title: 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.
abstract: 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.
authors.affiliation: Laboratory of Ethnopharmacology, Institute of Integrated Traditional Medicine and Western Medicine, Xiangya Hospital, Central South University, Changsha 410008, China.
authors.forename: Rong
authors.initials: R
authors.lastname: Fan
authors.forename: Xi
authors.initials: X
authors.lastname: Huang
authors.forename: Yang
authors.initials: Y
authors.lastname: Wang
authors.forename: Xiao
authors.initials: X
authors.lastname: Chen
authors.forename: Ping
authors.initials: P
authors.lastname: Ren
authors.forename: Hui
authors.initials: H
authors.lastname: Ji
authors.forename: Ying
authors.initials: Y
authors.lastname: Xie
authors.forename: Yingjin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Huang
authors.forename: Xinjian
authors.initials: X
authors.lastname: Qiu
authors.forename: Zhaoqian
authors.initials: Z
authors.lastname: Liu
authors.forename: Honghao
authors.initials: H
authors.lastname: Zhou
authors.forename: Lan
authors.initials: L
authors.lastname: Fan
authors.forename: Lichen
authors.initials: L
authors.lastname: Gao