BIOSYNTHTIC STUDY OF AERUGINOSINS FROM THE CYANOBACTERIA

绿脓毒苷是由3种氨基酸衍生物（Hpla、对羟基苯基乳酸、Choi、2-羧基-6-羟基辛烷吲哚和精氨酸衍生物）和1种常用氨基酸组成。这些肽对胰蛋白酶、纤溶酶和凝血酶具有较强的蛋白酶抑制活性。在这项研究中，我没有找到铜绿素生物合成的关键化合物，该化合物在肽的n端含有精氨酸。而铜绿素102-A和-B以及铜绿素103-A均是从病毒微囊藻（NIES-102,103）中分离得到的。这些肽在n端具有精氨酸。从agardhii振荡菌（nis -205）中分离出由agmatine、Choi、3-hydroxyleucine、xylopyranose和Hpla组成的aeruginosins 205-A和B。根据这些结果，铜绿球蛋白的生物合成途径被认为是精氨酸还原为精氨酸、精氨酸醇或蛋白的途径。遗憾的是，从标记的^<13>C-Tyr的合并经验中无法明确定义Choi的生物合成途径。此外，通过对trpsin和aeruginosin 98-B复合物的x射线分析，我可以明确aeruginosin 98-B的完整绝对立体结构以及对胰蛋白酶的抑制机制。

Aeruginosins, which were produced by the cyanobacteria, were composed by three amino acids derivatives (Hpla ; p-hydroxy-phenyllactic acid, Choi ; 2-carboxy-6-hydroxyoctahydroindole and Arg derivatives) and one usual amino acid. These peptides showed strong protease inhibitory acyivities against trypsin, plasmin and thrombin.In this study, I can not find the key compound of biosynthesis of aeruginosins, which was contained Arg at N-terminal of-peptide. But, the aeruginosins 102-A and -B,and the aeruginosin 103-A were isolated from the Microcystis viridis (NIES-102,103). These peptides possesed argininal at N-terminal. I also could isolate the aeruginosins 205-A and B from Oscillatoria agardhii (NIES-205), which were composed by agmatine, Choi, 3-hydroxyleucine, xylopyranose and Hpla. From these results, the biosynthetic pathway of aeruginosins was thought to be reducing pathway from Arg to argininal, argininol or agmatin. Unfortunately, the biosynthetic pathway of Choi could not be clearly defined from the incorpolation experience of labeled ^<13>C-Tyr.Furthermore, I can clarified the aeruginosin 98-B's complete absolute stereostructure along with the mechanism of trypisn inhibition from the Xray analisis of the complex of trpsin and aeruginosin 98-B.