JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A
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2021
·Vol. 109
·期 12
·2506-2515
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IF 4.396
Jing Wei Jin,Min Zhi Rong,Ming Qiu Zhang,Wing-Leung Wong
β-1,3-D-glucan has been reported to have a series of bioactivities including antitumor, antimicrobial, anti-inflammatory and antioxidative effects; however, its insolubility in neutral aqueous solution significantly restricts the potential application in biological and medicine fields. Herein, a water-soluble aminated β-1,3-D-glucan (AG) was synthesized and the anti-inflammatory effect, cytotoxicity and plasmid DNA (pDNA) binding capacity of AG, serum stability, the particle sizes and zeta potentials of AG/pDNA nanocomposites, and the transfection efficiency and mechanism of action were studied. AG shows no obvious cytotoxicity within the range of working concentration (1–64 μg/ml) and it exerts potent anti-inflammatory effect independent on Dectin-1 and TLR2. AG/pDNA nanocomposites prepared by electrostatic interaction possess an appropriate particle size ranged from 192.8 to 118.4 nm and zeta potentials ranged from 20.880 to 27.16 mV with the N/P ratios from 5 to 100. AG/pDNA nanocomposites at the N/P ratios of 10 and 20 were able to show superior transfection efficiencies in RAW 264.7 cells as a result of their suitable particle size, zeta potential, anti-inflammatory effect, and the specific interaction with pattern recognition receptors (Dectin-1 and TLR2). These results indicate that AG is a potential candidate for DNA delivery system due to its potent anti-inflammatory effect and high transfection efficiency.
研究领域:
药学
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生物技术
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免疫学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
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2017
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IF 4.4
Liu Qing,Xiao Xu-Hui,Hu Liu-Bing,Jie Hui-Yang,Wang Ying,Ye Wen-Cai,Li Man-Mei,Liu Zhong
Anemone flaccida Fr. Schmidt (Ranunculaceae) (Di Wu in Chinese) is used to treat punch injuries and rheumatoid arthritis (RA). Our previous report has shown that crude triterpenoid saponins from Anemone flaccida exhibited anti-arthritic effects on type II collagen-induced arthritis in rats. Furthermore, anhuienoside C (AC), a saponin compound isolated from A. flaccida, was observed to suppress the nitric oxide production in lipopolysaccharide (LPS)-treated macrophage RAW 264.7 cells. In this study, we examined the effects of AC on the prevention and treatment of collagen-induced arthritis in a mouse model and evaluated the potential mechanisms involved. We observed that oral administration of AC significantly suppressed the paw swelling and arthritic score, decreased the body weight loss, and decreased the spleen index. Improvement in the disease severity was accompanied by the reduction of cluster of differentiation 68 (CD68)-positive cells in the ankle joint and inhibition of the pro-inflammatory cytokine tumor necrosis factor alpha (TNF-α) in the synovium of the joint. Mechanistic studies indicated that AC exerted its anti-inflammatory activity by inhibiting the mRNA expression levels of inducible nitric oxide synthase, cyclooxygenase-2, TNF-α, interleukin (IL)-1β, and IL-6 and by suppressing the production of inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in LPS-treated RAW 264.7 cells. AC also blocked the LPS-induced activation of the extracellular signal-regulated kinase, c-Jun N-terminal kinase, and p38 mitogen-activated protein kinase pathways. Additionally, the LPS-induced activation of nuclear factor kappa-B (NF-κB) was significantly suppressed by AC treatment, as indicated by down-regulation of TLR4 and inhibition of the nuclear translocation of NF-κB p65 and by activation and degradation of the inhibitor of kappa B. These findings indicated that AC has a great potential to be developed as a therapeutic agent for human RA.
研究领域:
药理学
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免疫学
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风湿病学
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产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
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2020
·
IF 3.701
Yilong Teng,Haohui Liang,Zeng Zhang,Yanming He,Yanna Pan,Shilin Yuan,Xiao Wu,Qingjie Zhao,Hongjie Yang,Ping Zhou
A proteoglycan, namely FYGL extracted from Ganoderma lucidum , was proved previously efficient for anti-diabetes in vivo . However, many medicine functions of FYGL have not been revealed, such as immunoregulation, an important function of Ganoderma in the traditional Chinese medicine. In this work, we firstly investigated the distribution of FYGL orally administrated by mice and found that FYGL was available in small intestine and viscera organs and enriched mostly in liver. Consequently, we studied the immunoregulation mechanism of FYGL in RAW 264.7 macrophages. The results showed that FYGL could induce initially ROS and trigger Ca 2+ ions influx into cells, leading to the activation of NF-κB and MAPK signaling to secret NO and cytokines for immune responses, and the promotion of phagocytosis. Meanwhile, FYGL absorbed in cells could reduce ROS, therefore preventing mitochondrial membrane from damage for cells safety. The results provided the immunoregulation basis of FYGL potentially applicable in clinics.
研究领域:
药理学
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免疫学
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分子生物学
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产品关联
DOI
高影响因子
Frontiers in Nutrition
·
2022
·
IF 6.59
Luo Bi,Lv Jia,Li Kejie,Liao Peiran,Chen Peng
This study aimed to extract polysaccharides from Citrus medica L. var. sarcodactylis (finger citron fruits) and analyze their structures and potential bioactivities. A new polysaccharide named K-CMLP was isolated and purified by Diethylaminoethylcellulose (DEAE)-Sepharose Fast Flow and DEAE-52 cellulose column chromatography with an average molecular weight of 3.76 × 103 kDa. Monosaccharide composition analysis revealed that K-CLMP consisted of rhamnose, galactose, and glucose, with a molar ratio of 6.75:5.87:1.00. Co-resolved by methylation and two-dimensional nuclear magnetic resonance (NMR), K-CLMP was alternately connected with 1, 2-Rha and 1, 4-Gal to form the backbone, and a small number of glucose residues was connected to O-4 of rhamnose. The results of DPPH⋅ and ABTS+⋅ radical scavenging assays indicated that both crude polysaccharide Citrus medica L. var. polysaccharide (CMLP) and K-CLMP exhibited strong free-radical-scavenging properties in a dose-dependent manner. In addition, K-CMLP significantly inhibited the production of pro-inflammatory cytokines (IL-6 and TNF-α) and reactive oxygen species (ROS) in RAW 264.7 cells treated with LPS. These results provide a basis for further use as one of the potential functions of food or natural medicine.
研究领域:
药理学
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生物化学
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食品科学
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植物科学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
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2021
·
IF 4.932
Jin Zhang,Changsong Wang,Hongliang Wang,Xueting Li,Jingjing Xu,Kaijiang Yu
Sepsis is a systemic inflammatory response syndrome resulted from severe infection. Excessive inflammation response plays an important role in sepsis-induced acute lung injury (ALI). Loganin is an iridoid glycoside isolated from Corni fructus and exerts an anti-inflammatory effect in multiple inflammatory diseases; however, the role of loganin in sepsis-induced ALI remains unknown. In the current study, the cecal ligation and puncture (CLP)-induced murine sepsis model was constructed to investigate the anti-inflammatory property of loganin in sepsis-induced ALI. Lipopolysaccharide (LPS)-treated Raw 264.7 cells and primary murine peritoneal macrophages were established to further explore underlying mechanism of loganin. Results showed that intragastrical administration of loganin significantly increased murine survival, reduced the alveolar structure damage and inflammatory cell infiltration. Loganin suppressed the release of the M1 macrophage-associated pro-inflammatory cytokines and induced the activation of M2-type anti-inflammatory cytokines. Besides, loganin dramatically inhibited NLRP3 inflammasome-mediated caspase-1 activation and subsequent IL-1β secretion. Further in vitro studies confirmed that loganin efficiently inhibited M1 macrophage polarization and NLRP3 inflammasome activation by blocking the extra-cellular signal-regulated kinase (ERK) and nuclear factor-kappa B (NF-κB) pathways. Taken together, the anti-inflammatory effect of loganin in sepsis-induced ALI was associated with the ERK and NF-κB pathway-mediated macrophage polarization and NLRP3 inflammasome activation. Our study offers a favorable mechanistic basis to support the therapeutic potential of loganin in anti-inflammatory diseases, such as sepsis-induced ALI.
研究领域:
药理学
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免疫学
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传染病学
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炎症研究
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产品关联
DOI
PubMed
高影响因子
PHYTOCHEMISTRY
·
2021
·
IF 4.072
Lanlan Nie,Rui Li,Jie Huang,Lingling Wang,Mengjie Ma,Chunyue Huang,Tong Wu,Renjie Yan,Xiao Hu
Five undescribed abietane diterpenoids , dracocephalumoids A–E, together with six known analogues were isolated from the aqueous EtOH extract of aerial parts of Dracocephalum moldavica L.. The structures were elucidated through extensive analysis of spectroscopic data , and their absolute configurations were established by Mosher's method and time-dependent density functional theory electronic circular dichroism (TDDFT ECD) calculation. Cell-based anti-inflammatory assays displayed that dracocephalumoid A, uncinatone, trichotomone F and caryopterisoid C showed potent suppressive effects against TNF- α , IL-1 β or NO production in LPS-induced RAW 264.7 cells, with IC 50 values ranging from 1.12 to 5.84 μM. The structure-activity relationship of these compounds was also discussed.
研究领域:
药理学
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有机化学
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生物化学
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药物化学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2021
·
IF 5.279
Ze-Rui Sun,Hua-Rong Liu,Di Hu,Mao-Si Fan,Ming-Yue Wang,Meng-Fei An,Yun-Li Zhao,Ze-Min Xiang,Jun Sheng
Hyperuricemia is a metabolic disease caused by impaired uric acid (UA) metabolism. Ellagic acid (EA) is a natural small-molecule polyphenolic compound with known antioxidative and anti-inflammatory properties. Here, we evaluated the regulatory effects of EA on hyperuricemia and explored the underlying mechanisms. We found that EA is an effective xanthine oxidase (XOD) inhibitor (IC50 = 165.6 μmol/L) and superoxide anion scavenger (IC50 = 27.66 μmol/L). EA (5 and 10 μmol/L) treatment significantly and dose-dependently reduced UA levels in L-O2 cells; meanwhile, intraperitoneal EA administration (50 and 100 mg/kg) also significantly reduced serum XOD activity and UA levels in hyperuricemic mice and markedly improved their liver and kidney histopathology. EA treatment significantly reduced the degree of foot edema and inhibited the expression of NLPR3 pathway-related proteins in foot tissue of monosodium urate (MSU)-treated mice. The anti-inflammatory effect was also observed in lipopolysaccharide-stimulated RAW-264.7 cells. Furthermore, EA significantly inhibited the expressions of XOD and NLRP3 pathway-related proteins (TLR4, p-p65, caspase-1, TNF-α, and IL-18) in vitro and in vivo. Our results indicated that EA exerts ameliorative effects in experimental hyperuricemia and foot edema via regulating the NLRP3 signaling pathway and represents a promising therapeutic option for the management of hyperuricemia.
研究领域:
药理学
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代谢疾病
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炎症
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生物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2024
·
IF 4.8
Ze Li,Jing Yuan,Yue Dai,Yufeng Xia
Ethnopharmacological relevance For centuries, Shaoyao-Gancao-Fuzi decoction (SGFD) has been a reliable traditional Chinese medicine for treating rheumatoid arthritis (RA). Despite its long history of use, the specific active components and underlying mechanisms of its therapeutic effects have yet to be fully understood. Aim of the study The aim of this study was to investigate the active ingredients and therapeutic effects of SGFD on RA, and to further understand its underlying mechanism. Materials and methods The chemical constituents in SGFD extract and in rat serum after oral administration of SGFD were identified and evaluated using ultra-performance liquid chromatography quadrupole-time-flight mass spectrometry (UPLC-Q-TOF/MS) together with various data-processing methods, respectively. The efficacy of SGFD was assessed by using an adjuvant-induced arthritis (AIA) rat model and lipopolysaccharide-stimulated RAW 264.7 cell. Subsequently, cell metabolomic was conducted to clarify the potential biomarkers and pathways. ELISA, RT-qPCR, and WB were used to verify the anti-arthritis mechanism of SGFD. Results A total of 65 chemical constituents were identified in SGFD. 17 active components were distinguished in rat serum samples, of which 13 may be the main active ingredients for SGFD treatment of RA. The remarkable efficacy of SGFD in reducing the symptoms of RA is evident through its ability to alleviate the redness and swelling of the affected paws, as well as reduce the infiltration of inflammatory cells. Cell experiments revealed that rat serum of SGFD reduced IL-1 β , IL-6, and TNF- α secretion in RAW 264.7 cells. 27 potential biomarkers were identified through cell metabolomics analysis. The arachidonic acid (AA) metabolism signaling pathway was activated in RA, which could be reversed by rat serum of SGFD. SGFD effectively inhibited the expression and transformation of AA by downregulating the expression of key enzymes, including phospholipase A and cyclooxygenase. Conclusion SGFD may ameliorate RA symptoms by regulating the AA-PGH 2 -PGE 2 /PGF 2α pathway. The main active components include songorine, fuziline, neoline, albiflorin, paeoniflorin, liquiritin, benzoylmesaconine, isoformononetin, liquiritigenin, isoliquiritigenin, formononetin, glycyrrhizic acid, and glycyrrhetinic acid.
研究领域:
药理学
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民族药理学
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代谢组学
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中医
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风湿病学
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产品关联
DOI
PubMed
高影响因子
Bioactive Materials
·
2020
·
IF 8.724
Meng Zheng,Jiazhi Guo,Qing Li,Jian Yang,Yi Han,Hongcai Yang,Mali Yu,Lianmei Zhong,Di Lu,Limei Li,Lin Sun
Vascular grafts must avoid negative inflammatory responses and thrombogenesis to prohibit fibrotic deposition immediately upon implantation and promote the regeneration of small diameter blood vessels (<6 mm inner diameter). Here, polyurethane (PU) elastomers incorporating anti-coagulative and anti-inflammatory Gastrodin were fabricated. The films had inter-connected pores with porosities equal to or greater than 86% and pore sizes ranging from 250 to 400 μm. Incorporation of Gastrodin into PU films resulted in desirable mechanical properties, hydrophilicity, swelling ratios and degradation rates without collapse. The released Gastrodin maintained bioactivity over 21 days as assessed by its anti-oxidative capability. The Gastrodin/PU had better anti-coagulation response (less observable BSA, fibrinogen and platelet adhesion/activation and suppressed clotting in whole blood). Red blood cell compatibility, measured by hemolysis, was greatly improved with 2Gastrodin/PU compared to other Gastrodin/PU groups. Notably, Gastrodin/PU upregulated anti-oxidant factors Nrf2 and HO-1 expression in H 2 O 2 treated HUVECs, correlated with decreasing pro-inflammatory cytokines TNF-α and IL-1β in RAW 264.7 cells. Upon implantation in a subcutaneous pocket, PU was encapsulated by an obvious fibrous capsule, concurrent with a large amount of inflammatory cell infiltration, while Gastrodin/PU induced a thinner fibrous capsule, especially 2Gastrodin/PU. Further, enhanced adhesion and proliferation of HUVECs seeded onto films in vitro demonstrated that 2Gastrodin/PU could help cell recruitment, as evidenced by rapid host cell infiltration and substantial blood vessel formation in vivo . These results indicate that 2Gastrodin/PU has the potential to facilitate blood vessel regeneration, thus providing new insight into the development of clinically effective vascular grafts.
研究领域:
生物材料
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组织工程
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生物医学工程
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药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
·
2022
·
IF 5.756
Jinhua Zhu,Danyang Zhou,Dandan Wu,Wei Liu,Xiuhua Liu
In this work, a highly effective separation approach mediated by 5-Lipoxygenase (5-LOX) was established for screening and isolation of anti-inflammatory ingredients from leaves of Lonicera japonica Thunb. (LLJT). Using 5-LOX immobilised on TiO2 nanotubes as a microreactor, the targeted screening was exploited by combining with HPLC-MS system. Four compounds confirmed as luteolin, luteoside, lonicerin, and isochlorogenic acid C and a fraction (M1) were screened out to be potent inhibitors of 5-LOX. Their anti-inflammatory activities were further investigated and confirmed by RAW 264.7 cells inflammation model and rat foot swelling model. Furthermore, M1 was prepared by MCI GEL CHP20P column chromatography, and further separated by Pre-HPLC. One new compound confirmed to be 5,7,3′,4′-tetrahydroxyflavone-7-O-sambubioside was first isolated from LLJT. The results provide a new method for the effective separation of active components derived from natural products.HighlightsA 5-LOX mediated separation method was established for isolation of anti-inflammatory compounds.An anti-inflammatory ingredient was separated by MCI GEL CHP20P column chromatography.One new compound was first isolated from leaves of Lonicera japonica Thunb.5-LOX was immobilised on TiO2 nanotubes and exploited by combining with HPLC-MS system.The anti-inflammatory activity of screened components was evaluated.
研究领域:
药理学
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分析化学
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天然产物研究
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
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2023
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IF 10.8
Deqing Lin,Xiaoning Xu,Lin Chen,Lei Chen,Mengyun Deng,Jinrun Chen,Zhibin Ren,Lei Lei,Jiaqing Wang,Jie Deng,Xingyi Li
Herein, we report a facile method for converting carboxylate-containing indomethacin (Idm) into a cyclooxygenase-2 (COX-2) selective inhibitor via the amidation of an unnatural peptide sequence (Nal-Nal-Asp). The resulting indomethacin amides ( i.e., Idm-Nal-Nal-Asp) have high selectivity for COX-2, and can self-assemble into a one-component supramolecular hydrogel that acts as a ‘self-delivery’ system for boosting anti-inflammatory efficacy. Self-assembled Idm-Nal-Nal-Asp hydrogel robustly inhibits COX-2 expression in lipopolysaccharide (LPS)-activated Raw 264.7 macrophages while also exhibits superior anti-inflammatory and antioxidant activities via reactive oxygen species (ROS)-related NF-κB and Nrf2/HO-1 pathways. Moreover, a rabbit model of endotoxin-induced uveitis (EIU) reveals that the Idm-Nal-Nal-Asp hydrogel outperforms clinically used 0.1 wt% diclofenac sodium eye drops in terms of in vivo anti-inflammatory efficacy via topical instillation route. As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications.
研究领域:
药物化学
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材料科学
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生物医学工程
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药理学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2021
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IF 6.953
Fengwei Ma,Hongbing Liu,Su Xu,Yongyou Cheng,Qiang Fei,Haijiang Chen
A water-soluble polysaccharide (LCP-05) was isolated from the flowers of Leucosceptrum canum Smith. LCP-05 was an acidic polysaccharide with a molecular weight of approximately 8.9 kDa. Monosaccharide composition analysis indicated that LCP-05 was composed of Man, Rha, GlcA, GalA, Glc, Gal and Ara in a molar ratio of 0.83:1.68:0.33:2.15:1.00:1.45:1.22. The framework of LCP-05 was speculated to be a branched rhamnogalacturonan with the backbone consisting of α-1,2,4-linked Rha p and α-1,4-linked GalA p , and bearing branches at the O -4 position of the Rha residues. The side chains are terminated primarily with the Ara f and Glc p residues. LCP-05 was found to be able to significantly induce the production of NO, IL-6, and TNF-α in RAW 264.7 cells, and to induce RAW 264.7 cell's suppressive effect on both cell growth and cell migration of 4 T1 mammary breast cancer cells.
研究领域:
植物学
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免疫学
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药理学
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癌症研究
✓ 已验证
DOI
PubMed
高影响因子
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