肽抗生素hPAB-β的化学合成及其杀菌活性的初步证实

Synthesis and bactericidal activities of peptide antibiotics hPAB-β

目的 化学合成、纯化并初步测定肽抗生素hPAB β的活性 ,为后续研究奠定基础。 方法 采用固相合成法合成肽抗生素hPAB β ,经RP HPLC纯化 ,用质谱进行分子量鉴定 ,谷胱甘肽氧化 还原法复性合成产物 ,进一步用阳离子交换柱纯化复性产物 ,收集主峰 ,药敏法初步测定合成肽的抗菌活性。结果 合成肽抗生素hPAB β的纯度为 86 5 2 % ,经质谱分析 ,合成肽的分子量测定值与理论值相符。用谷胱甘肽氧化 还原法复性合成肽取得了较好的效果。复性产物对大肠埃希菌、铜绿假单胞菌、金黄色葡萄球菌具有杀灭作用。结论 化学合成的肽抗生素hPAB β具有良好的杀菌活性。

Objective To synthesize, purify and explore bactericidal activities of peptide antibiotics hPAB β. Methods Peptides were synthesized with solid phase strategies. After cleavage of peptides from resin, the released peptides were purified with reversed phase high performance liquid chromatography (RP HPLC) and characterized with mass spectrometry. Renaturation of synthetic peptides was carried out in glutathione oxidized/reduced system. The renatured hPAB β was purified again with cationic exchange chromatography. The bactericidal activities of purified hPAB β to E. coli, pseudomonas aeruginosa and staphylococcus aureus were performed with plate method. Results The final purity was at least 86.52% identified by RP HPLC. The obtained molecular mass was identical to its theoretical value. The tested microorganisms included E. coli, pseudomonas aeruginosa, staphylococcus aureus were sensitive to the synthetic peptides. Conclusion The synthetic hPAB β has good bactericidal activities.