Ballesteros J F, Sanz M J, Ubeda A, Miranda M A, Iborra S, Payá M, Alcaraz M J
Departamento de Farmacología, Universidad de Valencia, Facultad de Farmacia, Burjassot, Spain.
J Med Chem. 1995 Jul 7;38(14):2794-7. doi: 10.1021/jm00014a032.
2'-Hydroxy-3,4-dimethoxy-3',4'-dimethylchalcone (3a), 2'-hydroxy-3',4',3,4-tetramethoxychalcone (3b), and their corresponding flavones, 3',4'-dimethoxy-7,8-dimethylflavone (4a) and 3',4',7,8-tetramethoxyflavone (4b), were prepared from 3,4-dimethoxycinnamic acid and the respective phenol. The four compounds inhibited enzymic lipid peroxidation and showed weak peroxyl scavenging activity. They also reduced LTB4 release from human neutrophils stimulated by A23187. The chalcone 3b was the only compound able to inhibit in a concentration-dependent way, synovial human recombinant phospholipase A2 activity, human platelet TXB2 generation, and human neutrophil degranulation. This chalcone exerted topical antiinflammatory effects in mice.
