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Inhibition of Human Cytochrome P450 2C8-catalyzed Amodiaquine N-desethylation: Effect of Five Traditionally and Commonly Used Herbs

1, 2★, 3, 4★ Corresponding author

  1. 1Pharmacogenetics Research Group, Institute for Research in Molecular Medicine, Universiti Sains Malaysia
  2. 2School of Pharmacy, Monash University Malaysia 47500 Bandar Sunway, Selangor
  3. 3Department of Pharmacology, School of Medical Sciences, Universiti Sains Malaysia 16150 Kubang Kerian, Kelantan
  4. 4Centre of Excellence for Research in AIDS, Universiti Malaya 59990 Kuala Lumpur, Malaysia

CORRESPONDENCE

Chin Eng Ong

School of Pharmacy, Monash University Malaysia, 47500 Bandar Sunway, Selangor

ceong98@gmail.com

Volume 8, Issue 4 · pp. 292-297 · 2016 · DOI: 10.4103/0974-8490.188886

ABSTRACT

In Southeast Asia and many parts of the world, herbal products are increasingly used in parallel with modern medicine. This study aimed to investigate the effects of herbs commonly used in Southeast Asia on activity of cytochrome P450 2C8 (CYP2C8), an important human hepatic enzyme in drug metabolism. The selected herbs, such as Eurycoma longifolia Jack (ELJ), Labisia pumila (LP), Echinacea purpurea (EP), Andrographis paniculata (AP), and Ginkgo biloba (GB), were subjected to inhibition studies using an in vitro CYP2C8 activity marker, amodiaquine N-desethylase assay. Inhibition parameters, inhibitory concentration 50% (IC50), and Ki values were determined to study the potency and mode of inhibition. All herbs inhibited CYP2C8 with the following order of potency: LP > ELJ > GB > AP > EP. LP and ELJ inhibited potently at Ki’s of 2 and 4 times the Ki of quercetin, the positive control. The inhibition by LP was uncompetitive in nature as compared to competitive or mixed type inhibition observed with other herbs. GB exhibited moderate inhibitory effect at a Ki 6 times larger than quercetin Ki. AP and EP, on the other hand, showed only weak inhibition. The herbs we chose represented the more commonly used herbs in Southeast Asia where collision of tradition and modernization in healthcare, if not properly managed, may lead to therapeutic misadventures. We conclude that concurrent consumption of some herbs, in particular, LP and ELJ, may have relevance in drug-herb interactions via CYP2C8 inhibition in vivo.

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    Muthiah, Y. D., Ong, C. E., Sulaiman, S. A., & Ismail, R. (2016). Inhibition of Human Cytochrome P450 2C8-catalyzed Amodiaquine N-desethylation: Effect of Five Traditionally and Commonly Used Herbs. Pharmacognosy Research, 8(4), 292-297. https://doi.org/10.4103/0974-8490.188886

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    © 2016 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms. CC BY-NC-SA 4.0