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采用固相合成方法,以Rink Amide树脂为载体,Fmoc保护氨基酸为原料,经苯并三唑-1-四甲基六氟磷酸酯(HBTU)/N,N-二异丙基乙胺(DIEA)缩合,三氟乙酸/苯甲硫醚/乙二硫醇/苯甲醚裂解体系脱除保护基制得IB-367线性肽(4);4经双氧水氧化制得IB-367一环肽(5);5经碘乙醇溶液氧化合成抗菌肽IB-367(6),收率34.1%,纯度>95.0%,其结构经MS(ESI)和氨基酸组成分析确证。抑菌活性研究结果表明:6对大肠杆菌和金黄色葡萄球菌的最小抑菌浓度为5.0μg·mL~(-1)。
Solid-phase synthesis was carried out by using Rink Amide resin as carrier and Fmoc-protected amino acid as starting material. Benzotriazole-1-tetramethylphosphonium hexafluorophosphate (HBTU) / N, ) IB-367 linear peptide (4) was obtained by condensation with trifluoroacetic acid / thioanisole / ethanedithiol / anisole cleavage system; 4 IB-367 monocyclic peptide was prepared by hydrogen peroxide oxidation 5). The antibacterial peptide IB-367 (6) was synthesized by the oxidation of iodoethanol. The yield was 34.1% with a purity of> 95.0%. The structure was confirmed by MS (ESI) and amino acid composition analysis. The results of antibacterial activity showed that the minimum inhibitory concentration (MIC) against Escherichia coli and Staphylococcus aureus was 5.0 μg · mL -1.