Effects of Standardized Medicinal Plant Extracts on Drug Metabolism Mediated by CYP3A4 and CYP2D6 Enzymes

The use of medicinal plants concomitantly with conventional drugs can result in herb–drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb–drug interactions. Among CYP...

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Published inChemical research in toxicology Vol. 33; no. 9; pp. 2408 - 2419
Main Authors Feltrin, Clarissa, Farias, Ingrid Vicente, Sandjo, Louis Pergaud, Reginatto, Flávio Henrique, Simões, Cláudia Maria Oliveira
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 21.09.2020
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Abstract The use of medicinal plants concomitantly with conventional drugs can result in herb–drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb–drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of in vitro interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants (Bauhinia forficata, Cecropia glaziovii, Cimicifuga racemosa, Cynara scolymus, Echinacea sp., Ginkgo biloba, Glycine max, Ilex paraguariensis, and Matricaria recutita) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, C. glaziovii (red embaúba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while I. paraguariensis (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.
AbstractList The use of medicinal plants concomitantly with conventional drugs can result in herb-drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb-drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants ( , , , , sp., , , , and ) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, (red embaúba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.
The use of medicinal plants concomitantly with conventional drugs can result in herb–drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb–drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of in vitro interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants (Bauhinia forficata, Cecropia glaziovii, Cimicifuga racemosa, Cynara scolymus, Echinacea sp., Ginkgo biloba, Glycine max, Ilex paraguariensis, and Matricaria recutita) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, C. glaziovii (red embaúba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while I. paraguariensis (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.
Author Reginatto, Flávio Henrique
Feltrin, Clarissa
Sandjo, Louis Pergaud
Simões, Cláudia Maria Oliveira
Farias, Ingrid Vicente
AuthorAffiliation Departamento de Química
Programa de Pós-Graduação em Farmácia, Centro de Ciências da Saúde
AuthorAffiliation_xml – name: Programa de Pós-Graduação em Farmácia, Centro de Ciências da Saúde
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Author_xml – sequence: 1
  givenname: Clarissa
  surname: Feltrin
  fullname: Feltrin, Clarissa
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  givenname: Ingrid Vicente
  surname: Farias
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  surname: Simões
  fullname: Simões, Cláudia Maria Oliveira
  email: claudia.simoes@ufsc.br
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Snippet The use of medicinal plants concomitantly with conventional drugs can result in herb–drug interactions that cause fluctuations in drug bioavailability and...
The use of medicinal plants concomitantly with conventional drugs can result in herb-drug interactions that cause fluctuations in drug bioavailability and...
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Title Effects of Standardized Medicinal Plant Extracts on Drug Metabolism Mediated by CYP3A4 and CYP2D6 Enzymes
URI http://dx.doi.org/10.1021/acs.chemrestox.0c00182
https://www.ncbi.nlm.nih.gov/pubmed/32786546
Volume 33
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