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Black pepper and piperine reduce cholesterol uptake and enhance translocation of cholesterol transporter proteins

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Abstract

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.

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Acknowledgments

The authors would like to thank Dr. Norman Scholfield for suggestions in preparing the manuscript. This study was financial supported by the National Research Council of Thailand to Naresuan University (RX-AR-032/2552) and the Thailand Research Fund (MRG5180254). The graduate student was supported by the program Strategic Scholarships for Frontier Research Network for the Ph.D. Program Thai Doctoral degree from the Commission on Higher Education, Thailand, and the Center of Excellence for Innovation in Chemistry (PERCH-CIC).

Conflict of interest

All authors declare no conflict of interest in any aspects. All funding agencies supported this works are non-profit organizations. This work has been designed based on scientific judgment of the authors with no potential of influences from outsiders.

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Authors and Affiliations

  1. Department of Pharmacy Practice, Center of Excellence for Innovation in Chemistry, Pharmacological Research Unit, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, 65000, Thailand

    Acharaporn Duangjai, Sakonwun Praputbut & Nanteetip Limpeanchob

  2. School of Medical Sciences, University of Phayao, Phayao, Thailand

    Acharaporn Duangjai

  3. Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand

    Kornkanok Ingkaninan

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  1. Acharaporn Duangjai
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  3. Sakonwun Praputbut
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Correspondence to Nanteetip Limpeanchob.

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Duangjai, A., Ingkaninan, K., Praputbut, S. et al. Black pepper and piperine reduce cholesterol uptake and enhance translocation of cholesterol transporter proteins. J Nat Med 67, 303–310 (2013). https://doi.org/10.1007/s11418-012-0682-7

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  • DOI: https://doi.org/10.1007/s11418-012-0682-7

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