title: 2',5'-Dihydroxychalcone as a potent chemical mediator and cyclooxygenase inhibitor.
abstract: Eleven chalcone derivatives have been tested for their inhibitory effects on platelet aggregation in rabbit platelet suspension and the activation of mast cells and neutrophils. Arachidonic acid-induced platelet aggregation was potently inhibited by almost all the compounds and some also had a potent inhibitory effect on collagen-induced platelet aggregation and cyclooxygenase. Some hydroxychalcone derivatives showed strong inhibitory effects on the release of beta-glucuronidase and lysozyme, and on superoxide formation by rat neutrophils stimulated with the peptide fMet-Leu-Phe (fMLP). We found that the anti-inflammatory effect of 2',5'-dihydroxychalcone was greater than that of trifluoperazine. 2'5'-Dihydroxy and 2',3,4,5'-tetrahydroxyl chalcones, even at low concentration (50 microM), tested in platelet-rich plasma from man almost completely inhibited secondary aggregation induced by adrenaline. These results suggest that the anti-platelet effects of the chalcones are mainly a result of inhibition of thromboxane formation.
authors.affiliation: School of Pharmacy, Kaohsiung Medical College, Taiwan, ROC.
authors.forename: C N
authors.initials: CN
authors.lastname: Lin
authors.forename: T H
authors.initials: TH
authors.lastname: Lee
authors.forename: M F
authors.initials: MF
authors.lastname: Hsu
authors.forename: J P
authors.initials: JP
authors.lastname: Wang
authors.forename: F N
authors.initials: FN
authors.lastname: Ko
authors.forename: C M
authors.initials: CM
authors.lastname: Teng
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D016718:Arachidonic Acid / Q000494:pharmacology; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D047188:Chalcones; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D007213:Indomethacin / Q000494:pharmacology; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D010972:Platelet Activating Factor / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000494:pharmacology
chemical_list: C107497:2',5'-dihydroxychalcone; D000894:Anti-Inflammatory Agents, Non-Steroidal; D047188:Chalcones; D016861:Cyclooxygenase Inhibitors; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D016718:Arachidonic Acid; D009240:N-Formylmethionine Leucyl-Phenylalanine; D002599:Chalcone; D013917:Thrombin; D007213:Indomethacin