Disease relevance of C09321

• Inhibitory effects of synthetic 2'-hydroxychalcone derivatives on rat lens aldose reductase (RLAR) and on platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications [1].
• Since most breast cancers received estrogen supplied from local tissues, we employed a breast cancer cell line expressing aromatase to screen for the inhibitory potentials of five hydroxychalcones, i.e. 2-hydroxychalcone, 2'-hydroxychalcone, 4-hydroxychalcone, 4,2',4'-trihydroxy-chalcone (isoquiritigenin), 3,4,2',4'-tetrahydroxychalcone (butein) [2].

High impact information on C09321

• 2'-hydroxychalcone inhibits the induction of steady-state transcript levels of ICAM-1, VCAM-1, and E-selectin by tumor necrosis factor-alpha as determined by reverse transcription-polymerase chain reaction, and therefore it may interfere with the transcription of their genes [3].
• We demonstrate here that 2'-hydroxychalcone inhibits the adhesion of peripheral neutrophils to the endothelial cell monolayers by inhibiting the expression of ICAM-1, VCAM-1, and E-selectin in a concentration-dependent manner [3].
• Heme oxygenase-1 mediates the anti-inflammatory actions of 2'-hydroxychalcone in RAW 264.7 murine macrophages [4].
• These findings suggest that the inhibition of the LPS-induced production of NO and TNF-alpha by the 2'-hydroxychalcone derivatives is due to the inhibition of NF-kappaB and AP-1 activations [5].
• Inhibition of lipopolysaccharide-induced expression of inducible nitric oxide synthase and tumor necrosis factor-alpha by 2'-hydroxychalcone derivatives in RAW 264.7 cells [5].

Biological context of C09321

• However, reporter gene assays indicated that 2'-hydroxychalcone suppressed XRE-transactivation, whereas 2-hydroxychalcone induced it when 7,12-dimethylbenz[a]anthracene (DMBA) was co-administered [6].
• Mechanistic approach to the cyclization reaction of a 2'-hydroxychalcone analogue with light and solvent [7].

Associations of C09321 with other chemical compounds

• In this study, we investigated the anti-inflammatory action of 2'-hydroxychalcone (2-HC) in a model of lipopolysaccharide (LPS)-induced inflammation in RAW 264.7 macrophages and examined the role of HO-1 in this process [4].
• Synthesis and PPAR-gamma ligand-binding activity of the new series of 2'-hydroxychalcone and thiazolidinedione derivatives [8].
• These findings suggest that 4'-methoxyl and 6'-methoxyl groups are required for the expression of more potent inhibitory activity against PGE2 production, and that the inhibition of PGE2 production by these 2'-hydroxychalcone derivatives is due to the inhibition of TPA-induced COX-2 protein expression [9].

References