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Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative

P-glycoprotein (P-gp) is known to be involved in multidrug resistance (MDR) and modulation of pharmacokinetic (PK) profiles of substrate drugs. Here, we studied the effects of synthesized ferulic acid (FA) derivatives on P-gp function in vitro and examined PK alteration of paclitaxel (PTX), a well-k...

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Autores principales: Lee, Jaeok, Chae, Song Wha, Ma, LianJi, Lim, So Yeon, Alnajjar, Sarah, Park Choo, Hea-Young, Lee, Hwa Jeong, Rhie, Sandy Jeong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920777/
https://www.ncbi.nlm.nih.gov/pubmed/31717555
http://dx.doi.org/10.3390/pharmaceutics11110593
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author Lee, Jaeok
Chae, Song Wha
Ma, LianJi
Lim, So Yeon
Alnajjar, Sarah
Park Choo, Hea-Young
Lee, Hwa Jeong
Rhie, Sandy Jeong
author_facet Lee, Jaeok
Chae, Song Wha
Ma, LianJi
Lim, So Yeon
Alnajjar, Sarah
Park Choo, Hea-Young
Lee, Hwa Jeong
Rhie, Sandy Jeong
author_sort Lee, Jaeok
collection PubMed
description P-glycoprotein (P-gp) is known to be involved in multidrug resistance (MDR) and modulation of pharmacokinetic (PK) profiles of substrate drugs. Here, we studied the effects of synthesized ferulic acid (FA) derivatives on P-gp function in vitro and examined PK alteration of paclitaxel (PTX), a well-known P-gp substrate drug by the derivative. Compound 5c, the FA derivative chosen as a significant P-gp inhibitor among eight FA candidates by in vitro results, increased PTX AUC(inf) as much as twofold versus the control by reducing PTX elimination in rats. These results suggest that FA derivative can increase PTX bioavailability by inhibiting P-gp existing in eliminating organs.
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spelling pubmed-69207772019-12-24 Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative Lee, Jaeok Chae, Song Wha Ma, LianJi Lim, So Yeon Alnajjar, Sarah Park Choo, Hea-Young Lee, Hwa Jeong Rhie, Sandy Jeong Pharmaceutics Communication P-glycoprotein (P-gp) is known to be involved in multidrug resistance (MDR) and modulation of pharmacokinetic (PK) profiles of substrate drugs. Here, we studied the effects of synthesized ferulic acid (FA) derivatives on P-gp function in vitro and examined PK alteration of paclitaxel (PTX), a well-known P-gp substrate drug by the derivative. Compound 5c, the FA derivative chosen as a significant P-gp inhibitor among eight FA candidates by in vitro results, increased PTX AUC(inf) as much as twofold versus the control by reducing PTX elimination in rats. These results suggest that FA derivative can increase PTX bioavailability by inhibiting P-gp existing in eliminating organs. MDPI 2019-11-09 /pmc/articles/PMC6920777/ /pubmed/31717555 http://dx.doi.org/10.3390/pharmaceutics11110593 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Lee, Jaeok
Chae, Song Wha
Ma, LianJi
Lim, So Yeon
Alnajjar, Sarah
Park Choo, Hea-Young
Lee, Hwa Jeong
Rhie, Sandy Jeong
Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title_full Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title_fullStr Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title_full_unstemmed Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title_short Pharmacokinetic Alteration of Paclitaxel by Ferulic Acid Derivative
title_sort pharmacokinetic alteration of paclitaxel by ferulic acid derivative
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6920777/
https://www.ncbi.nlm.nih.gov/pubmed/31717555
http://dx.doi.org/10.3390/pharmaceutics11110593
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