Pharmacometrics of 3-methoxypterostilbene: a component of traditional chinese medicinal plants.

3-Methoxypterostilbene is a naturally occurring stilbene with potential in the treatment of diabetes. The preclinical pharmacokinetics and pharmacodynamics of 3-methoxypterostilbene were evaluated in the present study. The right jugular veins of male Sprague-Dawley rats were cannulated. The rats were dosed 10 mg/kg or 100 mg/kg of 3-methoxypterostilbene intravenously (IV) or orally (PO), respectively. Serum and urine samples were analyzed using a previously validated reversed-phase HPLC method. Serum AUC, serum t 1/2, urine t 1/2, Cltotal, and Vd for IV dosing were 48.1 ± 23.8  μ g/h/mL, 18.9 ± 10.9 h, 9.54 ± 1.51 h, 47.8 ± 23.7 L/h/kg, and 5.11 ± 0.38 L/kg, respectively (mean ± SEM, n = 4) . Serum AUC, serum t 1/2, urine t 1/2, Cltotal, and Vd for PO dosing were 229 ± 44.6  μ g/h/mL, 73.3 ± 8.91 h, 20.6 ± 3.01 h, 0.48 ± 0.008 L/h/kg, and 52.0 ± 10.5 L/kg, respectively (mean ± SEM, n = 4). Bioavailability of the stilbene was determined to be 50.6%  ± 10.0%. A 3-methoxypterostilbene glucuronidated metabolite was detected in both serum and urine. 3-Methoxypterostilbene exhibited antidiabetic activity including α-glucosidase and α-amylase inhibition as well as concentration-dependent antioxidant capacity similar to resveratrol. 3-Methoxypterostilbene also exhibited anti-inflammatory activity. 3-Methoxypterostilbene appears to be a bioactive compound and may be useful in reducing postprandial hyperglycemia.