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Shengmin Sang - One of the best experts on this subject based on the ideXlab platform.
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Metabolism and pharmacokinetics of resveratrol and Pterostilbene.
BioFactors (Oxford England), 2018Co-Authors: Pei Wang, Shengmin SangAbstract:Beneficial properties of resveratrol and Pterostilbene, a dimethyl ether analog of resveratrol, have attracted increasing interest in recent years. Resveratrol and Pterostilbene exhibit many pharmacological similarities and both of them are generally considered to be safe for human consumption. Beyond the structural and general bioactivity similarities between them, large amounts of data are now available to reveal the metabolic fate and pharmacological differences between them. Pterostilbene was found to be more metabolically stable and usually exhibited stronger pharmacological activities than that of resveratrol. As a contribution to clarify and compare aspects like metabolic stability and pharmacokinetics of resveratrol and Pterostilbene, as well as explain the pharmacological similarities and differences between them, this review presents and compares recent data on the metabolism and pharmacokinetics of resveratrol and Pterostilbene. © 2018 BioFactors, 44(1):16-25, 2018.
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structural identification of mouse urinary metabolites of Pterostilbene using liquid chromatography tandem mass spectrometry
Rapid Communications in Mass Spectrometry, 2010Co-Authors: Xi Shao, Xiaoxin Chen, Vladimir Badmaev, Shengmin SangAbstract:Pterostilbene, the dimethoxy derivative of resveratrol, has drawn much attention recently due to its potential beneficial health effects. The metabolic fate of Pterostilbene, however, is not well understood. In the present study, we identified nine novel mouse urinary Pterostilbene metabolites, Pterostilbene glucuronide, Pterostilbene sulfate, mono-demethylated Pterostilbene glucuronide, mono-demethylated Pterostilbene sulfate, mono-hydroxylated Pterostilbene, mono-hydroxylated Pterostilbene glucuronide, mono-hydroxylated Pterostilbene sulfate, and mono-hydroxylated Pterostilbene glucuronide sulfate, using liquid chromatography/atmospheric pressure chemical ionization and electrospray ionization tandem mass spectrometry. The structures of these metabolites were confirmed by analyzing the MS(n) (n = 1-3) spectra. To our knowledge, this is the first report of the identification of urinary metabolites of Pterostilbene in mice.
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Structural identification of mouse urinary metabolites of Pterostilbene using liquid chromatography/tandem mass spectrometry.
Rapid communications in mass spectrometry : RCM, 2010Co-Authors: Xi Shao, Xiaoxin Chen, Vladimir Badmaev, Shengmin SangAbstract:Pterostilbene, the dimethoxy derivative of resveratrol, has drawn much attention recently due to its potential beneficial health effects. The metabolic fate of Pterostilbene, however, is not well understood. In the present study, we identified nine novel mouse urinary Pterostilbene metabolites, Pterostilbene glucuronide, Pterostilbene sulfate, mono-demethylated Pterostilbene glucuronide, mono-demethylated Pterostilbene sulfate, mono-hydroxylated Pterostilbene, mono-hydroxylated Pterostilbene glucuronide, mono-hydroxylated Pterostilbene sulfate, and mono-hydroxylated Pterostilbene glucuronide sulfate, using liquid chromatography/atmospheric pressure chemical ionization and electrospray ionization tandem mass spectrometry. The structures of these metabolites were confirmed by analyzing the MS(n) (n = 1-3) spectra. To our knowledge, this is the first report of the identification of urinary metabolites of Pterostilbene in mice.
Agnes M. Rimando - One of the best experts on this subject based on the ideXlab platform.
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Pterostilbene a dimethyl ether derivative of resveratrol reduces fat accumulation in rats fed an obesogenic diet
Journal of Agricultural and Food Chemistry, 2014Co-Authors: Saioa Gomezzorita, Alfredo Fernandezquintela, Leixuri Aguirre, Arrate Lasa, Agnes M. Rimando, María P. PortilloAbstract:The current study aimed to demonstrate the effects of Pterostilbene in rats fed an obesogenic diet. For this purpose, Pterostilbene was administered at doses of 15 mg/kg body weight/day (PT15 group) or 30 mg/kg body weight/day (PT30 group) for 6 weeks. Pterostilbene reduced adipose tissue mass -15.1% (PT15) and -22.9% (PT30). In this tissue, it decreased malic enzyme (-39.4 and -49.5% for PT15 and PT30 groups, respectively) and fatty acid synthase (-45 and -53.4% for PT15 and PT30) activities. Acetyl-CoA carboxylase activity was reduced and AMPK activity was increased only in the PT30 group. In the liver, Pterostilbene (PT30) reduced malic enzyme (-29.5%) and glucose-6-P dehydrogenase (-43.2%) activities and increased carnitine palmitoyltransferase-1a (37.5%) and acyl-coenzyme A oxidase (42.5%) activities. This increased oxidative capacity was not associated with increased mitochondriogenesis. Among biochemical serum parameters, only insulin was modified by Pterostilbene (-31.6%) in the PT15 group. The amounts of Pterostilbene in serum and tissues from rats in the PT30 group were in not all cases 2-fold greater than those found in the PT15 group. In conclusion, Pterostilbene shows antiobesity properties due, at least in part, to reduced lipogenesis in adipose tissue and increased fatty acid oxidation in liver.
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Pterostilbene a dimethyl ether derivative of resveratrol reduces fat accumulation in rats fed an obesogenic diet
Journal of Agricultural and Food Chemistry, 2014Co-Authors: Saioa Gomezzorita, Alfredo Fernandezquintela, Leixuri Aguirre, Arrate Lasa, Agnes M. Rimando, María P. PortilloAbstract:The current study aimed to demonstrate the effects of Pterostilbene in rats fed an obesogenic diet. For this purpose, Pterostilbene was administered at doses of 15 mg/kg body weight/day (PT15 group) or 30 mg/kg body weight/day (PT30 group) for 6 weeks. Pterostilbene reduced adipose tissue mass −15.1% (PT15) and −22.9% (PT30). In this tissue, it decreased malic enzyme (−39.4 and −49.5% for PT15 and PT30 groups, respectively) and fatty acid synthase (−45 and −53.4% for PT15 and PT30) activities. Acetyl-CoA carboxylase activity was reduced and AMPK activity was increased only in the PT30 group. In the liver, Pterostilbene (PT30) reduced malic enzyme (−29.5%) and glucose-6-P dehydrogenase (−43.2%) activities and increased carnitine palmitoyltransferase-1a (37.5%) and acyl-coenzyme A oxidase (42.5%) activities. This increased oxidative capacity was not associated with increased mitochondriogenesis. Among biochemical serum parameters, only insulin was modified by Pterostilbene (−31.6%) in the PT15 group. The am...
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Anxiolytic action of Pterostilbene: involvement of hippocampal ERK phosphorylation.
Planta medica, 2013Co-Authors: Md Al Rahim, Agnes M. Rimando, Kalpten Silistreli, Abir T El-alfyAbstract:Pterostilbene, a natural analog of resveratrol, has diverse health-beneficial properties. However, the neurological activities of this compound are largely unexplored. Here, we report that Pterostilbene shows anxiolytic-like actions by down-regulating phosphorylated levels of extracellular regulated kinases in the hippocampus of mice. Adult male mice administered Pterostilbene (1-10 mg/kg, p. o.) were subjected to the elevated plus maze test. Pterostilbene manifested anxiolytic activity at 1 and 2 mg/kg doses, demonstrated by increases in % permanence time and number of open arm entries. The locomotor activity of the animals was unaffected at all doses. Western blot analysis revealed a decrease in both extracellular regulated kinase 1 and extracellular regulated kinase 2 phosphorylation in hippocampal homogenates from mice treated with 1 and 2 mg/kg Pterostilbene. Moreover, Pterostilbene was detected in the plasma and brains of mice following single oral administration. Anxiolytic activity was not observed at the higher doses (5 and 10 mg/kg). However, no impairment of motor function was observed either, suggesting a favorable safety index for the compound. These results suggest that Pterostilbene has the potential for therapeutic drug development for anxiety disorders.
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Low-dose Pterostilbene, but not resveratrol, is a potent neuromodulator in aging and Alzheimer's disease.
Neurobiology of aging, 2011Co-Authors: Jaewon Chang, Agnes M. Rimando, Mercè Pallàs, Antoni Camins, David Porquet, Jennifer Reeves, Barbara Shukitt-hale, Mark A. Smith, James A. Joseph, Gemma CasadesusAbstract:Recent studies have implicated resveratrol and Pterostilbene, a resveratrol derivative, in the protection against age-related diseases including Alzheimer's disease (AD). However, the mechanism for the favorable effects of resveratrol in the brain remains unclear and information about direct cross-comparisons between these analogs is rare. As such, the purpose of this study was to compare the effectiveness of diet-achievable supplementation of resveratrol to that of Pterostilbene at improving functional deficits and AD pathology in the SAMP8 mouse, a model of accelerated aging that is increasingly being validated as a model of sporadic and age-related AD. Furthermore we sought to determine the mechanism of action responsible for functional improvements observed by studying cellular stress, inflammation, and pathology markers known to be altered in AD. Two months of Pterostilbene diet but not resveratrol significantly improved radial arm water maze function in SAMP8 compared with control-fed animals. Neither resveratrol nor Pterostilbene increased sirtuin 1 (SIRT1) expression or downstream markers of sirtuin 1 activation. Importantly, markers of cellular stress, inflammation, and AD pathology were positively modulated by Pterostilbene but not resveratrol and were associated with upregulation of peroxisome proliferator-activated receptor (PPAR) alpha expression. Taken together our findings indicate that at equivalent and diet-achievable doses Pterostilbene is a more potent modulator of cognition and cellular stress than resveratrol, likely driven by increased peroxisome proliferator-activated receptor alpha expression and increased lipophilicity due to substitution of hydroxy with methoxy group in Pterostilbene.
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dietary intake of Pterostilbene a constituent of blueberries inhibits the β catenin p65 downstream signaling pathway and colon carcinogenesis in rats
Carcinogenesis, 2010Co-Authors: Shiby Paul, Agnes M. Rimando, Andrew J Decastro, Hong Jin Lee, Amanda K Smolarek, Barbara Simi, Chung Xiou Wang, Renping Zhou, Nanjoo SuhAbstract:Stilbenes are phytochemicals present in grapes, berries, peanuts and red wine. A widely studied stilbene, resveratrol (trans-3,5,4'-trihydroxystilbene), has been shown to exert antioxidant, anti-inflammatory, chemopreventive and antiaging effects in a number of biological systems. We reported earlier that Pterostilbene (trans-3,5-dimethoxy-4'-hydroxystilbene), a structurally related stilbene found in blueberries, was effective in reducing the incidence and multiplicity of aberrant crypt foci formation in the colon of rats injected with azoxymethane (AOM). Our present study was to identify the chemopreventive potential of Pterostilbene with colonic tumor formation as an end point and further to evaluate the mechanistic action of Pterostilbene during colon carcinogenesis. F344 rats were given two AOM injections subcutaneously when they were 7 and 8 weeks old and continuously fed the control or 40 p.p.m. Pterostilbene diet for 45 weeks. Overall analyses indicated that Pterostilbene reduced colon tumor multiplicity of non-invasive adenocarcinomas, lowered proliferating cell nuclear antigen and downregulated the expression of beta-catenin and cyclin D1. Pterostilbene decreased mucosal levels of the proinflammatory cytokines, tumor necrosis factor-alpha, interleukin (IL)-1beta and IL-4. Colon tumors from Pterostilbene-fed animals showed reduced expression of inflammatory markers as well as nuclear staining for phospho-p65, a key molecule in the nuclear factor-kappaB pathway. In HT-29 cells, Pterostilbene reduced the protein levels of beta-catenin, cyclin D1 and c-MYC, altered the cellular localization of beta-catenin and inhibited the phosphorylation of p65. Our data with Pterostilbene in suppressing colon tumorigenesis, cell proliferation as well as key inflammatory markers in vivo and in vitro suggest the potential use of Pterostilbene for colon cancer prevention.
Min-hsiung Pan - One of the best experts on this subject based on the ideXlab platform.
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Occurrence, Bioavailability, Anti-inflammatory, and Anticancer Effects of Pterostilbene.
Journal of agricultural and food chemistry, 2020Co-Authors: Wei-sheng Lin, Jane V. Leland, Min-hsiung PanAbstract:Supplementation with natural compounds found in fruits and vegetables has long been associated with a reduced risk of several types of cancer. Pterostilbene is a natural stilbenoid and a dimethylated analogue of resveratrol which is found primarily in blueberries. Pterostilbene exhibits a range of pharmacological properties, particularly anti-inflammatory and anticancer effects. Due to two methoxy groups in its skeleton, Pterostilbene is more lipophilic than resveratrol and thus possesses higher intestinal permeability and cellular uptake and enhanced stability. Moreover, Pterostilbene exhibits less toxicity and fewer adverse effects, providing it with superior potential in cancer chemoprevention and chemotherapy applications. Numerous research studies have demonstrated that Pterostilbene possesses detoxification activities, mediating the anti-inflammation response, regulating the cell cycle, augmenting apoptosis, enhancing autophagy, and inhibiting tumor angiogenesis, invasion, and metastasis by modulating signal transduction pathways which block multiple stages of carcinogenesis. In this review, we illustrate that Pterostilbene is a natural compound having bioavailability. The extensive metabolism of Pterostilbene will be discussed. We also summarize recent research on Pterostilbene's anti-inflammatory and anticancer properties in the multistage carcinogenesis process and related molecular mechanism and conclude that it should contribute to improved cancer management.
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Prevention of Vascular Inflammation by Pterostilbene via Trimethylamine-N-Oxide Reduction and Mechanism of Microbiota Regulation.
Molecular nutrition & food research, 2019Co-Authors: Yen Chun Koh, Pei Yu Chen, Nagabhushanam Kalyanam, Min-hsiung PanAbstract:Scope A gut-microbiota-dependent metabolite of L-carnitine, trimethylamine-N-oxide (TMAO), has been recently discovered as an independent and dose-dependent risk factor for cardiovascular disease (CVD). This study aims to investigate the effects of Pterostilbene on reducing TMAO formation and on decreasing vascular inflammation in carnitine-feeding mice. Methods and results C57BL/6 mice are treated with 1.3% carnitine in drinking water with or without Pterostilbene supplementation. Using LC-MS/MS, the result shows that mice treated with 1.3% carnitine only significantly increased the plasma TMAO and Pterostilbene supplementation group can reverse it. Additionally, Pterostilbene decreases hepatic flavin monooxygenase 3 (FMO3) mRNA levels compared to carnitine only group. It appears that Pterostilbene can alter host physiology and create an intestinal microenvironment favorable for certain gut microbiota. Gut microbiota analysis reveals that Pterostilbene increases the abundance of Bacteroides. Further, Pterostilbene decreases mRNA levels of vascular inflammatory markers tumor necrosis factor-α (TNF-α), vascular cell adhesion molecule 1 (VCAM-1), and E-selectin). Conclusion These data suggest that amelioration of carnitine-induced vascular inflammation after consumption of Pterostilbene is partially mediated via modulation of gut microbiota composition and hepatic enzyme FMO3 gene expression.
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Pterostilbene inhibits dimethylnitrosamine induced liver fibrosis in rats
Food Chemistry, 2013Co-Authors: Ming-fen Lee, Meiling Tsai, Anchin Cheng, Min Lung Liu, Wen Shiung Liou, Min-hsiung PanAbstract:Pterostilbene, found in grapes and berries, exhibits pleiotropic effects, including anti-inflammatory, antioxidant, and anti-proliferative activities. This study was conducted to investigate the effect of Pterostilbene on liver fibrosis and the potential underlying mechanism for such effect. Sprague-Dawley rats were intraperitoneally given dimethyl n-nitrosamine (DMN) (10mg/kg) 3 days per week for 4 weeks. Pterostilbene (10 or 20mg/kg) was administered by oral gavage daily. Liver function, morphology, histochemistry, and fibrotic parameters were examined. Pterostilbene supplementation alleviated the DMN-induced changes in the serum levels of alanine transaminase and aspartate transaminase (p<0.05). Fibrotic status and the activation of hepatic stellate cells were improved upon Pterostilbene supplementation as evidenced by histopathological examination as well as the expression of α-smooth muscle actin (α-SMA), transforming growth factor-β1 (TGF-β1), and matrix metalloproteinase 2 (MMP2). These data demonstrated that Pterostilbene exhibited hepatoprotective effects on experimental fibrosis, potentially by inhibiting the TGF-β1/Smad signaling.
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Pterostilbene inhibits dimethylnitrosamine-induced liver fibrosis in rats.
Food chemistry, 2012Co-Authors: Ming-fen Lee, Meiling Tsai, Anchin Cheng, Min Lung Liu, Wen Shiung Liou, Min-hsiung PanAbstract:Pterostilbene, found in grapes and berries, exhibits pleiotropic effects, including anti-inflammatory, antioxidant, and anti-proliferative activities. This study was conducted to investigate the effect of Pterostilbene on liver fibrosis and the potential underlying mechanism for such effect. Sprague-Dawley rats were intraperitoneally given dimethyl n-nitrosamine (DMN) (10mg/kg) 3 days per week for 4 weeks. Pterostilbene (10 or 20mg/kg) was administered by oral gavage daily. Liver function, morphology, histochemistry, and fibrotic parameters were examined. Pterostilbene supplementation alleviated the DMN-induced changes in the serum levels of alanine transaminase and aspartate transaminase (p
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chemopreventive effects of Pterostilbene on urethane induced lung carcinogenesis in mice via the inhibition of egfr mediated pathways and the induction of apoptosis and autophagy
Journal of Agricultural and Food Chemistry, 2012Co-Authors: Min-hsiung Pan, Rong-jane Chen, Shang Jie Tsai, Ying-jan WangAbstract:Lung cancer is the most commonly diagnosed cancer and the leading cause of cancer deaths globally. Due to the lack of successful chemopreventive agents for lung cancer, there is an emerging need to evaluate new and effective agents for lung cancer prevention. Pterostilbene, a naturally occurring analogue of resveratrol, has been reported to be an effective chemopreventive agent against many cancers. The aim of this study is to investigate the chemopreventive effects of Pterostilbene in urethane-induced murine lung tumors. Pretreatment with Pterostilbene at 50 or 250 mg/kg significantly reduced tumor multiplicity by 26 and 49%, respectively. Pterostilbene also significantly inhibited tumor volume by 25 and 34% and decreased the tumor burden per mouse by 45 and 63%, respectively. The mechanisms by which Pterostilbene suppresses lung tumorigenesis have been investigated in lung tissues and homogenates. The results indicate that the Pterostilbene-mediated chemopreventive effects in vivo were a result of the i...
Vladimir Badmaev - One of the best experts on this subject based on the ideXlab platform.
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Pterostilbene inhibits colorectal aberrant crypt foci acf and colon carcinogenesis via suppression of multiple signal transduction pathways in azoxymethane treated mice
Journal of Agricultural and Food Chemistry, 2010Co-Authors: Yi Siou Chiou, Vladimir Badmaev, Ying-jan Wang, Meiling Tsai, Anchin Cheng, Wei Ming Lai, Min-hsiung PanAbstract:Pterostilbene (PS), a natural dimethylated analogue of resveratrol, is known to have diverse pharmacologic activities including anticancer, anti-inflammation, antioxidant, apoptosis, antiproliferation, and analgesic potential. This paper reports the inhibitory effect of dietary administration of Pterostilbene against the formation of azoxymethane (AOM)-induced colonic aberrant crypt foci (ACF) preneoplastic lesions and adenomas in male ICR mice and delineates its possible molecular mechanisms. ICR mice were given two AOM injections intraperitoneal and continuously fed a 50 or 250 ppm Pterostilbene diet for 6 or 23 weeks. It was found that the dietary administration of Pterostilbene effectively reduced AOM-induced formation of ACF and adenomas and inhibited the transcriptional activation of iNOS and COX-2 mRNA and proteins in mouse colon stimulated by AOM. Treatment with Pterostilbene resulted in the induction of apoptosis in mouse colon. Moreover, administration of Pterostilbene for 23 weeks significantly...
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structural identification of mouse urinary metabolites of Pterostilbene using liquid chromatography tandem mass spectrometry
Rapid Communications in Mass Spectrometry, 2010Co-Authors: Xi Shao, Xiaoxin Chen, Vladimir Badmaev, Shengmin SangAbstract:Pterostilbene, the dimethoxy derivative of resveratrol, has drawn much attention recently due to its potential beneficial health effects. The metabolic fate of Pterostilbene, however, is not well understood. In the present study, we identified nine novel mouse urinary Pterostilbene metabolites, Pterostilbene glucuronide, Pterostilbene sulfate, mono-demethylated Pterostilbene glucuronide, mono-demethylated Pterostilbene sulfate, mono-hydroxylated Pterostilbene, mono-hydroxylated Pterostilbene glucuronide, mono-hydroxylated Pterostilbene sulfate, and mono-hydroxylated Pterostilbene glucuronide sulfate, using liquid chromatography/atmospheric pressure chemical ionization and electrospray ionization tandem mass spectrometry. The structures of these metabolites were confirmed by analyzing the MS(n) (n = 1-3) spectra. To our knowledge, this is the first report of the identification of urinary metabolites of Pterostilbene in mice.
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Structural identification of mouse urinary metabolites of Pterostilbene using liquid chromatography/tandem mass spectrometry.
Rapid communications in mass spectrometry : RCM, 2010Co-Authors: Xi Shao, Xiaoxin Chen, Vladimir Badmaev, Shengmin SangAbstract:Pterostilbene, the dimethoxy derivative of resveratrol, has drawn much attention recently due to its potential beneficial health effects. The metabolic fate of Pterostilbene, however, is not well understood. In the present study, we identified nine novel mouse urinary Pterostilbene metabolites, Pterostilbene glucuronide, Pterostilbene sulfate, mono-demethylated Pterostilbene glucuronide, mono-demethylated Pterostilbene sulfate, mono-hydroxylated Pterostilbene, mono-hydroxylated Pterostilbene glucuronide, mono-hydroxylated Pterostilbene sulfate, and mono-hydroxylated Pterostilbene glucuronide sulfate, using liquid chromatography/atmospheric pressure chemical ionization and electrospray ionization tandem mass spectrometry. The structures of these metabolites were confirmed by analyzing the MS(n) (n = 1-3) spectra. To our knowledge, this is the first report of the identification of urinary metabolites of Pterostilbene in mice.
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Pterostilbene inhibited tumor invasion via suppressing multiple signal transduction pathways in human hepatocellular carcinoma cells
Carcinogenesis, 2009Co-Authors: Yi Siou Chiou, Vladimir Badmaev, Weijen Chen, Ju Ming Wang, Chitang HoAbstract:Pterostilbene, a natural dimethylated analog of resveratrol, is known to have diverse pharmacologic activities including anticancer, anti-inflammation, antioxidant, apoptosis, anti-proliferation and analgesic potential. However, the effects of Pterostilbene in preventing invasion of cancer cells have not been studied. Here, we report our finding that Pterostilbene significantly suppressed 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced invasion, migration and metastasis of human hepatoma cells (HepG 2 cells). Increase in the enzyme activity, protein and messenger RNA levels of matrix metalloproteinase (MMP)-9 were observed in TPA-treated HepG 2 cells, and these were blocked by Pterostilbene. In addition, Pterostilbene can inhibit TPA-induced expression of vascular endothelial growth factor, epidermal growth factor and epidermal growth factor receptor. Transient transfection experiments also showed that Pterostilbene strongly inhibited TPA-stimulated nuclear factor kappa B (NF-κB) and activator protein-1 (AP-1)-dependent transcriptional activity in HepG 2 cells. Moreover, Pterostilbene can suppress TPA-induced activation of extracellular signal-regulated kinase 1/2, p38 mitogen-activated protein kinase, c-Jun N-terminal kinases 1/2 and phosphatidylinositol 3-kinase/Akt and protein kinase C that are upstream of NF-κB and AP-1. Significant therapeutic effects were further demonstrated in vivo by treating nude mice with Pterostilbene (50 and 250 mg/kg intraperitoneally) after inoculation with HepG 2 cells into the tail vein. Presented data reveal that Pterostilbene is a novel, effective, anti-metastatic agent that functions by down-regulating MMP-9 gene expression.
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Pterostilbene suppressed lipopolysaccharide induced up expression of inos and cox 2 in murine macrophages
Journal of Agricultural and Food Chemistry, 2008Co-Authors: Min-hsiung Pan, Yen-hui Chang, Meiling Tsai, Ching Shu Lai, Vladimir BadmaevAbstract:Pterostilbene, an active constituent of blueberries, is known to possess anti-inflammatory activity and also to induce apoptosis in various types of cancer cells. Here, we investigated the inhibitory effects of Pterostilbene on the induction of NO synthase (NOS) and cyclooxygenase-2 (COX-2) in murine RAW 264.7 cells activated with lipopolysaccharide (LPS). Western blotting and real-time polymerase chain reaction (PCR) analyses demonstrated that Pterostilbene significantly blocked the protein and mRNA expression of iNOS and COX-2 in LPS-induced macrophages. Treatment with Pterostilbene resulted in the reduction of LPS-induced nuclear translocation of the nuclear factor-κB (NFκB) subunit and the dependent transcriptional activity of NFκB by blocking phosphorylation of inhibitor κB (IκB)α and p65 and subsequent degradation of IκBα. Transient transfection experiments using NFκB reporter constructs indicated that Pterostilbene inhibits the transcriptional activity of NFκB in LPS-stimulated mouse macrophages. W...
María P. Portillo - One of the best experts on this subject based on the ideXlab platform.
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Activity of Pterostilbene Metabolites against Liver Steatosis in Cultured Hepatocytes
Molecules (Basel Switzerland), 2020Co-Authors: Jenifer Trepiana, Stéphanie Krisa, María P. PortilloAbstract:Pterostilbene is a dimethyl ether derivative of resveratrol, less metabolized than its analogue, due to the substitution of two hydroxyl groups with methoxyl groups. Nevertheless, the amounts of Pterostilbene phase II metabolites found in plasma and tissues are higher than those of the parent compound. The first aim of this study was to assess whether Pterostilbene-4'-O-glucuronide (PT-G) and Pterostilbene-4'-O-sulfate (PT-S) were able to prevent triglyceride accumulation in AML12 (alpha mouse liver 12) hepatocytes. This being the case, we aimed to analyze the mechanisms involved in their effects. For this purpose, an in vitro model mimicking the hepatocyte situation in fatty liver was developed by incubating mouse AML12 hepatocytes with palmitic acid (PA). For cell treatments, hepatocytes were incubated with 1, 10 or 25 µM of Pterostilbene, Pterostilbene-4'-O-glucuronide or Pterostilbene-4'-O-sulfate for 18 h. Triglycerides and cell viability were assessed by a commercial kit and crystal violet assay, respectively. Protein expression of enzymes and transporters involved in triglyceride metabolism was analyzed by immunoblot. The results showed for the first time the anti-steatotic effect of Pterostilbene metabolites and thus, that they contribute to the preventive effect induced by Pterostilbene on steatosis in in vivo models. This anti-steatotic effect is mainly due to the inhibition of de novo lipogenesis.
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Pterostilbene Inhibits Lipogenic Activity similar to Resveratrol or Caffeine but Differently Modulates Lipolysis in Adipocytes.
Phytotherapy research : PTR, 2017Co-Authors: Saioa Gómez-zorita, María P. Portillo, Chloé Belles, Anaïs Briot, Alfredo Fernández-quintela, Christian CarpénéAbstract:The anti-obesity effects of resveratrol shown in rodents are not transposed into an efficient therapy of human obesity. Consequently, the search for molecules mimicking or surpassing resveratrol actions is ongoing. The natural phenolic compound Pterostilbene exhibits beneficial health effects and has the capacity to limit fat mass in animal models. In this study, we tested whether Pterostilbene modulates triacylglycerol accumulation/breakdown. Prolonged exposure to Pterostilbene or resveratrol inhibited adipocyte differentiation in 3T3-F442A preadipocytes. Acute effects on lipolysis, antilipolysis and lipogenesis were determined for Pterostilbene in mouse adipocytes, and compared with resveratrol. Pterostilbene was also tested on glycerol release and glucose uptake in subcutaneous human adipocytes. Dose–response analyses did not reveal a clear lipolytic effect in both species. The antilipolytic effect of insulin was improved by Pterostilbene at 1–10 μM in mouse fat cells only, while at 1 mM, the phenolic compound was antilipolytic in human fat cells in a manner not additive to insulin. Pterostilbene dose-dependently inhibited glucose incorporation into lipids similarly to resveratrol and caffeine. However, only the former did not inhibit insulin-stimulated glucose uptake. Indeed, Pterostilbene abolished the insulin lipogenic effect without inhibiting its antilipolytic action and rapid activation of glucose uptake. Pterostilbene therefore exhibits a unique panel of direct interactions with adipocytes that relies on its reported anti-obesity and antidiabetic properties. Copyright © 2017 John Wiley & Sons, Ltd.
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Pterostilbene a dimethyl ether derivative of resveratrol reduces fat accumulation in rats fed an obesogenic diet
Journal of Agricultural and Food Chemistry, 2014Co-Authors: Saioa Gomezzorita, Alfredo Fernandezquintela, Leixuri Aguirre, Arrate Lasa, Agnes M. Rimando, María P. PortilloAbstract:The current study aimed to demonstrate the effects of Pterostilbene in rats fed an obesogenic diet. For this purpose, Pterostilbene was administered at doses of 15 mg/kg body weight/day (PT15 group) or 30 mg/kg body weight/day (PT30 group) for 6 weeks. Pterostilbene reduced adipose tissue mass −15.1% (PT15) and −22.9% (PT30). In this tissue, it decreased malic enzyme (−39.4 and −49.5% for PT15 and PT30 groups, respectively) and fatty acid synthase (−45 and −53.4% for PT15 and PT30) activities. Acetyl-CoA carboxylase activity was reduced and AMPK activity was increased only in the PT30 group. In the liver, Pterostilbene (PT30) reduced malic enzyme (−29.5%) and glucose-6-P dehydrogenase (−43.2%) activities and increased carnitine palmitoyltransferase-1a (37.5%) and acyl-coenzyme A oxidase (42.5%) activities. This increased oxidative capacity was not associated with increased mitochondriogenesis. Among biochemical serum parameters, only insulin was modified by Pterostilbene (−31.6%) in the PT15 group. The am...
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Pterostilbene a dimethyl ether derivative of resveratrol reduces fat accumulation in rats fed an obesogenic diet
Journal of Agricultural and Food Chemistry, 2014Co-Authors: Saioa Gomezzorita, Alfredo Fernandezquintela, Leixuri Aguirre, Arrate Lasa, Agnes M. Rimando, María P. PortilloAbstract:The current study aimed to demonstrate the effects of Pterostilbene in rats fed an obesogenic diet. For this purpose, Pterostilbene was administered at doses of 15 mg/kg body weight/day (PT15 group) or 30 mg/kg body weight/day (PT30 group) for 6 weeks. Pterostilbene reduced adipose tissue mass -15.1% (PT15) and -22.9% (PT30). In this tissue, it decreased malic enzyme (-39.4 and -49.5% for PT15 and PT30 groups, respectively) and fatty acid synthase (-45 and -53.4% for PT15 and PT30) activities. Acetyl-CoA carboxylase activity was reduced and AMPK activity was increased only in the PT30 group. In the liver, Pterostilbene (PT30) reduced malic enzyme (-29.5%) and glucose-6-P dehydrogenase (-43.2%) activities and increased carnitine palmitoyltransferase-1a (37.5%) and acyl-coenzyme A oxidase (42.5%) activities. This increased oxidative capacity was not associated with increased mitochondriogenesis. Among biochemical serum parameters, only insulin was modified by Pterostilbene (-31.6%) in the PT15 group. The amounts of Pterostilbene in serum and tissues from rats in the PT30 group were in not all cases 2-fold greater than those found in the PT15 group. In conclusion, Pterostilbene shows antiobesity properties due, at least in part, to reduced lipogenesis in adipose tissue and increased fatty acid oxidation in liver.
