Studies on Biologically Active Lignans from Medicinal Plants

1.从杜仲皮和刺五加茎皮中分离得到二氧二环辛烷木脂素的单糖和双糖，分别为松脂醇、中脂醇和丁香酚。讨论了苷元及其糖苷对环磷酸二酯酶抑制作用的构效关系。抑制作用大小顺序为二葡萄糖苷元和单糖苷。结论：1.紫丁香酚二-O-β-D-葡萄糖苷具有强抑制作用，对大鼠游泳运动有延长作用。从天花粉中分离得到的L芝麻素具有凝血活性。与之相关的木脂素类化合物d-芝麻素、松脂醇、异胡萝卜素、雷公藤内酯、牛至皂苷元和松脂素没有显示出活性。用来治疗瘀血的鸡血藤茎段水提物具有抑制超氧化物歧化生成和松弛组胺引起的豚鼠气管肌肉收缩的活性。结果表明，这些活性依赖于可溶于乙醚部分的木脂素、牛至皂苷元、松脂素、去甲酚和去甲酚。糖苷类化合物没有显示活性。

1. Mono- and di-glucosides of dioxabicyclooctane lignans, pinoresinol, medioresinol and syringaresinol, were isolated from Eucommiae Cortex and Acanthopanax senticosus Stem Bark, which have been used as a restorative tonic. The structureinhibitory activity relationships of the aglycone and its glucosides on cyclic AMP phosphodiesterase inhibition were discussed. The order of inhibitory effect was diglucoside aglycone>monoglucoside. Syringaresinol di-O-beta-D-glucoside, which shows trong inhibitory activity, exhibited the prolonging effect on swimming exercise in rats.2. l-Sesamin isolated from Hydrocotgle sibthorpioides showed the blood coagulation activity. The related lignans, d-sesamin, pinoresinol, isohinokinin, pluviatolide, arctigenin and matairesinol, did not show the activity.3. Aqueous extract of stem part of Caulis Trachelospermi, which has been used for treatment of blood stagnant (oketsu), showed inhibitory activity of superoxide production and relaxant activity against histamine-induced contraction of tracheal muscles in guinea pig. It was shown that these activities depends on lignans, arctigenin, matairesinol, trachelogenin and nortrachelogenin, which are soluble in ether fraction. The glucosides did not show the activities.