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        Inhibition of human Kv3.1 current expressed in Xenopus oocytes by the toxic venom fraction of Androctonus australis hector

        Amani Cheikh,Rym Benkhalifa,Zied Landoulsi,Imen Chatti,Mohamed El Ayeb 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.11

        AahG50, the toxic fraction of Androctonus australishector venom, was studied on human Kv3.1 channelsactivation, stably expressed in Xenopus oocytes using the twoelectrodevoltage clamp technique. AahG50 reduced Kv3.1currents in a reversible concentration-dependent manner,withan IC50 value and a Hill coefficient of 40.4 ± 0.2 lg/ml and1.3 ± 0.05, respectively. AahG50 inhibited IKv3.1 withoutmodifying the current activation kinetics. The AahG50-induced inhibition of Kv3.1 channels was voltage-dependent,with a gradual increase at lower concentrations and over thevoltage range of channels opening. However, at higher concentrations,the inhibition exhibited voltage dependence onlyin the first range of channels opening from -20 to ?10 mV,but demonstrates a low degree of voltage-dependence whenchannels are fully activated. In the literature, toxins havepreviously been isolated from AahG50, KAaH1 and KAaH2and were reported not to have any effect on IKv3.1. Thepresent article’s findings suggest that AahG50 may contain apeptidic component active on Kv3.1 channels, which inhibitsIKv3.1 in a selective manner.

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