Butyrolactones,inhibitors of 5-lipoxygenase from fungal metabolites  

真菌来源的5-脂氧合酶抑制剂:Butyrolactones(英文)

作　　者：王福生[1] 可爱兵 朱京童 李业英 路新华 郑智慧 张华 马瑛 任晓 王亚婷[1] 赵宝华[1] 

机构地区：[1]河北师范大学生命科学学院,河北石家庄050016 [2]华北制药集团新药研发中心,河北石家庄050016

出　　处：《Journal of Chinese Pharmaceutical Sciences》2010年第4期251-255,共5页中国药学（英文版）

基　　金：National Basic Research Project of China(Grant No.2009CB526513);National New Drug Research and Development Proiect(Grant No.2008ZX09401-05)

摘　　要：In our ongoing search for new inhibitors of 5-lipoxygenase（5-LOX） from microbial resources,Aspergillus F06Z-509 was found to produce active components.Three active compounds named F06Z-509-A,B and C were obtained and identified as butyrolactoneⅡ,ⅠandⅢby NMR and MS data analyses.They showed inhibitory activity against 5-LOX with IC50 of 21.43, 22.51 and 11.83μg/mL,respectively.Butyrolactones are shown to be inhibitors of 5-LOX for the first time.我们在进行微生物来源的5-脂氧合酶抑制剂的筛选过程中,得到了一株具有活性的曲霉菌F06Z-509。经过对其发酵产物进行分离纯化,最终得到三个活性化合物,分别为F06Z-509-A,B和C。通过对它们核磁和质谱数据进行分析,确定其结构分别与已知化合物butyrolactoneⅡ,Ⅰ和Ⅲ相同。它们对5-脂氧合酶都表现出较强的抑制活性,IC_(50)值分别为21.43,22.51和11.83μg/mL。它们对5-脂氧合酶的抑制活性未见报道。

关 键 词：5-Lipoxygenase inhibitors BUTYROLACTONES Fungal metabolites 

分 类 号：R284[医药卫生—中药学]