ACTA PHARMACOLOGICA SINICA
·
2016
·Vol. 37
·期 4
·545-554
·
IF 3.166
Su Hui-fang,Lin Qing,Wang Xin-yi,Fu Yao,Gong Tao,Sun Xun,Zhang Zhi-rong
Aim: (+)-Catechin and puerarin are polyphenol and flavonoid, respectively, in green tea and foodstuffs. They exhibit potent antioxidant activity and are widely used for treating cardiocerebrovascular diseases. The aim of this work was to investigate the potential interactions between (+)-catechin and puerarin following concurrent oral administration in rats, and their absorption mechanisms in Caco-2 cell monolayers. Methods: Pharmacokinetic studies were conducted in male rats received (+)-catechin (140 mg/kg, po ) and/or puerarin (200 mg/kg, po ). The cell uptake and transport behavior in Caco-2 cell monolayers and the interactions of the two compounds were analyzed. Results: When (+)-catechin and puerarin were administered concurrently, the AUC 0-12 h and C max values of puerarin were 2.48-fold and 3.91-fold, respectively, as large as those of puerarin alone; the AUC 0-12 h and C max values of (+)-catechin were decreased to 57.62% and 77.55%, respectively, compared with those of (+)-catechin alone. In Caco-2 cell monolayers, (+)-catechin (300 and 600 μmol/L) significantly increased the cell uptake and transport of puerarin, whereas puerarin (300 and 600 μmol/L) significantly decreased the cellular uptake and transport of (+)-catechin. Furthermore, both cyclosporine A (P-glycoprotein inhibitor) and MK-571 (MRP-2 inhibitor) significantly increased the cellular uptake and transport of (+)-catechin and puerarin. Conclusion: Concurrent oral administration of (+)-catechin and puerarin significantly increased the absolute oral bioavailability of puerarin, but decreasing that of (+)-catechin. The competitive efflux of (+)-catechin and puerarin by P-glycoprotein and MRP-2 might lead to this interaction during their absorption process in the small intestine.
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RSC Advances
·
2022
·Vol. 12
·期 6
·3416-3422
·
IF 4.036
Jing Yuan,Ningning Zhou,Jieyu Wu,Tianxiang Yin,Yunbin Jia
Ionic liquids, especially the cholinium-amino acid-based ionic liquids (CHAAILs), have recently been found to be effective ingredients in formulation of transdermal drug delivery system. In this work, we synthesized six CHAAILs, and investigated their ability to enhance the solubility and permeation of two active pharmaceutic ingredients (APIs), i.e. ferulic acid and puerarin. The solubility measurements showed that a low amount of CHAAILs can significantly increase the solubility of APIs. Moreover, the effective enhancement of permeation of APIs across a polyethersulfone (PES) membrane was achieved at low concentration (4 mg ml−1) of CHAAILs. It is more worthwhile that the presence of CHAAIL brings much less cytotoxicity as compared to traditional types of ionic liquids. Therefore, CHAAILs can be considered as great potential candidates of green and effective additives in transdermal drug delivery systems.
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Nano Today
·
2026
·
IF 10.9
Mu-xuan Wang,Ying-ying Chen,Shu-tao Sun,Mohamed A. Farag,Zhi-yong Zhao,Shi-hai Lu,Min-hsiung Pan,Ning-yang Li,Xu Guo,Chao Liu
Hyperuricemic nephropathy (HUN) is a chronic kidney disease, as featured by the large amount of uric acid (UA) deposited in the kidney. Lipid peroxidation and macrophage infiltration caused by UA are two prominent risk factors linked in the occurrence of HUN. Puerarin (PEA) has anti-hyperuricemia, antioxidant, and anti-inflammatory activity, albeit the poor water solubility and a short half-life limit its application. To improve the bioavailability of PEA, this study prepared PEA-loaded hyaluronic acid (HA) self-assembled nanoparticles (PEA-HA NPs). Release kinetics showed that PEA-HA NPs achieved the pH-responsive sustained-release in the weakly acidic microenvironment of HUN. In vivo biodistribution indicated that PEA-HA NPs was preferably internalized by renal tubular epithelial cells in HUN, which was attributed to the specific binding between HA and CD44 receptor. In vitro health benefits confirmed that PEA-HA NPs modulated lipid peroxidation though a distinctive four-pronged strategy in UA-induced HK-2 cells, including scavenging ROS, restoration of mitochondrial function, regulation of inflammatory pathways, and inhibition of apoapsis. Likewise, PEA-HA NPs could transform the pro-inflammatory macrophages (M1-type) of into anti-inflammatory macrophages (M2-type), thereby inhibiting UA-caused macrophage infiltration. In vivo analysis also showed that PEA-HA NPs could alleviate renal dysfunction and fibrosis by modulating lipid peroxidation and macrophage polarization. This study improves the bioavailability and long-lasting therapeutic duration of PEA, which provides a convenient strategy for the efficient treatment of HUN.
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Molecular Medicine Reports
·
2026
·Vol. 33
·期 4
·1-14
·
IF 5
Xiaoyu Zheng,Jinping Li,Tianyang Hu,Li Tan,Ding Lan,Ying Deng
Covers molecular medicine topics such as pharmacology, pathology, genetics, neuroscience, infectious diseases, molecular cardiology, and molecular surgery.
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Bioactive Materials
·
2022
·
IF 16.874
Xiaoling Zeng,Baohui Chen,Luping Wang,Yingxiao Sun,Zhao Jin,Xuanyong Liu,Liping Ouyang,Yun Liao
Wound healing is one of the major global health concerns in patients with diabetes. Overactivation of pro-inflammatory M1 macrophages is associated with delayed wound healing in diabetes. miR-29ab1 plays a critical role in diabetes-related macrophage inflammation. Hence, inhibition of inflammation and regulation of miR-29 expression have been implicated as new points for skin wound healing. In this study, the traditional Chinese medicine, puerarin, was introduced to construct an injectable and self-healing chitosan@puerarin (C@P) hydrogel. The C@P hydrogel promoted diabetic wound healing and accelerated angiogenesis, which were related to the inhibition of the miR-29 mediated inflammation response. Compared to healthy subjects, miR-29a and miR-29b1 were ectopically increased in the skin wound of the diabetic model, accompanied by upregulated M1-polarization, and elevated levels of IL-1β and TNF-α. Further evaluations by miR-29ab1 knockout mice exhibited superior wound healing and attenuated inflammation. The present results suggested that miR-29ab1 is essential for diabetic wound healing by regulating the inflammatory response. Suppression of miR-29ab1 by the C@P hydrogel has the potential for improving medical approaches for wound repair.
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Foods
·
2021
·Vol. 10
·期 4
·705
·
IF 4.35
Yejun Zhong,Jincheng Zhao,Taotao Dai,Jiangping Ye,Jianyong Wu,Tingting Chen,Chengmei Liu
Protein–polyphenol interactions influence emulsifying properties in both directions. Puerarin (PUE) is an isoflavone that can promote the formation of heat-set gels with whey protein isolate (WPI) through hydrogen bonding. We examined whether PUE improves the emulsifying properties of WPI and the stabilities of the emulsions. We found that forming composites with PUE improves the emulsifying properties of WPI in a concentration-dependent manner. The optimal concentration is 0.5%, which is the highest PUE concentration that can be solubilized in water. The PUE not only decreased the droplet size of the emulsions, but also increased the surface charge by forming composites with the WPI. A 21 day storage test also showed that the maximum PUE concentration improved the emulsion stability the most. A PUE concentration of 0.5% improved the stability of the WPI emulsions against environmental stress, especially thermal treatment. Surface protein loads indicated more protein was adsorbed to the oil droplets, resulting in less interfacial WPI concentration due to an increase in specific surface areas. The use of PUE also decreased the interfacial tension of WPI at the oil–water interface. To conclude, PUE improves the emulsifying activity, storage, and environmental stability of WPI emulsions. This result might be related to the decreased interfacial tension of WPI–PUE composites.Keywords:puerarin;polyphenol;whey protein isolates;emulsion;interfacial tension;thermal stability
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PHYTOMEDICINE
·
2020
·
IF 4.268
Chunjun Wang,Jihong Yao,Linjie Ju,Xiaohua Wen,Luan Shu
Background Diabetes is characterized by β-cell loss and dysfunction. A strategy for diabetes treatment is to promote new β-cell formation. Puerarin is an isoflavone from the root of Pueraria lobata (Willd.) Ohwi . Our previous study demonstrated puerarin could ameliorate hyperglycemia in diabetic mice. However, related mechanisms and potential roles of puerarin in β-cell neogenesis have not been elucidated. Purpose The present study aims to investigate whether anti-diabetic effect of puerarin is dependent on promoting β-cell neogenesis via GLP-1R signaling activation. Methods A high-fat diet (HFD) induced diabetic mouse model was applied to investigate effects of puerarin in vivo , exendin-4 (GLP-1R agonist) and metformin were used as positive controls. Moreover, related mechanisms and GLP-1R downstream signal transduction were explored in isolated cultured mouse pancreatic ductal cells. Results Puerarin improved glucose homeostasis in HFD diabetic mice significantly. Markers of new β-cell formation (insulin, PDX1 and Ngn3) were observed in pancreatic ducts of HFD mice treated by puerarin. Of note, efficacy of puerarin in vivo was suppressed by GLP-1R antagonist exendin9-39, but enhanced by exendin-4 respectively. In cultured mouse pancreatic ductal cells, puerarin induced expressions of insulin and PDX1, upregulated GLP-1R expression and activated β-catenin and STAT3 subsequently. Expressions of insulin and PDX1 in ductal cells could be blocked by exendin9-39, or β-catenin inhibitor ICG001, or JAK2 inhibitor AG490 . Conclusion These data clarified puerarin ameliorated hyperglycemia of HFD mice via a novel mechanism involved promoting β-cell neogenesis. Our finding highlights the potential value of puerarin developing as an anti-diabetic agent.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Lu Jin,Xiumin Li,Xu Chen,Xinghao Chen,Ye Liu,Haonan Xu,Qiao Wang,Zhan Tang
Puerarin (PUE), an isoflavonoid isolated from Pueraria lobata (Willd) Ohwi root, is a β -adrenergic receptor inhibitor used in treating glaucoma. The concentration range of gellan gum was determined based on the formulation viscosity and gelling capacity. PVP-K30 and gellan gum were used as variables, with the viscosity of formulation: STF = 40: 21, the 4 h permeation rate of rabbit isolated sclera, and 2 h in vitro release rate as response values. The JMP software was used to optimize the results, presenting that gellan gum was the main factor influencing viscosity. The in vitro release and permeation rate were primarily influenced by PVP-K30. The optimal prescription was 0.45% gellan gum and 6.0% PVP-K30. The in vitro release and permeation characteristics of puerarin in situ gel (PUE-ISG) were investigated using PUE solution as a control. The dialysis bag method results indicated that the release of the solution group leveled off after 4 h, while the PUE-ISG group had been continuously releasing. However, the cumulative release rates of the two were no longer significantly different at 10 h. The cumulative permeation rates of the ISG and solution groups were not significantly different ( P > 0.05) in the rabbit isolated sclera. The apparent permeability Papp and steady-state flux Jss of PUE-ISG were 0.950 ± 0.059 cm/h and 9.504 ± 0.587 mg·(cm·h), respectively. A sensitive and stable HPLC-MS/MS analytical method for quantifying aqueous humor concentrations of PUE was validated. A microdialysis technique was successfully used in the aqueous humor pharmacokinetics study to sample aqueous humor from rabbit eye continuously. The results revealed that PUE-ISG significantly increased the drug concentration in the aqueous humor, with C max and AUC (0-t) 3.77 and 4.40 times higher than those of the solution group, respectively. T max was also significantly prolonged, indicating good prospects for clinical application. The developed PUE-ISG preparation has the characteristics of rapid drug release and sustained permeation, and increase the drug concentration in aqueous humor, with all inactive ingredients remaining within the maximum allowable limits recommended by the FDA guideline.
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JOR Spine
·
2024
·Vol. 7
·期 4
·e70020
·
IF 3.4
Xiaoqiang Wang,Chao Song,Daqian Zhou,Yongliang Mei,Weiye Cai,Rui Chen,Jiale Lv,Houyin Shi,Zongchao Liu
Intervertebral disc degeneration (IVDD) stands as a prevalent chronic orthopedic ailment, profoundly impacting patients' well‐being due to incapacitating low back pain. Studies have highlighted a close correlation between IVDD and the programmed cell death of nucleus pulposus (NP) cells orchestrated by interleukin‐1 beta (IL‐1β), tumor necrosis factor‐alpha (TNF‐α), and caspase‐3 (CASP3). Puerarin, renowned for its anti‐inflammatory attributes and its influence on IL‐1β and TNF‐α, emerges as a promising candidate for IVDD treatment. However, the precise mechanism by which it regulates apoptosis via these pathways remains ambiguous. This investigation utilizes bioinformatics to unveil the molecular intricacies of puerarin‐mediated apoptosis regulation in IVDD, substantiated by preliminary in vitro experiments. Analysis exposes aberrant expression of pivotal apoptosis‐associated proteins (IL‐1β, TNF‐α, CASP3, CASP8, and BCL2) in IVDD patients, with network pharmacology indicating puerarin's potential efficacy in IVDD treatment by modulating apoptosis and cellular senescence pathways. Further experiments elucidate puerarin's capacity to stimulate NP cell proliferation while inhibiting apoptosis, potentially contributing to IVDD mitigation. Western blot and PCR outcomes reveal escalated expression of apoptosis‐related proteins (IL‐1β, TNF‐α, and CASP3) in lipopolysaccharide‐treated NPCs, ameliorated by puerarin intervention. Molecular docking simulations demonstrate favorable binding properties of puerarin with apoptotic proteins, while flow cytometry analysis indicates its ability to diminish NPC apoptosis. These discoveries imply that puerarin might alleviate NPC apoptosis by modulating key targets, thereby potentially ameliorating IVDD. In summary, this study unveils the intrinsic mechanism of puerarin in regulating NPC apoptosis to alleviate IVDD, underscoring its therapeutic promise. Network pharmacology and bioinformatics analyses suggest that puerarin may mitigate intervertebral disc degeneration (IVDD) by inhibiting nucleus pulposus (NP) cell apoptosis. This hypothesis was validated through in vitro experiments, which demonstrated that puerarin significantly reduces apoptosis in NPCs.
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FOOD CHEMISTRY
·
2012
·
IF 3.655
Jie-Ping Fan,Jing Cao,Xue-Hong Zhang,Jun-Zhong Huang,Tao Kong,Sheng Tong,Zhe-You Tian,Yan-Long Xie,Rui Xu,Jian-Hang Zhu
Ionic liquid (IL) based ultrasonic assisted extraction (ILUAE) was developed for the effective extraction of puerarin from Radix Puerariae Lobatae (RPL). The ILUAE parameters including the type of ILs, IL concentration, RPL amount, ultrasonic power and time were optimized by single-factor experiment and response surface methodology. Under the optimized experimental conditions, the best results were obtained using RPL amount 0.43 g in 10 mL 1.06 mol L −1 1-butyl-3-methylimidazolium bromide aqueous solution, ultrasonic time 27.43 min and ultrasonic power 480 W. Scanning electron microscope images of RPL samples were obtained to provide visual evidence of the sonication effect. Compared with the conventional ultrasonic assisted extraction and refluent extraction, the proposed ILUAE offered shorter extraction time and remarkable higher efficiencies due to the higher penetration ability and solubility of IL and the cavitation phenomenon produced in the solvent by the passage of an ultrasonic wave, which further supported the suitability of the proposed approach.
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FOOD CHEMISTRY
·
2017
·
IF 4.529
Shuya Wang,Ziwei Yang,Na Peng,Jun Zhou,Xiaoyu Yong,Haoran Yuan,Tao Zheng
Ionic liquids-based microwave-assisted hydrolysis was successfully applied for hydrolysis of puerarin and daidzein derivatives from Radix Puerariae Lobatae extract. The ionic liquids with different cations and anions have been investigated, and [Omim]HSO 4 was selected as catalyst. In addition, the hydrolysis parameters, including catalyst quantity, ionic liquids concentration, microwave power and microwave time, were optimized by Response Surface Methodology. The optimal conditions were as follows: 0.82 mol/L [Omim]HSO 4 ; catalyst quantity, 1.42 mL; microwave time, 7 min; microwave power, 400 W. Under those condition the average hydrolysis efficiency of puerarin and daidzein derivatives was 57.93 ± 3.08%. Compared with the traditional acidic catalysts, the [Omim]HSO 4 exhibited higher efficiency, which demonstrates that ionic liquids-based microwave-assisted hydrolysis was a rapid, efficient, and simple hydrolysis technique.
研究领域:
中药化学
·
分析化学
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Frontiers in Pharmacology
·
2026
·
IF 5.4
Hongmei Tang,Yanjiao Li,Yuting Pu,Lingxue Wang,Yunfang Yang,Lu Liu,Xue Bai
Background Vascular dementia (VaD) is the second most common type of dementia after Alzheimer’s disease. Puerarin (PUE) is a natural compound isolated from Puerariae Lobatae Radix , plays an important role in treating neurodegenerative and neurovascular diseases. Studies have confirmed that Puerarin can reduce neuroinflammation and protect the blood-brain barrier (BBB). However, the precise mechanism by which PUE treats VaD remains to be elucidated. Objective To investigate the therapeutic effect of Puerarin on VaD and its underlying molecular mechanisms. Materials and Methods Cognitive performance was assessed using the behavioral testing. Hematoxylin and Eosin staining (H&E) and Nissl staining were employed to assess neuronal morphology in the hippocampus. Additionally, network pharmacology (NP) was used to identify putative bioactive compounds in PUE and candidate targets associated with VaD. Transmission electron microscopy (TEM), enzyme-linked immunosorbent assay (ELISA), quantitative PCR (qPCR), and Western blotting were used for experimental validation. To further interrogate pathway involvement, lipopolysaccharide (LPS), a Toll-like receptor 4 (TLR4) agonist, was administered, followed by repeated behavioral testing and molecular analyses. Results Behavioral testing showed that PUE mitigated two-vessel occlusion (2VO)-induced cognitive deficits and reduced hippocampal neuronal injury. NP identified 17 putative active compounds and 100 overlapping targets between PUE and VaD. GO and KEGG enrichment analyses indicated that these targets were enriched in Toll-like receptor and NF-κB signaling, implicating an anti-neuroinflammatory mechanism. Experimental assays showed that PUE reduced TLR4 and myeloid differentiation primary response 88 (MyD88) expression, decreased nuclear factor-kappa-B p65 (NF-κB p65) phosphorylation, and lowered pro-inflammatory mediator levels. Importantly, the administration of the TLR4 agonist LPS effectively counteracted the therapeutic effects of Puerarin. Conclusion Puerarin improves learning and cognitive abilities in VaD rats by inhibiting the TLR4/MyD88/NF-κB signaling pathway, thereby attenuating pathological alterations in the hippocampus, protecting the BBB integrity from cerebral ischemic damage, and exerting anti-neuroinflammatory effects.
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