Journal
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 59, Issue 4, Pages 1072-1077Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jf1043019
Keywords
trans-3,4,5,4 '-Tetramethoxystilbene; HPLC; pharmacokinetics; absolute oral bioavailability
Funding
- Agency for Science, Technology and Research (BMRC), Republic of Singapore [06/1/21/19/441]
- NUS [R-148000084112]
- Universita degli Studi di Catania (Progetti di Ricerca di Ateneo, Catania, Italy)
- MIUR, Ministero dell'Universita e della Ricerca (Rome, Italy)
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A simple HPLC method was established to quantify trans-3,4,5,4'-tetramethoxystilbene (MR-4 or DMU-212) in rat plasma. Chromatographic separation was obtained with a reversed-phase HPLC column through an 11 min gradient delivery of a mixture of acetonitrile and water at a flow rate of 1.5 mL/min at 50 degrees C. The limit of quantification was 15 ng/mL. The intra- and interday precisions in terms of relative standard deviation were <9% at all concentrations. Similarly, the accuracy was good, and the bias rates ranged within +/- 7%. The pharmacokinetic profiles of MR-4 were subsequently assessed in rats using 2-hydroxypropyl-beta-cyclodextrin as a dosing vehicle. Upon intravenous administration, MR-4 displayed moderate clearance (46.5 +/- 7.6 mL/min/kg) and terminal elimination half-life (154 +/- 80 mm). However, the absolute oral bioavailability of MR-4 was low (6.31 +/- 3.30%). Future investigation on MR-4 as a chemotherapeutic agent should be focused on colorectal cancers.
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