P-49 新規ホスホリパーゼA_2阻害活性物質crgophilonc AおよびBの構造(ポスター発表の部)

概要

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In our screening program for new phospholipase A_2(PLA_2) inhibitors, we isolated novel potent inhibitors named ergophilone A and B from mycelium of Penicillium sp. BM-99. The molecular formula of ergophilone A and B were determined as C_<50>H_<60>O_<10> and C_<49>H_<58>O_<10> by high resolution FAB-MS data. The results of detailed NMR analyses, especially pulsed field gradient (PFG) HMBC spectra, revealed the structures which had three partial structures, i.e. ergosta-5,8(14),22-trien-3-ol, azaphilone chromophore and o-orsellinic acid moieties. The connectivity of each partial structures were also determined by PFG-HMBC spectra. The full assignments of ^1H-and ^<13>C-NMR data of ergophilone A and B were carried out. The stereochemistry of ergophilone A and B were determined on the bases of NOE experimental data, ^1H-^1H coupling constant values and the comparison of the CD spectra with related azaphilones. Ergophilone A and B showed inhibitory activities against the rat platelet PLA_2 with IC_<50> value of 0.44μM and 0.56μM, respectively.
天然有機化合物討論会の論文
1994-09-20