CARBOHYDRATE POLYMERS
·
2016
·
IF 4.219
Yongqin Wei,Jin Zhang,Yan Zhou,Weiya Bei,Yuan Li,Qipeng Yuan,Hao Liang
Various biological activities of glabridin have been reported in literature, however, the bioavailability and clinical application was limited by its low water solubility. In this study, we developed a novel inclusion complex of glabridin and hydroxypropyl-β-cyclodextrin (HP-β-CD) that features improved solubility and bioactivity. The formation of the inclusion complex was supported by data from FT-IR, PXRD, SEM and NMR. Specifically, the NMR results indicated that the aromatic ring of glabridin was merged into and located at the narrow side the cavity of HP-β-CD. The in vitro tests showed that the formation of the inclusion complex led to 9 times increase in the DPPH radical-scavenging capacity and 20 times increase in the tyrosinase inhibitory activity compared to the free glabridin at the same concentration. Therefore, the glabridin/HP-β-CD inclusion complex adds a promising strategy for the clinical application of glabridin in the future.
研究领域:
药剂学
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天然产物化学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Xier Pan,Yushu Li,Weilin Pang,Yaqi Xue,Zhuxian Wang,Cuiping Jiang,Chunyan Shen,Qiang Liu,Li Liu
Poly(vinyl alcohol) (PVA) and carbomer were used as the hydrogel system to fabricate glabridin-loaded hydrogel-forming microneedles (HFMNs) by chemical cross-linking (CCMNs) and physical cross-linking (PCMNs). The properties and drug permeation effects of glabridin-loaded HFMNs with different methods were compared. They both owned excellent shapes, mechanical and insertion properties. PCMNs showed collapsed shapes during swelling due to the low cross-linking rate and high porosity, which probably results in resealing of skin pores during transdermal drug delivery. However, CCMNs could rapidly swell within 2 h with slightly bending. The infrared spectra indicate that CCMNs and PCMNs might form the hydrogel network by generating hydrogen and covalent bonds, respectively. The in vitro release studies showed that cumulative permeation amount within 24 h (1654 μg/cm 2 ) of CCMNs significantly higher than that (372 μg/cm 2 ) achieved by PCMNs and that (118 μg/cm 2 ) achieved by glabridin-loaded gel. The skin barrier recovery test suggests the desirable security of both microneedles (MNs), notwithstanding the presence of mild erythema in the mouse skin applied CCMNs. These results indicate that CCMNs were more desirable for glabridin delivery using PVA and carbomer as a skeleton of the hydrogel network.
研究领域:
药剂学
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生物材料
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皮肤科学
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产品关联
DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
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2020
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IF 3.594
Lu Wang,Qiong Liu,Baoxian Ye
This paper reports on the first electrochemical investigation of glabridin . Under hydrothermal conditions, poly(diallyldimethylammonium chloride) (PDDA) was attached to a graphene (GR) surface via a noncovalent reaction. Moreover, the morphology and structure of PDDA-GR were characterized by transmission electron microscopy (TEM), Fourier transform-infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) analysis. Based on the nanocomposite, a (PDDA-GR/GCE) sensor was prepared, which showed a significant voltammetric response to glabridin. A simple voltammetric method for the investigation of glabridin with a wide concentration range (6.0 × 10 −8 mol L −1 –6.0 × 10 −6 mol L −1 ) and a low detection limit (2.0 × 10 −8 mol L −1 ) was proposed. The kinetic parameters were calculated, and the reaction mechanism of glabridin was obtained. Additionally, when employed for the analysis of real-life samples, the proposed method showed high accuracy and selectivity.
研究领域:
分析化学
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电化学
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材料科学
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产品关联
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2016
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IF 2.653
Jianmin Chen,Xiaojing Yu,Yufeng Huang
Tyrosinase is an oxidase that is the rate-limiting enzyme for controlling the production of melanin in the human body. Overproduction of melanin could lead to a variety of skin disorders. Glabridin , an isoflavan , isolated from the root of Glycyrrhiza glabra Linn, has exhibited several pharmacological activities, including excellent inhibitory effects on tyrosinase. In this paper, the inhibitory kinetics of glabridin on tyrosinase and their binding mechanisms were determined using spectroscopic, zebrafish model and molecular docking techniques. The results indicate that glabridin reversibly inhibits tyrosinase in a noncompetitive manner through a multiphase kinetic process with the IC 50 of 0.43 μmol/L. It has been shown that glabridin had a strong ability to quench the intrinsic fluorescence of tyrosinase mainly through a static quenching procedure, suggesting a stable glabridin-tyrosinase complex may be generated. The results of molecular docking suggest that glabridin did not directly bind to the active site of tyrosinase. Moreover, according to the results of zebrafish model system, glabridin shows no effects on melanin synthesis in zebrafish but presents toxicity to zebrafish embryo. The possible inhibitory mechanisms, which will help to design and search for tyrosinase inhibitors especially for glabridin analogues, were proposed.
研究领域:
药理学
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生物化学
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皮肤病学
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产品关联
DOI
PubMed
高影响因子
Current Drug Delivery
·
2021
·Vol. 18
·期 10
·1585-1594
·
IF 2.565
Chen Jianmin,Wang Meixia,Ran Mengnan,Liu Xinying,Liu Siwan,Ruan Zhipeng,Jin Nan
Background: The clinical application of glabridin in treating skin diseases has been constrained by the limitations of its poor chemical stability and low skin permeability. Objective: Here, we describe Tip-loading Dissolving Microneedles (TDMNs) encapsulating drugs only in the
tips of needles for glabridin delivery with improved stability and skin permeability. Methods: The TDMNs fabricated by solvent casting technique had sufficient mechanical strength to penetrate through the excised rat's skin without fracture. Drug delivery efficiency and drug residual
in the skin of TDMNs were 63.16% and 49.28%, respectively. Glabridin encapsulated in the tips of TDMNs was effectively delivered into the abdominal skin of rat, and the in vivo delivery efficiency was inversely proportional to the drug doses. Results: Transepidermal Water Loss (TEWL)
significantly increased to 34.80 g/m2·h after the application of TDMNs and returned to normal levels (11.31 g/m2·h) after 8 h, indicating that the TDMNs were well tolerated. The stability of glabridin at room temperature was appreciably improved when loaded in TDMNs. Conclusion:
These results suggest that intradermal delivery of glabridin by TDMNs is a safe and efficient alternative to currently available routes of administration.
研究领域:
药剂学
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皮肤科学
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生物医学工程
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DOI
PubMed
高影响因子
BIOORGANIC CHEMISTRY
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2026
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IF 5.1
Kaleem Majeed,Jia-Jia Gao,Usama,Muhammad Yasir Nawabi,Sheng Zhang,Hong-Hua Ge,Ji-Ming Song
The bioactive isoflavan glabridin of Glycyrrhiza glabra remains in the limelight because of its widespread pharmacological prospect. Here, a better and eco-friendly synthetic method to (±)-glabridin has been introduced, that relies on a six-step protocol, and that is more overall yielding, less dependent on chromatographic purification, and more operationally simpler than previously described and patented ones. The synthesized (±)-glabridin is very effective antioxidant, showing 87.46% the percentage of inhibition. Antibacterial assay indicates that there is a distinct strain-dependent reaction, with a significant response against Escherichia coli (MIC = 33.8 μM) and moderate efficacy against Staphylococcus aureus (MIC = 125 μM). Cytotoxicity assay and IC50 values show a dose-response profile, (±)-glabridin would not be cytotoxic until 62.5 μM and therefore, these concentrations would be more applicable to mechanistic or efficacy research which would need minimal viability decline and a good safety margin within the assayed concentration range. In addition, molecular docking experiments have been performed against the chosen biological targets, which are in agreement with the experimental findings. On the whole, this study holds a viable and green chemistry principles guided synthesis of (±)-glabridin that indicates how it could be used in multidrug functions and pertains to the future bioorganic and medicinal chemistry research.
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DOI
PubMed
高影响因子
Advanced Healthcare Materials
·
2026
·
IF 11
Yuruo Zhang,Haoran Zhang,Lihua Xia,Yuqi Zhou,Yijun Han,Quanjie Lv,Linxuan Zhang,Yuhao Cai,Zeinab Marfavi,Ruihao Yang,Yongjie Wu,Chunyan Wang,Congli Yuan,Ke Tao
Plant-derived compounds are widely used to treat bacterial infections. However, most of them exhibit poor antibacterial activity, particularly against Gram-negative bacteria, and this is further compounded by dose-limiting toxicity. Herein, we present that the antibacterial activity of a plant component, glabridin (GLA), can be enhanced by an ultrasound-triggered perfluorooctyl bromide (PFOB)-liposome nanoformulation, and the biocompatibility thereby improves. When combined with ultrasound, PFOB serves as seed bubbles that generate mechanical forces, inducing liposome rupture and releasing GLA. Meanwhile, the sublethal membrane perturbation caused by US and PFOB synergizes with a low dosage of GLA, resulting in remarkable bactericidal efficacy against both E. coli and P. aeruginosa , with no resistance developing after 30 passages. The irreversible damage to the membrane triggers metabolic collapse in the treated E. coli , as demonstrated by non-targeted metabolomics analysis. We further validated the efficacy of our nanoformulation in treating E. coli -infected wounds in vivo by reducing bacterial load, accelerating healing, and mitigating excessive inflammation. Our work suggested an approach to strengthen the applicability of plant extracts in combating antibiotic resistance.
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产品关联
DOI
PubMed
高影响因子
ARCHIV DER PHARMAZIE
·
2024
·
IF 4.3
Wanru Wang,Kewen Tang,Chenggang Huang,An Liu
As the main active compound of Glycyrrhiza glabra L., glabridin (GLD) has been shown to have multiple bioactivities, whereas the clinical application of GLD is restricted by its low water solubility. In this study, GLD was encapsulated into a sulfobutylether-β-cyclodextrin (SBE-β-CD)-based inclusion complex (SBE-β-CD/GLD) by the freeze-drying method. The materials characterization, antibacterial activity, stimulated cellular behavior and in vivo full-thickness diabetic wound healing ability of the hydrogels were assessed and analyzed. The successful encapsulation of the inclusion complex was confirmed by ultraviolet (UV) visible spectroscopy, Fourier transform infrared (FT-IR), X-ray diffractometer (XRD), scanning electron microscope (SEM), and nuclear magnetic resonance (NMR). SBE-β-CD as an excipient significantly enhances the water solubility of GLD, and SBE-β-CD/GLD showed excellent biocompatibility on human vascular endothelial cells (HUVECs) and erythrocytes. The SBE-β-CD/GLD inclusion complex exerted a pronounced antibacterial activity on Staphylococcus aureus and Escherichia coli in vitro. The SBE-β-CD/GLD inclusion complex markedly enhanced the antioxidant activity compared with free GLD. The SBE-β-CD/GLD inclusion complex potently accelerates the healing of full-thickness skin defects by inhibiting inflammation. The outcomes suggest that SBE-β-CD could be used as a promising drug delivery system for the clinical application of GLD.
研究领域:
药剂学
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生物医学工程
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材料科学
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产品关联
DOI
PubMed
高影响因子
Pharmacognosy Magazine
·
2024
·
IF 0.6
Yongjie Lu,Lushi Cheng,Lu Ren,Dongqiu Chen,Shumin Guan,Siyang Zhu,Xian Xu,Bing Zhang,Minghui Tang,Chijian Zhang,Yong Ai,Lanyue Zhang,Tinggang He
Background: One of the primary flavonoids found in the Glycyrrhiza glabra is called glabridin, which has anti-inflammatory, anti-bacterial, and antineoplastic effects. However, the insolubility of glabridin in water limits its application. Liposomes can increase the solubility of insoluble drugs and improve their bioavailability.Objective: We examined the potential for the treatment of glabridin liposomes on histamine-induced atopic dermatitis.Materials and Methods: After GL treatment, histopathology, inflammatory cytokines, and atopic dermatitis-related proteins were used to evaluate the therapeutic effect of GL.Results: Glabridin liposomes alleviated histamine-induced scratching behavior; reduced mast cell proliferation, infiltration, and degranulation; and restrained the expression of associated pro-inflammatory cytokines. Additionally, glabridin liposomes restored nerve growth factor to normal levels and enhanced the expression of filaggrin to promote cuticle growth and repair skin damage caused by atopic dermatitis.Conclusion: Glabridin liposomes may relieve histamine-induced skin hypersensitivity and cortical hyperplasia by inhibiting the production of inflammatory cytokines, demonstrating their potential for the clinical treatment of atopic dermatitis.
研究领域:
药理学
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皮肤科
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免疫学
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产品关联
DOI
高影响因子
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
·
2017
·
IF 2.625
Jianmin Chen,Qiaoyuan Fang,Shiqi Liu,Guozhong Yang,Yunhua Gao
In order to design more stable formulations for glabridin and to assess the degradation of glabridin as a pollutant in the environment, the photodegradation of glabridin by UV irradiation was investigated. The influences of initial concentrations, solvents, pH values, H 2 O 2 , metal ions and UV absorbers on the photolysis of glabridin were all taken into account. It was found that the photodegradation rate constant increased when decreasing the initial glabridin concentrations, and the degradation of glabridin followed pseudo first-order reaction kinetics. Glabridin in pure methanol exhibited the highest stability with lowest rate constant of 0.357 ± 0.054 h −1 , compared to other saturated monohydric alcohols, and degradation seemed to be affected by the polarity of the solvent. From the experiments to test the effect of pH values on the photolysis of glabridin, we found that glabridin was unstable in both acidic and alkaline solutions. In the UV/H 2 O 2 process, the photodegradation increased with increasing the initial H 2 O 2 concentration. Addition of metal ions such as Fe 2+ , Fe 3+ and Cu 2+ to the glabridin solutions also induced faster degradation compared to negative control, and the degradation processes were dependent on the UV irradiation. In order to stabilize glabridin in the UV process, UV absorbers were added to the solutions. The results suggested that cinnamate and phenyl salicylate could protect glabridin against UV irradiation effectively. More interestingly, we demonstrated that photodegradation products of glabridin would be a valuable source for discovering new tyrosinase inhibitors with higher activity and better stability.
研究领域:
环境科学
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药理学
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化学
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DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2021
·
IF 4.36
Qingquan Guo,Shaojuan Wu,Wenyao Liang,Jianhua Tan,Xiangmei Liu,Yuxi Yuan,Xiaohong Li,Haishan Zhao
Ethnopharmacological relevance Glabridin , extracted from Glycyrrhiza glabra L., is widely used for the treatment of hyperpigmentation because of its anti-inflammatory and antioxidant activities and its ability to inhibit melanin synthesis. This led to the strict regulation of its quality and safety. However, traditional quality control methods used for plant extracts cannot reflect the product quality owing to multiple unknown impurities, which necessitates the further analysis of impurities. Aim of the study The study identified the toxic impurities of glabridin and their toxicological mechanism . Materials and methods In total, 10 glabridin samples from different sources were quantified using high-performance liquid chromatography. Sample toxicities were evaluated using zebrafish and cell models. To identify impurities, samples with different toxicity were analyzed by ultra-high-performance liquid chromatography coupled with quadrupole-Orbitrap mass spectrometry. The toxicity of related impurities was verified in the zebrafish model. Phalloidin stain was used to evaluate subtle changes in myofibril alignment. Results Although glabridin content in the samples was similar, there were significant differences in toxicity. The results were verified using four different mammalian cell lines. Higher contents of glabrone and glabrol were identified in the sample with the highest toxicity. In the zebrafish model, the addition of glabrol reduced the LC 50 of glabridin to 9.224, 6.229, and 5.370 μM at 48, 72, and 96 h post-fertilization, respectively, whereas glabrone did not have any toxic effect. Phalloidin staining indicated that a glabrol impurity exacerbates the myotoxicity of glabridin in zebrafish embryos. Conclusion Glabrol, but not glabrone, was identified as a key impurity that increased glabridin toxicity. This finding indicates that controlling glabrol content is necessary during glabridin product production.
研究领域:
药理学
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毒理学
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民族药理学
·
分析化学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Zhiqiang Guo,Mengdie Tian,Min Zhou,Zhuoer Li,Meijun Li
In this study, the formation of the immunoglobulin G-glabridin (IgG-GB) complex and nanocomplex was analyzed by assessing the structure, stability, solubility, and anticancer effects against the human epithelial ovarian cancer cell line SKOV3. The hydrodynamic sizes of the prepared IgG-GB nanocomplex were 190.1 ± 25.68 nm (PDI: 0.19 ± 0.02), and the solubility levels of GB in the free and nanoformulated forms were 97.28 μg/mL and 368.95 ± 59.63 μg/mL, respectively. Additionally, the IgG-GB nanocomplex exhibited a slower and more sustained release of GB in a pH-sensitive manner. Spectroscopic measurements indicated logKb values of 4.01 and 4.66 for the IgG-GB complex and the IgG-GB nanocomplex, respectively. Furthermore, the main reaction type between IgG and GB was found to be hydrophobic forces, which led to the partial folding of IgG and nanoformulated IgG. Cellular assays demonstrated that the IC50 concentrations of GB, the IgG-GB complex, and the IgG-GB nanocomplex in ovarian cancer SKOV3 cells were 10.74, 10.05, and 6.39 μM, respectively, while these amounts were > 77.84 μM in normal epithelial FHC cells. Moreover, the IgG-GB nanocomplex resulted in increased membrane leakage, mitochondrial dysfunction, and upregulation of Bax/Bcl-2 and caspase-3, along with caspase-3 activity determined by LDH, MP, real-time PCR, and enzyme activity assays. In conclusion, an efficient IgG-GB nanocomplex was potentially prepared and developed as a selective anticancer system against ovarian cancer cells.
研究领域:
药理学
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肿瘤学
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生物化学
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DOI
PubMed
高影响因子
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