CELL BIOCHEMISTRY AND BIOPHYSICS
·
2014
·Vol. 71
·期 1
·367-373
·
IF 2.38
Gan Maozhou,Yin Xiaodong
This research designed to explore the antitumor activity of puerarin against human mantle cell lymphoma (MCL). Cell proliferation and apoptosis were assessed by MTS and flow cytometry. Caspase-3, -8, and -9 activities were assessed with the colorimetric caspase protease assay. Apoptotic proteins like PARP, cyclin D1, Bcl-2 family, XIAP, and cIAP I were researched by western blot. The PI3K inhibitor LY294002 was used to investigate the possible mechanism relating the PI3K/Akt signaling pathway. Puerarin in vitro inhibited proliferation and induced apoptosis of Z138 cells. Expressions of PI3K and p-Akt were downregulated by puerarin. Puerarin negatively regulated NF-κB activity by inhibiting NF-κB phosphorylation with nuclear translocation inhibition. This kind of effects was correlated with the suppression of expression of cyclin D1, BAX, Bcl-2, XIAP etc. This function was modulated by the PI3K inhibitor. Our results demonstrated that puerarin can induce growth arrest and apoptosis in MCL cells and that the mechanism may involve the NF-κB signaling pathway. Puerarin may have therapeutic applications in the treatment of MCL.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
·
信号转导
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PubMed
高影响因子
JOURNAL OF MATERIALS SCIENCE
·
2020
·Vol. 55
·期 15
·6669-6677
·
IF 3.553
Li Wan
Hydrogels as drug carriers for delivery of antibiotics are rarely derived from natural molecules and often require complicated synthesis. Puerarin is an herbal natural product that can self-assemble to form pH-sensitive hydrogels without any structural modification. However, Puerarin hydrogels have poor thermostability and weak mechanical strength. In this work, we prepared N -(9-fluorenylmethoxycarbonyl)- l -phenylalanine (Fmoc–Phe–OH) nanofiber-reinforced Puerarin hydrogels with good mechanical and antibacterial properties for suitable drug carriers. The phase transition temperature of Puerarin hydrogels can be increased from 35 to 55 °C by adding only 6 mg/mL of Fmoc–Phe–OH. Rheological study indicated that the presence of Fmoc–Phe–OH not only increased the storage modulus of Puerarin hydrogels by five times, but also did not affect their pH sensitivity. SEM study and pore analysis indicated that Fmoc–Phe–OH nanofibers intertwined with the Puerarin assembly, leading to enhancement of mechanical property of hydrogel. Antibacterial test indicated that the reinforced Puerarin hydrogels have antibacterial property compared with Puerarin hydrogels. Based on these features, a controllable release of loaded model drug (berberine hydrochloride) can be realized from the reinforced Puerarin hydrogels, showing a good synergistic antimicrobial effect on the S. aureus .
研究领域:
药学
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材料科学
·
生物医学工程
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DOI
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
·
2024
·
IF 4.4
Yanqiu Long,Jie Hu,Yan Liu,Danqing Wu,Zhiyun Zheng,Shuangying Gui,Ning He
Diabetic retinopathy, an ocular complication of diabetes, is an important cause of blindness in adults. Puerarin is considered to have promising potential for clinical use in treating diabetic retinopathy. In this study, we designed a novel puerarin-loaded poly(lactic acid) sustained-release microspheres suitable for ocular administration, and we assessed its in vitro and in vivo properties. The preparation of puerarin-loaded microspheres was optimized by Box-Behnken response surface design. The encapsulation efficiency and drug loading of microspheres were 35.71% and 3.85%, respectively. The microspheres exhibited good dispersion and high safety, making it suitable for ocular drug delivery . In vitro release demonstrated that microspheres had a well-sustained release effectiveness, and its release behavior complied with the zero-order kinetic characteristics. The results of ocular tissue distribution revealed that the C max and AUC 0-∞ of the microspheres group in the retina and choroid were considerably higher than those of the solution group and the intravenous injection group. This research revealed that intravitreal injection of microspheres can significantly prolong the half-life of puerarin in eye tissues and achieve sustained drug release . Therefore, intravitreal injection of microspheres has positive implications for the treatment of diabetic retinopathy.
研究领域:
药学
·
眼科学
·
药物递送系统
·
糖尿病研究
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DOI
PubMed
高影响因子
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.
研究领域:
药理学
·
药剂学
·
细胞生物学
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DOI
PubMed
高影响因子
International Journal of Endocrinology
·
2025
·Vol. 2025
·期 1
·4473803
·
IF 2.3
Song Xue,Wei Fan,Qingping Li,Hong Huang,Yibo Tang,Min Wu
Background: This study aimed to investigate the potential mechanisms of puerarin in alleviating diabetic nephropathy (DKD) in mice. Method: The DKD model was induced by multiple low-dose injections of streptozotocin (STZ) and a high-sugar and high-fat diet in male C57BL/6J mice. After confirming the onset of DKD, mice were given irbesartan, distilled water, or different concentrations of puerarin (40 and 80 mg/kg/d) by gavage for 8 weeks. HE staining and PAS staining were adopted to assess the pathological changes in the kidney tissues. Meanwhile, the levels of superoxide dismutase, catalase, creatinine, and cystatin C in the serum and the urine albumin and creatinine were measured, and the renal indices as well as the urinary albumin-to-creatinine ratio (UACR) were calculated. The changes of podocin and protein expression levels associated with AMPK/Nrf2 signaling pathway were evaluated by western blot. Results: Puerarin significantly reduced the level of fasting blood glucose, renal index, glomerular mesangial expansion index, renal function, and oxidative stress induced by STZ ( p < 0.05). The pathological injuries in kidney tissues were also alleviated. Furthermore, we demonstrated that the expression level of podocin and protein related to the AMPK/Nrf2 signaling pathway was also decreased significantly by the treatment of puerarin. At the same time, the efficacy of puerarin in the treatment of DKD was better than that of irbesartan, and the treatment effect of the high-dose group (80 mg/kg/d) was also significantly better than that of the low-dose group (40 mg/kg/d). Conclusion: Puerarin could attenuate the severity of DKD and protect the podocyte in mice in a dose-dependent way. Also, it might be performed by regulating the AMPK/Nrf2 pathway. These findings may provide a theoretical basis for updating the clinical management of DKD.
研究领域:
医学
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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
EUROPEAN JOURNAL OF PHARMACOLOGY
·
2025
·
IF 4.7
Shuai Wang,Yue Liu,Mengyao Cui,Xingyu Zou,Mengjun Pan,Dayuan Jiang,Tingting Chang,Hongye Xu,Deling Wu,Xiaoqin Chu
The low oral bioavailability of puerarin (Pue) affects its therapeutic effect. The aim of this study is to enhance the absorption of Pue and improve therapeutic efficacy by adding cinnamaldehyde (CA). The pharmacokinetics of Pue in rats were studied using oral administration: CA+Pue, and single Pue. The Caco-2 cell model was used to investigate the effect of CA on the absorption and transport of Pue. The absorption sensitivity of TSG to P-gp inhibitors verapamil (Ver), Ko143, and MK-571 in vivo were simultaneously evaluated, and assessed the effects of ATP binding cassette (ABC) transporter inhibitors (such as P-gp inhibitors verapamil, MK-571, and BCRP inhibitor Ko143) on predicting targeted transport of active ingredients to explore the relationship between Pue transport and inhibition of these efflux proteins. A rat model of middle cerebral artery occlusion (MCAO) was established to explore the therapeutic effect of single Pue and Pue with CA on ischemic stroke (IS). The results showed that compared with Pue suspension, CA increased the absorption of Pue in rats, with C max and AUC (0-t) being 4.84 times and 11.54 times higher, respectively. Both P-gp and MRP play a role in the transport mechanism of Pue. Compared with single Pue, the transmembrane transport from Basolateral (BL) to Apical (AP) side of Pue was significantly reduced when Pue was applied in combination with CA. In addition, the efflux ratio (ER) value also significantly decreased. This discovery suggests that CA may reduce the secretion of Pue, thereby enhancing its absorption and transport by inhibiting exocytosis mediated by efflux transporters, similar to the effect of Ver. On the other hand, in the MCAO rat model, Pue+CA reduced the extent of cerebral infarction, alleviated pathological damage, significantly reduced the level of inflammatory mediators, and increased the release of anti-inflammatory factors, suggesting that CA can synergize with Pue to exert a better therapeutic effect on IS. Therefore, the combination of Pue and CA for the treatment of IS has profound scientific significance and rationality from the points of disposition and pharmacodynamics in vivo.
研究领域:
药理学
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神经科学
·
中药学
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DOI
PubMed
高影响因子
Materials Today Bio
·
2025
·
IF 10.2
Shaobo Zhai,Jiaqian You,Zheng Yang,Yang Liu,Tianming He,Yuchuan Wu,Xuyan Wei,Mucong Li,Xiaolu Shi,Fengxiang Gao,Shunli Chu
Wound infection is a serious clinical challenge, often accompanied by persistent inflammatory response and the threat of increased bacterial resistance, there is an urgent requirement to develop a wound dressing with potent antimicrobial as well as immunomodulatory effects. In this study, we developed a multifunctional wound dressing to promote healing of infected wounds by doping puerarin-loaded mesoporous polydopamine nanoparticles into a carboxymethyl chitosan/sodium alginate oxide-based hydrogel. The hydrogel has good injectability, adhesion, and self-healing capabilities, and can be well matched to irregular wounds and against external injuries. The loaded PUE is rapidly released from the hydrogel in response to near-infrared (NIR) laser irradiation, which has a controlled release property. In addition, under NIR laser irradiation, the hydrogel with good photothermal properties exerted good antimicrobial properties through localized high temperature, and exhibited good antioxidant, immune microenvironment modulation, and pro-angiogenic effects through accelerated released PUE. In the E. coli-infected full-thickness skin wounds healing experiments, the hydrogel can effectively kill bacteria, regulate the immune microenvironment, promote collagen deposition and angiogenesis, and significantly accelerate the wound healing, showing promising applications.
研究领域:
生物医学工程
·
药剂学
·
感染与免疫
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DOI
PubMed
高影响因子
npj Science of Food
·
2025
·Vol. 9
·期 1
·1-11
·
IF 7.8
Ma Bo,Miao Yuanxin,Xu Yan,Li Feng,Zhu Deyan,Li Rong,Huang Yechuan
This study evaluated the in vitro and in vivo antioxidant activities of puerarin (PUE) and β-lactoglobulin (β-lg). The results of the in vitro antioxidant assay revealed that the DPPH and ABTS radical scavenging rates of the PUE/β-lg complex were generally superior to those of free PUE within the tested experimental concentration range. The in vivo antioxidant activity assay, using Caenorhabditis elegans ( C. elegans ) as a model organism, showed that the PUE/β-lg complex significantly increased the superoxide dismutase (SOD) activity and reduced glutathione (GSH) content in C. elegans , and also increased the mean lifespan of C. elegans under oxidative and thermal stress conditions. Transcriptomic analysis showed that the PUE/β-lg complex regulated the mRNA expression levels of genes associated with the activation of various signaling pathways, such as the longevity regulation pathway, insulin signaling pathway, and GSH metabolism. Overall, this study demonstrated the potential of the PUE/β-lg complex as an antioxidant, which can lead to its development into food products or pharmaceuticals.
研究领域:
生物化学
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分子生物学
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药理学
·
食品科学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
Bioactive Materials
·
2025
·
IF 20.3
Yi Wang,Yansheng Qu,Xiangmei Liu,Jin Huang,Congyang Mao,Chaofeng Wang,Shengli Zhu,Yufeng Zheng,Zhaoyang Li,Zhenduo Cui,Hui Jiang,Yang Lv,Jie Shen,Shuilin Wu
Periodontitis is an inflammatory disease caused by the imbalance of the periodontal microbial ecosystem. Traditional treatment methods not only kill pathogenic bacteria but also inhibit the growth of beneficial bacteria, thereby disrupting the balance of the oral microbial ecosystem. In this study, chitosan, hyaluronic acid, and puerarin were coated on live Lactobacillus rhamnosus to form probiotic-based PSCLR nanoparticles. Subsequently, these nanoparticles were encapsulated in hydrogel microspheres through emulsion polymerization and immobilized in the hydrogel network via the covalent cross-linking of methacrylate-modified hyaluronic acid. This hydrogel restores the balance of oral microbiota by reducing pathogenic bacteria and promoting probiotic diversity, which helps maintain ecological stability and minimize risks associated with microbial community dysbiosis. In addition, puerarin in the gel achieves analgesic and neuromodulatory effects by specifically antagonizing the P2X 3 receptor, which affects pain transmission. This study provides a potential strategy for the antibiotic-free treatment of periodontitis and the neuropathic pain associated with it.
研究领域:
生物医学工程
·
口腔医学
·
免疫学
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DOI
PubMed
高影响因子
Foods
·
2026
·Vol. 15
·期 13
·2292
·
IF 6
Linfen Wu,Siqian Guo,Minxin Liu,Kexi Ma,Yu Lan,Jingming Li
Glycyrrhizic acid (GA), a high-potency natural sweetener derived from licorice, has long been limited in alcoholic beverages due to its characteristic lingering sweetness in both aqueous and ethanol matrices. From an industrial perspective, licorice extract offers superior economic viability and processing efficiency compared to high-purity monomers. To clarify the sensory behaviour of licorice extract in formulated spirits, this study characterized the sensory attributes of licorice extract (containing 23.75% GA) in 42% and 52% vol base spirits. Quantitative results showed that the detection thresholds, recognition thresholds, and upper limits of comfort were 2.23, 15.45, and 75.13 mg/L in the 42% vol base spirit, and 5.28, 25.64, and 72.98 mg/L in the 52% vol base spirit, respectively. Suitable addition levels were identified as 30 mg/L for 42% vol and 40 mg/L for 52% vol base spirits. The relative sweetness of GA was determined to be 175.83 times that of sucrose. Sucrose showed a sweetness duration of 10 to 12 s, whereas licorice extract exceeded 16 s. Puerarin showed the strongest effect in mitigating lingering sweetness, reducing the sweetness duration to values comparable to those of sucrose at 50 mg/L in the water system and 30 mg/L in the 10% vol edible alcohol system. Molecular docking suggested that puerarin may interact more favourably with the sweet taste receptor than GA, with a binding energy of −52.72 kJ/mol, and may weaken the predicted GA–receptor interaction, as reflected by the shift in GA binding energy from −41.00 to −21.30 kJ/mol. Overall, this study provides sensory parameters specific to different ethanol matrices for applying licorice extract in formulated spirits and offers a plausible receptor-level explanation, supported by molecular docking, for the ability of puerarin to mitigate GA-induced lingering sweetness, thereby supporting the development of formulated spirits with reduced sugar content.
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DOI
PubMed
高影响因子
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.
研究领域:
药学
·
材料科学
·
药物递送系统
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DOI
高影响因子
Food & Function
·
2021
·Vol. 12
·期 13
·5949-5958
·
IF 5.396
Lan Mo,Guang-lei Zhao,Xiao-feng Li,Xing-long Xiao,Ning He,Juan-juan Ma,Yi-gang Yu
Acylation has become one of the most widely used methods to improve the lipid solubility and bioavailability of flavonoids. In this study, puerarin acid esters (PAES) with different chain lengths were synthesized via biocatalytic acylation. This was the first study to evaluate the digestion and transport profiles and immunocompetence of PAES. The relationship between the digestion and transport profiles and potential immunocompetence of the acylated derivatives in Caco-2 cell monolayers was also explored. Puerarin and PAES remained stable in gastric phases, whereas different degrees of hydrolysis of PAES were found in the intestine. PAES with less than 12 carbon chains were positively correlated with the degree of hydrolysis, while those with more than 12 carbon chains showed higher resistance to hydrolysis by the artificial human digestive juice. The apparent permeability coefficients of puerarin, puerarin acetate, puerarin propanoate, puerarin butyrate, puerarin hexanoate, puerarin octanate and puerarin laurate were 1.62 ± 0.09, 1.70 ± 0.15, 1.89 ± 0.19, 1.86 ± 0.18, 2.29 ± 0.12, 4.06 ± 1.01 and 2.32 ± 0.88 × 10−6 cm s−1, respectively, in Caco-2 cell monolayers. The results of the immune factor assays indicated that puerarin propanoate, puerarin hexanoate and puerarin myristate could significantly promote the secretion of IL-6, TNF-α and IL-10. These findings suggested that a better absorption could be predicted after oral intake using PAES. Meanwhile, the concentration of esters and their metabolites (puerarin) found in the digestion and transport profiles directly affected their potential immunocompetence.
研究领域:
药理学
·
生物化学
·
免疫学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）