TABLE 1

Effect of (+)-kawain and individual kavalactones on P-glycoprotein ATPase activity


Treatment

ATPase Activity
nmol Pi/mg protein/min
(+)-Kawain
   Control (MeOH) 0.20 ± 0.12
   87 nM 3.35 ± 0.00
   0.87 μM 4.09 ± 1.04
   8.7 μM 6.14 ± 0.08
   Verapamil (positive control)a 29.4 ± 4.1
Kavalactones
   Control (MeOH) 1.41
   Dihydrokawain (8.6 μM) N.D.
   Desmethoxyyangonin (8.8 μM) 2.97 ± 4.19
   Yangonin (7.8 μM) 1.17 ± 4.65
   Kavab 1.73 ± 1.00
   Verapamil (positive control)a (20 μM)
29.6 ± 2.0
  • N.D., not detectable.

  • a Verapamil was assayed at a concentration of 9 μg/ml

  • b 2 μg extract/ml, 3.3 μM in kavalactones