Referenced in: none

Automatically associated channels: TRP , TRPA , TRPA1 , TRPM , TRPM8 , TRPV , TRPV3

Title: Identification of natural compound carnosol as a novel TRPA1 receptor agonist.

Authors: Chenxi Zhai, Qing Liu, Yuxin Zhang, Shifeng Wang, Yanling Zhang, Shiyou Li, Yanjiang Qiao

Journal, date & volume: Molecules, 2014 , 19, 18733-46

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/25405290

Abstract
The transient receptor potential ankyrin 1 (TRPA1) cation channel is one of the well-known targets for pain therapy. Herbal medicine is a rich source for new drugs and potentially useful therapeutic agents. To discover novel natural TRPA1 agonists, compounds isolated from Chinese herbs were screened using a cell-based calcium mobilization assay. Out of the 158 natural compounds derived from traditional Chinese herbal medicines, carnosol was identified as a novel agonist of TRPA1 with an EC50 value of 12.46 µM. And the agonistic effect of carnosol on TRPA1 could be blocked by A-967079, a selective TRPA1 antagonist. Furthermore, the specificity of carnosol was verified as it showed no significant effects on two other typical targets of TRP family member: TRPM8 and TRPV3. Carnosol exhibited anti-inflammatory and anti-nociceptive properties; the activation of TRPA1 might be responsible for the modulation of inflammatory nociceptive transmission. Collectively, our findings indicate that carnosol is a new anti-nociceptive agent targeting TRPA1 that can be used to explore further biological role in pain therapy.