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Polydatin
Pharmaceuticals · 2026 ·Vol. 19 ·期 5 ·659 · IF 5.7

Optimization of Polydatin Hydrolysis Process Through Response Surface Methodology for Efficient Resveratrol Production

Dong Wang,Yating Xiao,Xia Yang,Jie Cui,Yangyang Cai,Hua Chen

Background/Objectives:Resveratrol is a naturally occurring polyphenolic stilbene compound exhibiting a wide range of biological activities, and it has been extensively utilized as both a food additive and a pharmaceutical active ingredient. Typically, it can be directly extracted from natural sources such as grapes, mulberries, and peanuts, or obtained through catalytic hydrolysis of polydatin. To establish an efficient and optimized method for resveratrol production, we conducted a comprehensive study to refine the acid-catalyzed hydrolysis conditions of polydatin.Methods:A high-performance liquid chromatography method was developed for the quantitative determination of polydatin and resveratrol. To identify the optimal ranges of reaction temperature, HCl concentration, and ethanol concentration, single-factor experiments were conducted by evaluating their influences on hydrolysis kinetics and resveratrol yield. Based on these results, response surface methodology incorporating a Box–Behnken design was employed to optimize the hydrolysis process, using resveratrol yield as the response variable. Furthermore, time-course experiments were performed to determine the optimal reaction duration under the established optimal conditions.Results:Single-factor experiments demonstrated that increasing temperature and HCl concentration significantly accelerated hydrolysis, but resveratrol yield increased initially and then decreased with excessive increases in either factor. To further optimize the process, response surface methodology optimization experiments were conducted at temperatures of 60, 70, and 80 °C; HCl concentrations of 1.0, 1.5, and 2.0 M; and ethanol concentrations of 75%, 85%, and 95%. The optimal conditions were identified as follows: temperature, 70 °C; HCl concentration, 1.5 M; ethanol volume fraction 85%; and reaction time, 5 h. Under these conditions, the theoretical resveratrol yield was 85.68%, and the average yield from triplicate validation experiments was 86.01% (RSD = 0.56%), which was consistent with the theoretical value.Conclusions:The optimized acid-catalytic hydrolysis process using RSM is stable, feasible, and efficient, offering a promising approach for enhancing resveratrol production from polydatin.

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Frontiers in Cellular and Infection Microbiology · 2026 · IF 5.5

Polydatin as a natural ClpP modulator for combating methicillin-resistant Staphylococcus aureus infection

Ying Qin,Jingjing Yang,Guangming Wang,Luna Yang,Dacheng Wang,Yongxin Luan

IntroductionMethicillin resistant Staphylococcus aureus, MRSA, is a major cause of hospital acquired infections and poses a serious therapeutic challenge because of multidrug resistance and potent virulence. Targeting virulence rather than bacterial growth may provide an alternative strategy to combat MRSA infection. This study investigated polydatin, a stilbenoid glucoside from Polygonum cuspidatum, as a potential antivirulence agent targeting caseinolytic protease P, ClpP.MethodsClpP inhibitory activity was evaluated by enzymatic assay. The effects of polydatin on bacterial growth, hemolytic activity, virulence gene expression, adhesion to fibrinogen, and host cell invasion were assessed in vitro. Target engagement was examined by thermal shift assay, fluorescence quenching, and computational simulation. Therapeutic efficacy was evaluated in a murine pneumonia model.ResultsPolydatin showed limited antibacterial activity but significantly inhibited ClpP and reduced the expression of key virulence factors, including Hla, PVL, and RNAIII. It also impaired bacterial adhesion to fibrinogen and invasion of host cells. Binding studies supported the interaction between polydatin and ClpP. In vivo, polydatin markedly alleviated S. aureus induced pneumonia, as shown by reduced lung bacterial burden, lower inflammatory cytokine levels, and attenuated tissue injury.DiscussionPolydatin attenuates MRSA pathogenicity by targeting ClpP associated virulence regulation rather than bacterial viability. These findings identify polydatin as a promising antivirulence candidate and provide a basis for developing alternative therapeutic strategies against MRSA infections.

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Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy · 2020 ·Vol. 30 ·期 1 ·28-33 · IF 1.407

1H NMR Quantification of Polydatin and Emodin in Huganning, a Chinese Patent Herbal Medicine

Wang Cong,Zhang Pengpeng,Zhang Xiuli,Yu Mingming,Lv Zhihua

Huganning, a Chinese patent medicine, has been used in clinical practice for the treatment of hepatitis in China for more than 20 years, and its main physiologically active components are polydatin and emodin. In this study, a rapid and accurate proton nuclear magnetic resonance method for the quantification of these constituents was developed. 4-Nitrochlorobenzene was selected as an internal standard, and the signals for polydatin at δ 6.44 ppm and emodin at δ 7.54 ppm were chosen for the quantification. Validation of the method was performed in terms of specificity, precision, and stability. The results indicated that the method was precise and in line with the China Food and Drug Administration guidance. The method has been successfully applied to characterize tablets and capsules obtained from six pharmaceutical companies. This study indicated that the rapid 1 H NMR method is more suitable for the quality control of Huganning than the high-performance liquid chromatography method. Graphical Abstract

研究领域: 药学 · 中药学
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Food Bioscience · 2025 · IF 5.9

Polydatin mitigates seizures via mitochondrial protection: Mechanisms unraveled by network pharmacology and experimental validation

Yahong Cheng,Yi Ding,Ziyan Tang,Xiaoyi Lei,Yufang Ma,Mengxin Xia,Jiaying Li,Gaoge Hu,Jiahui Zhang,Jing Rao

This study investigated the antiepileptic effects of polydatin (PD) and its potential mechanisms. Racine scoring and EEG were used to assess seizure severity in a PTZ-induced mouse epilepsy model. The results demonstrated that PD significantly reduced the intensity of seizures. Behavioral tests revealed that PD improved learning, memory, and motor coordination. Histological analysis using HE and Nissl staining showed that PD alleviated hippocampal neuronal damage. TUNEL staining further confirmed that PD effectively prevented neuronal apoptosis. Network pharmacology predicted SIRT1 as a potential target of PD, and GO and KEGG pathway enrichment analyses indicated that PD regulated mitochondrial function. Therefore, PD may reduce neuronal damage by protecting mitochondrial function through SIRT1. This process was tested both in vitro and in vivo . In a Mg 2+ -free neuronal excitability model, CCK-8, LDH, and Hoechst staining results demonstrated that PD significantly increased cell survival and reduced apoptosis. Reduced mitosox staining, along with increased activity of Complexes IV and V and ATP production, indicated that PD mitigated mitochondrial function. Gene expression studies revealed that PD activated the SIRT1-PGC-1α signaling pathway via AMPK. In conclusion, PD exerted neuroprotective effects by regulating mitochondrial function, suggesting a potential therapeutic target for epilepsy.

CAS / MDL: 9004-32-4 92-84-2
研究领域: 药理学 · 神经科学 · 生物信息学
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JOURNAL OF ELECTROANALYTICAL CHEMISTRY · 2016 · IF 2.822

Electrochemical behavior of polydatin and its highly-sensitive determination based on graphene modified electrode

Yinfeng Li,Lu Wang,Haipeng Zhao,Lingzhi Du,Baoxian Ye

A voltammetric sensor for polydatin sensing was simply fabricated by in-situ electrochemically reducing graphene oxide at a glassy carbon electrode. The redox behavior of polydatin was investigated systematically. For the first time, the kinetics parameters of electrode reaction of polydatin were calculated using various electrochemical techniques. Significant electrochemical signal increases were achieved by the excellent conductivity and large surface area of reduced graphene oxide. Thereafter, a highly-sensitive electroanalytical method for polydatin was established with a good linear relationship from 4.0   ×   10 −   8   mol   L −   1 to 3.5   ×   10 −   6   mol   L −   1 and a detection limit of 4.0   ×   10 −   8   mol   L −   1 . In addition, the practical application of present method was demonstrated by determining the concentration of polydatin in real sample with satisfactory result.

研究领域: 分析化学 · 电化学
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BIOMEDICINE & PHARMACOTHERAPY · 2020 · IF 4.545

Polydatin attenuates hepatic stellate cell proliferation and liver fibrosis by suppressing sphingosine kinase 1

Tian Lan,Lihang Zhuang,Shengwen Li,Guizhi Yang,Yuanyuan Xuan,Jiao Guo

Sphingosine kinase 1 (SphK1) plays critical roles in the activation of hepatic stellate cells (HSCs) and liver fibrosis. Our previous study found that polydatin ameliorates chronic liver injury and fibrosis by inhibiting oxidative stress. However, whether polydatin exerts an anti-fibrotic effect on liver fibrosis dependent on SphK1 signaling is unknown. We aimed to investigate the role of polydatin in SphK1, which mediates HSC activation and liver fibrosis. C57BL/6 mice were induced using CCl 4 5 μL g −1 i.p. twice a week for 6 weeks and treated with or without polydatin. Human immortalized HSC line (LX-2) was induced using platelet-derived growth factor-BB (PDGF-BB) or adenovirus-SphK1 and treated with polydatin. Hepatic macrophage filtration, collagen deposition, expression of α-smooth muscle, active caspase-3, and terminal deoxynucleotidyl transferase dUTP nick end labeling-positive cells were markedly increased in mice induced by CCl 4 for 6 weeks. In contrast, polydatin attenuated collagen synthesis and hepatocyte apoptosis. Furthermore, polydatin exhibited significant anti-proliferative activity against PDGF-BB-induced activated hepatic stellate cells (HSCs). SphK1 was strongly induced in mice exposed to CCl 4 , whereas its expression and activity were inhibited by polydatin treatment. Finally, SphK1 overexpression in LX-2 cells promoted proliferation of activated HSCs, which could not be reversed by polydatin treatment. These results demonstrate that polydatin attenuates HSC proliferation and activation through inhibition of SphK1 signaling, contributing to the suppression of liver fibrosis.

研究领域: 药理学 · 肝病学 · 细胞生物学
✓ 已验证 DOI PubMed 高影响因子
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CELLULAR AND MOLECULAR BIOLOGY · 2019 ·Vol. 65 ·期 7 · IF 1.463

Ameliorative effect of polydatin on hyperglycemia and renal injury in streptozotocin-induced diabetic rats

Lijuan Wang,Liji Huang,Nan Li,Junjun Miao,Wei Liu,Jiangyi Yu

To investigate the effect of polydatin on glucose transporter, blood glucose homeostasis and renal injury in streptozotocin (STZ)-induced diabetic rats. The in vitro inhibitory effect of polydatin on sodium-glucose cotransporter-1 (SGLT1) and 2 (SGLT2) was determined using HEK293 cells. The inhibitory effect of polydatin on GLUT1 and GLUT4 was evaluated using 3T3-L1 adipocytes. Streptozotocin-induced diabetic rats were used for this study. Fasting blood glucose (FBG), glycosylated hemoglobin (HbA1c), urea nitrogen, serum creatinine and urinary protein were determined using biochemical analyzer. Histopathological examination was performed on renal tissue. Serum levels of interleukin 1β (IL-1β), tumor necrosis factor α (TNF-α), monocyte chemoattractant protein 1 (MCP-1) and C-reactive protein (CRP) were also determined. Polydatin significantly inhibited SGLT1/2 and exhibited high selectivity for both GLUT1 and GLUT4. It significantly and dose-dependently decreased hyperglycemia, enhanced urine glucose excretion in the diabetic rats. The polydatin treatment significantly ameliorated symptoms of DN such as polyuria, polydipsia and hyperphagia. The hypoglycemic effect of polydatin was maintained throughout the treatment period. In addition,the levels of IL-1β, TNF-α, MCP-1 and CRP were significantly reduced in treated group. Treatment with polydatin significantly ameliorated most of the structural and morphological changes induced by STZ. Moreover, the levels of urinary protein, serum creatinine and urea nitrogen were significantly reduced after treatment with polydatin.  As a potential dual inhibitor of SGLT1/2, polydatin has high selectivity for GLUT1 and GLUT4. Its long-term administration delays the development of DN, protects renal function and ameliorates renal tissue injury.

研究领域: 药理学 · 内分泌学 · 分子生物学
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Journal of Food Measurement and Characterization · 2023 ·Vol. 17 ·期 4 ·3918-3926 · IF 3.4

Polydatin-based natural product as an activatable molecular sensor toward viscosity detection in liquid

Xu Lingfeng,Zou Ying,Wu Kui,Han Runlin,Huang Yanrong,Yi Xiuguang

Effective and non-invasive inspection method toward viscosity is expected to ease the burden of continued increased health problems worldwide. Herein, we proposed that viscosity is one of the most important markers in the liquid microenvironment. Then, a natural product was further developed from resveratrol derivate, polydatin, as an activatable molecular sensor for monitoring liquid micro-environmental viscosity alterations for metamorphic extent determination. This natural molecular sensor was constructed by the single double bond alternating conjugate structure, which can rotate freely in the low viscosity media, and in the highly viscous media, bright fluorescent signals are specifically activated (around 383 nm, 53-fold), endowing the natural sensor with the capacity to avoid autofluorescence from the additives and achieving high signal-to-noise ratio imaging. With the lower detection limit 1.125 cP, the sensor polydatin exhibits higher viscosity sensitive coefficient (0.60), and 75.5 nm of Stokes shift was found in the distilled water. Afterward, polydatin achieved non-invasively identifying the thickening effects of food thickeners. In addition, the capability of polydatin to evaluate the deterioration extent of liquids with viscosity as a robust marker was explored. It was found that the viscosity level in microenvironments is highly dependent on the liquid food metamorphic period. The fluorescent intensity increment and viscosity value changes were fitted into a linear equation. We expected that this approach would reinvigorate the fluorescent analytical methods toward liquid safety inspection.

研究领域: 生物化学 · 分析化学 · 食品科学
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FOOD AND CHEMICAL TOXICOLOGY · 2023 · IF 4.3

Polyvinylpyrrolidone-Polydatin nanoparticles protect against oxaliplatin induced intestinal toxicity in vitro and in vivo

Shilin Zhou,Yuxuan Sun,Kaidi Wang,Xintao Gao,Kehong Dong,Jing Wang,Xiaochen Wu,Chuanlong Guo

Oxaliplatin (OXL) is a first-line drug for the treatment of colon cancer , with excellent efficacy. Intestinal toxicity is a common side effect of OXL, with unclear pathogenesis and a lack of effective treatment strategies. Polydatin (PD) has anti-inflammatory and antioxidant activities and is a potential drug for treating intestinal diseases , but its poor water solubility limits its application. In this study, polyvinylpyrrolidone (PVP) was used as a carrier to prepare nanoparticles loaded with PD (PVP-PD), with a particle size of 92.42 nm and exhibiting sustained release properties. In vitro results showed that PVP-PD protected NCM460 cells from OXL induced injury, mitochondrial membrane potential (MMP) disruption, and accumulation of reactive oxygen species (ROS). The in vivo results demonstrated the protective effect of PVP-PD on intestinal toxicity induced by OXL, such as alleviating weight loss and colon length reduction induced by OXL. Both in vivo and in vitro mechanisms indicated that OXL induced DNA damage and activated the cGAS-STING pathway, further inducing the expression of inflammatory factors such as IL-1β and TNF-α. PVP-PD alleviated the aforementioned changes induced by OXL by inhibiting the DNA damage-cGAS-STING pathway. In summary, our study demonstrated that the DNA damage-cGAS-STING pathway was involved in OXL induced intestinal toxicity, and PVP-PD provided a potential strategy for treating OXL induced intestinal toxicity.

研究领域: 药理学 · 毒理学 · 纳米技术 · 细胞生物学 · 分子生物学
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JOURNAL OF FOOD SCIENCE · 2015 ·Vol. 80 ·期 6 ·C1156 · IF 1.696

Characterization of the Supermolecular Structure of Polydatin/6-O-α-Maltosyl-β-cyclodextrin Inclusion Complex

Benguo Liu,Yun Li,Huizhi Xiao,Yonglan Liu,Haizhen Mo,Hanjun Ma,Guizhao Liang

en This link goes to a English section pt This link goes to a English section Polydatin is the main bioactive ingredient in many medicinal plants, such as Hu-zhang ( Polygonum cuspidatum ), with many bioactivities. However, its poor aqueous solubility restricts its application in functional food. In this work, 6-O-α-Maltosyl-β-cyclodextrin (Malt-β-CD), a new kind of β-CD derivative was used to enhance the aqueous solubility and stability of polydatin by forming the inclusion complex. The phase solubility study showed that polydatin and Malt-β-CD could form the complex with the stoichiometric ratio of 1:1. The supermolecular structure of the polydatin/Malt-β-CD complex was characterized by ultraviolet–visible spectroscopy (UV), Fourier transform infrared spectroscopy (FT-IR), X-ray diffractometry (XRD), thermogravimetric/differential scanning calorimetry (TG/DSC), and proton nuclear magnetic resonance ( 1 H-NMR) spectroscopy. The changes of the characteristic spectral and thermal properties of polydatin suggested that polydatin could entrap inside the cavity of Malt-β-CD. Furthermore, to reasonably understand the complexation mode, the supermolecular structure of polydatin/Malt-β-CD inclusion complex was postulated by a molecular docking method based on Autodock 4.2.3. It was clearly observed that the ring B of polydatin oriented toward the narrow rim of Malt-β-CD with ring A and glucosyl group practically exposed to the wide rim by hydrogen bonding, which was in a good agreement with the spectral data. Practical Application en This link goes to a English section pt This link goes to a English section Polydatin was a nutraceutical with potential prospect in functional food. In this study, 6-O-α-Maltosyl-β-cyclodextrin, a new kind of β-CD derivative was used to improve its poor aqueous solubility by forming the inclusion complex, which can be used to develop new functional food. The introduced spectral technologies and molecular docking method could be used to characterize other complexes of bioactive compounds with CDs.

研究领域: 药剂学 · 食品科学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Stem Cells International · 2015 · IF 2.813

Polydatin Protects Bone Marrow Stem Cells against Oxidative Injury: Involvement of Nrf 2/ARE Pathways

Meihui Chen,Yu Hou,Dingkun Lin

Polydatin, a glucoside of resveratrol, has been reported to possess potent antioxidative effects. In the present study, we aimed to investigate the effects of polydatin in bone marrow-derived mesenchymal stem cells (BMSCs) death caused by hydrogen peroxide (H2O2), imitating the microenvironment surrounding transplanted cells in the injured spinal cord in vitro. In our study, MTT results showed that polydatin effectively prevented the decrease of cell viability caused by H2O2. Hochest 33258, Annexin V-PI, and Western blot assay showed H2O2-induced apoptosis in BMSCs, which was attenuated by polydatin. Further studies indicated that polydatin significantly protects BMSCs against apoptosis due to its antioxidative effects and the regulation of Nrf 2/ARE pathway. Taken together, our results indicate that polydatin could be used in combination with BMSCs for the treatment of spinal cord injury by improving the cell survival and oxidative stress microenvironments.

CAS / MDL: 27208-80-6 65914-17-2
研究领域: 药理学 · 干细胞生物学 · 神经科学
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Oncology Letters · 2019 ·Vol. 17 ·期 5 ·4505-4513 · IF 1.871

Polydatin inhibits hepatocellular carcinoma via the AKT/STAT3‑FOXO1 signaling pathway Corrigendum in /10.3892/ol.2019.10856

Jian Jiang,Yaodong Chen,Tianxiu Dong,Minlu Yue,Yu Zhang,Tingting An,Jiuwei Zhang,Pengfei Liu,Xiuhua Yang

Polydatin, extracted from Polygonum cuspidatum, is known for its anti‑platelet aggregation and anti‑inflammatory effects. However, studies on the association of polydatin with cancer are limited, particularly with regards to epithelial‑mesenchymal transition (EMT)‑associated migration and invasion of cancer cells. The purpose of the present study was to reveal the potential anticancer effects of polydatin on hepatocellular carcinoma (HCC) cells, particularly its effects on EMT. MTT assay was used to determine cell viability. Migration and invasion were evaluated through wound healing and transwell assays. Colony formation efficiency assay was conducted to detect proliferation. Flow cytometric analyses of apoptosis and cell cycle progression were performed following cells staining with Annexin V‑fluorescein isothiocyanate (FITC)/propidium iodide (PI) and PI alone, respectively. Western blotting was used to investigate relevant molecular mechanisms. The results indicated that polydatin inhibited proliferation via G2/M arrest, suppressed migration and invasion of HCC cells, and promoted their apoptosis. In addition, phosphorylated (p)‑protein kinase B (AKT), p‑Janus kinase 1 and p‑signal transducer and activator of transcription 3 (STAT3) levels were decreased as polydatin concentrations increased, and forkhead box protein O1 (FOXO1) expression was upregulated. Furthermore, the expression levels of various markers of EMT were reversed following treatment with polydatin. In conclusion, the present study validated that polydatin may inhibit proliferation via G2/M arrest, and suppressed EMT‑associated migration and invasion of HCC cells. The results also suggested that polydatin may promote HCC cell apoptosis by blocking the AKT/STAT3‑FOXO1 signaling pathway.

研究领域: 肿瘤学 · 药理学 · 细胞生物学 · 分子生物学
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