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Updated: May 4, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Molecular regulation of cholesterol metabolism: HDL-based intervention through drugs and diet
Amit Kumar Rai1, Patrizia Debetto1, Federica Dabbeni Sala1
1Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Largo E. Meneghetti, 2, 35131 Padova, Italy.
Abstract:
The overloading of cholesterol in the arteries remains the principal cause of cardiovascular diseases. Since available anticholesterolemic drugs are not completely effective and have several severe adverse effects, the aim of this review is to analyze current research focused on the emerging, innovative therapeutic strategies based on both pharmacological and nutritional interventions to control cholesterol metabolism. Pharmacological interventions mainly involve the use of molecules capable of interfering with high-density lipoprotien (HDL) metabolism and the reverse cholesterol transport (RCT) through genetic control of apolipoprotein A-I (ApoA-I), agonism at liver X-receptor alpha (LXRalpha), or inhibition of cholesteryl ester transport protein (CETP), scavenger receptor BI(SR-BI), and ecto F0F1ATPase/synthase. Nutritional interventions are based on the use of fibres, phytosterols, and probiotics acting through interference with absorption and reabsorption of cholesterol by enterocyte and hepatocyte specific transporters, thus influencing RCT final step. The search for new drugs is still at the very beginning and new molecules are not yet ready to enter clinical use. However, several promising findings coming from innovative biotechnological research are expected shortly to produce probiotics, fibres, and phytosterols to be used as therapeutic tools. Among the most important advantages of natural products in respect to traditional drugs are the lack of severe adverse effects and their low cost.
Insights
New strategies targeting cholesterol metabolism, including pharmacological and nutritional approaches, show promise for cardiovascular disease treatment. Natural products offer a low-cost, safe alternative to traditional drugs.
Area of Science:
- Cardiovascular Science
- Metabolic Research
- Pharmacology
Background:
- Arterial cholesterol overload is a primary driver of cardiovascular diseases.
- Current anticholesterolemic drugs have limitations in efficacy and adverse effects.
Purpose of the Study:
- To review innovative pharmacological and nutritional strategies for cholesterol metabolism control.
- To analyze emerging therapeutic interventions for cardiovascular disease.
Main Methods:
- Review of current research on pharmacological interventions targeting high-density lipoprotein (HDL) metabolism and reverse cholesterol transport (RCT).
- Analysis of nutritional interventions including fibers, phytosterols, and probiotics influencing cholesterol absorption and RCT.
- Examination of genetic control, receptor agonism, and protein inhibition in pharmacological approaches.
Main Results:
- Pharmacological strategies involve targeting apolipoprotein A-I (ApoA-I), liver X-receptor alpha (LXRalpha), cholesteryl ester transport protein (CETP), scavenger receptor BI (SR-BI), and ecto F0F1ATPase/synthase.
- Nutritional interventions focus on modulating cholesterol absorption and reabsorption via fibers, phytosterols, and probiotics, impacting the final steps of RCT.
- Emerging biotechnological research is yielding promising probiotics, fibers, and phytosterols.
Conclusions:
- Innovative pharmacological and nutritional strategies offer new therapeutic avenues for managing cholesterol metabolism.
- Natural products like probiotics, fibers, and phytosterols present advantages of reduced adverse effects and lower cost compared to traditional drugs.
- While new drug development is ongoing, natural interventions are nearing clinical readiness.
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