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Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats

The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in humanidad. As an artificial synthetic piperine analog, silepcimide (ILE) has significant...

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Autores principales: Wang, Peijian, Li, Hui, Lin, Zhexuan, Luo, Hongjun, Luo, Wenhong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8586700/
https://www.ncbi.nlm.nih.gov/pubmed/34776952
http://dx.doi.org/10.3389/fphar.2021.725362
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author Wang, Peijian
Li, Hui
Lin, Zhexuan
Luo, Hongjun
Luo, Wenhong
author_facet Wang, Peijian
Li, Hui
Lin, Zhexuan
Luo, Hongjun
Luo, Wenhong
author_sort Wang, Peijian
collection PubMed
description The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in humanidad. As an artificial synthetic piperine analog, silepcimide (ILE) has significant advantages because of the low price and simple synthesis process. In this study, a simple and rapid HPLC-UV method was developed for determination of the plasma concentration of CUR, PIP,ILE and dihydrocurcumin (DHC, a metabolite of CUR) simultaneously. Meanwhile, the effects of PIP and ILE on the plasma concentration and pharmacokinetics of DHC in SD rats was studied to explore whether ILE could serve as a CUR bioavailability enhancer. The metabolic pathway of CUR was studied by comparing the differences of CUR plasma concentration between intravenous injection and oral administration over the same time period, and reacting with small intestine homogenate without microbes of SD rats. The results of drug-time curve showed that combined administration of ILE and CUR had significant effect on plasma concentrations of DHC. Repeated administration of PIP or ILE could significantly increase the plasma concentration of DHC. Plasma CUR could be detected in the samples of from intravenous injection of CUR rats, whereas, it couldn’t be detected in the plasma sample form oral administration rats. CUR incubated with intestinal homogenate without intestinal bacteria could not be transformed into DHC. In conclusion, our results show that ILE can improve the bioavailability of CUR. Additionally, it was inferred that most of the CUR was reduced to DHC by NADPH when it was absorbed from gastrointestinal tract, and our results demonstrated that this pathway might be mediated by gastrointestinal microorganisms.
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spelling pubmed-85867002021-11-13 Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats Wang, Peijian Li, Hui Lin, Zhexuan Luo, Hongjun Luo, Wenhong Front Pharmacol Pharmacology The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in humanidad. As an artificial synthetic piperine analog, silepcimide (ILE) has significant advantages because of the low price and simple synthesis process. In this study, a simple and rapid HPLC-UV method was developed for determination of the plasma concentration of CUR, PIP,ILE and dihydrocurcumin (DHC, a metabolite of CUR) simultaneously. Meanwhile, the effects of PIP and ILE on the plasma concentration and pharmacokinetics of DHC in SD rats was studied to explore whether ILE could serve as a CUR bioavailability enhancer. The metabolic pathway of CUR was studied by comparing the differences of CUR plasma concentration between intravenous injection and oral administration over the same time period, and reacting with small intestine homogenate without microbes of SD rats. The results of drug-time curve showed that combined administration of ILE and CUR had significant effect on plasma concentrations of DHC. Repeated administration of PIP or ILE could significantly increase the plasma concentration of DHC. Plasma CUR could be detected in the samples of from intravenous injection of CUR rats, whereas, it couldn’t be detected in the plasma sample form oral administration rats. CUR incubated with intestinal homogenate without intestinal bacteria could not be transformed into DHC. In conclusion, our results show that ILE can improve the bioavailability of CUR. Additionally, it was inferred that most of the CUR was reduced to DHC by NADPH when it was absorbed from gastrointestinal tract, and our results demonstrated that this pathway might be mediated by gastrointestinal microorganisms. Frontiers Media S.A. 2021-10-29 /pmc/articles/PMC8586700/ /pubmed/34776952 http://dx.doi.org/10.3389/fphar.2021.725362 Text en Copyright © 2021 Wang, Li, Lin, Luo and Luo. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Wang, Peijian
Li, Hui
Lin, Zhexuan
Luo, Hongjun
Luo, Wenhong
Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title_full Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title_fullStr Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title_full_unstemmed Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title_short Comparing the Effect of Piperine and Ilepcimide on the Pharmacokinetics of Curcumin in SD Rats
title_sort comparing the effect of piperine and ilepcimide on the pharmacokinetics of curcumin in sd rats
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8586700/
https://www.ncbi.nlm.nih.gov/pubmed/34776952
http://dx.doi.org/10.3389/fphar.2021.725362
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