【摘要】：先采用Fmoc固相多肽合成法,以2-Chlorotrityl chloride(2-CTC)樹脂做載體,DIC/HOBt做縮合劑,逐步縮合得到全保護(hù)谷胱甘肽樹脂,以TFA/EDT/m-Cresol為裂解液脫除保護(hù)基團(tuán),粗肽經(jīng)半制備反相高效液相色譜法純化得α-GSH、γ-GSH純品,后將所得γ-GSH純品分別采用空氣,雙氧水,碘氧化得GSSG,經(jīng)純化得GSSG純品,合成的α-GSH、γ-GSH純品純度達(dá)99%,GSSG純度達(dá)98%,利用標(biāo)準(zhǔn)品,經(jīng)外標(biāo)法計算總收率分別為60%、64%、57%。并觀察三者對CCl4誘導(dǎo)的小鼠急性肝損傷的治療效果結(jié)果顯示都能顯著降低ALT與AST的活性,且與注射用γ-GSH沒有顯著性差異,可以為工業(yè)化生產(chǎn)提供借鑒。
[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. 偽-GSH, 緯-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,. 偽-GSH, was synthesized. The purity of 緯-GSH was 98. The total yield of 緯-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 緯-GSH for injection, which could be used as a reference for industrial production.
【作者單位】： 河北省中藥研究與開發(fā)重點(diǎn)實驗室承德醫(yī)學(xué)院中藥研究所;
【基金】：河北省海外高層次人才“百人計劃”(E2012100002) 承德醫(yī)學(xué)院博士基金(201303)
【分類號】：R914.5

【參考文獻(xiàn)】

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