Characterization of the inhibitory effect of gastrodigenin and gastrodin on M-type K⁺ currents in pituitary cells and hippocampal neurons

Gastrodigenin (HBA) and gastrodin (GAS) are phenolic ingredients found in Gastrodia elata Blume (GEB), a traditional Chinese herbal medicine. These compounds have been previously used to treat cognitive dysfunction, convulsion, and dizziness. However, at present, there is no available information regarding their potential ionic effects in electrically excitable cells. In the current study, the possible effects of HBA and GAS on different ionic currents in pituitary GH3 cells and hippocampal mHippoE-14 neurons were investigated using the patch-clamp technique. The addition of HBA or GAS resulted in the differential inhibition of the M-type K⁺ current (I_K(M)) density in a concentration-dependent manner in GH₃ cells. HBA resulted in a slowing of the activation time course of I_K(M), while GAS elevated it. HBA also mildly suppressed the density of erg-mediated or the delayed-rectifier K⁺ current in GH₃ cells. Neither GAS nor HBA (10 µM) modified the voltage-gated Na⁺ current density, although they suppressed the L-type Ca²⁺ current density at the same concentration. In hippocampal mHippoE-14 neurons, HBA was effective at inhibiting I_K(M) density as well as slowing the activation time course. Taken together, the present study provided the first evidence that HBA or GAS could act on cellular mechanisms, and could therefore potentially have a functional influence in various neurologic disorders.