Discovery of Flavonoids from Scutellaria baicalensis with Inhibitory Activity Against PCSK 9 Expression: Isolation, Synthesis and Their Biological Evaluation.

Nine flavonoids were isolated and identified from a chloroform-soluble fraction of the roots of through a bioactivity-guided fractionation using a proprotein convertase subtilisin/kexin type 9 (PCSK9) monitoring assay in HepG2 cells. All structures were established by interpreting the corresponding spectroscopic data and comparing measured values from those in the literature. All compounds were assessed for their ability to inhibit PCSK9 mRNA expression; compounds (3,7,2'-trihydroxy-5-methoxy-flavanone) and (skullcapflavone II) were found to suppress PCSK9 mRNA via SREBP-1. Furthermore, compound was found to increase low-density lipoprotein receptor protein expression. Also, synthesis of compound as a racemic mixture form () was completed for the first time. Natural compound and synthetic racemic were evaluated for their inhibitory activities against PCSK9 mRNA expression and the results confirmed the stereochemistry of was important.