Synthesis Of Biotinylated Artemisinin Derivatives And Fluorescent Labeled Sinomenine Derivatives

(1) Artemisinin (Qinghaosu), isolated from the Chinese medicinal herb Artenisia annua L in 1971, is a sesquiterpene lactone containing a unique endoperoxide bridge. Some derivatives of artemisinin have been developed and applied as antimalarial drugs for the treatment of multi-drug resistant Plasmodium falciparum. Recent research has also showed that artemisinin and its derivatives have significant anticancer activities. The detailed mechanisms of these drugs remain unclear yet. To investigate the mechanisms of their biological actions, development of suitable molecular probes including biotinylated derivatives is of extreme significance. Four new biotinylated artemisinin derivatives (for identidication their target proteins) were therefore designed and synthesised in this pape.(2) Sinomenine is naturall alkaloid isolated from Chinese medicinal plant Sinomenium acutum. It exhibits immunomodulating and anti-inflammatory activities with unambiguous clinical effets. To study signal transduction pathways of sinomenine and its derivatives, and to explain its molecular mechanisms, fluorescent- probe protocols were used. Considering the influence of labeled group, multi-site labelings were carried on sinomenine and its derivatives, in order to find a suitable fluorescein-labeled compound for biological reaearch.