Bioactivities of Qinghaosu Derivatives and Analogs

Since artemisinin antimalarial dmgs were developed by Chinese scientists in the 1980s, over 10 million patients infected with falciparum malaria including 

Many experimental and clinical studies performed in China reveal that artemisinin, artemether, and artesunate are not only the potent antimalarial drugs but also the 

Some components of A. annua L., such as qinghaosu (1), artemisinin B (10), arte-misinic acid (20), artemisitene (26), flavnoids, and other terpenoids, showed antitumor activities at varying concentrations against L-1210, P-388, A-549, HT-29, MCF-7, and KB in vitro.  

In the assay of cytotoxicity of qinghaosu and related compounds against Ehrlich ascites tumor cells, qinghaosu, artemether, arteether, and artesunate exhibited cytotoxicity (IC50 12.2 29.8 pM), artemisitene 51 was more active (IC50 6.8 pM), and the dimer of dihydroartemisinin was the most potent (IC50 1.4 pM).  

The antitumor effect of artesunate was tested in vitro and in vivo in China.  

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