intestinal inflammatory

Acotiamide monohydrochloride trihydrate (Z-338 HCl) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.

Oxazolone is a haptenating agent that can induce models of acute or chronic colitis and atopic dermatitis. It activates Th1 Th2 responses, leading to weight loss and diarrhea, and the resulting inflammation can be alleviated by anti-IL-4 antibodies, anti-TNF-α antibodies, or IL-13R2α-Fc fusion proteins. It is also suitable for studying gene expression related to inflammatory bowel disease in zebrafish.

Dersalazine (Dersalazine Free Base), an inhibitor of platelet-activating factor, exerts intestinal anti-inflammatory activity in different rodent types of colitis by down-regulating IL-17 expression, with potential efficacy in patients with ulcerative colitis.

Dextran sulfate sodium salt (MW 4500-5500) is a polymer of dehydrated glucose and an inhibitor of complement and coagulation pathways. Dextran sulfate sodium salt (MW 4500-5500) can be used as an anticoagulant, antiviral agent and antilipidemic agent. Dextran sulfate sodium salt (MW 4500-5500) can prevent the HIV-1 virus from adsorbing onto host cells. Dextran sulfate sodium salt (MW 4500-5500) can inhibit NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 4500-5500) can inhibit the immediate blood-mediated inflammatory response (IBMIR).

Dextran sulfate sodium salt (MW 36,000–50,000) is a medium molecular weight polyanionic dextran derivative with strong intestinal epithelial permeability. It is the most commonly used agent for inducing inflammatory bowel disease (IBD) models, effectively inducing both acute and chronic colitis. Its mechanism may involve macrophage dysfunction and gut microbiota dysbiosis. Due to its colonic epithelial toxicity, long-term use can also induce colorectal cancer models.

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

3-Indoleacrylic acid is a metabolite of tryptophan produced by Peptostreptococcus species. 3-Indoleacrylic acid has a beneficial effect on intestinal epithelial barrier function and mitigates inflammatory responses by immune cells.

Thalifendine is one of the main products of Berberine demethylation catalyzed by CYP51 (secreted by intestinal flora), which has anti-inflammatory effects, reduces intestinal inflammation, improves intestinal barrier function, and reduces the production of inflammatory factors.

Terlipressin Acetate, a highly selective vasopressin V1 receptor agonist, on oxygen and glucose deprivation/re-oxygenation (OGD/R)-induced damage in intestinal epithelial cells (IEC-6).Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

L-Homocysteine is a biological thiol involved in various diseases and pathological conditions. It is a marker for atherosclerosis and can exacerbate intestinal inflammation in inflammatory bowel disease (IBD) by promoting the expression of 5-LOX and COX-2, making it suitable for inducing vascular endothelial inflammation models.

Stercobilin hydrochloride (mixture of isomers) is a bile pigment metabolized by intestinal bacteria and also acts as an inhibitor of HIV protease (HIVProtease) with a Ki of 4 μM. This compound can induce pro-inflammatory activity in mouse macrophage RAW264 cells, including the production of TNF-α and IL-1β. Stercobilin hydrochloride (mixture of isomers) is utilized in research on inflammation and viral infections.

X-17 is a potent Vanin-1 inhibitor known for its anti-inflammatory and antioxidant properties. It reduces the expression of inflammatory factors and inhibits myeloperoxidase activity, while enhancing colonic glutathione reserves and restoring the intestinal barrier.

ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 μM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.

Deprodone is an active compound that inhibits key processes such as bacterial cell wall synthesis by interacting with hydrolase and transferase proteins of methicillin-resistant Staphylococcus aureus (MRSA). It is applied in the research of MRSA infections, inflammatory skin diseases, intestinal disorders, and fatty acid metabolism disorders.

4-Iodobutyl benzoate is structurally related to bicyclic heterocyclic compounds such as indole and indoline. It functions as a metabolite of drug amides and is utilized in the treatment of inflammatory bowel disease, degenerative diseases, and intestinal disorders. 4-Iodobutyl benzoate inhibits the activity of proteolytic enzymes by binding to their active sites.

DHMB (2,3-Dihydroxy-4-Methoxybenzaldehyde) exerts protective effects on intestinal epithelial cells. DHMB exhibits anti-inflammatory and antifungal capacity.

Acotiamide is an orally active, selective, and reversible acetylcholinesterase (AChE) inhibitor with an IC50 of 1.79 μM. It is a gastroprokinetic agent that enhances gastric contractility and accelerates delayed gastric emptying, with potential for research in functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory [1] [2] [3].

3,4-DAA has anti-inflammatory activity, ameliorates acute hepatic allograft injury, and alleviates severe acute pancreatitis by inhibiting intestinal barrier dysfunction and NF-κB activation.3,4-DAA inhibits EOC20 cell-inducible nitric oxide synthase (iNOS) induced by IFN-γ and lipopolysaccharide.

κ-Carrageenan is a natural polymer predominantly found in red seaweeds that can serve as an effective carrier to deliver curcumin to cancer cells and induce apoptosis. It can also be used to induce paw swelling models and acts as a potential inflammatory agent that amplifies existing intestinal inflammation.

GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addition, GSK143 exhibits promising anti-inflammatory properties by reducing inflammation and impeding the recruitment of immune cells in the intestinal muscularis of mice.

GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The compound demonstrates anti-inflammatory properties and hinders the recruitment of immune cells in the intestinal muscularis of mice.

Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1/mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell culture. It possesses anti-inflammatory actions via inhibition of Cox (cyclooxygenase) and inhibits Cl-/HCO3- exchange activity. It also increases survival in a cystic fibrosis mouse model of the distal intestinal obstructive syndrome.

Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) is an agonist for the human Aryl Hydrocarbon Receptor (AhR), a key regulator of immune-inflammatory conditions. A metabolite of tryptophan derived from dietary protein, it is produced by intestinal bacteria and metabolized in the liver. In chronic kidney disease patients with impaired renal function, it accumulates in serum as a uremic toxin, inducing oxidative stress and accelerating disease progression. At 250 μM, it activates NF-Κb, promoting TGF-β1 and Smad3 expression in rat proximal tubular cells, which is associated with profibrotic activity.

Aloin B (Isobarbaloin) is an isomer of aloin.1. The extract of A. vera and its active ingredient aloin cause melanin aggregation leading to skin lightening via alpha adrenergic receptor stimulation, the result opens new vistas for the use of A. vera regarding its clinical application as a new nontoxic melanolytic agent for the treatment of hyperpigmentation. 2. Dietary supplementation of aloe components (aloin, aloesin and aloe-gel) can ameliorate intestinal inflammatory responses in a 3% dextran sulfate sodium (DSS)-induced ulcerative colitis rat model, in particular, aloesin is the most potent inhibitor.