Objective   To investigate the cytotoxicity of 3 artemisinin derivatives

artemisinin (ART)

dihydroartemisinin (DHA) and artesunate (AS) to 2 glioma cell lines CHG-5 and U87

to select a compound which have radiosensitization on both cell lines when synergized with β-ray.    Methods   Firstly

we employed MTT assay to measure the IC

50

of 2 cell lines to ART and its derivatives. When synergized with β

-ray

the radiosensitization of drugs with 20% IC

50

and selected the optimal one were observed. Subsequently

sensitivity enhancement ratio (SER) was determined by colonyforming assay. Scratch test was used to observe the effect of objective drug on cell migration. Then

intracellular reduced GSH was measured. Finally

flow cytometry was employed to assay the cell apoptosis and cell cycle distribution.    Results   For CHG-5

the IC

50

of ART

DHA and AS was 1.47

0.20 and 0.29 mmol/L

respectively. Correspondingly

the IC

50

for U87 was 1.61

0.25 and 0.46 mmol/L

respectively. Only AS suppressed the proliferation of both cell lines under the concentration of 20% IC

50

when combined with β-ray. Furthermore

the SER of 0.06 mmol/L AS for CHG-5 was 1.25. Meanwhile

0.06 mmol/L AS significantly inhibited the cell migration. Compared with medium group

GSH production was reduced after the treatment of 0.06 mmol/L AS (P0.05). Flow cytometry indicated that the cell cycle was arrested in G

1

phase after 0.06 mmol/L AS treatment.    Conclusion   Our results indicate that AS from the 3 artemisinin derivatives enhances the radiosensitivity of human glioma cell line CHG-5 to β-ray

which may be associated with the decreased intracellular GSH and G

1

arrest.