the inhibition of lipid peroxidation induced by AAPH, hydroxyl radical scavenging assay, ABTS+-decoloration assay, DPPH scavenging assay, and inhibition of soybean lipoxygenase. The inhibitory effect on monoamine oxidases and cholinesterases and inhibition of β-amyloid aggregation were also investigated. As a result, (Z)-N-benzyl-1-(2-(3-(piperidin-1-yl)propoxy)phenyl)methanimine oxide (5) was found to be one of the most potent antioxidants, with high ABTS+ scavenging activity (19%), and potent lipoxygenase inhibitory capacity (IC50 = 10 µM), selectively inhibiting butyrylcholinesterase (IC50 = 3.46 ± 0.27 µM), and exhibited neuroprotective profile against the neurotoxicant okadaic acid in a neuronal damage model. Overall, these results pave the way for the further in-depth analysis of the neuroprotection of nitrone 5 in in vitro and in vivo models of stroke and possibly other neurodegenerative diseases in which oxidative stress is identified as a critical player.
Jezik:
Angleški jezik
Ključne besede:
butyrylcholinesterase
,
free radical scavengers
,
neuroprotection
,
α-phenyl-tert-butyl(benzyl)nitrones
,
in vitro digestion
,
extractable and bound phenolics
Tipologija:
1.01 - Izvirni znanstveni članek
Organizacija:
FFA - Fakulteta za farmacijo
Status publikacije:
Objavljeno
Različica publikacije:
Objavljena publikacija
Datum objave:
31.08.2022
Leto izida:
2022
Št. strani:
20 str., art. 1735
Številčenje:
Vol. 11, Iss. 9
PID:
20.500.12556/RUL-139371
UDK:
612.015:616.127-005.8
ISSN pri članku:
2076-3921
DOI:
10.3390/antiox11091735
COBISS.SI-ID:
119819011
Datum objave v RUL:
01.09.2022
Število ogledov:
518
Število prenosov:
71
Metapodatki:
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Objavi na:
Gradivo je del revije
Naslov:
Antioxidants
Skrajšan naslov:
Antioxidants
Založnik:
MDPI
ISSN:
2076-3921
COBISS.SI-ID:
522976025
Licence
Licenca:
CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
Povezava:
http://creativecommons.org/licenses/by/4.0/deed.sl
Opis:
To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.
Začetek licenciranja:
01.09.2022
Sekundarni jezik
Jezik:
Slovenski jezik
Ključne besede:
antioksidanti
,
butirilholinesteraza
,
lovilci prostih radikalov
,
nevroprotekcija
,
α-fenil-terc-butil(benzil)nitroni
,
oksidativni stres
Projekti
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P1-0208-2022
Naslov:
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Spanish Ministerio de Economía y Competividad, Ramón y Cajal
Številka projekta:
SAF2015-65586-R
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