谷胱甘肽的合成与其活性初步评价
发布时间：2018-11-22 13:31
【摘要】：先采用Fmoc固相多肽合成法,以2-Chlorotrityl chloride(2-CTC)树脂做载体,DIC/HOBt做缩合剂,逐步缩合得到全保护谷胱甘肽树脂,以TFA/EDT/m-Cresol为裂解液脱除保护基团,粗肽经半制备反相高效液相色谱法纯化得α-GSH、γ-GSH纯品,后将所得γ-GSH纯品分别采用空气,双氧水,碘氧化得GSSG,经纯化得GSSG纯品,合成的α-GSH、γ-GSH纯品纯度达99%,GSSG纯度达98%,利用标准品,经外标法计算总收率分别为60%、64%、57%。并观察三者对CCl4诱导的小鼠急性肝损伤的治疗效果结果显示都能显著降低ALT与AST的活性,且与注射用γ-GSH没有显著性差异,可以为工业化生产提供借鉴。
[Abstract]:Using Fmoc solid phase peptide synthesis method, 2-Chlorotrityl chloride (2-CTC) resin as carrier and DIC/HOBt as shrinkage agent, the whole protected glutathione resin was synthesized step by step, and the protective group was removed with TFA/EDT/m-Cresol as pyrolysis solution. 伪-GSH, 纬-GSH was purified by semi-preparation of crude peptide by reversed-phase high performance liquid chromatography, and then purified by air, hydrogen peroxide and iodine to obtain GSSG,. 伪-GSH, was synthesized. The purity of 纬-GSH was 98. The total yield of 纬-GSH was calculated by external standard method. The results of treatment of acute liver injury induced by CCl4 in mice showed that the activity of ALT and AST was significantly decreased, and there was no significant difference between them and 纬-GSH for injection, which could be used as a reference for industrial production.
【作者单位】： 河北省中药研究与开发重点实验室承德医学院中药研究所;
【基金】：河北省海外高层次人才“百人计划”(E2012100002) 承德医学院博士基金(201303)
【分类号】：R914.5
[Abstract]:Using Fmoc solid phase peptide synthesis method, 2-Chlorotrityl chloride (2-CTC) resin as carrier and DIC/HOBt as shrinkage agent, the whole protected glutathione resin was synthesized step by step, and the protective group was removed with TFA/EDT/m-Cresol as pyrolysis solution. 伪-GSH, 纬-GSH was purified by semi-preparation of crude peptide by reversed-phase high performance liquid chromatography, and then purified by air, hydrogen peroxide and iodine to obtain GSSG,. 伪-GSH, was synthesized. The purity of 纬-GSH was 98. The total yield of 纬-GSH was calculated by external standard method. The results of treatment of acute liver injury induced by CCl4 in mice showed that the activity of ALT and AST was significantly decreased, and there was no significant difference between them and 纬-GSH for injection, which could be used as a reference for industrial production.
【作者单位】： 河北省中药研究与开发重点实验室承德医学院中药研究所;
【基金】：河北省海外高层次人才“百人计划”(E2012100002) 承德医学院博士基金(201303)
【分类号】：R914.5
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