Synthesis and Pharmacological Properties of Novel Esters Based on Monoterpenoids and Glycine

Pharmaceuticals
Mariia Nesterkina, Iryna Kravchenko

Abstract

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

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Citations

Oct 24, 2018·Journal of Liposome Research·Mariia NesterkinaIryna Kravchenko
Aug 25, 2020·The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology·Phuong Thao Thi NguyenSeong Kyu Han
Apr 16, 2021·Plant Molecular Biology·Chisato TsuzukiGen-Ichiro Arimura

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