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      Pterostilbene on Metabolic Parameters: A Randomized, Double-Blind, and Placebo-Controlled Trial

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          Abstract

          Introduction. The purpose of this trial was to evaluate the effect of pterostilbene on metabolic parameters. Methods. A prospective, randomized, double-blind, and placebo-controlled study that enrolled 80 patients with a total cholesterol ≥200 mg/dL and/or LDL ≥ 100 mg/dL. Subjects were divided into four groups: (1) pterostilbene 125 mg twice daily; (2) pterostilbene 50 mg twice daily; (3) pterostilbene 50 mg + grape extract (GE) 100 mg twice daily; (4) matching placebo twice daily for 6–8 weeks. Endpoints included lipids, blood pressure, and weight. Linear mixed models were used to examine and compare changes in parameters over time. Models were adjusted for age, gender, and race. Results. LDL increased with pterostilbene monotherapy (17.1 mg/dL; P = 0.001) which was not seen with GE combination ( P = 0.47). Presence of a baseline cholesterol medication appeared to attenuate LDL effects. Both systolic (−7.8 mmHg; P < 0.01) and diastolic blood pressure (−7.3 mmHg; P < 0.001) were reduced with high dose pterostilbene. Patients not on cholesterol medication ( n = 51) exhibited minor weight loss with pterostilbene (−0.62 kg/m 2; P = 0.012). Conclusion. Pterostilbene increases LDL and reduces blood pressure in adults. This trial is registered with Clinicaltrials.gov NCT01267227.

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          Most cited references23

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          2013 ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce Atherosclerotic Cardiovascular Risk in Adults

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            Heart disease and stroke statistics--2013 update: a report from the American Heart Association.

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              Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethylether analog, pterostilbene, in rats.

              Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a naturally occurring polyphenol with a broad range of possible health benefits, including anti-cancer activity. However, the biological activity of resveratrol may be limited by poor absorption and first-pass metabolism: only low plasma concentrations of resveratrol are seen following oral administration, and metabolism to glucuronide and sulfate conjugates is rapid. Methylated polyphenol analogs (such as pterostilbene [3,5-dimethoxy-4'-hydroxy-trans-stilbene], the dimethylether analog of resveratrol) may overcome these limitations to pharmacologic efficacy. The present study was designed to compare the bioavailability, pharmacokinetics, and metabolism of resveratrol and pterostilbene following equimolar oral dosing in rats. The agents were administered orally via gavage for 14 consecutive days at 50 or 150 mg/kg/day for resveratrol and 56 or 168 mg/kg/day for pterostilbene. Two additional groups were dosed once intravenously with 10 and 11.2 mg/kg for resveratrol and pterostilbene, respectively. Plasma concentrations of agents and metabolites were measured using a high-pressure liquid chromatograph-tandem mass spectrometer system. Noncompartmental analysis was used to derive pharmacokinetic parameters. Resveratrol and pterostilbene were approximately 20 and 80% bioavailable, respectively. Following oral dosing, plasma levels of pterostilbene and pterostilbene sulfate were markedly greater than were plasma levels of resveratrol and resveratrol sulfate. Although plasma levels of resveratrol glucuronide exceeded those of pterostilbene glucuronide, those differences were smaller than those of the parent drugs and sulfate metabolites. When administered orally, pterostilbene demonstrates greater bioavailability and total plasma levels of both the parent compound and metabolites than does resveratrol. These differences in agent pharmacokinetics suggest that the in vivo biological activity of equimolar doses of pterostilbene may be greater than that of resveratrol.
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                Author and article information

                Journal
                Evid Based Complement Alternat Med
                Evid Based Complement Alternat Med
                ECAM
                Evidence-based Complementary and Alternative Medicine : eCAM
                Hindawi Publishing Corporation
                1741-427X
                1741-4288
                2014
                25 June 2014
                25 June 2014
                : 2014
                : 459165
                Affiliations
                1The University of Mississippi School of Pharmacy, 2500 North State Street, Jackson, MS 39216, USA
                2The University of Mississippi Medical Center, 2500 North State Street, Jackson, MS 39216, USA
                3Department of Pharmacy Practice, University of Mississippi School of Pharmacy, 2500 North State Street, Jackson, MS 39216, USA
                4Department of Medicine, University of Mississippi Medical Center, 2500 North State Street, Jackson, MS 39216, USA
                5St. Dominic-Jackson Memorial Hospital, 969 Lakeland Drive, Jackson, MS 39216, USA
                6Center of Biostatistics, University of Mississippi Medical Center, 2500 North State Street, Jackson, MS 39216, USA
                7Cleveland Clinic, 9500 Euclid Avenue, Cleveland, OH 44195, USA
                Author notes
                *Daniel M. Riche: driche@ 123456umc.edu

                Academic Editor: Yong Chool Boo

                Article
                10.1155/2014/459165
                4099343
                25057276
                1938fc2f-7d07-42bb-9312-e422809a63df
                Copyright © 2014 Daniel M. Riche et al.

                This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 11 April 2014
                : 3 June 2014
                : 7 June 2014
                Categories
                Research Article

                Complementary & Alternative medicine
                Complementary & Alternative medicine

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