MATERIALS & DESIGN
·
2026
·
IF 8.2
Nanxiang Zhang,Haoyun Tan,Mingxin Xu,An Liu
Diabetic wounds are hard to heal and prone to infection. Glabridin (GLD) can promote wound repair but suffers from poor solubility and photostability. This study developed an adhesive eutectogel (GLD/CS/DES) by combining a deep eutectic solvent (DES) formed from sulfobutyl ether-β-cyclodextrin and levulinic acid with chitosan (CS). The DES not only solubilizes GLD but also acts as a dynamic crosslinker, imparting favorable mechanical properties. The gel enabled sustained GLD release for over 10 days and effectively protected GLD from photodegradation. In vitro antibacterial assays demonstrated > 99% efficacy against S. aureus and E. coli by disrupting bacterial membrane integrity. In an infected diabetic wound model, the gel achieved a wound closure rate of 94.3% by day 21. Mechanistic studies revealed that the gel scavenged reactive oxygen species, inhibited the NF-κB pathway, and promoted macrophage polarization from the pro-inflammatory M1 to the reparative M2 phenotype, thereby ameliorating the immune microenvironment, enhancing angiogenesis, and accelerating tissue regeneration.
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DOI
高影响因子
Current Traditional Medicine
·
2024
·Vol. 11
·期 6
·E22150838296794
·
IF 0.6
Jie Huang,Chong Xie,Zhi Pan,Mengya Lin,Qingsheng Chen,Shengzhao Gong,Yadong Huang
BackgroundPlant extracts have wide applications in food, nutrition, and cosmetics, which results in a deeper investigation of natural ingredients. Numerous natural ingredients have been demonstrated to exhibit multiple activities, including antioxidation, anti-inflammation, and anti-melanogenesis. However, their combinations have not been well investigated, which could provide stronger performance with less toxicity and easier applications.MethodsWe used B16F10 cells treated with alpha-melanocyte stimulating hormone (αMSH) for melanogenesis-related studies, including cellular melanin content, tyrosinase activity, and gene or protein expression. MTT assay was used to evaluate cell viability. DPPH scavenging activity was measured for antioxidation. Nitric oxide (NO) content was evaluated in lipopolysaccharide (LPS) treated RAW264.7 cells to indicate the performance on anti-inflammation.ResultsIn this study, six different compounds and their combinations were tested for melanogenesis. The results showed that the combination of glabridin, resveratrol, and ellagic acid (GRE) exhibited the highest efficiency, which was mainly manifested as inhibition of melanin production and tyrosinase activity, higher DPPH scavenging rate, and inhibition of nitric oxide (NO) production. Meanwhile, our results showed that GRE could significantly downregulate the expression of microphthalmia-associated transcription factor (MITF) related genes and proteins and could also inhibit the phosphorylation of cyclic AMP response element-binding protein (CREB), which was the upstream signal of MITF.ConclusionThe results suggest GRE exhibits high efficiency in inhibiting anti-melanogenesis, antioxidation, and anti-inflammation. Furthermore, GRE could downregulate the phosphorylation of the CREB and MITF signal pathway, which provides a theoretical basis for its application in pigmentation disorder disease and cosmetics.
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DOI
高影响因子
POLYMER
·
2024
·
IF 4.1
Yong Chen,An Liu
As a natural isoflavone compound, glabridin (GLD) has excellent skin-whitening properties, but its biomedical applications are greatly limited due to its poor water solubility and low skin permeability. In the current work, GLD was complexed with hydroxypropyl-β-cyclodextrin (HP-β-CD) to form a GLD/HP-β-CD inclusion complex that would improve the water solubility and skin permeability by changing the physicochemical properties of GLD, including the formation of intermolecular hydrogen bonds and amorphous transformation. The cytotoxicity of GLD/HP-β-CD on HaCaT keratinocytes is lower than that of GLD, while it has a more substantial inhibitory effect on melanin than GLD. Furthermore, a dual thermo- and pH-responsive hydrogel called PCG was established as the carrier of GLD/HP-β-CD. The PCG hydrogel presented a porous structure, biodegradability, and excellent biocompatibility. GLD had a dual thermo- and pH-responsive release behavior from the PCG hydrogel and displayed an accelerated release rate at weakly acidic pH conditions compared to the neutral pH environment. Moreover, GLD/HP-β-CD/PCG hydrogel can significantly inhibit melanin deposition in vivo . Taken together, this study provides a low toxicity and high efficiency new method for the application of GLD in biomedical fields, demonstrating its enormous potential in skin-whitening.
研究领域:
药学
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生物医学工程
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功能性化妆品
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药物递送系统
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DOI
高影响因子
Biomaterials Research
·
2026
·
IF 9.8
Ayesha Younas,Muhammad Sohail,Yueting Li,Quan Zhou,Yonghui Shen,Shuanghu Wang,Yaru Shi,Zhenqiu Shang,Chuxiao Shao,Jian Xiao
Hypertrophic scars (HSs) are a prevalent skin condition that imposes substantial functional, financial, and aesthetic burdens, with existing treatments often leading to recurrence, pain, and adverse effects. To address these issues, we propose a first-in-class fast-dissolving sodium alginate-based microneedle patch (sMN) that achieves sequential, dual-release kinetics by integrating tranilast (TS) and glabridin (GL)-loaded nanoparticles (GLNPs), termed TS+GLNPs@sMN. Our system uniquely integrates rapid TS release for immediate “OFF” switching, suppression of fibroblast activation, stabilization of mast cells, and relief of pruritus, with sustained GL release from GLNPs for prolonged “ON” switching, which promotes fibroblast apoptosis and modulates scar matrix deposition. This sequential “OFF-to-ON” paradigm mirrors the temporal progression of HS pathophysiology, with early inflammatory events preceding fibrotic remodeling. The cone-shaped microneedle patch (~565 μm) demonstrated efficient skin penetration/recovery, even drug distribution, fast dissolution (180 ± 20 s), high loading capacity, and desirable release kinetics. In vitro evaluations confirmed promising anti-proliferative, anti-migratory, and anti-angiogenic effects. Preliminary in vivo biocompatibility in mice was satisfactory, with no skin irritation and normal complete blood count, renal, and hepatic function. In vivo studies in a rabbit ear HS model demonstrate accelerated HS healing, reduced HS thickness, epidermal thickness index (ETI), scar elevation index (SEI), and collagen deposition, along with decreased profibrotic markers, inflammatory cytokines, and angiogenic factors. Overall, the TS+GLNPs@sMN patch offers a minimally invasive, self-administrable, dual-action therapeutic strategy for enhanced HS management, with safety and efficacy in preclinical models.
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DOI
PubMed
高影响因子
Pharmaceuticals
·
2026
·Vol. 19
·期 3
·469
·
IF 5.7
Lili Li,Xiaoya Zhang,Guangyuan Tang,Jianxin Wu,Qing Huang
Background: Glabridin, a natural compound derived fromGlycyrrhiza glabraL., possesses skin-lightening effects. This study aims to further elucidate the depigmentation mechanism of glabridin by investigating its effects on melanogenesis and melanin transfer.Methods: We initially confirmed the anti-melanogenic effects of glabridin in MNT-1 human melanoma cells. Then, we investigated the mechanism of its anti-melanogenic effect by evaluating the protein expression of β-catenin and MITF via Western blot. To investigate melanin transfer, we compared glabridin’s efficacy with that of niacinamide, a recognized inhibitor of melanosome transfer and employed two complementary experimental models: (1) α-melanocyte-stimulating hormone (α-MSH)-stimulated MNT-1 cells to analyze dendrite formation, and (2) a UVB-irradiated co-culture system of MNT-1 cells and HaCaT keratinocytes to evaluate melanin transfer.Results: By measuring glabridin’s effects on melanin content, tyrosinase activity, and melanogenesis-related protein expression confirmed its inhibition of melanin synthesis. Further investigation demonstrated that glabridin suppresses melanogenesis by downregulating β-catenin and MITF, indicating inhibition of the Wnt/β-catenin pathway. Furthermore, in α-MSH-treated MNT-1 cells, both glabridin and niacinamide were found to suppress dendrite formation and elongation. In a UVB-exposed co-culture system, both glabridin and niacinamide inhibited melanin transfer to keratinocytes. Mechanistically, these effects were linked to the regulation of Rho GTPases (Rac1, RhoA, Cdc42) and suppression of F-actin reorganization.Conclusions: This study provides, for the first time, evidence that the skin-lightening effect of glabridin involves two complementary mechanisms: inhibition of melanogenesis through suppression of the Wnt/β-catenin pathway, and attenuation of both dendricity and melanin transfer via the influence of Rho family GTPases expression.
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产品关联
DOI
PubMed
高影响因子
ULTRASONICS SONOCHEMISTRY
·
2022
·
IF 9.336
Chen Xing,Wen-Qiang Cui,Yue Zhang,Xin-Shu Zou,Jing-You Hao,Si-Di Zheng,Ting-Ting Wang,Xiao-Zhen Wang,Tong Wu,Yan-Yan Liu,Xue-Ying Chen,Shu-Guang Yuan,Zhi-Yun Zhang,Yan-Hua Li
Licorice ( Glycyrrhiza glabra ) is extensively used owing to the superior pharmacological effects. However, its maximum application potential has not been fully exploited due to the limitation of currently available extraction solvent and methods. In this study, an eco-friendly deep eutectic solvent (NADESs) based ultrasound-assisted extraction (DES-UAE) method was applied to prepare licorice extracts. The DES-UAE using choline chloride and lactic acid as solvent was optimized and modeled by using response surface methodology to maximize the extraction yields of glabridin (GLA) and isoliquiritigenin (ISL). The optimized extracts possessed higher contents of GLA and ISL than available extraction methods, and the enriched products showed superior pharmacological activities in vitro. Furthermore, scanning electron microscopy (SEM) and molecular dynamic simulation analyses were performed to deeply investigate the interaction between solvent and targeted compounds. This study not only provides an eco-friendly method for high-efficient extraction of GLA and ISL from licorice but also illustrates the mechanism of the increased extraction efficacy, which may contribute to the application of licorice and deep insight into extraction mechanism using DES.
研究领域:
药学
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分析化学
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生物技术
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植物科学
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产品关联
DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
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2023
·
IF 8.6
Xiaoyun Liu,Su Yan,Hua Zhou,Hao Wu,Shuya Wang,Xiaoyu Yong,Jun Zhou
Glabridin has beneficial antioxidant, anti-inflammatory, and tyrosinase inhibitory activities, with many applications in the pharmaceutical and cosmetics industries. After industrial extraction of glycyrrhizic acid, Glycyrrhiza glabra residue contains abundant glabridin. Glabridin was extracted from Glycyrrhiza glabra residue with a deep eutectic solvent (DES), followed by the recovery of the glabridin by organic solvent extraction, and then partial purification with hydrophobic macroporous resin. Ethyl acetate was the best extraction solvent, with an extraction yield of 91.63 %. Twelve macroporous resins were evaluated and LSA-21 yielded the best recovery of glabridin. Adsorption of glabridin by LSA-21 resin conformed to pseudo-second-order kinetic and Langmuir models. The thermodynamic parameters ΔH (enthalpy change) and ΔG (Gibbs free energy) were both negative, ΔS (entropy change) was positive. These results indicated that LSA-21 resin spontaneously and exothermically adsorbs glabridin to form a monolayer. The optimum conditions for separating and purifying glabridin by LSA-21 resin were 50 % ethanol aqueous solution(v/v) with a concentration of 56.90 µg/mL glabridin at a flow rate of 2 bed-volumes (BV)/h, and elution with 4 BV of ethanol at 2 BV/h, producing a glabridin yield of 97.80 %. The resin could be reused four times and the glabridin yield slightly decreased to 94 %. The overall recovery of glabridin from the DES Glycyrrhiza glabra extract solution after the ethyl acetate and LSA-21 steps was 89.61 %, with a purity of 17.38 %. This approach is an effective method for the recovery and purification of glabridin from a DES extract of Glycyrrhiza glabra residue, which has potential industrial application for producing glabridin and other natural plant products.
研究领域:
植物化学
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药学
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生物工程
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DOI
高影响因子
PHYTOMEDICINE
·
2024
·
IF 6.7
Jiaxing Yang,Laiying Zhang,Xinlian He,Xupeng Gou,Zhiyong Zong,Youfu Luo
Background The increase in antimicrobial resistance leads to complications in treatments, prolonged hospitalization, and increased mortality. Glabridin (GLA) is a hydroxyisoflavan from Glycyrrhiza glabra L. that exhibits multiple pharmacological activities. Colistin (COL), a last-resort antibiotic, is increasingly being used in clinic against Gram-negative bacteria. Previous reports have shown that GLA is able to sensitize first line antibiotics such as norfloxacin and vancomycin on Staphylococcus aureus , implying that the use of GLA as an antibiotic adjuvant is a promising strategy for addressing the issue of drug resistance. However, the adjuvant effect on other antibiotics, especially COL, on Gram-negative bacteria such as Escherichia coli has not been studied. Purpose The objective of our study was to investigate the targets of GLA and the synergistic effect of GLA and COL in E. coli , and to provide further evidence for the use of GLA as an antibiotic adjuvant to alleviate the problem of drug resistance. Methods We first investigated the interaction between GLA and enoyl-acyl carrier protein reductase, also called "FabI", through enzyme inhibition assay, differential scanning fluorimetry, isothermal titration calorimetry and molecular docking assay. We tested the transmembrane capacity of GLA on its own and combined it with several antibiotics. The antimicrobial activities of GLA and COL were evaluated against six different susceptible and resistant E. coli in vitro . Their interactions were analyzed using checkerboard assay, time-kill curve and CompuSyn software. A series of sensitivity tests was conducted in E. coli overexpressing the fabI gene. The development of COL resistance in the presence of GLA was tested. The antimicrobial efficacy of GLA and COL in a mouse model of urinary tract infection was assessed. The anti-biofilm effects of GLA and COL were investigated. Results In this study, enzyme kinetic analysis and thermal analysis provided evidence for the interaction between GLA and FabI in E. coli . GLA enhanced the antimicrobial effect of COL and synergistically suppressed six different susceptible and resistant E. coli with COL. Overexpression experiments showed that targeted inhibition of FabI was a key mechanism by which GLA synergistically enhanced COL activity. The combination of GLA and COL slowed the development of COL resistance in E. coli . Combined GLA and COL treatment significantly reduced bacterial load and mitigated urinary tract injury in a mouse model of E. coli urinary tract infection. Additionally, GLA + COL inhibited the formation and eradication of biofilms and the synthesis of curli. Conclusion Our findings indicate that GLA synergistically enhances antimicrobial activities of COL by targeting inhibition of FabI in E. coli . GLA is expected to continue to be developed as an antibiotic adjuvant to address drug resistance issues.
研究领域:
微生物学
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药理学
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感染病学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2017
·
IF 3.154
Kaiqin Liu,Fuwei Pi,Hongxia Zhang,Jian Ji,Shuang Xia,Fangchao Cui,Jiadi Sun,Xiulan Sun
Inflammation has been shown to play a critical role in the development of many diseases. In this study, we used metabolomics to evaluate the inflammatory effect of lipopolysaccharide (LPS) and the anti-inflammatory effect of glabridin (GB, a polyphenol from Glycurrhiza glabra L. roots) in RAW 264.7 cells. Multivariate statistical analysis showed that in comparison with the LPS group, the metabolic profile of the GB group was more similar to that of the control group. LPS impacted the amino acid, energy, and lipid metabolisms in RAW 264.7 cells, and metabolic pathway analysis showed that GB reversed some of those LPS impacts. Metabolomics analysis provided us with a new perspective to better understand the inflammatory response and the anti-inflammatory effects of GB. Metabolic pathway analysis can be an effective tool to elucidate the mechanism of inflammation and to potentially find new anti-inflammatory agents.
研究领域:
药理学
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免疫学
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代谢组学
·
细胞生物学
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DOI
PubMed
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2025
·Vol. 39
·期 6
·e70227
·
IF 0
Safdar Ali Amur,Quratulain Khuhro,Najaf Ali Soomro,Muhammad Tariq,Hao Liang,Khalid Hussain Thebo,Mohsin Kazi
This study reports a green one-pot synthesis of glabridin-loaded Zeolitic Imidazolate Framework-8 (Glab@ZIF-8) drug delivery system (DDS) with exceptional drug loading encapsulation (DLE) of ≈ 98.7% and drug loading capacity (DLC) of 32%, surpassing values reported in previous ZIF-8-based DDS. Characterizations using Fourier-transform infrared (FTIR), UV–Visible spectroscopy, dynamic light scattering (DLS), and X-ray diffraction (XRD) confirmed successful encapsulation of Glab within ZIF-8 while preserving its crystallinity. Glab@ZIF-8 exhibited a hexagonal morphology with increased particle size (138.6 ± 5.4 nm) and a higher zeta potential (+41.9 mV), suggesting enhanced colloidal stability and efficient drug entrapment. Thermogravimetric analysis (TGA) demonstrated a total of 32.1% decomposition of Glab@ZIF-8 up to 644 °C. Antibacterial assays revealed that Glab@ZIF-8 exhibited superior activity against Staphylococcus aureus (inhibition zone: 26.2 ± 0.3 mm) and Escherichia coli (23.3 ± 0.2), comparable to that of ampicillin. The minimum inhibitory concentration (MIC) was determined to be 32.5 μg/100 μL. Furthermore, the time-kill studies confirmed a dose- and time-dependent antibacterial effects of Glab@ZIF-8. In vitro drug release studies showed strong pH- and temperature-responsive behavior, with a cumulative release of 93.7% ± 2.4% release at pH 5 (at 37°C) over 72 h. The Glab@ZIF-8 system thus combines high drug loading efficiency, excellent antibacterial activity, and tuneable release characteristics, highlighting its potential as a promising DDS for combating drug-resistant infections.
研究领域:
药剂学
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微生物学
·
材料科学
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产品关联
DOI
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2014
·
IF 2.694
Lingxiao Chen,Wenhua Ji,Wenjuan Duan,Xiao Wang,Qianshan Gao,Yanling Geng,Luqi Huang
Molecularly imprinted polymers (MIPs) with high selectivity and affinity to glabridin were designed based on the screening results of the library of non-imprinted polymers (NIPs). The NIP library contained 48 polymers that were polymerized with the combinations of different functional monomers, cross-linkers, and porogenic solvents. The distribution coefficient ( k ) values were used to estimate the affinity of NIPs to glabridin. The corresponding MIPs of the best three NIPs were prepared. After evaluating the imprinting effects and selectivity of the three MIPs, the performance of the best MIP as solid phase extraction sorbent was investigated. Glabridin with percent recovery of 83 was obtained from the extract of Glycyrrhiza glabra L. ( G. glabra L.) residues by molecularly imprinted solid phase extraction (MISPE). Thus, this material can be successfully used for the extraction and purification of glabridin from G. glabra L. residues.
研究领域:
植物化学
·
分析化学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）