Determination of naturally occurring resveratrol analog trans-4,4′-dihydroxystilbene in rat plasma by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study

Wan, Chen; Yeo, Samuel Chao Ming; Elhennawy, Mai Gamal; Xiang, Xiaoqiang; Lin, Hai‐Shu

doi:10.1007/s00216-015-8762-7

Cited by 34 publications

(31 citation statements)

References 22 publications

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“…Evaluate the effect of resveratrol on insulin resistance, glucose and lipid metabolism in non-alcoholic fatty liver disease (NAFLD) (Chen et al, 2015).…”

Section: Aim Treatment Resultsmentioning

confidence: 99%

Bioavailability of resveratrol: Possibilities for enhancement

Vries

Strydom²,

Steenkamp

2018

Journal of Herbal Medicine

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“…Evaluate the effect of resveratrol on insulin resistance, glucose and lipid metabolism in non-alcoholic fatty liver disease (NAFLD) (Chen et al, 2015).…”

Section: Aim Treatment Resultsmentioning

confidence: 99%

Bioavailability of resveratrol: Possibilities for enhancement

Vries

Strydom²,

Steenkamp

2018

Journal of Herbal Medicine

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“…In the recent years, considerable attention has been given to synthetic resveratrol derivatives, and numerous studies have reported that methoxylated, hydroxylated, and halogenated derivatives display more effective disease prevention characteristics than resveratrol . RV01 is the quinolyl‐substituted derivative of resveratrol.…”

Section: Discussionmentioning

confidence: 99%

A Novel Quinolyl‐Substituted Analogue of Resveratrol Inhibits LPS‐Induced Inflammatory Responses in Microglial Cells by Blocking the NF‐κB/MAPK Signaling Pathways

Hou

Zhang

et al. 2019

Molecular Nutrition Food Res

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Scope The anti‐neuroinflammatory effect of a novel quinolyl‐substituted analogue of resveratrol (RV01) on lipopolysaccharide (LPS)‐induced microglial activation is investigated, as well as the possible underlying mechanisms. Methods and results Cell viability is measured using an MTT assay. Nitric oxide (NO) release is determined by nitrite assay. The interaction between RV01 and inducible nitric oxide synthase (iNOS) is studied using molecular docking. Free radical scavenging activity and reactive oxygen species (ROS) production are determined by DPPH reduction assay and DCFH‐DA assay. Pretreatment with RV01 (1–30 µm) prior to LPS (1 µg mL–1) stimulation decreased NO release and iNOS expression without observable cytotoxicity. RV01 reduced the mRNA levels and secretion of tumor necrosis factor‐α (TNF‐α) and interleukin‐6 (IL‐6). RV01 also inhibited LPS‐induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation. Furthermore, RV01 decreases the protein expression of toll‐like receptor 4 (TLR4) and inhibits the LPS‐induced activation of the mitogen‐activated protein kinase (MAPK) and nuclear transcription factor‐κB (NF‐κB) signaling pathways. Additionally, conditioned medium from microglia co‐treated with LPS and RV01 alleviates the death of SH‐SY5Y cells induced by conditioned medium from activated N9 microglial cells. Lastly, a mouse neuroinflammation model is further used to confirm the effect of RV01 in vivo. Conclusion These results show that RV01 suppresses microglia‐mediated neuroinflammation and protects neurons from inflammatory damage, which indicates that RV01 has great potential as a nutritional preventive strategy for neuroinflammation‐related diseases.

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“…The jugular veins of the rats were cannulated for blood sampling and i.v. dosing according to a well‐established protocol in our laboratory (Yeo et al, ; Chen et al, ).…”

Section: Methodsmentioning

confidence: 99%

Isorhapontigenin, a bioavailable dietary polyphenol, suppresses airway epithelial cell inflammation through a corticosteroid‐independent mechanism

Yeo

Fenwick

Barnes

et al. 2017

British J Pharmacology

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*Equal contribution. BACKGROUND AND PURPOSEChronic obstructive pulmonary disease (COPD) is a corticosteroid-resistant airway inflammatory condition. Resveratrol exhibits anti-inflammatory activities in COPD but has weak potency and poor pharmacokinetics. This study aimed to evaluate the potential of isorhapontigenin, another dietary polyphenol, as a novel anti-inflammatory agent for COPD by examining its effects in vitro and pharmacokinetics in vivo. EXPERIMENTAL APPROACHPrimary human airway epithelial cells derived from healthy and COPD subjects, and A549 epithelial cells were incubated with isorhapontigenin or resveratrol and stimulated with IL-1β in the presence or absence of cigarette smoke extract. Effects of isorhapontigenin and resveratrol on the release of IL-6 and chemokine (C-X-C motif) ligand 8 (CXCL8), and the activation of NF-κB, activator protein-1 (AP-1), MAPKs and PI3K/Akt/FoxO3A pathways were determined and compared with those of dexamethasone. The pharmacokinetic profiles of isorhapontigenin, after i.v. or oral administration, were assessed in Sprague-Dawley rats. KEY RESULTSIsorhapontigenin concentration-dependently inhibited IL-6 and CXCL8 release, with IC 50 values at least twofold lower than those of resveratrol. These were associated with reduced activation of NF-κB and AP-1 and, notably, the PI3K/Akt/FoxO3A pathway, that was relatively insensitive to dexamethasone. In vivo, isorhapontigenin was rapidly absorbed with abundant plasma levels after oral dosing. Its oral bioavailability was approximately 50% higher than resveratrol. CONCLUSIONS AND IMPLICATIONSIsorhapontigenin, an orally bioavailable dietary polyphenol, displayed superior anti-inflammatory effects compared with resveratrol. Furthermore, it suppressed the PI3K/Akt pathway that is insensitive to corticosteroids. These favourable efficacy and pharmacokinetic properties support its further development as a novel anti-inflammatory agent for COPD. AbbreviationsA549, human alveolar epithelial cells; AP-1, activator protein-1; AUC 0!last , plasma exposure; Cl, clearance; C max , maximal plasma concentration; COPD, chronic obstructive pulmonary disease; CXCL8, chemokine (C-X-C motif) ligand 8; ECL, Enhanced chemiluminescence; F, absolute oral bioavailability; FoxO3A, forkhead box O3A; H 2 DCF-DA, 2′,7′-dichlorodihydrofluorescein diacetate; MTT 0!last , mean transition time; TBS, Tris balanced salt solution

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Determination of naturally occurring resveratrol analog trans-4,4′-dihydroxystilbene in rat plasma by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study

Cited by 34 publications

References 22 publications

Bioavailability of resveratrol: Possibilities for enhancement

Bioavailability of resveratrol: Possibilities for enhancement

A Novel Quinolyl‐Substituted Analogue of Resveratrol Inhibits LPS‐Induced Inflammatory Responses in Microglial Cells by Blocking the NF‐κB/MAPK Signaling Pathways

Isorhapontigenin, a bioavailable dietary polyphenol, suppresses airway epithelial cell inflammation through a corticosteroid‐independent mechanism

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