FOOD CHEMISTRY
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2018
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IF 4.946
Li Zeng,Huafang Ding,Xing Hu,Guowen Zhang,Deming Gong
Inhibition of α-glucosidase and non-enzymatic glycation is considered as an effective approach to treat type 2 diabetes. Herein, multispectroscopic techniques and molecular docking analysis were used to investigate the inhibition of galangin on α-glucosidase and non-enzymatic glycation. Galangin showed a reversible inhibition on α-glucosidase activity in a mixed-type manner through a monophasic kinetic process, and induced the fluorescence quenching and conformational changes of α-glucosidase by forming α-glucosidase-galgangin complex. Molecular docking revealed that galangin primarily interacted with the amino acid residues within the active site of α-glucosidase, which may prevent the entrance of substrate resulting in a decrease in catalytic efficiency of α-glucosidase. Moreover, galangin moderately inhibited the formation of intermediates of non-enzymatic glycation, fructosamine and α-dicarbonyl compounds and strongly inhibited the formation of advanced glycation end products.
研究领域:
生物化学
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药理学
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糖尿病研究
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DOI
PubMed
高影响因子
PeerJ
·
2021
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IF 2.984
Rangru Liu,Hailong Li,Na Wei,Yinfeng Tan
Galangin has multiple pharmacological efficacies, such as anti-cancer, anti-inflammation and anti-oxidation. Galangin can be rapidly converted into glucuronidated metabolites in vivo. This study aimed to establish an UFLC-MS/MS analytical method to simultaneously determine the concentrations of two glucuronidated metabolites of galangin, galangin-3-O-β-D-glucuronic acid (GG-1) and galangin-7-O-β-D-glucuronic acid (GG-2) in rat plasma. After oral administration of galangal extract (0.3 g/kg), blood samples were collected from the orbital sinus, then treated by methanol precipitation and further gradient-eluted with Phenomenex Kinetex 2.6 µm XB-C18 column. The mass spectrometer was manipulated in the negative electrospray ionization (ESI) and selected multiple reaction monitoring (MRM) mode for the analytes. The precursor-to-product ion pairs applied for GG-1, GG-2 and chrysin (as the internal standard, IS) were m/z 445.2→269.0, 445.2→268.9 and 253.0→142.9, respectively. The results showed that the linear ranges for both GG-1 and GG-2 were 2.0–2000.0 ng/mL ( r 2 > 0.995). The inter- and intra-day precision were 89.3%–109.2%, RSD was less than 15%, and the repeatability was good. The recoveries of both metabolites and IS were over 89%, and matrix effect was within 15%. The validated analytical method was further applied to study the pharmacokinetic profiles of GG-1 and GG-2 in vivo. The pharmacokinetic parameters suggested that T max of GG-1 was equivalent to that of GG-2, and MRT 0-t , t 1/2 of GG-2 were a little higher than those of GG-1. Importantly, AUC 0-t and C max of GG-2 were almost twice as those of GG-1. In short, the validated UFLCMS/MS analytical method was feasible to simultaneously determine two galangin metabolites GG-1 and GG-2 in rat plasma and further analyze in vivo metabolism of galangin.
研究领域:
药物分析
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药理学
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生物化学
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DOI
高影响因子
BRITISH JOURNAL OF PHARMACOLOGY
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2025
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IF 7.7
Wenjing Wei,Abudureyimu Alimujiang,Zehua Zhang,Zulipikaer Wusiman,Xiangran Liu,Yong Zhu,Yipeng Bai,Ziqi Zhu,Zhijian Li,Dengqiu Xu,Shixia Huo
Background and Purpose Vitiligo, a common depigmenting skin disorder, is characterised by the selective loss of melanocytes, which leads to distinctive non-scaly, chalky-white macules. Galangin is a flavonoid found in galangal and propolis; our previous study highlighted the therapeutic potential of galangin. However, the contributions of galangin to restoring skin pigmentation and maintaining immune homeostasis, as well as its detailed molecular roles in vitiligo management, have not been fully elucidated. Experimental Approach We used C57BL/6J mice with H 2 O 2 -induced vitiligo or imiquimod-induced erythema, to test the anti-vitiligo effects and anti-inflammatory effects of galangin. Other techniques used included immunoprecipitation-mass spectrometry, pull-down assays, Autodock and surface plasmon resonance (SPR) analysis in cultured cells. Key Results Galangin exerted anti-inflammatory and antioxidant effects through two mechanisms, promoting melanocyte proliferation while inhibiting macrophage proliferation. Using immunoprecipitation-mass spectrometry, pull-down assays, Autodock and SPR analyses, we found that galangin bound to annexin A2 and promoted its degradation in macrophages. This interaction led to inhibition of macrophage proliferation, activation and polarisation. In vivo, galangin significantly improved skin conditions in mice with H 2 O 2 -induced vitiligo or imiquimod-induced erythema. Furthermore, annexin A2 knockout abolished the protective effects of galangin in these models. Conclusions and Implications Galangin bound to annexin A2 and promoted its degradation in macrophages, decreasing release of inflammatory factors and chemokines. These findings provide experimental evidence supporting the potential application of galangin in clinical treatments for vitiligo and highlight ANXA2 as a promising therapeutic target for managing this condition.
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DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2018
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IF 2.297
Jing Zhu,Qilong Wang,Huihua Li,Huiyun Zhang,Yuan Zhu,Emmanuel Omari-Siaw,Congyong Sun,Qiuyu Wei,Wenwen Deng,Jiangnan Yu,Ximing Xu
The aim of this study was to develop liver targeting galangin-loaded liposomes (Galangin-Liposomes) and evaluate their oral bioavailability. Box Behnken design was applied to optimize the formulation of Galangin-Liposomes by assessing encapsulation efficiency. The optimized Galangin-Liposomes were characterized by zeta potential , encapsulation efficiency, morphology, stability and in vitro release. Meanwhile, in vivo pharmacokinetics and tissue distributions were studied. Morphology of the selected Galangin-Liposomes revealed spherical and uniformly distributed nanoparticles with size of 74.67 ± 7.09 nm and encapsulation efficiency of 92.36 ± 2.71%. The formulation also significantly increased the extent of galangin release in vitro as well as its oral bioavailability (470.12%) in vivo . Furthermore, the tissue distribution studies further showed that the Galangin-Liposomes were enriched in the liver and exhibited better hepatoprotective effects in CCl 4 -intoxicated mice compared with the free galangin (p < 0.01). Collectively, these results indicated that the liposomes could serve as an effective delivery system to achieve improved oral bioavailability and liver targeting of galangin.
研究领域:
药剂学
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药理学
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纳米技术
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DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2024
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IF 4.8
Kaiwen Lin,Zhongtao Wang,Erhao Wang,Xueer Zhang,Xiaofei Liu,Faming Feng,Xiaodan Yu,Guohui Yi,Yan Wang
Ethnopharmacological relevance Galangin, a bioactive compound extracted from Alpinia officinarum Hance (Zingiberaceae), a plant with significant ethnopharmacological importance, has been used for thousands of years as a spice, condiment, and medicinal agent for various conditions, including gastrointestinal disorders. Although there is evidence suggesting its potential to improve gastric ulcers, the molecular mechanisms underlying its anti-ulcer properties are not fully understood. Objective of the Study: This study aimed to investigate the effects of galangin on ethanol-induced acute gastric mucosal injury (AGMI) in mice and elucidate its molecular mechanisms. Materials and methods Sixty BALB/c mice were randomly assigned into two main groups: a normal control group (n = 10) and an ethanol-induced group (n = 50). After establishing the AGMI model in mice using a combination of 40% ethanol and anhydrous ethanol, the ethanol-induced group was further subdivided into five subgroups (n = 10): an omeprazole control group (20 mg/kg), an untreated ethanol group, and three treatment groups receiving high-dose (50 mg/kg) or low-dose (25 mg/kg) galangin or capsazepine (CPZ, 2 mg/kg). The protective effects of galangin were evaluated through mucosal injury indices, hematoxylin and eosin staining, and quantification of inflammatory markers (IL-1β, IL-6, IL-8, and TNF-α). Oxidative stress levels and matrix metalloproteinase activity were measured using specific assay kits. Molecular docking was conducted to assess the binding affinity of galangin to key proteins within the transient receptor potential vanilloid 1 (TRPV1) pathway. Real-time fluorescence quantitative PCR (qPCR) was used to determine mRNA expression levels of TRPV1, calmodulin (CaM), substance P (SP), and CGRP in gastric tissues. Protein expression levels of TRPV1, nerve growth factor (NGF), tropomyosin receptor kinase A (TRKA), transforming growth factor beta (TGF-β), cyclooxygenase-2 (COX-2), and nuclear factor kappa B (NF-κB) were assessed through Western blot analysis. In cellular experiments, Culture of Human Gastric Epithelial Cells (GES-1) were treated with various concentrations of galangin after 7% ethanol induction. Cell proliferation, apoptosis, and migration were evaluated using Hoechst 33258 staining and transwell migration assays. TRPV1 protein expression was detected using immunofluorescence, and the expression levels of Bcl-2, BCL2-Associated X (BAX), and Caspase-3 were quantified by qPCR. Additionally, specific probe kits were used to measure intracellular calcium ions (Ca 2+ ) and mitochondrial membrane potential. Results The findings indicate that galangin significantly improved mucosal pathology by reducing ulcer indices and inflammatory levels, while enhancing superoxide dismutase (SOD) activity and decreasing malondialdehyde (MDA) concentration. Galangin also reduced matrix metalloproteinase-2 (MMP-2), m metalloproteinase-9 (MMP-9) levels, promoting mucosal repair. At the cellular level, galangin decreased intracellular calcium ion concentration and mitigated the decline in mitochondrial membrane potential, enhance the restoration of mucosal cells, increased migration and proliferation, and reduced apoptosis. Molecularly, galangin demonstrated favorable binding to TRPV1, NGF, TRKA, TGF-β, COX-2, and NF-κB, and reversed the elevated expression of these proteins. Additionally, galangin downregulated the mRNA expression of TRPV1, CaM, SP, CGRP, BAX, and Caspase-3 in gastric tissues/cells, while upregulating Bcl-2 mRNA expression. Conclusion Galangin mitigates AGMI by inhibiting the overactivation of the TRPV1 pathway, thereby blocking aberrant signal transduction. This study suggests that galangin has therapeutic potential against ethanol-induced AGMI and may be a viable alternative for the treatment of alcohol-induced gastric mucosal injuries.
研究领域:
药理学
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胃肠病学
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分子生物学
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细胞生物学
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DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
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2016
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IF 3.182
Cen Zhang,Guowen Zhang,Junhui Pan,Deming Gong
Galangin is a natural flavonol isolated from plants with potent biological activities. Galangin was found to significantly inhibit xanthine oxidase (XOD) activity in a competitive manner with the generation of superoxide radical (O 2 − ) in the enzyme catalysis, but galangin showed insignificant scavenging activity on 1,1-diphenyl-2-picryhydrazyl (DPPH) and O 2 – radicals. These results demonstrated that inhibition of O 2 – radical generation by galangin may be due to the competitive inhibition of uric acid formation by a ping-pong mechanism. XOD had one high affinity binding site for galangin with a binding constant of 3.60 × 10 4 L mol − 1 at 298 K. Hydrogen bond and hydrophobic interaction dominated the binding process on account of the negative enthalpy and positive entropy changes. The binding of galangin to XOD induced an increase in α-helix and random coil contents and a decrease in β-sheet and β-turn contents of XOD. Further molecular docking study validated that galangin can competitively bind to the site in the molybdenum atomic (Mo) domain, occupying the catalytic center to avoid the entrance of the substrate xanthine, resulting in the inhibition of XOD activity. These findings have provided new insights into the two-substrate kinetics of galangin on XOD and useful information for functional research of galangin in the treatment of gout and oxidative damage.
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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DOI
PubMed
高影响因子
Chemistry Central Journal
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2015
·Vol. 9
·期 1
·1-10
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IF 2.187
Chen Feng,Tan Yin-Feng,Li Hai-Long,Qin Zhen-Miao,Cai Hong-Die,Lai Wei-Yong,Zhang Xiao-Po,Li Yong-Hui,Guan Wei-Wei,Li You-Bin,Zhang Jun-Qing
Background Galangin (3,5,7-trihydroxyflavone) is present in high concentrations in herbal medicine such as Alpinia officinarum Hance. Galangin shows multifaceted in vitro and in vivo biological activities. The number and position of hydroxyl groups in this molecule play an important role in these biological activities. However, these hydroxyl groups undergo glucuronidation and sulfation in in vitro assay system. However, the systemic exposure to galangin after dosing in animals and/or humans remains largely unknown. Thus it is not clear whether the galangin exists in the body at concentrations high enough for the biological effects. Furthermore, the metabolite identification and the corresponding plasma pharmacokinetics need to be characterized.Results Two LC-MS/MS methods were developed and validated and successfully applied to analyze the parent drug molecules and aglycones liberated from plasma samples via β-glucuronidase hydrolysis. Our major findings were as follows: (1) The routes of administration showed significant influences on the systemic exposure of galangin and its metabolites. (2) Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication. (3) Kaempferol conjugates were detected demonstrating that oxidation reaction occurred; however, both glucuronidation and sulfation were more efficient. (4) Oral bioavailability of free parent galangin was very low.Conclusion sSystemic exposure to galangin and its metabolites was different in rat plasma between oral and intravenous administration. Further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.
Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication.
研究领域:
药理学
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药物代谢动力学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2025
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IF 6.2
Yanan Zhao,Rui Wang,Ran Cao,Leyao Chen,Lei Chen,Hui Teng
Hyperuricemia (HUA) is often associated with renal injury and intestinal flora disturbance. Galangin, a polyphenolic compound found in Alpinia officinarum and propolis, has demonstrated the capacity to inhibit xanthine oxidase (XO) activity both in vitro and in silico; however, the precise mechanisms underlying its effects in vivo remain unclear. This study aims to investigate the effect of galangin on uric acid (UA) metabolism as a prospective strategy for lowering UA and further explore the underlying mechanisms. Galangin mitigates kidney tissue injury and fibrosis, reduces the serum UA level via inhibiting UA synthesis in the liver, and promotes UA excretion in the kidney. Molecular docking results also uncovered the structure–activity relationship of galangin and the UA transporters GLUT9, URAT1, ABCG2, and OAT1, implying a potential interaction. Also, galangin mitigated the HUA-activated NF-κB/MAPK signaling pathway in the kidney, as well as colon tissue damage and barrier dysfunction, which are closely linked to deteriorated intestinal permeability. Moreover, galangin remedied the alterations in intestinal microecology caused by HUA, encompassing changes in the structure and composition of gut microbial species as well as the metabolism of SCFAs. Collectively, this study demonstrates that galangin exerted an improvement on HUA by ameliorating gut–kidney axis dysfunction.
研究领域:
药理学
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代谢生物学
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肾脏病学
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微生物组学
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DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2026
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IF 10.4
Yitong Wang,Lei Chen,Ruoxin Liu,Liya Wen,Zhixian Deng,Ximin Huang,Qifu Tan,Hui Teng,Yanan Zhao
Adjusting the oleogel-hydrogel ratio dictates the micro- and macro-properties of bigels. • The bigel structure evolves from O/W to bicontinuous and finally to W/O by increasing the oleogel ratio. • Bigel with Hydrogel and Oleogel ratio of 5H:5O is optimal for swallowing and show significant commercial potential for addressing the needs of the dysphagia diet market. • 5H:5O bigel formulation optimally enhances the release rate of Galangin. This study comprehensi v ely investigates the structure-function relationship of bigels tailored by varying oleogel-to-hydrogel ratios (3O:7H, 5O:5H, and 7O:3H v /v) for the delivery of the model bioactive compound, galangin (GAL). Through microstructural, spectroscopic, rheological, and in vitro analyses, it was shown that the ratio of oleogel/hydrogel greatly influences the physicochemical, mechanical, digestive, and release properties. The 5O:5H bigels exhibited excellent structural stability, optimal swelling behavior, and IDDSI Level 5–6 compliance, making it suitable for dysphagia-friendly foods. FTIR and XRD analyses confirmed the role of monoglyceride in promoting β-sheet formation and crystalline network development, while LF-NMR and rheology revealed composition-dependent water distribution and viscoelastic behavior. During in vitro digestion, hydrogel-rich bigels exhibited faster lipid digestion and greater FFA release, with cumulative FFA release decreasing from 93.87% in 3O:7H to 56.32% in 5O:5H and 52.80% in 7O:3H. In contrast, oleogel-rich systems showed slower lipid digestion, suggesting improved potential for controlled release. Electronic nose results further highlighted temperature- and composition-dependent volatile release profiles. Overall, this work establishes that bigel composition can be precisely modulated to meet specific requirements in functional foods and pharmaceutical formulations. The 5O:5H bigel, conforming to IDDSI Level 5–6, is identified as the optimal formulation for dysphagia-friendly food due to its excellent structural stability and swallowing safety. The 7O:3H bigel exhibits superior sustained-release capacity and high bioavailability, making it the optimal candidate for controlled delivery of GAL. These findings provide a theoretical basis for the precise formulation design of bigels. Download: Download high-res image (146KB) Download: Download full-size image
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PubMed
高影响因子
MOLECULAR NUTRITION & FOOD RESEARCH
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2025
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IF 4.2
Daermu Qumu,Mu Tian,Hengxi Li,Xiujuan Yang,Binhui Han,Lanting Wei,Bo Li,Mengxue Ma,Junjie He,Xiaoni Shao
Galangin (GAL), a flavonol found in Alpinia officinarum and propolis, is a promising functional food. This study investigated the therapeutic effects and mechanisms of GAL in mice with hyperuricemic nephropathy (HN) by focusing on renal metabolomics and network pharmacology. In this study, we conducted untargeted metabolomic analysis and network pharmacology prediction. Subsequently, a compound-reaction-enzyme-gene network was constructed based on the results of metabolomics and network pharmacology to elucidate potential connections. The results demonstrated that GAL can improve renal interstitial fibrosis and inflammatory infiltration and reduce serum levels of uric acid (UA), urea nitrogen (UREA), and creatinine (CREA). Metabolome analysis indicated that GAL affected thiamine, pyrimidine, nicotinate, nicotinamide, pyruvate, glyoxylate, and dicarboxylate metabolism. Network pharmacology and experimental results showed that GAL reduced the key target expression of the tumor protein P53 (TP53), tumor necrosis factor (TNF), signal transducer and activator of transcription 3 (STAT3), heat shock protein 90 alpha family class A member 1 (HSP90aa1), albumin (ALB), and caspase-3 (CASP3). GAL also downregulated the expression of Janus kinase 2 (JAK2), phospho-JAK2 (P-JAK2), and phospho-STAT3 (P-STAT3). Furthermore, a joint analysis of the metabolome and network pharmacology showed that GAL can reverse HN through amino acid metabolism, nucleotide metabolism, energy metabolism, and endocrine system pathways. GAL can alleviate HN effectively and might play synergistic therapeutic roles through regulating metabolic profiles and the JAK2/STAT3 signaling pathway.
研究领域:
医学
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药理学
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代谢组学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2026
·
IF 6.7
Yanan Zhao,Rui Wang,Ran Cao,Leyao Chen,Siting Ju,Hui Teng,Lei Chen
Hyperuricemia (HUA), a metabolic disorder characterized by elevated serum uric acid (UA) levels, is closely linked to various chronic diseases. Galangin (GAL), a natural polyphenol abundant in Alpinia officinarum and propolis, has been reported to alleviate HUA by inhibiting hepatic UA production and promoting renal UA excretion. However, its impact on intestinal UA elimination is poorly understood. This study investigated GAL’s protective role in HUA mice, focusing on intestinal UA transport, inflammatory response, and barrier integrity. Our findings demonstrate that GAL suppressed xanthine oxidase activity in the serum, jejunum, and ileum, attenuated intestinal morphological damage and oxidative stress, and enhanced expression of ABCG2 and GLUT9 in the small intestine. GAL also upregulated the tight junction proteins Occludin and ZO-1 while inhibiting MAPK/NF-κB pathway in the intestine. Collectively, GAL ameliorates HUA by modulating intestinal UA metabolism and repairing intestinal injury, highlighting its potential as a nutraceutical for UA-lowering therapy.
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DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
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2026
·
IF 13.8
Qiaochun Chen,Yuanyuan Chen,Qian Zhou,Mingfu Wang
Galangin (Gal), a hydrophobic flavonoid prevalent in galangal, exhibits remarkable inhibitory effects against the formation of β -carboline, a subclass of heterocyclic amines. However, its poor aqueous water solubility hinders its application in water-based food systems, such as braised meats. To address this issue, Gal-loaded zein/pectin nanoparticles (ZGP-NPs) were designed to integrate the potential inhibitory effects of Gal and pectin against HAs formation while improving Gal dispersion in aqueous systems. The nanoparticle formulation was optimized, achieving high encapsulation efficiency (96.07%) and loading capacity (7.93%) at a Gal concentration of 2 mg/mL. Microstructural and physicochemical characterization revealed successful encapsulation, yielding uniform spherical particles with an average size of 123.42 nm. ZGP-NPs demonstrated satisfactory stability across different chemical and physical conditions. In brine models and braised lamb applications, ZGP-NPs significantly suppressed β -carboline formation, achieving 35.43–68.30% (free type) reductions in β -carbolines in brine model systems, and 10.58–28.24% (free type) and 31.72–55.22% (free + bounded type) reductions in braised lamb. Mechanistic insights suggest that ZGP-NPs may suppress β -carboline generation via trapping of aldehydes (precursors for β -carboline formation), free radical scavenging, and direct binding of β -carbolines. This work demonstrates a pioneering strategy for mitigating HAs using polyphenol-encapsulated nanoparticles, providing a novel, efficient, and cost-effective approach for improving meat safety.
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高影响因子
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