Title

Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist

Authors

Chenxi Zhai, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Qing Liu, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Yuxin Zhang, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Shifeng Wang, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Yanling Zhang, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
Shiyou Li, National Center for Pharmaceutical Crops, Arthur Temple College of Forestry and Agriculture, Stephen F. Austin State University
Yanjiang Qiao, Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China

Document Type

Article

Publication Date

2014

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.

Comments

Originally published in Molecules. 2014 Nov 14;19 (11):18733-46

doi: 10.3390/molecules191118733 PMID: 25405290

Repository Citation

Zhai, Chenxi; Liu, Qing; Zhang, Yuxin; Wang, Shifeng; Zhang, Yanling; Li, Shiyou; and Qiao, Yanjiang, "Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist" (2014). NCPC Publications and Patents. 6.
https://scholarworks.sfasu.edu/ncpc_articles/6

DOI

10.3390/molecules191118733