胡椒属植物中木脂素类血小板活化因子拮抗活性成分及构效关系的研究

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。

THE STUDIES OF NATURAL PAF ANTAGONISTIC NEOLIGNANS FROM PIPER GENUS AND THEIR STRUCTURE-ACTIVITY RELATIONSHIPS

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.