[The inhibitory effects of artemisinin-derivatives on Na+ and K+ channels in comparison with those of procaine].
Some derivatives of artemisinin have been shown to have local anesthesia action. By using patch-clamp whole cell recording configuration, the effects of five artemisinin-derivatives on the voltage-gated INa and IK have been studied on differentiated NG108-15 cells with reference to procaine. The results showed that all the five artemisinin-derivatives clearly inhibited the voltage-gated sodium current (INa) of the cells in a dose-dependent manner and the effect was partially reversibly. Among the five artemisinin-derivatives, SM541 has been shown to be most potent, approaching that of procaine. However, 300 mumol/L procaine showed only a slight inhibition of IK, whereas all the five derivatives at the same concentration not only decreased IK clearly, but also accelerated its inactivation. Except for SM541, the inhibitory effects on IK decreased rapidly with perfusion of the rest 4 derivatives.
Huang
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FS
Key Laboratory of Neurobiology, Shanghai Institute of Physiology, Chinese Academy of Sciences, Shanghai 200031.
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Shi
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D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D037621:Artemisinins; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005910:Glioma / Q000473:pathology; D006822:Hybrid Cells; D051379:Mice; D009447:Neuroblastoma / Q000473:pathology; D015221:Potassium Channels / Q000187:drug effects*; D011343:Procaine / Q000494:pharmacology*; D051381:Rats; D012717:Sesquiterpenes / Q000494:pharmacology*; D015222:Sodium Channels / Q000187:drug effects*; D014407:Tumor Cells, Cultured
D000779:Anesthetics, Local; D037621:Artemisinins; D004365:Drugs, Chinese Herbal; D015221:Potassium Channels; D012717:Sesquiterpenes; D015222:Sodium Channels; D011343:Procaine; C031327:artemisinin