AIM: To study the braking effectiveness of artesunate on transforming growth factor (TGF)-β2 mediated epithelial-mesenchymal transition (EMT) in retinal pigment epithelium (RPE) in vitro. METHODS: The fostered ARPE-19 cells were processed with artesunate alone or combined with the TGF-β2. The CCK-8 examination was utilized to test the cell propagation. Cell migration was detected by scratch as well as the Transwell examination. The EMT characters and activation of PI3K/Akt signal channel were estimated by Western blotting and immunofluorescence. The Western blotting was utilized in order to confirm the vitreous of controls as well as patients with proliferative vitreoretinopathy (PVR) were collected and the levels of PI3K, phospho-PI3K, Akt. RESULTS: Disposal of ARPE-19 cells with artesunate (50-150 μmol/L) obviously suppressed their propagation and immigration, which dependent on the concentration and time. Artesunate suppressed the EMT which was induced by TGF-β2 in ARPE-19 cells through sustaining the expression of vimentin and α-SMA through the suppression of PI3K, phospho-PI3K, phospho-Akt and Akt. Levels of PI3K, phospho-PI3K, AKT and phospho-Akt was increased in the vitreous in PVR (P<0.05). CONCLUSION: Such findings indicate that PI3K/Akt signal channel is highly activated in vitreous of PVR. Artesuante is an operative depressor of the propagation, immigration and TGF-β2-mediated EMT of ARPE-19 cells by reduced the expression of PI3K/Akt channel.