New lipoxygenase inhibitors isolated from Chinese plants. Development of new anti-allergic drugs.
Some natural compounds isolated from Chinese plants were found to have strong inhibitory activity for 5-lipoxygenase and were thus able to inhibit leucotriene synthesis. Among these compounds, caffeic acid was selected for study; more than 100 of its derivatives were synthesized and tested for 5-lipoxygenase inhibitory activity. Two derivatives, TMK-919 and TMK-920, proved to be 100 times more potent than the parent compound and were able to inhibit the homologous PCA reaction significantly in rats at a dose of 10 mg/kg, i.v.
D000818:Animals; D001091:Arachidonate Lipoxygenases / Q000037:antagonists & inhibitors*; D001249:Asthma / Q000188:drug therapy; D002109:Caffeic Acids / Q000302:isolation & purification / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification*; D016859:Lipoxygenase Inhibitors; D008297:Male; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013189:SRS-A / Q000096:biosynthesis
D002109:Caffeic Acids; D004365:Drugs, Chinese Herbal; D016859:Lipoxygenase Inhibitors; D013189:SRS-A; D001091:Arachidonate Lipoxygenases