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Molecules 2014, 19(7), 9577-9590; doi:10.3390/molecules19079577

Quantification of the Resveratrol Analogs trans-2,3-Dimethoxy-stilbene and trans-3,4-Dimethoxystilbene in Rat Plasma: Application to Pre-Clinical Pharmacokinetic Studies

Department of Pharmacy, Faculty of Science, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260, Singapore
Dipartimento di Scienze Chimiche, Università di Catania, Viale A. Doria 6, I-95125 Catania, Italy
Author to whom correspondence should be addressed.
Received: 4 May 2014 / Revised: 26 June 2014 / Accepted: 28 June 2014 / Published: 7 July 2014
(This article belongs to the Special Issue Resveratrol)
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trans-2,3-Dimethoxystilbene (2,3-DMS) and trans-3,4-dimethoxystilbene (3,4-DMS) are two synthetic resveratrol (trans-3,5,4'-trihydroxystilbene) analogs. In this study, a simple HPLC method was developed and validated to determine 2,3-DMS and 3,4-DMS in rat plasma. Chromatographic separation was obtained with a reversed-phase HPLC column through a 12.5-min gradient delivery of a mixture of acetonitrile and water at the flow rate of 1.5 mL/min at 50 °C. The lower limit of quantification was 10 ng/mL. After successful validation, the pharmacokinetic profiles of 2,3-DMS and 3,4-DMS were subsequently studied in Sprague-Dawley rats. Upon single intravenous administration (4 mg/kg), 2,3-DMS had a medium volume of distribution of the central compartment (Vc = 2.71 ± 0.51 L/kg), quite rapid clearance (Cl = 52.0 ± 7.0 mL/min/kg), moderate mean transit time (MTT0→last = 131.0 ± 4.5 min) but a fairly long terminal elimination half-life (t1/2 λZ = 288.9 ± 92.9 min). Interestingly, 3,4-DMS displayed a pharmacokinetic profile apparently distinct from 2,3-DMS and it had more extensive distribution (Vc = 5.58 ± 1.73 L/kg), faster clearance (Cl = 143.4 ± 40.5 mL/min/kg) and shorter residence (MTT0→last = 61.4 ± 27.1 min). Following single oral administration (10 mg/kg), 2,3-DMS had low and erratic plasma exposure (Cmax = 37.5 ± 23.7 ng/mL) and poor oral bioavailability (2.22% ± 2.13%) while the oral bioavailability of 3,4-DMS was even poorer than 2,3-DMS. Clearly, the location of the methoxy groups had a significant impact on the pharmacokinetics of resveratrol analogs. This study provided useful information for the design of resveratrol derivatives in future study. View Full-Text
Keywords: resveratrol; trans-2,3-dimethoxystilbene; trans-3,4-dimethoxystilbene; HPLC; pharmacokinetics resveratrol; trans-2,3-dimethoxystilbene; trans-3,4-dimethoxystilbene; HPLC; pharmacokinetics

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Ng, S.Y.; Cardullo, N.; Yeo, S.C.M.; Spatafora, C.; Tringali, C.; Ong, P.-S.; Lin, H.-S. Quantification of the Resveratrol Analogs trans-2,3-Dimethoxy-stilbene and trans-3,4-Dimethoxystilbene in Rat Plasma: Application to Pre-Clinical Pharmacokinetic Studies. Molecules 2014, 19, 9577-9590.

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