intestinal disease

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.

Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,

Ursodeoxycholic acid (UDCA) is a potent inhibitor of liver-specific fatty acid transporter 5 (FATP5). Ursodeoxycholic acid inhibits cholesterol absorption and is used to dissolve gallstones.

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.

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.

Deoxycholic acid (DCA) is a natural product and a TGR5 receptor agonist with cell permeability and oral activity. As a metabolite of intestinal flora, this compound is widely used in research on bile acid signal transduction, glucose and lipid metabolism, and anti-inflammatory mechanisms, and has shown therapeutic potential in diabetes and liver disease models.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Vitexin 2''-glucoside (Flavosativaside) is a potent and selective alpha-glucosidase inhibitor found in hawthorn leaf flavonoids. Vitexin 2''-glucoside reversibly inhibits α-glucosidase activity on the brush border of the small intestine, with stronger inhibitory activity than acarbose. Vitexin 2''-glucoside is utilized in biomedical research focused on carbohydrate metabolism regulation, intestinal enzymatic activity, and glucose absorption pathway studies relevant to metabolic disease models.

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.

TU-100 is frequently used in the treatment of chronic gastrointestinal disorders, and it is commonly applied to alleviate symptoms such as abdominal pain, bloating, Crohn’s disease, irritable bowel syndrome, adhesive intestinal obstruction, and paralytic ileus. Additionally, TU-100 can improve gastrointestinal motility abnormalities in patients with grade B liver impairment after hepatectomy and reduce serum CRP levels.

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.

Triethylenetetramine (Trientine) tetrahydrochloride is an orally active, potent, and selective copper chelator. It aids in the excretion of divalent copper ions from the body, reduces intestinal copper absorption, and minimizes copper accumulation. Additionally, Triethylenetetramine tetrahydrochloride exhibits potential anticancer properties through mechanisms such as telomerase inhibition, anti-angiogenesis, and promoting cancer cell apoptosis (apoptosis). This compound shows promise in the study of Wilson's disease, cancer, and diabetic complications.

Cholic acid-Glu is a derivative of Cholic acid. Its abundance rises in Crohn's disease. This compound can enhance the activation of PXR in intestinal organoid tissues and significantly increase the expression of the downstream PXR target gene, Cyp3a11.

t9,t11,c15-CLNA is an isomer of conjugated linolenic acid (CLNA) produced by Lactobacillus plantarum ZS2058. It exhibits key activities including anti-inflammatory and antioxidant effects, as well as enhancement of intestinal barrier function. The regulatory mechanisms of t9,t11,c15-CLNA involve the upregulation of tight junction proteins, the inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6), and the activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be utilized in research on inflammatory bowel disease (like colitis).

sEH-IN-21 is an orally active inhibitor of sEH, exhibiting IC50 values of 0.1 nM for both hsEH and msEH. It significantly suppresses the NF-κB signaling pathway. sEH-IN-21 demonstrates potent anti-inflammatory activity by reducing IL-6 and TNF-α release and maintaining intestinal barrier integrity. It is applicable in research on inflammatory bowel disease (IBD).

IMU-856 is an orally active, systemic small molecule modulator of SIRT6. It effectively and selectively inhibits the deacetylase activity of SIRT6 while enhancing the protein levels of SIRT6. IMU-856 has the potential to restore intestinal barrier function and can be used in research on celiac disease.

Loperamide oxide (R 58425) is a secreted antidiarrheal agent that increases peristalsis and inhibits intestinal absorption of water and ions and is used in the study of chronic diarrhea in patients with Crohn's disease.

Methantheline Bromide is a synthetic spasmolytic used to relieve cramps or spasms of the stomach, bowel, and bladder. It is also useful for intestinal or gastric ulcers (peptic ulcer disease), intestinal problems, pancreatitis, gastritis, biliary dysmotil

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.

AT-1001 (Larazotide) is an orally active tight junction regulator and Zonulin antagonist. It reduces intestinal permeability in celiac and inflammatory bowel disease models by blocking Zonulin receptor signaling to maintain the integrity of epithelial tight junctions.

Glepaglutide (ZP1848), a long-acting glucagon-like peptide-2 (GLP-2) analogue, functions as a potent GLP-2 receptor (GLP-2R) agonist, effectively reducing fecal output and enhancing intestinal absorption while alleviating small intestine inflammation. It holds potential for researching inflammatory bowel disease (IBD) and Crohn's disease [1] [2] [3].

Glepaglutide (ZP1848) acetate is a long-acting glucagon-like peptide-2 (GLP-2) analogue and a potent GLP-2 receptor (GLP-2R) agonist. It significantly reduces fecal output and enhances intestinal absorption while also mitigating inflammation in the small intestine. Glepaglutide acetate is relevant in researching inflammatory bowel disease (IBD) and Crohn's disease [1] [2] [3].

Etrolizumab (rhuMAb Beta7) is a humanized intestinal-selective anti-β7 integrin monoclonal antibody that selectively blocks the transport and retention of lymphocytes in the intestinal tract for the study of inflammatory bowel disease (IBD).

ROCK-IN-8 (Example 4), a ROCK inhibitor, exhibits anti-inflammatory properties and is suitable for respiratory and gastro-intestinal disease research, demonstrating an IC50 value below 100 nM [1].