Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid

Title
Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
Authors
이윤석김혜연김영수서재홍노은주Hogyu Han신계정
Keywords
Alzheimer disease; aggregation inhibitor; β-amyloid; bis-styryl aromatic compound
Issue Date
2012-08
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 20, NO 16, 4921-4935
Abstract
Aggregated β-amyloid (Aβ) plays crucial roles in Alzheimer’s disease (AD) pathogenesis, therefore blockade of Aβ aggregation is considered as a potential therapeutic target. We designed and synthesized small molecules to reduce Aβ-induced cytotoxicity by inhibiting Aβ aggregation. The small molecules were screened via ThT, MTT, and cell-based cytotoxicity assay (Aβ burden assay). Selected compounds 1c, 1d, 1e, and 1f were then investigated by evaluating their effects on cognitive impairment of acute AD mice model. Learning and memory dysfunction by injection of Aβ(1–42) was recovered by administration of these molecules. Especially, 1d showed the best recovery activity in Y-maze task, object recognition task, and passive avoidance task with dose dependent manner. These results suggest that 1d has high potential as a therapeutic agent for AD.
URI
http://pubs.kist.re.kr/handle/201004/42900
ISSN
09680896
Appears in Collections:
KIST Publication > Article
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