Abstract
Decreasing circulating low-density lipoprotein (LDL) cholesterol levels leads to decreased risk of cardiovascular diseases. Natural compounds are capable of lowering LDL-cholesterol even on top of lifestyle modification or medication. To identify novel plant-derived compounds to lower plasma LDL cholesterol levels, we performed high-content screening based on the transcriptional activation of the promoter of the LDL receptor (LDLR). The identified hits were thoroughly validated in human hepatic cell lines in terms of increasing LDLR mRNA and protein levels, lowering cellular cholesterol levels and increasing cellular LDL uptake. By means of this incremental validation process in vitro, aqueous extracts prepared from leaves of lingonberries (Vaccinium vitis-idaea) as well as blackberries (Rubus fruticosus) were found to have effects comparable to lovastatin, a prototypic cholesterol-lowering drug. When applied in vivo in mice, both extracts induced subtle increases in hepatic LDLR expression. In addition, a significant increase in high-density lipoprotein (HDL) cholesterol was observed. Taken together, aqueous extracts from lingonberry or blackberry leaves were identified and characterized as strong candidates to provide cardiovascular protection.
Highlights
Cardiovascular diseases including ischemic heart disease and stroke are the major causes of mortality on a global scale.[1]
Plant extracts of interest identified in the screening approach were prepared in-house as follows: Dried leaves of lingonberry (Vaccinium vitis-idaea), dried leaves of blackberry (Rubus fruticosus) and dried agrimony herb (Agrimonia eupatoria) were obtained from a local pharmacy. 90 ml of dH2O were boiled on a heat plate
In order to identify novel plant-based cholesterol-lowering drugs, we established a screening assay based on the measurement of the activity of the LDL receptor (LDLR) promoter
Summary
Cardiovascular diseases including ischemic heart disease and stroke are the major causes of mortality on a global scale.[1] Low-density lipoprotein (LDL) is the main transport vehicle of cholesterol in humans. Desired LDL-cholesterol levels are dependent on the individual’s risk for cardiovascular diseases. For instance, might be advantageous for individuals (i) with borderline LDL-cholesterol levels at low or intermediate cardiovascular risk, who do not qualify for statin treatment; (ii) who are statin-intolerant; and (iii) who fail to achieve desired LDL-cholesterol levels on pharmacological treatment and aim to use natural compounds as adjuvant therapy.[4] the additive effects of several natural compounds on LDL-cholesterol decrease are observed on top of lipid lowering clinical drugs as well as on top of other lifestyle modifications.[5]
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