Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via\nSteglich esterification and characterized by 1H-NMR, IR, and mass spectral studies. Their analgesic\nand anti-inflammatory activities were investigated after transdermal delivery on models of formalin,\ncapsaicin, and AITC-induced pain, respectively. Glycine esters of menthol and borneol exhibited\nhigher antinociceptive action, whereas eugenol derivative significantly suppressed the development\nof the inflammatory process. The mechanism of competitive binding between terpenoid esters\nand TRPA1/TRPV1 agonists was proposed explaining significant analgesic effect of synthesized\nderivatives. For an explanation of high anti-inflammatory activity, competitive inhibition between\nterpenoid esters and AITC for binding sites of the TRPA1 ion channel has been suggested.
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