The Study on Seaching for the Biologically Active Compounds Containd in the Medicinal Plants

采用体外生物测定系统，对日本、中国、台湾、香港、印度尼西亚等东南亚国家的200多种药用植物和植物源药材中所含的生物活性成分进行了研究。我们发现，许多具有抗过敏活性的化合物都含有木脂素、二苯乙烯和黄酮等两个芳香环。两个苯环的距离和方向被认为对抗过敏活性非常重要。在这种构效关系的基础上，11个具有两个苯环并通过酰胺键相连的化合物，如苯甲胺和苯甲酸的偶联产物。对合成的化合物进行了抑制组胺释放活性和抗血小板聚集活性的测试。一些合成的化合物显示出显著的活性。活体活性的测定正在进行中。绿飞虱是一种多年生灌木，主要分布于中国南部和台湾。在初步的生物活性测试中，其甲醇提取物具有抗血小板聚集的活性，并在台湾台中采集的植物材料中对其成分进行了研究。分离得到了一种新的四环稠合结构生物碱，命名为非索尔德明，其结构经X-射线分析确定。有关非索利特明生物活性的细节正在调查中。

We have been investigated the biologically active compounds contained in more than two-hundred of the medicinal plants and plant origin crude drugs obtained in Japan, China, Taiwan, Hong-Kong, Indonesia and other country of southeast Asia, using the in vitro bioassay system. We found that many of the compounds which had anti-allergy activity had two aromatic rings such as lignan, stillbene and flavone. The distance and direction of two benzene ring are supposed to be very important for ant-allergy activity. On the bases of such structure-activity relationship, the eleven compounds having the two benzene ring which were connected by amide bond such as the product of the coupling of benzylamine and benzoic acid. The synthesized compounds were tested for repression of histamine release activity and anti-platelet aggregation activity. Some of the synthesized compounds revealed significant activity. The testing of in vivo activity are under investigation.Fissistigma oldhamii(Memsl.)Merr.(Annonaceace)is a perennial shrub which is distributed mainly in southern China and Taiwan. In a preliminary bioassay, its methanol extract showed anti-platelet aggregation activity and its constituents were investigated in the plant material collected in Taichung, Taiwan. A new alkaloid of hydro-oxadiazine with four-ring fused structure has been isolated and named fissoldhimine, the structure of which was solved by X-ray analysis. The detail of biological activities of fissolidhmine is under investigation.