JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
·
IF 5.7
Yanan Zhao,Bin Li,Hongting Deng,Chang Zhang,Yitong Wang,Lei Chen,Hui Teng
Prolonged and excessive intake of alcohol results in the onset of alcoholic liver disease, which is marked by oxidative stress, intestinal barrier dysfunction, and disturbance in the intestinal microbiome. Galangin, a potent flavonoid from Alpinia officinarum Hance, has been recognized for its diverse biological properties; however, its ability for protecting against alcohol-stimulated hepatotoxicity remains unexplored in prior research. In the current study, a Gao-Binge mouse model was established to assess the positive role and mechanisms of galangin upon alcohol-induced liver injury. The administration of galangin relieved liver pathological damage, oxidative stress, and NLRP3-mediated inflammation induced by alcohol. In addition, galangin significantly reversed abnormal intestinal histopathological manifestations and damaged the intestinal barrier function. Furthermore, microbiota composition revealed that galangin improved intestinal imbalance by improving the gut microbiota dysbiosis and short-chain fatty acid level. Collectively, this study explored the interactions between phytochemical factors and virulence factors and discovered that galangin powerfully improved alcohol-induced liver disease by repressing the inflammatory cascade via the gut microbiota-mediated gut–liver axis. These results suggested that alcohol-targeted natural products could have potential applications in promoting food safety and human health and offer valuable insights into the possible use of these substances in these important areas.
研究领域:
药理学
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肝病学
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微生物学
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免疫学
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营养学
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DOI
高影响因子
RSC Advances
·
2023
·Vol. 13
·期 16
·10987-11001
·
IF 3.9
Yuanguo Xiong,Bing Wu,Xianxi Guo,Dong Shi,Hao Xia,Hanlin Xu,Xiaoxiong Liu
Hepatic fibrosis (HF) is a chronic hepatic pathological process induced by various liver injuries, with few available therapies. Previous research studies revealed that HF is characterized by the accumulation of excess extracellular matrix in the liver, mainly overexpressed by activated hepatic stellate cells (HSC). Therefore, HSC have been targeted in clinical trials for the management of HF. The aim of the present study was to develop an anti-HF drug delivery system with acrylic resin (Eudragit® RS100, Eud RS100) nanoparticles (NPs) through modification by retinoic acid (RA), modified for binding the retinol-binding protein reporter (RBPR) in HSC. Galangin (GA), is a multiple effects flavonoid which has demonstrated an anti-HF effect in our previous studies. In this study, GA was utilized for the treatment of HF. The results revealed that the NPs were well formed (diameter: 70 nm), spherical in shape, and exhibited uniform distribution and a high encapsulation efficiency. Moreover, a prominent controlled release effect and a significant increase in bioavailability was observed following the encapsulation of GA in NPs. These findings indicated that the limitation of low bioavailability due to the hydrophobic feature of GA was overcome. Furthermore, the pharmacodynamics studies demonstrated that NPs could drastically influence the anti-HF effects of GA after modification with retinoic acid. The results of the present study suggested that retinoic acid-modified GA NPs represent a promising candidate in the development of an anti-HF drug delivery system for the treatment of HF.
研究领域:
药理学
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肝病学
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纳米医学
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DOI
PubMed
高影响因子
CHEMICAL & PHARMACEUTICAL BULLETIN
·
2024
·Vol. 72
·期 7
·669-675
·
IF 1.5
Xiongwei Deng,Qiang Li,Haitao Yuan,Hejun Hu,Shaoyong Fan
Tendon injury is a prevalent orthopedic disease that currently lacks effective treatment. Galangin (GLN) is a vital flavonoid found abundantly in galangal and is known for its natural activity. This study aimed to investigate the GLN-mediated molecular mechanism of tendon-derived stem cells (TDSCs) in tendon repair. The TDSCs were characterized using alkaline phosphatase staining, alizarin red S staining, oil red O staining, and flow cytometry. The effect of GLN treatment on collagen deposition was evaluated using Sirius red staining and quantitative (q)PCR, while a Western bot was used to assess protein levels and analyze pathways. Results showed that GLN treatment not only increased the collagen deposition but also elevated the mRNA expression and protein levels of multiple tendon markers like collagen type I alpha 1 (COL1A1), decorin (DCN) and tenomodulin (TNMD) in TDSCs. Moreover, GLN was also found to upregulate the protein levels of transforming growth factor β1 (TGF-β1) and p-Smad3 to activate the TGF-β1/Smad3 signaling pathway, while GLN mediated collagen deposition in TDSCs was reversed by LY3200882, a TGF-β receptor inhibitor. The study concluded that GLN-mediated TDSCs enhanced tendon repair by activating the TGF-β1/Smad3 signaling pathway, suggesting a novel therapeutic option in treating tendon repair.
研究领域:
骨科
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干细胞研究
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分子生物学
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药理学
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DOI
PubMed
高影响因子
MOLECULES
·
2018
·Vol. 23
·期 12
·3083
·
IF 3.098
Xiaojian Ouyang,Xican Li,Wenbiao Lu,Xiaojun Zhao,Dongfeng Chen
To clarify the role of theB-ring in antioxidant flavonols, we performed a comparative study between galangin with a nullB-ring and 3,5,7-trihydroxychromone without aB-ring using five spectrophotometric assays, namely,•O2−-scavenging, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH•)-scavenging, 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide radical-scavenging, 2,2′-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) radical-scavenging, and Fe3+-reducing activity. The DPPH•-scavenging reaction products of these assays were further analyzed by ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) technology. In the five spectrophotometric assays, galangin and 3,5,7-trihydroxychromone dose-dependently increased their radical-scavenging (or Fe3+-reducing) percentages. However, galangin always gave lower IC50values than those of 3,5,7-trihydroxychromone. In the UPLC-ESI-Q-TOF-MS/MS analysis, galangin yielded galangin-DPPH adduct MS peaks (m/z662, 434, 301, 227,196, and 151) and galangin-galangin dimer MS peaks (m/z538, 385, 268, 239, 211, 195, and 151). 3,5,7-Trihydroxychromone, however, only generatedm/z3,5,7-trihydroxychromone-DPPH adduct MS peaks (m/z586, 539, 227, 196, and 136). In conclusion, both galangin and 3,5,7-trihydroxychromone could similarly undergo multiple antioxidant pathways, including redox-dependent pathways (such as electron transfer (ET) and ETplusproton transfer (PT)) and a non-redox-dependent radical adduct formation (RAF) pathway; thus, the nullB-ring could hardly change their antioxidant pathways. However, it did improve their antioxidant levels in these pathways. Such improvement of theB-ring toward an antioxidant flavonol is associated with its π-π conjugation, which can provide more resonance forms and bonding sites.Keywords:antioxidant;galangin;3,5,7-trihydroxychromone;flavonol;structure–activity;B-ring
研究领域:
生物化学
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药理学
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DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2023
·
IF 10.7
Huishan Rao,Fei Chen,Lianzhu Lin,Mouming Zhao
Flavonoids have a variety of bioactivities, but their poor solubility, low bioavailability, and weak stability limit their application as functional factors in food systems. Soy extracts (SE) mainly composed of soy proteins and soluble polysaccharides at mass ratios of 4.1–5.8: 1 and possessing good bioactivity and nutritional property might be candidate functional encapsulation carriers to improve defects of flavonoids and enhance overall nutritional quality . In this study, galangin (Gal), a poorly water-soluble flavonoid, was used as an example to evaluate the application potential of SE in flavonoid delivery system. Gal-loaded SE nanoparticles (Gal-loaded SE NPs) with high Gal solubility, encapsulation efficiency and bioaccessibility were successfully constructed by pH-driven method. The solubilizing effect of SE on Gal largely depended on the concentrations of SE and Gal. Combining the encapsulation efficiency and retention rate, the optimal conditions were identified as SE concentration of 40 mg/mL, binding time of 5 min, and Gal to SE mass ratio of 1%. Gal-loaded SE NPs showed good storage, thermal, redissolution, and sodium ions stabilities. Based on Fourier transform infrared spectroscopy , X-ray diffraction, and transmission electron microscope analysis , the proteins in SE might undergo a typical de-folding and re-folding process during pH-shifting and mainly combine with Gal by hydrophobic interaction to form Gal-loaded SE NPs with spherical shape (particle diameter <100 nm). This study broadened the application of SE in flavonoid delivery system and provided new ideas for the design and development of new plant-based health food ingredients with multiple functional factors and high nutritional quality.
研究领域:
食品科学
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营养学
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生物化学
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DOI
高影响因子
Korean Journal of Pain
·
2024
·
IF 3.4
Kaiwen Lin,Datian Fu,Zhongtao Wang,Xueer Zhang,Canyang Zhu
Background Galangin, commonly employed in traditional Chinese medicine for its diverse medicinal properties, exhibits potential in treating inflammatory pain. Nevertheless, its mechanism of action remains unclear. Methods Mice were randomly divided into 4 groups for 7 days a normal control group, a galangin-treated (25 and 50 mg/kg), and a positive control celecoxib (20 mg/kg). Analgesic and anti-inflammatory effects were evaluated using a hot plate test, acetic acid-induced writhing test, acetic acid-induced vascular permeability test, formalin-induced paw licking test, and carrageenan-induced paw swelling test. The interplay between galangin, transient receptor potential vanilloid 1 (TRPV1), NF-κB, COX-2, and TNF-α proteins was evaluated via molecular docking. COX-2, PGE2, IL-1β, IL-6, and TNF-α levels in serum were measured using ELISA after capsaicin administration (200 nmol/L). TRPV1 expression in the dorsal root ganglion was analyzed by Western blot. The quantities of substance P (SP) and calcitonin gene-related peptide (CGRP) were assessed using qPCR. Results Galangin reduced hot plate-induced licking latency, acetic acid-induced contortions, carrageenan-triggered foot inflammation, and capillary permeability in mice. It exhibited favorable affinity towards TRPV1, NF-κB, COX-2, and TNF-α, resulting in decreased levels of COX-2, PGE2, IL-1β, IL-6, and TNF-α in serum following capsaicin stimulation. Galangin effectively suppressed the upregulation of TRPV1 protein and associated receptor neuropeptides CGRP and SP mRNA, while concurrently inhibiting the expression of NF-κB, TNF-α, COX-2, and PGE2 mRNA. Conclusions Galangin exerts its anti-inflammatory pain effects by inhibiting TRPV1 activation and regulating COX-2, NF-κB/TNF-α expression, providing evidence for the use of galangin in the management of inflammatory pain.
研究领域:
药理学
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生物化学
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分子生物学
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炎症研究
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疼痛管理
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2026
·
IF 10.4
Yitong Wang,Rui Wang,Qiaoying Guo,Xiaoqian Xu,Hui Teng,Lei Chen,Yanan Zhao
Hydrogen bonding and hydrophobic interactions were the major forces involved in the OVA-FUC complex. • The formation of the OVA-FUC complex resulted in enhanced emulsifying properties compared to individual OVA or FUC. • The galangin-loaded emulsion based on the OVA-FUC complex possessed potent antioxidant activity. • Galangin-loaded emulsion potentiates the oxidative stress resistance of Caenorhabditis . The effective delivery of hydrophobic bioactive compounds remains a major challenge in functional food and nutraceutical applications because of their poor aqueous solubility, limited physicochemical stability, and insufficient bioavailability. In this study, ovalbumin-fucoidan (OVA-FUC) complexes were constructed as food-grade stabilizers to develop galangin (GAL)-loaded emulsions with improved stability and antioxidant efficacy. The interaction mechanism, emulsion stability, and antioxidant activity were evaluated using structural characterization, interfacial analysis, storage tests, chemical antioxidant assays, and an ethanol-induced oxidative stress model in Caenorhabditis elegans . Results showed that OVA and FUC formed complexes mainly through hydrogen bonding and hydrophobic interactions. The 1-1 OVA-FUC complex exhibited the most favorable interfacial behavior and produced emulsions with superior storage stability. The GAL-loaded emulsion showed strong ABTS radical-scavenging activity (74.33 ± 7.60%) and effectively reduced ROS, lipofuscin, and MDA levels while increasing glutathione content and improving locomotor activity in C. elegans. These findings reveal that controlled OVA-FUC interactions can optimize interfacial assembly and emulsion stability, offering a practical strategy to improve the functional delivery of hydrophobic antioxidants in food systems. Download: Download high-res image (200KB) Download: Download full-size image
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PubMed
高影响因子
Separations
·
2025
·Vol. 12
·期 9
·249
·
IF 2.7
Ru Zhao,Xiaoli Li,Yazhou Bao,Wenjun Xu,Chen Xu,Rongrong Wang,Tianlan Xia,Tingli Liu,Ailing Ben
In this investigation, pinocembrin and galangin were efficiently extracted from the male inflorescence ofPopulus albaL. ×berolinensisK. Koch through an enzymatic pretreatment–ultrasonic-assisted strategy (EP-UAS), and the feasibility of their pilot-scale application was validated. The optimal parameters (ethanol volume fraction, cellulase dosage, incubation temperature, incubation time, pH, liquid‒solid ratio, ultrasonic irradiation power during incubation, duty cycle, ultrasonic irradiation power and time during extraction) affecting pinocembrin and galangin yields were systematically explored. The Box–Behnken design (BBD) results provided optimal parameters for the EP-UAS process. Under the optimal conditions, the actual yields of pinocembrin and galangin were 2158.33 ± 0.13 μg/g and 1257.96 ± 0.06 μg/g, respectively. Stability, recovery and reproducibility were determined under the above optimized conditions to evaluate the proposed EP-UAS method. Moreover, laboratory-scale experimental results revealed that the conditions selected via single-factor and response surface experiments were also applicable to pilot-scale production, facilitating industrialization.
研究领域:
天然产物化学
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植物生物技术
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药物提取工艺
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应用植物学
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生物制药工程
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产品关联
DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·
IF 6.2
Yanan Zhao,Rui Wang,Ziyang Huang,Siting Ju,Binghua Dong,Hui Teng,Lei Chen
The gut is often referred to as the “second brain” and is highly vulnerable to alcohol exposure. Galangin, a flavonoid extracted from traditional medicinal herbs, Alpinia officinarum Hance, has manifested auspicious clinical application potential. This study aims to explore the regulatory effect of galangin on ferroptosis in an alcohol-related intestinal injury model and its underlying mechanism. In vivo, we confirmed that galangin administration could alleviate alcohol-induced iron metabolism dysfunction and ferroptosis and activate the SESN2/KEAP1/NRF2 signaling pathway in mice colon. In vitro, alcohol-caused disruption of iron homeostasis and ferroptosis could also be significantly reduced by galangin. Using specific small interfering RNA targeting SESN2 (Si-SESN2) or the NRF2 inhibitor ML385 significantly abrogated the protective effect of galangin. Molecular docking and Co-IP results further revealed that galangin activates NRF2 nuclear translocation by promoting KEAP1/SESN2 formation as well as KEAP1/NRF2 dissociation. Collectively, galangin suppressed ferroptosis by activating the SESN2/KEAP1/NRF2 pathway in mice and Caco-2 cells.
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产品关联
DOI
PubMed
高影响因子
TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH
·
2023
·Vol. 22
·期 1
·15-22
·
IF 0.6
Jingwen Gong,Yu Xie,Yinfen Tan,Hailong Li,Junqing Zhang
Purpose: To investigate the mechanism of action of galangin (GAL) against indomethacin (Indo)-induced gastric injury.
Methods: Ten micromolar GAL with 2 mM Indo or 0.5 mM L-NAME or 2 mM propargylglycine were co-administered to human gastric mucosal epithelial cells GES-1 for 24 h. Cell viability assay and reactive oxygen species (ROS) test were conducted with commercial kits. Protein expressions of constitutive and inducible nitric oxide synthase (cNOS and iNOS, respectively), and cystathionine-γ-lyase (CSE) in GSE-1 cells were investigated by western blot. After 100 - 300 mg/kg, GAL was daily administered to rats for 5 days, and 30 mg/kg Indo was administered to induce gastric injury. Protein expressions of endothelial NOS (eNOS), iNOS, CSE, nuclear factor (NF)-κB, PKC, Akt, phospho-eNOS (Ser-1177), and phospho-eNOS (Thr-495) were investigated by western blot.
Results: Galangin ameliorated the proliferative inhibitions of Indo, propargylglycine, and L-NAME on GSE-1 cells (p < 0.05), rapidly scavenged ROS, and increased cNOS protein expressions (p < 0.05). Galangin (300 mg/kg) inhibited protein expressions of iNOS (p < 0.01), NF-κB, Akt, and PKC (p < 0.05), inhibited the Ser-1177 and Thr 495 phosphorylation of eNOS, elevated eNOS and CSE protein expressions (p < 0.001).
Conclusion: Galangin protects gastric mucosa from Indo by scavenging ROS and inhibiting protein expressions of Akt and PKC. The inhibition leads to Ser-1177 and Thr 495 dephosphorylation of eNOS, thereby prolonging eNOS activity. Besides, GAL inhibits iNOS-produced NO by inhibiting NF-κB to ameliorate the inflammatory reaction induced by Indo.
研究领域:
药理学
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胃肠病学
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细胞生物学
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分子生物学
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DOI
高影响因子
Frontiers in Pharmacology
·
2025
·
IF 4.8
Weirui Ren,Chuang Zhang,Hanyan Wang,Hongzhao Song,Xuejuan Zhu,Zhijun Zhang,Suxian Zhao,Junmin Wang
Background: Primary biliary cholangitis (PBC) is an immune-mediated cholestatic liver disease with currently limited therapeutic options. This study aimed to identify novel therapeutic targets for PBC via systematic druggable genome-wide Mendelian randomization (MR) analysis, predict candidate drugs, and experimentally validate the candidates.Methods: The study integrated druggable genome data, cis-expression quantitative trait loci (cis-eQTL) in blood and liver tissues, and summary data from PBC genome-wide association studies (GWAS). Two-sample MR analysis and colocalization analysis were used to screen genes significantly associated with PBC, followed by phenome-wide association study (PheWAS), functional enrichment analysis, protein-protein interaction (PPI) network construction, drug prediction, and molecular docking. Finally, the therapeutic potential of the candidate drug galangin (GAL) was validated using an α-naphthylisothiocyanate (ANIT)-induced PBC mouse model.Results: A total of 15 druggable genes significantly associated with PBC were identified, primarily enriched in biological processes regulating immune homeostasis, inflammatory signaling, and apoptosis, among others. Subsequent bioinformatic drug prediction and molecular docking identified GAL as a promising drug candidate, showing strong binding affinity to the target ADORA2A. Animal experiments showed that GAL reduced portal tract inflammation and bile duct hyperplasia in liver tissues, while reducing serum levels of liver enzymes (ALT, AST, ALP, etc.) and hepatic expression of inflammatory cytokines (IL-1β, IL-6, TNF-α).Conclusion: By integrating systematic druggable genome-wide MR analysis with experimental validation, this study identified 15 druggable genes associated with PBC. More importantly, it identified GAL as a therapeutic candidate for PBC, with its effects potentially mediated by the ADORA2A target. These findings provide novel therapeutic targets and drugs for PBC. Future research will focus on validating the functions of these druggable genes and elucidating the mechanistic pathway of the galangin-ADORA2A interaction, laying a more solid and comprehensive theoretical and practical foundation for PBC treatment.
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PubMed
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
·
2023
·
IF 6
Jing Kong,Mingyuan Li,Yutong Li,Min Liu,Qian Zhang,Jie Liu,HongZhuan Xuan
A surfactant that can regulate interactions between drugs and proteins would be a material that is medicinally excipient and biomimetic that has great theoretical and practical significance. Thus, the interactions and binding mechanism of flavonoid isomers [galangin (Gal) and baicalein (Bai)] and hemoglobin (HB) under physiological conditions were studied using multispectral methods, dynamic light scattering (DLS), and antioxidant, antibacterial, and cytotoxicity assay techniques. Then, one bile salt biosurfactant [sodium taurodeoxycholate (NaTDC)] was added to explore the effects that it has on the interactions and functional properties of Gal-HB and Bai-HB systems. For Gal-HB and Bai-HB systems, the fluorescence quenching mechanism of flavonoids on HB was always a static quenching. Driven mainly by electrostatic forces, the conformation of HB became loose, and its secondary structure changed as a result of the presence of Gal or Bai. Three adjacent hydroxyl groups on the A-ring had an obvious binding interaction with protein, and thus, Bai had a stronger binding affinity with HB than Gal, and this has a greater influence on the secondary structure of HB than Gal. In the presence of NaTDC, the binding constants were significantly increased for both systems; also, the antioxidant character, stability, solubility, antibacterial properties, and cancer cell growth inhibition of flavonoids were improved to a certain extent. These findings help us understand the pharmacokinetics, pharmacodynamic function and mechanism of Gal and Bai at the molecular level and also lay the scientific foundation for the design of flavonoid-based foods and drugs.
研究领域:
生物化学
·
药理学
·
分子生物学
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产品关联
DOI
高影响因子
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