19 新規ホスホリパーゼA_2阻害物質、チ***シン類の構造(口頭発表の部)

概要

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Novel phospholipase A_2 (PLA_2) inhibitors were obtained from the culture broth of a fungus: Thielavia terricola RF-143. Bioassay guided isolation afforded twelve new compounds: thielocins A1α (1a), A1β(1b), A2α (6a), A2β (6b), A3 (fig.3), A4α (fig.4), A4β (fig.4), B1 (12a), B2 (16) and B3 (20) along with thielavins D (32) and E (33). Structrues of these novel compounds were determined on the bases of chemical degradation and spectral analysis. Method of synthesis of thielocin B3 was developed strating from thielavin B which was produced in large amount in the culture broth. Total synthesis of the tridepside thielavins B and D were also reported. Studies on their PLA_2 inhibitory activities have shown their specificity on the group II type enzymes. IC_<50> values of the most potent compound, thielocin B3, were 0.074μM for human synovial fluid PLA_2, 4.2μM for the human pancreas enzyme, respectively.
天然有機化合物討論会の論文
1992-09-10