Investigation of Medicinal Lead Compounds from Natural Resource

在天然资源中一种药用先导化合物的研究项目下，我们从药用植物和蘑菇中分离和鉴定了几种天然物质的结构。从巴西植物叶鞘藻中分离得到3个新的异戊二烯类化合物，分别为异戊二烯、异戊二烯和异异戊二烯。由于这些化合物是具有抗肿瘤活性的贫民窟的同系物，因此应该研究其作用机制。从亚黑蘑菇中分离得到一种具有细胞毒性的成分--红苏酚，并对其化学结构进行了鉴定。分离具有光学活性的红苏酚的生物合成酶可能是有意义的。合流酸和2‘-O-甲基过戊二醇酸是从巴西植物雪莲中分离得到的。由于合流酸对单胺氧化酶-B具有较强的特异性，合成的类似物的活性增加，因此合流酸有可能作为一种先导化合物应用于新型药物的开发。鹅掌酸是从蘑菇蘑菇中分离得到的。分离得到了(S)-顺-2-氨基-5-氯-4-戊烯酸，并对其结构进行了鉴定。从香菇Laccaria vinaceovellanea中分离得到一种新的生物碱--漆树素，作为cAMP磷酸二酯酶的抑制剂，并对其化学结构进行了鉴定。

Under the research project on the investigation of a medicinal lead compound from natural resource, we have isolated and elucidated the structures of several natural substances from medicinal plants and mushrooms. Three new isoprenoids, faveloxide, favelol and isofavelol were isolated from Brazilian plant Cnidoscolus phyllacanthus. Since those compounds are congeners of faveline that has anti tumor activity, the mode of action should be studied. As a cytotoxic component of mushroom Russula subnigricans, russuphelol was isolated and the chemical structure was determined. It may be of interest to isolate the biosynthetic enzyme of russuphelol having optical activity. Confluentic acid and 2'-O-methylperlatolic acid were isolated from the Brazilian plant Himatamthus sucuuba. Because of its potent and specific activity against monoamine oxidase-B and the increase of the activity of the synthetic analogs, confluentic acid may act as a lead compound in the development of a new type of medicine. Ibotenic acid was isolated from the mushroom Tricholoma muscarium. As a new chlorinated amino acid in the mushroom Amanita vergineoides, (S)-cis-2-amino-5-chloro-4-pentenoic acid was isolated and structure was elucidated. From the mushroom Laccaria vinaceoavellanea, a new alkaloid laccarin was isolated as a inhibitor of cAMP phosphodiesterase and the chemical structure was elucidated.