谷胱甘肽、表面活性剂共存体系对青蒿素过氧键稳定性的影响

Influence of Peroxy Bond′s Stability of Artemisinin in the Presence of Glutathione and Surfactant

青蒿素的过氧桥键是其抗疟作用的关键部位。采用循环伏安法研究了谷胱甘肽、表面活性剂共存体系对青蒿素过氧键稳定性的影响。实验表明,当青蒿素浓度为1.0mmol/L,谷胱甘肽浓度≥2.0×10-5mol/L时,加入阳离子表面活性剂(1.0×10-5mol/L,DBDAB),在体系中形成了谷胱甘肽-青蒿素-DBDAB三元加合物,该加合物在-0.88V电位下还原,其还原峰电位比游离青蒿素的还原峰电位负移了240mV,其还原反应活化能升高了46·3kJ/moL,使青蒿素的过氧键更趋稳定;而阴离子表面活性剂对体系没有影响。进一步探讨了该三元加合物形成的电极机理。

The characteristic endoperoxide bridge in the artemisinin plays an important role in the antimalarial action. The eyelie voltammetrie experiments were used to study the influence of peroxy bond＇s stability in artemisinin in the presence of glutathione （GSH） and suffaetant. The eyelie voltammetry experiments indicated that when the concentration of artemisinin was 1.0×10^-3 mol/L, CCSH≥2.0×10^-5 mol/L, adding the cationic surfaetant dodeeyl dimethyl benzylamine （DBDAB, 1.0 ×10^-5 moL/L）, the tri-adduet of Glutathione-artemisinin-DBDAB were formed in the ternary system. This tri-adduet reduced at the potential of -0.88 V and its potential shifted 240 mV toward the negative direction compared with that of the free artemisinin. The activation energy is 46.3 kJ/moL higher than that of free artemisinin. So the peroxy bond of artemisinin is more steady. But the anionic suffaetant couldn＇t form the tri-adducts with artermisinin and glutathione. The mechanisms of the tri-adduets formed at the surface of the electrode were discussed.