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 , urine , , and Vd for IV dosing were μg/h/mL, h, h, L/h/kg, and L/kg, respectively (mean ± SEM, ) . Serum AUC, serum , urine , , and Vd for PO dosing were μg/h/mL, h, h, L/h/kg, and L/kg, respectively (mean ± SEM, ). 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 -glucosidase and -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.