Black pepper and piperine reduce cholesterol uptake and enhance translocation of cholesterol transporter proteins.
Black pepper (Piper nigrum L.) lowers blood lipids in vivo and inhibits cholesterol uptake in vitro, and piperine may mediate these effects. To test this, the present study aimed to compare actions of black pepper extract and piperine on (1) cholesterol uptake and efflux in Caco-2 cells, (2) the membrane/cytosol distribution of cholesterol transport proteins in these cells, and (3) the physicochemical properties of cholesterol micelles. Piperine or black pepper extract (containing the same amount of piperine) dose-dependently reduced cholesterol uptake into Caco-2 cells in a similar manner. Both preparations reduced the membrane levels of NPC1L1 and SR-BI proteins but not their overall cellular expression. Micellar cholesterol solubility of lipid micelles was unaffected except by 1 mg/mL concentration of black pepper extract. These data suggest that piperine is the active compound in black pepper and reduces cholesterol uptake by internalizing the cholesterol transporter proteins.
Department of Pharmacy Practice, Center of Excellence for Innovation in Chemistry, Pharmacological Research Unit, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, 65000, Thailand.
Acharaporn
A
Duangjai
Kornkanok
K
Ingkaninan
Sakonwun
S
Praputbut
Nanteetip
N
Limpeanchob
D000470:Alkaloids / Q000494:pharmacology*; D052117:Benzodioxoles / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D002784:Cholesterol / Q000378:metabolism*; D006801:Humans; D008565:Membrane Proteins / Q000378:metabolism; D026901:Membrane Transport Proteins / Q000378:metabolism*; D029222:Piper nigrum / Q000737:chemistry*; D010880:Piperidines / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D053284:Polyunsaturated Alkamides / Q000494:pharmacology*; D021381:Protein Transport / Q000187:drug effects; D051122:Scavenger Receptors, Class B / Q000378:metabolism
D000470:Alkaloids; D052117:Benzodioxoles; D008565:Membrane Proteins; D026901:Membrane Transport Proteins; C410800:NPC1L1 protein, human; D010880:Piperidines; D010936:Plant Extracts; D053284:Polyunsaturated Alkamides; C495124:SCARB1 protein, human; D051122:Scavenger Receptors, Class B; D002784:Cholesterol; C008922:piperine