Project/Area Number |
05557097
|
Research Category |
Grant-in-Aid for Developmental Scientific Research (B)
|
Allocation Type | Single-year Grants |
Research Field |
Chemical pharmacy
|
Research Institution | University of Tokyo |
Principal Investigator |
SANKAWA Ushio University of Tokyo, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (60012613)
|
Co-Investigator(Kenkyū-buntansha) |
SATO Toshitsugu Tsumura Phamaceutical Company Institution of Pharmacology, Head Researcher, 研究所, 研究員
SHIBUYA Masaaki University of Tokyo, Faculty of Pharmaceutical Sciences, Assistant Professor, 薬学部, 助手 (50170923)
NOGUCHI Hiroshi University of Tokyo, Faculty of Pharmaceutical Sciences, Lecturer, 薬学部, 講師 (60126141)
|
Project Period (FY) |
1993 – 1994
|
Project Status |
Completed (Fiscal Year 1994)
|
Budget Amount *help |
¥13,200,000 (Direct Cost: ¥13,200,000)
Fiscal Year 1994: ¥3,700,000 (Direct Cost: ¥3,700,000)
Fiscal Year 1993: ¥9,500,000 (Direct Cost: ¥9,500,000)
|
Keywords | Biologically Active Compound / Screening / Anti-PAF / Anti-Allergy / Lignan / Stillbene / Flavone / Ca Antagonist |
Research Abstract |
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.
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