Inhibition of cytochrome P450 enzymes by rhein in rat liver microsomes.
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Tang JC, Yang H, Song XY, Song XH, Yan SL, Shao JQ, Zhang TL, Zhang JN
Inhibition of cytochrome P450 enzymes by rhein in rat liver microsomes.
Phytother Res. 2009 Feb;23(2):159-64. doi: 10.1002/ptr.2572.
- PubMed ID
- 18814214 [ View in PubMed]
- Abstract
Rhein, an active ingredient extensively found in plants such as Aloe, Cassitora L., rhubarb and so on, has been used for a long time in China. Pharmacological tests revealed that rhein not only had a strong antibacterial action, but also may be useful in cancer chemotherapy as a biochemical modulator. Its therapeutic action and toxicity is still the subject of considerable research. With microsome incubation assays in vitro and HPLC methods, the inhibition of rat liver CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A enzymes by rhein were studied kinetically. The results showed the most inhibition of CYP2E1 by rhein (K(i) = 10 microm, mixed); CYP3A and CYP2C9 were also inhibited by rhein, K(i) = 30 microm (mixed) and K(i) = 38 microm (mixed), respectively; rhein revealed some inhibition of CYP1A2 (K(i) = 62 microm, uncompetitive) and CYP2D6 (K(i) = 74 microm, mixed). Drug-drug interactions, especially cytochrome P450 (CYP)-mediated interactions, cause an enhancement or attenuation in the efficacy of co-administered drugs. Inhibition of the five major CYP enzymes observed for rhein suggested that changes in pharmacokinetics of co-administered drugs were likely to occur. Therefore, caution should be paid to the possible drug interaction of medicinal plants containing rhein and CYP substrates.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Diacerein Cytochrome P450 1A2 Protein Humans UnknownInhibitorDetails Diacerein Cytochrome P450 2C9 Protein Humans UnknownInhibitorDetails Diacerein Cytochrome P450 2D6 Protein Humans UnknownInhibitorDetails Diacerein Cytochrome P450 2E1 Protein Humans UnknownInhibitorDetails Diacerein Cytochrome P450 3A Subfamily (Protein Group) Protein group Humans UnknownInhibitorDetails - Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Rhein Cytochrome P450 1A2 Protein Humans UnknownInhibitorDetails Rhein Cytochrome P450 2C9 Protein Humans UnknownInhibitorDetails Rhein Cytochrome P450 2D6 Protein Humans UnknownInhibitorDetails Rhein Cytochrome P450 2E1 Protein Humans UnknownInhibitorDetails Rhein Cytochrome P450 3A Subfamily (Protein Group) Protein group Humans UnknownInhibitorDetails