Sadineni Vikram, Schöneich Christian
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence, Kansas 66047, USA.
J Pharm Sci. 2007 Jul;96(7):1844-7. doi: 10.1002/jps.20834.
The purpose of this study is to quantitate the sensitivity of Zn2+ -insulin to oxidation catalyzed by various redox active transition metals, Cu2+, Fe2+, Mn2+, Ni2+, Co2+, Cr3+. Human recombinant insulin (INS) was subjected to oxidation under various conditions in the presence and absence of Zn2+ and ascorbate. The extent of oxidation was monitored by RP-HPLC. Only Cu2+, but none of the other metals or combination thereof, for example, Ni2+/Co2+, Co2+/Cr3+, and Ni2+/Cr3+, catalyzed INS oxidation, for example, to an extent of 45% when 20 microM INS/8.8 microM Zn2+ were exposed to 8 microM Cu2+ and 50 microM ascorbate for 90 min. The Cu2+ -catalyzed oxidation mainly targeted the B chain of INS, where the two histidine residues are located.
本研究的目的是定量锌离子胰岛素对各种具有氧化还原活性的过渡金属(铜离子、亚铁离子、锰离子、镍离子、钴离子、铬离子)催化氧化的敏感性。在有和没有锌离子及抗坏血酸的情况下,人重组胰岛素(INS)在各种条件下进行氧化。通过反相高效液相色谱法监测氧化程度。只有铜离子能催化胰岛素氧化,而其他金属或其组合(如镍离子/钴离子、钴离子/铬离子和镍离子/铬离子)均不能,例如,当20微摩尔胰岛素/8.8微摩尔锌离子暴露于8微摩尔铜离子和50微摩尔抗坏血酸中90分钟时,氧化程度达45%。铜离子催化的氧化主要针对胰岛素的B链,该链上有两个组氨酸残基。