Inhibitory Effect of Isoliquiritigenin in Niemann-Pick C1-Like 1-Mediated Cholesterol Uptake.

Content Provider	Europe PMC
Author	Zeng, Jun Liu, Wenjing Liang, Bing Shi, Lingyu Yang, Shanbo Meng, Jingsen Chang, Jing Hu, Xiaokun Zhang, Renshuai Xing, Dongming
Editor	Lin, Ligen Gan, Lishe Christensen, Lars Porskjær
Copyright Year	2022
Abstract	Isoliquiritigenin (ISL) is a flavonoid with a chalcone structure extracted from the natural herb Glycyrrhiza glabra. Its anti-inflammatory, antibacterial, antioxidant, and anticancer activities have been extensively studied. Moreover, ISL also possess hypolipidemic and atherosclerosis-reducing effects. However, its cholesterol-lowering mechanisms have not been reported yet. Niemann Pick C1 Like 1 (NPC1L1) is a specific transporter of cholesterol uptake. In this study, we found for the first time that ISL downregulates NPC1L1 expression and competitively inhibits cellular cholesterol uptake by binding to NPC1L1 in a concentration-dependent manner in vitro. This study provides a theoretical basis for further investigation of the molecular mechanisms of its cholesterol-lowering effect in vivo and inspired emerging drug research for cholesterol-lowering purposes through NPC1L1 inhibition.
Journal	Molecules
Volume Number	27
DOI	10.3390/molecules27217494
PubMed Central reference number	PMC9654431
Issue Number	21
PubMed reference number	36364321
e-ISSN	14203049
Language	English
Publisher	Molecular Diversity Preservation International (MDPI)
Publisher Date	2022-11-03
Access Restriction	Open
Subject Keyword	Niemann-Pick C1-Like 1 (NPC1L1) inhibitors isoliquiritigenin cholesterol uptake cardiovascular disease
Content Type	Text
Resource Type	Article
Subject	Physical and Theoretical Chemistry Medicine Chemistry Drug Discovery Pharmaceutical Science Analytical Chemistry Molecular Medicine Organic Chemistry