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RAW264.7
INTERNATIONAL IMMUNOPHARMACOLOGY · 2017 · IF 2.956

Bergapten prevents lipopolysaccharide-induced inflammation in RAW264.7 cells through suppressing JAK/STAT activation and ROS production and increases the survival rate of mice after LPS challenge

Yi Zhou,Jing Wang,Weidong Yang,Xiaowen Qi,Lei Lan,Lan Luo,Zhimin Yin

Bergapten (BG) is a cumarine-derivate compound in many medicinal plants . Here, in vitro and in vivo experimental results indicated that BG possesses anti-inflammatory properties, Based on this, we further investigated the precise molecular mechanisms of BG in LPS-stimulated inflammation response . Studies revealed that BG inhibited LPS-stimulated productions of TNF-α, IL-1β, IL-6, PGE2 and NO as well as the expression of iNOS and COX-2, and at the same time, it increased LPS-induced release of IL-10 in a dose-dependent manner in RAW264.7 cells. Mechanistically, BG suppressed the activations of JAK/STAT, but not that of MAPKs and NF-κB. In addition, BG, as an antioxidant, prevented the accumulation of ROS , which further exerted its anti-inflammatory function. In vivo researches revealed that BG decreased LPS-induced mortality in mice. In conclusions, BG may be a potential candidate for inflammation therapy via inhibiting JAK/STAT activation and ROS production in RAW264.7 cells.

CAS / MDL: 616-91-1 97232-16-1
研究领域: 药理学 · 免疫学 · 细胞生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2025 · IF 4.6

Insights on the synergistic effects of glycyrrhetinic acid and isoliquiritigenin on HMGB1-induced inflammation by multi-spectroscopic and molecular docking studies

Xuewa Jiang,Shaoyan Yi,Pingping Shen,Richa Raj,Jian Zhang,Haixia Ge

Chronic low-grade inflammation, driven by elevated levels of circulating high mobility group box1 (HMGB1), plays a crucial role in the pathogenesis of multiple chronic diseases. Glycyrrhetinic acid (GA) and isoliquiritigenin (ISL) are representative metabolites in licorice, exhibit potent regulatory effects on HMGB1-mediated chronic inflammation. In this research, we investigated the interactions of GA and ISL with HMGB1 using multi-spectroscopy, surface plasmon resonance (SPR), and molecular docking. Fluorescence spectroscopy revealed that GA or ISL binds to HMGB1, leading to static fluorescence quenching of the protein. Additionally, the binding of GA or ISL altered the microenvironment of tryptophan and decreased the α-helix content of HMGB1 to varying extents. Dynamic light scattering (DLS) showed that GA induced aggregation of the HMGB1 complex into large particles, while ISL reduced the particle size of HMGB1. SPR analysis confirmed that GA and ISL bound reversibly to HMGB1 with K d values of 53.0 ± 3.6 and 16.3 ± 0.5 μM, respectively. Molecular docking further elucidated the binding modes and sites of GA and ISL on HMGB1, showing that GA binds to the B-box and ISL binds to the A-box of HMGB1, with hydrogen bonding and hydrophobic interactions as the primary driving forces. Isobologram analysis demonstrated that the combination of GA and ISL exhibited a significant synergistic inhibitory effect on HMGB1-induced inflammation on RAW264.7 cells, with an optimal combination ratio of 1:1. This study reveals that GA and ISL synergistically exert anti-inflammatory effect by modulating HMGB1 conformation, offering new insights into licorice extracts for preventing chronic inflammatory diseases.

研究领域: 药理学 · 生物化学 · 分子生物学 · 免疫学 · 药物化学
✓ 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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JOURNAL OF PHARMACEUTICAL SCIENCES · 2024 · IF 3.7

Liposomes Enhance the Immunological Activity of Polygonatum Cyrtonema Hua Polysaccharides

Dong Liu,Tingting Hou,Chunye Geng,Lu Song,Xuefeng Hou,Yanjun Chen,Fang Wang,Wei Wang,Bangxing Han,Leilei Gao

Poor stability and difficult uptake of natural polysaccharides have been the main problems in their application. The purpose of this study was to optimize the preparation conditions of Polygonatum cyrtonema Hua polysaccharides liposomes (PCPL) and to investigate the immune enhancement activity of PCPL in vitro and in vivo, with a view to discovering new ways of natural polysaccharide application. The optimal preparation conditions of PCPL were as follows: the adding amount of Tween 80 of 0.5 %, the ultrasound time of 2 min and the ultrasound times of once. Under these conditions, the entrapment efficiency, drug loading rate and particle size of PCPL were 38.033 %±0.050, 2.172 %±0.003 and 146 nm, which indicated that PCPL with small particle size could be prepared by the reverse-phase evaporation method. Furthermore, PCPL promoted proliferation, phagocytosis, and secretion of nitric oxide and related cytokines in RAW264.7 cells. Moreover, PCPL improved spleen and thymus indices, increased the number or proportion of red blood cells, platelets, and lymphocytes in the blood, and ameliorated spleen and thymus atrophy in immunosuppressed mice. This study provides a new idea for applying Polygonatum cyrtonema Hua polysaccharides (PCP) and references for studying other polysaccharides.

CAS / MDL: 57-88-5
研究领域: 药学 · 免疫学 · 生物技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMEDICINE & PHARMACOTHERAPY · 2019 · IF 3.743

Bilirubin alleviates alum–induced peritonitis through inactivation of NLRP3 inflammasome

Yanke Lin,Shuai Wang,Zemin Yang,Lu Gao,Ziyue Zhou,Pei Yu,Baojian Wu

Bilirubin is an endogenous substance derived from heme catabolism. In this study, we aimed to assess the anti-inflammatory activity of bilirubin, and to determine the mechanism thereof. The anti-inflammatory activity of bilirubin was evaluated using lipopolysaccharide (LPS)-treated peritoneal macrophages (PMs) and Raw264.7 cells, and mice with alum-induced peritonitis. The mRNA and proteins of NOD-like receptor family pyrin domain containing 3 (Nlrp3) and inflammatory cytokines were determined using qPCR and Western blotting, respectively. Distribution of phosphorylated (p) p65 [a NF-κB (nuclear factor-κB) subunit] in the cytoplasm and nucleus were evaluated by immunofluorescence analysis and electrophoretic mobility shift assay. Bilirubin prior to LPS treatment decreased protein expressions of Nlrp3, pro-interleukin (IL)-1β and mature IL-1β in PMs, whereas bilirubin post LPS treatment showed no effects. Bilirubin prior to LPS treatment dose-dependently repressed expressions of Nlrp3 and IL-1β, and inhibited translocation of p-p65 to nucleus in Raw264.7 cells. Bilirubin treatment decreased myeloperoxidase activity and reduced the levels of inflammatory cytokines (i.e., IL-1β, TNFα and IL-6) in lavage fluid in mice with alum-induced peritonitis. This was accompanied by a lower mortality rate. In addition, the mRNAs of Nlr p3 and IL-1β in peritoneal exudates cells were decreased, and the levels of p-p65 and mature IL-1β proteins were reduced. In conclusion, bilirubin acted on inflammation and alleviated alum–induced peritonitis through inactivation of Nlrp3 inflammasome.

CAS / MDL: 635-65-4
研究领域: 免疫学 · 炎症 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS · 2023 · IF 4.4

Explore the underlying oral efficacy of α-, β-, γ-Cyclodextrin against the ulcerative colitis using in vitro and in vivo studies assisted by network pharmacology

Weiqin Wang,Xuefeng Li,Hangyi Wu,Fanli Shi,Zhenhai Zhang,Huixia Lv

The incidence of ulcerative colitis (UC) is rising worldwide. As a refractory and recurrent disease, UC could seriously affect the patients’ quality of life. However, current clinical medical treatments for UC are accompanied by various side effects, especially for long-term applications. Here, the underlying efficacy of cyclodextrins (CDs) was studied. As common excipients, CDs endow proven safety for long-term applications. Results of predictive methods derived from network pharmacology prompted the potential anti-inflammatory effects of CDs by oral administration. RAW264.7 cell experiments verified that CDs could inhibit the excessive secretion of TNF-α (β-CD > α-CD ≈ γ-CD), IL-6, and NO (α-CD > β-CD ≈ γ-CD) as predicted. In mice with DSS-induced acute UC, oral administration of CDs could effectively mitigate the pathological damage of colon tissue and reduce the level of inflammatory mediators. Moreover, 16S rRNA sequencing displayed that gut microbes disturbed by DSS were significantly regulated by CDs. Conclusively, the study showed the therapeutic application prospects of CDs in UC treatment and indicated the feasibility and advantages of developing ‘new’ therapeutic activities of ‘old’ ingredients.Communicated by Ramaswamy H. Sarma

CAS / MDL: 89-57-6
研究领域: 药理学 · 炎症 · 胃肠病学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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RSC Advances · 2019 ·Vol. 9 ·期 52 ·30144-30153 · IF 3.049

Nutritional characteristics of marine fish Sardinella zunasi Bleeker and immunostimulatory activities of its glycoprotein

Yu Han,Huili Hao,Lihong Yang,Guolian Chen,Yucong Wen,Riming Huang

Sardinella zunasi Bleeker, an edible and medicinal marine fish, is largely distributed in tropical oceans. However, the chemical composition and nutritional properties of this species have not yet been investigated. In the present study, proximate composition, fatty acids, amino acids, taurine, and minerals of S. zunasi Bleeker were characterized, and the immunostimulatory properties of its glycoprotein were evaluated. The results indicated the presence of crude protein (19.66%), crude lipid (6.29%) and carbohydrate (0.74%) in S. zunasi Bleeker; monounsaturated fatty acids and polyunsaturated fatty acids in the fatty acid composition of S. zunasi Bleeker were 25.00% and 31.01%, respectively; S. zunasi Bleeker was rich in taurine (219 mg/100 g) and essential amino acids (5.57 g/100 g). In addition, the glycoprotein of S. zunasi consisted of protein and sugars, with a total content of 34.25% and 16.27%, respectively. The glycoprotein showed significant effects on promoting NO, TNF-α and IL-6 in a dose-dependent manner in RAW264.7 macrophage cells. Thus, these findings provide a scientific basis for the further utilization of glycoprotein from S. zunasi Bleeker.

研究领域: 海洋生物学 · 营养学 · 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 · 2023 · IF 8.2

Structural characterization and anti-inflammatory activity of polysaccharides from Astragalus membranaceus

Guangming Chen,Nan Jiang,Junping Zheng,Haiming Hu,Huabing Yang,Aizhen Lin,Baifei Hu,Hongtao Liu

In this study, two homogeneous polysaccharides (APS-A1 and APS-B1) were isolated from Astragalus membranaceus by DEAE-52 cellulose and Sephadex G-100 column chromatography. Their chemical structures were characterized by molecular weight distribution, monosaccharide composition, infrared spectrum, methylation analysis, and NMR. The results revealed that APS-A1 (2.62 × 10 6  Da) was a 1,4-α-D-Glc p backbone with a 1,4,6-α-D-Glc p branch every ten residues. APS-B1 (4.95 × 10 6  Da) was a heteropolysaccharide composed of glucose, galactose, and arabinose (75.24:17.27:19.35). Its backbone consisted of 1,4-α-D-Glc p , 1,4,6-α-D-Glc p , 1,5-α-L-Ara f and the sidechains composed of 1,6-α-D-Gal p and T-α/β-Glc p . Bioactivity assays showed that APS-A1 and APS-B1 had potential anti-inflammatory activity. They could inhibit the production of inflammatory factors (TNF-α, IL-6, and MCP-1) in LPS-stimulated RAW264.7 macrophages via NF-κB and MAPK (ERK, JNK) pathways. These results suggested that the two polysaccharides could be potential anti-inflammatory supplements.

研究领域: 药理学 · 免疫学 · 生物化学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Molecular Medicine Reports · 2023 ·Vol. 29 ·期 2 ·1-11 · IF 3.4

TIFA contributes to periodontitis in diabetic mice via activating the NF‑κB signaling pathway

Xiaoqian Guo,Guangwei Qiao,Jingjiao Wang,Changyi Yang,Min Zhao,Qian Zhang,Yingbiao Wan

Diabetic periodontitis (DP) refers to destruction of periodontal tissue and absorption of bone tissue in diabetic patients. Tumor necrosis factor receptor‑associated factor (TRAF)‑interacting protein with forkhead‑associated domain (TIFA) as a crucial regulator of inflammation activates the NF‑κB signaling pathway to regulate cell biological behavior. However, the function and mechanism of TIFA on DP suffer from a lack of research. In the present study, TIFA was upregulated in the periodontal tissue of a DP mouse model. In addition, the expression of TIFA in RAW264.7 cells was induced by high glucose (HG) culture and increased by lipopolysaccharide (LPS) from Porphyromonas gingivalis treatment in a time‑dependent manner. Knockdown of TIFA significantly reduced the levels of inflammatory cytokines, including TNF‑α, IL‑6, IL‑1β and monocyte chemoattractant protein‑1, in HG and LPS‑induced RAW264.7 cells. The nuclear translocation of NF‑κB p65 was induced by HG and LPS and was clearly suppressed by absence of TIFA. The expression of downstream factors Nod‑like receptor family pyrin domain‑containing 3 and apoptosis‑associated speck‑like protein was inhibited by silencing TIFA. Moreover, TIFA was increased by receptor activator of NF‑κB (RANK) ligand (RANKL) in a concentration dependent manner. The expression of cathepsin K, MMP9 and nuclear factor of activated T cells cytoplasmic 1 was downregulated by depletion of TIFA. RANKL‑induced osteoclast differentiation was inhibited by silencing of TIFA. Meanwhile, the decrease of TIFA blocked activation of the NF‑κB pathway in RANKL‑treated RAW264.7 cells. In conclusion, TIFA as a promoter regulates the inflammation and osteoclast differentiation via activating the NF‑κB signaling pathway.

CAS / MDL: 28718-90-3 18883-66-4
研究领域: 牙科 · 分子生物学 · 免疫学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Biomedical Nanotechnology · 2020 ·Vol. 16 ·期 10 ·1463-1470 · IF 4.483

Anti-Inflammatory Efficacy of Fabricated Rhein Micelles

Ding Xiangyu,Wang Yuan,Wen Chunmei,Wang Silu,Ruan Qingqing,Li Zhaofeng,Xu Jinzhong,Xu Zheng,Deng Jie

Rhein is a potential anti-inflammatory agent, but its poor water solubility significantly restricts its clinical application. In this study, rhein micelles (RMs) with improved water solubility were fabricated on Pluronic F127 (F-127). Transmission electron microscopy showed that the as-prepared RMs displayed a mean diameter of approximately 20 nm and a spherical morphology. The encapsulation efficiency of the micelles towards drugs varied from 81.38 ± 4.35% to 24.87 ± 4.32%. The RMs exhibited a burst release during the first 6 h and a following sustained release up to 96 h with a biphasic drug release pattern as suggested by the drug release assay. Cytotoxicity assessment showed that the RMs caused no change in cell viability at drug concentrations below 40 μM after 24 and 48 h of incubation. In RAW264.7 macrophages, the RMs inhibited the lipopolysaccharide-induced activation of p65/NF-κB, which in turn suppressed the transcription of its downstream inducible nitric oxide synthase, and cytokine genes such as interleukin-1β and tumor necrosis factor-α . Simultaneously, the RMs led to reduced cytokine secretions, including cyclooxygenase-2, prostaglandin E2, nitric oxide, and interleukin-6 in a dose-dependent manner. The RMs reported herein may be a promising candidate for developing anti-inflammatory therapeutic formulations.

研究领域: 药学 · 纳米技术 · 炎症研究
✓ 已验证 DOI PubMed 高影响因子
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FITOTERAPIA · 2024 · IF 2.5

Ingenane diterpenoids with anti-inflammatory activity from Euphorbia antiquorum

Ren-Fen Ma,Qian Wu,Yin-Po Pan,Hu Liu,Xin-Cheng Zhuang,Hua Zhang

The Euphorbia plants are famous for their diterpenoid constituents with diverse structures and broad biological activities. Herein, the discovery of 15 ingenane diterpenoids including 10 previously unreported ones ( 1 − 10 ) from Euphorbia antiquorum was presented. Structures of the undescribed compounds were established via detailed spectroscopic analyses. Meanwhile, a preliminary anti-inflammatory screening revealed that compound 6 showed significant inhibitory activity against the production of nitric oxide, as well as downregulated the expression of COX-2 and IL-6, in lipopolysaccharide-stimulated RAW264.7 macrophages. Further mechanistical exploration revealed that compound 6 could exert its anti-inflammatory effect by inhibiting NF-κB and activating Nrf2 signaling pathways.

CAS / MDL: 117-39-5
研究领域: 药理学 · 化学 · 免疫学 · 植物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOSCIENCE REPORTS · 2020 ·Vol. 40 ·期 7 · IF 2.942

Artesunate inhibits osteoclastogenesis through the miR-503/RANK axis

Huang Ming-Zhi,Zhuang Yong,Ning Xu,Zhang Hao,Shen Zhi-Min,Shang Xian-Wen

Osteoporosis is a metabolic bone disease that is characterized by decreased bone density and strength due to excessive loss of bone protein and mineral content, which can be induced by increased osteoclast activity. Developing agents targeting osteoclast activation is considered to be the most effective method to reverse bone destruction and alleviate the pain caused by osteoporosis. MTT assay was conducted to detect the cell viability after artesunate treatment of RAW264.7 cells. TRACP staining and pit formation assays were performed to examine the TRACP-positive cells and pit-forming activity of osteoclasts. qRT-PCR and Western blot analysis were performed to assess the mRNA and protein expression levels of the osteoclastogenesis-related genes NFATc1, TRAP, and cathepsin k. The protein levels of RANK, p-Akt, p-p38, and p-ERK were examined by Western blotting. Luciferase reporter assay was conducted to determine whether miR-503 targeted RANK directly. Artesunate inhibited TRACP-positive cells and the pit-forming activity of osteoclasts. However, artesunate increased the expression of miR-503. Artesunate suppressed osteoclastogenesis-related gene expression and RANKL-induced activation of MAPKs and the AKT pathway. In addition, miR-503 inhibited RANK expression by directly targeting RANK during osteoclast differentiation. Artesunate inhibited osteoclastogenesis and osteoclast functions in vitro by regulating the miR-503/RANK axis and suppressing the MAPK and AKT pathways, which resulted in decreased expression of osteoclastogenesis-related markers.

CAS / MDL: 88495-63-0
研究领域: 药理学 · 骨骼生物学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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