title: Analogues of perillaketone as highly potent agonists of TRPA1 channel.
abstract: Transient receptor potential (TRP) channels represent interesting molecular target structures involved in a number of different physiological and pathophysiological systems. In particular, TRPA1 channel is involved in nociception and in sensory perception of many pungent chemesthetic compounds, which are widespread in spices and food plants, including Perilla frutescens. A natural compound from P. frutescens (isoegomaketone) and 16 synthetic derivatives of perillaketone have been prepared and tested in vitro on rTRPA1 expressed in HEK293 cells and their potency, efficacy and desensibilisation activity measured. Most derivatives proved to be high potency agonists of TRPA1, with a potency higher than most natural agonists reported in the literature. These furylketones derivatives, represent a new class of chemical structures active on TRPA1 with many potential applications in the agrifood and pharmaceutical industry.
authors.affiliation: Department of Food, Environment and Nutritional Sciences, University of Milano, Via Celoria 2, Milano 20133, Italy. angela.bassoli@unimi.it
authors.forename: A
authors.initials: A
authors.lastname: Bassoli
authors.forename: G
authors.initials: G
authors.lastname: Borgonovo
authors.forename: G
authors.initials: G
authors.lastname: Morini
authors.forename: L
authors.initials: L
authors.lastname: De Petrocellis
authors.forename: A
authors.initials: A
authors.lastname: Schiano Moriello
authors.forename: V
authors.initials: V
authors.lastname: Di Marzo
mesh_terms: D000818:Animals; D057809:HEK293 Cells; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D039821:Monoterpenes / Q000138:chemical synthesis / Q000737:chemistry*; D031343:Perilla / Q000737:chemistry*; D010936:Plant Extracts / Q000138:chemical synthesis / Q000737:chemistry*; D051381:Rats; D050051:Transient Receptor Potential Channels / Q000819:agonists* / Q000737:chemistry
chemical_list: D039821:Monoterpenes; D010936:Plant Extracts; D050051:Transient Receptor Potential Channels; C015426:perilla ketone
keywords: Chemesthesis; Perilla frutescens; Perillaketone; TRPA1 ion channels; Transient receptor potential