Antioxidants
·
2021
·Vol. 10
·期 9
·1333
·
IF 6.313
Mengyuan Fang,Tingfeng Zou,Xiaoxiao Yang,Zhen Zhang,Peichang Cao,Jihong Han,Yajun Duan,Ban-Feng Ruan,Qing-Shan Li
Sepsis remains one of the most common life-threatening illnesses that is characterized by a systemic inflammatory response syndrome (SIRS) and usually arises following severe trauma and various septic infections. It is still in urgent need of new effective therapeutic agents, and chances are great that some candidates can be identified that can attenuate oxidative stress and inflammatory responses. Pterostilbene, which exerts attractive anti-oxidative and anti-inflammatory activities, is a homologue of natural polyphenolic derivative of resveratrol. Starting from it, we have made several rounds of rational optimizations. Firstly, based on the strategy of pharmacophore combination, indanone moiety was introduced onto the pterostilbene skeleton to generate a novel series of pterostilbene derivatives (PIF_1–PIF_16) which could possess both anti-oxidative and anti-inflammatory activities for sepsis treatment. Then, all target compounds were subjected to their structure–activity relationships (SAR) screening of anti-inflammatory activity in mouse mononuclear macrophage RAW264.7 cell line, and their cytotoxicities were determined after. Finally, an optimal compound,PIF_9, was identified. It decreased the mRNA levels of lipopolysaccharide (LPS)-induced interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), inducible nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX2). We also found that the anti-inflammatory effects might be contributed by its suppression on the nuclear factor-κB (NF-κB) and MAPKs signaling pathway. Moreover,PIF_9also demonstrated potent anti-oxidative activity in RAW264.7 macrophages and the sepsis mouse model. Not surprisingly, with the benefits mentioned above, it ameliorated LPS-induced sepsis in C57BL/6J mice and reduced multi-organ toxicity. Taken together,PIF_9was identified as a potential sepsis solution, targeting inflammation and oxidative stress through modulating MAPKs/NF-κB.Keywords:antioxidants;anti-inflammatory agents;indanone;pterostilbene;sepsis
研究领域:
药理学
·
传染病学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
BIOLOGICAL & PHARMACEUTICAL BULLETIN
·
2015
·Vol. 38
·期 10
·1658-1662
·
IF 1.828
Lu-yang Lu,Yuan Liu,Zhi-feng Zhang,Xiao-jun Gou,Jun-hao Jiang,Ji-zhong Zhang,Qian Yao
Pomegranate seed oil (PSO) has diverse bioactivities. It was hyphothesized that if PSO were employed to construct a trans-resveratrol-loaded self-nanoemulsifying drug delivery system (RES SNEDDS-PSO), not only could PSO serve as an oil phase but also exert synergistic effects with resveratrol to yield better therapeutic outcomes. In this study, we prepared RES SNEDDS-PSO for the first time to validate that hypothesis. The anti-inflammatory and anticancer activities of RES SNEDDS-PSO were compared with another SNEDDS composed of oil phase isopropyl palmitate (RES SNEDDS-IP). The results showed that upon exposure to a 10-fold amount of water, RES SNEDDS-PSO was converted into nanoemulsions with a mean size of 44 nm. Nanoemulsions enhanced the water solubility of resveratrol by 20-fold, significantly improved resveratrol stability in intestinal fluid, and slowed the decomposition of resveratrol in water by 1-fold. An in vivo anti-infection test showed that the degree of inflammatory swelling in mice given RES SNEDDS-PSO was only 60 and 76% that of the group fed with RES SNEDDS-IP at doses of 10 and 20 mg/kg, respectively. An in vitro anticancer study showed that the inhibitory rate of RES SNEDDS-PSO against MCF-7 breast cancer cells was 2.03- and 1.24-fold that of RES SNEDDS-IP at a concentration of 12.5 and 25 µg/mL, respectively. This study demonstrated that the newly developed SNEDDS may be a prospective formulation in the functional food and clinical fields.
研究领域:
药剂学
·
生物医学
·
食品科学
✓ 已验证
DOI
PubMed
高影响因子
Evidence-based Complementary and Alternative Medicine
·
2014
·
IF 2.175
Chuan-li Lu,Wei Zhu,Min Wang,Xiao-jie Xu,Chuan-jian Lu
Smilax glabra Roxb. has been used for a long time as both food and folk medicine. In the present study, phenolic-enriched extract of S. glabra (PEESG) was extracted with 70% ethanol and purified by HP-20 column chromatography. Its antioxidant and anti-inflammatory activities were evaluated by radical scavenging assay, reducing power determination, and lipopolysaccharide (LPS)-induced RAW264.7 cells assays, respectively. PEESG exhibited obviously scavenging capacity for DPPH and ABTS radicals, as well as significant reducing power for ferric ion. Particularly, PEESG (12.5–50 μg/mL) showed a significantly higher efficiency for scavenging ABTS than that of ascorbic acid and no significant difference with ascorbic acid for DPPH scavenging. PEESG also possessed a significant suppression effect on proinflammatory mediators production, such as nitric oxide (NO), tumor necrosis factor- (TNF-), and interleukin-6 (IL-6), in LPS-induced RAW264.7 cells. In addition, the main ingredients of PEESG were identified using ultrahigh pressure liquid chromatography coupled to electrospray mass spectrometry (U-HPLC-ESI-MS). Seventeen components, including 5-O-caffeoylshikimic acid, neoastilbin, astilbin, neoisoastilbin, isoastilbin, engetin and isoengeletin were identified. These findings strongly suggest the potential of PEESG as a natural antioxidant and anti-inflammatory agent.
研究领域:
药理学
·
植物化学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Jingwei Wu,Zhihui Li,Zhuoting Zhang,Jian Zhang,Hangyu Hu,Hanglian Lan,Weilian Hong,Zhennai Yang
Exopolysaccharides (EPSs) produced by lactic acid bacteria have been extensively studied, but the EPSs as postbiotics are much less investigated. In this study, the EPS, designated as ET22-EPS, was extracted and purified from the culture broth of Lacticaseibacillus paracasei ET-22 previously characterized with strong postbiotic activities. ET22-EPS was determined with a molecular weight of 5.12 × 10 5 Da, and a monosaccharide composition of mannose, galactose, glucose, and N -acetylglucosamine in a molar ratio of 0.662:0.103:0.095:0.026. ET22-EPS exhibited a sheet-like and fibrous stacking morphology with a networked structure. ET22-EPS also showed high thermal stability with a degradation temperature of 295.33 °C. ET22-EPS was identified to consist of an octasaccharide repeating unit with a backbone structure of four consecutively linked →2)-α-D-Man p (1 → together with →2,6)-α-D-Man p (1 → 2)-α-D-Glc p (1→, and a branch chain of α-D-Gal p (1 → 6)-α-D-Man p (1→. The in vitro bioassay indicated that ET22-EPS effectively scavenged the free radicals of diammonium 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate), 1,1-diphenyl-2-picrylhydrazyl, hydroxyls, and superoxide anion. ET22-EPS showed strong anti-inflammatory effects by reducing cell phagocytosis, nitric oxide production, pro-inflammatory cytokine secretion, and the TNF-α/IL-10 ratio in a RAW264.7 cell model. Therefore, ET-22-EPS shows good prospects as potential postbiotics in the development of health foods.
研究领域:
食品科学
·
微生物学
·
营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Materials Horizons
·
2025
·
IF 10.7
Jin Zhang,Lingzhuang Meng,Yinan Jia,Jianshu Li,Xinyuan Xu,Xin Xu
Periodontitis, a chronic inflammatory disease triggered by dental plaque, often presents challenges in management, particularly in severe cases where mechanical debridement alone may be insufficient. As a result, adjunctive therapies, particularly localized drug delivery systems with both antimicrobial and anti-inflammatory properties, are essential to enhance the efficacy of periodontitis management. In this study, we developed a multifunctional hydrogel by incorporating a salicylic acid–choline deep eutectic solvent (DES) into a chitosan/β-glycerol phosphate sodium (CS/GP) hydrogel matrix for the treatment of periodontitis. The DES-CS/GP hydrogel demonstrated favorable physicochemical properties, including gelation and injectability, making it highly suitable for application in the oral cavity. The hydrogel effectively inhibited the growth of key periodontal pathogens, Porphyromonas gingivalis and Fusobacterium nucleatum, and significantly downregulated the expression of pro-inflammatory cytokines TNF-α and IL-1β in vitro. Cytocompatibility assessments showed over 80% cell viability in human gingival fibroblasts, human gingival epithelial cells, and human oral keratinocytes over 5 days treated with DES-CS/GP, with fluorescence microscopy confirming robust cytoskeletal integrity. Furthermore, the hydrogel enhanced permeability through gingival tissues in vitro. In a rat model of periodontitis, the hydrogel significantly mitigated bone loss, reduced bacterial loads of P. g, and suppressed TNF-α and IL-1β expression in gingival tissues. These findings underscore the hydrogel's potential as a safe and effective adjunctive therapy for periodontitis, offering a combination of antimicrobial, anti-inflammatory, and tissue-permeating properties with high biosafety and ease of application.
研究领域:
口腔医学
·
药剂学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yawen Zhao,Mingyu Li,Nuoya Chen,Kaiyang Huang,Xiaofeng Wu,Yanfei Tan,Qinsheng Hu,Rifang Luo,Yunbing Wang
Ensuring excellent anticoagulant, anti-inflammatory, and endothelialization properties in vascular stents through coating construction is crucial for their satisfactory performance post-implantation. In this study, we propose a cell-membrane mimetic multifunctional hyaluronic acid (HA)-based coating by combining the aminolyzed methacryloyloxyethyl phosphorylcholine (MPC) copolymer with oxidized hyaluronic acid (Ox-HA) through Schiff base reaction. Compared with traditional anti-fouling design, the composite coating present a stage-specific ability, which can resist the adhesion of blood components, while mediating vascular cell fate with the incorporation of HA. The coating exhibited promoted endothelial cell (EC) growth and inhibited the proliferation of smooth muscle cells (SMCs) by inducing a phenotype change. Besides, the multifunctional HA-based coating can mediate macrophages to a M2 phenotype. The coated stents were implanted in rabbits, and exhibited ideal capabilities in promoting endothelialization and inhibiting inflammation and restenosis in vivo , offering a potential approach to address multifunctionality for vascular implants.
研究领域:
生物医学工程
·
心血管医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Mengyao Zhang,Jiali Tang,Jiaying Wang,Chenchen Qi,Guohui Chen,Wei Chen,Chengtao Wang
This study explores the grafting of syringic acid onto fucoidan and assesses the resultant graft's (F S) enhanced functional properties and therapeutic potential in a histamine-induced liver injury model. Utilizing a redox system of ascorbic acid and hydrogen peroxide, the grafting process achieved a grafting rate of 290.45 mg CAE/g, confirmed through UV–Vis spectroscopy, FT-IR spectroscopy, scanning electron microscopy, and thermogravimetric analysis. In vivo investigations using histamine-sensitive mice demonstrated that F S significantly mitigated histamine-induced damage, evidenced by improvements in body weight, organ index, and colon length. F S exhibited superior efficacy in restoring liver function indices (ALT, AST, ALP, GGT), enhancing antioxidant defenses (GSH, SOD), and reducing oxidative stress markers (MDA). Anti-inflammatory effects included reduced levels of pro-inflammatory cytokines (TNF- α , IL-6, IL-1 β ) and modulation of apoptosis-related proteins (BCl 2 , BAX). Additionally, F S upregulated key antioxidant genes in the Nrf2/KEAP1 pathway and downregulated inflammatory genes in the NF- κ B pathway. Restoration of colonic tight junction proteins (ZO-1, Occludin, Claudin-1) and normalization of gut microbiota composition further underscored the therapeutic potential of F S. The study highlights the significant enhancement in functional properties of fucoidan through SA grafting, presenting F S as a promising candidate for developing functional foods and nutraceuticals aimed at preventing and mitigating liver damage and related disorders.
研究领域:
生物化学
·
药理学
·
营养学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Small
·
2024
·
IF 13
Cheng Gu,Shu Fang,Lin Liu,Benjin Chen,Lingling Xu,Min Shao,Jianan Sun,Haisheng Qian,Wanni Wang
The production of bacterial toxins and excessive accumulation of reactive oxygen species (ROS) can induce localized oxidative stress, triggering an exaggerated immune response that impedes wound healing and culminates in chronic wounds. To address this issue, a microneedle (MN) system loaded with copper-manganese oxide (CMO) is developed to modulate the hyperimmune response in wounds. CMO@MN exhibits excellent antimicrobial and anti-inflammatory properties by effectively killing bacteria, scavenging ROS, and modulating macrophage polarization through their multiple enzymatic activities and photothermal properties. RNA sequencing revealed that CMO@MN improved the therapeutic effect on the infected skin of mice by balancing the ratio of M1/M2 macrophages and promoting cell migration and angiogenesis through the regulation of relevant pathways. Overall, this CMO@MN patch skillfully balances the complex issues between the immune response and wound healing and has potential applications in the treatment of other serious bacterial infections.
研究领域:
生物医学工程
·
免疫学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Heliyon
·
2022
·
IF 3.776
Wenjun Zhu,Qianqian Gu,Boyan Liu,Yanhong Si,Huirong Sun,Jingjie Zhong,Yi Lu,Dan Wang,Junli Xue,Shucun Qin
As an antioxidant, anti-inflammatory and anti-apoptotic agent, hydrogen (H 2 ) shows a promising potential in basic and clinical research against various diseases owing to its safety and efficacy. However, knowledge involving its underlying mechanisms of action, dosage effects, and dose duration remains limited. Previously, the dynamics of H 2 concentrations in different tissues of rats after exogenous H 2 inhalation had been detected by our team. Here, sequential changes of H 2 concentrations in different tissues of another most commonly used experimental rodent mice were monitored in real time with an electrochemical H 2 gas sensor during continuous different concentrations of H 2 inhalation targeting on five tissues including brain, liver, spleen, kidney, and gastrocnemius. The results showed that the H 2 saturation concentrations varied among tissues significantly regardless of the concentration of H 2 inhaled, and they were detected the highest in the kidney but the lowest in the gastrocnemius. Meantime, it required a significant longer time to saturate in the thigh muscle. By comparing the H 2 saturation concentrations of mice and rats, we found that there were no differences detected in most tissues except the kidney and spleen. Both gas diffusion and bloodstream transport could help the H 2 reach to most organs. The results provide data reference for dosage selection, dose duration determination to ensure optimal therapeutic effects of H 2 for mice experiments.
研究领域:
医学
·
生物化学
✓ 已验证
DOI
高影响因子
MOLECULES
·
2020
·Vol. 25
·期 20
·4815
·
IF 3.267
Minmin Sun,Yaoting Ji,Zhen Li,Rourong Chen,Shuhui Zhou,Chang Liu,Minquan Du
Conventional treatments for chronic periodontitis are less effective in controlling inflammation and often relapse. Therefore, it is necessary to explore an immunomodulatory medication as an adjuvant. Ginsenoside Rb3 (Rb3), one of the most abundant active components of ginseng, has been found to possess anti-inflammatory and immunomodulatory properties. Here, we detected the anti-inflammatory effect of Rb3 onPorphyromonas gingivalisLPS-stimulated human periodontal ligament cells and experimental periodontitis rats for the first time. We found that the expression of pro-inflammatory mediators, including IL-1β, IL-6 and IL-8, upregulated by lipopolysaccharide (LPS) stimulation was remarkably downregulated by Rb3 treatment in a dose-dependent manner at both transcriptional and translational levels. Network pharmacological analysis of Rb3 showed that the mitogen-activated protein kinase (MAPK) signaling pathway had the highest richness and that p38, JNK, and ERK molecules were potential targets of Rb3 in humans. Western blot analysis revealed that Rb3 significantly suppressed the phosphorylation of p38 MAPK and p65 NF-κB, as well as decreased the expression of total AKT. In experimental periodontitis rat models, reductions in alveolar bone resorption and osteoclast generation were observed in the Rb3 treatment group. Thus, we can conclude that Rb3 amelioratedPorphyromonas gingivalisLPS-induced inflammation by inhibiting the MAPK/AKT/NF-κB signaling pathways and attenuated alveolar bone resorption in experimental periodontitis rats.Keywords:anti-inflammatory agents;chronic periodontitis;ginsenoside;lipopolysaccharides
研究领域:
药理学
·
牙科
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Biomaterials Science & Engineering
·
2025
·
IF 5.5
Xinyun Pu,Xu Peng,Shubin Shi,Shaoxiong Feng,Xu Wei,Xi Gao,Xixun Yu
Valvular heart disease (VHD) poses a significant threat to human health, and the transcatheter heart valve replacement (THVR) is the best treatment for severe VHD. Currently, the glutaraldehyde cross-linked commercial bioprosthetic heart valves (BHVs) remain the first choice for THVR. However, the cross-linking by glutaraldehyde exhibits several drawbacks, including calcification, inflammatory reactions, and difficult endothelialization, which limits the longevity and applicability of BHVs. In this study, λ-carrageenan with anticoagulant function was modified by carboxymethylation into carboxymethyl λ-carrageenan (CM-λC); subsequently, CM-λC was used as a cross-linking agent to stabilize decellularized bovine pericardial tissue through amide bonds formed by a 1-(3-(Dimethylamino)propyl)-3-ethylcarbodiimide/N-Hydroxysuccinimide (EDC/NHS)-catalyzed reaction between the amino functional groups within pericardium and the carboxyl group located on CM-λC. Lastly, the inclusion complex (CD/Rutin) (formed by encapsulating the rutin molecule through the hydrophobic cavity of the mono-(6-ethylenediamine-6-deoxy)-β-cyclodextrin) was immobilized onto above BHVs materials (λCar-BP) through the amidation reaction. The treated sample exhibited mechanical properties and collagen stability similar to those of GA-BP, except for improved flexibility. Because of the presence of sulfonic acid groups and absence of aldehyde group as well as the Rutin release from CD/Rutin immobilized onto BHVs, the hemocompatibility, anti-inflammatory, HUVEC-cytocompatibility, and anticalcification properties, of the CM-λC-fixed BP modified with CD/Rutin was significantly better than that of GA-BP. In summary, this nonaldehyde-based natural polysaccharide cross-linking strategy utilizing the combination of CM-λC and CD/Rutin provides a novel solution to obtain BHVs with durable and stable anticoagulant, anticalcification, and anti-inflammatory properties, and has a wide range of potential applications in improving the various properties of BHVs.
研究领域:
医学材料学
·
心血管病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nanomaterials
·
2024
·Vol. 14
·期 5
·389
·
IF 4.4
Feng Gao,Wenyu Liang,Qixin Chen,Bairu Chen,Yuchen Liu,Zhibo Liu,Xu Xu,Rongrong Zhu,Liming Cheng
Disordered reactive oxygen/nitrogen species are a common occurrence in various diseases, which usually cause cellular oxidative damage and inflammation. Despite the wide range of applications for biomimetic nanoparticles with antioxidant or anti-inflammatory properties, designs that seamlessly integrate these two abilities with a synergistic effect in a simple manner are seldom reported. In this study, we developed a novel PEI-Mn composite nanoparticle (PM NP) using a chelation method, and the curcumin was loaded onto PM NPs via metal–phenol coordination to form PEI-Mn@curcumin nanoparticles (PMC NPs). PMC NPs possessed excellent dispersibility and cytocompatibility, was engineered to serve as an effective nanozyme, and exhibited specific SOD-like and CAT-like activities. In addition, the incorporation of curcumin granted PMC NPs the ability to effectively suppress the expression of inflammatory cytokines in microglia induced by LPS. As curcumin also has antioxidant properties, it further amplified the synergistic efficiency of ROS scavenging. Significantly, PMC NPs effectively scavenged ROS triggered by H2O2in SIM-A9 microglia cells and Neuro-2a cells. PMC NPs also considerably mitigated DNA and lipid oxidation in Neuro-2a cells and demonstrated an increase in cell viability under various H2O2concentrations. These properties suggest that PMC NPs have significant potential in addressing excessive ROS and inflammation related to neural diseases.Keywords:nanozyme;ROS scavenging;anti-inflammatory;neuroprotective
研究领域:
纳米技术
·
神经科学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）