Serotomide and safflomide modulate forskolin-stimulated cAMP formation via 5-HT1 receptor

Abstract 

Serotomide (trans-N-caffeoylserotonin) and safflomide (trans-N-caffeoyltryptamine) belong to serotonin-derived phenylpropenoid amides found in plants. In this paper, serotomide and safflomide were investigated to determine their effects on serotonin receptor 5-HT1 in the renal epithelial (OK) cells, due to their structural similarity to 5-HT1 receptor ligands. At the concentration of 10μM, serotomide was able to inhibit forskolin-stimulated cAMP formation in the OK cells by 31% (p<0.019). The inhibition was repressed by Nan-190 and spiperone (5-HT1 antagonists), suggesting that serotomide suppresses cAMP formation via binding to 5-HT1 receptors in the OK cells. Meanwhile, safflomide could not inhibit forskolin-stimulated cAMP formation at the same concentration (10μM), but repress the inhibition of forskolin-stimulated cAMP by serotonin agonists (e.g., serotonin and 8-OH-DPAT) by 31% (p<0.018), suggesting that safflomide may block 5-HT1 receptors in a similar way to Nan-190 and spiperone. All together the data indicate that serotomide and safflomide may be potent compounds that respectively act to activate and to block 5-HT1 receptors on OK cells.

Keywords: Serotomide, Safflomide, Coffee, 5-HT1 receptor, cAMP, Renal epithelial (OK) cells, Forskolin