Abstract
Digeda-4 decoction is a traditional Mongolian medicine; its effects on cytochrome (CYP) enzymes are still unclear. CYP450 isoenzymes are the main drug metabolic enzymes, and their activities may be induced or inhibited by certain drugs, which lead to drug interactions in clinical use. Effects of Digeda-4 decoction on the activities of CYP450 subtype enzymes CYP1A2, CYP2C9, CYP2E1, CYP2C19, and CYP3A4 in rats were studied by cocktail method, and the pharmacokinetic parameters of five specific probe drugs (theophylline, tolbutamide, chlorzoxazone, omeprazole, and midazolam) were calculated by DAS software; changes of parameters can be used to evaluate the effects of Digeda-4 decoction on enzyme activities. The experimental rats were divided into three groups: control group, Digeda group, and positive group. Rats in Digeda group were given Digeda-4 decoction through continuous gavage for 14 days. After fasting for 12 hours, the mixed probes drug solution was injected into the tail vein; the blood samples were collected through the orbital vein at different time points. The concentrations of probe drugs in rat plasma were measured by HPLC. Compared with the control group, the half-life time (t1/2) of the pharmacokinetic parameters of theophylline, tolbutamide, omeprazole, and midazolam was prolonged, the area under the curve (AUC) increased, and the plasma clearance (CL) decreased in the Digeda group. Continuous gavage administration for 14 days may inhibit the activities of CYP450 subtype enzymes CYP1A2, CYP2C9, CYP2C19, and CYP3A4 of rats. Herb-drug interaction should be noted between Digeda-4 decoction and the drugs metabolized by CYP1A2, CYP2C9, CYP2C19, and CYP3A4.
Highlights
Traditional herbs are widely used throughout the world, while the herb-drug interactions resulting from which are increasingly reported
There are several cases reporting that H. perforatum reduced the blood concentration of cyclosporine, resulting in organ rejection, such as the case of a kidney transplant patient who had been taking cyclosporin for several years in whom organ rejection appeared after taking H. perforatum
The blood concentration of cyclosporin decreased to 0.48 ng/(mL x mg) from 0.84 ng/(mL x mg) after combination with H. perforatum; the herb-drug interaction was the cause of organ rejection [2]
Summary
Traditional herbs are widely used throughout the world, while the herb-drug interactions resulting from which are increasingly reported. The blood concentration of cyclosporin decreased to 0.48 ng/(mL x mg) from 0.84 ng/(mL x mg) after combination with H. perforatum; the herb-drug interaction was the cause of organ rejection [2]. A patient who took imatinib for 7 years suffered liver damage after taking Ginseng as an energy drink for 3 months, which may have been caused by interaction between imatinib and Ginseng [4]. This interaction may be due to the active constituents in Ginseng, which influenced the expression of the CYP450 enzymes [5].
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