In vitro and in vivo evaluation of the effects of piperine on P-gp function and expression

Toxicology and Applied Pharmacology
Yi HanLee Yong Lim

Abstract

Piperine, a major component of black pepper, is used as spice and nutrient enhancer. The purpose of the present study was to evaluate the effects of acute and prolonged piperine exposure on cellular P-gp expression and function in vitro and in vivo. Piperine at concentrations ranging from 10 to 100 microM, determined by MTT assay to be non-cytotoxic, was observed to inhibit P-gp mediated efflux transport of [(3)H]-digoxin across L-MDR1 and Caco-2 cell monolayers. The acute inhibitory effect was dependent on piperine concentration, with abolishment of [(3)H]-digoxin polarized transport attained at 50 microM of piperine. In contrast, prolonged (48 and 72 h) co-incubation of Caco-2 cell monolayers with piperine (50 and 100 microM) increased P-gp activity through an up-regulation of cellular P-gp protein and MDR1 mRNA levels. The up-regulated protein was functionally active, as demonstrated by a higher degree of [(3)H]-digoxin efflux across the cell monolayers, but the induction was readily reversed by the removal of the spice from the culture medium. Peroral administration of piperine at the dose of 112 microg/kg body weight/day to male Wistar rats for 14 consecutive days also led to increased intestinal P-gp levels. However, ther...Continue Reading

Citations

Jun 19, 2013·Critical Reviews in Food Science and Nutrition·Masood Sadiq ButtWaqas Ahmed
May 3, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xinchi FengXin Di
Mar 26, 2011·Expert Opinion on Drug Metabolism & Toxicology·Hyo-Kyung Han
Jun 24, 2009·Expert Opinion on Drug Metabolism & Toxicology·Wenxia ZhangLee Yong Lim
Dec 2, 2014·Pharmacology & Therapeutics·Renata SilvaFernando Remião
Dec 4, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yu-Jie ZhangHua-Bin Li
Jun 2, 2010·Chemico-biological Interactions·Elisabetta ChieliGabino Garrido
Aug 25, 2015·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Pawin PongkorpsakolChatchai Muanprasat
Jan 3, 2013·The Journal of Pharmacy and Pharmacology·Naphassamon SukhaphiromSuree Jianmongkol
Mar 29, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Daniela Elisabeth EigenmannMouhssin Oufir
Jul 24, 2015·Journal of Pharmaceutical and Biomedical Analysis·Xin DiYouping Liu
Jun 12, 2016·Journal of Pharmaceutical and Biomedical Analysis·Chenrui LiZhong Zuo
Sep 18, 2016·Advanced Drug Delivery Reviews·Yan LiJames W Paxton
Nov 9, 2016·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Suhaili ShamsiLee Yong Lim
Dec 17, 2016·European Journal of Clinical Pharmacology·Satish Kumar Bedada, Praveen Kumar Boga
Jul 4, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Jun-Hui YangBao-Chang Cai
Jan 18, 2018·Journal of Chromatographic Science·Vasanti M Suvarna, Preeti C Sangave
Jun 8, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Saikat DewanjeeMuhammad Zia-Ul-Haq
Feb 8, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Tae Hwan KimBeom Soo Shin
Nov 22, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Tianjing RenZhong Zuo
Dec 19, 2017·Expert Opinion on Drug Metabolism & Toxicology·Sang Hoon LeeHyo-Kyung Han
Oct 1, 2019·Expert Opinion on Drug Metabolism & Toxicology·Tianjing Ren, Zhong Zuo
Sep 25, 2017·Pharmacological Reports : PR·Jin-Ah LeeInwook Choi
Oct 31, 2015·Asian Pacific Journal of Cancer Prevention : APJCP·Muhammad KhanTonghui Ma
Jul 4, 2019·Current Pharmaceutical Design·Katarina SmilkovMustafa Atalay
Jun 7, 2020·Cell Biochemistry and Biophysics·Fisayo OlotuMahmoud E S Soliman
Jan 23, 2021·Pharmaceutics·Maria D AuxteroAna I Fernandes
Feb 14, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Julia QuartiVivian M Rumjanek

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