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pterostilbene
PHYTOTHERAPY RESEARCH · 2023 · IF 7.2

Pterostilbene could alleviate diabetic cognitive impairment by suppressing TLR4/NF-кB pathway through microbiota-gut-brain axis

Zhi-Tong Zhang,Si-Min Deng,Chong Chen,Qing-Hui He,Xian-Wu Peng,Qing-Feng Liang,Guo-Dong Zhuang,Shu-Mei Wang,Dan Tang

Diabetic cognitive impairment (DCI) is a serious neurodegenerative disorder caused by diabetes, with chronic inflammation being a crucial factor in its pathogenesis. Pterostilbene is a well-known natural stilbene derivative that has excellent anti-inflammatory activity, suggesting its potential medicinal advantages for treating DCI. Therefore, this study is to explore the beneficial effects of pterostilbene for improving cognitive dysfunction in DCI mice. A diabetic model was induced by a high-fat diet plus streptozotocin (40 mg·kg −1 ) for consecutive 5 days. After the animals were confirmed to be in a diabetic state, they were treated with pterostilbene (20 or 60 mg·kg −1 , i.g.) for 10 weeks. Pharmacological evaluation showed pterostilbene could ameliorate cognitive dysfunction, regulate glycolipid metabolism disorders, improve neuronal damage, and reduce the accumulation of β-amyloid in DCI mice. Pterostilbene alleviated neuroinflammation by suppressing oxidative stress and carbonyl stress damage, astrocyte and microglia activation, and dopaminergic neuronal loss. Further investigations showed that pterostilbene reduced the level of lipopolysaccharide, modulated colon and brain TLR4/NF-κB signaling pathways, and decreased the release of inflammatory factors, which in turn inhibited intestinal inflammation and neuroinflammation. Furthermore, pterostilbene could also improve the homeostasis of intestinal microbiota, increase the levels of short-chain fatty acids and their receptors, and suppress the loss of intestinal tight junction proteins. In addition, the results of plasma non-targeted metabolomics revealed that pterostilbene could modulate differential metabolites and metabolic pathways associated with inflammation, thereby suppressing systemic inflammation in DCI mice. Collectively, our study found for the first time that pterostilbene could alleviate diabetic cognitive dysfunction by inhibiting the TLR4/NF-κB pathway through the microbiota-gut-brain axis, which may be one of the potential mechanisms for its neuroprotective effects.

研究领域: 药理学 · 神经科学 · 免疫学 · 代谢组学 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF NUTRITIONAL BIOCHEMISTRY · 2026 · IF 5.2

Pterostilbene targets microglia-mediated neuroinflammation for Alzheimer therapy

Feichi Chen,Xinhuang Lv,Kun Xiang,Xiaoou Lin,Conghui Dai,Chuhua Wei,Yang Zhang,Jiaming Liu,Jing Li

Microglia-mediated neuroinflammation is a key driver of Alzheimer’s disease (AD) progression, exacerbating neuronal damage and pathological changes. Pterostilbene (PTE), a natural anti-inflammatory stilbenoid, shows neuroprotective potential in AD, but its specific mechanism in regulating AD-related neuroinflammation remains unclear. Here, we explored the anti-neuroinflammatory effect and mechanisms of PTE against AD. APPswe/PS1dE9 (APP/PS1) transgenic mice were treated intragastrically with PTE for 4 weeks, followed by evaluation of cognitive function and pathological changes. Amyloid-β (Aβ) burden, Tau protein phosphorylation, microglial activation and proinflammatory cytokines production were analyzed. To further investigate the potential mechanism of PTE, an integrated approach combining network pharmacology, RNA sequencing, molecular docking, molecular dynamics simulations, and cell transfection techniques were conducted. Our results showed that PTE treatment improved cognitive impairment, Aβ deposits, Tau protein phosphorylation, microglia activation, and production of tumor necrosis factor (TNF)-α, interleukin (IL)-1β and IL-6 in vivo and in vitro. Notably, molecular docking predicted that PTE has binding affinity for JAK2 at LYS-857, LYS-882, and LEU-932. Consistently, site-directed mutagenesis reduced the inhibitory effect of PTE on JAK2/STAT3 phosphorylation, supporting JAK2 as a functional target. Meanwhile, we revealed that PTE effectively inhibited activation of microglia in the APP/PS1 mice by regulating JAK2-STAT3 pathway. These findings indicate that PTE treatment could attenuate microglia-mediated neuroinflammation via regulating JAK2-STAT3 signaling pathway, which might provide a novel option to elucidate the effects of PTE on AD.

✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2022 · IF 6.51

Self-assembled micelle derived from pterostilbene ameliorate acute inflammatory bowel disease

Hongyao Zhong,Huanxiao Zhang,Yiwei Hu,Shoukai He,Huiting Qu,Jie He,Jianqing Chen,Jinghua Chen,Leyao Zhang,Chao Deng

PEGylated pterostilbene micelle (PTENPs) with higher bioavailability, biocompatibility, and water solubility were prepared. Then we detected the therapeutic effects in the treatment of inflammatory bowel disease (IBD), together with its potential mechanisms. The anti-oxidant effects and anti-inflammatory effects of PTENPs were determined under in vitro and in vivo conditions. Besides, the cellular toxicity of the PTENPs was determined in vitro , and biocompatibility testing was performed on a colitis mice model to determine its safety. The self-assembled PTENPs showed potency in treating IBD, which was featured by effectively anti-oxidant capacity, inhibition of cellular damages, and an anti-inflammatory role. In addition, PTENPs could inhibit the activation of TLR4, thereby inhibiting the NF-κB and MAPK signaling pathways. Meanwhile, it could protect colonic tissues from oxidative damage, which promoted the remission of colonic inflammation with low toxicity. Compared with free PTE, PTENPs could effectively ameliorate acute IBD with low toxicity, which may be related to the inactivation of TLR4, and inhibition of NF-κB and MAPK signaling pathways.

CAS / MDL: 38215-36-0
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD HYDROCOLLOIDS · 2023 · IF 10.7

Pterostilbene binding to whey protein: Multi-spectroscopy and the antioxidant activity

Xiuping Liang,Long Chen,Zipei Zhang,Ruojie Zhang,David Julian McClements,Zhenlin Xu,Man Meng,Zhengyu Jin

In this study, Pterostilbene (Pte) was incorporated into whey protein isolate (WPI) to form a whey protein isolate-pterostilbene (WPI-Pte) complex. The interaction mechanism between these two components and its impact on the antioxidant performance of Pte were investigated through multispectral techniques and molecular docking. UV and fluorescence analyses revealed a distinct fluorescence static quenching mechanism of WPI by Pte, resulting in the formation of a complex with a 1:1 M ratio. Thermodynamic parameter assessments indicated that the interaction between Pte and WPI is a spontaneous non-covalent binding process, primarily driven by hydrophobic interactions, followed by hydrogen bonding. Molecular docking confirmed that Pte molecules become stably embedded within hydrophobic pockets formed by amino acid residues of the protein after interacting with protein and are surrounded by these residues. DPPH and ABTS free radical scavenging assays demonstrated that the binding of WPI and Pte enhances the antioxidant capacity by more than fourfold compared to free Pte. This study provides insights into the interaction, modification, and development of novel polyphenol antioxidant systems, thereby effectively harnessing its physiological benefits.

研究领域: 食品科学 · 生物化学
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Food Bioscience · 2024 · IF 4.8

Whey protein nanoparticles: Enhancing solubility, environmental resistance, and bio-accessibility of pterostilbene

Xiuping Liang,David Julian McClements,Zhengyu Jin,Long Chen

Pterostilbene (Pte) is a dietary phenolic compound derived from plants that offers numerous physiological advantages. Nonetheless, its low water solubility and limited oral bioavailability restrict its bioactivity. To address these limitations, nanoparticles were prepared using anti-solvent precipitation method. Optimal nanoparticles were achieved at a 10:1 mass ratio of whey protein isolate (WPI) to Pte, resulting in a particle size of 104.54 nm, a polydispersity index of 0.42, and an impressive encapsulation efficiency of Pte at 85.02%. The water solubility of Pte in the nanoparticles was found to be 53.14 times higher than that of free Pte and remained stable under various environmental conditions. Furthermore, the DPPH and ABTS + free radical scavenging activities of the nanoparticles were maximized at 55.58% and 92.97%, respectively. Pte release from WPI-Pte nanoparticles was well-fitted to Korsmeyer-Peppas model and followed a non-Fickian mechanism controlled by both diffusion and erosion. This environmentally friendly, straightforward, and efficient approach shows promise for large-scale production of Pte products with amplified health benefits.

CAS / MDL: 1898-66-4 28752-68-3
研究领域: 食品科学 · 药理学 · 纳米技术
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EUROPEAN POLYMER JOURNAL · 2021 · IF 4.598

Synthesis and properties of biobased mono-benzoxazine resins from natural renewable pterostilbene

Yin Lu,Kan Zhang

Two novel fully biobased mono-benzoxazine resins have been designed and synthesized using pterostilbene , furfurylamine/stearylamine and paraformaldehyde via a solventless reaction. The structures of newly obtained mono-benzoxazine monomers have been characterized by nuclear magnetic resonance (NMR) spectroscopy, Fourier transform infrared (FT-IR) spectroscopy and high-resolution mass spectrometry (HR-MS). The detailed assignments for oxazine-ring protons and carbons in each benzoxazine are identified using 1 H– 13 C heteronuclear multiple quantum coherence spectroscopy (HMQC). Besides, the polymerization processes of benzoxazine resins are studied by differential scanning calorimetry (DSC) and in situ FT-IR spectroscopy, and the thermal stability of their corresponding polybenzoxazines are investigated by thermogravimetric analysis (TGA). Moreover, coatings of both polybenzoxazines on glass slides and low-carbon steels have also been prepared to evaluate their anticorrosion performance. The results indicate that both polybenzoxazines possess good thermal stability and can play efficient roles for shielding corrosion as coatings. Therefore, the current study highlights the utility of the natural renewable pterostilbene as a promising candidate to prepare high-performance bio-based polybenzoxazines.

研究领域: 材料科学 · 有机化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Electrospun pullulan nanofibers containing pterostilbene-hydroxypropyl-β-cyclodextrin inclusion complex: Preparation and characterization

Yuanyuan Bao,Dan Yang,Hui Liu,Shujing Li,Hong Meng

Preservative-free dry masks made from natural active ingredients have attracted much attention in the spirit of safety and environmental protection, which should be in line with the future trend of skin care products. Pterostilbene (PTS) is a natural antioxidant ingredient derived from plants that has received great interest in the field of biomedicine and cosmetics. However, the low water solubility and stability of PTS limiting its wide application. In this study, we first self-assembled Pterostilbene (PTS) and hydroxypropyl-β-cyclodextrin (HP-β-CD) into water-soluble inclusion complexes (IC) to solve the solubility problem of Pterostilbene. The dry mask (PUL-PTS-HP-β-CD-NF) was then successfully produced using electrostatic spinning technology via combining IC with pullulan polysaccharide as co-spinning agents. The PUL-PTS-HP-β-CD-NF masks were detailedly analyzed using SEM, FTIR, and XRD, and the antioxidant capacity, water retention capacity, in vitro release, and safety were comprehensively assessed at the same time. The results showed that the nanofiber mask (PUL-PTS-HP-β-CD-NF) was dense, uniform, and well-distributed, which exhibited a higher level of antioxidant activity compared to isolated PTS counterparts. As the IC increases, the water retention capacity of the PUL-PTS-HP-β-CD-NF mask becomes more evident, and the in vitro dissolving studies further demonstrated that the release of PTS from PUL-PTS-HP-β-CD-NF was concentration-dependent, which exhibited a direct relationship with time and followed a kinetic model of first-order reaction. In addition, the biosafety of the nanofiber mask was confirmed using red blood cell hemolysis. This work not only provide a very novel approach to prepare dry mask but also offer a sustainable way to create environmentally-friendly chemicals.

CAS / MDL: 537-42-8
研究领域: 化妆品科学 · 材料科学 · 生物医药
✓ 已验证 产品关联 DOI PubMed 高影响因子
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AQUACULTURE INTERNATIONAL · 2025 ·Vol. 33 ·期 7 ·1-22 · IF 2.4

Pterostilbene feeding experiment on Litopenaeus vannamei: network pharmacology, molecular docking, and physiological enhancement mechanism

Chen Zhengxu,Jing Futao,Zhang Tengwen,Yu Xin,Liao Liwen,Li Yaobing,Wen Yuxin,Pan Luqing

This study integrates network pharmacology, molecular docking, and a 56-day feeding trial to evaluate the effects of dietary pterostilbene (PTE) on growth, physiological status, and underlying regulatory pathways in Litopenaeus vannamei . The results indicate that dietary supplementation with a specific dose of PTE enhances shrimp growth, improves metabolic capacity, boosts antioxidant defenses, strengthens immune responses, and reduces inflammation. The regulatory mechanism of PTE involves targeting and binding to key proteins in lipid metabolism-related signaling pathways, including AKT , INSR , and SIRT1 within the insulin and SIRT1 - AMPK pathways. This binding significantly increases the gene expression levels of these targets ( P  < 0.05), thereby activating the respective signaling pathways and enhancing glycolipid metabolism capacity. In terms of immune function, PTE targets and binds to key antioxidants and immune proteins, including Nrf2 , Relish , and Dorsal , resulting in a significant increase in the expression levels of these genes ( P  < 0.05). Consequently, the expression of downstream antioxidant enzymes associated with Nrf2 ( SOD , CAT , GPX ) was significantly elevated ( P  < 0.05), enhancing antioxidant capacity. Additionally, the expression of antibacterial lysosomal factors ( PEN3 , CRU , ALF , and LYC ) also increased ( P  < 0.05), thereby strengthening immune function. Moreover, dietary PTE reshapes the structure of gut microbiota and increases the abundance of beneficial bacteria. This study elucidates the molecular mechanisms and optimal dosage of dietary PTE in improving the physiological function of shrimp by combining molecular docking with in vivo findings, providing a theoretical basis for the development of efficient and safe aquaculture feed additives.

CAS / MDL: 537-42-8
研究领域: 水产养殖 · 分子生物学 · 营养生理学 · 免疫学 · 生物信息学 · 药理学
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FOOD RESEARCH INTERNATIONAL · 2024 · IF 7

Enhancing the water dispersibility and intestinal targeting of pterostilbene using tannic acid-whey protein conjugates

Xiuping Liang,Linlang Zhou,Yetong Zhang,Bohan Yang,David Julian McClements,Zhengyu Jin,Long Chen

In this study, three types of whey protein isolate (WPI)-tannic acid (TA) covalent conjugates (WPI-TA) were synthesized via alkaline treatment, free radical-induced method, and laccase induction. These conjugates were subsequently utilized in the antisolvent precipitation method to encapsulate pterostilbene (Pte). The structural and functional properties of these conjugates as carriers for intestinal-targeted Pte delivery were thoroughly evaluated. SDS-PAGE, total phenolic content measurement, grafting efficiency, and FT-IR analysis confirmed the successful formation of three distinct covalent conjugates. Among them, the laccase-induced WPI-TA conjugates exhibited the highest TA grafting efficiency. The particle size of this conjugate was measured at 115.25 nm with a PDI of 0.31. Upon encapsulation of Pte, this conjugate exhibited superior thermal stability, enhanced antioxidant properties, and sustained release within the gastrointestinal tract. The water solubility of Pte in these nanoparticles was found to be 361.19 times higher than that of free Pte, presenting a promising strategy for targeted intestinal delivery of Pte.

CAS / MDL: 1707-75-1 28752-68-3
研究领域: 食品科学 · 药学 · 纳米技术 · 生物技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2022 · IF 3.682

Electrospun membranes of carboxylated poly(ester urethane)urea/gelatin encapsulating pterostilbene for adaptive and antioxidative purposes

Leilei Zang,Quhan Cheng,Shan Bai,Kai Wang,Xiaoyan Yuan

Oxidative stress caused by the harsh microenvironment after implantation of an artificial graft with mismatching mechanical properties usually triggers inflammation responses, which have adverse impacts on tissue regeneration. For coping with these problems, in this work, bioactive fibrous scaffolds were developed from specially synthesized carboxylated poly(ester urethane)urea (PEUU) and gelatin (Gel) by encapsulating pterostilbene (Pte) for the first time. The prepared electrospun membranes exhibited self-adaptable mechanical properties with high elasticity owing to the bonded electrospun fibers, cross-linking network between PEUU and Gel, and the inherent flexibility of the PEUU polymer in the fibrous matrix. The PEUU/Gel/Pte electrospun membrane containing 7% Pte could promote in vitro proliferation of human umbilical vein endothelial cells, and regulate vascular smooth muscle cells with excellent antioxidant properties via free radical scavenging. In vivo results in a rat subcutaneous implantation model further demonstrated the positive effect of the specially prepared PEUU/Gel/Pte scaffold on both normal cell growth and anti-inflammatory by promoting cellularization and polarizing macrophages toward the M2 phenotype. These PEUU/Gel/Pte electrospun membranes with adaptability benefit to tissue regeneration by modulating inflammation responses, especially applications in vascular regeneration.

CAS / MDL: 7722-84-1 477-73-6
研究领域: 生物材料 · 组织工程 · 生物医学工程 · 药剂学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Antioxidants · 2022 ·Vol. 11 ·期 12 ·2360 · IF 7.675

Pterostilbene Ameliorates Fumonisin B1-Induced Cytotoxic Effect by Interfering in the Activation of JAK/STAT Pathway

Jian Jin,Yiyi Shan,Liangliang Zhang,Zhengchang Wu,Shenglong Wu,Mingan Sun,Wenbin Bao

Fumonisin B1 (FB1) is a mycotoxin that poses a great threat to agricultural production and the health of humans and animals. Pterostilbene (PTE) is a natural plant polyphenolic compound with good anti-inflammatory, antioxidant and cell regeneration effects, yet its effectiveness in treating FB1-induced cytotoxicity remains to be explored. In this study, we used porcine alveolar macrophages (3D4/21) as a model to characterize the cytotoxicity induced by FB1, and to investigate the potential alleviating effect of PTE on FB1-induced cytotoxicity. We demonstrate that FB1 induces cytotoxicity, apoptosis, pro-inflammatory cytokine production and mitochondrial damage, which can be largely recovered by PTE treatment, suggesting the promising application of PTE to treat FB1-induced damage. Mechanistically, FB1 activates the JAK/STAT signaling pathway, while PTE attenuates FB1-induced cytotoxicity through the inhibition of key JAK/STAT genes such asJAK2andSTAT3. Overall, our study characterized the molecular mechanism for FB1-induced cytotoxicity and found PTE to be a promising component which can alleviate FB1-induced cytotoxicity by interfering in the activation of JAK/STAT pathway.Keywords:fumonisin B1;pterostilbene;alveolar macrophage;cytotoxicity;JAK/STAT signaling pathway;pig

研究领域: 毒理学 · 药理学 · 细胞生物学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Food & Function · 2022 ·Vol. 13 ·期 19 ·9868-9877 · IF 6.317

Novel pterostilbene-loaded pro-phytomicelles: preclinical pharmacokinetics, distribution, and treatment efficacy against acetaminophen-induced liver injury

Lu Liu,Liping Zhou,Cuicui Wang,Zhixin Yuan,Qilong Cao,Mengshuang Li,Xianggen Wu

A novel pro-phytomicelle formulation with small molecule phytochemicals as nanomaterials was developed for the oral delivery of pterostilbene (PTE) in our previous work. The present report was designed to preclinically evaluate the in vivo oral bioavailability, organ and tissue distribution, as well as the strengthened efficacy against acetaminophen-induced liver damage of this novel formulation, named PTE pro-phytomicelles. After oral administration in rats, an improvement in the area under the curve (AUC)0→t of the PTE pro-phytomicelles (34832.25 vs. 13115.72 ng ml−1 h) and an increase in their maximum plasma concentration (Cmax) (4.940 vs. 2.175 μg ml−1), as compared with those of bare PTE, were observed. The organ and tissue distribution further showed that the PTE pro-phytomicelles could effectively increase the concentration of PTE in all the tested organs and gastrointestinal segments. In the efficacy evaluation, the overdose of Acetaminophen induced severe liver injury in mice, and the oral administration of PTE pro-phytomicelles could efficiently suppress ALT and AST levels in serum, restore histopathological changes, and result in more effective improvement against liver damage via oxidative stress and inflammation cytokine inhibition. The mechanism through which high-mobility group box 1 (HMGB1) signaling was regulated was involved in this treatment. These results reveal that PTE pro-phytomicelles could achieve significantly improved in vivo profiles than bare PTE, and these pro-phytomicelles might provide a new concept and promising therapeutic potential in terms of PTE nanomedicines.

研究领域: 药理学 · 纳米技术 · 肝病学 · 毒理学
✓ 已验证 DOI PubMed 高影响因子
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