ABSTRACT
Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide, CAP) is an important ingredient in spicy foods consumed throughout the world. Vinblastine (VBL) is a naturally occurring alkaloid prescribed to cancer patients. Many cancer patients treated with VBL were taking CAP at the same time. This study attempted to investigate the effect of CAP on the pharmacokinetics of VBL, which is the substrate of CYP3A, P-gp, and Mrp2. CAP, cyclosporine (CsA) or olive oil was given to rats for seven consecutive days, and on the seventh day, VBL (1.3 mg/kg) was administered intravenously. CsA was used as a CYP3A1/2 and transporter inhibitor, and olive oil was used as a vehicle. The results showed that pretreatment of rats with CAP (3.0 mg/kg) for seven consecutive days resulted in an increase in the AUC0-t of VBL of about 29.8% (P < 0.05) compared with the control group. Moreover, CAP decreased the CL of VBL to 75.5% (P < 0.05). At this time, CYP3A1/2 and Mrp2/Abcc2 in the liver was decreased at the mRNA and protein levels. These results demonstrate that chronic ingestion of CAP will increase systemic exposure and reduce clearance of VBL in rats. The food-drug interaction between CAP and VBL appears to be due to modulation of CYP3A1/2 and Mpr2 expression by CAP.
Subject(s)
Capsaicin/pharmacology , Cytochrome P-450 CYP3A/drug effects , Multidrug Resistance-Associated Proteins/drug effects , Vinblastine/pharmacokinetics , ATP Binding Cassette Transporter, Subfamily B, Member 1/drug effects , Animals , Area Under Curve , Blotting, Western , Cyclosporine/pharmacology , Food-Drug Interactions , Male , Multidrug Resistance-Associated Protein 2 , RNA, Messenger/drug effects , Rats , Reverse Transcriptase Polymerase Chain ReactionABSTRACT
OBJECTIVE: To establish a new identification and analysis method of Herba Hedyotidis. METHOD: HPLC fingerprint pattern method. RESULT: Experiment and analysis were carried out on seven samples, the standard HPLC fingerprint pattern method and characterisitic diffraction peaks of Herba Hedyotidis were obtained. CONCLUSION: This method can be used for the identification of Herba Hedyotidis.
