TRPA1 Modulating C14 Polyacetylenes from the Iranian Endemic Plant Echinophora platyloba

Author:

Chianese Giuseppina,Sirignano Carmina,Shokoohinia Yalda,Mohammadi Zeynab,Bazvandi Leili,Jafari Fataneh,Jalilian Fereshteh,Schiano Moriello Aniello,De Petrocellis Luciano,Taglialatela-Scafati Orazio,Rigano DanielaORCID

Abstract

Phytochemical investigation of the apolar extract obtained from aerial parts of the Iranian endemic plant Echinophora platyloba DC (Apiaceae) resulted in the characterization of the polyacetylene fraction of this plant. This resulted to be composed of the known echinophorins A and B, embedding the very rare α-pyrone terminal, and of the new echinophorin D (3), including also three conjugated triple bonds. The chemical structures of these compounds were secured by detailed inspection of MS and 1D/2D NMR spectra. The isolated polyacteylenes were evaluated for their modulation of six thermo-TRP channels and they revealed a selective activity on TRPA1, an ion channel involved in the mediation of neuropathic and inflammatory pain. This is the first report on the activity of plant polyacetylenes on transient receptor potential (TRP) channels.

Funder

Ministero dell’Istruzione, dell’Università e della Ricerca

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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