Inhibition of Acyl-CoA: cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules

Journal of Medicinal Chemistry
Laxman PokhrelDuy H Hua

Abstract

A major effort in Alzheimer's disease therapeutic development has targeted Aβ and downstream events. We have synthesized a small library of tricyclic pyrone compounds. Their protective action in MC65 cells and inhibition of ACAT along with the upregulation of cholesterol transporter gene were investigated. Five active compounds exhibited potencies in the nanomolar ranges. The multiple effects of the compounds on Aβ and cellular cholesterol pathways could be potential mechanisms underlying the protective effects in vivo.

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Citations

Jul 1, 2020·Biopolymers·Chelladurai Karthikeyan BalavigneswaranNira Misra
Jan 3, 2013·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Duy H Hua
May 10, 2017·Journal of Alzheimer's Disease : JAD·Izumi MaezawaLee-Way Jin
Jun 7, 2020·Archives of Biochemistry and Biophysics·Jelena Mustra Rakic, Xiang-Dong Wang

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