Frigerio Jessica, Tedesco Erik, Benetti Federico, Insolia Violetta, Nicotra Giovanna, Mezzasalma Valerio, Pagliari Stefania, Labra Massimo, Campone Luca
FEM2-Ambiente, Milano, Italy.
Zooplantlab, Department of Biotechnology and Biosciences, University of Milano-Bicocca, Milano, Italy.
Front Pharmacol. 2021 Nov 23;12:726199. doi: 10.3389/fphar.2021.726199. eCollection 2021.
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 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.
肝脏相关疾病,尤其是高脂血症和高胆固醇血症,是全球各国卫生机构面临的棘手问题。事实上,肝脏脂质和胆固醇失调可能导致动脉粥样硬化斑块形成和心血管疾病。目前,他汀类药物给药和食用莫纳可林K是针对这种令人担忧的关联提出的主要治疗方法,但已知存在相关副作用。为克服这一问题,具有抗胆固醇活性的安全营养制剂和/或植物提取物可能有助于预防和治疗高胆固醇血症。在本研究中,采用基于肝癌细胞系HepG2的方法,研究了三种传统医学中使用的植物提取物(洋蓟、菜瓜和胡芦巴)、它们的独特混合物(ACFB)以及含莫纳可林K的红曲提取物(RYR)的抗胆固醇功效。通过测定肝细胞总胆固醇和游离胆固醇以及胆汁酸生物合成,研究了这三种提取物、它们的混合物和RYR对胆固醇的影响。根据我们的结果,证实了植物提取物的抗胆固醇活性,并证明了菜瓜提取物具有一种新的利胆活性。ACFB显示比RYR更安全,同时在总胆固醇和游离胆固醇以及胆汁酸合成方面与RYR具有相似的效果。与单一植物提取物相比,混合物在较低植物提取物浓度下即可获得抗胆固醇活性,这可能表明提取物之间存在相加作用。总之,植物提取物及其混合物ACFB是安全的,具有抗胆固醇活性,可能为高脂血症和高胆固醇血症相关并发症提供基于他汀类药物的补充疗法。