90 海生菌Phoma sp.の生産するPAF拮抗物質phomactin類の構造(口頭発表の部)

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PAF (platelet activating factor, 1-O-alkyl-2(R)-acetylglyceryl-3-phosphoryl choline) causes platelet aggregation, chemotaxis and degranulation of polymorphonuclear leukocytes, smooth muscle contraction, vascular permeability, and hypotension. Recent studies have shown that PAF may be involved in many inflammatory, respiratory, and cardiovascular diseases. In our program for finding PAF antagonists from marine sources, we focused on marine fungi. We systematically screened lipophilic extracts of marine fungal isolates for inhibition of PAF-induced platelet aggregation and binding of PAF to its receptors, and found that a marine fungus Phoma sp. produced a novel PAF antagonist, phomactin A (1) and its derivatives B (2), B1 (3), B2 (4). Their structures were determined by NMR studies, chemical conversion and X-ray analysis. Phomactin A, B, B1, B2 inhibited PAF-induced platelet aggregation at IC_<50> 1.0x10^<-5>M, 1.7x10^<-5>M, 9.8x10^<-6>M, 1.6x10^<-6>M respectively, and A, B1, B2 also inhibited binding of PAF to its receptors at IC_<50> 2.3x10^<-6>M, 2.0x10^<-5>M, 5.4x10^<-6>M.
天然有機化合物討論会の論文
1991-09-07