Regulation of PCSK9 by nutraceuticals
Abstract
PCSK9 (proprotein convertase subtilisin kexin type 9) is a liver secretory enzyme that regulates plasma low-density lipoprotein (LDL) cholesterol (LDL-C) levels through modulation of LDL receptor (LDLR) density on the surface of hepatocytes. Inhibition of PCSK9 using monoclonal antibodies can efficiently lower plasma LDL-C, non-high-density lipoprotein cholesterol and lipoprotein (a). PCSK9 inhibition is also an effective adjunct to statin therapy; however, the cost-effectiveness of currently available PCSK9 inhibitors is under question. Nutraceuticals offer a safe and cost-effective option for PCSK9 inhibition. Several nutraceuticals have been reported to modulate PCSK9 levels and exert LDL-lowering activity. Mechanistically, those nutraceuticals that inhibit PCSK9 through a SREBP (sterol-responsive element binding protein)-independent pathway can be more effective in lowering plasma LDL-C levels compared with those inhibiting PCSK9 through the SREBP pathway. The present review aims to collect available data on the nutraceuticals with PCSK9-inhibitory effect and the underlying mechanisms.
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Berberine, curcumin, polydatin, PUFA-enriched fish oil, DHA-enriched canola oil, and marine n-3 PUFAs have been identified to lower PCSK9 levels.
“Berberine, curcumin, polydatin, PUFA-enriched fish oil, docosahexaenoic acidenriched canola oil, and marine n-3 PUFAs have been identified to lower PCSK9 levels, an important regulator of lipid metabolism and an efficient target for plasma LDL-C reduction (170).”
From The Role of Nutraceuticals in Statin Intolerant Patients (2018) · cites this paper as [170]
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References 195 · Cited by 131
- Authors
- Momtazi, A. A., Banach, M., Pirro, M., Katsiki, N., & Sahebkar, A.
- Affiliations
- Medical University of Lodz (PL)
- University of Perugia (IT)
- Aristotle University of Thessaloniki (GR)
- Mashhad University of Medical Sciences (IR)
- Corresponding author
- Sahebkar, Amirhossein
- Venue
- Pharmacological Research
- Publisher
- Elsevier BV
- Published
- 2017-06
- Volume
- 120
- Pages
- 157-169
- ISSN
- 1043-6618 (ISSN-L)
- OpenAlex
- W2603623680
- Semantic Scholar
- 7589281fff789600a720a9d7e55d2b3435bcd6bc
- Cited by
- 131
- References
- 195
- Citations by year
- 2026: 4 · 2025: 13 · 2024: 16 · 2023: 15 · 2022: 9 · 2021: 13 · 2020: 16 · 2019: 17 · 2018: 22 · 2017: 6
- FWCI
- 3.54
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Pharmacological Research (publishedVersion)
- PubMed (publishedVersion)
- UWA Profiles and Research Repository (UWA) (submittedVersion)
- Topics
- Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Health Sciences › Medicine › Surgery › Natural Products and Biological Research
- Keywords
- PCSK9, nutraceuticals, PCSK9 inhibition, LDL cholesterol, LDL receptor, SREBP pathway, statin therapy, hypercholesterolemia, lipoprotein(a), cost-effectiveness, hepatocytes
- MeSH terms
- Proprotein Convertase 9, PCSK9 Inhibitors, Animals, Anticholesteremic Agents, Enzyme Inhibitors, Humans, Cholesterol, LDL, Signal Transduction, Transcriptional Activation, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Dietary Supplements
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