期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 56, 期 24, 页码 11718-11726出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf803298z
关键词
Black cohosh; N-methylserotonin; Cimicifuga; menopause; serotonin
资金
- Office of Dietary Supplements (ODS) [P50 AT00155]
- National Center for Complementary and Alternative Medicine (NCCAM)
- Office for Research on Women's Health (ORWH)
- National Institute of General Medicine (NIGMS) of the National Institutes of Health (NIH)
- NCCAM [F31 AT 003995]
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-omega-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-omega-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-omega-methylserotonin may be responsible for the serotonergic activity of black cohosh.
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