The actions of peppermint oil and menthol on calcium channel dependent process in intestinal, neuronal and cardiac preparations

Author(s): Ferrante, J., Luchowski, E., Rutledge, A., Wei, X., Triggle, D.

Journal/Book: Aliment Pharmacol Ther. 1988; 2: 101-118.

Abstract: The activities of menthol and peppermint oil were determined in guineapig ileal smooth muscle, in rat and guinea-pig atrial and papillary muscle, in rat brain synaptosomes and in chick retinal neurones by pharmacological 45Caz2+ uptake and radioligand binding assays. Menthol is a major constituent of peppermint oil and is approximately twice as potent as peppermint oil as an inhibitor of K+ depolarization-induced and electrically stimulated responses in ileum and electrically stimulated atrial and papillary muscles. IC50 values in the deal preparation ranged from 7.7 to 28.1 ?g ml-1 and in the cardiac preparations from 10.1 to 68.5 ?g ml-1. Similar potencies were demonstrated against K+ depolarization-induced 45Caz2+ uptake in synaptosomes and against K+ depolarization and Bay K 8644-induced uptake in chick retinal neurons. IC50 values for menthol inhibition of K+ and Bay K 8644 responses in the retinal neurons were 1.1 x 10-4 M (17.2 ?g ml-1) and 1.75 x 10-4 M (26.6 /?g ml-1), respectively, and for peppermint oil were 20.3 and 41.7?g ml-1 respectively. Both menthol and peppermint oil inhibited specific [3H]nitrendipine and [3H]PN 200-110 binding to smooth and cardiac muscle and neuronal preparations with potencies comparable to, but slightly lower than, those measured in the pharmacological and 45Caz2+ uptake experiments. Binding of menthol and peppermint oil, studied at 78?g ml-1, was competitive against [3H] nitrendipine in both smooth muscle and synaptosome preparations. The data indicate that both menthol and peppermint oil exert Ca2+ channel blocking properties which may underlie their use in irritable bowel syndrome. Ca2+ channel antagonism may not be the only pharmacological effect of menthol and peppermint oil contributing to intestinal smooth muscle relaxation.

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