PLoS One
·
2016
·Vol. 11
·期 9
·e0161566
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IF 3.057
Ming Guo,Xiaomeng Wang,Xiaowang Lu,Hongzheng Wang,Peter E. Brodelius
In order to obtain the biological active compound, α-mangostin, from the traditional native mangosteen ( Garcinia mangostana L.), an extraction method for industrial application was explored. A high yield of α-mangostin (5.2%) was obtained by extraction from dried mangosteen pericarps with subsequent purification on macroporous resin HPD-400. The chemical structure of α-mangostin was verified mass spectrometry (MS), nuclear magnetic resonance ( 1 H NMR and 13 C NMR), infrared spectroscopy (IR) and UV-Vis spectroscopy. The purity of the obtained α-mangostin was 95.6% as determined by HPLC analysis. The binding of native α-mangostin to human serum albumin (HSA) or transferrin (TRF) was explored by combining spectral experiments with molecular modeling. The results showed that α-mangostin binds to HSA or TRF as static complexes but the binding affinities were different in different systems. The binding constants and thermodynamic parameters were measured by fluorescence spectroscopy and absorbance spectra. The association constant of HSA or TRF binding to α-mangostin is 6.4832×10 5 L/mol and 1.4652×10 5 L/mol at 298 K and 7.8619×10 5 L/mol and 1.1582×10 5 L/mol at 310 K, respectively. The binding distance, the energy transfer efficiency between α-mangostin and HSA or TRF were also obtained by virtue of the Förster theory of non-radiation energy transfer. The effect of α-mangostin on the HSA or TRF conformation was analyzed by synchronous spectrometry and fluorescence polarization studies. Molecular docking results reveal that the main interaction between α-mangostin and HSA is hydrophobic interactions, while the main interaction between α-mangostin and TRF is hydrogen bonding and Van der Waals forces. These results are consistent with spectral results.
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ACS Biomaterials Science & Engineering
·
2025
·
IF 5.5
Tianhui Liu,Qingshuang Wang,Wenxin Geng,Xue Jiang,Changshun Lu,Zhe Zhang,Xiangru Feng
The cancer-associated fibroblasts (CAFs) in tumor stroma present substantial barriers to drug penetration, resulting in tumor resistance and progression. One promising strategy is to reprogram CAFs into a quiescent state, which necessitates novel approaches. Our study introduces a sequential treatment strategy using chitosan thermosensitive hydrogels loaded with α-Mangostin (α-M), a small molecule drug with antifibrotic properties, aimed at reprogramming CAFs within the breast cancer tumor microenvironment (TME). We developed glutathione (GSH)-responsive nanoparticles (NPc) that carry the chemotherapeutic drug doxorubicin (DOX). Treatment with α-M results in the downregulation of CAF-specific biomarkers and a remodeled TME, which improves the penetration of NPc/DOX deep into the tumor tissue. This strategy holds great promise in enhancing cancer therapeutic outcomes in tumors rich in CAFs, particularly in the case of breast cancer.
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MEDICINAL CHEMISTRY RESEARCH
·
2024
·
IF 2.6
Cheng Wenhui,Zhang Yuejuan,Chen Cheng,Gao Lei,Lv Yuwei,Yu Dian,Chen Bin,Wan Yi
The production of carbapenemases is a significant mechanism contributing to carbapenem resistance in Enterobacteriaceae . Among these carbapenemases, OXA-48 presents a distinct challenge and threat, as most β-lactamase inhibitors do not effectively inhibit its activity. In this study, we investigated the inhibitory potential of α-mangostin against OXA-48 with an IC 50 value of 0.52 μM. Enzyme activity assays demonstrated that α-mangostin inhibited OXA-48 reversibly through a non-competitive and dose-dependent inhibition mode. The docking analysis revealed that the 7-hydroxyl group of α-mangostin formed hydrogen bonds with Thr197 and Trp222, whereas the 5-hydroxyl group and the 4-carbonyl group interacted with Lys116 and Met115. Our study indicates that α-mangostin exhibits significant inhibition against OXA-48 and holds promise as a potential compound for the development of β-lactamase inhibitors.
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Scientific Reports
·
2025
·
IF 3.9
Li Xinmei,Zhu Xinyu,Wang Bingqian,Sun Jiaming,Xia Yun
A-Mangostin is the predominant xanthone found in the pericarp of mangosteen. It has been scientifically proven to possess anti-proliferative and apoptotic properties against different types of human cancer cells. In Asia, α-mangostin is widely used as a natural ingredient in cosmetic and medicinal products, particularly for treating acne and skin issues.Our objective was to evaluate the impact of α-mangostin on microphthalmia-associated transcription factor ( MITF ) and pigmentation related genes, and to explore the mechanism of α-mangostin on ultraviolet (UV)-B or forskolin (FSK)-induced pigmentation in cultured skin. We designed subgroups to evaluate the expression level of pigmentation related genes in cultured skin and B16F10 cells by α-mangostin and the melanin production level induced by UVB or FSK, respectively. The results showed that 40 µM α-mangostin could significantly reduce the melanin content in UVB-stimulated hair follicles treated with H 2 O 2 , and it had a lower melanin level compared with the control group. Besides, the study found that α-mangostin also reduced the expression of MITF , tyrosinase (TYR), and TY receptors induced by FSK in B16F10 cells, which is regulated by retinoid x receptors (RXR) and retinoic acid receptors (RAR). α-Mangostin can inhibit the formation of RAR/RXR heterodimers to mediate MITF expression. The results of our experiments provide evidence that α -Mangostin can inhibit melanogenesis by regulating the MITF protein and protecting MITF protein from damage caused by oxidative stress pathways. The above research shows that α -Mangostin can effectively reduce the content of melanin, and as a natural whitening active ingredient, it has great application prospects in the development of sunscreen.
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BioNanoScience
·
2026
·Vol. 16
·期 2
·120
·
IF 3.2
He Yifei,Wang Zhe
Pathogenic bacteria such as Staphylococcus aureus ( S. aureus ) represent a serious global health concern by forming biofilms that enhance bacterial resistance and persistence in host and environmental niches. Natural compounds such as α-mangostin (α-m) exhibit promising antibacterial potential but low solubility, instability and limited bioavailability restrict their biomedical application. This study prepared α-mangostin-loaded casein–chitosan nanoparticles (α-m NPs) via ionic crosslinking–emulsification under neutral pH conditions and characterized them using dynamic light scattering, scanning electron microscopy, and Fourier-transform infrared spectroscopy, which confirmed efficient encapsulation and structural stability. The results showed that α-m NPs achieved sustained drug release over 72 h and exhibited significantly enhanced bacteriostatic and bactericidal effects. Biofilm assays further revealed that α-m NPs more effectively suppressed extracellular polysaccharide secretion and biofilm formation in MRSA T144 and ATCC 29213 strains. These findings as a whole validate α-m NPs as an efficient antibacterial and anti-biofilm nanosystem and establish a polysaccharide–protein nanoplatform with considerable potential for applications in nanomedicine and anti-infective therapy. Graphical abstract
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FOOD CHEMISTRY
·
2026
·
IF 9.8
Naymul Karim,Ke Zhang,Mohammad Rezaul Islam Shishir,Mohammad Nasiruddin Rana,Gobinath Marappan,Muhammad Arslan,Haroon Elrasheid Tahir,Li Zhihua,Xiaodong Zhai,Isam A. Mohamed Ahmed,Jitbanjong Tangpong,Xiaobo Zou
α-mangostin (αM), a poorly soluble xanthone, was encapsulated in cocoa butter emulsions stabilized by xanthan gum (XG; 0–0.5%) to enhance its stability and control its gastrointestinal release. The emulsions exhibited high encapsulation efficiency (77–85%) with submicron droplet sizes (440–540 nm), low polydispersity index (<0.3), and negative zeta potential (> −20 mV). Increasing XG concentration enhanced viscosity, shear-thinning behavior, centrifugal stability, and thermal resistance, while ensuring excellent stability over 21 days of storage without oxidative/microbial degradation. Structural analyses (FTIR, XRD) confirmed successful αM encapsulation in a semi-crystalline matrix (crystallinity >60%). Microscopy (CLSM, FESEM) revealed near-spherical droplets with reduced porosity. During simulated digestion, XG-stabilized emulsions provided concentration-dependent control over droplet behavior, αM bioaccessibility, and antioxidant retention, attributed to increased aqueous-phase viscosity and steric hindrance. These findings establish xanthan gum-stabilized cocoa butter emulsions as a promising vehicle for enhancing the stability and controlled intestinal delivery of hydrophobic bioactives like αM.
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ChemistrySelect
·
2025
·Vol. 10
·期 35
·e01362
·
IF 2
Changshun Lv,Xiangru Feng,Boyuan Jian,Xue Jiang,Tianhui Liu,Leijiao Li,Qingshuang Wang
One of the main challenges in wound healing is bacterial infection, and the emergence of antibiotic resistant superbugs in recent years has exacerbated these concerns. In this study, we developed a chitosan/tannic acid/poloxamer 407/poloxamer 188 thermo-sensitive hydrogel (CTPP). The bioactive compound α-Mangostin (α-M) extracted from mangosteen fruit was incorporated into CTPP (CTPP@α-M). The results indicate that CTPP@α-M can slowly and continuously release α-M within 11.5 h. In addition, CTPP@α-M effectively inhibits bacterial proliferation, accelerates collagen deposition, reduces inflammatory response, and promotes rapid wound healing in the presence of wound infection. The biosafety experiment showed that the hydrogel had excellent biocompatibility. Overall, these findings suggest that CTPP@α-M has the potential to become a potential treatment for repairing infectious wounds. Graphical In this study, CTPP hydrogel and CTPP @ α - M drug carrying hydrogel were prepared by physical crosslinking method. CTPP shows excellent performance and can be converted to semi-solid gel at 37 ° C. CTPP @ α - M showed strong inhibitory effects on MRSA and accelerated wound healing, reducing the expression of pro-inflammatory cytokines. The data show that CTPP @ α - M is a highly effective antibacterial thermosensitive hydrogel with excellent performance.
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JOURNAL OF MEDICINAL CHEMISTRY
·
2020
·
IF 6.205
Jinhao Liang,Yi-You Huang,Qian Zhou,Yuqi Gao,Zhe Li,Deyan Wu,Si Yu,Lei Guo,Zhen Chen,Ling Huang,Steven H. Liang,Xixin He,Ruibo Wu,Hai-Bin Luo
To validate PDE4 inhibitors as novel therapeutic agents against vascular dementia (VaD), 25 derivatives were discovered from the natural inhibitor α-mangostin (IC50 = 1.31 μM). Hit-to-lead optimization identified a novel and selective PDE4 inhibitor 4e (IC50 = 17 nM), which adopted a different binding pattern from PDE4 inhibitors roflumilast and rolipram. Oral administration of 4e at a dose of 10 mg/kg exhibited remarkable therapeutic effects in a VaD model and did not cause emesis to beagle dogs, indicating its potential as a novel anti-VaD agent.
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Drug Design Development and Therapy
·
2022
·
IF 4.319
Wen-Gang Chen,Sa-Sa Zhang,Shu Pan,Zhong-Fang Wang,Jin-Ying Xu,Xue-He Sheng,Qin Yin,Yi-Jin Wu
Background Studies have found that α-mangostin (MG) can relieve experimental arthritis by activating cholinergic anti-inflammatory pathway (CAP). It affects the polarization of macrophages and the balance of related immune cell subpopulations, but the specific mechanism is still unclear. It has been found that silent information regulator 1 (SIRT1) is closely related to macrophage activity. The purpose of this study is to explore the mechanism of MG intervening in macrophage polarization during treatment of early adjuvant-induced (AIA) rats through the CAP-SIRT1 pathway.Methods We investigated the polarization of M1 macrophages and the differentiation of Th1 in AIA rats by flow cytometry. Activity of acetylcholinesterase (AChE) and the level of nicotinic adenine dinucleotide (NAD+) in serum were also detected, and immunohistochemical was used to detect the levels of α7 nicotinic cholinergic receptor (α7nAChR) and SIRT1. Then in macrophages, the molecular mechanism of MG regulating the abnormal activation of macrophages in rats with early AIA through the CAP-SIRT1 pathway was studied.Results MG can significantly inhibit the polarization of M1 macrophages and the differentiation of Th1 in AIA rats in the acute phase of inflammation. MG can significantly inhibit the activity of AChE and increase the level of NAD+, thereby further up-regulated the expression levels of α7nAChR and SIRT1. Meanwhile, MG inhibited nuclear factor-κB (NF-κB)-mediated inflammation by activating the CAP-SIRT1 pathway in macrophages.Conclusion In summary, the stimulation of MG induced CAP activation, which up-regulated SIRT1 signal, and thereby inhibited M1 polarization through the NF-κB pathway, and improved the pathological immune environment of early-stage AIA rats.
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MACROMOLECULAR RESEARCH
·
2025
·
IF 3.4
Lv Changshun,Wang Qingshuang,Li Zhaoxin,Jiang Xue,Liu Tianhui,Xu Xiaoru,Feng Xiangru
Chitosan-based pluronic thermo-sensitive hydrogels represent a class of biomaterials characterized by their favorable biocompatibility and exceptional thermo-sensitive properties. The purpose of this study was to investigate their potential as carriers for embedding α-Mangostin (α-M), a bioactive compound derived from mangosteen peel, with the aim of inhibiting methicillin-resistant Staphylococcus aureus (MRSA). During the synthesis process, chitosan (CS), tannic acid (TA), pluronic F-127 (F127), and pluronic F-68 (F68) were combined to form the thermo-sensitive hydrogel, into which α-M was physically incorporated through crosslinking (designated as CTFF@α-M). We are very interested in the results obtained during the research process. The results of fluorescence imaging in small animals showed that CTFF extended the residence time of α-M in the body from 3 to 9 days, improved the bioavailability of α-M, and achieved the goal of sustained drug release. In vitro antibacterial experiments showed that CTFF@α-M (30 mg/mL) had an inhibition rate of 79.69% against MRSA, which was higher than CTFF@amoxicillin (AM) (5 mg/mL) increased by 71.68%. This study is expected to provide new insights into the integration of biomaterials and natural therapy, and emphasize the therapeutic potential of thermosensitive hydrogels and α-M in antibacterial treatment, especially in the fight against MRSA infection. Graphic In this study, a CTPP hydrogel was prepared using a physical cross-linking method, and α-M was encapsulated to create the CTPP@α-M drug-loaded hydrogel. Various characterization techniques, including SEM, FT-IR, and XRD, were employed to confirm its physicochemical properties. The hydrogel exhibited excellent water solubility, swelling capacity, sustained release characteristics, and biocompatibility, with the ability to transform into a semi-solid gel at 37 °C. In vitro experiments demonstrated that the CTPP@α-M hydrogel showed a powerful inhibitory effect on MRSA, exhibiting strong resistance to antibiotic resistance. Infection experiments using a mouse model confirmed that CTPP@α-M not only accelerated wound healing but also significantly reduced bacterial counts at the wound site. Moreover, the CTPP@α-M group significantly decreased the expression of pro-inflammatory cytokines while increasing the levels of anti-inflammatory factors, indicating its promising anti-inflammatory properties. Collectively, these data suggest that CTPP@α-M is a highly effective antibacterial thermo-sensitive hydrogel with excellent performance.
Diagram of the preparation of protocol CTFF@α-M and the treatment process of bacterial infection wounds
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CHEMICAL ENGINEERING JOURNAL
·
2026
·
IF 12.5
Cunchun Dai,Quanying Li,Guiyu Zhou,Yunjie Liu,Xirui You,Binghu Fang
A novel nanoparticle (WSLM) encapsulating α-mangostin and Lycium barbarum polysaccharide for oral co-delivery. • WSLM effectively eradicates intracellular methicillin-resistant Staphylococcus aureus . • WSLM suppresses pro-inflammatory cytokines to alleviate the inflammatory response. • WSLM combats intestinal infection via integrated antibacterial and anti-inflammatory. Methicillin-resistant Staphylococcus aureus (MRSA) is a globally prevalent pathogen responsible for severe and often refractory gastrointestinal infections. Current therapeutic strategies predicated on bactericidal activity overlook the critical pathological consequence of bacterial lysis, which involves the release of cell components that trigger excessive host inflammatory responses and exacerbate intestinal injury. Inspired by the need for integrated host-pathogen modulation, we developed an oral co-delivery nanoparticle system (WSLM) based on chitosan and whey protein isolate, which encapsulates α-mangostin and Lycium barbarum polysaccharide, to enable coordinated antibacterial and anti-inflammatory intervention within the gastrointestinal tract. WSLM effectively inhibited MRSA biofilm formation and bacterial colonization while significantly attenuating infection-associated inflammation, reducing TNF-α and IL-6 levels by approximately 76.1% and 59.3%, respectively. In a mouse model of MRSA intestinal infection, oral administration of WSLM significantly alleviated intestinal pathology, restored colon length, and decreased bacterial load by approximately three orders of magnitude. Mechanistically, WSLM promoted epithelial barrier repair through the upregulation of tight junction proteins. Furthermore, microbiome analysis revealed that WSLM showed enrichment of beneficial commensal families, including Lachnospiraceae and Oscillospiraceae . Overall, this study has established a multifunctional nano-delivery system targeting bacterial infection and hyperinflammation simultaneously, providing an experimental paradigm for the treatment of bacterial intestinal infections. Download: Download high-res image (119KB) Download: Download full-size image
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Yuanbiao Ma,Xu Liu,Zhewen Deng,Jiaqi Li,Ruoxi Liu,Shanshan Li,Can Zhang,Yutong Chen,Senqiang Zhu,Qi Zhang,Rui Liu,Bo Ma
CMCSMA/F127/TPGS@α-MG hydrogel promotes infected diabetic wound healing. • F127/TPGS micelles improve the aqueous solubility and sustained release of α-MG. • The composite hydrogel disrupts biofilms and achieves 99.6% wound closure. • α-MG modulates PPAR-γ, attenuating inflammation and promoting angiogenesis. Diabetic wounds pose a major clinical challenge owing to their complex microenvironment and persistent inflammation. To address this issue, we engineered a multifunctional, in situ photocrosslinkable composite hydrogel (CMCSMA/F127/TPGS@α-MG) to promote wound healing. To overcome the hydrophobicity of the antimicrobial agent α-mangostin (α-MG), it was first encapsulated in F127/TPGS nanomicelles. These micelles were then integrated into a methacrylated carboxymethyl chitosan (CMCSMA) matrix, enabling rapid conformal gelation upon 405 nm light irradiation. The resulting hydrogel exhibited a biphasic sustained-release profile, excellent biocompatibility, and potent contact-killing and anti-biofilm activities against Staphylococcus aureus ( S. aureus ). In an S. aureus -infected diabetic wound model, the hydrogel significantly accelerated wound closure, achieving 99.6% closure by day 14, and facilitated high-quality tissue regeneration characterized by complete re-epithelialization and orderly collagen deposition. Furthermore, an integrated approach combining network pharmacology, molecular docking, molecular dynamics simulations, and experimental validation revealed that the therapeutic efficacy of sustained local α-MG delivery involves the modulation of the PPAR-γ pathway. This regulatory process suppresses the NF-κB/COX-2 inflammatory axis and upregulates pro-angiogenic markers, including VEGF, CD31, and α-SMA. Collectively, this dual-action platform, which synergizes physical barrier protection with targeted molecular modulation, represents a promising translational strategy for refractory diabetic wounds. Schematic illustration of the preparation process and functional attributes of the in situ forming CMCSMA/F127/TPGS@α-MG hydrogel. Download: Download high-res image (67KB) Download: Download full-size image
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