Chloride channel inhibition by a red wine extract and a synthetic small molecule prevents rotaviral secretory diarrhoea in neonatal mice was written by Ko, Eun-A.;Jin, Byung-Ju;Namkung, Wan;Ma, Tonghui;Thiagarajah, Jay R.;Verkman, A. S.. And the article was included in Gut in 2014.Product Details of 1003-07-2 This article mentions the following:
Background Rotavirus is the most common cause of severe secretory diarrhoea in infants and young children globally. The rotaviral enterotoxin, NSP4, has been proposed to stimulate calcium-activated chloride channels (CaCC) on the apical plasma membrane of intestinal epithelial cells. We previously identified red wine and small mol. CaCC inhibitors. Objective To investigate the efficacy of a red wine extract and a synthetic small mol., CaCCinh-A01, in inhibiting intestinal CaCCs and rotaviral diarrhoea. Design Inhibition of CaCC-dependent current was measured in T84 cells and mouse ileum. The effectiveness of an orally administered wine extract and CaCCinh-A01 in inhibiting diarrhoea in vivo was determined in a neonatal mouse model of rotaviral infection. Results Screening of ∼150 red wines revealed a Cabernet Sauvignon that inhibited CaCC current in T84 cells with IC50 at a ∼1:200 dilution, and higher concentrations producing 100% inhibition. A >1 kdalton wine extract prepared by dialysis, which retained full inhibition activity, blocked CaCC current in T84 cells and mouse intestine. In rotavirus-inoculated mice, oral administration of the wine extract prevented diarrhoea by inhibition of intestinal fluid secretion without affecting rotaviral infection. The wine extract did not inhibit the cystic fibrosis chloride channel (CFTR) in cell cultures, nor did it prevent watery stools in neonatal mice administered cholera toxin, which activates CFTR-dependent fluid secretion. CaCCinh-A01 also inhibited rotaviral diarrhoea. Conclusions Our results support a pathogenic role for enterocyte CaCCs in rotaviral diarrhoea and demonstrate the antidiarrhoeal action of CaCC inhibition by an alc.-free, red wine extract and by a synthetic small mol. In the experiment, the researchers used many compounds, for example, Isothiazol-3(2H)-one (cas: 1003-07-2Product Details of 1003-07-2).
Isothiazol-3(2H)-one (cas: 1003-07-2) belongs to isothiazole derivatives. Isothiazole is more toxic than pyridine. But the more substituted isothiazoles are usually far less toxic. Many compounds with an isothiazole scaffold demonstrated a wide range of biological profiles, including antiinflammatory, antithrombotic, and anticonvulsive agents.Product Details of 1003-07-2
Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com