Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist
AbstractThe 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. View Full-Text
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Zhai, C.; Liu, Q.; Zhang, Y.; Wang, S.; Zhang, Y.; Li, S.; Qiao, Y. Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist. Molecules 2014, 19, 18733-18746.
Zhai C, Liu Q, Zhang Y, Wang S, Zhang Y, Li S, Qiao Y. Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist. Molecules. 2014; 19(11):18733-18746.Chicago/Turabian Style
Zhai, Chenxi; Liu, Qing; Zhang, Yuxin; Wang, Shifeng; Zhang, Yanling; Li, Shiyou; Qiao, Yanjiang. 2014. "Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist." Molecules 19, no. 11: 18733-18746.