Time-dependent Inhibition of CYP2C8 and CYP2C19 by Hedera helix Extracts, A Traditional Respiratory Herbal Medicine

Shaheed Ur Rehman, In Sook Kim, Min Sun Choi, Seung Hyun Kim, Yonghui Zhang, Hye Hyun Yoo

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The extract of Hedera helix L. (Araliaceae), a well-known folk medicine, has been popularly used to treat respiratory problems, worldwide. It is very likely that this herbal extract is taken in combination with conventional drugs. The present study aimed to evaluate the effects of H. helix extract on cytochrome P450 (CYP) enzyme-mediated metabolism to predict the potential for herb-drug interactions. A cocktail probe assay was used to measure the inhibitory effect of CYP. H. helix extracts were incubated with pooled human liver microsomes or CYP isozymes with CYP-specific substrates, and the formation of specific metabolites was investigated to measure the inhibitory effects. H. helix showed significant inhibitory effects on CYP2C8, CYP2C19 and CYP2D6 in a concentration-dependent manner. In recombinant CYP2C8, CYP2C19 and CYP2D6 isozymes, the IC50 values of the extract were 0.08 ± 0.01, 0.58 ± 0.03 and 6.72 ± 0.22 mg/mL, respectively. Further investigation showed that H. helix extract has a positive time-dependent inhibition property on both CYP2C8 and CYP2C19 with IC50 shift value of 2.77 ± 0.12 and 6.31 ± 0.25, respectively. Based on this in vitro investigation, consumption of herbal medicines or dietary supplements containing H. helix extracts requires careful attention to avoid any CYP-based interactions.

Original languageEnglish
JournalMolecules (Basel, Switzerland)
Volume22
Issue number7
DOIs
Publication statusPublished - 2017 Jul 24

Fingerprint

Hedera
Pulmonary Medicine
Herbal Medicine
medicine
helices
cytochromes
Cytochrome P-450 Enzyme System
Cytochrome P-450 CYP2D6
Isoenzymes
Inhibitory Concentration 50
drugs
Araliaceae
Dietary supplements
Herb-Drug Interactions
Drug interactions
metabolites
Traditional Medicine
supplements
Liver Microsomes
metabolism

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

Rehman, Shaheed Ur ; Kim, In Sook ; Choi, Min Sun ; Kim, Seung Hyun ; Zhang, Yonghui ; Yoo, Hye Hyun. / Time-dependent Inhibition of CYP2C8 and CYP2C19 by Hedera helix Extracts, A Traditional Respiratory Herbal Medicine. In: Molecules (Basel, Switzerland). 2017 ; Vol. 22, No. 7.
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Time-dependent Inhibition of CYP2C8 and CYP2C19 by Hedera helix Extracts, A Traditional Respiratory Herbal Medicine. / Rehman, Shaheed Ur; Kim, In Sook; Choi, Min Sun; Kim, Seung Hyun; Zhang, Yonghui; Yoo, Hye Hyun.

In: Molecules (Basel, Switzerland), Vol. 22, No. 7, 24.07.2017.

Research output: Contribution to journalArticle

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