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INTERNATIONAL DAIRY JOURNAL · 2025 · IF 3.4

The effects of β-lactoglobulin-puerarin interaction on the properties of protein hydrogels

Peng Man,Lina Sun,Jinghua Pei,Xiue Han,Huajiang Zhang,Haowei Ren

This study investigated the impact of protein-polyphenol interactions on the properties of heat-set protein hydrogels. β-lactoglobulin (βLG) served as the model protein, while puerarin (PUE) was employed as the model polyphenol. Molecular docking simulations, combined with fluorescence spectroscopy, revealed that hydrophobic interactions dominated the interaction between PUE and βLG. Following PUE treatment, the particle size increased by 219 nm, and significant alterations were observed in the secondary structure. Scanning electron microscopy data illustrated notable surface modifications. The rheological properties of hydrogels can be modulated by varying polyphenol concentrations. Specifically, both the composite shear modulus and hardness of the hydrogels were enhanced with rising PUE concentrations. This study demonstrates that puerarin acts as a dual-functionality agent: a nutraceutical and a gelling enhancer. Its hydrophobic-driven complexation with βLG significantly increased particle size (by 131 %), storage modulus (by 220 %), and hardness (by 322 %).

CAS / MDL: 7647-14-5
研究领域: 食品科学 · 生物物理学 · 分子生物学 · 材料科学 · 营养药物学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2018 · IF 3.412

Whole-Cell Catalytic Synthesis of Puerarin Monoesters and Analysis of Their Antioxidant Activities

Xiao-Feng Li,Tingting Yuan,Haixia Xu,Xuan Xin,Guanglei Zhao,Hui Wu,Xinglong Xiao

Puerarin, an important isoflavonoid from the edible root of Pueraria lobata, shows multiple bioactivities but suffers from low bioavailability. In this study, a new whole-cell catalytic method for acylation modification of puerarin was developed. Among the 12 strains tested, Aspergillus oryzae showed the highest catalytic activity and selectively catalyzed acylation of puerarin at the 6″-hydroxyl group. The organic solvents used significantly influenced the catalytic efficiency of the cells. In the green solvent 2-methyltetrahydrofuran, the reaction showed high substrate conversion (92.5%) and regioselectivity (95.8%), with results similar to those with tetrahydrofuran (94.2% and 98.5%, respectively) under optimal conditions. The monoester products showed higher liposolubility in comparison to puerarin, and those with C3–C8 fatty acid chain lengths showed evidently improved antioxidant activity toward erythrocyte hemolysis. Considering the operational stability of the cells and efficiency of the scaled-up reactions, this method is efficient and cost effective, with promising applications in the health food industry.

研究领域: 药理学 · 生物化学 · 食品科学
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Food Production Processing and Nutrition · 2025 ·Vol. 7 ·期 1 ·1-14 · IF 5.7

Puerarin esters mitigate oxygen and glucose deprivation-reoxygenation-induced injury in microglial cells

Mo Lan,Zhao Guang-lei,Li Xiao-feng,He Ning,Xiao Xing-long,Xu Hai-xia,Yu Yi-gang

Puerarin esters (PAES) are novel isoflavone derivatives of puerarin. Network pharmacology analysis revealed that PAES with medium-long chain lengths may exert a neuroprotective effect against ischemic stroke through NF-κB signaling, TNF signaling, and apoptosis-related signaling pathways. To clarify the protective role of PAES in ischemic stroke, the present study was carried out by using a typical cell model:oxygen and glucose deprivation-reoxygenation (OGD/R)-induced microglial cells model. Results showed that pretreatment with PAES (25 μM) remarkably increased cell viability and promoted microglial polarization toward the anti-inflammatory M2 phenotype under OGD conditions. Furthermore, PAES decreased OGD/R-induced cell death via suppressing cleaved-caspase 3 expression and decreasing the Bax/Bcl-2 ratio. PAES treatment up-regulated SOD1 and Nrf2 expression, P-Akt, while P-JNK, P-P38, NF-κB expressions were significantly down-regulated. In conclusion, this study reports that PAES effectively mitigates OGD/R-caused inflammatory damage and oxidative stress in microglia cells, thereby suggesting a potential therapeutic approach for ischemic stroke.Graphical

CAS / MDL: 3681-99-0
研究领域: 神经生物学 · 药理学 · 分子医学 · 脑血管病学 · 炎症与免疫
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ACS Applied Materials & Interfaces · 2019 · IF 8.456

Nanoparticles Mediating the Sustained Puerarin Release Facilitate Improved Brain Delivery to Treat Parkinson’s Disease

Tongkai Chen,Wei Liu,Sha Xiong,Dongli Li,Shuhuan Fang,Zhenfeng Wu,Qi Wang,Xiaojia Chen

Recent work has highlighted the potential of puerarin (PU) as a valuable compound to treat Parkinson’s disease (PD), but its undesirable water solubility and bioavailability have constrained its utility. In this study, we sought to develop nanoparticles (NPs) that could be used to encapsulate PU, thereby extending its in vivo half-life and improving its bioavailability and accumulation in the brain to treat the symptoms of PD. We prepared spherical NPs (88.36 ± 1.67 nm) from six-armed star-shaped poly(lactide-co-glycolide) (6-s-PLGA) NPs that were used to encapsulate PU (PU-NPs) with 89.52 ± 1.74% encapsulation efficiency, 42.97 ± 1.58% drug loading, and a 48 h sustained drug release. NP formation and drug loading were largely mediated by hydrophobic interactions, while changes in the external environment led these NPs to become increasingly hydrophilic, thereby leading to drug release. Relative to PU alone, PU-NPs exhibited significantly improved cellular internalization, permeation, and neuroprotective effects. Upon the basis of Förster resonance energy transfer (FRET) of NPs-administered zebrafish, we were able to determine that these NPs were rapidly absorbed into circulation whereupon they were able to access the brain. We further conducted oral PU-NPs administration to rats, revealing significant improvements in PU accumulation within the plasma and brain relative to rats administered free PU. In MPTP-mediated neurotoxicity in mice, we found that PU-NPs treatment improved disease-associated behavioral deficits and depletion of dopamine and its metabolites. These findings indicated that PU-NPs represent a potentially viable approach to enhancing PU oral absorption, thus improving its delivery to the brain wherein it can aid in the treatment of PD.

研究领域: 药剂学 · 神经科学 · 生物医学工程
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ACS Applied Bio Materials · 2026 · IF 5.6

Click-Chemistry-Based Antibacterial Hybrid Hydrogel with Sustained Puerarin Release for Diabetic Wound Healing

Shuangyan Jiang,Hanglu Li,Pei Zhang,Luyao Wang,Linjie Chen,Xinyi Liu,Mengshi Chen,Xiaolei Zhou,Zhihua Chen,Rengcheng Qian,Bo Li,Zhifeng You,Huaqiong Li,Ke Peng

The abnormal microenvironment of chronic diabetic wounds leads to the disorder of the tissue repair process. Herein, based on the principles of click chemistry, a multifunctional rapid gelation hydrogel dressing (MSFP hydrogel) was designed for the treatment of diabetic wounds. The hydrogel was formed via thiol–ene click reaction between thiolated Pluronic F127 (F127SH) and maleimide-modified gelatin (GelatinMAL). This thiol–ene click reaction required no metal catalyst, exhibited good biocompatibility, and proceeded under mild conditions. The system incorporated antimicrobial component F127-acetylbromide (F127AcBr) and puerarin (PUE) and responded to overexpressed matrix metalloproteinase 9 (MMP-9) at wound sites, enabling controlled drug release. In vitro experiments demonstrated that the MSFP hydrogel effectively eliminated ROS; modulated macrophage polarization; promoted human umbilical vein endothelial cell proliferation, migration, and tube formation; and exhibited robust antibacterial activity against Staphylococcus aureus and Escherichia coli. In vivo diabetic mouse wound models confirmed that the MSFP hydrogel synergistically improved the wound microenvironment by establishing barrier protection, inhibiting bacterial growth, reducing inflammation, promoting M2 macrophage polarization, and enhancing vascularization. Collectively, this multifunctional hydrogel can promote diabetic wound healing through immunoregulation, angiogenesis, and antibacterial activity, presenting a promising therapeutic strategy for clinical application.

CAS / MDL: 25952-53-8 6066-82-6
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2024 ·Vol. 25 ·期 2 ·709 · IF 4.9

Enhanced Enzymatic Synthesis of Puerarin Palmitate with Different Acyl Donors for Lipid Solubility Improvement

Seungmee Lee,Hyeonmi Shin,Jihyun Bae,Taek Lee,Minji Kim,Heung Bae Jeon,Kang Hyun Lee,Hah Young Yoo,Chulhwan Park

Puerarin is a flavonoid known as a natural antioxidant found in the root ofPueraria robata. Its antioxidant, anticancer, and anti-inflammatory effects have attracted attention as a potential functional ingredient in various bioindustries. However, puerarin has limited bioavailability owing to its low lipid solubility and stability. Acylation is proposed as a synthesis method to overcome this limitation. In this study, lipase-catalyzed acylation of puerarin and various acyl donors was performed, and the enzymatic synthetic condition was optimized. Under the condition (20 g/L of Novozym 435, palmitic anhydride, 1:15, 40 °C, tetrahydrofuran (THF)), the synthesis of puerarin ester achieved a significantly high conversion (98.97%) within a short time (3 h). The molecule of the synthesized puerarin palmitate was identified by various analyses such as liquid chromatography–mass spectrometry (LC–MS), Fourier-transform infrared spectroscopy (FT-IR), and carbon-13 nuclear magnetic resonance (13C NMR). The lipid solubility and the radical scavenging activity were also evaluated. Puerarin palmitate showed a slight decrease in antioxidant activity, but lipid solubility was significantly improved, improving bioavailability. The high conversion achieved for puerarin esters in this study will provide the foundation for industrial applications.Keywords:antioxidant;flavonoid;puerarin;flavonoid ester;lipase;lipid solubility

CAS / MDL: 112-39-0
研究领域: 生物化学 · 制药工程
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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY · 2013 · IF 1.333

Polyamidomine dendrimers: an excellent drug carrier for improving the solubility and bioavailability of puerarin

Lin Gu,Zheng hong Wu,Xiaole Qi,Huan He,Xiaoli Ma,Xiaohua Chou,Xiaoguang Wen,Miao Zhang,Fang Jiao

The potential of polyamidoamine (PAMAM) dendrimers as solubility enhancers and oral drug delivery system was well known. Herein, we investigated the possibility of PAMAM dendrimers for promoting the solubility and oral bioavailability of puerarin. In the present study, the effect of PAMAM dendrimers with different generations (G1.5, G2, G2.5, and G3) on the solubility of puerarin was evaluated at different concentrations and pH conditions. Further more, the puerarin–G2 dendrimer complex was conducted for the in vitro hemolytic toxicity studies and pharmacokinetics studies in rats. The solubility of puerarin was significantly higher in the presence of the full generation dendrimers (e.g. G2 and G3). No significant hemolysis was observed on erythrocytes (G2, 0–2.5 mg/mL) in the hemolytic toxicity studies. The pharmacokinetics parameters Tmax, Cmax, and AUC0–8 h of puerarin suspension solution and puerarin–G2 dendrimer complex solution were 0.76 h, 1.50 µg/mL, 7.33 µg·h/mL and 0.33 h, 6.49 µg/mL, 14.02 µg·h/mL, respectively. These studies demonstrate that PAMAM dendrimers may be a promising strategy for peroral delivery of puerarin.

研究领域: 药剂学 · 药物递送系统 · 生物医学工程
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2020 · IF 4.389

Puerarin-loaded ultrasound microbubble contrast agent used as sonodynamic therapy for diabetic cardiomyopathy rats

Xue Jintao,Zhou Nanqian,Yang Yuping,Jing Yun,Qiu Yue,Liu Yanhua,Lu Junxiu,Tian Xinqiao,Yin Yaling,Li Peng

In this study, a puerarin-loaded ultrasound sulfur hexafluoride microbubble contrast agent as a sonodynamic therapy (SDT) was developed to improve targeted drug delivery and pharmacodynamic effects in diabetic cardiomyopathy (DCM) treatment. Fluorescence microscope morphology was applied to confirm the fabrication of the puerarin - microbubbles (PMBs). The average size distribution and zeta potential of PMBs were 760.0 ± 101.2 nm and −20.4 ± 6.59 mV, respectively. In vitro and in vivo experiments were carried out to study the pharmacodynamic effects and targeted drug delivery of PMBs. The cytotoxicity, assessed by the cell viability of human umbilical vein endothelial cells (HUVECs), showed that the microbubbles were nontoxic even in high concentration of 2.500 mg/mL, and the wound healing scratch assay proved that PMBs cloud obviously improve the migration ability of HUVECs. Furthermore, streptozotocin (STZ) accompanied with high-energy diets was employed to build the DCM rat model. The blood glucose, histological changes of the pancreas and heart, and cardiac function were used to confirm the obtainment of the DCM rat model. Histological and physiological changes of the PMBs treatment group indicated that PMBs had a significant therapeutic efficacy when compared to the DCM model group. Therefore, PMBs are a promising strategy for a targeted drug delivery system and a novel noninvasive treatment for DCM.

CAS / MDL: 3681-99-0
研究领域: 药理学 · 心脏病学 · 治疗超声 · 药物递送系统
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Molecular Medicine Reports · 2019 ·Vol. 20 ·期 2 ·1017-1024 · IF 1.851

Puerarin prevents cataract development and progression in diabetic rats through Nrf2/HO‑1 signaling

Duzhen Zhang,Man Li

Puerarin is the major bioactive ingredient isolated from the dry root of Pueraria lobata, a plant used in traditional Chinese medicine. Puerarin has been used to treat diabetes and cataracts in China; however, its underlying mechanism of action remains unclear. The aim of the present study was to investigate the effectiveness and mechanism of puerarin in preventing cataracts in diabetic rats. Diabetes was induced by streptozocin (STZ) administration and rats were intraperitoneally injected with puerarin (25, 50 and 100 mg/kg). Blood glucose levels and cataract development were examined in the different experimental groups. In addition, the expression levels of markers associated with oxidative stress, including nuclear factor erythroid 2 like 2 (Nrf2) and heme oxygenase‑1 (HO‑1), were analyzed. The present results suggested that treatment with puerarin at 25, 50 and 100 mg/kg significantly reduced blood glucose levels and the incidence of cataract in STZ‑induced diabetic rats. Additionally, puerarin treatment reduced oxidative stress, restoring the levels of malondialdehyde and glutathione, and the activity of glutathione peroxidase. Furthermore, puerarin administration decreased the expression levels of retinal vascular endothelial growth factor and interleukin‑1β and increased the mRNA expression levels of Nrf2 and HO‑1, thus inhibiting oxidative stress. The present findings suggested that puerarin had hypoglycemic effects and that it prevented cataract development and progression in diabetic rats by reducing oxidative stress through the Nrf2/HO‑1 signaling pathway.

CAS / MDL: 3681-99-0
研究领域: 药理学 · 糖尿病研究 · 眼科学 · 分子生物学
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CARBOHYDRATE POLYMERS · 2023 · IF 11.2

Gel properties and interactions of hydrogels constructed with low acyl gellan gum and puerarin

Shi-Qi Xu,Yi-Nan Du,Zhu-Jun Zhang,Jia-Nan Yan,Jin-Jian Sun,Li-Chao Zhang,Ce Wang,Bin Lai,Hai-Tao Wu

To develop composite hydrogels based on low acyl gellan gum (GG), the effect of puerarin (PUE) on the gel properties of GG was investigated. The results showed that the maximum storage modulus ( G ′) of the 1.2 % GG/0.8 % PUE composite hydrogel was 377.4 Pa at 0.1 Hz, which was enhanced by 4.7-fold compared with that of 1.2 % GG. The melting temperature of this composite hydrogel increased from 74.1 °C to >80.0 °C. LF-NMR results showed that a significant amount of free water was present in the hydrogel matrix. The surface structure aggregation and the shrinkage of the honeycomb meshes in the composite hydrogel proved the cross-linking of PUE and GG. XRD , FTIR and molecular simulation results illustrated that hydrogen bonds were the most important factor controlling the interaction between GG and PUE. Thus, the GG/PUE composite hydrogel has good elasticity, thermal stability and water retention, which lays a good foundation for further application in the food industry.

CAS / MDL: 3681-99-0
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Drug Delivery and Translational Research · 2023 · IF 5.4

Metal-polyphenol microgels for oral delivery of puerarin to alleviate the onset of diabetes

Li Si-hui,Li Yan-fei,Wu Di,Xu Yu,Yan Hui-jia,Hu Jiang-Ning

Puerarin (Pue) is a naturally bioactive compound with many potential functions in regulating blood glucose and lipid metabolism. However, the low bioavailability and rapid elimination in vivo limit the application of Pue in diabetic treatment. Here, we developed a metal-polyphenol-functionalized microgel to effectively deliver Pue in vivo and eventually alleviate the onset of diabetes. Pue was initially encapsulated in alginate beads through electrospray technology, and further immersed in Fe 3+ and tannic acid solution from tannic acid (TA)–iron (Fe) coatings (TF). These constructed Pue@SA-TF microgels exhibited uniform spheres with an average size of 367.89 ± 18.74 µm and high encapsulation efficiency of Pue with 61.16 ± 1.39%. In vivo experiments proved that compared with free Pue and microgels without TF coatings, the biological distribution of Pue@SA-TF microgels specifically accumulated in the small intestine, prolonged the retention time of Pue, and achieved a high effectiveness in vivo. Anti-diabetic experimental results showed that Pue@SA-TF microgels significantly improved the levels of blood glucose, blood lipid, and oxidative stress in diabetic mice. Meanwhile, histopathological observations indicated that Pue@SA-TF microgels could significantly alleviate the damage to the liver, kidney, and pancreas in diabetic mice. Our study provided an effective strategy for oral delivery of Pue and achieved high anti-diabetic efficacy. Graphical Abstract

CAS / MDL: 9005-38-3
研究领域: 药学 · 生物医学工程 · 糖尿病研究 · 药物递送系统
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Advanced Healthcare Materials · 2026 · IF 11

Puerarin-Loaded Radially Aligned Tussah Silk/Chitosan/Graphene Oxide Nanofibrous Scaffolds for Enhanced Wound Healing

Yi Luo,Na Li,Shijun Lu,Yingchao Shen,Minxuan Han,Feng Zhang,Xue Wang

Wound healing remains a critical clinical challenge due to uncontrolled bleeding, bacterial infections, poor vascularization, and cell migration at damaged tissue sites. To address this challenge, we developed a radially structured, multifunctional biomimetic scaffold. Tussah silk was subjected to physical shearing and alkaline hydrolysis treatment to obtain tussah silk nanofibers (TSn). The TSn, chitosan (CS), and graphene oxide (GO) were then processed into radially aligned TSn/CS/GO scaffolds. These anisotropic composite scaffolds demonstrated not only antibacterial activity and rapid hemostatic properties but also effectively guided cell migration from the wound periphery toward the center. To achieve multifunctionality, including antioxidant activity, enhanced cell migration, and vascularization, the central void of the TSn/CS/GO scaffold was filled with a silk fibroin hydrogel integrated with Puerarin (PUE). In vivo studies using rat models confirmed that the TSn/CS/GO@PUE3 scaffold significantly accelerated wound healing (99.98 ± 0.02%), angiogenesis (the positive expression rates of CD31 and α-SMA were 21.66 ± 0.74% and 41.28 ± 1.09%, respectively), and collagen deposition (75.26 ± 2.10%). This study thus provides a valuable strategy for developing multifunctional biomimetic scaffolds to accelerate wound repair.

CAS / MDL: 1401-55-4
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