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.
摘要：
异甘草素（ISL）是从天然草本甘草中提取的具有查尔酮结构的类黄酮。它的抗炎作用,抗菌，抗氧化剂，和抗癌活性已被广泛研究。此外，ISL还具有降血脂和减少动脉粥样硬化的作用。然而,其降胆固醇机制尚未报道。NiemannPickC1Like1(NPC1L1)是胆固醇摄取的特异性转运体。在这项研究中,我们首次发现,ISL下调NPC1L1的表达,并在体外以浓度依赖的方式与NPC1L1结合,竞争性抑制细胞胆固醇的摄取.本研究为进一步研究其体内降胆固醇作用的分子机制提供了理论依据，并启发了通过NPC1L1抑制降胆固醇的新兴药物研究。
