从淡水蓝藻束丝藻中分离得到的凝血酶抑制剂。
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.
机构信息
Division of Environmental Materials Science, Graduate School of Environmental Science, Hokkaido University, Sapporo 060-0810, Japan.
出版信息
J Nat Prod. 2012 Sep 28;75(9):1546-52. doi: 10.1021/np300282a. Epub 2012 Sep 5.
Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey's methodology. Compounds 1 and 2 inhibited thrombin with EC(50) values of 4.9 and 2.1 μM, and 0.7 and 0.2 μM in the cathepsin B inhibitory assay, respectively. The MM-GBSA methodology predicted spumigin A with 2S-4-methylproline as the better thrombin inhibitor.
基于生物测定的指导，对蓝藻鱼腥藻提取物进行研究，得到了海绵抑素 J（1）和已知的凝血酶抑制剂海绵抑素 A（2）。通过先进的 Marfey 方法学分析了 1 的绝对构型。化合物 1 和 2 对凝血酶的抑制活性的 EC50 值分别为 4.9 和 2.1 μM，在组织蛋白酶 B 抑制试验中分别为 0.7 和 0.2 μM。MM-GBSA 方法预测 2S-4-甲基脯氨酸是海绵抑素 A 更好的凝血酶抑制剂。
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