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Effects of Radix Astragali and Radix Rehmanniae, the components of an anti-diabetic foot ulcer herbal formula, on metabolism of model CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 probe substrates in pooled human liver microsomes and specific CYP isoforms
Or P.M.Y.; Lam F.F.Y.; Kwan Y.W.; Cho C.H.; Lau C.P.; Yu H.; Lin G.; Lau C.B.S.; Fung K.P.; Leung P.C.; Yeung J.H.K.
2012-04-15
Source PublicationPhytomedicine
ISSN09447113 1618095X
Volume19Issue:6Pages:535-544
Abstract

The present study investigated the effects of Radix Astragali (RA) and Radix Rehmanniae (RR), the major components of an anti-diabetic foot ulcer herbal formula (NF3), on the metabolism of model probe substrates of human CYP isoforms, CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4, which are important in the metabolism of a variety of xenobiotics. The effects of RA or RR on human CYP1A2 (phenacetin O-deethylase), CYP2C9 (tolbutamide 4-hydroxylase), CYP2D6 (dextromethorphan O-demethylase), CYP2E1 (chlorzoxazone 6-hydroxylase) and CYP3A4 (testosterone 6β-hydroxylase) activities were investigated using pooled human liver microsomes. NF3 competitively inhibited activities of CYP2C9 (IC = 0.98 mg/ml) and CYP3A4 (IC = 0.76 mg/ml), with K of 0.67 and 1.0 mg/ml, respectively. With specific human CYP2C9 and CYP3A4 isoforms, NF3 competitively inhibited activities of CYP2C9 (IC = 0.86 mg/ml) and CYP3A4 (IC = 0.88 mg/ml), with K of 0.57 and 1.6 mg/ml, respectively. Studies on RA or RR individually showed that RR was more important in the metabolic interaction with the model CYP probe substrates. RR dose-dependently inhibited the testosterone 6β-hydroxylation (K = 0.33 mg/ml) while RA showed only minimal metabolic interaction potential with the model CYP probe substrates studied. This study showed that RR and the NF3 formula are metabolized mainly by CYP2C9 and/or CYP3A4, but weakly by CYP1A2, CYP2D6 and CYP2E1. The relatively high K values of NF3 (for CYP2C9 and CYP3A4 metabolism) and RR (for CYP3A4 metabolism) would suggest a low potential for NF3 to cause herb-drug interaction involving these CYP isoforms. © 2011 Elsevier GmbH.

KeywordCyp1a2 Cyp2c9 Cyp2d6 Cyp2e1 Cyp3a4 Human Liver Microsomes Radix Astragali Radix Rehmanniae
DOI10.1016/j.phymed.2011.12.005
URLView the original
Indexed BySCIE
WOS Research AreaPlant Sciences ; Integrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Integrative & Complementary Medicine ; Pharmacology & Pharmacy
WOS IDWOS:000304576400010
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Cited Times [WOS]:29   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
AffiliationChinese University of Hong Kong
Recommended Citation
GB/T 7714
Or P.M.Y.,Lam F.F.Y.,Kwan Y.W.,et al. Effects of Radix Astragali and Radix Rehmanniae, the components of an anti-diabetic foot ulcer herbal formula, on metabolism of model CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 probe substrates in pooled human liver microsomes and specific CYP isoforms[J]. Phytomedicine,2012,19(6):535-544.
APA Or P.M.Y..,Lam F.F.Y..,Kwan Y.W..,Cho C.H..,Lau C.P..,...&Yeung J.H.K..(2012).Effects of Radix Astragali and Radix Rehmanniae, the components of an anti-diabetic foot ulcer herbal formula, on metabolism of model CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 probe substrates in pooled human liver microsomes and specific CYP isoforms.Phytomedicine,19(6),535-544.
MLA Or P.M.Y.,et al."Effects of Radix Astragali and Radix Rehmanniae, the components of an anti-diabetic foot ulcer herbal formula, on metabolism of model CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 probe substrates in pooled human liver microsomes and specific CYP isoforms".Phytomedicine 19.6(2012):535-544.
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