Esculetin has been described as an inhibitor of tyrosinase and polyphenol oxidase and, therefore, of melanogenesis. In this work, we demonstrate that esculetin is not an inhibitor but a substrate of mushroom polyphenol oxidase (PPO) and horseradish peroxidase (POD), enzymes which oxidize esculetin, generating its o-quinone. Since o-quinones are very unstable, the usual way of determining the en...

Chronic allograft damage, defined by interstitial fibrosis and tubular atrophy (IF/TA), is a leading cause of allograft failure. Few effective therapeutic options are available to prevent the progression of IF/TA. We applied a meta-analysis approach on IF/TA molecular datasets in Gene Expression Omnibus to identify a robust 85-gene signature, which was used for computational drug repurposing an...

BACKGROUND Umbelliferone, also known as 7-hydroxycoumarin, is a phenolic metabolite found in many familiar plants. Its derivatives have been shown to have various pharmacological and chemo-preventive effects on human health. A uridine diphosphate glycosyltransferase YjiC from Bacillus licheniformis DSM 13, a cytochrome P450BM3 (CYP450 BM3) variant namely mutant 13 (M13) from Bacillus megaterium...

Activation of hepatic stellate cells (HSC) leads to initiation and progression fibrosis. HSC senescence is inversely correlated with proliferation activation. Therefore, induction may be a strategy treat Coumarin-derivatives like esculetin have been suggested inhibit fibrogenic cells. in this study we aimed investigate the effect on activation . Primary rat were used all experiments. Real-time ...

Esculetin, a hydroxycoumarin, has been reported to have neuroprotective action against several neurotoxins. Aluminum, nonessential element and potent neurotoxin, suggested link with the etiology progression of Alzheimer's disease (AD). In this experiment, possible role esculetin on aluminium chloride mediated cognitive impairments in rats was investigated. Rats were orally treated aluminum (100...

We investigated the effects of piroxicam, a cyclooxygenase inhibitor, and esculetin, a lipoxygenase inhibitor, on 7,12-dimethylbenz[a]anthracene (DMBA)-induced mammary carcinogenesis in female rats. Seven days after receiving a 5-mg dose of DMBA, rats were fed either a high-fat (20% soybean oil) or low-fat (0.5% soybean oil) diet. One third of the rats received diets containing 0.01% piroxicam ...

OBJECTIVES Esculetin (6,7-dihydroxycoumarin) is a natural coumarin with anti-oxidant, anti-inflammatory and anti-nociceptive activity. It acts as a potent inhibitor of lipoxygenases (5-LOX and 12-LOX) and decreases the production of matrix metalloproteinases (MMP-1, MMP-3 and MMP-9). Because both inhibition of lipoxygenases and inhibition of matrix metalloproteinases are effective strategies in...

An optimized, sensitive and validated reversed-phase high-performance liquid chromatography (RP-HPLC) method with UV detection is described for simultaneous determination of esculin and its aglycone, esculetin, in rat plasma. After addition of internal standard (chrysin), plasma samples were pretreated by solid-phase extraction and introduced into the HPLC system. Analytes were separated on a R...

One of the most frequent genetic aberrations in acute myeloid leukemia (AML) is chromosomal translocation between AML1/RUNX1 on chromosome 21 and ETO gene on chromosome 8 resulting in the expression of chimeric oncogene AML1-ETO. Although patients with t(8;21) translocation have good prognosis, 5-year survival is observed only in 50% of the cases. AML1-ETO translocation is usually accompanied b...

Commercially available dyes of the esculetin and alizarin families are identified as lead structures for constructing ratiometric fluorescent probes for zinc ions.