STUDIES ON BIOACTIVE SUBSTANCES FROM MARINE MICROORGANISMS

血管收缩化合物zooxanhtellatoxin-A （ZT-A）和ZT-B从一种共生的海洋双鞭毛藻Symbiodinium sp.中分离得到。高酸钠氧化ZT-A后，硼氢化钠还原得到含有特征功能的片段，包括外甲氧基、二氧化物、硫酸盐、共轭二烯、螺缩醛和酰胺。这些结构相当于ZT-A全部结构的80%左右。ZT-A在不同条件下的TOCSY谱使我们能够将由降解产物推导出的部分结构联系起来。通过HMBC、HMQC和13-C核磁共振谱的详细分析得到了揭示的结构。根据光谱数据和化学降解实验确定了ZT-A的结构是一种新型的62元内酯和酰胺键。根据构效关系，设计了促瘤物质、应用毒素的模型化合物。最终合成了一个包含生物活性必需功能的模型。

Vasoconstrictive compounds, zooxanhtellatoxin-A (ZT-A) and ZT-B were isolated from a symbiotic marine dinoflagellate Symbiodinium sp. Sodium periodate oxidation of Zt-A followied by sodium borohydride reduction gave fragments containing characteristic functionalities including an exomethyoene, a diexpoxide, a sulfate, a conjugated diene, a spiroacetal, and an amide. The structures correspond to about 80% of the full structure of ZT-A.TOCSY spectra of ZT-A under various conditions enable us to connect the partial structures deduced from the degradation products. The unveiled structures were obtained by detailed analyes of HMBC, HMQC and 13-C NMR spectra. The structure of ZT-A was determined on the basis of the spectral data and chemical degradation experiments to be a novel 62-membered lactonewith and amide linkage.Model compounds of tumor-promorting sabstance, aplysiatoxin were designed on the basis of the structure-activity relationship. Synthesis of a model containing functionalities essential for biological activity was finally achieved.