Pharmacometrics of 3-methoxypterostilbene: A component of traditional Chinese medicinal plants

Abstract

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 t1/2, urine t1/2, Cltotal, and Vd for IV dosing were 48.1±23.8 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 t1/2, urine t1/2, Cltotal, and Vd for PO dosing were 229±44.6 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. © 2013 Stephanie E. Martinez et al.