Abstract: 　Objective To study the effect of mitochondrial membrane potential and cellular membrane permeability in the neurotoxicity of artemether. Methods Mitochondrial membrane potential and cellular membrane permeability in pheochromocytoma cell and primary cultured rat neuronal cell were measured by flow cytometry, using rhodamine 123(Rh123) and PI as fluorescent dye, respectively. Mitochondrial swelling was measured by spectrometer. Results Artemether could decrease the mitochondrial membrane potential and increase the cellular membrane permeability in both cell types in a dose-dependent manner. In addition, artemether led to mitochondrial swelling with dose-effect and time-effect relationships. Conclusion The decrease of mitochondrial membrane potential plays an important role in the neurotoxicity of artemether. The drug can change the mitochondrial membrane potential and mitochondrial swelling by affecting the permeability transition pore complex located in the mitochondrial membrane, increasing cellular membrane permeability, causing an obstruction and finally leading to neurotoxicity.

Key words: artemether, mitochondria, mitochondrial membrane potential, membrane permeability, membrane swelling