Calycosin Influences the Metabolism of Five Probe Drugs in Rats
Authors Wu M, Lin Y, Wei Y, Du H, Ying X, Tan W, Tang B
Received 26 October 2019
Accepted for publication 17 December 2019
Published 29 January 2020 Volume 2020:14 Pages 429—434
Checked for plagiarism Yes
Review by Single-blind
Peer reviewer comments 2
Editor who approved publication: Dr Anastasios Lymperopoulos
Mei-ling Wu, Yi-ping Lin, Yan-li Wei, Hong-jian Du, Xiao-qian Ying, Wen-zhuang Tan, Bi-e Tang
Faculty of Medicine, Jinhua Polytechnic, Zhejiang, People’s Republic of China
Correspondence: Bi-e Tang
Faculty of Medicine, Jinhua Polytechnic, No. 1188 Wuzhou Street, Jinhua City, Zhejiang Provinc, People’s Republic of China
Background: Calycosin (CAL), a type of O-methylated isoflavone extracted from the herb Astralagusmembranaceus (AM), is a bioactive chemical with antioxidative, antiphlogistic and antineoplastic activities commonly used in traditional alternative Chinese medicine. AM has been shown to confer health benefits as an adjuvant in the treatment of a variety of diseases.
Aim: The main objective of this study was to determine whether CAL influences the cytochrome P450 (CYP450) system involved in drug metabolism.
Methods: Midazolam, tolbutamide, omeprazole, metoprolol and phenacetin were selected as probe drugs. Rats were randomly divided into three groups, specifically, 5% Carboxymethyl cellulose (CMC) for 8 days (Control), 5% CMC for 7 days + CAL for 1 day (single CAL) and CAL for 8 days (conc CAL), and metabolism of the five probe drugs evaluated using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS).
Results: No significant differences were observed for omeprazole and midazolam, compared to the control group. Tmax and t1/2 values of only one probe drug, phenacetin, in the conc CAL group were significantly different from those of the control group (Tmax h: 0.50± 0.00 vs 0.23± 0.15; control vs conc CAL). Cmax of tolbutamide was decreased about two-fold in the conc CAL treatment group (conc vs control: 219.48 vs 429.56, P< 0.001).
Conclusion: Calycosin inhibits the catalytic activities of CYP1A2, CYP2D6 and CYP2C9. Accordingly, we recommend caution, particularly when combining CAL as a modality therapy with drugs metabolized by CYP1A2, CYP2D6 and CYP2C9, to reduce the potential risks of drug accumulation or ineffective treatment.
Keywords: calycosin, herb-drug interactions, UPLC-MS/MS, cocktail, CYP450
This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.Download Article [PDF] View Full Text [HTML][Machine readable]