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Abstract
Hepatic-related diseases, in particular hyperlipidemia and hypercholesterolemia, are a thorn on the side of the national health institutes around the globe. Indeed, liver lipid and cholesterol dysregulation could lead to atherosclerotic plaque formation and cardiovascular diseases. Currently, statin administration and monacolin K consumption are the main therapies proposed to counter this alarming connection, but relevant side effects are known. To overcome this issue, safe nutraceutical formulations and/or vegetal extracts, endowed with anticholesterolemic activity, could be instrumental in hypercholesterolemia prevention and treatment. In the present work, the anticholesterolemic efficacy of three vegetal extracts used in traditional medicine (artichoke, caigua, and fenugreek), their unique blend (ACFB), and the monacolin K-containing red yeast extract (RYR), was investigated with an in vitro approach based on hepatic cell line HepG2. The impact on cholesterol of the three extracts, their blend, and RYR were investigated by determining hepatocyte total and free cholesterol and bile acids biosynthesis. According to our results, the anticholesterolemic activity of the vegetal extracts was confirmed, and a novel choleretic activity of caigua extract was evidenced. ACFB showed to be safer than RYR while showing a similar effect on total and free cholesterol and bile acids synthesis compared to it. The anticholesterolemic activity of the blend was obtained with lower vegetal extract concentrations compared with the single vegetal extract, potentially indicating an additive effect between the extracts. In conclusion, the vegetal extracts and their blend, ACFB, are safe and are endowed with anticholesterolemic activity, potentially providing complementary therapies to the statin-based ones for hyperlipidemia and hypercholesterolemia-related complications.
Highlights
The liver is considered one of the most active organs in the human body (Ozougwu and Eyo, 2014)
The research for vegetal extracts endowed with anticholesterolemic activity, but without the statin longterm side effects has catalyzed the efforts of nutraceutical and food supplement industries, in particular, toward novel vegetal extracts used in traditional medicine
Our results indicate that ACFB significantly enhances, with a holistic approach, hepatic functionality and cholesterol elimination, by reducing total cholesterol synthesis while improving bile acid and free cholesterol production, as determined by total cholesterol, free cholesterol, and bile acids assays
Summary
The liver is considered one of the most active organs in the human body (Ozougwu and Eyo, 2014). While its consumption is still very limited, recent studies have highlighted its potential use for hypercholesterolemia treatment, since it effectively lowers serum cholesterol level by regulating low- and high-density lipoproteins (LDL and HDL) (Gonzales et al, 1995; Montoro et al, 2001). Of the hepato-specific functions, these cells retain the ability to express the major regulatory enzymes of hepatic, plasma, and biliary cholesterol metabolism and are reported to synthesize and secrete bile acids including chenodeoxycholate and cholate (Everson and Polokoff, 1986). These activities respond in a manner consistent with what is known about human cholesterol metabolism in vivo, at least at a qualitative level. HepG2 has a hepatocyte-like differentiated plasma membrane including a bile canalicular region, closely resembling primary hepatocyte morphology (Geuze et al, 1983)
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