Physicochemical and digestive properties of corn starch nanoparticles incorporated different polyphenols.

The corn starch nanoparticles were prepared by incorporating three kinds of polyphenols, including quercetin, proanthocyanidins and tannin acid. The physicochemical and digestive properties of corn starch nanoparticles were researched. The quercetin showed a higher complexation index than proanthocyanidins and tannin acid when they complexed with corn starch. The mean size of corn starch quercetin, proanthocyanidins and tannin acid were 168.5 nm, 179.1 nm and 188.6 nm, respectively. XRD results indicated that all the corn starch-polyphenols complex showed V-type crystalline structure, the crystallinity of corn starch-quercetin complex was 19.31 %, which showed more formation of amylose-quercetin single helical formed than the other two starch-polyphenol complexes. In vitro digestion revealed that polyphenols could resist digestion and quercetin increased the content of resistant starch from 23.32 % to 35.24 % and polyphenols can form complexes with starch through hydrophobic interactions or hydrogen bonding. This study indicated the hydrophobic polyphenols had a more significant effect on the digestibility of corn starch. And the cell toxicity assessments demonstrated that all nanoparticles were nontoxic and biocompatible.

Recent advances in dietary androgen receptor inhibitors.

As a nuclear transcription factor, the androgen receptor (AR) plays a crucial role not only in normal male sexual differentiation and growth of the prostate, but also in benign prostatic hyperplasia, prostatitis, and prostate cancer. Multiple population-based epidemiological studies demonstrated that prostate cancer risk was inversely associated with increased dietary intakes of green tea, soy products, tomato, and so forth. Therefore, this review aimed to summarize the structure and function of AR, and further illustrate the structural basis for antagonistic mechanisms of the currently clinically available antiandrogens. Due to the limitations of these antiandrogens, a series of natural AR inhibitors have been identified from edible plants such as fruits and vegetables, as well as folk medicines, health foods, and nutritional supplements. Hence, this review mainly focused on recent experimental, epidemiological, and clinical studies about natural AR inhibitors, particularly the association between dietary intake of natural antiandrogens and reduced risk of prostatic diseases. Since natural products offer multiple advantages over synthetic antiandrogens, this review may provide a comprehensive and updated overview of dietary-derived AR inhibitors, as well as their potential for the nutritional intervention against prostatic disorders.

Hydroxyl group-induced enhancement of antioxidant activity of resveratrol over pterostilbene by binding to lactoferrin.

The reduced antioxidant capacity of trans-resveratrol (Res) than the second generation of Res, namely pterostilbene (Pte), severely prohibits its in-depth intriguing radical-scavenging applications in food formulations. Herein, a unique chemical structure-dependent strategy was proposed to specifically enhance the radical scavenging activity of Res over Pte, relying on the two more hydroxyl groups on the A-benzene ring of Res, thus facilitating its binding with lactoferrin (LF) to form stable complexes through more hydrogen bonds. We prepared LF-Res and LF-Pte complexes, revealed their binding mechanisms by multispectral analysis and molecular docking/dynamics simulations, further evaluated their antioxidant properties via ABTS and DPPH assays and a model of inhibiting apple browning, eventually elucidated their structure-binding-property relationships. This contribution offers a new approach to restore the antioxidant capability of Res, also paves the way to precisely regulate the fascinating bioactivities of hydrophobic compounds by protein-binding in a chemical structure-, especially hydroxyl group-dependent manner.

Comparison of interactions between alpha-lactalbumin and three protopanaxadiol ginsenosides: Impacts on the structure and antitumor properties.

In this research, interactions between α-lactalbumin (ALA) and three protopanaxadiol ginsenosides [20(S)-Rg3, 20(S)-Rh2, and 20(S)-PPD] were compared to explore the effects of similar ligand on structure and cytotoxicity of ALA. Multi-spectroscopy revealed the binding between ALA and ginsenoside changed the conformation of ALA, which related to different structures and solubility of ligands. Scanning electron microscope illustrated that all ALA-ginsenoside complexes exhibited denser structures via hydrophobic interactions. Additionally, the cytotoxic experiments confirmed that the cytotoxicity of ginsenoside was enhanced after binding with ALA. Molecular docking showed all three ginsenosides were bound to the sulcus depression region of ALA via hydrogen bonding and hydrophobic interaction. Furthermore, molecular dynamics simulation elucidated the precise binding sites and pertinent system properties. Among all three composite systems, 20(S)-Rh2 had optimal binding affinity. These findings enhanced understanding of the synergistic utilization of ALA and ginsenosides as functional ingredients in food, medicine, and cosmetics.

Nuclear Receptors-Mediated Endocrine Disrupting Effects of Non-Phthalate Plasticizers: A Review.

In 2021, the global market for non-phthalate plasticizers reached $3.1 billion, and it is projected to grow by 25.8% by 2025. These plasticizers have gained substantial attention as substitutes for phthalates in various industrial applications due to their potential health and environmental risks, particularly in agroecosystems where they have emerged as contaminants. Furthermore, recent studies have demonstrated that non-phthalate plasticizers can exert endocrine-disrupting effects through mechanisms mediated by nuclear receptors. This review aims to summarize the present understanding of the molecular mechanisms by which non-phthalate plasticizers modulate the activity of nuclear receptors, including estrogen receptor, androgen receptor, glucocorticoid receptor, and peroxisome proliferator-activated receptors. Furthermore, the potential health impacts of exposure to conventional phthalate plasticizers are discussed, with a particular emphasis on developmental and reproductive toxicity, metabolic disorders, and carcinogenesis. Overall, this review underscores the significance of evaluating the endocrine-disrupting effects of non-phthalate plasticizers and lays the foundation for the development of safer alternatives within the plastic industry.

In vitro and in silico assessment of endocrine disrupting effects of food contaminants through pregnane X receptor.

As a promiscuous xenobiotic receptor, pregnane X receptor (PXR) has been confirmed to participate in numerous physiological process. In addition to the conventional estrogen/androgen receptor, PXR also serves as an alternative target for environmental chemical contaminants. In this work, the PXR-mediated endocrine disrupting effects of typical food contaminants were explored. Firstly, the time-resolved fluorescence resonance energy transfer assays confirmed the PXR binding affinities of 2,2',4,4',5,5'-hexachlorobiphenyl, bis(2-ethylhexyl) phthalate, dibutyl phthalate, chlorpyrifos, bisphenol A, and zearalenone, with IC50 values ranging from 1.88 to 4284.00 nM. Then their PXR agonist activities were assessed by PXR-mediated CYP3A4 reporter gene assays. Subsequently, the regulation of gene expressions of PXR and its targets CYP3A4, UGT1A1, and MDR1 by these compounds was further investigated. Intriguingly, all the tested compounds interfered with these gene expressions, confirming their endocrine disrupting effects via PXR-mediated signaling. The compound-PXR-LBD binding interactions were explored by molecular docking and molecular dynamics simulations to unravel the structural basis of their PXR binding capacities. The weak intermolecular interactions are key players in stabilizing these compound-PXR-LBD complexes. During the simulation process, 2,2',4,4',5,5'-hexachlorobiphenyl remained stable while the other 5 compounds underwent relatively severe disturbances. In conclusion, these food contaminants might exhibit endocrine disrupting effects via PXR.

Lycopene-loaded emulsions stabilized by whey protein covalently modified with pectin or/and chlorogenic acid: Enhanced physicochemical stability and reduced bio-accessibility.

Lycopene-loaded emulsions were formulated with whey protein isolate (WPI) covalently modified with high methoxylated pectin (HMP) or/and chlorogenic acid (CA) prepared by dry heating or/and alkali grafting. Covalent WPI products were confirmed by SDS-PAGE and degree of graft/CA binding equivalent values. The α-helix and ß-sheet percentage, surface hydrophobicity and fluorescence intensity of WPI decreased significantly (p < 0.05) upon binding. Both binary and ternary complexes enhanced the stability of the emulsions, and lycopene retained more after UV irradiation, thermal treatment, storage, compared with emulsions stabilized by WPI, with the best protection by both ternary complexes. In vitro simulated digestion results showed that free fatty acids were released in the order of WPI > WPI-HMP > WPI-CA > WPI-HMP-CA ≈ WPI-CA-HMP. Bio-accessibility analysis showed the same trend as the fatty acid release rate. These results may provide a theoretical basis for applications of conjugating protein with polysaccharide or/and polyphenol emulsions.

Pea protein based nanocarriers for lipophilic polyphenols: Spectroscopic analysis, characterization, chemical stability, antioxidant and molecular docking.

The current research aims to construct and assess pea protein isolate (PPI) nanocarriers for lipophilic polyphenols of curcumin (CUR), quercetin (QUE) and resveratrol (RES), respectively. Fluorescence analysis demonstrated that the binding affinity declined in sequence of QUE > CUR > RES and about one polyphenol compound was bound to protein. Thermodynamic parameters revealed that hydrophobic interaction was mainly responsible for complexation between CUR/RES and PPI, while hydrogen bonding for QUE with PPI. All nanoparticles showed particle size of 154-159 nm. Three lipophilic polyphenols were successfully encapsulated into PPI, with loading capacity of RES > QUE > CUR. Complexation of three polyphenols did not change the secondary structure of PPI. Results of FTIR, DSC and XRD confirmed that polyphenols changed from crystalline to amorphous state after combination with PPI. SEM pictures exhibited regular spherical microstructure of nanocomplexes. PPI shielded polyphenols from sensitive environment of ultraviolet light and thermal treatment. ABTS and DPPH radical scavenging activity of polyphenols were considerably improved through complexation with PPI. Molecular docking studies showed binding energy with 11S legumin in sequence of QUE > RES > CUR, and stronger hydrogen bonds were built between QUE and the protein than the other two polyphenols. Data in the present work may provide helpful information for encapsulation of lipophilic polyphenols with pea protein and the potential application in food science, pharmaceutical and cosmetics industries in the future.

Polysaccharides from Hericium erinaceus Fruiting Bodies: Structural Characterization, Immunomodulatory Activity and Mechanism.

Five fractions from crude Hericium erinaceus polysaccharides (HEPs), including HEP-1, HEP-2, HEP-3, HEP-4 and HEP-5, were obtained through column chromatography with a DEAE Cellulose-52 column and Sephadex G-100 column. The contents of total carbohydrates and uronic acid in HEPs were 53.36% and 32.56%, respectively. HEPs were mainly composed of Fuc, Gal and Glu in a molar ratio of 7.9:68.4:23.7. Its chemical structure was characterized by sugar and methylation analysis, along with 1H and 13C NMR spectroscopy. HEP-1 contains the backbone composed of (1→6)-linked-galactose with branches attached to O-2 of some glucose. The immunological activity assay indicated that HEP-1 significantly promoted the production of nitric oxide, interleukin-6, interleukin-10, interferon-γ and tumor necrosis factor-α and the phosphorylation of signaling molecules. Collectively, these results suggested that HEP-1 could improve immunity via NF-κB, MAPK and PI3K/Akt pathways. Hericium erinaceus polysaccharides might be explored as an immunomodulatory agent for use in dietary supplements.

Selenium nanoparticles: Enhanced nutrition and beyond.

Selenium is a trace nutrient that has both nutritional and nutraceutical functions, whereas narrow nutritional range of selenium intake limits its use. Selenium nanoparticles (SeNPs) are less toxic and more bioavailable than traditional forms of selenium, suggesting that SeNPs have the potential to replace traditional selenium in food industries and/or biomedical fields. From the perspective of how SeNPs can be applied in health area, this review comprehensively discusses SeNPs in terms of its preparation, nutritional aspect, detoxification effect of heavy metals, nutraceutical functions and anti-pathogenic microorganism effects. By physical, chemical, or biological methods, inorganic selenium can be transformed into SeNPs which have increased stability and bioavailability as well as low toxicity. SeNPs are more effective than traditional selenium form in synthesizing selenoproteins like glutathione peroxidases. SeNPs can reshape the digestive system to facilitate digestion and absorption of nutrients. SeNPs have shown excellent potential to adjunctively treat cancer patients, enhance immune system, control diabetes, and prevent rheumatoid arthritis. Additionally, SeNPs have good microbial anti-pathogenic effects and can be used with other antimicrobial agents to fight against pathogenic bacteria, fungi, or viruses. Development of novel SeNPs with enhanced functions can greatly benefit the food-, nutraceutical-, and biomedical industries.

Complexation mechanism between 20(R, S)-ginsenoside Rh1 and serum albumin: Multi-spectroscopy, in vitro cytotoxicity, and in silico investigations.

As rare ginsenosides, 20(R, S)-ginsenoside Rh1 [20(R, S)-Rh1] are isomers and have been reported to exhibit multiple biological effects. However, the application of 20(R, S)-Rh1 is still limited due to their poor solubilities and low bioavailabilities. Here, the complexation mechanism between 20(R, S)-Rh1 and serum albumin (SA) was explored by a combination of multi-spectroscopy and in silico investigations. Results of spectra experiments showed that 20(R, S)-Rh1 could form complexes with bovine serum albumin (BSA) and quench its intrinsic fluorescence. In addition, the influence of BSA on the anti-cancer activity of 20(R, S)-Rh1 was also evaluated in A549 cells. The result of the MTT assay indicated that anti-cancer activity of 20(R, S)-Rh1 was enhanced when combined with BSA. The results of molecular docking and dynamics simulation demonstrated that the subtle structural differences of 20(R, S)-Rh1 at the 20-carbon atom may be responsible for their different binding capacities and binding stabilities with human serum albumin. The cytotoxicity assay for 20(R, S)-Rh1 alone and their complexes with BSA demonstrated the enhancement effect of BSA for inhibition of cell proliferation. In conclusion, this work provided insight into the complexation mechanism between 20(R, S)-Rh1 and SA. PRACTICAL APPLICATION: The complexation mechanism between 20(R, S)-ginsenoside Rh1 [20(R, S)-Rh1] and serum albumin (SA) was explored by a combination of multi-spectroscopy and in silico investigations in this work. The cytotoxicity assay for 20(R, S)-Rh1 alone and their complexes with bovine serum albumin (BSA) demonstrates the enhancement effect of BSA for inhibition of cell proliferation. Hence, this work provided insight into the complexation mechanism between 20(R, S)-Rh1 and SA.

Identification of 20(S)-Ginsenoside Rh2 as a Potential EGFR Tyrosine Kinase Inhibitor.

As the main active ingredients of Panax ginseng, ginsenosides possess numerous bioactivities. Epidermal growth factor receptor (EGFR) was widely used as a valid target in anticancer therapy. Herein, the EGFR targeting activities of 20(S)-ginsenoside Rh2 (20(S)-Rh2) and the relationship of their structure-activity were investigated. Homogeneous time-resolved fluorescence assay showed that 20(S)-Rh2 significantly inhibited the activity against EGFR kinase. 20(S)-Rh2 was confirmed to effectively inhibited cell proliferation in a dose-dependent manner by MTT assay. Furthermore, quantitative real-time PCR and western blotting analysis revealed that 20(S)-Rh2 inhibited A549 cells growth via the EGFR-MAPK pathway. Meanwhile, 20(S)-Rh2 could promote cell apoptosis, block cell cycle, and reduce cell migration of A549 cells, respectively. In silico, the result suggested that both hydrophobic interactions and hydrogen-bonding interactions could contribute to stabilize their binding. Molecular dynamics simulation showed that the side chain sugar moiety of 20(S)-Rh2 was too flexible to be fixed at the active site of EGFR. Collectively, these findings suggested that 20(S)-Rh2 might serve as a potential EGFR tyrosine kinase inhibitor.

Formation and characterization of noncovalent ternary complexes based on whey protein concentrate, high methoxyl pectin, and phenolic acid.

Protein-polysaccharide-polyphenol noncovalent ternary complexes possess unique physicochemical, structural, and functional properties. In the present study, ternary complexes based on whey protein concentrate (WPC; 2%, wt/vol) and high methoxyl pectin (HMP; 0.5%, wt/vol) complexes and 0.2 to 0.6% (wt/vol) chlorogenic acid (CA) or rosmarinic acid (RA) were formed and characterized at 3 pH values (4, 4.5, and 5). The pH conditions were decided according to phase diagram of WPC and HMP during acidification. Fluorescence quenching experiments indicated that WPC-HMP complexes bound RA stronger than CA and the binding constant increased with increasing pH for both phenolic acids. Particle size of ternary complexes decreased and absolute ζ-potential increased with pH values changing from 4 to 5, and RA influenced the particle size of WPC-HMP complexes greater than CA. The CA and RA in ternary complexes showed good stability against UV light with pH order of pH 5 > pH 4.5 > pH 4. Fourier-transform infrared spectroscopy spectra indicated the involvement of hydrogen bonding between WPC-HMP and CA or RA. Antibacterial tests showed that ternary complexes had good antibacterial activity against Staphylococcus aureus and Escherichia coli at concentrations of 6.2 mg/mL and the ability increased with decreasing pH values. All ternary complexes possessed strong scavenging radical capacities with median inhibitory concentration (IC50) values ranging from 2.71 ± 0.05 to 6.20 ± 0.41 µg/mL. Antioxidative ability of ternary complexes increased as pH went up and WPC-HMP-RA showed significantly higher antioxidative property compared with WPC-HMP-CA. Data may provide useful information for rational design of ternary complexes and applications of the formed complexes in food matrices such as beverages and emulsions.

Complexation of ellagic acid with α-lactalbumin and its antioxidant property.

Ellagic acid possesses numerous bioactivities such as antioxidant activity and anti-inflammatory effect. In this work, the binding interaction between ellagic acid and α-lactalbumin was investigated by multi-spectroscopy and the results suggested that ellagic acid could change the conformation of α-lactalbumin. Chromatographic analysis proved the interaction of α-lactalbumin with ellagic acid taken place in less than 30 min and this interaction was stable. Computer simulations showed that both aromatic clusters Ⅰ and Ⅱ of α-lactalbumin were active sites for ellagic acid. Interestingly, both the results of molecular docking and molecular dynamics simulations suggested that ellagic acid tended to bind to aromatic cluster Ⅱ rather than aromatic cluster Ⅰ. Moreover, α-lactalbumin could enhance the antioxidant property of ellagic acid, indicating that the solubility of ellagic acid might be improved by combining α-lactalbumin. Overall, this work suggested that α-lactalbumin exhibited binding affinity for ellagic acid and enhanced its antioxidant property.

In vitro and in silico evaluation of EGFR targeting activities of curcumin and its derivatives.

As polyphenols from Curcuma longa, curcumin and its derivatives possess numerous bioactivities. Herein, the epidermal growth factor receptor (EGFR) targeting activities of curcumin and its derivatives, as well as their structure-activity relationship were investigated. All of the tested compounds exhibited significant inhibition activities against EGFR kinase in homogeneous time-resolved fluorescence assay. Then their antiproliferative activities against Caco-2 were confirmed. The expressions of EGFR and phospho-EGFR proteins were regulated by curcumin and its derivatives. The 3,5-dione and methoxyl groups exerted significant influence on their electrostatic interactions with EGFR. Both hydrogen bonds and hydrophobic contacts were crucial for their binding with EGFR. Interestingly, their EGFR targeting activities were structure-dependent. The binding stabilities of curcumin and its derivatives were different from each other due to their structural diversity. This work indicated that curcumin and its derivatives were potential tyrosine kinase inhibitors that target EGFR.

Preparation and Characterization of Ginger Essential Oil Microcapsule Composite Films.

New food packaging has shown research significance in the face of increasing demand for high-quality foods and growing attention paid to food safety. In this study, ginger essential oil microcapsule composite films were prepared by combining microcapsules prepared by a complex coacervation method with gelatin films, and the mechanical properties and active functions of the composite films were analyzed. Fourier-transform infrared spectroscopy and differential scanning calorimetry confirmed the successful encapsulation of ginger essential oil. The scanning electron microscopy of the composite films showed the microcapsules and gelatin film matrix were highly compatible. During the entire storage period, the antioxidant capacity of the ginger essential oil microcapsule films weakened more slowly than ginger essential oil microcapsules and could be maintained at a relatively high level for a long time. The microcapsule films had excellent inhibitory effects on Escherichia coli, Staphylococcus aureus, and Bacillus subtilis. Therefore, the direct addition of microcapsules to a film matrix can broaden the application range of microcapsules and increase the duration of the release of active ingredients. Ginger essential oil microcapsule films are potential biodegradable food packaging films with long-lasting activity.

Anti-inflammatory action of betulin and its potential as a dissociated glucocorticoid receptor modulator.

Although the medical application of betulin has been presented in previous studies, the potential mechanism of the anti-inflammatory action of betulin should be further investigated. This work aims to confirm the hypothesis that betulin has dexamethasone-like anti-inflammatory action through glucocorticoid receptor (GR)-mediated pathway. Firstly, the binding ability of betulin with GR was measured by a fluorescence polarization-based competitive binding assay, with the IC50 value of 79.18 ± 0.30 mM. Betulin could bind to GR and then induced GR nuclear translocation, but lacked GR transcriptional activity in HeLa cells. Hence, betulin exhibited the potential to be a dissociated modulator for GR, with the loss of glucocorticoid response element (GRE)-associated side effects. In addition, betulin downregulated GRE-driven protein expression of G6P involved in gluconeogenesis, namely side effect. The results of pro-inflammatory cytokines analysis showed that betulin exerted anti-inflammatory action in vitro. Both of the hydrophobic and hydrogen-bonding interactions stabilized the binding between betulin and GR during the simulation process. In conclusion, betulin might be a potential dissociated GR modulator with a reduced side effect profile yet keeping its anti-inflammatory action.

A review on pharmacological activities and synergistic effect of quercetin with small molecule agents.

BACKGROUND: Quercetin is a natural flavonoid, which widely exists in nature, such as tea, coffee, apples, and onions. Numerous studies have showed that quercetin has multiple biological activities such as anti-oxidation, anti-inflammatory, and anti-aging. Hence, quercetin has a significant therapeutic effect on cancers, obesity, diabetes, and other diseases. In the past decades, a large number of studies have shown that quercetin combined with other agents can significantly improve the overall therapeutic effect, compared to single use. PURPOSE: This work reviews the pharmacological activities of quercetin and its derivatives. In addition, this work also summarizes both in vivo and in vitro experimental evidence for the synergistic effect of quercetin against cancers and metabolic diseases. METHODS: An extensive systematic search for pharmacological activities and synergistic effect of quercetin was performed considering all the relevant literatures published until August 2021 through the databases including NCBI PubMed, Scopus, Web of Science, and Google Scholar. The relevant literatures were extracted from the databases with following keyword combinations: "pharmacological activities" OR "biological activities" OR "synergistic effect" OR "combined" OR "combination" AND "quercetin" as well as free-text words. RESULTS: Quercetin and its derivatives possess multiple pharmacological activities including anti-cancer, anti-oxidant, anti-inflammatory, anti-cardiovascular, anti-aging, and neuroprotective activities. In addition, the synergistic effect of quercetin with small molecule agents against cancers and metabolic diseases has also been confirmed. CONCLUSION: Quercetin cooperates with agents to improve the therapeutic effect by regulating signal molecules and blocking cell cycle. Synergistic therapy can reduce the dose of agents and avoid the possible toxic and side effects in the treatment process. Although quercetin treatment has some potential side effects, it is safe under the expected use conditions. Hence, quercetin has application value and potential strength as a clinical drug. Furthermore, quercetin, as the main effective therapeutic ingredient in traditional Chinese medicine, may effectively treat and prevent coronavirus disease 2019 (COVID-19).

In vitro and in silico investigations of endocrine disruption induced by metabolites of plasticizers through glucocorticoid receptor.

The endocrine disruptive capability of plasticizers to activate nuclear receptors has attracted great interest. This study is aimed to assess the potential glucocorticoid effects of metabolites of plasticizers. The effects of metabolites of plasticizers on the transcriptional activity of glucocorticoid receptor (GR) were investigated using reporter gene assays. All of them failed to exhibit agonistic/antagonistic effects on GR. However, a combination of dexamethasone and monobutyl phthalate (MBP) could synergistically activate GR. MBP combined with dexamethasone also enhanced GR nuclear translocation by Western blot, while mifepristone restrained GR cytoplasmic-to-nuclear translocation. MBP co-treated with dexamethasone resulted in synergistic induction of PEPCK and MKP-1 gene expression by real-time PCR and PEPCK protein level by Western blot. Furthermore, the carboxyl and ester groups of MBP have influences on the charge distribution of MBP, leading to change of electrostatic interactions between MBP and GR by calculations on electronic properties. Both hydrophobic and hydrogen bonding interactions play a crucial role in the stabilization between MBP and GR conducted by molecular docking and dynamics simulation. This work confirms that GR could remain stable upon binding to MBP. In conclusion, dexamethasone and MBP could synergistically activate GR, resulting in synergetic enhancement of subsequent GR-mediated endocrine disrupting effect.

GR-mediated anti-inflammation of α-boswellic acid: Insights from in vitro and in silico studies.

Although multiple bioactivities of α-boswellic acid have been reported, the molecular mechanism of its anti-inflammatory action is not yet clear. Hence, glucocorticoid receptor (GR)-mediated anti-inflammation of α-boswellic acid was investigated in this work. Fluorescence polarization assay suggested that α-boswellic acid bound to GR with IC50 value of 658.00 ± 0.21 µM. Upon binding to α-boswellic acid, GR translocated from cytoplasm into nucleus of HeLa cells, facilitating sequential transcriptional regulation of GR-related genes. Luciferase reporter assay suggested that α-boswellic acid lacked GR transcriptional activity, indicating its potential as a dissociative GR ligand. Interestingly, α-boswellic acid selectively modulated the anti-inflammatory gene CBG (marker for GR transrepression), while leaving the "side-effect" gene TAT (marker for GR transactivation) unaffected in HepG2 cells. Furthermore, α-boswellic acid inhibited lipopolysaccharide-stimulated cytokines production in U937 macrophages, confirming its anti-inflammation property in vitro. Molecular docking showed that both hydrogen-bonding and hydrophobic interactions helped to stabilize α-boswellic acid-GR binding. Their binding stability was further confirmed in a 70-ns dynamics simulation. In summary, α-boswellic acid could bind to and translocate GR but did not induce glucocorticoid response element-mediated transcription. Since α-boswellic acid showed the dissociated characteristic that separated transrepression from transactivation, it might be a selective GR modulator against inflammatory disorders.