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目的:设计合成一种新型还原敏感型阳离子寡肽脂质材料,以期由其制得的脂质体可用作核酸药物载体在细胞质还原性环境促发下降解而释放药物。方法:以胱胺为原料引入二硫键,合成还原敏感型阳离子寡肽脂质材料H-SS-E2C14,并用其制备还原敏感型阳离子寡肽脂质体H-SS-E2C14-L;同时,以半胱胺为原料合成H-SS-E2C14的降解产物CS-E2C14,且采用HPLC法定量考察H-SS-E2C14在模拟细胞质还原性环境中的降解动力学。结果:合成的H-SS-E2C14在模拟细胞质还原性环境中的24h累积降解率约为70%。结论:H-SS-E2C14-L有望成为一种理想的基因药物载体。
OBJECTIVE: To design and synthesize a new type of reduction-sensitive cationic oligopeptide lipid material, in the hope that the liposomes prepared from them can be used as nucleic acid drug carriers to promote the degradation and release of drugs in the cytoplasmic reducing environment. Methods: The disulfide bond was introduced from cystamine to synthesize the reduction-sensitive cationic oligopeptide lipid material H-SS-E2C14. H-SS-E2C14-L, a reducing sensitive cationic oligopeptide liposome, was prepared. At the same time, CS-E2C14, a degradation product of H-SS-E2C14, was synthesized using cysteamine as starting material and the degradation kinetics of H-SS-E2C14 in a simulated cytoplasmic reducing environment was quantitatively investigated by HPLC. Results: The cumulative 24 h degradation rate of synthetic H-SS-E2C14 in simulated cytoplasmic reducing environment was about 70%. Conclusion: H-SS-E2C14-L is expected to become an ideal gene drug carrier.