Cloricromene, a semi-synthetic coumarin derivative, inhibits tumor necrosis factor-α production at a pre-transcriptional level

Cloricromene effect on the enzyme activities of the tryptophan–nicotinic acid pathway in diabetic/hyperlipidemic rabbits

“…Several mechanisms of action of the drug have been proposed and mainly focused on cell-to-cell interactions at the endothelial level; the drug blunts polymorphonuclear superoxide gener- ation and influences leukocyte function (Groban et al, 1998;Zatta and Bevilacqua, 1999;Bertocchi et al, 1989). The drug has been studied for its effects on the extension of myocardial damage and the production of oxygen free radicals during periods of ischemia and reperfusion; evidence has been found for a protective effect of cloricromene against myocardial ischemia -reperfusion injury (Zvara et al, 1997;Groban et al, 1998;Corsini et al, 2001;Milei et al, 1992) and for a regenerating property on rabbit aortic endothelium after cryoinduced vascular damage (Aliev et al, 1999). Another interesting field of application emerged from clinical studies suggesting a possible role of cloricromene for the treatment of intermittent claudication, in patients with moderate walking impairment (Gresele et al, 2000).…”

“…Cloricromene is a semi-synthetic coumarin derivative (ethyl({8-chloro-3-[2-(diethylamino) ethyl]-4-methyl-2-oxo-2H-1-benzopyran-7-yl}oxy) acetate) used as an antiplatelet drug with vasodilating and endothelium-protective activity (Squadrito et al, 1991;Hoult and Paya, 1996). The drug has been found to decrease myocardial infarct size after ischemic reperfusion injury (Squadrito et al, 1993;Zvara et al, 1997;Groban et al, 1998;Corsini et al, 2001) by inhibiting tumor necrosis factor-alpha (TNF-a) and plateletactivating factor. Cloricromene has been also found to protect rats from lipopolysaccharide-induced endotoxemia by blocking nuclear factor-nB activation, leading to inhibition of NO and TNF-a overproduction (Ianaro et al, 2004), reversing the lipopolysaccharide-induced vascular hyporeactivity.…”

Role of SP-1 in SDS-Induced Adipose Differentiation Related Protein Synthesis in Human Keratinocytes

“…Protein concentration was measured using a commercial kit (Bio-Rad). SP-1 activation was evaluated both by electrophoretic mobility shift assay (EMSA) as previously described (Corsini et al 2001), and by a specific colorimetric method using a commercially available kit (BD Mercury TransFactor kit, BDBio-sciences, San Jose, CA, U.S.A.). Briefly, the TransFactor kit is a 96-well plate with oligonucloetides containing the consensus binding sequence for each transcription factors coated on the wells.…”

Coumarinic derivatives show anti-inflammatory effects on alveolar macrophages, but their anti-elastase activity is essential to reduce lung inflammation in vivo

“…Several coumarins possess antioxidant capacity scavenging superoxide anion radicals [17,18], reduce edema in rat paw carrageenan test and other inflammatory rodent models [19], and inhibit both the lipoxygenase and cyclooxygenase pathways of arachidonic acid metabolism [20,21]. In murine macrophages, examples of coumarinic derivatives have been shown to inhibit lipopolysaccharide (LPS)-stimulated release of nitric oxide, interleukin (IL)-1β, IL-6, prostaglandin E 2 , and tumor necrosis factor (TNF) via the suppression of NF-кB activation [22][23][24].…”