A Molecular Basis for the Inhibition of Transient Receptor Potential Vanilloid Type 1 by Gomisin A

Figure 1

Effect of gomisin A on control oocytes or oocytes expressing human TRPV1 receptor channel. (a) Chemical structure of gomisin A. (b) Application of capsaicin (1 μM) stimulated an inward current, whereas gomisin A (100 μM) alone had no effect on oocytes expressing human TRPV1 receptor channel at a holding potential of −80 mV. Cotreatment of capsaicin (1 μM) and capsazepine (10 μM), which the respective TRPV1 receptor channel antagonist that blocked capsaicin-stimulated inward current, indicated that these receptors were functionally expressed in the experiment. (c) The effect of gomisin A on the capsaicin-stimulated inward current mediated by human TRPV1 receptor channel expressed in Xenopus oocytes. The coapplication of the oocytes with gomisin A (100 μM) with 1 μM capsaicin inhibited the capsaicin-induced inward current in a reversible manner ( from four different frogs). (d) The percent inhibition was % and % by 100 μM gomisin A and 10 μM capsazepine. The preapplication of gomisin A was %, indication that either coapplication or preapplication causes the same extent of inhibition (data not shown). , compared with response of capsaicin.

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