芋螺毒素G1.9的氧化折叠及活性

Oxidative Folding and Activity of Conotoxin G1.9

【目的】通过合成芋螺毒素线性肽G1.9并优化氧化折叠体系,测试其对昆虫细胞毒性,为新型多肽类杀虫剂的设计提供依据。【方法】采用固相多肽合成法(SPPS)制备含4个半胱氨酸的芋螺毒素线性肽G1.9并优化氧化折叠体系,采用一罐法氧化芋螺毒素G1.9并验证其生物活性。【结果与结论】采用SPPS法成功地合成了线性肽G1.9,优化获得芋螺毒素G1.9-G型异构体的最佳氧化折叠体系是在0.1 mol/L碳酸氢铵缓冲液(pH 8.0)中氧化36 h。MTT法实验表明G1.9-G能显著抑制昆虫细胞sf9的生长,为后续研究开发新型、安全和高效的多肽类生物杀虫剂奠定基础。

【Objective】To synthesize conotoxin linear peptide G1.9 and optimize the oxidative folding system,test its cytotoxicity to insect cells,and provide a basis for the design of new peptide insecticides.【Method】Conotoxin linear peptide G1.9 containing four cysteines was prepared by solid phase peptide synthesis(SPPS)and the oxidative folding system was optimized.Conotoxin G1.9 was oxidized using a one pot method and its biological activity was verified.【Result and Conclusion】The linear peptide G1.9 was successfully synthesized by SPPS method.The optimal oxidation folding system of natural active G1.9-globular(G1.9-G)isomer to oxidize in 0.1 mol/L ammonium bicarbonate buffer system(pH 8)for 36 h.MTT assay showed that G1.9-G could significantly inhibit the growth of insect cell sf9.It could lay a foundation for the development of novel,safe and efficient peptide biological insecticides.