Work

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

Year: 2012

Type: article

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.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm3012189

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

Institutions: Kansas State University, University of California Davis Medical Center, UC Davis Health

Language: English

Topic: Alzheimer's disease research and treatments

Subfield: Physiology

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: green