Aida Y, Kasama T, Takeuchi N, Tobinaga S
Showa College of Pharmaceutical Sciences, Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1995 May;43(5):859-67. doi: 10.1248/cpb.43.859.
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)
白花前胡（Peucedanum praeruptorum DUUN.）中的凯刺酮类化合物，包括前胡素A（= Pd-Ia，2）和前胡素B（= Pd-II，11），在检测的各种聚集剂中，对血小板活化因子（PAF）诱导的血小板聚集具有特异性拮抗作用，代表了一类新型的PAF拮抗剂。我们研究了20种化合物对PAF诱导的血小板聚集以及对组胺和白三烯D4（LTD4）诱导的豚鼠离体回肠收缩的影响。化合物2、（±）-顺式-3'，4'-二乙酰基凯刺酮（3）、（±）-顺式-4'-乙酰基-3'-巴豆酰基凯刺酮（5）、（±）-顺式-4'-乙酰基-3'-四氢呋喃甲酰基凯刺酮（6）、（±）-顺式-4'-乙酰基-3'-惕各酰基凯刺酮（7）、（±）-顺式-4'-乙酰基-3'-（2''-甲基丁酰基）凯刺酮（8）、（±）-顺式-3'，4'-二惕各酰基凯刺酮（10）和11均强烈抑制PAF诱导的血小板聚集。（±）-顺式-
