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( )-Taxifolin
Catalysts · 2022 ·Vol. 12 ·期 9 ·1037 · IF 4.501

Production of Taxifolin from Astilbin by Fungal Biotransformation

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

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MATERIALS & DESIGN · 2025 · IF 7.9

Antibacterial NIR responsive targeted nanocomposite hydrogels loaded with Taxifolin for bone repair

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.

CAS / MDL: 9004-61-9
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

In vitro and in vivo inhibitory activity of taxifolin on three digestive enzymes

Hang Su,Yi-Ting Ruan,Ying Li,Ji-Guang Chen,Zhong-Ping Yin,Qing-Feng Zhang

The inhibitory activity of taxifolin on three digestive enzymes were investigated in both vitro and vivo. Taxifolin exhibited inhibitory effect on α-glucosidase, α-amylase and pancreatic lipase with IC50 values of 0.038, 0.647 and 0.993 mg/mL, respectively. Inhibitory kinetics indicated that taxifolin was more like a competitive inhibitor of α-glucosidase and α-amylase, while it was a non-competitive inhibitor of pancreatic lipase. The binding of taxifolin caused the quenching of intrinsic fluorescence intensity of enzymes, and the binding constant (lgK a ) and the number of binding site (n) were further calculated through fluorescence titration. The values of lgK a were in the range of 4.93‐6.65, and the values of n were all close to 1. Molecular docking indicated that taxifolin could interact with α-glucosidase and α-amylase through many kinds of secondary interaction, such as hydrogen bond, π-π stack, etc. In vivo study revealed that pre-administration with taxifolin can significantly improve the postprandial hyperglycemia in rat. Furthermore, its can also decrease triglyceride absorption through the inhibition of pancreatic lipase.

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JOURNAL OF ELECTROANALYTICAL CHEMISTRY · 2019 · IF 3.218

A new electrochemical sensor for Taxifolin based on RGO-Co3S4@MoS2 modified electrode

Di Huang,Lingxi Yang,Xing lin Li,Lina Zou,Baoxian Ye

A novel electrochemical sensor was designed and constructed for high-sensitive detection of Taxifolin based on Co 3 S 4 @MoS 2 loaded on reduced graphene oxide (RGO-Co 3 S 4 @MoS 2 ) as modified materials. It’s the first time for Co 3 S 4 @MoS 2 was exploited to constructed electrochemical sensor. Owing to the Co 3 S 4 @MoS 2 providing a huge surface area to enrich more Taxifolin and the excellent electric conductivity of RGO, Taxifolin was detected sensitively with a linear range from 5.0 × 10 −9 to 1.0 × 10 −6  mol L − 1 and limit of detection down to 1.67 × 10 −9  mol L − 1 (S/N = 3). In addition, the sensor also demonstrated strong anti-interference properties in the presence of some metal ions and organic compounds. The proposed method was successfully applied for determination of Taxifolin in traditional Chinese medicine in fructus polygoni orientalis with satisfactory results.

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Natural Product Communications · 2017 · IF 0.773

Inhibitory Mechanism of Taxifolin against α-Glucosidase Based on Spectrofluorimetry and Molecular Docking

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.

CAS / MDL: 480-18-2
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ANALYTICA CHIMICA ACTA · 2019 · IF 5.256

Molybdenum sulfide-based electrochemical platform for high sensitive detection of taxifolin in Chinese medicine

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.

CAS / MDL: 480-18-2
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Journal of Food Measurement and Characterization · 2023 · IF 3.4

Interaction with taxifolin reduces the digestibility of corn starch in vitro and in vivo

Li Mang-Mang,Peng Rui-Yan,Wang Wen-Jun,Xu Hai-Xia,Yin Zhong-Ping,Chen Ji-Guang,Zhang Qing-Feng

Reducing the hydrolysis of starch in the gastrointestinal tract can improve postprandial hyperglycemia, which is beneficial for diabetes. The blends of corn starch with taxifolin (CS-Tax) were prepared with different taxifolin proportion. Iodine binding test showed that taxifolin can occupy the helix of starch, and the affinity is stronger than that of iodine. FTIR and XRD characterization revealed secondary interaction between taxifolin and starch in the blends, and the crystallization of taxifolin was suppressed. Taxifolin decreased the gelatinization temperature and enthalpy for starch. Scanning electron microscopy showed that the morphology of the blends was the same as starch granules. In vitro digestion experiment showed that taxifolin could slow down starch hydrolysis. Compared with native starch, the content of rapidly digestible starch in CS-10%Tax decreased from 56.35 to 49.20%, while the content of resistant starch increased from 17.62 to 29.61%. The comparison in vivo showed that after intragastric administration of CS-10%Tax in rats, the increase of blood glucose slowed down and the maximum decreased from 7.1 to 6.2 mM. Hence, taxifolin is prospective in preparing low glycemic index starchy foods and deserves further study.

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Food Chemistry-X · 2026 · IF 9.2

Non-covalent interactions between whey protein isolate and taxifolin and their potential application in yogurt

Chenligen Bao,Mi Yan,Fangyu Li,Liqing Jiang,Tiehua Zhang

This study investigated the interaction mechanism of non-covalent complexes between whey protein isolate (WPI) and taxifolin (Tax) and subsequently applied the complexes into yogurt to evaluate their effects on the quality and functionality of yogurt during storage. The results demonstrated that the WPI and Tax can form granular aggregates with average particle sizes between 184.57 and 287.03 nm. As Tax concentration increases, WPI exhibits enhanced UV–visible absorption alongside intensified static fluorescence quenching, primarily driven by conventional hydrogen bonding and π-alkyl interactions between the two compounds. And the incorporation of the WPI + Tax complex into yogurt significantly improves its water-holding capacity and reduces syneresis, with the WPI + 40 μM group showing the optimal effect. The complexes also enhanced yogurt's antioxidant activity and inhibitory effects against α-glucosidase and α-amylase, which reached the highest levels on day 14 of storage, while maintaining good sensory acceptability.

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Viruses-Basel · 2022 ·Vol. 14 ·期 12 ·2731 · IF 5.818

Taxifolin Inhibits WSSV Infection and Transmission by Increasing the Innate Immune Response in Litopenaeus vannamei

Xu Zhang,Li-Peng Shan,Qi Zhao,Lei Liu,Xu OuYang,Yang Hu,Chen-Jie Fei,Jiong Chen

An outbreak of white spot syndrome virus (WSSV) can hit shrimp culture with a devastating blow, and there are no suitable measures to prevent infection with the virus. In this study, the activity of active molecules from Chinese herbs against WSSV was evaluated and screened. Taxifolin had the highest rate (84%) of inhibition of the WSSV infection. The viral infectivity and genome copy number were reduced by 41% when WSSV virion was pretreated with taxifolin prior to shrimp infection. A continuous exchange of taxifolin significantly reduced the mortality of shrimp infected with WSSV. Due to the WSSV virion infectivity being affected by taxifolin, the horizontal transmission of the virus was blocked with an inhibition rate of up to 30%, which would further reduce the cost of a viral outbreak. Additionally, the viral genome copy number was also reduced by up to 63% in shrimp preincubated in taxifolin for 8 h. There may be a connection to the enhancement of innate immunity in shrimp that resulted in a 15% reduction in mortality for taxifolin-fed shrimp after the WSSV challenge. After dietary supplementation with taxifolin, the resistance of larvae to WSSV was improved, indicating that taxifolin may be a potential immunostimulant for shrimp to prevent WSD. Therefore, the results indicate that taxifolin has application potential for blocking a WSSV outbreak and reducing the loss of shrimp culture.Keywords:taxifolin;WSSV;antiviral;Chinese herbs;Litopenaeus vannamei

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Taxifolin-loaded cellulose/l-arginine-chitosan hydrogel promoting bone defect repair through osteogenesis and angiogenesis

Jiali Yang,Yuanyuan Han,Lifeng Zhang,Qiteng Ding,Shuwen Sun,Shuai Zhang,Yue Wang,Ning Wang,Hewei Wei,Taojing Yu,Wencong Liu,Chuanbo Ding

Bone defects have always been a difficult problem in clinical practice. Taxifolin (TAX) is beneficial to bone regeneration. In order to obtain more attractive biomaterials, we extracted cellulose (LC) from larch sawdust and prepared a TAX-loaded hydrogel (DCT) together with L-arginine chitosan (CA). The hydrogel had a uniform porous structure and good mechanical properties. After drug loading, the adhesion, antibacterial, and antioxidant properties of the hydrogel were improved. In addition, DCT has good biocompatibility. In vitro cell experiment results showed that DCT can promote cell proliferation and migration, and DCT has a certain ability to promote the osteogenic activity and enhance the expression of osteoblastic factors (OCN and Osx) and vascular endothelial growth factor (VEGF) in MC3T3-E1 cells. In addition, in vivo studies showed that the DCT treatment could promote bone regeneration by increasing the levels of osteogenic markers (OPN, OCN, and Osx) and VEGF. Transcriptome analysis showed that DCT intervention affected the hematopoiesis function in bone tissue. Meanwhile, KEGG analysis showed that DCT promoted bone regeneration mainly by activating the PI3K/AKT signaling pathway, which was verified by a western blot. Therefore, DCT is a good material for bone repair.

CAS / MDL: 5470-11-1
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FOOD AND CHEMICAL TOXICOLOGY · 2020 · IF 4.679

Taxifolin attenuates the developmental testicular toxicity induced by di-n-butyl phthalate in fetal male rats

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.

CAS / MDL: 175606-05-0
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International Journal of Nanomedicine · 2025 · IF 6.5

Nanometerizing Taxifolin Into Selenized Liposomes to Ameliorate Its Hypoglycemic Effect by Optimizing Drug Release and Bioavailability

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.

CAS / MDL: 70-18-8 10102-18-8
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