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Evidence-Based Complementary and Alternative Medicine
Volume 2012, Article ID 607584, 8 pages
Research Article

Ethnopharmacokinetic- and Activity-Guided Isolation of a New Antidepressive Compound from Fructus Aurantii Found in the Traditional Chinese Medicine Chaihu-Shugan-San: A New Approach and Its Application

1Laboratory of Ethnopharmacology, Institute of Integrated Traditional Medicine and Western Medicine, Xiangya Hospital, Central South University, Changsha 410008, China
2National Key Clinical Specialist Vocational School of TCM Encephalopathy, Xiangya Hospital, Central South University, Changsha 410008, China
3TCM Pharmacogenetics Laboratory, Central South University, Changsha 410008, China
4Jiangxi Qingfeng Pharmaceutical Company Ltd, Ganzhou 341000, China
5Institute of Clinical Pharmacology, Central South University, Changsha 410008, China

Received 10 August 2011; Revised 9 October 2011; Accepted 17 October 2011

Academic Editor: Boli Zhang

Copyright © 2012 Rong Fan et al. 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.


Aims. We aimed to identify an antidepressive compound found in traditional Chinese medicine (TCM) by a new approach called ethnopharmacokinetic- and activity-guided isolation (EAGI). Methods. The new approach targets an unknown chromatographic peak produced by an absorbed compound found in oral Chaihu-Shugan-San (CSS) taken by patients with depression. Once the compound was isolated from Fructus Aurantii (FA), spectral data was employed to identify the compound. The effects of this compound, FA, and CSS on depressive behaviors were investigated. Results. The identified compound was merazin hydrate (MH) according to the new approach. MH, FA, and CSS significantly reduced immobility time and increased locomotor activity. The effects of MH, FA and CSS were similar to Fluoxetine at high doses. Conclusion. MH, a compound whose antidepressive effect is similar to FA and CSS, was isolated for the first time from FA via targeting its corresponding unknown chromatographic peak, and its antidepressive effect was compared with FA or CSS. These findings highlight the potential for drug R&D and pharmacological research of ∼100,000 TCMs.