Effects of α-Asarone on the Glutamate Transporter EAAC1 in Xenopus Oocytes

The major excitatory neurotransmitter transporter EAAC1 in the mammalian central nervous system is considered a possible target for Chinese herbal medicine. Extracts of ACORUS TATARINOWII (Schott) were tested for their effects on EAAC1 activity. XENOPUS oocytes with heterologously expressed EAAC1 were used as the model system. Rate of glutamate uptake was determined by means of the isotopic tracer technique. Glutamate-induced current was recorded under a two-electrode voltage clamp. As a highly effective component, α-asarone was identified. The rate of glutamate uptake was stimulated by 200 μM of α-asarone by about 15 %. In contrast, the same concentration reduced the EAAC1-mediated current by about 35 % at a holding potential of − 60 mV; half maximum inhibition was obtained at about 60 μM. Our experimental data suggest that both stimulation of glutamate uptake and inhibition of EAAC1-mediated current by α-asarone could contribute to reduced excitatory activity.