Table 3

Furanocoumarins in grapefruit and other citrus fruit juices and their inhibitory effects on CYP3A activity

Code3-aFuranocoumarin in Juice3-bResidual Percentage Activity3-c (Mean ± S.D.)
μM3-b
DHBGF-I-5GF-I-1GF-I-6GF-I-2GF-I-4
Grapefruit juices
 Ki-134.7  (1)0.77  (1)0.49  (2)8.70  (1)20.4  (2)0.37  (2)29.3  ± 2.9
 Jo2.3  (4)0.64  (3)0.60  (1)6.15  (2)29.6  (1)0.53  (1)32.7  ± 1.7
 Ito1.1  (6)0.48  (7)0.10  (5)UD11.5  (6)0.17  (6)35.8  ± 3.0
 Ber1.2  (5)0.60  (4)0.23  (4)UD20.3  (3)0.31  (4)37.3  ± 2.1
 Ki-214.1  (2)0.65  (2)0.36  (3)3.46  (3)14.5  (4)0.35  (3)43.0  ± 2.3
 BbW0.8  (7)0.52  (6)0.09  (6)0.24  (4)13.9  (5)0.21  (5)46.0  ± 0.5
 Kag6.0  (3)0.56  (5)UDUD10.8  (7)0.11  (7)49.1  ± 2.9
 BbPUD0.48  (7)0.04  (7)UD7.2  (8)0.10  (8)57.6  ± 4.3
Sweetie juices
 Sw-149.52.590.288.0543.090.5120.2  ± 1.7
 Sw-29.63.480.091.659.400.5064.1  ± 0.3
Pomelo juices
 ToB1.90.87UDUD0.700.0645.8  ± 2.0
 SoW1.0UD0.160.541.360.6137.2  ± 1.1
 SoP0.8UDUDUD0.500.3552.2  ± 3.7
Sour orange juice
 Dd10.31.390.040.230.800.0657.9  ± 6.2
Sweet orange juices
 BbOUDUDUDUDUDUD75.5  ± 5.1
 CalOUDUDUDUDUDUD98.2  ± 5.8
  • 3-a See Table 2 for sample descriptions.

  • 3-b Mean concentration of triple tests for each juice sample. UD, under the limit of detection; figure in parentheses, order of ranking within grapefruit juices.

  • 3-c Residual percentage of testosterone 6β-hydroxylation by human liver microsomes when incubated with 2.5% juice sample. Data are shown as mean ± S.D. of at least three determinations.