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

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