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Molecules 2017, 22(12), 2138; doi:10.3390/molecules22122138

Support for Natural Small-Molecule Phenols as Anxiolytics

1
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Liangxiang Town, Fangshan District, Beijing 102488, China
2
National Institute on Drug Dependence, Peking University, 38#, Xueyuan Road, Haidian District, Beijing 100191, China
*
Authors to whom correspondence should be addressed.
Received: 29 October 2017 / Revised: 30 November 2017 / Accepted: 30 November 2017 / Published: 6 December 2017
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Abstract

Natural small-molecule phenols (NSMPs) share some bioactivities. The anxiolytic activity of NSMPs is attracting attention in the scientific community. This paper provides data supporting the hypothesis that NSMPs are generally anxiolytic. The anxiolytic activities of seven simple phenols, including phloroglucinol, eugenol, protocatechuic aldehyde, vanillin, thymol, ferulic acid, and caffeic acid, were assayed with the elevated plus maze (EPM) test in mice. The oral doses were 5, 10 and 20 mg/kg, except for phloroglucinol for which the doses were 2.5, 5 and 10 mg/kg. All tested phenols had anxiolytic activity in mice. The phenolic hydroxyl group in 4-hydroxycinnamic acid (4-OH CA) was essential for the anxiolytic activity in the EPM test in mice and rats compared to 4-chlorocinnamic acid (4-Cl CA). The in vivo spike recording of rats’ hippocampal neurons also showed significant differences between 4-OH CA and 4-Cl CA. Behavioral and neuronal spike recording results converged to indicate the hippocampal CA1 region might be a part of the anxiolytic pathways of 4-OH CA. Therefore, our study provides further experimental data supporting NSMPs sharing anxiolytic activity, which may have general implications for phytotherapy because small phenols occur extensively in herbal medicines. View Full-Text
Keywords: anxiety; phenolic hydroxyl group; elevated plus-maze test; phenolic compounds; neuronal spike; hippocampus anxiety; phenolic hydroxyl group; elevated plus-maze test; phenolic compounds; neuronal spike; hippocampus
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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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MDPI and ACS Style

Wang, X.; Chen, Y.; Wang, Q.; Sun, L.; Li, G.; Zhang, C.; Huang, J.; Chen, L.; Zhai, H. Support for Natural Small-Molecule Phenols as Anxiolytics. Molecules 2017, 22, 2138.

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