Studies of platelet activating factor (PAF) antagonists from microbial products. I. Bisdethiobis(methylthio)gliotoxin and its derivatives.
Studies of platelet activating factor (PAF) antagonists from microbial products. I. Bisdethiobis(methylthio)gliotoxin and its derivatives.
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DOI：
10.1248/cpb.34.340
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发表时间：
1986-01
影响因子：
1.7
通讯作者：
M. Okamoto;K. Yoshida;I. Uchida;M. Nishikawa;M. Kohsaka;H. Aoki
中科院分区：
文献类型：
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作者：
M. Okamoto;K. Yoshida;I. Uchida;M. Nishikawa;M. Kohsaka;H. Aoki
从特氏青霉发酵产物中分离得到一种血小板活化因子（PAF）拮抗剂FR-49175，经鉴定为双硫代双（甲硫基）胶霉毒素（1）。该化合物对PAF诱导的家兔血小板聚集的IC_（50）值为8.4 μM。本文合成了双硫代双（甲硫基）胶霉毒素（1）的一些衍生物，并测定了它们对PAF诱导的血小板聚集的抑制活性。在这些化合物中，5a，6-脱水双脱硫基-3，10a-双（甲硫基）胶霉毒素（8）显示出最强的PAF抑制活性（IC 50; 4.4 μM）。
A platelet activating factor (PAF) antagonist, designated as FR-49175, was isolated from fermentation products of Penicillium terlikowskii and identified as bisdethiobis(methylthio)-gliotoxin (1). The IC50 value of this compound for PAF-induced rabbit platelet aggregation was 8.4 μM.Some derivatives of bisdethiobis(methylthio)gliotoxin (1) were synthesized and their inhibitory activities of PAF-induced platelet aggregation were examined. Among these compounds, 5a, 6-anhydrobisdethio-3, 10a-bis(methylthio)gliotoxin (8) showed the most potent PAF inhibitory activity (IC50; 4.4 μM).