The Antagonistic Effects of Khellactones on Platelet-Activating Factor, Histamine, and Leukotriene D4.
Copyright policy )The Antagonistic Effects of Khellactones on Platelet-Activating Factor, Histamine, and Leukotriene D4.
Khellactones of Peucedanum praeruptorum DUUN., including praeruptorins A (= Pd-Ia, 2) and B (= Pd-II,11), had an antagonistic effect specifically on platelet aggregation induced by platelet activating factor (PAF) among various aggregating agents examined, and represent a new class of PAF antagonists. We examined the effects of twenty compounds on PAF-induced platelet aggregation and on histamine- and leukotriene D4 (LTD4)-induced contractions in isolated guinea pig ileum. Compounds 2, (+/-)-cis-3',4'-diacetylkhellactone (3), (+/-)-cis-4'-acetyl-3'-crotonoylkhellactone (5), (+/-)-cis-4'-acetyl-3'-tetrolylkhellactone (6), (+/-)-cis-4'-acetyl-3'-tigloylkhellactone (7), (+/-)-cis-4'-acetyl-3'-(2"-methylbutyryl)khellactone (8), (+/-)-cis-3',4'-ditigloylkhellactone (10), and 11 all strongly inhibited PAF-induced platelet aggregation. (+/-)-cis-4'-Acetyl-3'-(2"-methyl-2"-dodecenoyl)khellactone (9), (+/-)-cis-4'-ethyl-3'-tigloylkhellactone (13), (+/-)-cis-4'-ethyl-3'-[N-(2"-triethylammonio)ethylcarbamoyl] khellactone iodide (16), (+/-)-trans-3',4'-diacetylkhellactone (18), (+/-)-trans-4'-acetyl-3'-crotonoylkhellactone (19), (+/-)-trans-4'-acetyl-3'-valerylkhellactone (20), (+/-)-trans-4'-acetyl-3'-isovalerylkhellactone (21), and (+/-)-trans-4'-acetyl-3'-tigloylkhellactone (22) were weakly inhibitory. Most of the compounds exhibited noncompetitive antagonist actions on histamine- and LTD4-induced contractions.(ABSTRACT TRUNCATED AT 250 WORDS)
Male, Platelet Aggregation, Plant Extracts, Guinea Pigs, Histamine Antagonists, Mice, Inbred Strains, Muscle, Smooth, In Vitro Techniques, Plant Roots, Leukotriene D4, Lactones, Mice, Coumarins, Ileum, Animals, Drug Interactions, Platelet Activating Factor, Platelet Aggregation Inhibitors, Histamine, Muscle Contraction
Male, Platelet Aggregation, Plant Extracts, Guinea Pigs, Histamine Antagonists, Mice, Inbred Strains, Muscle, Smooth, In Vitro Techniques, Plant Roots, Leukotriene D4, Lactones, Mice, Coumarins, Ileum, Animals, Drug Interactions, Platelet Activating Factor, Platelet Aggregation Inhibitors, Histamine, Muscle Contraction
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).25 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Average
Citations provided by BIP!Popularity provided by BIP!