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CARBOHYDRATE POLYMERS · 2022 · IF 10.723

The potential therapeutic effects of hydroxypropyl cellulose on acute murine colitis induced by DSS

Xuefeng Li,Huixia Lv,Fanli Shi,Jie Song,Zhenhai Zhang

In this study, high-substituted hydroxypropyl cellulose (HHPC) and low-substituted hydroxypropyl cellulose (LHPC) were orally administered (150 or 300 mg/kg) to investigate the inflammation inhibitory effects on DSS-induced colitis mice. In addition, the anti-inflammatory potential of HHPC in-vitro (RAW 264.7 cells) was evaluated. The result showed that HHPC could inhibit the excessive secretion of TNF-α, IL-6, and NO in RAW 264.7 cells induced by lipopolysaccharide . Oral administration of HHPC and LHPC could dose-dependently mitigate the pathological damage of colon tissue, suppressed spleen edema, preserved thymus index, reduced the serum level of inflammatory mediators (TNF-α, IL-6, IL-1β, and MPO), increased the secretion of sIgA in the colon, and restored the balance of the intestinal flora such as Rikenellaceae_RC9_gut_group, Lachnospiraceae_UCG-006, and Blautia . Overall, this study elucidated the therapeutic potential of LHPC and HHPC as a prebiotic to treat acute ulcerative colitis.

研究领域: 药理学 · 免疫学 · 胃肠病学
✓ 已验证 DOI PubMed 高影响因子
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MACROMOLECULAR RESEARCH · 2019 ·Vol. 27 ·期 9 ·888-894 · IF 1.758

Alginate and Probiotics Synergistically Reversed Dextran Sulfate Sodium Salt (DSS)-Induced Gut Barrier Damage

Zhao Cheng,Hu Qiongyuan,Wu Xiuwen,Chen Guopu,Wu Hua,Ren Jianan

Previous studies have established that sole probiotics or fibre could be used to relieve colitis. However, few studies evaluated the synergistical effect of fibre and probiotics in treating colitis. This study, examined the effect of alginate, one of the commonest biomaterials and dietary fibre, and/or probiotics on the gut barrier in colitis mice. A synergistical effect was found between alginate and probiotics in colitis. Dextran sulfate sodium salt (DSS), a chemical toxic substance, was used to induce colitis model. Body weight, oxidative stress, inflammatory factors, gut barrier, intestinal morphology and the apoptosis of intestine epithelial cells were analyzed. A combination of probiotics and alginate was used to analyze their synergistic effect. The results showed that the combination of alginate and probiotics had a better therapeutic effect on colitis than using them individually, and they protected the gut barrier from DSS induced oxidative stress. The combination exhibited a greater ability in reducing pro-inflammatory factors and protecting the gut barrier from further damage. The synergistic effect of alginate and probiotics provides a great prospect for biotherapy in bowel diseases and oral drug delivery system.

研究领域: 胃肠病学 · 药理学 · 营养学
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INTERNATIONAL IMMUNOPHARMACOLOGY · 2025 · IF 4.7

Apigenin alleviates dextran sulfate sodium-induced ulcerative colitis via regulation of endoplasmic reticulum stress in goblet cells

Zhong-Hao Ji,Hai-Xiang Guo,Bingbing Wang,Wen-Zhi Ren,Jin-Ping Hu,Chengzhen Chen,Bao Yuan

Ulcerative colitis (UC) significantly impairs quality of life and incurs substantial economic costs. Apigenin, a flavonoid abundant in fruits and vegetables, has demonstrated potential in UC management. Utilizing DSS-induced UC mouse models and LS 174 T goblet cell models, this study elucidates apigenin's protective mechanisms. Dietary supplementation with 40 mg/kg apigenin markedly alleviated UC symptoms. Antibiotic-mediated microbiota depletion confirmed that apigenin's efficacy is independent of gut microbiota. Mechanistically, apigenin enhances SERCA2 expression to maintain intracellular calcium homeostasis, thereby inhibiting excessive activation of the PERK-eIF2α-ATF4-CHOP pathway, reducing goblet cell apoptosis, and preserving mucosal barrier integrity. These findings provide a robust theoretical foundation for apigenin as a dietary supplement in the prevention and mitigation of colitis.

CAS / MDL: 520-36-5
研究领域: 生物学 · 医学 · 药理学 · 细胞生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Functional Foods · 2025 · IF 4

Canthaxanthin improves dextran sulfate sodium-induced chronic colitis by modulating intestinal barrier and gut microbiota

Xiaoxiang Chen,Yan Chen,Zhichao Chen,Jiayao He,Xiahao Sun,Zuisu Yang

This study explored the beneficial effects of canthaxanthin (CX) on dextran sulfate sodium (DSS)-induced chronic colitis in mice and its underlying mechanisms. Oral administration of CX alleviated colitis severity, as demonstrated by reduced weight loss, diarrhea, hematochezia, colon shortening, and pathological colon injury. Improvements in intestinal permeability and inflammation were indicated by significantly decreased levels of permeability markers and pro-inflammatory cytokines. Moreover, CX mitigated mucus barrier dysfunction by enhancing goblet cell proliferation and mucin-2 secretion. CX reinforced the epithelial barrier by preserving tight junction function and preventing excessive apoptosis of colonic epithelial cells. Furthermore, CX modulated DSS-induced gut microbiota dysbiosis by reshaping the diversity and structure of both bacterial and fungal communities, increasing the abundance of beneficial microbes while reducing the prevalence of harmful microbes. To conclude, CX can effectively alleviate chronic colitis via modulating intestinal barrier function and maintaining microbiome homeostasis, providing a potential dietary therapy for UC.

CAS / MDL: 89-57-6
研究领域: 免疫学 · 营养学 · 微生物学
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ChemMedChem · 2025 · IF 3.4

Discovery of Safe COX-2 Inhibitors: Achieving Reduced Colitis Side Effects through Balanced COX Inhibition

Xinlin Zhu,Qin Li,Junhui Wu,Zhiran Ju

Graphical In recent years, the development of COX-2 inhibitors has shifted from a focus on highly selective inhibition to emphasizes more moderate selectivity. This study presents a potent balanced COX-2 inhibitor, compound 21d, which effectively alleviates histological damage and provides protection against DSS-induced colitis. The severe adverse effects associated with imbalanced cyclooxygenase-2 (COX-2) inhibition continue to pose significant challenges in the development of contemporary anti-inflammatory drugs. In recent years, the approach to COX-2 inhibitor drug development has shifted from a focus on highly selective inhibition of COX-2 to a strategy that emphasizes more moderate selectivity. The amino acid sequence and structural similarities between inducible COX-2 and constitutive cyclooxygenase-1 (COX-1) isoforms present both substantial opportunities and challenges for the design of next generation of balanced COX-2 inhibitors. As part of our ongoing research into the discovering novel and safer COX-2 inhibitors, we reported herein a highly potent and balanced COX-2 inhibitor 21 d (IC 50 value=1.35 μM, selectivity profile (IC 50 (COX-1)/IC 50 (COX-2)=22.34)). In vivo assays demonstrated that 21 d significantly alleviated histological damage and provided robust protection against dextran sulfate sodium (DSS)-induced acute colitis.

研究领域: 药理学 · 分子生物学 · 药物开发
✓ 已验证 DOI PubMed 高影响因子
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Food Bioscience · 2024 · IF 4.8

Curcumin loaded high internal phase emulsions: Formulation and potential to alleviate DSS-induced ulcerative colitis

Xiao-Long Li,Bao-Qiu Yang,Wen-Jie Liu,Han Tao,Bao Zhang

Ulcerative colitis (UC) is a chronic, incurable disease that causes great suffering to patients. High internal phase emulsions (HIPEs) are promising carriers of curcumin (Cur), which has a beneficial effect on UC. The retention rate of Cur encapsulated in HIPEs prepared by pea protein isolated nanoparticles/octenyl succinic anhydride-modified linear dextrin composite particles (PPINs/OSA-LD) or PPINs reached 84.85% and 85.98%, respectively, which was significantly higher than that of Cur dissolved in corn oil (73.84%) due to the superior protection of the emulsion interfacial structure. The HIPEs showed higher bioaccessibility of Cur (31.16%) due to the higher degree of free fatty acid release. After emulsion treatment, the symptoms of UC were ameliorated, mainly manifested by the recovery of body weight, growth of the colon, down-regulation of pro-inflammatory factors, up-regulation of anti-inflammatory factors, and balance of gut microbiota composition. The Cur-loaded HIPEs show an outstanding improvement in UC.

CAS / MDL: 9011-18-1
研究领域: 药学 · 结肠炎 · 药物递送系统 · 纳米技术 · 炎症
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2024 · IF 5.4

Tauroursodeoxycholic acid liposome alleviates DSS-induced ulcerative colitis through restoring intestinal barrier and gut microbiota

Junke Zhao,Suqi Hao,Yan Chen,Xiaoxing Ye,Pengchao Fang,Haiyan Hu

Ulcerative colitis (UC) is a chronic and progressive inflammatory disease that damages the colonic mucosa and disrupts the intestinal epithelial barrier. The current clinical treatment for UC is mainly chemotherapy, which has the limited effectiveness and severe side effects. It mainly focuses on the treatment of inflammation while neglecting the repair of the intestinal mucosa and the restoration of the microbiota balance. Here, we aimed to address these challenges by using an amphipathic bile acid -tauroursodeoxycholic acid (TUDCA) to replace cholesterol (CHL) in conventional liposomes. We prepared TUDCA/Emodin liposomes by incorporating the hydrophobic drug emodin. The experimental results indicated that TUDCA/Emodin Lip had uniform particle size distribution, good stability, low cytotoxicity, and exhibited good mucus permeability and anti-inflammatory activity in in vitro experiments, and was able to protect cells from oxidative stress. After oral administration, TUDCA/Emodin Lip significantly alleviated the severity of UC. This was evidenced by increased colon length, decreased inflammation and reduced colonic endoplasmic reticulum stress (ERS). Furthermore, TUDCA/Emodin Lip maintained the normal levels of the tight junction proteins Claudin-1 and ZO-1, thereby restoring the integrity of the intestinal barrier. Importantly, TUDCA/Emodin Lip also promoted the ecological restoration of the gut microbiota, increased overall abundance and diversity. Taken together, TUDCA/Emodin Lip can fundamentally restore intestinal homeostasis, this work provides a new, efficient and easily transformable treatment for UC.

CAS / MDL: 38215-36-0
研究领域: 药理学 · 胃肠病学 · 炎症性肠病
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2025 · IF 5.2

Dextran sulfate-coated curcumin nanocrystals for the treatment of DSS-induced ulcerative colitis in mice

Yunmei Li,Huilin Ma,Huan Shi,Biaobiao Wang,Desheng Li,He Tian,Xifan Mei,Chao Wu

Ulcerative colitis is an inflammatory disease that primarily involves intestinal inflammation and epithelial damage. The nano-targeted drug delivery system delivers drugs to the disease site, exerting effects such as inhibiting inflammatory response and reducing reactive oxygen species expression, thereby promoting recovery from ulcerative colitis. In this experiment, dextran sulfate-coated curcumin nanocrystals (NBD) were prepared for the oral treatment of ulcerative colitis (UC). NBD not only significantly enhances the water solubility and stability of curcumin but also possesses the ability of sustained release and targeting inflammatory macrophages. The sustained release effect of NBD was demonstrated by in vitro release experiments. In simulated gastric fluid, the cumulative release amount of NBD at 2 h was 21.99 ± 1.93 %, while in simulated colonic fluid, the cumulative release amount of NBD at 12 h was 84.98 ± 2.02 %. The ability of NBD to target inflammatory macrophages was verified through the transwell system, rat one-way intestinal perfusion experiment and in vivo imaging system. The in vitro and in vivo (mice) anti-inflammatory and antioxidant capacities of NBD were validated using immunofluorescence experiment, ELISA kits and reactive oxygen species-related detection kits. The results indicated that NBD could reduce inflammatory responses, promote macrophage polarization and inhibit oxidative stress. In addition, the therapeutic effect of NBD was further confirmed in this experiment by the clostridium perfringens-induced necrotizing enteritis model in chickens. In conclusion, NBD might be a potential pharmaceutical preparation for the treatment of UC.

研究领域: 药理学 · 纳米医学 · 消化病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOLOGICAL TRACE ELEMENT RESEARCH · 2026 · IF 4.3

Cobalt Metal-organic Framework Alleviates DSS-Induced Ulcerative Colitis Via Barrier-protective and Immunomodulatory Effects

Abbas Mubbashar,Suliman Khan,Chen Min,Ying Zhao,Ashaq Muhammad Sameer,Asif Ali,Khan Muhammad Ali,Chen Dongmei,Xie Shuyu

Ulcerative colitis (UC) is characterized by excessive cytokine production, epithelial barrier disruption, and oxidative stress. It necessitates therapeutics with immunomodulation and mucosal integrity restoration. This study aimed to evaluate in-vivo and in-vitro therapeutic potential of Fe-MOF, Cr-MOF, and Co-MOF. RAW264.7 macrophages and DSS-induced murine colitis model were used. SEM, FTIR, XRD, and ICP-MS were used for characterization of MOFs. Cytotoxicity, immunofluorescence, ELISA, histopathology, immunoblotting, and qPCR analyses were used to evaluate effects of MOFs. Co-MOF showed a significant immunomodulatory effect by reducing LPS-induced TNF-α, IL-6, and IL-1β expression at both mRNA and protein levels in RAW264.7 macrophages. It also alleviated DSS-induced TNF-α, IL-6, and IL-1β levels in mouse colon, as indicated by ELISA and immunofluorescence. Co-MOF also reduced DAI score, improved body weight loss, and preserved colon length in the DSS-induced colitis model. Co-MOF also restored tight-junction proteins such as Occludin and ZO-1, significantly reduced by DSS in colon. Histopathological examination validated substantial protection of mucosal architecture, including intact crypts, restored goblet cell populations, and attenuated immune-cell infiltration. A notable antioxidant effect of Co-MOF was also observed, as it increases SOD and CAT activities while reducing MDA. Co-MOF significantly normalized platelets, lymphocytes, and neutrophils, elevated by DSS. Co-MOFs did not induce systemic toxicity and vital organ injury, predicting their biosafety. Conclusively, Co-MOF showed better immunomodulatory effects and barrier protection compared to Fe-MOF and Cr-MOF in UC, which further requires mechanistic validation.

CAS / MDL: 7789-02-8
✓ 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

CAZymes-associated method to explore glycans that mitigate DSS-induced colitis via targeting Bacteroides cellulosilyticus

Xiaoxiang Gao,FuSheng Xu,Tangjun Li,Pan Huang,Leilei Yu,Fengwei Tian,Jianxin Zhao,Wei Chen,Qixiao Zhai

Improving Bacteroides cellulosilyticus abundance is a feasible approach to treating inflammatory bowel disease (IBD). Although B. cellulosilyticus is responsive to dietary components, untargeted manipulation cannot focus on target microbe and lead to an increase in harmful bacteria in the microbiota . Breakthroughs in methods for regulating specific microbes, but the protocols are expensive, time-consuming, and difficult to follow. Glycans based on microbial-carbohydrate-active enzymes (CAZymes) would provide a potential solution. We propose a method based on CAZymes to explore polysaccharides that target specific gut microbes and alleviate diseases. The designed polysaccharides (Arabinogalactan, AG) enrich the abundance of B. cellulosilyticus in single-strain co-cultures, fermentation in vitro , and mouse models in vivo . Supplementation with AG relieved mice from colitis and clinical symptoms. We reveal that AG directly alters B. cellulosilyticus level and cooperative microbes, resulting in remission of colitis. Our glycan design pipeline is a promising way to improve disease through the targeted enhancement of specific microbes.

研究领域: 微生物学 · 肠道健康 · 分子生物学
✓ 已验证 DOI 高影响因子
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ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS · 2019 · IF 3.559

Syringin protects against colitis by ameliorating inflammation

Haihua Zhang,Haijun Gu,Qinghui Jia,Yanqing Zhao,Hongqiang Li,Shurui Shen,Xin Liu,Guisheng Wang,Qiumei Shi

Inflammatory bowel disease (IBD) is a chronic inflammatory condition with high incidence. Syringin exhibits multiple pharmacological properties, including anti-inflammatory effects. However, the effect of syringin on inflammation of IBD is still unclear. Here, the dextran sulfate sodium (DSS)-induced colitis model was established in vivo . Rat intestinal epithelium IEC6 cells were treated with lipopolysaccharide (LPS) in vitro . Syringin inhibited DSS or LPS-induced overproduction of proinflammatory cytokines (IL-1β, IL-6, TNF-α) and proinflammatory substances (iNOS, COX-2). Moreover, syringin inactivated the proinflammatory NF-κB p65 pathway by decreasing IκBα phosphorylation at Ser 32. The activation of antioxidant Nrf2 signaling pathway was promoted by syringin. Additionally, LPS-induced inflammation in IEC6 cells was also suppressed by NF-κB inhibitor PDTC and Nrf2 activator RTA408. The anti-inflammatory effects of syringin were comparable to these two reagents. Taken together, our results suggest that syringin shows protective effects on intestinal inflammation through inhibiting NF-κB, while activating Nrf2 signaling pathway in colitis.

CAS / MDL: 11061-68-0
研究领域: 药理学 · 免疫学 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2024 · IF 6

Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition

Zhiran Ju,Junde Xu,Keshuang Tang,Fener Chen

COX-2/NLPR3-targeted therapy might be beneficial for the inflammation diseases. To discover novel anti-inflammatory compounds with favorable safety profiles, three new series of non-carboxylic diclofenac analogues bearing various ring systems, such as oxadiazoles 4a - 4w , triazoles 6a - 6m , and cyclic imides 7a and 7b , were synthesized. The synthesized analogues were evaluated for their inhibitory activity against COX-2 enzyme. Among them, compound 6k exhibited potent selective COX-2 inhibition (IC 50  = 1.53 μM; selectivity ((IC 50 (COX-1)/IC 50 (COX-2) = 17.19). Treatment with compound 6k effectively suppressed the NF-κB/NLRP3 signaling pathway, resulting in reduced expression of pro-inflammatory factors. The in vivo ulcerative colitis assay demonstrated that compound 6k significantly ameliorated histological damages and showed strong protection against DSS-induced acute colitis. The collected results indicated that compound 6k displays anti-inflammatory activity through COX-2/NLRP3 inhibition. Therefore, compound 6k represents a promising candidate for further development as a new lead compound with reduced colitis side effects.

研究领域: 药理学 · 药物化学 · 炎症研究
✓ 已验证 DOI PubMed 高影响因子
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