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JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY · 2015 ·Vol. 82 ·期 3 ·453-460 · IF 1.488

An investigation into the preparation, characterization and antioxidant activity of puerarin/cyclodextrin inclusion complexes

Li Shujing,Yue Junzhi,Zhou Wei,Li Li

The inclusion complexes between puerarin and three cyclodextrins (CDs), namely β-cyclodextrin (β-CD), (2-hydroxy)propyl-β-cyclodextrin (HP-β-CD, DS = 4.2) and methyl-β-cyclodextrin (Me-β-CD, DS = 12.5) were prepared. The effects of the complexation on the stability of puerarin were investigated in both solution and the solid state by methods of phase solubility study, XRD, DSC and SEM. Furthermore, the antioxidant activities of puerarin and puerarin/CDs inclusion complexes were determined by reducing power and 1,1-diphenyl-2-picryl-hydrazyl methods. Results showed that puerarin formed 1:1 stoichiometric inclusion complexes with β-CD, HP-β-CD and Me-β-CD. Additionally, the solubility and thermal stability of puerarin was improved after encapsulating by CDs. Antioxidant activity studies showed that the antioxidant performance of the inclusion complex was better than the native puerarin, and puerarin/Me-β-CD complex was the most effective form. It can be a potentially promising way to develop a new formulation of puerarin for herbal medicine or healthcare products.

研究领域: 药学 · 化学
✓ 已验证 DOI 高影响因子
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ULTRASONICS SONOCHEMISTRY · 2024 · IF 8.7

Improving complexation of puerarin with kudzu starch by various ultrasonic pretreatment: Interaction mechanism analysis

Yuheng Li,Chao Zhang,Shuyi Li,Zhenzhou Zhu,Xuehua Wang,Giancarlo Cravotto

The industrial preparation of kudzu starch (KS) significantly reduces the remaining of flavonoids like puerarin (PU) in the product, weakening its biological activity and making pre-treatments on kudzu crucial. Ultrasonic technique, widely used for modifying biomolecules, can enhance nutrient interactions like those between starch and polyphenols in foods. Thus, a puerarin-kudzu starch (PKS) complex was prepared with the introduction of ultrasonic pretreatment. The results indicated that sonication increased the binding of PU to KS from 0.399 ± 0.01 to 0.609 ± 0.05 mg/g. Particle size analysis and SEM revealed that the particles of the ultrasonic puerarin-kudzu starch complex (UPKS) were larger than those of the untreated complexes. XRD, UV–vis, and FT-IR spectroscopic analyses indicated that hydrogen bonding primarily governs the interaction between PU and KS. Additionally, incorporating PU decreased the starch structure’s orderliness, while ultrasonic treatment altered the helical configuration of straight-chain starch, leading to the formation of a new, ordered structure through the creation of new hydrogen bonds. Additionally, gels formed from UPKS exhibited higher viscosity, elasticity, and shear stress, suggesting that ultrasound significantly altered the intermolecular interactions between PKS. In conclusion, the use of ultrasound under optimal conditions has demonstrated its effectiveness in preparing PKS complexes, highlighting its significant potential to produce high value-added kudzu-based products.

CAS / MDL: 7553-56-2 7681-11-0
研究领域: 食品科学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SENSORS AND ACTUATORS B-CHEMICAL · 2016 · IF 4.758

Engineering graphene/quantum dot interfaces for high performance electrochemical nanocomposites in detecting puerarin

Hucheng Zhang,Yingying Shang,Ting Zhang,Kelei Zhuo,Jianji Wang

CdTe quantum dots (QDs) capped by 1-ethyl-3-methylimidazolium mercaptopropionate ([emim]MP) and the reduced graphene oxide (RG) modified by the amine-terminated ionic liquid ([amim]Br) were synthesized in this work. The coordinating interface interactions between QD and RG render the nanocomposite the excellent electrochemical performances as revealed by cyclic voltammetry, chronocoulometry, and electrical impedance spectroscopy. Based on the experimental results obtained from amimRG, CdTe@MP-amimRG, CdTe@[bmim]MP-amimRG, and CdTe@[emim]MP-amimRG nanocomposites, it is proposed that the synergistic effects between imidazolium rings and graphene are responsible for the enhanced performances. Taking the CdTe@[emim]MP-amimRG nanocomposite as the electrochemical sensor of puerarin, the proposed method demonstrates the linear range over 0.01–4.0   μmol   L −1 with the detection limits of 6   nmol   L −1 in the aqueous solution (S/N   =   3). Moreover, the sensor exhibits fast response time (2s), high sensitivity (74.57   μA   μmol   L −1   cm −2 ), as well as reproducibility (RSD   ≤   8%), and can maintain the stability at 4   °C for two weeks.

研究领域: 材料科学 · 分析化学 · 生物医学工程
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EUROPEAN JOURNAL OF PHARMACOLOGY · 2019 · IF 3.17

Puerarin inhibits vascular calcification of uremic rats

Hailin Liu,Xiuli Zhang,Xinglong Zhong,Zehua Li,Shaoai Cai,Pingzhen Yang,Caiwen Ou,Minsheng Chen

The risk of cardiovascular events in patients with chronic kidney disease is tremendously increased due to vascular calcification . Local vascular inflammation significantly promotes vascular calcification. A previous study has shown that puerarin inhibits calcification of mouse vascular smooth muscle cells (VSMCs) in vitro, but whether puerarin can inhibit vascular calcification in vivo and the underlying mechanisms remain unclear. In this study, we found that rat VSMCs treated with calcifying medium showed more mineral deposition, and this effect was inhibited by puerarin in a dose-dependent manner, as detected by alizarin red staining and calcium content assay. Puerarin also prevented the trans-differentiation of VSMCs into osteoblast-like cells, indicated by down-regulation of bone-related genes including Runx2 and BMP2 . In vivo study of uremic rats induced by renal nephrectomy further confirmed the inhibitory effect of puerarin on vascular calcification in uremic rats. Puerarin treatment significantly prevented mineral deposition in rat aortas and down-regulated the expression of Runx2 and BMP2. Furthermore, we detected the levels of pro-inflammatory cytokines including IL-1β, IL-6, IL-18 and TNFα in vitro and in vivo . The levels of IL-1β were remarkably increased in both calcified VSMCs and aortas of uremic rats, while puerarin treatment markedly decreased the expression of IL-1β. In addition, we found that puerarin reduced IL-1β possibly through targeting NLRP3/Caspase1/IL-1β and NF-κB signaling pathways and inhibiting the generation of reactive oxygen species . Taken together, we demonstrated that puerarin has the capability of inhibiting vascular calcification in uremic rats by inhibiting inflammation.

CAS / MDL: 32222-06-3
研究领域: 药理学 · 心血管疾病 · 肾脏疾病 · 炎症
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food Frontiers · 2026 ·Vol. 7 ·期 5 ·e70343 · IF 6.3

Puerarin-Loaded Macrophage-Derived Exosomes for Experimental Atherosclerosis

Zijian Zou,Liangxing Tu,Ye Yang,Jianfang Feng,Yi Jin,Ruyue Yang,Meng Cheng

Atherosclerotic cardiovascular disease (AS) remains a leading global health concern. In this study, we investigated a macrophage-derived exosome-based delivery system for puerarin (Pue). The isolated vesicles were characterized by transmission electron microscopy, particle-size and zeta-potential analysis, and Western blot validation of extracellular vesicle-associated markers, including CD63, CD9, CD81, TSG101, and Alix, together with Calnexin as an endoplasmic-reticulum-associated negative/depletion marker. In vitro experiments showed that exosome-based delivery enhanced cellular uptake of puerarin and was associated with reduced oxidative-stress-related signals, decreased macrophage migratory activity, and reduced foam-cell-related readouts under the tested conditions. In vivo studies using an ApoE−/− mouse model showed that Pue–Exos reduced aortic plaque burden, promoted collagen deposition, and improved serum lipid-related indices. No obvious histopathological abnormalities were observed in major organs after treatment, suggesting preliminary in vivo tolerability. Mechanistic evaluation in C57BL/6 mice showed that treatment was associated with increased expression of HIF-1α, NF-κB, IL-6, IL-1β, CD68, and α-SMA under the present experimental conditions. Therefore, these findings are more appropriately interpreted as inflammation-associated signaling changes and remodeling-related responses, rather than definitive evidence of a uniformly suppressed inflammatory state or a confirmed anti-atherosclerotic mechanism. Taken together, these results suggest that macrophage-derived exosome-based delivery may improve the performance of puerarin in atherosclerosis-related experimental settings, although the underlying mechanism requires further clarification.

CAS / MDL: 28718-90-3 38215-36-0
✓ 已验证 产品关联 DOI 高影响因子
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Oncology Letters · 2017 ·Vol. 14 ·期 3 ·3006-3010 · IF 1.39

Puerarin increases the chemosensitivity of hepatocellular carcinoma cells

Zhen Wu,Jing Wu,Ping Fang,Shifeng Kan

The present study investigated the effect of puerarin (Pu) on the sensitivity of HepG2 human hepatocellular carcinoma (HCC) cells to chemotherapeutic drugs to determine the possible mechanism. HepG2 cells were treated with different concentrations of Pu and cisplatin (CDDP), alone or in combination. MTT assay was used to determine the inhibitory effects of the different drugs on HepG2 cells. Cell morphology was observed by inverted microscopy. The expression of B-cell lymphoma 2 (Bcl-2) and Bax protein was measured by western blot analysis. Pu and CDDP, alone or in combination, inhibited the proliferation of HepG2 cells. The inhibitory effect of CDDP combined with Pu on HepG2 cells was significantly higher than that of the single drug treatments (p<0.01). In addition, compared with the single drug groups, cellular morphology was significantly altered and the apoptotic rate of cells and the expression of Bax protein were significantly increased (p<0.01). However, the expression of Bcl-2 protein was significantly decreased (p<0.01) in the combined drug group. In conclusion, Pu can increase the sensitivity of HCC to chemotherapeutic drugs, enhance the inhibitory effect of chemotherapeutic drugs on cell proliferation and synergistically induce apoptosis of HepG2 cells. The mechanism is likely related to the upregulation of Bax protein and the downregulation of Bcl-2 protein.

研究领域: 肿瘤学 · 药理学 · 细胞生物学
✓ 已验证 DOI PubMed 高影响因子
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Frontiers in Behavioral Neuroscience · 2021 · IF 3.558

Puerarin Alleviates Vascular Cognitive Impairment in Vascular Dementia Rats

Zhu Tiantian,Zhu Moli,Qiu Yue,Wu Zeqing,Huang Ning,Wan Guangrui,Xu Jian,Song Ping,Wang Shuangxi,Yin Yaling,Li Peng

Cerebral ischemia triggers vascular dementia (VD), which is characterized by memory loss, cognitive deficits, and vascular injury in the brain. Puerarin (Pur) represents the major isoflavone glycoside of Radix Puerariae, with verified neuroprotective activity and cardiovascular protective effects. However, whether Pur ameliorates cognitive impairment and vascular injury in rats with permanent occlusion of bilateral common carotid arteries (BCCAO) remains unknown. This work aimed to assess Pur’s effects on BCCAO-induced VD and to dissect the underlying mechanisms, especially examining the function of transient receptor potential melastatin-related 2 (TRPM2) in alleviating cognitive deficits and vascular injuries. Rats with BCCAO developed VD. Pur (50, 100, and 150 mg/kg) dose-dependently attenuated the pathological changes, increased synaptic structural plasticity in the dorsal CA1 hippocampal region and decreased oxidative stress, which eventually reduced cognitive impairment and vascular injury in BCCAO rats. Notably, Pur-improved neuronal cell loss, synaptic structural plasticity, and endothelial vasorelaxation function might be mediated by the reactive oxygen species (ROS)-dependent TRPM2/NMDAR pathway, evidenced by decreased levels of ROS, malondialdehyde (MDA), Bax, Bax/Bcl2, and TRPM2, and increased levels of superoxide dismutase (SOD), Bcl2, and NR2A. In conclusion, Pur has therapeutic potential for VD, alleviating neuronal cell apoptosis and vascular injury, which may be related to the ROS-dependent TRPM2/NMDAR pathway.

CAS / MDL: 3681-99-0
研究领域: 神经科学 · 药理学 · 心血管研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

Enhanced Intestinal Barriers by Puerarin in Combination with Tryptophan

You Wu,Jiaojiao Li,Wenjiao Ding,Zheng Ruan,Li Zhang

The intestinal barrier is essential for maintaining human intestinal health. The growing number of studies has shown that both puerarin and tryptophan and its metabolites have a beneficial effect on the intestinal barrier. This study aims at the combination of puerarin and tryptophan or its metabolites for improving the intestinal barrier. In our study, 40 female Sprague–Dawley rats were randomly divided into five groups (n = 8) for a 4-week experiment and dextran sodium sulfate was used to induce an intestinal barrier injury in rats. Our results showed that puerarin combined with tryptophan or its metabolites (indole-3-propionic acid, IPA) improved the intestinal barrier by enhancing the mucus layer barrier, which was mainly achieved by increasing the number of goblet cells and promoting the secretion of MUC2. Both TRPM5 and VAMP8 promoted MUC2 secretion in goblet cells through exocytosis, but their mechanisms of action are different. In our study, we found that puerarin and tryptophan showed different effects on TRPM5 and VAMP8, respectively. Puerarin enhances the expression of TRPM5, and tryptophan inhibits the expression of TRPM5; however, puerarin and tryptophan have no significant effect on the expression of VAMP8.

CAS / MDL: 67-63-0
研究领域: 药理学 · 胃肠病学 · 营养学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL SCIENCES · 2024 · IF 3.7

Differentiation of puerarin chelate from salt by phase solubility test

Yuanfeng Wei,Xin Chen,Runxue Ding,Jingwen Zhang,Hui Chen,Junxiao Zhu,Jianjun Zhang,Peiya Shen

Different from salt, metal chelate is a novel state of drug constructed by more separate coordinate bonds to form a chelating circle. Due to their composition similarity, it is hard to distinguish them except identifying ionic bond (i.e., salt) or coordinate bond (i.e., chelate) in the single crystal structure. In this study, sodium chelate (CDCC No: 1865670) and lithium salt (CDCC No: 2161617) of puerarin (PUE) was prepared. In addition to difference in single crystal structure, it was found that they showed totally different phase solubility behaviors: lithium salt demonstrated a typical inverse proportion curve as other common salts, while sodium chelate exhibited disordered scatters. However, when incorporating the unit PUE-Na complex in solution state and complexation constant K 11 in chemical equation, the scatters in phase solubility diagram of chelate could be well fitted and the value of K 11 was dramatically higher with orders of magnitude than the dissociation constant K c ; while processing phase solubility curve of lithium salt by incorporating complex item, it could not well match the curve at all. PUE sodium chelate is more likely to be a weak electrolyte with partial dissociation, while PUE lithium salt acted as a strong electrolyte with complete dissociation. The phase solubility test would be served as a surrogate tool for differentiation of chelates from salts when single crystal was not available.

CAS / MDL: 1310-65-2 7447-41-8
研究领域: 药学 · 化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF APPLIED POLYMER SCIENCE · 2020 ·Vol. 137 ·期 48 ·49599 · IF 2.52

Puerarin, an efficient natural stabilizer for both polyethylene and polypropylene

Huimin Xia,Hui Gao,Qiqi Sun,Fazong Wu,Tengteng Ge,Kun Sui,Zhongwei Wang,Liang Song,Xiaowen Huang,Qing Yu

Puerarin, a natural compound, was used as multifunctional protector for polyethylene (PE) and polypropylene (PP). Firstly, puerarin and tetrakis(2,4-di-tert-butylphenol)[1,1-biphenyl]-4,4′-diylbisphosphite (PEPQ) could protect PE and PP against thermos-oxidative degradation: after modification, the oxidation induction time (OIT) of increased ca. 4,160% (PE-P 1200 -P sample) and 130% (PP-P 1200 -P sample); the carbonyl index (CI) obtained through accelerated aging decreased ca. 58% (PE-P 1200 -P sample). Secondly, it is excited to find that puerarin and PEPQ could pretect PE agianst photooxidative degradation: CI value decreased ca. 35% after modification. Thridly, the coorperation of puerarin and PEPQ was also benefit for the processing stability: the change of melt flow rate (MFR) between first and fifth extrusions decreased ca. 83% (PE-P 1200 -P sample) and 99% (PP-P 1200 -P sample). Forthly, puerarin and PEPQ could still protect PE against degradation after five extrusions: the loss of tensile strength and elongation at break decreased ca. 96% and 95% after modification. Finally, the interaction of puerarin with PEPQ was discussed and the role of puerarin in protecting polyolefins was proposed.

研究领域: 材料科学 · 化学工程 · 天然产物化学
✓ 已验证 产品关联 DOI 高影响因子
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Food & Function · 2023 ·Vol. 14 ·期 4 ·2149-2161 · IF 6.1

Puerarin extends the lifespan of Drosophila melanogaster by activating autophagy

Ai-Wen Kang,Chi Sun,Hai-Tao Li,Kun Zhong,Xu-Hui Zeng,Zhi-Feng Gu,Bing-Qian Li,Xiao-Ning Zhang,Jian-Lin Gao,Tian-Xing Chen

Lifespan longevity has attracted increasing attention with societal development. To counter the effects of aging on longevity, we focused on the natural chemicals of plants. In this study, we investigated the effects of puerarin supplementation on the lifespan of Drosophila melanogaster. Puerarin supplementation significantly extended the lifespan of D. melanogaster at 60 μM and 120 μM by upregulating proteasome subunit beta 5 (prosbeta5) and sirtuin-1 (Sirt1). However, puerarin-induced longevity of male flies (F0 generation) may not be passed on to descendants. Additionally, a puerarin diet for 10 and 25 days did not influence the body weight and food intake of male Canton-S flies. Puerarin significantly improved the climbing ability, starvation resistance, and oxidation resistance of male flies by upregulating the expression of Shaker, catalase (CAT), superoxide dismutase 1 (SOD1), and Methuselah, and downregulating poly [ADP-ribose] polymerase (PARP-1) and major heat shock 70 kDa protein Aa (HSP70). Moreover, 120 μM puerarin supplementation for 25 days significantly increased adenosine 5′ triphosphate (ATP) content by increasing adenosine 5′-monophosphate (AMP)-activated protein kinase (AMPK) levels. Additionally, the puerarin diet for 25 days suppressed male fecundity in male flies by decreasing the levels of Bam and Punt. Mechanistically, puerarin enhanced lysosome-involved autophagy by promoting the expression of lysosome markers [β-galactosidase and lysosomal associated membrane protein 1 (LAMP1)], and elevating the levels of autophagy-related genes, including autophagy-associated gene 1 (ATG1), ATG5, and ATG8b. However, puerarin decreased the phosphorylation of the target of rapamycin (TOR) protein. In conclusion, puerarin is a promising compound for improving the longevity of D. melanogaster by activating autophagy.

CAS / MDL: 3681-99-0
研究领域: 衰老研究 · 药理学 · 分子生物学 · 遗传学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF APPLIED POLYMER SCIENCE · 2015 ·Vol. 132 ·期 40 · IF 1.768

PEGylated chitosan microspheres as mucoadhesive drug-delivery carriers for puerarin

Xiaofen Hu,Yuyan Zhang,Huifen Zhou,Haitong Wan

PEGylated chitosans with different degrees of grafting were synthesized, and the application potential of microspheres based on PEGylated chitosan as mucoadhesive drug-delivery carriers for puerarin was investigated. Compared with chitosan microspheres, PEGylated chitosan microspheres (PCMs) exhibited better physical stability and higher swelling capacity, and the amount of water uptake increased as the content of poly(ethylene glycol) methyl ether in the microspheres increased. PCMs showed obviously improved mucoadhesive behavior on a mucosa-like surface. Puerarin was incorporated into the microspheres, and the release experiments in vitro showed that the PEGylation of chitosan accelerated puerarin release from the particles and decreased the retention of the drug. The abilities of all of the tested microspheres to open tight junctions and improve the permeability of puerarin were demonstrated with a Caco-2 cell monolayer as an in vitro model. The amount of puerarin permeating across the Caco-2 cell monolayer was significantly increased by the incorporation of puerarin into the PCMs. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132 , 42623.

CAS / MDL: 9012-76-4
研究领域: 药剂学 · 生物材料 · 药物传递系统
✓ 已验证 产品关联 DOI 高影响因子
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