MICROPOROUS AND MESOPOROUS MATERIALS
·
2021
·
IF 5.455
Qunqun Du,Qiang Liu
Excessive UV irradiation induces photoaging and overproduction of melanin , which darkens the skin and affects appearance. To efficiently enhance transdermal delivery and anti-pigmentation, a novel ROS-responsive transdermal nanocarrier for the whitening agent Glabridin by integrating the cell-penetrating peptide polyarginine R8 and borate ester bond into hollow mesoporous silica nanoparticles (HMSNs) has been designed, in which beta-cyclodextrin (β-CD) was grafted onto the surfaces of HMSNs via boronic ester bond to avoid premature release of Glabridin, and R8 conjugated adamantane (Ada) was anchored on HMSN-β-CD via host-gust interaction to enhance the drug delivery efficiency. The ROS-responsive HMSN-β-CD/Ada-R8 nanocarrier was characterized by TEM, FTIR , TGA , Zeta potential , N 2 adsorption, stability, and other parameters. The nanocarrier rapidly penetrated through the epidermis into the keratinocytes and melanocytes and released Glabridin in a controlled ROS-responsive manner. Glabridin released from nanocarriers reversed UV-induced oxidative damage and phototoxicity and reduced hyperpigmentation. Taken together, our study provides a guidance for the design and fabrication of functional transdermal drug nanocarriers for cosmetic applications.
研究领域:
化妆品科学
·
纳米技术
·
药学
·
材料科学
·
皮肤科
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DOI
高影响因子
Heliyon
·
2022
·
IF 3.776
Xiang Cui,Min Cui
Glabridin, a polyphenolic flavonoid isolated from the root of the glycyrrhiza glabra , has been demonstrated to have anti-tumor properties in human malignancies. This study found that glabridin decreased the viability of human breast cancer MDA-MB-231 and MCF7 cells in a dose-dependent manner that was not involved in the caspase-3 cascade. Glabridin promoted the formation of extensive cytoplasmic vacuolation by increasing the expression of endoplasmic reticulum (ER) stress markers BiP, XBP1s, and CHOP. The transmission electron microscopy and fluorescence with the ER chaperon KDEL suggested that the vacuoles were derived from ER. Glabridin-induced vacuolation was blocked when protein synthesis was inhibited by cycloheximide, demonstrating that protein synthesis is crucial for this process. Furthermore, we determined that glabridin causes loss of mitochondrial membrane potential as well as the production of reactive oxygen species, both of which lead to mitochondrial dysfunction. These features are consistent with a kind of programmed cell death described as paraptosis. This work reports for the first time that glabridin could induce paraptosis-like cell death, which may give new therapeutic approaches for apoptosis-resistant breast cancers.
研究领域:
肿瘤学
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细胞生物学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yuyang Cao,Duoling Xu,Zhaoji Zu,Genlu Xu,Yixi Zeng,Jiyu Weng,Zhenhai Huang,Hongping Xiang,Lanyue Zhang,Jinlong Ding,Hui Li
Thermosensitive hydrogels show great potential in healing diabetic wounds, but they are still challenged by the long healing time, risk of infectivity, and accumulation of melanin. Herein, a dual network hydrogel is designed, which consists of chlorogenic acid (CA) modified chitosan (CS) (CA@CS), poly(N-isopropylacrylamide) (PNIPAm), and glabridin liposomes (GL). The gelation transition temperature of the hydrogel is 32–34 °C, which thus endows it with superior injectability at ambient temperature. Moreover, GL/PNIPAm/CA@CS also exhibits excellent biocompatibility, and can promote the growth of epidermal cells, and the healing of diabetic wounds. GL/PNIPAm/CA@CS can also control the immune reactions by enhancing the release of CD206, and decreasing the formation of CD86 and ROS, which further promotes the production of CD31 and VEGF, and reduces the expression of pro-inflammatory factors, thus aiding in the healing of diabetic wounds. Furthermore, GL/PNIPAm/CA@CS can also suppress the growth bacterial, which can thus decrease the wound microbiota levels and facilitate the recovery of diabetic wounds. More importantly, it can reduce melanin production by 80 % due to the action of glabridin. Consequently, GL/PNIPAm/CA@CS shows significant promise in enhancing the wound healing in future and decreasing the accumulation of melanin.
研究领域:
生物材料学
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医学
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药剂学
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产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2026
·
IF 2.9
Huarun Li,Shiyu Wen,Xiangyue Zhao,Xiuxian Zhou,Xianwen Li,Hongping Xiang,Lanyue Zhang,Si Qin
Traditional Chinese medicine Glycyrrhiza uralensis ( G. uralensis ) exerts anti-inflammatory and anti-allergic effects. However, there is currently no valid evidence regarding its anti-histamine effect. This study aimed to elucidate the antihistamine effect of Glycyrrhiza uralensis Fisch essential oils (GUEOs) and glabridin (Gla) extracted from G. uralensis in SPF KM mice and investigate the underlying mechanisms. The chemical components of GUEOs were analyzed using gas chromatography–mass spectrometry (GC–MS), and quality control was conducted. An acute histamine allergy model was established in SPF KM mice following one week of continuous histamine administration. Scratching behavior and appearance of back scratches were observed. Hematoxylin and eosin staining was used to detect the thickness of the mouse dermis. Toluidine blue staining was performed on dermal tissues to count the number of mast cells. Immunohistochemistry was used to determine the integrated optical density (IOD) values of nerve growth factor (NGF) and interleukin-1β (IL-1β). Quantitative Real-time polymerase chain reaction (qRT-PCR) was used to determine the relative intensity of IL-4 and IL-6. Enzyme-linked immunosorbent assay (ELISA) was employed to detect the content of interferon-γ (IFN-γ)，IL-1 and filaggrin (FLG). Compared with the model group, both the GUEOs and Gla groups exhibited reduced scratching behavior in mice, accompanied by epidermal thinning, decreased mast cell numbers, downregulated expression of IL-1β, NGF, IL-4, IL-6, IFN-γ, and IL-1, and upregulated FLG expression. We showed that GUEOs and Gla exert a favorable inhibitory effect on histamine-induced allergic inflammation in mice, suggesting that G. uralensis can serve as a promising natural anti-histamine agent.
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY
·
2021
·
IF 2.351
Chijian Zhang,Yongjie Lu,Yong Ai,Xian Xu,Siyang Zhu,Bing Zhang,Minghui Tang,Lanyue Zhang,Tinggang He
Glabridin, a compound of the flavonoid, has shown outstanding skin-whitening and anti-aging properties, but its water insolubility limits its wide application. Therefore, glabridin liposome (GL) has been developed to improve its poor bioavailability, while there are few studies to evaluate its amelioration of UVB- induced photoaging. This study is performed to investigate the amelioration of GL against UVB- induced cutaneous photoaging. The prepared GL has a spheroidal morphology with an average diameter of 200 nm. The GL shows lower cytotoxicity than glabridin, but it has a more effective role in inhibition of melanin. Moreover, the application of GL can effectively relieve UV radiation induced erythema and leathery skin, associated with the down-regulated expression of inflammatory cytokines (TNF-α, IL-6 and IL-10). Taken together, these results demonstrate that GL has potentials as topical therapeutic agents against UVB radiation induced skin damage through inhibiting inflammation.
研究领域:
药学
·
皮肤病学
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化妆品科学
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产品关联
DOI
PubMed
高影响因子
Food Science and Human Wellness
·
2022
·
IF 8.022
Chunxing Pan,Xiaoying Liu,Yating Zheng,Zejun Zhang,Yongliang Li,Biao Che,Guangrong Liu,Lanyue Zhang,Changzhi Dong,Haji Akber Aisa,Zhiyun Du,Zhengqiang Yuan
Glabridin is the main ingredient of hydrophobic fraction in licorice extract and has been shown to have anti-melanogenesis activity in skins. However, the underlying mechanism(s) remain not completely understood. The aim of this study is thus to elucidate the possible mechanisms related to the melanogenesis suppression by glabridin in cultured B16 murine melanoma cells and in UVA radiation induced hyperpigmentation model of BALB/c mice as well. Molecular docking simulations revealed that between catalytic core residues and the compound. The treatment by glabridin significantly downregulated both transcriptional and/or protein expression of melanogenesis-related factors including melanocyte stimulating hormone receptor (MC1R), microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), TYR-related protein-1 (TRP-1) and TRP-2 in B16 cells. Both PKA/MITF and MAPK/MITF signaling pathways were found to be involved in the suppression of melanogenesis by glabridin in B16 cells. Also in vivo glabridin therapy significantly reduced hyperpigmentation, epidermal thickening, roughness and inflammation induced by frequent UVA exposure in mice skins, thus beneficial for skin healthcare. These data further look insights into the molecular mechanisms of melanogenesis suppression by glabridin, rationalizing the application of the natural compound for skin healthcare.
研究领域:
药理学
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分子生物学
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皮肤科
·
细胞生物学
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产品关联
DOI
高影响因子
INDUSTRIAL CROPS AND PRODUCTS
·
2024
·
IF 5.6
Mei-yuan Li,Zhi-peng Jia,De-min Li,Man-ping Luo,Ying-ying Meng,Kang- xu Wang,Bei Wang,Bing Liu,Xin-guo Zhang,Qin Li
Glycyrrhizic acid (GA) and glabridin (GD) are very important sweeteners and whitening agents present in Glycyrrhiza glabra L. This study investigates the cellulase and pectinase produced by endophytes in G. glabra to optimize and enhance the extraction of GA and GD from licorice using enzyme-assisted extraction (EAE) and microbial co-culture-assisted extraction (MCAE) approaches. Twelve strains with cellulase and pectinase activities were isolated from G. glabra. Notably, the strain G1–5, preliminarily identified as Penicillium sp., demonstrated superior performance in enzyme production and extraction efficiency of GA. Compared to the traditional extraction methods, the EAE process showed an obvious improvement of 32.21% and 56.37% in GA and GD extraction rates, respectively. Similarly, the MCAE process with the enzyme-producing strain G1–5 exhibited an increase of 25.52% and 38.45% in GA and GD extraction rates, respectively. These findings provide valuable guidance and innovative strategies for the extraction of active ingredients.
研究领域:
植物化学
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生物技术
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药用植物学
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产品关联
DOI
高影响因子
INFLAMMOPHARMACOLOGY
·
2024
·
IF 4.6
Weng Jiyu,Wang Ying,Tan Zekai,Yuan Yanghe,Huang Shiyuan,Li Zexi,Li Yiming,Zhang Lanyue,Du Zhiyun
Objectives Chronic neuroinflammation has become one of the important causes of common neurodegeneration disease. Therefore, the target of this study was to explore the protective action of glabridin on lipopolysaccharide (LPS)-induced neuroinflammation in vivo and in vitro and its mechanism. Methods The neuroinflammation model was established by LPS-induced BV2 cells. The cell viability with various concentrations of glabridin was determined by MTT assay, and the content of NO in each group was detected. A neuroinflammatory model was established in male C57BL/6J mice for a water maze test. Subsequently, NF-κB and SOD indices were measured by ELISA, GFAP and IBA-1 indices were measured by immunofluorescence, and Nissl staining was used to explore the Nissl bodies in the hippocampus of mice. Results In vitro experiments, our results expressed that glabridin could markedly increase the cell activity of LPS-induced BV2 cells and reduce the NO expression in cells. It indicated that glabridin had a remarkable impact on the neuroinflammation of LPS-induced BV2 cell protection. In vivo neuroinflammation experiments, mice treated with different doses of glabridin showed significantly improved ability of memory compared with the LPS group in the Morris water maze test. The levels of NF-κB, GFAP, and the number of positive cells in Nissl staining were decreased. High-dose glabridin significantly increased the SOD content in the brain tissue and decreased the IBA-1 levels. Conclusion Glabridin can significantly reduce or even reverse LPS-induced neuroinflammation, which may be related to the fact that glabridin can reduce the NO expression, NF-κB, IBA-1, GFAP, and other inflammatory mediators, upregulate the expression of SOD to relieve oxidative stress of brain and inhibit the activation of gliocyte in brain tissue.
研究领域:
神经科学
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药理学
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免疫学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
PLoS One
·
2025
·Vol. 20
·期 6
·e0325247
·
IF 2.6
Haiyan Liu,Anning Wang,Xiaoyi Chen,Sen Hou,Anzhang Li
Glabridin is widely used as a whitening agent in cosmetics, but its cytotoxicity remains a key concern in safety evaluations. In typical cytotoxicity assays, glabridin is dissolved in dimethyl sulfoxide (DMSO) before being added to the cell culture medium because it is insoluble in water. However, our study revealed that when the DMSO solution of glabridin was mixed with cell culture medium, glabridin was rapidly released due to its poor solubility in the DMSO/water mixture. The released glabridin rapidly formed crystals, which failed to enter cells. Consequently, the whitening efficacy of glabridin was reduced. Moreover, the glabridin crystals produced higher cytotoxicity, possibly due to the physical damage caused by their sharp crystalline structures. However, encapsulating glabridin in cyclodextrin (CD) can address these challenges, offering a better approach for glabridin cytotoxicity assays. The CD encapsulation method, compared to the DMSO solution method, not only decreased the cytotoxicity of glabridin but also increased its whitening efficacy. By comparing the efficacy of glabridin dissolved in DMSO and encapsulated in CD, we discovered that the reported cytotoxicity of glabridin may have been overestimated in previous cytotoxicity studies which used DMSO as a solvent, while its whitening efficacy may have been underestimated. These findings not only offer new insights for in vitro studies of glabridin-like reagents, but also facilitate the development of safer and more effective whitening products.
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产品关联
DOI
PubMed
高影响因子
Heliyon
·
2024
·
IF 3.4
Youwu Wen,Jiajia Teng,An Liu
This study concentrated on developing a novel sprayable hydrogel by the combination of a thermosensitive hydrogel (Pluronic F-127, PF-127) and an inclusion complex of glabridin (GLD) and sulfobutylether-β-cyclodextrin (SBE-β-CD). GLD was encapsulated into SBE-β-CD by the freeze-drying method. The successful encapsulation of the inclusion complex was verified by Fourier transform infrared (FT-IR), X-ray diffractometer (XRD), scanning electron microscope (SEM), and nuclear magnetic resonance spectroscopy (NMR). The prepared GLD/SBE-β-CD inclusion complex exhibited 93.24%～96.46% encapsulation efficiency and 11.24%～11.93% loading capacity, and GLD/SBE-β-CD showed excellent biocompatibility on human vascular endothelial cells (HUVECs) and erythrocytes. GLD/SBE-β-CD inclusion complex exerts higher antioxidant and antibacterial activity than GLD alone. The GLD/SBE-β-CD inclusion complex was well dispersed within 20% PF-127 solution to form the PF-127/GLD/SBE-β-CD hydrogel. Introducing the inclusion complex into the PF-127 hydrogel did not influence its loose and porous structure, while PF-127/GLD/SBE-β-CD hydrogel demonstrated controlled GLD release in a sustained manner. The full-thickness skin wound model showed that the PF-127/GLD/SBE-β-CD hydrogel accelerated the healing of traumatic skin defects. In one aspect, the porous and biocompatible structure of the hydrogel provides favorable conditions for skin cell adhesion and proliferation. In another respect, GLD in therapeutic hydrogel markedly promotes the angiogenesis of endothelial cells, and the migration of keratinocytes. It also presents excellent antibacterial properties in wound surface. Taken together, this work established a novel sprayable hydrogel (PF-127/GLD/SBE-β-CD) and proved that it is an effective strategy for traumatic wound healing.
研究领域:
药剂学
·
生物医学工程
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Materials Chemistry B
·
2026
·Vol. 14
·期 18
·5707-5723
·
IF 6.2
Nanxiang Zhang,Haoyun Tan,Mingxin Xu,An Liu
Diabetic wounds, characterized by delayed healing and susceptibility to infection, pose a significant clinical challenge. Glabridin (GLD), a natural product, has the potential to promote wound repair, but its application is hindered by poor solubility and low photostability. This study developed a novel adhesive deep eutectic gel (eutectogel) by combining a deep eutectic solvent (DES) formed from sulfobutyl ether-β-cyclodextrin (SBE-β-CD) and levulinic acid (Lev) with chitosan (CS) for the efficient delivery of GLD. This system integrates DES with CS through supramolecular interactions, simultaneously addressing the solubility and photostability issues of GLD. The DES not only acts as a solubilizer but also serves as a dynamic crosslinker within the gel network, imparting favorable mechanical properties. The resulting GLD/CS/DES gel formed a flexible patch, enabling sustained GLD release for over 10 days and effectively protecting GLD from photodegradation. In vitro antibacterial assays demonstrated over 99% efficacy against S. aureus and E. coli, with the mechanism of action linked to disruption of bacterial cell membrane integrity. In an infected diabetic wound model, the GLD/CS/DES gel significantly accelerated wound healing, achieving a wound closure rate of 94.3% by day 21. Mechanistic studies revealed that the GLD/CS/DES gel ameliorated the immune microenvironment, promoted angiogenesis, and tissue regeneration by scavenging reactive oxygen species (ROS), inhibiting the nuclear factor kappa-B (NF-κB) signaling pathway, and facilitating macrophage polarization from the pro-inflammatory M1 phenotype to the reparative M2 phenotype. In summary, the GLD/CS/DES gel developed in this study integrates antibacterial, immunomodulatory, and pro-angiogenic functions, offering a promising therapeutic strategy for the management of infected diabetic wounds.
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DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2026
·
IF 6
Lehuan Ni,Ming Luo,Jiaxin Liu,Minghui Zeng,Lijuan Zeng,Janar Jenis,Hao Ji,Honglin Xia,Shilin Luo,Yongtao Yan,Ya Chen,Li Liu,Yuge Wu,Yongshi Feng,Jiansen Li,Yiquan Peng,Hongxia Zhu,Zhuxian Wang,Qiang Liu
Abnormal skin pigmentation is one of the most common skin conditions worldwide. The search for safe, effective, and well-tolerated skin-whitening agents remains a major challenge for the pharmaceutical and cosmetics industries. Glabridin (Gla), often referred to as the “whitening gold”, is widely recognized as one of the most potent natural skin-whitening ingredients. However, its low bioavailability, poor skin permeability, and poor stability severely limit its efficacy in conventional topical formulations. Various studies have shown that glycyrrhizic acid (GA), as a drug carrier, can significantly improve the solubility, stability, and bioavailability of poorly soluble drugs, and the nanoparticles made from it have great potential. In this study, we propose using GA to encapsulate Gla, employing a “combined excipient and active ingredient” approach to improve the solubility, water dispersibility, and stability of Gla, thereby enhancing its transdermal delivery efficiency. After encapsulation, the size of the micelles was only about 37 nm, the encapsulation efficiency reached up to 80%, and the cumulative penetration over 48 h reached 7.44 μg/cm 3 . The micelles also inhibit melanin production and reduce tyrosinase activity. Compared with a simple physical mixed solution or using Gla alone, high-concentration micelles reduced the expression of tyrosinase (TYR) to 0.2, tyrosinase-related protein-1 (TRP-1) to 0.6, and tyrosinase-related protein-2 (TRP-2) to 0.3. At the same time, they downregulated the expression of α-melanocyte-stimulating hormone (α-MSH), cyclic adenosine monophosphate (cAMP), and microphthalmia-associated transcription factor (MITF); and downregulated the Brain and Muscle ARNT-Like 1 (BMAL1) expression whilst upregulating the Period Circadian Regulator 1 (PER1) expression. This study demonstrates that GA-Gla micelles exert a synergistic effect by simultaneously targeting classical skin-whitening pathways and circadian regulatory networks, indicating great potential for skin whitening and providing a new strategy for developing novel, highly effective skin-whitening agents. Download: Download high-res image (96KB) Download: Download full-size image
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DOI
高影响因子
危险品化学品经营许可证（带存储）