Bergamot (Citrus bergamia) peel extract as new hypocholesterolemic agent modulating PCSK9 expression

Ferrarese, Irene; Lupo, Maria Giovanna; Rossi, Ilaria; Sut, Stefania; Loschi, Francesca; Allegrini, Pietro; Riva, Antonella; Ferri, Nicola; Dall’Acqua, Stefano

doi:10.1016/j.jff.2023.105724

Cited by 3 publications

(3 citation statements)

References 43 publications

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Section: Regulation Of Cholesterol Homeostasismentioning

confidence: 99%

“…The methanol extract (50% methanol) of the bergamot fruit contains several glycosidic and nonglycosidic flavonoids, with naringenin-7- O -rutinoside and apigenin-6,8-C-glucoside exhibiting a greater effect on inducing LDLR expression among the compared compounds. 26 Moreover, bergamot peel extract can reduce PCSK9 and its transcription factor, hepatocyte nuclear factor 1 (HNF1-α), resulting in LDL uptake in Huh7 cell lines. Other flavonoids, such as a major compound isolated from the Gentiana veitchiorum flower, have exhibited an ameliorative effect on the liver by promoting the LDLR-lecithin-cholesterol acyltransferase (LCAT) signaling pathway and, thereby, preventing hepatic oxidative damage.…”

Section: Regulation Of Cholesterol Homeostasismentioning

confidence: 99%

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Exploring Phytochemical Mechanisms in the Prevention of Cholesterol Dysregulation: A Review

Weerawatanakorn,

Kamchonemenukool,

Koh

et al. 2024

J. Agric. Food Chem.

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Although cholesterol plays a key role in many physiological processes, its dysregulation can lead to several metabolic diseases. Statins are a group of drugs widely used to lower cholesterol levels and cardiovascular risk but may lead to several side effects in some patients. Therefore, the development of a plant-based therapeutic adjuvant with cholesterol-lowering activity is desirable. The maintenance of cholesterol homeostasis encompasses multiple steps, including biosynthesis and metabolism, uptake and transport, and bile acid metabolism; issues arising in any of these processes could contribute to the etiology of cholesterolrelated diseases. An increasing body of evidence strongly indicates the benefits of phytochemicals for cholesterol regulation; traditional Chinese medicines prove beneficial in some disease models, although more scientific investigations are needed to confirm their effectiveness. One of the main functions of cholesterol is bile acid biosynthesis, where most bile acids are recycled back to the liver. The composition of bile acid is partly modulated by gut microbes and could be harmful to the liver. In this regard, the reshaping effect of phytochemicals on gut microbiota has been widely reported in the literature for its significance. Therefore, we reviewed studies conducted over the past 5 years elucidating the regulatory effects of phytochemicals or herbal medicines on cholesterol metabolism. In addition, their effects on the recomposition of gut microbiota and bile acid metabolism due to modulation are discussed. This review aims to provide novel insights into the treatment of cholesterol dysregulation and the anticipated development of natural-based compounds in the near and far future.

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Section: Regulation Of Cholesterol Homeostasismentioning

confidence: 99%

Section: Regulation Of Cholesterol Homeostasismentioning

confidence: 99%

Exploring Phytochemical Mechanisms in the Prevention of Cholesterol Dysregulation: A Review

Weerawatanakorn,

Kamchonemenukool,

Koh

et al. 2024

J. Agric. Food Chem.

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“…Нещодавно отримано дані щодо впливу екстракту шкірки бергамоту та окремих його компонентів на рецептор ХС ЛПНЩ та пропротеїн конвертазу субтилізин/кексин типу 9 (PCSK9) [14], що відкриває перспективи можливого його використання в якості допоміжного засобу до медикаментозної ліпідознижувальної терапії.…”

Section: матеріали та методиunclassified

Lipid-lowering Potential of a Complex Dietary Supplement for Cholesterol Control and Vascular Protection

Mishchenko,

Matova

2024

СМ

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The objective: to analyze the lipid-lowering effect of a complex dietary supplement containing red fermented rice extract, bergamot extract and 5-methyltetrahydrofolate in patients with low, moderate and high cardiovascular risk (CVR) or patients who refused to use statins. Materials and methods. The open-label post-marketing study included 60 patients aged 48.1±0.7 years, 54 (90%) persons of whom were women. According to the results of the assessment of total CVR, most patients were in the low/moderate and high risk categories – 47 (78.3%) and 13 (21.7%) individuals, respectively, the last patients refused to use statins. Overweight and obesity were detected in 50% of the study participants – 24 (40%) and 6 (10%) people with degree I obesity, respectively. Arterial hypertension with a grade 1 increase in blood pressure was present in 45% of the study participants (27 persons, all women). Patients were prescribed a complex dietary supplement containing red fermented rice extract, bergamot extract, and 5-methyltetrahydrofolate in clearly defined doses for 3 months. At the screening stage and the final visit all patients underwent a general clinical and laboratory examination. Results. The use of a complex dietary supplement for cholesterol control and vascular protection for 3 months contributed to a decrease in total cholesterol (TC) by 8.1% (p=0.0001), low-density lipoprotein cholesterol (LDL-C) by 14.3% (p=0.0001), non-HDL-C by 12.5% (p=0.0001) and an increase in high-density lipoprotein cholesterol (HDL-C) by 7.1% (p=0.02). In patients with a baseline triglyceride (TG) level (>1.7 mmol/l), a significant reduction of 18.5% (p=0.04) was found, and in patients with signs of systemic inflammation the level of C-reactive protein (CRP) was >3 mg/ml. The use of a dietary supplement helped to reduce CRP by 33.3% (p=0.008). Positive dynamics of the albumin to creatinine ratio in patients with more severe albuminuria was determined. The results of the study indicate that the use of a dietary supplement containing red fermented rice extract, bergamot extract and 5-methyltetrahydrofolate does not affect carbohydrate metabolism and liver function tests. Conclusions. A dietary supplement containing a scientifically based combination of substances of natural origin for the normalization of lipid profile has a positive effect on lipid profile parameters, contributing to a decrease in LDL-C and TG levels in individuals with baseline hypertriglyceridemia and an increase in HDL-C content. The dietary supplement, which contains red fermented rice extract, bergamot extract and 5-methyltetrahydrofolate, improves endothelial function, as evidenced by a decrease in albuminuria and low-grade systemic inflammation in individuals with higher baseline vaules.

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The Evaluation of Citrus bergamia Phytochemicals as Potential Cholesterol-Lowering Agents against HMG-CoA Reductase: An In Silico Molecular Docking Study

Agosto,

Alambatin,

Bacalso

et al. 2024

Iecbm 2024

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Bergamot (Citrus bergamia) peel extract as new hypocholesterolemic agent modulating PCSK9 expression

Cited by 3 publications

References 43 publications

Exploring Phytochemical Mechanisms in the Prevention of Cholesterol Dysregulation: A Review

Exploring Phytochemical Mechanisms in the Prevention of Cholesterol Dysregulation: A Review

Lipid-lowering Potential of a Complex Dietary Supplement for Cholesterol Control and Vascular Protection

The Evaluation of Citrus bergamia Phytochemicals as Potential Cholesterol-Lowering Agents against HMG-CoA Reductase: An In Silico Molecular Docking Study

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