Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
- Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
- 이윤석; 김혜연; 김영수; 서재홍; 노은주; Hogyu Han; 신계정
- Alzheimer disease; aggregation inhibitor; β-amyloid; bis-styryl aromatic compound
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 20, NO 16, 4921-4935
- 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.
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