scholarly journals Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease

MedChemComm ◽  
2018 ◽  
Vol 9 (8) ◽  
pp. 1305-1310 ◽  
Author(s):  
Sang Won Park ◽  
Suhrid Banskota ◽  
Pallavi Gurung ◽  
You Jin Jin ◽  
Han-eol Kang ◽  
...  

Novel series of anti-inflammatory bowel disease (IBD) agent was identified through TNF-α-induced cell adhesion.

2021 ◽  
Vol 11 (4) ◽  
pp. 1629
Author(s):  
Vanessa Mateus ◽  
João Estarreja ◽  
Inês Silva ◽  
Paulo Barracosa ◽  
Edite Teixeira-Lemos ◽  
...  

Background: Cynara cardunculus L. var. altilis (DC) is a plant generally associated as an ingredient in the Mediterranean diet. The polyphenols present in this plant provide pharmacological and nutritional properties. C. cardunculus L. has been used throughout animal studies, which demonstrated an anti-inflammatory effect. Inflammatory bowel disease (IBD) is a chronic inflammatory disorder of the gastrointestinal tract. Since there is not a known cure, the research of new possible pharmacological approaches is essential. This study aims to evaluate the effect of an aqueous extract of C. cardunculus L. dry leaves in a 2,4,6-Trinitrobenzenesulfonic acid (TNBS)-induced colitis model. Methods: CD-1 mice with TNBS-induced colitis received an intraperitoneal (IP) administration of C. cardunculus L. once per day for 4 days. Results: The C. cardunculus L. demonstrated a beneficial effect in this experimental model of IBD with anti-inflammatory action through the reduction of tumor necrosis factor (TNF)-α levels. It also demonstrated a beneficial influence on the extra-intestinal manifestations related to IBD, with the absence of significant side effects of its use. Conclusions: The extract of C. cardunculus L. dry leaves can become an interesting tool for new possible pharmacological approaches in the management of IBD.


Author(s):  
Zhang Min ◽  
Hao Xiaona ◽  
Tariq Aziz ◽  
Zhang Jian ◽  
Yang Zhennai

Exopolysaccharides (EPSs) possess many bioactivities such as immune regulation, antioxidant, anti-tumor and modulation of intestinal microbial balance but their direct effect on inflammatory bowel disease (IBD) response has not been studied. The purpose of this study was to evaluate the anti-inflammatory effect of EPS produced by L. plantarum YW11 administered at different dosages in IBD mouse model induced with 5% dextran sulphate sodium (DSS). The DSS-induced colitis, accompanied by body weight loss, reduction of colon coefficient and histological colon injury was considerably ameliorated in mice fed the EPS (10 mg/kg). The middle dose of the EPS (25 mg/kg) could effectively recover the intestinal microbial diversity and increase the abundance of Roseburia, Ruminococcus and Blautia with increased content of butyric acid. Moreover, EPS also reduced the production of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, IFN-γ, IL-12 and IL-18) and enhanced the anti-inflammatory cytokine IL-10. This study showed that EPS might help in modulation of gut microbiota and improve the immunity of the host to reduce the risk of IBD symptoms.


Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 464 ◽  
Author(s):  
Jaemin Lee ◽  
Han-Seok Choi ◽  
Jinkyung Lee ◽  
Jimin Park ◽  
Sang-Back Kim ◽  
...  

Many medicinal plants have been used traditionally in East Asia for the treatment of gastrointestinal disease and inflammation. The aim of this study was to evaluate the anti-inflammatory activity of 350 extracts (175 water extracts and 175 ethanol extracts) from 71 single plants, 97 mixtures of two plants, and seven formulations based on traditional medicine, to find herbal formulations to treat inflammatory bowel disease (IBD). In the in vitro screening, nitric oxide (NO), tumor necrosis factor (TNF)-α, and interleukin (IL)-6 levels were determined in LPS-treated RAW264.7 cells and the TNF-α induced monocyte-epithelial cell adhesion assay was used for the evaluation of the anti-inflammatory activity of the compounds. Dextran sulfate sodium (DSS)-induced colitis model and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis model were used to evaluate the therapeutic effect against IBD of the samples selected from the in vitro screening. KM1608, composed of Zingiber officinale, Terminalia chebula and Aucklandia lappa, was prepared based on the screening experiments. The oral administration of KM1608 significantly attenuated the severity of colitis symptoms, such as weight loss, diarrhea, and rectal bleeding, in TNBS-induced colitis. In addition, inflammatory mediators, such as myeloperoxidase, TNF-α, and IL-6 levels decreased in the lysate of colon tissues treated with KM1608. Collectively, KM1608 ameliorated colitis through the regulation of inflammatory responses within the colon, which indicated that KM1608 had potential for the treatment of IBD.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Tzu-Fan Chen ◽  
Jeh-Ting Hsu ◽  
Kun-Chang Wu ◽  
Che-Fang Hsiao ◽  
Jou-An Lin ◽  
...  

Abstract Mu Dan Pi (MDP), also known as Moutan Cortex Radicis, is a traditional Chinese medicine used to treat autoimmune diseases. However, the impact of MDP and its principal active compounds on inflammatory bowel disease (IBD) is uncertain. This study therefore systemically assessed the anti-inflammatory effects of MDP and its known active compounds in IBD. The anti-inflammatory activities of water extract and individual compounds were screened by NF-κB and interferon regulatory factor (IRF) reporter assays in THP-1 cells induced with either Toll-like receptor or retinoic acid inducible gene I/melanoma differentiation-associated gene 5 activators and further verified in bone marrow-derived macrophages. MDP water extract significantly inhibited the activation of NF-κB and IRF reporters, downstream signaling pathways and the production of IL-6 and TNF-α, in a dose-dependent manner. Among 5 known active components identified from MDP (1,2,3,4,6-penta-O-galloyl-β-d-glucose [PGG], gallic acid, methyl gallate, paeoniflorin, and paeonol), PGG was the most efficient at inhibiting both reporters (with an IC50 of 5–10 µM) and downregulating IL-6 and TNF-α. Both MDP powder for clinical use and MDP water extract, but not PGG, reduced colitis and pathological changes in mice. MDP and its water extract show promise as a novel therapy for IBD patients.


2021 ◽  
Author(s):  
Xiao fan Song ◽  
Lei Qiao ◽  
Shuqi Yan ◽  
Yue Chen ◽  
Xina Dou ◽  
...  

Selenium (Se) as an essential micronutrient that has implications in human diseases, including inflammatory bowel disease (IBD), especially with respect to Se deficiencies. Recently, selenium nanoparticles (SeNPs) have attracted significant...


2021 ◽  
Vol 10 (5) ◽  
pp. 1040
Author(s):  
Jo L. W. Lambert ◽  
Sofie De Schepper ◽  
Reinhart Speeckaert

The biologic era has greatly improved the treatment of Crohn’s disease and ulcerative colitis. Biologics can however induce a wide variety of skin eruptions, especially those targeting the TNF-α and Th17 pathway. These include infusion reactions, eczema, psoriasis, lupus, alopecia areata, vitiligo, lichenoid reactions, granulomatous disorders, vasculitis, skin cancer, and cutaneous infections. It is important to recognize these conditions as treatment-induced adverse reactions and adapt the treatment strategy accordingly. Some conditions can be treated topically while others require cessation or switch of the biological therapy. TNF-α antagonists have the highest rate adverse skin eruptions followed by ustekinumab and anti-integrin receptor blockers. In this review, we provide an overview of the most common skin eruptions which can be encountered in clinical practice when treating IBD (Inflammatory bowel disease) patients and propose a therapeutic approach for each condition.


2008 ◽  
Vol 94 (2) ◽  
pp. 341-347 ◽  
Author(s):  
G. M. SCHUERMANN ◽  
A. E. ABER-BISHOP ◽  
P. FACER ◽  
J. C. LEE ◽  
D. S. RAMPTON ◽  
...  

Nutrients ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 1067
Author(s):  
Marjo J. E. Campmans-Kuijpers ◽  
Gerard Dijkstra

Diet plays a pivotal role in the onset and course of inflammatory bowel disease (IBD). Patients are keen to know what to eat to reduce symptoms and flares, but dietary guidelines are lacking. To advice patients, an overview of the current evidence on food (group) level is needed. This narrative review studies the effects of food (groups) on the onset and course of IBD and if not available the effects in healthy subjects or animal and in vitro IBD models. Based on this evidence the Groningen anti-inflammatory diet (GrAID) was designed and compared on food (group) level to other existing IBD diets. Although on several foods conflicting results were found, this review provides patients a good overview. Based on this evidence, the GrAID consists of lean meat, eggs, fish, plain dairy (such as milk, yoghurt, kefir and hard cheeses), fruit, vegetables, legumes, wheat, coffee, tea and honey. Red meat, other dairy products and sugar should be limited. Canned and processed foods, alcohol and sweetened beverages should be avoided. This comprehensive review focuses on anti-inflammatory properties of foods providing IBD patients with the best evidence on which foods they should eat or avoid to reduce flares. This was used to design the GrAID.


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