College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, 08826, Republic of Korea.
College of Pharmacy and Integrated Research Institute for Drug Development, Dongguk University-Seoul, Gyeonggi-do, 10326, Republic of Korea.
Phytochemistry. 2022 Jan;193:112980. doi: 10.1016/j.phytochem.2021.112980. Epub 2021 Oct 12.
Three acylated saponins and three flavonoid glycosides, along with nine known flavonoids, were isolated from the fruits of Stewartia koreana Nakai ex Rehder (Theaceae) using relative mass defect filtering analysis. The structures of these compounds were determined by performing spectroscopic analyses and using chemical methods. Furthermore, all the isolates were evaluated for their effects on the mRNA expression of the genes for proprotein convertase subtilisin/kexin type 9 (PCSK9) and low-density lipoprotein receptor (LDLR) as well as their inhibitory activities on PCSK9 and LDLR binding. None of the isolates was deemed to be active in PCSK9-LDLR binding inhibition. However, (+)-catechin was found to inhibit PCSK9 expression and increase LDLR expression, suggesting the potential of (+)-catechin to lower cholesterol level via the downregulation of PCSK9 expression.
从朝鲜稠李（Theaceae）的果实中，利用相对质量缺陷过滤分析，分离得到三种酰化皂素和三种黄酮苷，以及九种已知的黄酮类化合物。通过光谱分析和化学方法确定了这些化合物的结构。此外，还评估了所有分离物对前蛋白转化酶枯草溶菌素/克酶 9（PCSK9）和低密度脂蛋白受体（LDLR）基因的 mRNA 表达的影响，以及它们对 PCSK9 和 LDLR 结合的抑制活性。没有一种分离物被认为对 PCSK9-LDLR 结合抑制有活性。然而，（+）-儿茶素被发现可以抑制 PCSK9 的表达并增加 LDLR 的表达，这表明（+）-儿茶素通过下调 PCSK9 的表达降低胆固醇水平的潜力。
