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2-Phenylbenzofuran derivatives alleviate mitochondrial damage via the inhibition of β-amyloid aggregation
Authors:Yun Suk Lee  Hye Yun Kim  Hea Mee Youn  Jae Hong Seo  YoungSoo Kim  Kye Jung Shin
Institution:1. Integrated Research Institute of Pharmaceutical Sciences, College of Pharmacy, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon, Gyeonggi-do 420-743, Republic of Korea;2. Korea Institute of Science and Technology, 39-1 Hawolgog-dong, Sungbuk-gu, Seoul 136-791, Republic of Korea
Abstract:To obtain modulators for reducing mitochondrial damage by the inhibition of Aβ oligomer formation, 2-phenylbenzofuran derivatives were designed and prepared. Their inhibitory activity against Aβ fibril formation was screened using ThT fluorescence assay, and the effect of derivatives on mitochondrial function was evaluated using JC-1 and MTT assay. 2-Phenylbenzofuran derivatives with dimethylamino group at p-position had an excellent inhibitory activity against Aβ fibril formation. Particularly, compound 19m alleviated mitochondrial damage remarkably and possessed protective effects against Aβ-induced cytotoxicity.
Keywords:Alzheimer’s disease  2-Phenylbenzofuran  Aβ aggregation inhibitor  Mitochondria
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