High-Concentration Piperine: Capsaicin-Sensitive and -Insensitive Effects on Isolated Organs

Abstract

Piperine (P), a sensory stimulant in black pepper, is an agonist on TRPV1 receptors. Earlier work has showed capsaicin-sensitive and -insensitive mechanisms of the contractile action of P on the intestine. The current isolated organ study in the guinea-pig ileum, urinary bladder and trachea (a) confirms the presence of such components of effect (ileum and bladder); (b) indicates TRPV1 involvement in the effect of 5 or 30 µmol/l of P on the basis of an inhibitory action of the antagonist BCTC (ileum); (c) indicates that HC 030031-sensitive TRPA1 receptors and nifedipine-sensitive Ca(2+) channels contribute to the capsaicin-resistant contraction to 30 µmol/l P (ileum) and (d) shows that the contractile effect of P up to 100 µmol/l (guinea-pig trachea) or 30 µmol/l (guinea-pig urinary bladder) is capsaicin-sensitive and mediated by TRPV1 receptors/channels.