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

Laxman Pokhrel, Izumi Maezawa, Thi D T Nguyen, Kyeong Ok Chang, Lee-Way Jin, Duy H. Hua

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

A major effort in Alzheimers 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.

Original languageEnglish (US)
Pages (from-to)8969-8973
Number of pages5
JournalJournal of Medicinal Chemistry
Volume55
Issue number20
DOIs
StatePublished - Oct 25 2012

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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