Inhibitory Effects of Multiple-Dose Treatment with Baicalein on the Pharmacokinetics of Ciprofloxacin in Rats.
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.
KM Application Center, Korea Institute of Oriental Medicine, Daegu, South Korea.
Youn-Hwan
YH
Hwang
KM Application Center, Korea Institute of Oriental Medicine, Daegu, South Korea.
Hye Jin
HJ
Yang
KM Application Center, Korea Institute of Oriental Medicine, Daegu, South Korea.
Dong-Gun
DG
Kim
KM Application Center, Korea Institute of Oriental Medicine, Daegu, South Korea.
Jin Yeul
JY
Ma
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D002939:Ciprofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D044950:Flavanones / Q000737:chemistry* / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
D000900:Anti-Bacterial Agents; D044950:Flavanones; D005419:Flavonoids; C006680:baicalein; D002939:Ciprofloxacin
baicalein; ciprofloxacin; herb-drug interaction; pharmacokinetics