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

我们利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原料药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有两个芳香环，如木脂素、stillbene和黄酮。两个苯环的距离和方向对抗过敏活性有重要影响。在这种构效关系的基础上，将含有两个苯环并由酰胺键连接的11个化合物视为苯胺与苯甲酸偶联的产物。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实验。一些合成的化合物显示出显著的活性。体内活性测试正在调查中。Fissistigma oldhamii (Memsl)稳定。是一种多年生灌木，主要分布于中国南部和台湾地区。初步测定了其甲醇提取物具有抗血小板聚集活性，并对其成分进行了研究。从氢恶二嗪类化合物中分离出一种具有四环熔接结构的新生物碱，并将其命名为fissoldhimine，通过x射线分析对其结构进行了解析。目前正在对鱼碱的生物活性进行详细的研究。

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.