An octimibate derivative, Oxa17, enhances cholesterol efflux and exerts anti-inflammatory and atheroprotective effects in experimental atherosclerosis.
Atherosclerosis
Cholesterol efflux
Inflammation
Liver X receptor
Macrophage
Octimibate derivative
Journal
Biochemical pharmacology
ISSN: 1873-2968
Titre abrégé: Biochem Pharmacol
Pays: England
ID NLM: 0101032
Informations de publication
Date de publication:
06 2021
06 2021
Historique:
received:
25
01
2021
revised:
19
04
2021
accepted:
21
04
2021
pubmed:
26
4
2021
medline:
15
9
2021
entrez:
25
4
2021
Statut:
ppublish
Résumé
Atherosclerotic cardiovascular diseases (ASCVDs), associated with vascular inflammation and lipid dysregulation, are responsible for high morbidity and mortality rates globally. For ASCVD treatment, cholesterol efflux plays an atheroprotective role in ameliorating inflammation and lipid dysregulation. To develop a multidisciplinary agent for promoting cholesterol efflux, octimibate derivatives were screened and investigated for the expression of ATP-binding cassette transporter A1 (ABCA1). Western blotting and qPCR analysis were conducted to determine the molecular mechanism associated with ABCA1 expression in THP-1 macrophages; results revealed that Oxa17, an octimibate derivative, enhanced ABCA1 expression through liver X receptors alpha (LXRα) activation but not through the microRNA pathway. We also investigated the role of Oxa17 in high-fat diet (HFD)-fed mice used as an in vivo atherosclerosis-prone model. In ldlr
Identifiants
pubmed: 33895158
pii: S0006-2952(21)00187-8
doi: 10.1016/j.bcp.2021.114581
pii:
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Imidazoles
0
Cholesterol
97C5T2UQ7J
octimibate
S0SIQ441YZ
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
114581Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.