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Identification of natural compound carnosol as a novel TRPA1 receptor agonist.
Molecules. 2014 Nov 14; 19(11):18733-46.M

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.

Authors+Show Affiliations

Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. zhaichenxi1991@163.com.Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. liuqingtcm@gmail.com.Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. zhangyuxinwjzy@163.com.Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. alana6268@126.com.Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. zhangyuxinwjzy@163.com.Laboratory of Genome Variations and Precision Bio-Medicine, Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing 100101, China. lishiyou@big.ac.cn.Key Laboratory of TCM-information Engineer of State Administration of TCM, School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China. yjqiao@263.net.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25405290

Citation

Zhai, Chenxi, et al. "Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist." Molecules (Basel, Switzerland), vol. 19, no. 11, 2014, pp. 18733-46.
Zhai C, Liu Q, Zhang Y, et al. Identification of natural compound carnosol as a novel TRPA1 receptor agonist. Molecules. 2014;19(11):18733-46.
Zhai, C., Liu, Q., Zhang, Y., Wang, S., Zhang, Y., Li, S., & Qiao, Y. (2014). Identification of natural compound carnosol as a novel TRPA1 receptor agonist. Molecules (Basel, Switzerland), 19(11), 18733-46. https://doi.org/10.3390/molecules191118733
Zhai C, et al. Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist. Molecules. 2014 Nov 14;19(11):18733-46. PubMed PMID: 25405290.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Identification of natural compound carnosol as a novel TRPA1 receptor agonist. AU - Zhai,Chenxi, AU - Liu,Qing, AU - Zhang,Yuxin, AU - Wang,Shifeng, AU - Zhang,Yanling, AU - Li,Shiyou, AU - Qiao,Yanjiang, Y1 - 2014/11/14/ PY - 2014/10/09/received PY - 2014/11/06/revised PY - 2014/11/07/accepted PY - 2014/11/19/entrez PY - 2014/11/19/pubmed PY - 2015/10/6/medline SP - 18733 EP - 46 JF - Molecules (Basel, Switzerland) JO - Molecules VL - 19 IS - 11 N2 - 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. SN - 1420-3049 UR - https://www.unboundmedicine.com/medline/citation/25405290/Identification_of_natural_compound_carnosol_as_a_novel_TRPA1_receptor_agonist_ L2 - https://www.mdpi.com/resolver?pii=molecules191118733 DB - PRIME DP - Unbound Medicine ER -