Hepatocyte nuclear factor 1alpha plays a critical role in PCSK9 gene transcription and regulation by the natural hypocholesterolemic compound berberine - PubMed (original) (raw)

Berberine transcriptionally inhibits PCSK9 while upregulating LDLR mRNA quantity. A, HepG2 cells were exposed to BBR at a concentration of 20 μ

m

for various times. PCSK9, LDLR, and glyceraldehyde-3-phosphate dehydrogenase mRNA levels were quantified by real-time PCR, and mRNA relative levels are presented. Triplicate RNA samples were measured per condition. *, p < 0.05 and ***, p < 0.001 as compared with time 0 h of PCSK9 mRNA level; ###, p < 0.001 as compared with time 0 h of LDLR mRNA level. B, HepG2 cells were treated with indicated doses of BBR in the absence or the presence of 1 μ

m

of fluvastatin (Fluva), lovastatin (Lova), or simvastatin (Simva) for 24 h, and the PCSK9 mRNA abundance was assayed by real-time PCR. *, p < 0.05 and ***, p < 0.001 as compared with control. C, CL26 cells were incubated with BBR at various concentrations for 24 h. D, CL26 cells were incubated with BBR (40 μ

m

) alone or with 1 μ

m

of each statin for 24 h. Luciferase activities are expressed in relative to untreated control cells. Significant differences between control and treatment groups were assessed by one-way analysis of variance with post test of Bonferroni multiple comparison. *, p < 0.05 and ***, p < 0.001 as compared with untreated control. Data shown in A, B, and D are representative of two separate experiments with similar results. Data (mean ± S.D.) in C are derived from four separate assays.