Fig. 1: Luteolin is a new selective TRPM8 blocker.
From: Dietary targeting of TRPM8 rewires macrophage immunometabolism reducing colitis severity
From an evaluation of various diet-derived compounds affinity for TRPM8, luteolin emerged as a new selective TRPM8 blocker. A Scatter diagram of the theoretically estimated affinity of TRPM8 for 17 diet-derived compounds (Ki). Each point represents a natural compound. In red are reported rutin and luteolin. B Rutin structure and binding site on TRPM8. C Luteolin structure and binding site on TRPM8. D Concentration–response curve of luteolin (0.1–100 μM) on intracellular Ca2+ levels in TRPM8- HEK293, measured in the presence of icilin 0.25 μM, the TRPM8 reference agonist. Data represent the mean ± SEM of ≥5 determinations. E Effect of luteolin (0.1–30 μM) on intracellular Ca2+ levels on HEK293 cells over-expressing TRPM8, TRPV1, and TRPA1 in the presence or not of their respective agonists.
