Berberine decreases PCSK9 expression in HepG2 cells

The Epigenetic Drug 5-Azacytidine Interferes with Cholesterol and Lipid Metabolism

“…On the other hand, we noticed that the rapid mRNA turnover of LDLR and, to a lesser extent, of HMGCR was stabilized by the addition of 5-AzaC (Fig. 2C), similar to the effect of berberine, a cholesterol-lowering compound (30). Consequently, in human hepatoma HepG2 and Huh-7 cell lines, LDLR protein was strongly up-regulated by 5-AzaC concomitantly to the reduction of PCSK9 (Fig.…”

FoxO3 Transcription Factor and Sirt6 Deacetylase Regulate Low Density Lipoprotein (LDL)-cholesterol Homeostasis via Control of the Proprotein Convertase Subtilisin/Kexin Type 9 (Pcsk9) Gene Expression

“…PCSK9 gene expression can be induced by insulin and pioglitazone and also can be suppressed by glucagon, bile acids, berberine, fibrate, and oncostatin M (22)(23)(24)(25)(26)(27)(28)(29)(30)(31)(32). PCSK9 protein levels decrease in the course of fasting and increase after feeding (22,27,29,(32)(33)(34).…”

Novel Regulators of Low-Density Lipoprotein Receptor and Circulating LDL-C for the Prevention and Treatment of Coronary Artery Disease

“…However, it was reported that berberine, a natural product, dramatically reduced PCSK9 expression through transcriptional repression (Cameron et al, 2008;Li et al, 2009). While the mechanism is not entirely understood, this observation suggests the possibility that developing small molecule modulators to mediate PCSK9 expression is potentially viable.…”

“…In the clinic, however, the majority of available data point to the fact that fibrates significantly elevate PCSK9 levels in both diabetic and non-diabetic subjects, which possibly attenuates fibrate effects in reducing LDL-C levels (Konrad et al, 2011). Berberine, a compound that reduces LDL-C in humans and is derived from a Chinese herb (Coptis sinensis), dramatically reduces PCSK9 mRNA and protein expression in cultured hepatoma cells (Cameron et al, 2008). PCSK9 is regulated by several hormones.…”