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Review
. 2020 May 16;12(5):1440.
doi: 10.3390/nu12051440.

Naturally Occurring PCSK9 Inhibitors

Maria Pia Adorni  1 , Francesca Zimetti  2 , Maria Giovanna Lupo  3 , Massimiliano Ruscica  4 , Nicola Ferri  3
Affiliations
Free PMC article
Review

Naturally Occurring PCSK9 Inhibitors

Maria Pia Adorni et al. Nutrients. .
Free PMC article

Abstract

Genetic, epidemiological and pharmacological data have led to the conclusion that antagonizing or inhibiting Proprotein convertase subtilisin/kexin type 9 (PCSK9) reduces cardiovascular events. This clinical outcome is mainly related to the pivotal role of PCSK9 in controlling low-density lipoprotein (LDL) cholesterol levels. The absence of oral and affordable anti-PCSK9 medications has limited the beneficial effects of this new therapeutic option. A possible breakthrough in this field may come from the discovery of new naturally occurring PCSK9 inhibitors as a starting point for the development of oral, small molecules, to be used in combination with statins in order to increase the percentage of patients reaching their LDL-cholesterol target levels. In the present review, we have summarized the current knowledge on natural compounds or extracts that have shown an inhibitory effect on PCSK9, either in experimental or clinical settings. When available, the pharmacodynamic and pharmacokinetic profiles of the listed compounds are described.

Keywords: HNF1α; PCSK9; SREBP; berberine; cholesterol; nutraceuticals.

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Conflict of interest statement

F.Z.; M.P.A.; M.G.L. and M.R. declare no conflict of interest. N.F. has received a financial grant from PharmaNutra S.P.A.

Figures

Figure 1
Figure 1
Schematic representation of the to-date-known mechanism of action of natural Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors.
See this image and copyright information in PMC

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