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Review
. 2022 Apr 27;15(5):538.
doi: 10.3390/ph15050538.

A Comprehensive Review of the Cardiovascular Protective Properties of Silibinin/Silymarin: A New Kid on the Block

Nikolaos P E Kadoglou  1 , Chrystalla Panayiotou  1 , Michail Vardas  1 , Nikolaos Balaskas  1 , Nikolaos G Kostomitsopoulos  2 , Alexandra K Tsaroucha  3   4 , Georgia Valsami  5
Affiliations
Review

A Comprehensive Review of the Cardiovascular Protective Properties of Silibinin/Silymarin: A New Kid on the Block

Nikolaos P E Kadoglou et al. Pharmaceuticals (Basel). .

Abstract

Silibinin/silymarin has been used in herbal medicine for thousands of years and it is well-known for its hepato-protective properties. The present comprehensive literature review aimed to critically summarize the pharmacological properties of silymarin extract and its main ingredient silibinin in relation to classical cardiovascular risk factors (e.g., diabetes mellitus, etc.). We also assessed their potential protective and/or therapeutic application in cardiovascular diseases (CVDs), based on experimental and clinical studies. Pre-clinical studies including in vitro tests or animal models have predominantly implicated the following effects of silymarin and its constituents: (1) antioxidant, (2) hypolipidemic, (3) hypoglycemic, (4) anti-hypertensive and (5) cardioprotective. On the other hand, a direct amelioration of atherosclerosis and endothelial dysfunction after silymarin administration seems weak based on scarce data. In clinical trials, the most important findings are improved (1) glycemic and (2) lipid profiles in patients with type 2 diabetes mellitus and/or hyperlipidemia, while (3) the anti-hypertensive effects of silibinin/silymarin seem very modest. Finally, the changes in clinical endpoints are not robust enough to draw a firm conclusion. There are significant limitations in clinical trial design, including the great variety in doses and cohorts, the underlying conditions, the small sample sizes, the short duration and the absence of pharmacokinetic/pharmacodynamic tests prior to study commitment. More data from well-designed and high-quality pre-clinical and clinical studies are required to firmly establish the clinical efficacy of silibinin/silymarin and its possible therapeutic application in cardiovascular diseases.

Keywords: cardiovascular diseases; diabetes mellitus; dyslipidemia; hypertension; silibinin; silymarin.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Schematic representation of the most important cardiovascular protective properties of silymarin extract and its main active constituent silibinin and the related possible mechanism of action. Arrows indicate either increase (↑) or decrease (↓) of the respective biomarker expression. Key: IL: interleukin; TNFa: Tumour necrosis factor-a; NF-κB: nuclear factor kappa-light-chain-enhancer of activated B cells; INFγ: Interferon γ; SOD: superoxide dismutase; MDA: malondialdehyde; GPX: Glutathione peroxidase; GSH: Blood Glutathione; GSSG: oxidized glutathione; GSK-3b: glycogen synthase kinase-3b; HMG-CoA: 3-hydroxy-3-methylglutaryl coenzyme A; ERK1/2: extracellular signal-regulated kinase ½; PTP1B, tyrosine phosphatase 1B; NADPH: nicotinamide adenine dinucleotide phosphate; LDL: low density lipoproteins; ROS: Reactive oxygen species; Nrf2: Nuclear factor E2-related factor 2; PI3K: phosphatidylinositol 3-Kinase; Akt: protein kinase A,B; PEPCK: Phosphoenolpyruvate carboxykinase.
Figure 2
Figure 2
Chemical structures of the main ingredients (flavonoglicans) of Silymarin extract.
See this image and copyright information in PMC

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