Pharmacometrics of 3-Methoxypterostilbene : A Component of Traditional Chinese Medicinal Plants

• Published in: Evidence-based complementary and alternative medicine 2013-01, Vol.2013 (2013), p.1-11
• Main Authors: Martinez, Stephanie E., Davies, Neal M., Sayre, Casey L.
• Format: Article
• Language: English
• Subjects: Anti-inflammatory agents; Antidiabetics; Antioxidants; Bioactive compounds; Bioavailability; Cardiovascular disease; Cell cycle; Chemistry; Chromatography; Diabetes; Diabetes mellitus; Food; Glucosidase; Herbal medicine; High-performance liquid chromatography; Hyperglycemia; Inflammation; Laboratories; Liquid chromatography; Medicinal plants; Metabolism; Metabolites; Natural products; Obesity; Pharmacodynamics; Pharmacokinetics; Rats; Resveratrol; Rodents; Stilbene; Urine; α-Amylase; α-Glucosidase
• ISSN: 1741-427X; 1741-4288
• DOI: 10.1155/2013/261468

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 μg/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 μg/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.