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Molecules 2014, 19(11), 18733-18746;

Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist

Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Laboratory of Genome Variations and Precision Bio-Medicine, Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing 100101, China
Authors to whom correspondence should be addressed.
Received: 9 October 2014 / Revised: 6 November 2014 / Accepted: 7 November 2014 / Published: 14 November 2014
(This article belongs to the Section Natural Products Chemistry)
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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. View Full-Text
Keywords: TRPA1; canosol; anti-nociceptive; calcium mobilization TRPA1; canosol; anti-nociceptive; calcium mobilization

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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.

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