Inhibitory Effects of Multiple‐Dose Treatment with Baicalein on the Pharmacokinetics of Ciprofloxacin in Rats
2017
Hwang, Youn‐Hwan | Yang, Hye Jin | Kim, Dong‐Gun | Ma, Jin Yeul
Ciprofloxacin is used as a treatment for urinary and respiratory tract infections in clinical practice. Baicalein, a major flavonoid present in Scutellaria baicalensis, is a well‐known and potent antibacterial compound used in complementary and alternative medicine practices. The present study aimed to clarify the effects of multiple‐dose treatment with baicalein on the pharmacokinetics of ciprofloxacin in rats. Following the oral administration of baicalein (20, 40, or 80 mg/kg) for five consecutive days, the rats received an oral administration of ciprofloxacin (20 mg/kg). Blood samples were collected at specific time points, and the plasma concentrations of ciprofloxacin were determined by using high‐performance liquid chromatography. To evaluate the mechanisms underlying the interaction between baicalein and ciprofloxacin, a rhodamine 123 accumulation assay was performed in LS‐180 cells. A pharmacokinetic study revealed that multiple‐dose treatment with baicalein significantly decreased the peak serum concentration (Cₘₐₓ), area under the curve (AUC₀ → ₄₈₀ ₘᵢₙ), and relative bioavailability (Fᵣₑₗ) of ciprofloxacin (p < 0.05). The rhodamine 123 accumulation assay revealed that treatment with baicalein for 48 h markedly reduced the intracellular accumulation of rhodamine 123. Taken together, these findings suggest that baicalein may result in the therapeutic failure of ciprofloxacin or other quinolone‐based antibiotics used for chemotherapy in clinical practice. Copyright © 2016 John Wiley & Sons, Ltd.
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