Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A

1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine. 2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to...

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Bibliographic Details
Published in:Xenobiotica 2016-08, Vol.46 (8), p.677-682
Main Authors: Yu, Chung-Ping, Lin, Hui-Ju, Lin, Shiuan-Pey, Shia, Chi-Sheng, Chang, Pei-Hua, Hou, Yu-Chi, Hsieh, Yo-Wen
Format: Article
Language:English
Subjects:
Animals
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
Cyclosporine
Cyclosporine - pharmacology
CYP 3A
Cytochrome P-450 CYP3A - metabolism
Drugs, Chinese Herbal - pharmacology
herb-drug interaction
Immunosuppressive Agents - pharmacology
P-glycoprotein
Rats
Rheum - chemistry
rhubarb
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Summary:1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine. 2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to investigate the in vivo modulation effects of RP on P-gp and CYP 3A. 3. Rats were orally administered 2.5 mg/kg of CSP with and without 0.25 and 1.0 g/kg of RP. The blood CSP concentration was determined by a specific monoclonal fluorescence polarization immunoassay. 4. Both dosages of RP significantly decreased the C max and AUC 0-t of CSP in rats. Mechanism studies indicated that RP activated the functions of P-gp and CYP 3A. 5. RP ingestion reduced the systemic exposure of CSP through activating P-gp and CYP 3A.
ISSN:0049-8254
1366-5928
DOI:10.3109/00498254.2015.1117159