Biomolecules
·
2026
·Vol. 16
·期 3
·387
·
IF 5.6
Fangfang Chen,Yihan Cai,Jinxiong Wu,Nengzhen Fang,Fei Li,Hongtan Wu,Yu-Pei Chen
Taxifolin, a natural flavonoid, consistently exerts cytoprotective effects against various oxidative stresses. In this study, we systematically evaluated its photoprotective efficacy and underlying mechanisms against ultraviolet B (UVB)-induced injury in human immortalized keratinocytes (HaCaT). Cell viability and apoptosis were assessed by MTT, fluorescence staining, and flow cytometry, while integrative transcriptomic and proteomic analyses were employed to identify core pathways and key mediators. Taxifolin exhibited antioxidant capacity comparable to that of ascorbic acid under identical in vitro radical-scavenging assays. Moreover, it displayed a strong absorption peak at 289 nm that overlaps the UVB spectrum (280–320 nm), enabling it to act as a chemical sunscreen. In UVB-challenged HaCaT cells, taxifolin markedly reduced intracellular reactive oxygen species (ROS) and attenuated JNK/p38 MAPK activation, as evidenced by Western blot, thereby breaking the ROS-MAPK vicious cycle. Multi-omics revealed that taxifolin was associated with attenuation of UVB-imposed G1/S arrest concomitant with restored Cyclin expression, while up-regulating MYC, FOXQ1, HMOX1 and AP-1 components c-Jun/c-Fos and thereby switching on a pro-survival transcriptional program. Consequently, apoptosis was suppressed and survival was significantly improved. Collectively, taxifolin integrated chemical filtration, ROS scavenging and signaling modulation to support a multi-target photoprotective network, which provides mechanistic insight into taxifolin-mediated cytoprotection and identifies candidate molecular nodes for further validation.
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Food Science & Nutrition
·
2026
·Vol. 14
·期 1
·e71389
·
IF 3.8
Zunqiong Ke,Lishu Lin,Yunhong Long,Wenhui Zhang,Jianmin Guo,Leyong Yuan
Dihydroquercetin (DHQ), a crucial dihydroflavone found in nature, demonstrates notable antioxidant, anti‐inflammatory, and antifibrotic effects. Nevertheless, the impact on the gut microbiome and metabolites associated with silicosis remains unclear. Hence, the objective of this research was to examine how DHQ impacts silicosis and the associated mechanisms through analyzing gut microbiota with 16S rRNA sequencing and conducting serum metabolomic analysis. The findings of our study showed that administering DHQ significantly attenuated the level of inflammation and fibrosis in the lung tissues of C57BL/6 mice exposed to silica. Furthermore, DHQ clearly raised the amount of Muribaculaceae, while diminishing the amount of Lactobacillus . DHQ treatment significantly decreased the sphingomyelin, arachidonic acid and its metabolites. Significantly, the correlation analysis showed that the influence of DHQ on the arachidonic acid metabolism, steroid hormone biosynthesis, and sphingolipid signaling pathways were linked to changes in the levels of Muribaculaceae and Lactobacillus in the gut microflora. In summary, our research demonstrated that DHQ can attenuated inflammation and lung fibrosis caused by silica exposure in the C57BL/6 mice, potentially by modulating the gut microbiota and serum metabolites. (1) DHQ can attenuate silica‐induced inflammation and pulmonary fibrosis in the C57BL/6 mice. (2) The beneficial effects of DHQ were primarily attributed to the alteration of gut microbiota (particularly Muribaculaceae and Lactobacillus) mediated by serum metabolites.
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Food Bioscience
·
2023
·
IF 5.2
Huiqun Fan,Mingshun Chen,Taotao Dai,Lizhen Deng,Chengmei Liu,Wei Zhou,Jun Chen
This study determined the phytochemical composition and bioactivity (antioxidant and hypoglycemic) in five fractions (petroleum ether, chloroform , ethyl acetate, n -butanol, and water fractions) obtained from ethanol extract of Amomum tsaoko Crevost et Lemaire ( A. tsaoko ). Qualitative and quantitative analyses of phenolic compounds were carried out with UHPLC-ESI-QTOF-MS/MS. 50 bioactive compounds were identified from five different fractions, including 11 phenolic acids and derivatives, 18 flavonoids and derivatives, 14 proanthocyanidins , 2 organic acids, and 5 other compounds. It was found that ethyl acetate fraction (EF) was enriched with the most types and contents of substances. Flavonoids and derivatives (including epicatechin and catechin) were the primary phenolic compounds in EF. In addition, EF demonstrated excellent antioxidant activity (DPPH and ABTS with IC 50 = 0.17 and 0.07 mg/mL, FRAP of 546.10 mg VCE/g DW) and anti-α-glucosidase activity (IC 50 = 20.14 μg/mL). EF could ameliorate fasting blood glucose and glucose tolerance of diabetic mice. In conclusion, EF could be developed as a potential candidate for preventing or treating oxidative stress diseases and diabetes.
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Frontiers in Plant Science
·
2022
·
IF 6.627
Shi Xia,Fang Jiaxing,Du Huicong,Zhang Sufang,Liu Fu,Zhang Zhen,Kong Xiangbo
When Ips bark beetles invade and colonize the host plants, their associated pathogenic fungal partners are carried into the phloem of the host trees. Host trees are lethally attacked by the beetle-fungus complex and the collective damage severely limits forestry production worldwide. It is of great importance to verify whether bark beetles and their associated fungi show concordant performance in terms of biology, physiology, and biochemistry on host trees. In this study, the two Ips bark beetles Ips typographus and Ips subelongatus (Coleoptera: Curculionidae, Scolytinae), their respective associated pathogenic fungi Endoconidiophora polonica and Endoconidiophora fujiensis, and their respective host plants Picea jezoensis and Larix olgensis were selected as test material. Cross-inoculation experiments were conducted indoors and outdoors to investigate the differences in reproduction and development of two beetles and infectivity of two fungi on two plants, as well as the differences in physiological responses of two plants to two fungal infections. The results showed that I. typographus and E. polonica had excellent host performance on P. jezoensis; however, neither successfully colonized and infected L. olgensis. In contrast, I. subelongatus and E. fujiensis showed strong host suitability on L. olgensis and some degree of suitability on P. jezoensis, although the host suitability of P. jezoensis for E. polonica was significantly higher than that for E. fujiensis. In addition, we found that the absolute amount of ergosterol accumulated on the lesion was positively correlated with lesion area. The ergosterol amount and lesion area were both strongly correlated with the release of host monoterpenes, but had no obvious correlation with the concentration of fungi-induced phenols on the lesion area and the side-chain oxidation of lignin in the xylem of the infected sites. Based on these results, we confirmed that “I. typographus-E. polonica” and “I. subelongatus-E. fujiensis” complexes both showed the most suitable consistent performances on their own traditional hosts, establishing a stable species-specific association relationship in these two beetle-fungus complexes, with the “I. subelongatus-E. fujiensis” complex showing broader host suitability. From the perspective of physiological responses of plants to fungal infections, monoterpenes are an important indicator of host suitability.
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FOOD CHEMISTRY
·
2023
·
IF 8.8
Yuan Meng,Zihao Wei,Changhu Xue
Chickpea protein isolate (CPI) is a promising novel plant protein, and protein–flavonoid system has also been applied in various food products. However, the interaction mechanism between CPI and flavonoids remains to be elucidated. In this paper, the affinity behavior between flavonoids and CPI was explained by constructing the three-dimensional quantitative structure–activity relationship (R 2 = 0.988, Q 2 = 0.777). Subsequently, four representative flavonoids were selected for further study. Multi-spectroscopy analysis showed that the sequence of affinity for CPI was puerarin > apigenin > naringenin > epigallocatechin gallate. Meanwhile, flavonoids altered the secondary structure and spatial conformation of CPI, leading to the static quenching of CPI. Additionally, thermodynamic analysis indicated that hydrogen bonding and van der Waals forces were the main driving forces for complex binding. Molecular docking and molecular dynamics simulations further explored the binding sites and conformations of complexes. This study provides theoretical guidance for in-depth research on the interaction patterns between biomacromolecules and small molecules in food matrices.
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JOURNAL OF CHROMATOGRAPHIC SCIENCE
·
2023
·
IF 1.3
Xia Chenjie,Zhu Hongliu,Hu Changhui,Liu Jie,Hua Haibing,Yang Jianqiu,Chen Zhipeng,Gao Yihong
Pinus massoniana needles, a traditional herb, were applied to prevent hair loss in China. Studies available mainly focused on pine needle flavonoids with various biological activities. However, there has been no pharmacokinetics study of the flavonoids from Pinus needles extract. A selective and sensitive ultra-high performance liquid chromatography–tandem mass spectrometry (UHPLC-MS/MS) method was developed to simultaneously quantify taxifolin, quercetin and catechin in rat plasma. To separate the three constituents, an Agilent Extend-C18 column (2.1 mm × 100 mm, 1.8 μm) was used with a mobile phrase of (A) 0.1% formic acid and (B) acetonitrile. The analytes were measured by multiple reaction monitoring in the negative ionization mode. There was good linearity in the established UHPLC-MS/MS method, with a coefficient of determination (r2) of >0.99. The accuracy, intra-day and inter-day precision and recovery were all satisfactory and these 3 compounds were stable under the tested conditions. The validated method in this study was successfully applied to pharmacokinetic study in healthy rats after oral and transdermal administration of Pinus needles extract. The results could provide further research foundation for pine needle extract as external preparations.
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Food & Function
·
2022
·Vol. 13
·期 9
·5061-5074
·
IF 6.317
Jie Zhao,Lin Huang,Renjie Li,Zhuangwei Zhang,Jin Chen,Hongjin Tang
Gliadin, as a main component of wheat storage protein, is used as a drug encapsulation and delivery system owing to its specific characteristics. Flavonoids are regarded as active natural products with a variety of pharmacological effects. In this study, an integrated method including UV-vis, fluorescence, and FT-IR spectroscopy and molecular modelling was applied to explore the structure–affinity relationship and the interaction nature between a library of flavonoids and gliadin. The characteristic UV-vis spectral changes of gliadin mediated by flavonoids with absorption bands at 218 and 278 nm demonstrated the existence of an interaction depending on generating the ground-state complexes. Fluorescence quenching results showed that the intrinsic fluorescence of gliadin could be effectively quenched by flavonoids coupled with the formation of flavonoid–gliadin complexes through the static quenching mechanism. The structure–affinity relationship revealed the critical structural elements associated with the binding affinity on gliadin and underlined the favorable substituents at the specific positions of flavonoid skeletons leading to a stronger binding potency. From the analysis of synchronous fluorescence spectra, flavonoids could cause the conformation change of gliadin and impact the microenvironment around TYR and TRP residues. Moreover, the ANS fluorescent probe assay suggested that these flavonoids also influenced the surface hydrophobicity of glaidin based on the further exposure or blocking of hydrophobic domains. Molecular modelling was subsequently performed and illustrated the proposed binding conformation of flavonoids on gliadin. Combined with the FT-IR spectra, these results further confirmed the important role of hydrophobic interactions and hydrogen bonds in their binding process.
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Frontiers in Pharmacology
·
2022
·
IF 5.988
Leyong Yuan,Yan Sun,Ning Zhou,Weipeng Wu,Weidong Zheng,Yukun Wang
Silicosis is a fatal occupational lung disease which currently has no effective treatment. Dihydroquercetin (DHQ) is a flavonoid compound known for its anti-inflammatory, anti-oxidant and anti-cancer bioactivity. However, whether DHQ protects against silica-induced lung fibrosis remains unknown. Therefore, we aimed to investigate the effect of DHQ on silica-induced lung fibrosis and the underlying molecular mechanism in vivo and in vitro . Our results demonstrated that DHQ treatment markedly attenuated SiO 2 -induced inflammation and fibrosis degree of lung tissues in the C57BL/6 mice. Additionally, experiments in vitro also confirmed that conditioned medium from DHQ-treated human bronchial epithelial (HBE) cells significantly decreased expression of fibrosis markers of human fetal lung fibroblast cells (MRC-5), such as α-SMA, collagen1 and fibronectin. Interestingly, HBE cells treated by DHQ showed few morphological features of ferroptosis compared with SiO 2 -treated cells. Furthermore, DHQ treatment remarkably inhibited ferroptosis in activated HBE cells by decreasing the accumulation of iron and lipid peroxidation products, and increasing levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4), whereas stimulation of ferroptosis by specific inducer erastin deeply impaired anti-fibrosis effect of DHQ in vitro . More importantly, our results showed that DHQ also evidently suppressed ferritinophagy by down-regulation of microtubule-associated protein 1A/1B-light chain 3 (LC3), and up-regulation of ferritin heavy chain 1 (FTH1), nuclear receptor co-activator 4 (NCOA4) in activated HBE cells. Nevertheless, activation of ferritinophagy by specific inducer rapamycin (Rapa) evidently blocked DHQ-inhibited HBE cells ferritinophagy and anti-fibrosis effect of DHQ. Overall, our research revealed that inhibition of ferritinophagy-mediated HBE cells ferroptosis was responsible for DHQ to ameliorate SiO 2 -induced lung fibrosis, which provided a preliminary theoretical basis for the clinical application of DHQ in the treatment of silicosis.
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Food Chemistry-X
·
2023
·
IF 6.1
Chengyun He,Lu Bai,Daqun Liu,Benguo Liu
The binding capacity of 10 flavonoids with okra seed protein (OSP) was studied by fluorescence spectroscopy. The structure of flavonoids had an obvious impact on binding performance. The binding ability of flavanone was lower than that of flavone, isoflavone and dihydrochalcone. The binding capacity of flavonoid glycoside was superior to that of the corresponding flavonoid aglycone. The binding ability was positively correlated with the number of phenolic hydroxyl groups on the B ring. The steric field and electrostatic field model constructed by 3D-QSAR method could well explain the above interaction behavior. Thermodynamic analysis suggested that the quenching mechanism of OSP caused by flavonoids was static quenching, and the binding-site number was 1. In addition, hydrogen bonding and van der Waals force dominated this interaction. The 3D and synchronous fluorescence spectra showed that there was no significant change in the polarity of the environment around tryptophan and tyrosine residues during binding.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2020
·
IF 2.734
Hao Liu,Chenyun Gan,Houyin Shi,Kunyan Qu,Liuyang Jing,Muhe Lu,Benyu Su,Huayang Yu,Hang Yuan,Jingjing Chen,Ruirui Zhang,Weiling Zeng
Dihydromyricetin (DHM) is a natural flavonol compound that has shown significant pharmacological activities such as anti-atherosclerosis, anti-diabetes, anti-oxidation, and anti-inflammation, but its clinical application has been hindered by its poor stability and rapid metabolism that reduced its bioavailability in vivo . Since DHM is more stable under acidic conditions, selective and sustained absorption of DHM in the stomach via gastric floating drug carriers provide an attractive way to settle the problems. Previously, we reported a gastric floating tablet for DHM that demonstrated improved stability and bioavailability of the drug. However, the application of this drug carrier was still constrained by low drug content percentage, and short floating and drug releasing durations. Besides, the influences of dosage forms on the drug efficacy of DHM in vivo were not yet clear. In this study, gastric floating pill as a novel sustained-release dosage form for DHM (DHM-GFP) was developed using combined techniques of extrusion molding and freeze drying . The physicochemical properties of DHM-GFP could well meet the pharmacopoeial requirements for pills. Our data indicated that DHM-GFP had significantly higher drug content percentage, improved floating ability and more sustained drug release than the previously reported DHM tablet, and is promising to become a once-a-day dosing preparation. More importantly, this novel dosage form resulted in notably prolonged residence time, improved bioavailability, and enhanced anti-inflammatory effect of DHM in vivo , indicating its great potential to translate this natural compound into clinical application.
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2020
·
IF 3.232
Hongjin Tang,Lin Huang,Dongsheng Zhao,Chunyong Sun,Ping Song
The molecular structure properties-binding affinity relationship of a series of flavonoids and bovine serum albumin (BSA) was investigated in vitro from comparing the binding constants determined through the fluorescence method . As a result, the binding process was greatly influenced by different structural elements or substituents of flavonoids under analysis. The hydroxylation at the positions C3, C6, C4’, C5’ (for type I) and C5, C3’ (for type II) were in favor of forming hydrogen bonds with the amino acids of BSA, which was of great importance in the binding and interaction between flavonoids and the protein. The decreased affinity could be realized by the methoxylation (C8, C3’ and C4’) and glycosylation (C3 and C7) of flavonoid type I. However, the adverse trend on binding affinity was observed when the methoxylation and glycosylation appeared at the sites C4’ and C7, C4’ of structure type II, respectively. Meanwhile, glycosylation at C7 mainly induced the decline in the affinity of flavonoids (type III), and the hydrogenation of the C2 C3 double bond for type I was beneficial to increase the affinity on BSA. Moreover, part of flavonoids could mediate the conformational alteration of secondary structures of the protein during the interaction process, which was inferred by means of the synchronous fluorescence spectra . The determinations of ANS fluorescence probe suggested that hydrophobic interaction played an important role in the binding of a majority of flavonoids to BSA. Further evidences from the site-specific experiments revealed that the location of flavonoids 19 , 29 and 34 binding on BSA mainly belonged to site I, while compound 3 bound to both sites I and II. Additionally, molecular modelling studies further confirmed the indispensable character of hydrophobic interaction and hydrogen bonds, and illustrated the preferred complex binding behaviors.
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FOOD CHEMISTRY
·
2020
·
IF 6.306
Jie Zhao,Lin Huang,Chunyong Sun,Dongsheng Zhao,Hongjin Tang
In this study, some flavonoids were screened as potent xanthine oxidase (XO) inhibitors in vitro . Flavonoid 9 was demonstrated to exhibit the inhibitory activity through a ping-pong mechanism. Further structure-activity relationship revealed that different structural elements had greatly influenced the inhibition effect on XO and underlined the requirement of hydroxyl groups at C5 and C4′ of flavonoid type I. Moreover, some bioactive flavonoids could efficiently quench the intrinsic fluorescence of XO by either static or static-dynamic mixed mechanism. The synchronous fluorescence, ANS-binding fluorescence, Fourier transform infrared spectra and circular dichroism suggested that active flavonoids could bind to the active center of XO, prevent the entrance of substrate, and induce the rearrangement and conformation change of its secondary structures, ultimately resulting in the significant inhibition effect. Additionally, molecular docking further confirmed these conclusions and highlighted the great importance of hydrophobic interactions and hydrogen bonds for the formation of stable complex conformation.
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