Future Journal of Pharmaceutical Sciences
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2025
·Vol. 11
·期 1
·1-19
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IF 3
Anwar Maira,Badshah Ismail,Altaf Reem,Masaud Syed Muzzammil,Kiyani Amber,Murtaza Babar
Background Migraine is a neurological disorder and major cause of disability globally, especially in women and young adults. This study aimed to investigate the beneficial effects of polydatin (PD), a natural compound, against nitroglycerin (NTG) induced migraine like headache in mice. Materials and methods Behavioural paradigms included Von Frey filament test, tail flick test, light aversion test and assessment of migraine-associated pain like behaviour. In addition, biochemical investigations were undertaken to determine the effect of PD on migraine associated markers including oxidative stress, nitric oxide (NO) and calcitonin gene related peptide (CGRP). Integrated in vivo, in silico, and network pharmacology approaches were employed to evaluate PD’s antimigraine effects. Statistical significance was set at p < 0.05. Results Treatment with PD attenuated NTG-induced migraine like headache and related behavioural changes. PD-subjected animals exhibited enhanced levels of catalase, glutathione-S-transferase, and glutathione, as well as reduced lipid peroxidation, compared to NTG-only treated animals. Reduction in CGRP and nitrite levels along with reduced expression of neuronal nitric oxide synthase (nNOS) and inducible nitric oxide synthase (iNOS) was also observed in mouse cortex and trigeminal nucleus caudalis (TNc) after treatment with PD compared with disease controls. Histological sections from PD treated animals from these regions resembled closely with those of controls with improved cell viability. Molecular docking studies suggested that PD docked in the similar binding pocket as that of CGRP, Rimegepant (a CGRP receptor blocker) and Sumatriptan. Network pharmacology revealed potential interaction of hub genes with PD, with proteins like NOS1 (nNOS), NOS2 (iNOS), NOS3, PDE5A, GATM, ARG1 and ARG2 having significant role in network functionality and the potential mediation of PD therapeutic effect. Conclusion PD ameliorated NTG-induced migraine like headache through modulation of NO, CGRP and oxidative stress dependant mechanisms.
研究领域:
神经药理学
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分子医学
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植物疗法
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计算生物学
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疼痛研究
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DOI
高影响因子
LIFE SCIENCES
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2018
·
IF 3.234
Runxiao Lv,Lili Du,Lixin Zhang,Zhiqiang Zhang
Aims Spinal cord injury (SCI) is one of the most devastating central lesions, resulting in serious locomotor deficit. Polydatin is a glucoside of resveratrol with proven anti-cardiovascular, anti-inflammatory and anti-oxidative properties. The main purpose of this study was to investigate whether polydatin could alleviate SCI in rats and explore the underlying mechanisms. Materials and methods SCI rats induced by a weight-drop device were treated with intraperitoneal injection of 20 or 40 mg/kg polydatin. Then the locomotor function of SCI rats was evaluated by the Basso, Beattie and Bresnahan locomotor rating scale, spinal cord edema was measured by the wet/dry weight method, oxidative stress markers were detected by commercial kits and cell apoptosis status was measured by TUNEL staining. In addition, reactive oxygen species (ROS) generation, lactate dehydrogenase (LDH) production and apoptosis status were detected in murine microglia BV2 cells treated with 100 ng/ml lipopolysaccharides (LPS) and 4.0 μM polydatin. The expression of apoptosis-related proteins involved in nuclear factor E2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway was measured by western blot. Key findings Our data showed that polydatin treatment improved locomotor performance of SCI rats, as well as reduced oxidative stress and inhibited apoptosis by enhancing Nrf2/HO-1 signaling. In addition, polydatin was found to up-regulate Nrf2 activity and the inhibitory effects of polydatin on oxidative stress and apoptosis in LPS-stimulated BV2 microglia was neutralized by silencing Nrf2 using specific siRNA. Significance We demonstrate that polydatin may protect the spinal cord from SCI by suppression of oxidative stress and apoptosis via improving Nrf2/HO-1 signaling in microglia.
研究领域:
神经科学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2026
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IF 6.7
Yufei Cao,Yiqiang Zhang,Boran Zhou,Yingxue Zhang,Xu Han,Xinyuan Luan,Yu Wang,Hongjing Zhao
Zearalenone (ZEN) is a mycotoxin that induces hepatic oxidative injury by promoting ROS accumulation and compromising antioxidant defenses. Transcriptomic profiling revealed xanthine oxidase (XOD) as a key mediator. Structure-based molecular docking identified polydatin (PD) from Polygonum cuspidatum as a potent XOD inhibitor with strong binding affinity. Biochemical assays confirmed PD’s XOD inhibition. In vitro and in vivo studies demonstrated that PD significantly attenuated ZEN-induced oxidative stress, reduced ROS generation, and improved pathological markers of liver injury, with optimal efficacy at low concentrations. Molecular dynamics simulations revealed PD forms a stable complex with XOD. Concurrently, PD activated the Nrf2/HO-1 pathway, enhancing SOD and GSH-Px expression while reducing lipid peroxidation. These findings demonstrate that PD mitigates ZEN hepatotoxicity through dual mechanisms: direct XOD inhibition and enhancement of endogenous antioxidant capacity, supporting its therapeutic potential.
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高影响因子
International Journal of Pharmaceutics-X
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2025
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IF 6.4
Yinghan Wang,Shichao Liu,Feikai Zhu,Xuefei Wang,Hanyu Wang,Lin Long,Jun Xiao,Chuanlong Guo
Acute kidney injury (AKI) is a common and serious complication in clinical practice, especially when using chemotherapy drug cisplatin, which severely limits its anti-cancer efficacy. This study developed a novel nano delivery system (Fu-4-PBA/Po NPs) that combines fucoidan (Fu), endoplasmic reticulum stress (ERS) inhibitor 4-phenylbutyric acid (4-PBA), and natural antioxidant Polydatin (Po) to simultaneously alleviate cisplatin induced oxidative stress and ERS. The optimized Fu-4-PBA/Po NPs showed an average size of 102 ± 3.46 nm, a zeta potential of −16.5 ± 0.49 mV, and a high drug loading capacity of 10.34 ± 0.6 %. They exhibited excellent stability and a sustained release profile in vitro . In vitro results showed that treatment with Fu-4-PBA/Po NPs led to a marked increase in cell survival by 34.73 ± 3.54 percentage points compared to the model group, which had a survival rate of 45.97 ± 2.76 %. Furthermore, Fu-4-PBA/Po NPs effectively inhibited the accumulation of reactive oxygen species (ROS), mitochondrial membrane potential decline, and calcium ion release by targeting P-selectin and endoplasmic reticulum (ER) at the site of inflammation, and significantly alleviate cisplatin induced cell apoptosis. Mechanism studies showed that nanocomposites alleviate ERS by inhibiting the PERK-eIF2α-ATF4-CHOP pathway, while blocking the activation of the cGAS-STING pathway, thereby reducing DNA damage and inflammatory response. Pharmacokinetic studies showed that the peak concentration (Cmax) of the nanoparticles reached 2.2 times that of free Po, and the area under the curve (AUC) increased by 2 times. In animal studies, administration of Fu-4-PBA/Po NPs at a dose of 100 mg/kg notably ameliorated renal function, as indicated by reductions in serum creatinine (SCr) and blood urea nitrogen (BUN) levels by 84.3 % and 62.4 %, respectively, and also improved kidney histopathology. This study provided a dual targeted nano-delivery strategy for cisplatin induced AKI therapy, which has important clinical application potential.
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PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
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2018
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IF 3.118
Tingting Lv,Lei Shen,Lei Yang,Wenxiu Diao,Zhenming Yang,Ying Zhang,Shijie Yu,Yanxia Li
Background Inflammation, oxidative stress and epithelial barrier dysfunction have been implicated in inflammatory bowel disease (IBD) pathology. The targeted inhibition of these features may represent a promising therapeutic strategy for IBD. Polydatin is an effective natural antioxidant that possesses strong antioxidant and anti-apoptotic properties. Thus, we studied the protective effects of polydatin treatments on a mouse model of experimental colitis . Methods Acute colitis was experimentally induced by adding 3% dextran sulfate sodium (DSS) to the drinking water provided to mice for 7 days and by administering different doses of polydatin (15, 30, or 45 mg/kg) during the same period. Mice were also treated with the Sonic hedgehog (Shh) pathway inhibitor cyclopamine to estimate the efficacy of polydatin and Shh inhibitors on colitis. The disease activity index (DAI), colon length, histology, levels of oxidative and apoptotic mediators and levels of Shh pathway components were evaluated. Results The polydatin treatment significantly attenuated the DAI, colon shortening and histological damage. In addition, polydatin administration effectively decreased malondialdehyde (MDA) levels and increased the activities of the antioxidant enzymes superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). Polydatin also inhibited apoptosis in mice with colitis by downregulating the expression of the pro-apoptotic proteins Bax , caspase 3 and cleaved caspase 3 and increasing the expression of the anti-apoptotic protein Bcl-2. Furthermore, polydatin modulated Shh signaling pathway activation. After polydatin treatment, the main components of the Shh pathway, including Shh, Patched (Ptc), Smoothened (Smo), and glioblastoma-1 (Gli1), were upregulated at the mRNA and protein levels. Blockade of the Shh pathway using cyclopamine abolished the effects of polydatin on mice with colitis. Conclusion Based on these observations, polydatin may suppress experimental colitis at least partially by regulating the Shh signaling pathway.
研究领域:
药理学
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免疫学
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病理学
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分子生物学
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DOI
PubMed
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
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2019
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IF 4.191
Dong-Yang Zhang,Yi Wan,Xiao-Hui Yao,Cong Chen,Yu-Xiong Ju,Fei-Fan Shuang,Yu-Jie Fu,Tao Chen,Wei-Guo Zhao,Li Liu,Long Li
In this study, in order to bio-transform polydatin to resveratrol from Polygonum cuspidatum extract, a 3D-porous structured cellulose microsphere (CMs) immobilized with β-glucosidase acted as a micro-bioreactor. To successfully immobilize β-glucosidase, CMs was treated with epoxidation to attach three different functional amion groups, and finally combined with β-glucosidase. CMs provided large surface area (32.0 m²/g) and many sites for immobilization of β-glucosidase and chemical modification. The porosity of CMs was 90 % and its density was about 1.00 g/m 3 . According to SEM images, the 3D-porous structure was obviously found and the result of FTIR proved the successful modification of amino groups. The crystal structure of CMs was changed from crystalline cellulose I-β to crystalline cellulose II during the sol-gel method. In the biotransformation tests of the Polygonum cuspidatum extracts, the conversion rate of polydatin reached 93.06 %, and after conversion, the concentration of resveratrol was two times higher than the original Polygonum cuspidatum extract. In addition, the cellulose microsphere micro-bioreactor also possessed good reusability, which could maintain 89.2 % activity after being repeatedly operated 8 times. Therefore, this cellulose microsphere micro-bioreactor can be successfully used to produce resveratrol from polydatin, and this micro-bioreactor may also have the potential to convert other plant glycosides into aglycones. Moreover, because of their good biocompatibility, the 3D porous cellulose microspheres can also be used for immobilization of other enzymes to prepare efficient bioreactors.
研究领域:
生物技术
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植物化学
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DOI
高影响因子
Journal of Functional Foods
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2023
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IF 5.6
Wenjing Xu,Yufeng Chen,Fenfen Li,Xiaoxi Zhang,Cantao Li,Chenxi Wu,Yan Huang,Daozong Xia
Gout is a metabolic disease that seriously affects people's health. Polydatin, a stilbene compound isolated from Polygonum cuspidatum , has attracted much attention because of its rich biological activity and high safety. This study aimed to investigate the therapeutic effect and mechanism of polydatin on hyperuricemia (HUA) combined with gouty arthritis (GA). The results showed that polydatin reduced the levels of uric acid and inflammatory cytokines, indicating that polydatin had the effect of reducing uric acid and anti-GA. Then the inhibitors of ABCG2, NLRP3 inflammasome and NF-κB pathway (Ko143, MCC950 and QNZ) were used to demonstrate that polydatin played a role in reducing uric acid and anti-GA via regulating urate transporters, NLRP3 inflammasome and NF-κB pathway. Taken together, these results provided evidence that polydatin might be used as a potential functional ingredient for the synchronous treatment of HUA and GA.
研究领域:
药理学
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代谢性疾病
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炎症
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分子生物学
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DOI
高影响因子
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
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2026
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IF 2.5
Weiwei Yang,Shulan Pang,Yi Li,Jiahong Chen,Qiuhong Jiao,Ailin Liu,Tiansen Liu,Tao Huang,Hongjie Wang,Xiufeng Xu,Yuqing Zhang,Peikang Dong,Tao Wang
Integrative computational analyses identify PPARG as a key target of polydatin in aortic dissection. • Docking and MD support stable binding of polydatin to PPARγ and Keap1. • Transcriptomic and WGCNA analyses link polydatin to oxidative-stress regulation. • Polydatin attenuates BAPN-induced aortic dissection in mice. • Polydatin may protect the aortic wall via the PPARγ/Nrf2 antioxidant axis. Aortic dissection (AD) is a life-threatening vascular disease characterized by medial degeneration, extracellular matrix (ECM) destruction, inflammation, and oxidative stress. Polydatin (PD), a natural stilbene glucoside, has cardiovascular protective potential, but its mechanism against AD remains unclear. This study investigated the therapeutic mechanism of PD in AD by integrating network pharmacology, transcriptomic analysis, weighted gene co-expression network analysis (WGCNA), molecular modeling, and in vivo validation. IGF1, PPARG, and KDR were identified as core targets in the PD–AD network, with PPARG prioritized for its association with vascular redox homeostasis, inflammation, and antioxidant defense. Molecular docking and molecular dynamics simulations indicated stable interactions between PD and PPARγ and Keap1, a key regulator of Nrf2 stability. In a β-aminopropionitrile (BAPN)-induced AD mouse model, PD significantly reduced aortic dilation and medial injury, preserved elastic fiber architecture, and attenuated ECM degradation. PD also decreased ROS and MDA levels, restored SOD, GSH-Px, and CAT activities, and upregulated PPARγ, Nrf2, HO-1, and NQO1 expression. These findings suggest that PD alleviates AD by restoring vascular redox homeostasis, potentially involving PPARγ-associated signaling and Nrf2-related antioxidant responses, supporting PD as a potential therapeutic candidate for AD-related vascular degeneration. Download: Download high-res image (327KB) Download: Download full-size image
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高影响因子
BIOMEDICINE & PHARMACOTHERAPY
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2019
·
IF 3.743
Xiao-Jun Chen,Ying-Shan Shen,Min-Cong He,Fan Yang,Peng Yang,Feng-Xiang Pang,Wei He,Yan-ming Cao,Qiu-Shi Wei
Steroid-induced osteonecrosis of the femoral head (SONFH) is a refractory disease induced by glucocorticoids. Marrow mesenchymal stem cells (MSCs) differentiate into multiple bone matrix cells and have been used as cell-based therapies to treat ONFH. However, the osteogenesis of MSCs isolated from patients with SONFH is significantly decreased. Polydatin has been widely used in traditional Chinese remedies due to its multiple pharmacological actions. As shown in our previous study, Polydatin protects from oxidative stress and promotes BMSC migration. However, little is known about its role in BMSC (Bone marrow mesenchymal stem cells) osteogenesis; therefore, we further investigated the effect and mechanism of Polydatin in hBMSC osteogenesis. The ability of Polydatin to promote the proliferation and osteogenic differentiation of hBMSCs was determined using the MTT assay, ALP staining and the ALP activity assay. Next, qPCR and western blotting were performed to measure the levels of genes and proteins related to the osteogenesis of hBMSCs. Then, the effect of Polydatin on the nuclear translocation of β-catenin was determined using immunofluorescence staining. Polydatin (30 μM) markedly enhanced the proliferation of hBMSCs and alkaline phosphatase (ALP) activity. Additionally, it also significantly upregulated the expression of osteogenic genes (Runx2, osteopontin, DLX5, osteocalcin, collagen type I and BMP2) and components of the Wnt signaling pathway (β-catenin, Lef1, TCF7, c-jun, c-myc and cyclin D). These osteogenesis-potentiating effects of Polydatin were blocked by Noggin, an inhibitor of the BMP pathway, and DKK1, an inhibitor of the Wnt/β-catenin pathway. However, DKK1 did not affect Polydatin-induced BMP2 expression. Based on our results, Polydatin promotes the proliferation and osteogenic differentiation of hBMSCs through the BMP2-Wnt/β-catenin signaling pathway.
研究领域:
药理学
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干细胞研究
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骨科
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分子生物学
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PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2019
·
IF 2.606
Zhiwei Chen,Bin Han,Langkun Liao,Xuguang Hu,Qiaohong Hu,Yunhua Gao,Yuqin Qiu
Gout is a disease that affects quality of life and has economic implications. However, most patients with gout are not adequately managed due to the adverse effects of current medical treatments. This study was performed to investigate the transdermal delivery of polydatin via the combination of inclusion complexes and dissolving microneedles and the therapeutic effect of polydatin on the treatment of acute gout arthritis . In vitro cytotoxicity of polydatin on HaCaT cells was measured by a CCK-8 assay. The results showed that polydatin exerted less cytotoxicity compared to indomethacin and colchicine . The aqueous solubility of polydatin increased considerably to 124.47 mg/mL via the formation of polydatin/Hydroxypropyl-β-cyclodextrin inclusion complexes. The complexes loaded dissolving microneedles showed significant improvement for in vitro polydatin permeation compared to the absence of complexes. Pharmacodynamic studies indicated that the polydatin complexes-loaded dissolving microneedles had significant inhibitory effects on swelling of the ankle in the arthritic mice. Furthermore, compared to the oral colchicine treatment, the body weights of the polydatin-treated mice increased significantly during the treatment, which implied a lower toxicity of polydatin microneedles delivery. The overall results indicate that the combination of inclusion complexes with dissolving microneedles provides a potential route for treatment of acute gout arthritis by enhanced transdermal delivery of polydatin.
研究领域:
药剂学
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生物医学工程
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风湿病学
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DOI
高影响因子
Frontiers in Nutrition
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2023
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IF 5
Xueli Ge,Zhenguo Su,Yuhao Wang,Xue Zhao,Kaifei Hou,Shuna Zheng,Pengjiao Zeng,Zhongqi Shi,Senhao Hu,Yuqing Wang,Mengchen Zhou,Jiayu Zhang,Xiulian Li
Introduction Polydatin is a biologically active compound found in mulberries, grapes, and Polygonum cuspidatum , and it has uric acid-lowering effects. However, its urate-lowering effects and the molecular mechanisms underlying its function require further study. Methods In this study, a hyperuricemic rat model was established to assess the effects of polydatin on uric acid levels. The body weight, serum biochemical indicators, and histopathological parameters of the rats were evaluated. A UHPLC-Q-Exactive Orbitrap mass spectrometry-based metabolomics approach was applied to explore the potential mechanisms of action after polydatin treatment. Results The results showed a trend of recovery in biochemical indicators after polydatin administration. In addition, polydatin could alleviate damage to the liver and kidneys. Untargeted metabolomics analysis revealed clear differences between hyperuricemic rats and the control group. Fourteen potential biomarkers were identified in the model group using principal component analysis and orthogonal partial least squares discriminant analysis. These differential metabolites are involved in amino acid, lipid, and energy metabolism. Of all the metabolites, the levels of L -phenylalanine, L -leucine, O -butanoylcarnitine, and dihydroxyacetone phosphate decreased, and the levels of L -tyrosine, sphinganine, and phytosphingosine significantly increased in hyperuricemic rats. After the administration of polydatin, the 14 differential metabolites could be inverted to varying degrees by regulating the perturbed metabolic pathway. Conclusion This study has the potential to enhance our understanding of the mechanisms of hyperuricemia and demonstrate that polydatin is a promising potential adjuvant for lowering uric acid levels and alleviating hyperuricemia-related diseases.
研究领域:
药理学
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代谢组学
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生物化学
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医学
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2023
·Vol. 24
·期 9
·8265
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IF 5.6
Jing Li,Jianchao Zhang,Yan Zhu,Lukman O. Afolabi,Liang Chen,Xuesong Feng
Triple-negative breast cancer (TNBC) has been clearly recognized as a heterogeneous tumor with the worst prognosis among the subtypes of breast cancer (BC). The advent and application of current small-molecule drugs for treating TNBC, as well as other novel inhibitors, among others, have made treatment options for TNBC more selective. However, there are still problems, such as poor patient tolerance, large administration doses, high dosing frequency, and toxic side effects, necessitating the development of more efficient and less toxic treatment strategies. High expression of Nrf2, a vital antioxidant transcription factor, often promotes tumor progression, and it is also one of the most effective targets in BC therapy. We found that in MDA-MB-231 cells and SUM159 cells, brusatol (BRU) combined with polydatin (PD) could significantly inhibit cell proliferation in vitro, significantly downregulate the expression of Nrf2 protein as well as the expression of downstream related target genesHeme Oxygenase-1 (HO-1)andNAD(P)H dehydrogenase, quinone 1 (NQO1), and promote reactive oxygen species (ROS) levels to further strengthen the anti-tumor effect. Furthermore, we discovered in our in vivo experiments that by reducing the drug dosage three times, we could significantly reduce tumor cell growth while avoiding toxic side effects, providing a treatment method with greater clinical application value for TNBC treatment.Keywords:breast cancer;brusatol;polydatin;Nrf2;HO-1;NQO1;ROS
研究领域:
肿瘤学
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药理学
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分子生物学
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PubMed
高影响因子
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