Fukuyama Y, Kodama M, Miura I, Kinzyo Z, Kido M, Mori H, Nakayama Y, Takahashi M
Chem Pharm Bull (Tokyo). 1989 Feb;37(2):349-53. doi: 10.1248/cpb.37.349.
Eckol (1), a novel phlorotannin with a dibenzo-1,4-dioxin skeleton, has been isolated from the brown alga Ecklonia kurome Okamura as a potent and specific anti-plasmin inhibitor. Its structure has been elucidated based on the spectral data, in particular, by means of negative nuclear Overhauser effect (NOE), and finally established as 1-(3,5-dihydroxyphenoxy)-2,4,7,9-tetrahydroxydibenzo-1,4-dio xin by X-ray analysis. Some partially methoxylated derivatives of eckol were prepared by methylation with diazomethane and also by selective dimethylation of eckol permethylate (1b) to establish the structural requirements for inhibitory activities on alpha 2-macroglobulin and alpha 2-plasmin inhibitor, the main plasmin inhibitors in plasma.
eckol（1）是一种具有二苯并-1,4-二恶英骨架的新型间苯三酚鞣质，已从褐藻冈村鹅掌菜中分离出来，是一种强效且特异性的抗纤溶酶抑制剂。其结构已根据光谱数据阐明，特别是通过负核Overhauser效应（NOE），并最终通过X射线分析确定为1-（3,5-二羟基苯氧基）-2,4,7,9-四羟基二苯并-1,4-二恶英。eckol的一些部分甲氧基化衍生物通过重氮甲烷甲基化以及eckol全甲基化物（1b）的选择性二甲基化制备，以确定对α2-巨球蛋白和α2-纤溶酶抑制剂（血浆中的主要纤溶酶抑制剂）抑制活性的结构要求。
