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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

An exploration of the interaction, structural characterization and anti-oxidative properties of proanthocyanidin and beta-lactoglobulin complex

Cuicui Duan,Mengchun Qin,Lifan Liu,Yixue Sun,Lin Cai,Lin Ma,Xiaolei Li,Fumin Ma,Dan Li

Proanthocyanidin (PC) is with antioxidant, anticancer and neuroprotective effects. Cow’s milk beta-lactoglobulin (β-Lg) is reported with higher immunoregulatory activity but lower antioxidative function. In this study, a β-Lg-PC complex was prepared, and the interaction and structural characterization of β-Lg-PC complex were investigated by fluorescence spectral analysis, infrared spectroscopy and molecular docking, etc. PC quenched the intrinsic fluorescence and changed the conformation of β-Lg. The optimal ratio of β-Lg and PC (10:3, w/w) was determined by measuring the particle size and ζ potential. Molecular docking results implied that the covalent binding among complex was mainly concentrated on the binding of PC to amino acid residue ILE 71. Moreover, the antioxidant effects and mechanism of β-Lg-PC complex were explored using LPS-induced oxidative stress model of RAW264.7 cells. The results showed that β-Lg-PC could alleviate oxidative stress by slowing down the LPS-induced decline in SOD enzyme activity, increase in ROS level, loss of mitochondrial membrane potential and increase in apoptosis in RAW264.7 cells.

CAS / MDL: 9045-23-2 35065-28-2
研究领域: 食品科学 · 生物化学 · 免疫学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Structural characterization of an apple polysaccharide and its anti-inflammatory effect through suppressing TLR4/NF-κB signaling

Shanbo Ma,Rui Zhang,Long Li,Jin Wang,Meiling Zheng,Xiaodi Guo,Shan Miao,Wei Quan,Wenjuan Liu,Xiaopeng Shi

The current study isolated a homogeneous polysaccharide (AP) with a molecular weight of 7.9 kDa from the pomace of Fuji apples. AP was found to consists of rhamnose, galactose, arabinose, glucose, and galacturonic acid in a ratio of 4.3:5.2:2.6:1.0:11.9. Ten sugar residues in AP, including T-Ara f , 1,5-Ara f , 1,2-Rha p , 1,3-Rha p , T-Gal p , 1,3,5-Ara f, 1,4-Gal p , 1,4-Gal p A, 1,6-Glc p , and 1,3,6-Glc p were identified using methylation and GC–MS. Combined with 1D and 2D NMR, it was further revealed that AP possesses a backbone of α-Gal p- (1 → [3)-α-Rha p -(1 → 2)-α-Rha p -(1] 2  → [4)-α-Gal p A-(1] 10  → 3,6)-β-Glc p -(1 → 6)-β-Glc p -(1 → 4)-β-Gal p -(1 → 4)-β-Gal p -(1→, with two branches: α-Ara f -(1 → 5)-α-Ara f -(1 → 5)-α-Ara f -(1 → 3,5)-α-Ara f -(1 → 6)-β-Glc p -(1→ and →3)-α-Rha p -(1 → 5)-α-Ara f -(1 → 3,6)-β-Glc p -(1→ bonded to the C-3 of β-1,3,6-Glc p . AP significantly inhibited the release of cytokines and inflammatory mediators, such as TNF-α, IL-1β, IL-6, reactive oxygen species (ROS) and nitric oxide (NO). Western blotting results indicated that AP treatment markedly downregulated iNOS and NF-κB protein expression in LPS-induced RAW264.7 cells, leading to decreased levels of phosphorylated proteins (p-NF-κB and p-ΙκΒα) and preventing the degradation of ΙκΒα. Furthermore, in LPS-induced RAW264.7 macrophages, AP inhibited the expression of TLR4 protein, which in turn inhibited the activity of the NF-κB pathway. The findings demonstrated that AP exhibits anti-inflammatory properties in vitro by targeting the TLR4/NF-κB signaling pathway, thus impeding the nuclear translocation of NF-κBp65, suppressing the expression of related pro-inflammatory factors.

CAS / MDL: 329-98-6
研究领域: 食品科学 · 免疫学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BMC GASTROENTEROLOGY · 2023 ·Vol. 23 ·期 1 ·1-10 · IF 2.4

Protective role of circRNA CCND1 in ulcerative colitis via miR-142-5p/NCOA3 axis

Xiang Ping,Ge Tingrui,Zhou Jingyi,Zhang Yonggang

Background Increasing research indicates that circular RNAs (circRNAs) play critical roles in the development of ulcerative colitis (UC). This study aimed to determine the role of circRNA CCND1 in UC bio-progression, which has been shown to be downregulated in UC tissues. Methods Reverse transcription quantitative polymerase chain reaction was used to determine the levels of circRNA CCND1 , miR-142-5p, and nuclear receptor coactivator-3 ( NCOA3 ) in UC tissues and in lipopolysaccharide (LPS)-induced Caco-2 cells. Target sites of circRNA CCND1 and miR-142-5p were predicted using StarBase, and TargetScan to forecast potential linkage points of NCOA3 and miR-142-5p, which were confirmed by a double luciferase reporter-gene assay. Cell Counting Kit 8 and flow cytometry assays were performed to assess Caco-2 cell viability and apoptosis. TNF-α, IL-1β, IL-6, and IL-8 were detected using Enzyme-Linked Immunosorbent Assay kits. Results CircRNA CCND1 was downregulated in UC clinical samples and LPS-induced Caco-2 cells. In addition, circRNA CCND1 overexpression suppressed LPS-induced apoptosis and inflammatory responses in Caco-2 cells. Dual-luciferase reporter-gene assays showed that miR-142-5p could be linked to circRNA CCND1 . Moreover, miR-142-5p was found to be highly expressed in UC, and its silencing inhibited LPS-stimulated Caco-2 cell apoptosis and inflammatory responses. Importantly, NCOA3 was found downstream of miR-142-5p. Overexpression of miR-142-5p reversed the inhibitory effect of circRNA CCND1 -plasmid on LPS-stimulated Caco-2 cells, and the effects of miR-142-5p inhibitor were reversed by si- NCOA3 . Conclusion CircRNA CCND1 is involved in UC development by dampening miR-142-5p function, and may represent a novel approach for treating UC patients.

研究领域: 分子生物学 · 胃肠病学 · 免疫学 · 细胞生物学
✓ 已验证 DOI PubMed 高影响因子
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BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY · 2024 · IF 1.4

PDZK1 gene transfer ameliorates lipopolysaccharide-induced cholestasis in rats by rescuing hepatic ABC transporters

Wu Tao,Wu Ji,Liu Li,Song Hongping

Lipopolysaccharide (LPS) causes inflammatory cholestasis in sepsis. We investigated the role of PDZK1 in the repression of ABC transporters in LPS-induced cholestasis. Lentiviral gene transfer of PDZK1 to rats was conducted to explore its influence on cholestasis induced by LPS. And the effect of lentivirus-mediated shRNA targeting PDZK1 on ABC transporters in rat liver BRL-3A cells was evaluated. Lentiviral vector encoding rat PDZK1 was administered to rats by tail intravenous injection. Obviously elevated serum total bile acid (TBA) level and liver biochemical markers in cholestatic rats were decreased by the Lv-PDZK1 delivery. Also Lv-PDZK1 delivery stimulated the suppressed hepatic ABC transporters expression. In vitro, after the lentiviral vector LV3/PDZK1 shRNA transfection, no expression of PDZK1 and mild expression of ABC transporters were detected in BRL-3A cells by Western blotting. Our results indicate that the lentiviral-mediated hepatocyte PDZK1 expression ameliorates LPS-induced cholestasis in rats by rescuing hepatic ABC transporters expression.

CAS / MDL: L118716 93572-42-0
研究领域: 分子生物学 · 肝病学 · 基因治疗
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BRITISH JOURNAL OF PHARMACOLOGY · 2017 ·Vol. 175 ·期 5 ·840-854 · IF 5.491

Shikonin inhibits myeloid differentiation protein 2 to prevent LPS-induced acute lung injury

Yali Zhang,Tingting Xu,Zheer Pan,Xiangting Ge,Chuchu Sun,Chun Lu,Hongjin Chen,Zhongxiang Xiao,Bing Zhang,Yuanrong Dai,Guang Liang

Background and Purpose Acute lung injury (ALI) is a challenging clinical syndrome, which manifests as an acute inflammatory response. Myeloid differentiation protein 2 (MD2) has an important role in mediating LPS-induced inflammation. Currently, there are no effective molecular-based therapies for ALI or viable biomarkers for predicting the severity of disease. Recent preclinical studies have shown that shikonin, a natural naphthoquinone, prevents LPS-induced inflammation. However, little is known about the underlying mechanisms. Experimental Approach The binding affinity of shikonin to MD2 was analysed using computer docking, surface plasmon resonance analysis and elisa . In vitro , the anti-inflammatory effect and mechanism of shikonin were investigated through elisa , real-time quantitative reverse transcription PCR, Western blotting and immunoprecipitation assay. In vivo , lung injury was induced by intratracheal administration of LPS and assessed by changes in the histopathological and inflammatory markers. The underlying mechanisms were investigated by immunoprecipitation in lung tissue. Key Results Shikonin directly bound to MD2 and interfered with the activation of toll-like receptor 4 (TLR4) induced by LPS. In cultured macrophages, shikonin inhibited TLR4 signalling and pro-inflammatory cytokine production. These effects were produced through suppression of key signalling proteins including the NF-κB and the MAPK pathway. We also showed that shikonin inhibits MD2–TLR4 complex formation and reduces LPS-induced inflammatory responses in a mouse model of ALI. Conclusions and Implications Our studies have uncovered the mechanism underlying the biological activity of shikonin in ALI and suggest that the targeting of MD2 may prove to be beneficial as a treatment option for this condition.

CAS / MDL: 517-89-5 54952-43-1
研究领域: 药理学 · 免疫学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL IMMUNOPHARMACOLOGY · 2022 · IF 5.714

Disulfiram inhibits oxidative stress and NLRP3 inflammasome activation to prevent LPS-induced cardiac injury

Shanshan Wei,Zijun Xiao,Jie Huang,Zhenyu Peng,Bikui Zhang,Wenqun Li

Sepsis-induced cardiac injury leads to the high rate of mortality, the therapeutics for this disorder are limited. Disulfiram (DSF) is an FDA-approved treatment for chronic alcohol addiction, and its cardio-protection is gradually discovered in recent years. In present study, mice were injected with lipopolysaccharide (LPS, 15 mg/kg) to induce a septic cardiac injury model, and aimed to investigate the protective effect of DSF on sepsis-induced cardiac injury and the underlying mechanisms. Results showed that DSF treatment alleviated the lowered left heart function and myocardial cell apoptosis induced by LPS. Moreover, we found that LPS increased myocardium lipid peroxidation, DNA damage and the activation of NLRP3 inflammasome, which were significantly reduced by DSF. These results suggested the protective role of DSF in LPS-induced cardiac injury, and the mechanism involved the inhibition on the oxidative stress and NLRP3 inflammasome activation. Given the potent cardiac protection effect of DSF, repurposing DSF in the clinic would represent a new strategy to protect and treat sepsis-induced cardiac injury.

CAS / MDL: 93572-42-0
研究领域: 药理学 · 心脏病学 · 传染病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Frontiers in Nutrition · 2023 · IF 5

Anti-inflammatory effects and molecular mechanisms of bioactive small molecule garlic polysaccharide

Shao Xin,Li Jialong,Zhang Huidan,Zhang Xuhui,Sun Chongzhen,Ouyang Xin,Wang Yong,Wu Xiyang,Chen Chunbo

Although garlic polysaccharides have been found to possess anti-inflammatory activities, anti-inflammatory study on small molecule water-soluble garlic polysaccharide (WSGP) is few. In this study, a novel WSGP with a molecular weight of 1853 Da was isolated by DEAE-52 and Sephadex G-100 column and the chemical composition was identified by monosaccharide composition and methylation analysis. Furthermore, the antioxidant effects of WSGP and the potential molecular mechanisms on LPS-induced inflammatory responses in RAW264.7 macrophage cells were investigated. The results showed that WSGP has strong antioxidant activity, such as DPPH, hydroxyl, superoxide anion, ABTS radical scavenging capacity, Fe2+ chelating ability and reducing power. Meanwhile, WSGP could considerably suppress the manufacturing of NO and the mRNA and protein expression degrees of IL-6, TNF-α, and IL-1β in LPS inspired RAW264.7 macrophages WSGP could significantly suppress the production of NO and the mRNA and protein expression levels of IL-1β, IL-6, and TNF-α in LPS stimulated RAW264.7 macrophage cells (p < 0.05). In addition, the phosphorylated IκB-α, p65, and STAT3 proteins were significantly increased in LPS-induced macrophages, while this trend was significantly reversed by WSGP treatment in a concentration-dependent manner (p < 0.05). Consequently, WSGP supplementation might reduce LPS-induced inflammatory responses by suppressing proinflammatory cytokines and NF-κB and STAT3 pathway activation. The finding of this research would give scientific guidelines for the judicious use of small molecular garlic polysaccharide in anti-inflammatory treatments.

研究领域: 免疫学 · 药理学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2024 · IF 4.8

Investigating mechanisms of Sophora davidii (Franch.) skeels flower extract in treating LPS-induced acute pneumonia based on network pharmacology

Ping Chen,Cheng Lin,Qi Jin,Baibai Ye,Xinxu Liu,Keke Wang,Han Zhang,Jiahui Liu,Runan Zhang,Hao Huang,Chenning Zhang,Linfu Li

Ethnopharmacological relevance In TCM opinion, most of pneumonia is related to "lung heat". Sophora davidii (Franch.) Skeels flower was first documented in "Guizhou Herbal Medicine", and was recorded as having functions of clearing heat, detoxifying, and cooling blood. It can be used to treat lung heat cough. Aim of the study To investigate main mechanisms of Sophora davidii flower extract (SDFE) in Treating LPS-induced acute Pneumonia. Materials and methods Acute pneumonia models on BEAS-2B cells and rats were established using LPS. The rat model was used to verified the protective effects of SDFE through HE staining, lung tissue W/D ratio assay, white blood cell count analysis, and ammonia-induced coughing test. Network pharmacology was applied to predict the active compounds, core targets and main pathways of SDFE in treating acute pneumonia. Western Blot and ELISA kits were employed to validate representative proteins in selected pathway in vivo and in vitro . Results HE staining, lung tissue W/D ratio assay, white blood cell count analysis, and ammonia-induced coughing test showed SDFE could improve pathological features (leukocyte infiltration, pulmonary edema, lung injury and cough). Network pharmacology indicated MAPK/NF-κB pathway was the most relevant pathway. SDFE could significantly inhibit the expression of Fos and Jun, and the phosphorylation levels of p38, ERK, JNK, NF-κB and IκB. It also down-regulated the expression of pro-inflammatory factors (TNF-α, IL-6 and IL-1β). Conclusions SDFE can exert protective effects against acute pneumonia through the MAPK/NF-κB signaling pathway.

CAS / MDL: 1336-21-6
研究领域: 药理学 · 免疫学 · 中医药 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FITOTERAPIA · 2024 · IF 2.5

Multi-level chemical characterization and anti-inflammatory activity evaluation of the polysaccharides from Prunella vulgaris

He Sun,Jia Lou,Bo-Xue Chen,Jia-Qi Huang,Qi-Long Wang,Shao-Fei Song,Zi-Yue Jia,Rong Miao,Shi-Yu Wang,Xue Li,Wen-Zhi Yang

Prunella vulgaris (PV) is a medicine and food homologous plant, but its quality evaluation seldom relies on the polysaccharides (PVPs). In this work, we established the multi-level fingerprinting and in vitro anti-inflammatory evaluation approaches to characterize and compare the polysaccharides of P. vulgaris collected from the major production regions in China. PVPs prepared from 22 batches of samples gave the content variation of 5.76–24.524 mg/g, but displayed high similarity in the molecular weight distribution. Hydrolyzed oligosaccharides with degrees of polymerization 2–14 were characterized with different numbers of pentose and hexose by HILIC-MS. The tested 22 batches of oligosaccharides exhibited visible differences in peak abundance, which failed to corelate to their production regions. All the PVPs contained Gal, Xyl, and Ara, as the main monosaccharides . Eleven batches among the tested PVPs showed the significant inhibitory effects on NO production on LPS-induced RAW264.7 cells at 10 μg/mL, but the exerted efficacy did not exhibit correlation with the production regions. Conclusively, we, for the first time, investigated the chemical features of PVPs at three levels, and assessed the chemical and anti-inflammatory variations among the different regions of P. vulgaris samples.

CAS / MDL: 34819-78-8
研究领域: 生药学 · 分析化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Nanoscale Research Letters · 2021 ·Vol. 16 ·期 1 ·1-16 · IF 4.703

Preparation of ICA-loaded mPEG-ICA nanoparticles and their application in the treatment of LPS-induced H9c2 cell damage

Zhou Lin,Huang Zhi,Yang Shanyi,Wei Jiarui,Xu Yan,Hu Lin,Guo Xinrong,Yuan Limin,Yuan Zexuan,Yang Xiaoping,Tao Xiaojun,Zhang Qiufang

Hydrophilic polyethylene glycol monomethyl ether (mPEG) was grafted onto Icariin (ICA) by succinic anhydride to form a polyethylene glycol-Icariin (mPEG-ICA) polymer. The structure of the polymer was characterized by Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). mPEG-ICA nanoparticles loaded with ICA were prepared by physical embedding of ICA by dialysis. The particle size was determined to be (220 ± 13.7) nm, and the ζ potential was (2.30 ± 1.33) mV by dynamic light scattering (DLS). Under a transmission electron microscope (TEM), the nanoparticles were spherical, and the morphology was regular. In the medium with pH 7.4, the drug release rate of mPEG-ICA nanoparticles reached (52.80 ± 1.70)% within 72 h. At pH 6.8, the cumulative drug release of nanoparticles reached (75.66 ± 0.17)% within 48 h. Treatment of the nanoparticles with LPS-treated H9c2 cells maintained cell viability, reduced LDH release and exerted antiapoptotic effects. Moreover, ICA-loaded mPEG-ICA nanoparticles significantly decreased the mRNA expression of the myocardial inflammatory cytokines TNF-α, IL-1β and IL-6M. In conclusion, ICA-loaded mPEG-ICA nanoparticles protected against LPS-induced H9c2 cell injury.

CAS / MDL: 1122-58-3
研究领域: 药学 · 纳米技术 · 细胞生物学 · 炎症研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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DEVELOPMENTAL AND COMPARATIVE IMMUNOLOGY · 2021 · IF 3.636

Cordycepin inhibits inflammatory responses through suppression of ERK activation in zebrafish

Wei Liu,Ling Zhang,Shuo Sun,Long-sheng Tang,Shi-min He,An-qi Chen,Li-na Yao,Da-Long Ren

As a natural extract, cordycepin has been shown to play important regulatory roles in many life activities. In the study, the effects of cordycepin on inflammatory responses and the underlying mechanisms was explored using a zebrafish model. In the model of LPS-induced inflammation, cordycepin was found to significantly inhibited the expression of pro-inflammatory cytokines such as tnf-α, il-1β, il-6, and il-8 . Using in vivo imaging model, cordycepin significantly inhibited fluorescent-labeled neutrophils migrating towards injury sites. Furthermore, results showed that the phosphorylation level of ERK protein dramatically decreased after cordycepin treatment. Meanwhile, the ERK inhibitor, PD0325901, significantly inhibited the expression of pro-inflammatory cytokines in LPS-induced inflammatory model and neutrophils migration in the caudal fin injury model. This study indicated the important roles of cordycepin in inhibiting LPS and injury-induced inflammation and preliminarily explained the role of ERK protein in this process.

研究领域: 免疫学 · 药理学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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ACS Food Science & Technology · 2025 · IF 2.8

Impact of a Papain-Catalyzed Plastein Reaction of Salmon Skin Gelatin Hydrolysate and Exogenous Amino Acids on Anti-Inflammatory Activity in LPS-Stimulated Macrophages

Yun-Jiao Shi,Hua-Qiang Li,Xin-Huai Zhao

The hydrolysate of salmon skin gelatin (HSSG) was generated by hydrolyzing salmon skin gelatin with papain and then modified using a papain-catalyzed plastein reaction with or without one of the three exogenous Gly, Pro, and Hyp. The prepared samples including HSSG, the HSSG modifier alone (namely, PHSSG), three HSSG modifiers with one of the exogenous amino acids (namely, PHSSG-Gly, PHSSG-Pro, and PHSSG-Hyp), and three mixtures of HSSG plus one of the exogenous amino acids (namely, HSSG-Gly, HSSG-Pro, and HSSG-Hyp) were thus assessed for their activities toward the lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. These samples were all nontoxic to the macrophages but showed different abilities to promote cell growth. LPS promoted macrophage phagocytosis and lactate dehydrogenase release and enhanced the production levels of intracellular reactive oxygen species, NO, prostaglandin E2, and four inflammatory cytokines including TNF-α, IL-6, TGF-β1, and IL-10. Meanwhile, HSSG, PHSSG, and PHSSG-Hyp alleviated the LPS-induced macrophage inflammation by regulating the expression of 12 inflammation-related genes including iNOS, IL-6, TNF-α, IL-1β, COX-2, TLR4, IL-10, TGF-β1, miR-181a, miR-30d, miR-155, and miR-148a, downregulating the expression of five proteins including p-NF-κB-p65, MyD88, p-IKKα, p-IκBα, and iNOS that are associated with cell inflammation and reducing the nuclear translocation of p65 in the nucleus. Among the three evaluated samples, PHSSG-Hyp and HSSG had the respective highest and lowest anti-inflammatory activities in the LPS-induced macrophages via inactivating the NF-κB signaling pathway. It was thus concluded that the plastein reaction used in the presence of Hyp endowed HSSG with the highest anti-inflammatory activity in the macrophages, highlighting the potential use of this reaction in protein hydrolysates to reach activity enhancement and to produce functional peptide products.

CAS / MDL: 56-40-6 28648-78-4
研究领域: 生物化学 · 免疫学 · 食品科学
✓ 已验证 产品关联 DOI 高影响因子
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