Structural Modification Of Artemisinin And Its Effect On GSH And

Artemisinin (Qinghaosu) is well-known bioactive ingredients isolated from traditional Chinese herbs Qinghao. The main content of this thesis has conducted the mechanism and medicinal research of artemisinin employing chemistry principals. Two aspects experiments have been carried out, and some new results were obtained.1. 10α-Aryl artemisinin derivatives were synthesized. Using 10α-(2-hydroxy-1-naphthyl)-deoxoartemisinin as substrate, free radical behaviors were investigated upon its reactions with reduced glutathione in the presence of Fe (Ⅱ). Through HPLC separation, new compound 19, P-naphthol and compound 32 were gained, accordingly, we produced the process of free radical mechanism of product 19 and P-naphthol. The other work of structure determination was still in process.2. To explore influence of artemisinin derivatives to the related enzymes, chemical interactions of 10α-(2-hydroxy-1-naphthyl)-deoxoartemisinin and glutathione reductase were studied by LC-MS methods, Unfortunately, all these efforts failed, and no clear evidence was observed for limitation of sensitivity.Although the above results from our research on artemisinin is preliminary, and many difficulties were encountered, it will benefit our further exploration in future drug candidate development through structural modification, and development of new biological probes for molecular mechanism studies. Therefore, this thesis work sets up a starting point and the solid foundation for our future work on development of TCM bioactive components.