2-Phenylbenzothiazolyl iridium complexes as inhibitors and probes of amyloid ß aggregation.
Dalton Trans
; 53(34): 14258-14264, 2024 Aug 27.
Article
em En
| MEDLINE
| ID: mdl-39129539
ABSTRACT
The aggregation of amyloid ß (Aß) peptides is a significant hallmark of Alzheimer's disease (AD), and the detection of Aß aggregates and the inhibition of their formation are important for the diagnosis and treatment of AD, respectively. Herein, we report a series of benzothiazole-based Ir(III) complexes HN-1 to HN-8 that exhibit appreciable inhibition of Aß aggregation in vitro and in living cells. These Ir(III) complexes can induce a significant fluorescence increase when binding to Aß fibrils and Aß oligomers, while their measured log D values suggest these compounds could have enhanced blood-brain barrier (BBB) permeability. In vivo studies show that HN-1, HN-2, HN-3, and HN-8 successfully penetrate the BBB and stain the amyloid plaques in AD mouse brains after a 10-day treatment, suggesting that these Ir(III) complexes could act as lead compounds for AD therapeutic and diagnostic agent development.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos beta-Amiloides
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Benzotiazóis
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Complexos de Coordenação
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Doença de Alzheimer
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Agregados Proteicos
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Irídio
Limite:
Animals
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Humans
Idioma:
En
Revista:
Dalton Trans
Ano de publicação:
2024
Tipo de documento:
Article