摘要
血小板活化因子(PAF)是一种与炎症及过敏有关的脂类介质。应用PAF受体结合实验检测近20种自中草药海风藤、山蒟、樟叶胡椒、石南藤分离的新木脂素类化合物,其中14种为新结构。总结了波谱鉴定的一些规律。首次证明双环辛烷类、8,O,4’、8,3’三种新木脂素的结构骨架有PAF受体拮抗活性,第一类具强活性。并探讨了立体结构与活性的关系。
Platelet activating factor(PAF) is a recently discovered lipid mediator of hypersensitivity and inf-lammation. Studies have implicated PAF in such diseases as asthma, cardiac anaphylaxis, inflammationand arthritis. Using the PAF induced platelet aggregation assay as a guide, seventeen Piper plant spec-ies were screened, and a good number of PAF antagonistic neolignans were isolated from Piper kads-ura, P.hancei, P.wallichii and P.polysyphorum. The potent PAF antagonist kadsurenone were isolated fromthe former three species. The isolates of eight bicyclo(3,2,1)octane neolignans, four 8,3'-neolignansand two 8-O-4'-neolignans are new compounds. The configuration determination of bicyclo(3,2,1)oct-ane neolignans were summarized. All the isolates were tested on the [~3H] PAF receptor binding assay.Bicyclo(3,2,1)octane neolignans demonstrated potent PAF antagonistic properties. The 8, 3'-neolignansand 8-O-4'-neolignans were also found to be active. The structure-activity relationship was discussed.
出处
《北京医科大学学报》
CSCD
1992年第4期347-350,共4页
Journal of Peking University(Health Sciences)
基金
国家自然科学基金
关键词
血小板
活化因子
木脂素
胡椒属
Platelet activating factor
PAF antagonist
Neolignans