Natural Product Communications
·
2017
·
IF 0.773
Jiang Liu,Xiansheng Wang,Sheng Geng,Benguo Liu,Guizhao Liang
The α-glucosidase inhibitory activity and behavior of taxifolin was first investigated by spectrofluorimetry and molecular docking. It was found that taxifolin inhibits α-glucosidase in a competitive manner with the IC50 value of 0.16 mg/mL. The intrinsic fluorescence quenching of α-glucosidase in the presence of taxifolin was observed by the static quenching mechanism. According to the thermodynamic study, the complex of taxifolin and α-glucosidase was maintained by van der Waals and hydrogen bonding. The binding mode provided by molecular docking simulation indicated the existence of hydrogen bonding between taxifolin and the amino acid residues of α-glucosidase (Glu429, Asp 568 and Glu771), which coincided with the result of fluorescence analysis.
研究领域:
生物化学
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药物化学
·
酶学
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产品关联
DOI
高影响因子
Heliyon
·
2024
·
IF 3.4
Kun Jiao,Maolei Sun,Wenyuan Jia,Yun Liu,Shaoru Wang,Yuheng Yang,Zhihui Dai,Liping Liu,Zhiqiang Cheng,Guomin Liu,Yungang Luo
Electrospinning is a widely recognized method for producing Janus or core-shell nanofibers. In this study, nanofibrous membranes were fabricated through co-axial electrospinning utilizing polycaprolactone (PCL) and silk fibroin (SF) as the Janus shell, and taxifolin (TAX) and SF as the core. The resulting nanofibers had diameters of 816 ± 161 nm and core diameters of 73 ± 5 nm. The morphology and properties of the PCL-SF@SF/TAX nanofibers were subsequently analyzed. The results demonstrated that the nanofibrous membranes achieved physical and chemical characteristics potential for tissue engineering and drug delivery. Specifically, the membranes exhibited a Young's modulus of 9.64 ± 0.29 MPa, a water contact angle of 79.1 ± 1.3°, and a weight loss of 17.3 ± 1.0 % over a period of 28 days. The incorporation of TAX endowed the membranes with antibacterial properties, effectively combating Escherichia coli and Staphylococcus aureus . Furthermore, the membranes demonstrated antioxidant capabilities, with a DPPH radical scavenging efficiency of 38.5 ± 5.6 % and a Trolox-equivalent antioxidant capacity of 0.24 ± 0.01 mM. The release of the antioxidant was sustained over 28 days, following first-order release kinetics. The nanofibrous membranes, referred to as PSST, exhibit promising potential for use as biomaterials, characterized by their antibacterial activity, antioxidant and cytocompatibility.
研究领域:
生物材料学
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组织工程学
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药剂学
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产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2025
·
IF 6.5
Chunli Qi,Huijie Xing,Ning Ding,Weifeng Feng,Yongyi Wu,Xingwang Zhang,Yigang Yu
Purpose: Diabetes mellitus (DM) remains a significant health challenge, with traditional treatments often failing to provide lasting solutions. Taxifolin (Tax), a potential phytomedicine with antioxidant and anti-hyperglycemic properties, suffers from low water solubility and poor bioavailability, necessitating advanced delivery systems. This study aims to nanometerize taxifolin (Tax) into selenized liposomes (Tax-Se@LPs) for enhanced oral delivery and hypoglycemic effect.Methods: Tax-Se@LPs were fabricated through a thin-film hydration/in situ reduction technique. The resulting nanomedicine was characterized through in vitro release studies, pharmacokinetic and pharmacodynamic evaluations, cellular uptake assays, and formulation stability tests.Results: The optimized Tax-Se@LPs demonstrated an average particle size of 185.3 nm and an entrapment efficiency of 95.25% after optimization. In vitro release studies revealed that Tax-Se@LPs exhibited a slower and more sustained release profile compared to conventional liposomes, favoring gastrointestinal drug absorption. Pharmacokinetic evaluations in normal rats indicated that Tax-Se@LPs achieved a relative bioavailability of 216.65%, significantly higher than Tax suspensions and unmodified liposomes. Furthermore, in diabetic GK rats, Tax-Se@LPs resulted in a maximal blood glucose reduction of 46.8% and exhibited a more sustained therapeutic duration compared to other formulations. Cellular uptake tests manifested that selenization altered the internalization mechanisms of liposomes while preserving their absorption aptness by intestinal epithelial cells. The physiological and in vitro stability of Tax-Se@LPs was also reinforced by selenization.Conclusion: Overall, Tax-Se@LPs not only improve the oral bioavailability of Tax but also enhance its therapeutic efficacy. These findings underscore the potential of Tax-Se@LPs as a promising therapeutic strategy for DM management.
研究领域:
药剂学
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糖尿病研究
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纳米医学
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产品关联
DOI
PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
·
2020
·
IF 4.679
Zengqiang Li,Yige Yu,Yang Li,Feifei Ma,Yinghui Fang,Chaobo Ni,Keyang Wu,Peipei Pan,Ren-Shan Ge
Di-n-butyl phthalate (DBP) is widely used in consumer products as a plasticizer . Here, we report a natural product taxifolin that can attenuate developmental and reproductive toxicity of DBP. Pregnant rats were daily gavaged with 500 mg/kg DBP alone or together with taxifolin (10 and 20 mg/kg) from gestational day (GD) 12–21. At GD21, sera and testes of male fetus were collected. DBP significantly lowered serum testosterone level at 500 mg/kg and taxifolin can completely reverse its action. DBP caused abnormal aggregation of fetal Leydig cells and taxifolin can reverse it. DBP down-regulated the expression of the genes of cholesterol side-chain cleavage enzyme ( Cyp11a1 ), 17β-hydroxysteroid dehydrogenase 3 ( Hsd17b3 ), and insulin-like 3 ( Insl3 ) and taxifolin can reverse its action. DBP increased malondialdehyde levels and decreased superoxide dismutase and glutathione peroxidase expression and taxifolin can reverse it. DBP increased incidence of multinucleated gonocytes and taxifolin can prevent it. Moreover, DBP lowered sirtuin 1 (SIRT1)/peroxisome proliferator-activated receptor γ coactivator 1-α (PGC-1α) and phosphorylated AMP-activated protein kinase (pAMPK) signalling and taxifolin antagonized DBP. In conclusion, in utero exposure to DBP caused developmental/reproductive toxicity of male offspring via increasing reactive oxygen species and taxifolin is an effective food component that completely reverses DBP-mediated action.
研究领域:
毒理学
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生殖健康
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环境科学
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产品关联
DOI
PubMed
高影响因子
ANALYTICA CHIMICA ACTA
·
2019
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IF 5.256
Xia Zhang,Danqing Li,Chaoyang Dong,Jianguo Shi,Yangang Sun,Baoxian Ye,Yuandong Xu
MoS 2 and nitrogen doped active carbon composite (MoS 2 /ANC) is fabricated to detect taxifolin and exhibits superior redox current response and decreased redox potential difference. Further investigation reveals that the kinetic process of the redox reaction of taxifolin on MoS 2 /ANC electrode is controlled by both adsorption and diffusion process. Under the optimum conditions, the redox peak currents linearly relate with the concentration of taxifolin in the range of 1 × 10 −9 –1 × 10 −6 mol L −1 , accompanied by the low detection limit (3 × 10 −10 mol L −1 ). Meanwhile, outstanding selectivity , stability and repeatability are also obtained at MoS 2 /ANC electrode. At last, the proposed method is applied to quantitatively detect taxifolin in fructus polygoni orientalis and satisfactory results have been achieved.
研究领域:
中药分析
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材料科学
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分析化学
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产品关联
DOI
PubMed
高影响因子
TALANTA
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2016
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IF 4.035
Qinqin Wang,Lu Wang,Gaiping Li,Baoxian Ye
Palladium nanoparticles with diameter of around 5–10 nm supported on poly (diallyldimethylammonium chloride) (PDDA)-functionalized graphene composites were prepared by a simple chemical method. As-prepared nanocomposites were characterized by transmission electron microscopy (TEM), x-ray diffraction (XRD), ultraviolet-visible spectrophotometry (UV–vis) and electrochemical techniques, which were clearly demonstrated that palladium nanoparticles were uniformly dispersed on the graphene sheets. Based on the PDDA-Gr-Pd nanocomposites, a new voltammetric sensor was established and exhibited excellent electrocatalytic activity and fast electron transfer rate toward taxifolin . Under the optimal conditions, a lower detection limit of 1×10 −9 mol L −1 (S/N=3) and a wide linear detection range from 4×10 −8 to 1×10 −6 mol L −1 were achieved by square wave voltammetry (SWV). The proposed method was successfully applied for determination of taxifolin in fructus polygoni orientalis with well results.
研究领域:
分析化学
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材料科学
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药物分析
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2021
·Vol. 102
·期 4
·1598-1608
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IF 3.639
Hang Su,Wen-Jun Wang,Guo-Dong Zheng,Zhong-Ping Yin,Jing-En Li,Ling-Li Chen,Qing-Feng Zhang
BACKGROUND Taxifolin is a natural dihydroflavonol found in many plants and health products. In the present study, its anti-obesity and gut microbiota modulating effects were studied. C57BL/6J mice were fed with a high-fat diet (HFD) supplemented with taxifolin (0, 0.5 and 1 mg mL −1 , respectively) in drinking water for 15 weeks. RESULTS Taxifolin supplementation showed no influence on food and water intake. However, it decreased body weight gain, inhibited fat accumulation, and decreased total cholesterol and triacylglycerol level in mice liver. Taxifolin enhanced superoxide dismutase (SOD) activity in mice liver, which in turn protected the liver from lipid peroxidation damage. It also improved insulin resistance in obese mice. Metagenomic analysis of bacterial 16S rRNA demonstrated that HFD decreased gut microbiota diversity and caused dysbiosis. However, taxifolin improved the gut microbiota diversity and decreased the Firmicutes / Bacteroidetes ratio. In particular, it inhibited Proteobacteria from blooming, this being a signature of dysbiosis in gut microbiota. CONCLUSION Taxifolin ameliorated the symptoms of obesity, hepatic steatosis, lipid peroxidation, insulin resistance, and gut microbiota dysbiosis in HFD fed C57BL/6J mice. © 2021 Society of Chemical Industry.
研究领域:
营养学
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微生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
LIFE SCIENCES
·
2019
·
IF 3.448
Cheng Hu,Jiawen Ye,Licong Zhao,Xiulong Li,Yu Wang,Xinhua Liu,Lingyun Pan,Lisha You,Long Chen,Yiqun Jia,Jiaqi Zhang
Taxifolin (TAX) reportedly exerts protective and therapeutic effects in liver. Herein, the effects of TAX against acetaminophen (APAP)-induced hepatotoxicity were investigated. Pharmacodynamics, pharmacology and metabolomics analyses of TAX were assessed on C57 mice and L-02 cells. TAX was administered for 7 days, and APAP was given on the last day to establish an acute liver injury model. ALT and AST levels were determined, and liver ROS, MDA, GST, GSH and GPX1 were analysed. The expression and protein abundance of GPX1, GPS-Pi, GCLC and GCLM were assessed by PCR and western blotting, and metabolic changes in cells and serum were investigated by UPLC-Q-Orbitrap-MS. Serum ALT and AST, and liver ROS, MDA, GST, GSH and GPX1 levels confirmed the protective effects of TAX. Besides, we found Only treating with TAX decreased the expression of CYP2E1 in mice liver tissue. TAX reversed the APAP-induced decrease in cell viability in L-02 cells, and reduced cellular ROS levels. Furthermore, TAX reversed the APAP-induced decrease in antioxidant enzymes at both mRNA and protein levels. Metabolomics analysis identified metabolites mainly related to glutathione metabolism (36 in vivo and 23 in vitro ). The concentration of glutathione, oxidized glutathione, carnitine, succinic acid, pyroglutamic acid, citrulline, taurine, palmitoleic acid, phytoshingosine-1-P and sphingosine-1-P were close to normal levels after treating with TAX. These results indicate that TAX prevents APAP-induced liver injury by inhibiting APAP metabolic activation mediated by CYP450 enzymes, modulating glutathione metabolism, and expression of related antioxidative signals. These properties could be harnessed to prevent or treat hepatotoxicity.
研究领域:
药理学
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肝病学
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代谢组学
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毒理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NUTRITIONAL BIOCHEMISTRY
·
2024
·
IF 4.8
Yiming Ni,Xinghua Chen,Yiqun Jia,Long Chen,Mingmei Zhou
Currently, the hepatoprotective activity of taxifolin, a flavonoid isolated from Pseudotsuga taxifolia , has been reported in many animal models. However, whether the protective effect of taxifolin on the liver is related to its effect on lipidomics is unclear. Based on the significant therapeutic effect of taxifolin on CCl 4 induced subacute hepatic injury, we observed the intervention of taxifolin by lipidomics. The results demonstrate that taxifolin can effectively reverse the damage caused by CCl 4 , which including hepatocyte vacuolization and necrosis. Lipomic profiling based on liquid chromatography-mass spectrometry showed that taxifolin was able to restore lipidomic changes caused by CCl 4 , including the levels of lysophosphatidylserine (LPS), phosphatidylcholine (PC), coenzyme (Co), phosphatidylglyceride (PG), phosphatidylserine (PS), dimethylphosphatidylethanolamine (dMePE), ceramide (Cer), sphingosine (So), triglycerides (TG), and monogalactosyl diacylglycerol (MGDG) in the rat liver, and phosphatidylcarbinol (PMe) and phosphatidylethanolamine (PE), plant sphingosine (phSM), glucose ceramide (CerG1), TG, and diglycerides (DG) in serum. Spearman's correlation analysis showed that CerG1, phSM, PE, and PMe in serum, and Cer, dMePE, PG, PS, So, TG, and MGDG in liver were positively correlated with serum levels of aspartate transaminase, alanine transaminase, and liver index; while TG, DG in serum, and Co, LPS, PC in liver were negatively correlated with the parameters. In total, 43 and 34 lipid molecules were altered by taxifolin treatment in the liver and serum, respectively, mainly including glycerophosphoglycerols, glycerophosphocholines, glycerophosphoethanolamines, and linoleic acids and derivatives. Our findings help to provide novel insights into the mechanism of the hepatoprotective effect of taxifolin from a lipidomics approach.
研究领域:
药理学
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代谢组学
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肝脏病学
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产品关联
DOI
PubMed
高影响因子
Catalysts
·
2022
·Vol. 12
·期 9
·1037
·
IF 4.501
Jianfeng Mei,Xiang Chen,Pingya Wang,Yichun Wu,Yu Yi,Guoqing Ying
Taxifolin is known to have multiple biological functions. It has been widely used as a multifunctional food additive, and consequently, the global demand for taxifolin is increasing. The main method for taxifolin production is an extraction from larch wood, but the global resources of larch are limited. Astilbin, taxifolin-3-o-rhamnoside, is abundant in many plants and much more readily available, meaning taxifolin can be obtained by deglycosylation of astilbin. In this study, a fungal strain,Aspergillus fumigatusSQH4, was isolated from an enrichment culture ofSmilax glabrarhizome to achieve the deglycosylation reaction. A culture of SQH4, adjusted to pH 6.5, with 5 g/L astilbin achieved a yield of taxifolin of 91.3% after biotransformation for 14 h at 35 °C. These findings offer an alternative method for the production of taxifolin.Keywords:taxifolin;dihydroquercetin;astilbin;biotransformation;Aspergillus fumigatus
研究领域:
微生物学
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生物技术
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药理学
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DOI
高影响因子
CELLULAR & MOLECULAR BIOLOGY LETTERS
·
2017
·Vol. 22
·期 1
·1-11
·
IF 1.26
Li Xican,Xie Hong,Jiang Qian,Wei Gang,Lin Lishan,Li Changying,Ou Xingmei,Yang Lichan,Xie Yulu,Fu Zhen,Liu Yamei,Chen Dongfeng
The natural dihydroflavonol (+) taxifolin was investigated for its protective effect on Fenton reagent-treated bone marrow-derived mesenchymal stem cells (bmMSCs). Various antioxidant assays were used to determine the possible mechanism. These included •OH-scavenging, 2-phenyl-4, 4, 5, 5-tetramethylimidazoline-1-oxyl-3-oxide radical-scavenging (PTIO•-scavenging), 1, 1-diphenyl-2-picryl-hydrazl radical-scavenging (DPPH•-scavenging), 2, 2′-azino-bis (3-ethylbenzo-thiazoline-6-sulfonic acid) radical-scavenging (ABTS+•-scavenging), Fe3+-reducing, and Cu2+-reducing assays. The Fe2+-binding reaction was also investigated using UV-Vis spectra. The results revealed that cell viability was fully restored, even increasing to 142.9 ± 9.3% after treatment with (+) taxifolin. In the antioxidant assays, (+) taxifolin was observed to efficiently scavenge •OH, DPPH• and ABTS+• radicals, and to increase the relative Cu2+- and Fe3+-reducing levels. In the PTIO•-scavenging assay, its IC50 values varied with pH. In the Fe2+-binding reaction, (+) taxifolin was found to yield a green solution with two UV-Vis absorbance peaks: λmax = 433 nm (ε =5.2 × 102 L mol−1 cm −1) and λmax = 721 nm (ε = 5.1 × 102 L mol−1 cm −1). These results indicate that (+) taxifolin can act as an effective •OH-scavenger, protecting bmMSCs from •OH-induced damage. Its •OH-scavenging action consists of direct and indirect antioxidant effects. Direct antioxidation occurs via multiple pathways, including ET, PCET or HAT. Indirect antioxidation involves binding to Fe2+.
研究领域:
细胞生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
MATERIALS & DESIGN
·
2025
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IF 7.9
Hewei Wei,Feifei Feng,Qiteng Ding,Junran Yang,Taojing Yu,Xiaoyu Wu,Xiaohang Sun,Chuanbo Ding,Yupeng Song
s Bone defects have long posed a challenge in trauma orthopedics. Despite advancements in bone tissue engineering, there remains a bottleneck in developing bone implants that are less toxic, more effective, and reduce the need for secondary surgeries. To address this, we devised a light-responsive bone-targeted smart nano-delivery system. This system integrates polydopamine (PDA)-coated TAX-loaded ZIF-8 nanoparticles into a hydrogel with strong bioadhesion and biocompatibility (TAX@ZIF-8@PDA/ODEX-HD, TZPG). When exposed to near-infrared light, TZPG + NIR demonstrated a high photothermal conversion efficiency of 51.79 %. It exhibited a 99 % inhibition rate against Staphylococcus aureus, while also enhancing the proliferation and differentiation of osteoblasts (MC3T3-E1), thereby accelerating bone defect repair in a rat cranial bone defect model. Additionally, TZPG + NIR accelerates bone tissue repair by upregulating osteogenic-related proteins (ALP, RUNX2, OSX, OCN) while enhancing the expression of COL-I and PDGFA proteins to promote angiogenesis. Overall, TZPG + NIR created an antimicrobial microenvironment in vitro , enabled intelligent controlled release, and programmed degradation during the bone repair cycle, achieving a one-time therapeutic effect. This study highlights the promising applications of near-infrared light-responsive material TZPG in regenerative medicine, offering a novel approach to developing multifunctional bone scaffolds for repairing bone defects as a viable alternative to autografts.
研究领域:
生物材料学
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组织工程
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纳米医学
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骨科学
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再生医学
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药物递送系统
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生物相容性
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）