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目的筛选神经氨酸酶抑制剂,发现潜在的抗流感药物先导化合物。方法利用神经氨酸酶抑制剂高通量筛选方法,从海洋微生物菌库中筛选产生神经氨酸酶抑制剂的菌株,采用多种色谱技术分离纯化获得活性化合物,通过紫外、质谱、核磁共振等现代波谱学方法鉴定其结构。结果分离到两个吲哚生物碱类活性化合物1和化合物2,结构解析确定它们分别与SF2583 A和SF2583 B同质,对神经氨酸酶的IC50为67.8μmol/L和122.8μmol/L,Ki为13.5μmol/L和21.6μmol/L。结论本文首次报道该化学结构类型化合物对神经氨酸酶具有一定的抑制作用。
Objective To screen neuraminidase inhibitors and to find potential anti-flu lead compounds. Methods A neuraminidase inhibitor-producing strain was screened from marine microbial strains by high-throughput neuraminidase inhibitor screening. The compounds were isolated and purified by a variety of chromatographic techniques. The compounds were characterized by UV, MS and NMR Modern spectroscopy identifies its structure. As a result, two indole alkaloids, active compound 1 and compound 2, were isolated and structurally identified as being homogeneous with SF2583 A and SF2583 B respectively. IC50 values for neuraminidase were 67.8 μmol / L and 122.8 μmol / L, Ki 13.5 μmol / L and 21.6 μmol / L. Conclusions This paper reports for the first time that the compounds of this chemical structure have some inhibitory effect on neuraminidase.