Naturally Occurring PCSK9 Inhibitors

被引：72
作者：
Adorni, Maria Pia [1 ]
Zimetti, Francesca [2 ]
Lupo, Maria Giovanna [3 ]
Ruscica, Massimiliano [4 ]
Ferri, Nicola [3 ]
机构：
[1] Univ Parma, Dept Med & Surg, Unit Neurosci, I-43125 Parma, Italy
[2] Univ Parma, Dipartimento Sci Alimenti & Farmaco, I-43124 Parma, Italy
[3] Univ Padua, Dipartimento Sci Farmaco, I-35121 Padua, Italy
[4] Univ Milan, Dipartimento Sci Farmacol & Biomol, I-20122 Milan, Italy
来源：
NUTRIENTS | 2020年 / 12卷 / 05期
关键词：
nutraceuticals; PCSK9; SREBP; HNF1; alpha; berberine; cholesterol; KEXIN TYPE 9; DENSITY-LIPOPROTEIN CHOLESTEROL; PRIMARY HUMAN HEPATOCYTES; LDL RECEPTOR EXPRESSION; LUPIN PROTEIN; GREEN TEA; GENE-EXPRESSION; DOWN-REGULATION; HEPG2; CELLS; IN-VITRO;
D O I：
10.3390/nu12051440
中图分类号：
R15 [营养卫生、食品卫生]; TS201 [基础科学];
学科分类号：
100403 ;
摘要：
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.
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页数：30
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