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    Evaluation of the inhibitory effect of Gynostemma pentaphyllum extracts on CYP450 enzyme activities using LC-MS/MS

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    https://www.riss.kr/link?id=A108779779

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    Gynostemma pentaphyllum (Thunb.) Makino extract, a natural product with a history of traditional use, has gained attention for its potential health benefits. This study aimed to investigate its effects on key cytochrome P450 (CYP) enzymes using LC-MS/MS. Human liver microsomes and cDNA-expressed CYP2C8, CYP2C9, CYP2C19, and CYP3A4 supersomes were employed. Enzyme activity was assessed based on the formation of CYP-specific marker metabolites. The resulting data showed that the extract exhibited inhibitory effects on CYP2C8, CYP2C9, CYP2C19, and CYP3A4. Thus, G. pentaphyllum extract may influence the pharmacokinetics of drugs metabolized by CYP2C8, CYP2C9, CYP2C19, and CYP3A4. These find- ings emphasize the importance of considering potential herb-drug interactions when incorporating this extract into therapeutic regimens or dietary supplements.
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    Gynostemma pentaphyllum (Thunb.) Makino extract, a natural product with a history of traditional use, has gained attention for its potential health benefits. This study aimed to investigate its effects on key cytochrome P450 (CYP) enzymes using LC-MS/...

    Gynostemma pentaphyllum (Thunb.) Makino extract, a natural product with a history of traditional use, has gained attention for its potential health benefits. This study aimed to investigate its effects on key cytochrome P450 (CYP) enzymes using LC-MS/MS. Human liver microsomes and cDNA-expressed CYP2C8, CYP2C9, CYP2C19, and CYP3A4 supersomes were employed. Enzyme activity was assessed based on the formation of CYP-specific marker metabolites. The resulting data showed that the extract exhibited inhibitory effects on CYP2C8, CYP2C9, CYP2C19, and CYP3A4. Thus, G. pentaphyllum extract may influence the pharmacokinetics of drugs metabolized by CYP2C8, CYP2C9, CYP2C19, and CYP3A4. These find- ings emphasize the importance of considering potential herb-drug interactions when incorporating this extract into therapeutic regimens or dietary supplements.

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    참고문헌 (Reference)

    1 Ümit Yasar, "The role of CYP2C9 genotype in the metabolism of diclofenac in vivo and in vitro" Springer Science and Business Media LLC 57 (57): 729-735, 2001

    2 Chao Su, "Progress in the Medicinal Value, Bioactive Compounds, and Pharmacological Activities of Gynostemma pentaphyllum" MDPI AG 26 (26): 6249-, 2021

    3 San-Hu Gou, "Lipid-lowering, hepatoprotective, and atheroprotective effects of the mixture Hong-Qu and gypenosides in hyperlipidemia with NAFLD rats" Ovid Technologies (Wolters Kluwer Health) 79 (79): 111-121, 2016

    4 Min He, "Inhibitory effects of gypenosides on seven human cytochrome P450 enzymes in vitro" Elsevier BV 57 : 262-265, 2013

    5 Jun Yu, "Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity" Georg Thieme Verlag KG 83 (83): 895-900, 2017

    6 Sumitra Suntararuks, "Immunomodulatory Effects of Cadmium and Gynostemma pentaphyllum Herbal Tea on Rat Splenocyte Proliferation" American Chemical Society (ACS) 56 (56): 9305-9311, 2008

    7 Kiran C. Patki, "IN VITRO METABOLISM OF MIDAZOLAM, TRIAZOLAM, NIFEDIPINE, AND TESTOSTERONE BY HUMAN LIVER MICROSOMES AND RECOMBINANT CYTOCHROMES P450: ROLE OF CYP3A4 AND CYP3A5" American Society for Pharmacology & Experimental Therapeutics (ASPET) 31 (31): 938-944, 2003

    8 Xin-Sheng Lai, "Human CYP2C8: Structure, Substrate Specificity, Inhibitor Selectivity, Inducers and Polymorphisms" Bentham Science Publishers Ltd. 10 (10): 1009-1047, 2009

    9 J. A. Goldstein, "Evidence That CYP2C19 is the Major (S)-Mephenytoin 4'-Hydroxylase in Humans" American Chemical Society (ACS) 33 (33): 1743-1752, 1994

    10 Bulei Wang, "Effects of extraction methods on antioxidant and immunomodulatory activities of polysaccharides from superfine powder Gynostemma pentaphyllum Makino" Springer Science and Business Media LLC 37 (37): 777-789, 2020

    1 Ümit Yasar, "The role of CYP2C9 genotype in the metabolism of diclofenac in vivo and in vitro" Springer Science and Business Media LLC 57 (57): 729-735, 2001

    2 Chao Su, "Progress in the Medicinal Value, Bioactive Compounds, and Pharmacological Activities of Gynostemma pentaphyllum" MDPI AG 26 (26): 6249-, 2021

    3 San-Hu Gou, "Lipid-lowering, hepatoprotective, and atheroprotective effects of the mixture Hong-Qu and gypenosides in hyperlipidemia with NAFLD rats" Ovid Technologies (Wolters Kluwer Health) 79 (79): 111-121, 2016

    4 Min He, "Inhibitory effects of gypenosides on seven human cytochrome P450 enzymes in vitro" Elsevier BV 57 : 262-265, 2013

    5 Jun Yu, "Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity" Georg Thieme Verlag KG 83 (83): 895-900, 2017

    6 Sumitra Suntararuks, "Immunomodulatory Effects of Cadmium and Gynostemma pentaphyllum Herbal Tea on Rat Splenocyte Proliferation" American Chemical Society (ACS) 56 (56): 9305-9311, 2008

    7 Kiran C. Patki, "IN VITRO METABOLISM OF MIDAZOLAM, TRIAZOLAM, NIFEDIPINE, AND TESTOSTERONE BY HUMAN LIVER MICROSOMES AND RECOMBINANT CYTOCHROMES P450: ROLE OF CYP3A4 AND CYP3A5" American Society for Pharmacology & Experimental Therapeutics (ASPET) 31 (31): 938-944, 2003

    8 Xin-Sheng Lai, "Human CYP2C8: Structure, Substrate Specificity, Inhibitor Selectivity, Inducers and Polymorphisms" Bentham Science Publishers Ltd. 10 (10): 1009-1047, 2009

    9 J. A. Goldstein, "Evidence That CYP2C19 is the Major (S)-Mephenytoin 4'-Hydroxylase in Humans" American Chemical Society (ACS) 33 (33): 1743-1752, 1994

    10 Bulei Wang, "Effects of extraction methods on antioxidant and immunomodulatory activities of polysaccharides from superfine powder Gynostemma pentaphyllum Makino" Springer Science and Business Media LLC 37 (37): 777-789, 2020

    11 Mingzhe Zhao, "Cytochrome P450 Enzymes and Drug Metabolism in Humans" MDPI AG 22 (22): 12808-, 2021

    12 C. Circosta, "Cardiovascular effects of the aqueous extract of Gynostemma pentaphyllum Makino" Elsevier BV 12 (12): 638-643, 2005

    13 Z WANG, "Antioxidant activities of different fractions of polysaccharide purified from Gynostemma pentaphyllum Makino" Elsevier BV 68 (68): 54-58, 2007

    14 Aftab Ahmed, "Gynostemma pentaphyllum an immortal herb with promising therapeutic potential: a comprehensive review on its phytochemistry and pharmacological perspective" Informa UK Limited 26 (26): 808-832, 2023

    15 Xiaojin Liu, "Gynostemma pentaphyllum Makino extract induces hair growth and exhibits an anti‐graying effect via multiple mechanisms" Wiley 23 (23): 648-657, 2023

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