In Vitro Serotonergic Activity of Black Cohosh and Identification of Nω-Methylserotonin as a Potential Active Constituent

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• 作者：Sharla L. Powell ; Tanja Gdecke ; Dejan Nikolic ; Shao-Nong Chen ; Soyoun Ahn ; Birgit Dietz ; Norman R. Farnsworth ; Richard B. van Breemen ; David C. Lankin ; Guido F. Pauli ; Judy L. Bolton
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2008
• 出版时间：December 24, 2008
• 年：2008
• 卷：56
• 期：24
• 页码：11718-11726
• 全文大小：248K
• 年卷期：v.56,no.24(December 24, 2008)
• ISSN：1520-5118

文摘

Cimicifuga racemosa (L.) Nutt. (syn. Actaea racemosa L., black cohosh) is used to relieve menopausal hot flashes, although clinical studies have provided conflicting data, and the active constituent(s) and mechanism(s) of action remain unknown. Because serotonergic receptors and transporters are involved with thermoregulation, black cohosh and its phytoconstituents were evaluated for serotonergic activity using 5-HT₇ receptor binding, cAMP induction, and serotonin selective re-uptake inhibitor (SSRI) assays. Crude extracts displayed 5-HT₇ receptor binding activity and induced cAMP production. Fractionation of the methanol extract led to isolation of phenolic acids and identification of N_ω-methylserotonin by LC-MS/MS. Cimicifuga triterpenoids and phenolic acids bound weakly to the 5-HT₇ receptor with no cAMP or SSRI activity. In contrast, N_ω-methylserotonin showed 5-HT₇ receptor binding (IC₅₀ = 23 pM), induced cAMP (EC₅₀ = 22 nM), and blocked serotonin re-uptake (IC₅₀ = 490 nM). These data suggest N_ω-methylserotonin may be responsible for the serotonergic activity of black cohosh.