ACS Applied Polymer Materials
·
2021
·
IF 4.089
Yufen Han,Yarong Lv,Jia Chen,Ming Yao,Ce Wang,Ping Hu,Yong Liu
Nowadays, small-diameter vascular grafts are attracting considerable interest in tissue engineering and are in great demand in clinical trials. However, the defect of weak patency limits the application of small-caliber vessels in the coronary artery and peripheral vessel bypass graft surgery. Research shows that puerarin can protect endothelial cells from damage caused by inflammation, oxidative stress, and apoptosis. Simultaneously, puerarin can promote endothelial cell proliferation and differentiation. In this study, puerarin-loaded vascular grafts were made through coaxial electrospinning with gelatin by taking poly(l-lactic acid) as the carrier material and multiwalled carbon nanotubes as reinforced materials. The results showed that the resultant fibers have a core–shell structure with enhanced hydrophilicity, hydrophobicity, mechanical properties, and degradability, which are in good agreement with the properties of natural blood vessels. Compared with the commercially available puerarin drugs, the drug release cycle of the as-prepared puerarin-loaded core–shell structure fiber is effectively prolonged and highly efficient. Moreover, the biocompatibility test showed that the fiber that contains puerarin has no toxicity and side effects on endothelial cells, will not cause hemolysis, and meets the national safety regulations for medical materials.
研究领域:
生物材料学
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组织工程学
·
药理学
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高影响因子
SEPARATION SCIENCE AND TECHNOLOGY
·
2012
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IF 1.088
Jie-Ping Fan,Jing Cao,Xue-Hong Zhang,Jun-Zhong Huang,Tao Kong,Sheng Tong,Zhe-You Tian,Jian-Hang Zhu,Xiao-Kun Ouyang
Various ionic liquid-based aqueous two-phase systems (IL-ATPS) were evaluated to extract puerarin. The results indicated that the nature of ILs, the salting-out ability of salt, and the acidity and basicity of the salt-rich solution had important influence on the extraction efficiency. Various factors were optimized systematically, that is, the amount of IL, salt, puerarin, and short-chain alcohol. Under the optimal experimental conditions (the amount of K2HPO4 0.30–0.42 g/mL, [Bmim]Br 0.30–0.36 g/mL and 1.0 mL puerarin stock solution), the extraction efficiency of puerarin was over 99% by a single-step extraction, which indicated that the evaluated IL-ATPS was a prospective extraction medium. Finally, the IL-ATPS was successfully used to extract puerarin from Radix Puerariae Lobatae extracts.
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BIOMEDICINE & PHARMACOTHERAPY
·
2020
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IF 4.545
Min Chen,Cui Zhou,Haiman Xu,Tianpeng Zhang,Baojian Wu
Hyperhomocysteinemia is associated with poor health, including cardiovascular and brain diseases. Puerarin, initially isolated from Puerariae radix , has been shown to possess anti-hyperhomocysteinemia effect. However, the mechanism of puerarin action remains unknown. Here, we uncovered that puerarin targeted the circadian clock protein Rev-erbα to alleviate hyperhomocysteinemia in mice in a circadian time-dependent manner. We first identified puerarin as an antagonist of Rev-erbα based on luciferase reporter, Gal4 co-transfection and target gene expression assays. Consistent with an antagonistic effect, puerarin induced mRNA and protein expressions of Bhmt, Cbs and Cth (three enzymes involved in homocysteine catabolism and known targets of Rev-erbα) in Hepa-1c1c7 cells. These induction effects of puerarin were lost in Rev-erbα-deficient cells. Furthermore, puerarin dose-dependently alleviated methionine-induced hyperhomocysteinemia in mice as evidenced by decreased levels of total homocysteine and triglyceride. This was accompanied by increased expressions of Bhmt, Cbs and Cth in the liver. Moreover, puerarin dosed at ZT10 generated stronger pharmacological effects than drug dosed at ZT22 consistent with diurnally rhythmic expression of Rev-erbα (a high expression at ZT10 and a low expression at ZT22). In conclusion, puerarin targets Rev-erbα to alleviate hyperhomocysteinemia in mice in a circadian time-dependent manner. The finding of a circadian gene as drug target encourages chronotherapeutic practices on puerarin and related medications for optimized efficacy.
研究领域:
药理学
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分子生物学
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慢性疾病
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生物钟学
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DOI
PubMed
高影响因子
Experimental and Therapeutic Medicine
·
2020
·Vol. 20
·期 1
·275-282
·
IF 1.785
Junling Liu,Jianyun Liu,Mingming Bai,Hui Wang
The present study evaluated the potential protective effects of puerarin and its associated mechanism on burn-induced myocardial damage. A total of 40 healthy adult Wistar rats were randomly divided into four groups: i) Sham; ii) burn; iii) burn + puerarin; and iv) puerarin. Serum levels of interleukin (IL)‑1β, tumor necrosis factor‑α (TNF‑α) and IL‑6 were measured using ELISA. Myeloperoxidase (MPO) activity and malondialdehyde (MDA) levels were determined in myocardial homogenates using a commercial assay kit. TUNEL staining and western blot analysis of cleaved and pro‑caspase‑3 were also performed to assess apoptosis. Activation of p38‑MAPK, ERK, JNK and AKT were measured using western blot analysis. Left ventricular systolic pressure, maximum rates of increase/decrease in left ventricular pressure, creatine kinase MB activity and cardiac troponin T levels were found to be altered in the burn group 12 h after burn, which were reversed by puerarin treatment. Injection of puerarin following burn injury also reduced heart water content. Serum levels of IL‑1β, TNF‑α and IL‑6 were significantly higher in the burn group compared with those in the sham group. Puerarin treatment reduced serum levels of IL‑1β, TNF‑α and IL‑6, in addition to reducing MPO activity and MDA levels in myocardial tissues. Puerarin inhibited the activation of caspase‑3, p38, ERK and JNK following severe burn, but elevated Akt activation following severe burn. In conclusion, puerarin improved cardiac function in rats following severe burn injury, which may be due to reduced myocardial injury, inhibition of cardiomyocyte apoptosis and reduced oxidative inflammatory stress; the MAPK and AKT signaling pathways are proposed to the underlying mechanism of these findings.
研究领域:
药理学
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心脏病学
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病理生理学
·
免疫学
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DOI
PubMed
高影响因子
Current Molecular Pharmacology
·
2026
·
IF 7.2
Danhua Zhu,Qingmiao Shi,Xiaoxi Ouyang,Yanhong Zhang,Xiaopeng Yu,Long Yang,Kunkai Su,Lanjuan Li
Background Cholestatic liver fibrosis is a common pathological manifestation of various biliary tract diseases. Given the limited efficacy of current pharmacotherapies, there is a clear need to develop novel and effective treatment strategies. This study aims to evaluate the protective effects of puerarin against cholestatic liver fibrosis. Methods The therapeutic efficacy of puerarin was assessed in a bile duct ligation rat model. Collagen deposition was evaluated using picrosirius red staining and Masson’s trichrome staining. Immunohistochemistry for cytokeratin 7 (CK7) and CK19 was performed to assess bile duct proliferation. Hepatic mRNA expression profiles and metabolic profiles were analyzed by transcriptome sequencing and untargeted metabolomics, respectively. In parallel, in vitro experiments were conducted using HepaRG hepatocyte cultures exposed to a bile acid mixture, with cell proliferative capacity assessed via EdU assays. Results Puerarin treatment ameliorated serum biochemical abnormalities, histological injury, and bile duct proliferation in the cholestatic liver fibrosis rat model. Mechanistically, puerarin modulated extracellular matrix deposition and regulated the PI3K-Akt signaling pathway. Furthermore, metabolomic analysis indicated that puerarin altered the hepatic bile acid profile, promoting the conjugation of hydrophobic bile acids. In vitro studies demonstrated that puerarin attenuated bile acid mixture-induced hepatotoxicity in hepatocytes. Conclusion The present study suggests that puerarin may alleviate cholestatic liver fibrosis, potentially by reducing bile duct proliferation, modulating extracellular matrix deposition, and promoting the conjugation of toxic bile acids. These findings indicate that puerarin could be a candidate therapeutic agent for cholestatic liver fibrosis. Further studies are required to fully elucidate its net protective effect on bile acid homeostasis.
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高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2023
·
IF 7.5
Hai-Tao Li,Kun Zhong,Yun-Fei Xia,Jian Song,Xiao-Qing Chen,Wei Zhao,Xu-Hui Zeng,Tian-Xing Chen
Male infertility is a global concern, with a noticeable increase in the decline of spermatogenesis and sperm quality. However, there are limited clinically effective treatments available. This study aimed to investigate the potential effectiveness of puerarin in treating male infertility, which leads to gonadal changes. The results obtained from various analyses such as CASA, immunofluorescence, DIFF-Quick, hematoxylin and eosin (H&E), and periodic acid-Schiff (PAS) staining demonstrated that puerarin supplementation significantly alleviated the busulfan-induced reduction in spermatogenesis and sperm quality in both young and adult mice. Furthermore, puerarin exhibited a marked improvement in the damage caused by busulfan to the architecture of seminiferous tubules, causal epididymis, blood-testicular barrier (BTB), as well as spermatogonia and Sertoli cells. Similarly, puerarin significantly reduced the levels of total antioxidant capacity (T-AOC), malondialdehyde (MDA), and caspase-3 in the testes of busulfan-induced mice, as determined by microplate reader analysis. Additionally, RNA-seq data, RT-qPCR, and western blotting revealed that puerarin restored the abnormal gene expressions induced by busulfan to nearly healthy levels. Notably, puerarin significantly reversed the impact of busulfan on the expression of marker genes involved in spermatogenesis and oxidative stress. Moreover, puerarin suppressed the phosphorylation of p38, ERK1/2, and JNK in the testes, as observed through testicular analysis. Consequently, this study concludes that puerarin may serve as a potential alternative for treating busulfan-induced damage to male fertility by inactivating the testicular MAPK pathways. These findings may pave the way for the use of puerarin in addressing chemotherapy- or other factors-induced male infertility in humans.
研究领域:
生殖生物学
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药理学
·
分子生物学
·
细胞生物学
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DOI
PubMed
高影响因子
Food Bioscience
·
2025
·
IF 5.9
Bo Ma,Rong Li,Feng Li,Xiao Hu,Yechuan Huang
This paper uses inhibition kinetics, fluorescence spectroscopy, molecular docking, and molecular dynamics simulation to study how Puerarin (PUE) inhibits mushroom tyrosinase. Inhibition kinetics reveals that PUE inhibits tyrosinase in a reversible mixed-type manner with an IC 50 of 0.816 mmol/L and prefers binding to free tyrosinase. Fluorescence spectroscopy shows PUE binds spontaneously via static quenching with hydrophobic interactions as the main binding force and a single binding site. Synchronous and 3D fluorescence indicate PUE increases the microenvironment polarity of tyrosinase. Molecular docking confirms PUE can compete for the binding site and form a ternary complex. Molecular dynamics shows the tyrosinase/PUE complex is stable. In short, PUE inhibits tyrosinase by spontaneous binding in a reversible mixed-type manner. This characteristic provides theoretical support for its potential applications in the food industry, such as inhibiting browning and preserving fruits and vegetables, and in the cosmetics industry, such as serving as a natural whitening ingredient.
研究领域:
酶抑制
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食品科学
·
化妆品科学
·
计算生物学
·
生物化学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Min Pan,Linyu Nian,Lin Chen,Jiang Jiang,Debo Luo,Shijia Ying,Chongjiang Cao
As the largest emitter of greenhouse gases, the livestock and poultry industry is facing the challenge of increasing production to meet global demand while reducing environmental impacts. Improving feed digestibility by optimizing feed structure (e.g., exogenous additive) is one of the green breeding measures to alleviate carbon pressure. In this study, the interaction mechanism and in vitro digestibility properties of puerarin (PUE) with feed proteins (zein and soy protein isolate (SPI)) to form Zein-PUE and SPI-PUE complexes were investigated mainly by multispectral and molecular docking techniques. Results indicated that the addition of PUE improved the physicochemical properties of proteins (e.g., solubility and disulfide bond contents). Then, the spectral results showed that the binding processes were spontaneous, and the protein structure tended to loose and disordered after binding, and more hydrophobic residues were exposed to the hydrophilic microenvironment. Moreover, on the basis of molecular docking revealed that PUE bound to zein by hydrogen bond, electrostatic and hydrophobic interactions, while with SPI by hydrogen bond and hydrophobic interaction. Finally, in vitro digestion experiments demonstrated that the bioavailability of Zein-PUE and SPI-PUE complexes increased by 1.15 % and 2.11 %, respectively. Overall, PUE is a promising feed additive beneficial for enhancing protein digestibility and bioavailability.
研究领域:
农业科学
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食品科学
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生物技术
·
分子生物学
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DOI
PubMed
高影响因子
ACS Omega
·
2025
·
IF 4.3
Wenhui Chen,Huan Deng,Yuehan Dong,Xiangjie Wu,Zinuo Xia,Yang Zhou,Lin Yang,Zhijun Huang,Wenjin Xu,Peihu Xu,Haixing Xu
Osteochondral injuries, which could result in cartilage defects and damage to the subchondral bone, pose a significant challenge in the design of scaffolds for bone repair due to the different characteristics of bone and cartilage. In this study, we developed a double-network bilayer hydrogel scaffold composed of an upper layer and a lower layer reinforced with a ZnO nanoparticle. The double-network hydrogel consisted of carboxymethyl chitosan (CMCS), oxidized sodium alginate (OSA), and poly(vinyl alcohol) (PVA) networks. The upper and lower layers were, respectively, loaded with puerarin (Pue) and curcumin (Cur) to facilitate simultaneous repair of cartilage and bone. The scaffold exhibited better water absorption, mechanical properties (tensile strength: 0.8 MPa), self-healing capacity (healing efficiency ≥ 90%), and adhesion (adhesive stress: 0.1 MPa). Approximately 70% of Pue was rapidly released within the first 5 days, while Cur, encapsulated in ZnO, exhibited sustained release over a period of 20 d. In vitro cell experiments revealed that soluble extracts from the scaffolds were noncytotoxic and promoted elevated alkaline phosphatase (ALP) expression and calcium deposition in MC3T3-E1 subclone 14 (MC3T3-14) cells, thereby enhancing bone repair. Meanwhile, extracts fostered the proliferation of ATDC5 cells and glycosaminoglycan (GAG) production, contributing to cartilage repair. In conclusion, the bilayer hydrogel has good properties and is beneficial for the proliferation and differentiation of osteoblasts and chondrocytes.
研究领域:
生物材料学
·
组织工程
·
再生医学
·
骨科学
·
药剂学
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纳米医学
·
细胞生物学
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产品关联
DOI
PubMed
高影响因子
IN VITRO CELLULAR & DEVELOPMENTAL BIOLOGY-ANIMAL
·
2026
·
IF 2
Jiang Bo,Fu Fenyu,Yu Shiqiang,Wang Yinbo,Chen Lei,Xiu Zhilong
Corticosterone (CORT) is a glucocorticoid hormone whose prolonged elevation during stress can generate excessive reactive oxygen species (ROS), leading to hippocampal neuron dysfunction. Puerarin, a natural isoflavone extracted from Pueraria lobata , has known antioxidant and neuroprotective properties. However, its effects on CORT-induced neurotoxicity have not been well characterized. In this study, we investigated the effects of puerarin on CORT-induced damage in primary mouse hippocampal neurons. We found that CORT (100–800 μM) dose-dependently reduced neuronal viability, whereas cultured astrocytes remained viable except at the highest concentration (800 μM), indicating a relative resistance of astrocytes to CORT. CORT treatment also significantly impaired neurite outgrowth, increased lactate dehydrogenase (LDH) release, elevated intracellular ROS levels, and decreased antioxidant enzyme activities in neurons. Importantly, pretreatment with puerarin markedly ameliorated these CORT-induced effects: puerarin preserved neurite length, suppressed LDH leakage and ROS accumulation, and restored activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). These results demonstrate that puerarin can attenuate CORT-induced hippocampal neuron dysfunction in vitro. Our findings suggest that puerarin has potential therapeutic value for oxidative stress-related neural impairment in stress-related disorders.
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DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2021
·
IF 3.981
Lan Mo,Guang-lei Zhao,Xiao-feng Li,Xing-long Xiao,Ning He,Hai-xia Xu,Yi-gang Yu
Design and synthesis of prodrugs is an effective strategy to develop new drugs. Puerarin is well-known for its pharmacological properties in the treatment of many cardiovascular and cerebrovascular related diseases. To cope with its poor liposolubility that limited practical applications, we successfully developed a new type of clean and efficient esterification medium for acylation modification of puerarin and studied the relative oral absorption, including pharmacokinetics , tissue distribution and metabolite after oral taking of puerarin acid esters in comparison with free puerarin in rats. In the 1-Ethyl-3-Methylimidazoliumacetate, puerarin had the good solubility, and the reaction showed great initial rate (46.71 mmol/(L*h)) and substrate conversion (63.91%). The results of oral absorption showed that the administration of long-chain fatty acid esters of puerarin, puerarin hexanoate and puerarin myristate , resulted in significantly higher levels of puerarin in the plasma and tissues, especially in the heart, cerebral cortex, hippocampus and corpus striatum. Overall, these findings collectively supported that puerarin acid esters administration led to greater circulating concentration of puerarin and had a reduced excretion rate, providing significant advantages and theoretical basis for their application in functional foods and pharmaceutical industries.
研究领域:
药物化学
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药理学
·
生物医学工程
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DOI
高影响因子
ACS Omega
·
2025
·
IF 4.3
Yunxiao Liu,Chengguang Zhao,Xiang Hu,Chengde Wang,Yiyuan Xi,Xiaofen Ni
Puerarin (PU) helps slow down and control the harmful progression of atherosclerosis (AS) by reducing inflammation, inhibiting foam cell formation, and exhibiting anticoagulant effects. However, its clinical application is limited due to its low bioavailability and other drawbacks. In recent years, nanoparticle-based therapeutic strategies targeting reactive oxygen species (ROS) at AS pathological sites and enhancing drug bioavailability and biocompatibility have shown great potential for AS treatment. In this study, we developed ROS-responsive cinnamaldehyde polymer nanoparticles loaded with PU (RGCP@PU NPs) for the treatment of AS. These nanoparticles demonstrate good stability and biocompatibility in physiological environments and can respond to ROS in the AS pathological environment, thereby releasing the encapsulated PU. In vitro experiments showed that these nanoparticles effectively inhibited oxidative stress and inflammation levels. In in vivo studies, RGCP@PU NPs were able to stabilize atherosclerotic plaques, prevent their further deterioration, and delay the progression of AS. Moreover, compared to free PU, these nanoparticles exhibited superior therapeutic effects in inhibiting AS progression. Therefore, RGCP@PU NPs represent a promising nanocarrier that not only effectively suppresses AS progression but also provides a new approach for the design of responsive drug delivery systems for AS treatment.
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高影响因子
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