Effect of Citrus bergamia extract on lipid profile: A combined in vitro and human study

Abstract

With the aim of characterising the hypo‐lipidemic function of the Brumex™ ingredient obtained from the whole fruit of Citrus bergamia, a combined pre‐clinical and clinical study was conducted. In the HepG2 experimental model, we first demonstrated that Brumex™ does not trigger any significant alteration in cell viability over the tested concentration range of 1–2000 μg/mL (4 and 24 h). By stimulating the phosphorylation of AMP‐activated protein kinase (AMPK) at threonine 172, Brumex™ significantly reduces both cholesterol and triglyceride (TG) intracellular content of HepG2 cells and impairs the expression levels of lipid synthesis‐related genes (namely, SREBF1c, SREBF2, ACACA, SCD1, HMGCR and FASN). In vitro data have been validated in a dedicated double‐blind, placebo‐controlled, randomised clinical trial performed in 50 healthy moderately hyper‐cholesterolemic subjects, undergoing supplementation with either Brumex™ (400 mg) or placebo for 12 weeks. Clinical and blood laboratory data were evaluated at the baseline and at the end of the trial. Brumex™ positively impacted on both plasma lipid pattern and liver enzymes compared with the placebo, mainly in terms of significant reduction of total cholesterol (TC), TG, low‐density lipoprotein‐cholesterol (LDL‐C), non‐high‐density lipoprotein‐cholesterol (non‐HDL‐C), apolipoprotein B100 (ApoB), fasting plasma glucose (FPG), glutamic‐oxaloacetic transaminase (GOT), glutamate pyruvate transaminase (GPT) and gamma‐glutamyl‐transferase (gGT).