Donor | Age | Smoker | Alcohol Consumption | Medicine | Glucuronide formation | Ratio EM-652-7-G/ EM-652-4′-G | |
---|---|---|---|---|---|---|---|
EM-652-4′-G | EM-652-7-G | ||||||
pmol/min/mg of protein | |||||||
Pool (n = 5) | N.D. | N.D. | N.D. | N.D. | 15.6 ± 0.3 | 53.0 ± 2.2 | 3.4 |
Patient 1 | 59 | No | Yes | Nifedipine | 15.8 ± 0.3 | 48.4 ± 1.5 | 3 |
Diabetes | |||||||
Patient 2 | 65 | Yes | No | Glibenclamide, warfarin | 36.0 ± 2.3 | 134.9 ± 5.4 | 3.7 |
Diabetes | |||||||
Patient 3 | 52 | Yes | No | Insulin, Paroxetine, Buspirone | 11.5 ± 1.5 | 41.6 ± 4.9 | 3.6 |
Diabetes | |||||||
Patient 4 | 44 | Yes | No | Insulin, sumatriptan succinate, isometheptine mucate/ dichlovalphenazome/acetaminophen, Sulax | 9.9 ± 0.1 | 42.6 ± 1.2 | 4.3 |
Patient 5 | 42 | No | No | Clodine | 20.9 ± 0.5 | 86.9 ± 1.1 | 4.2 |
Patient 6 | 49 | No | No | Conjugated estrogen, Oxybutynin, Trazodone | 19.6 ± 1.0 | 91.8 ± 5.1 | 4.7 |
Anorexia | |||||||
Patient 7 | 34 | Yes | No | Lanotil, Diazepam | 36.9 ± 1.6 | 154.9 ± 4.9 | 4.2 |
Patient 8 | 53 | No | No | Estrogen | 25.7 ± 1.5 | 100.2 ± 6.5 | 3.9 |
The level of EM-652 glucurono-conjugation by female liver was determined for each hydroxyl position of the molecule by incubating microsomal proteins of liver samples (40 mg) and EM-652 (500 mM) for 3 h in presence of UDP-glucuronic acid (2 mM). EM-652-4′-glucuronide (EM-652-4′-G) and EM-652-7-glucuronide (EM-652-7-G) formation was detected and quantified using LC/MS-MS analysis. Values represent the mean of two independent esxperiments ± S.D.
N.D., not determined.