摘要/Abstract

利用培养基筛选策略从链霉菌LZ35的主产物敲除突变株SR111中分离得到2个新germicidin糖苷衍生物, 通过一维和二维核磁及高分辨质谱等数据分析确定其化学结构分别为germicidin A-4-O-β-D-glucuronide (1)和germicidin D-4-O-β-D-glucuronide (2). 采用滤纸片法测定了化合物1和2的抗细菌和抗真菌活性, 结果显示两者在20 μg条件下均无抗菌活性. 采用噻唑蓝比色法测定了化合物 1和2的细胞毒活性, 结果显示两者对肝癌细胞HepG2和宫颈癌细胞HeLa均无明显活性. 本研究发现了含有葡萄糖醛酸基团的germicidin衍生物, 丰富了该类化合物的结构多样性.
关键词: 链霉菌, 天然产物, 培养基筛选, germicidins
Two new germicidin glucuronides were isolated from the metabolites of Streptomyces sp. SR111, which is derived from Streptomyces sp. LZ35 through deletion of eight biosynthetic gene clusters by screening of culture media. The chemicla structures of 1 and 2 were determined to be germicidin A-4-O-β-D-glucuronide and germicidin D-4-O-β-D-glucuronide, respectively, by analysis of 1-D and 2-D NMR data and high resolution mass spectrometry. The antibacterial and antifungal activities of 1 and2were eveluated by disc diffusion assay, and they showed no inhibitory activity at 20 μg/disc. The cytotoxic activities of 1 and 2 were tested by methyl thiazolyl tetrazolium (MTT) colorimetric method, and they were inactive against the HepG2 (liver cancer) and HeLa (cervical cancer) cell lines. Remarkably, compounds 1 and 2 represent the first two germicidins with a glucuronic acid moiety, which expands the structural diversity of germicidins
Key words: Streptomyces, natural products, screening of culture media, germicidins


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