Comparison of the in Vitro Estrogenic Activities of Compounds from Hops (Humulus lupulus) and Red Clover (Trifolium pratense)
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- 作者：Cassia R. Overk ; Ping Yao ; Lucas R. Chadwick ; Dejan Nikolic ; Yongkai Sun ; Muriel A. Cuendet ; Yunfan Deng ; A. S. Hedayat ; Guido F. Pauli ; Norman R. Farnsworth ; Richard B. van Breemen ; and Judy L. Bolto
- 刊名：Journal of Agricultural and Food Chemistry
- 出版年：2005
- 出版时间：August 10, 2005
- 年：2005
- 卷：53
- 期：16
- 页码：6246 - 6253
- 全文大小：120K
- 年卷期：v.53,no.16(August 10, 2005)
- ISSN：1520-5118
文摘
Because the prevailing form of hormone replacement therapy is associated with the development ofcancer in breast and endometrial tissues, alternatives are needed for the management of menopausalsymptoms. Formulations of Trifolium pratense L. (red clover) are being used to alleviate menopause-associated hot flashes but have shown mixed results in clinical trials. The strobiles of Humulus lupulusL. (hops) have been reported to contain the prenylflavanone, 8-prenylnaringenin (8-PN), as the mostestrogenic constituent, and this was confirmed using an estrogen receptor ligand screening assayutilizing ultrafiltration mass spectrometry. Extracts of hops and red clover and their individualconstituents including 8-PN, 6-prenylnaringenin (6-PN), isoxanthohumol (IX), and xanthohumol (XN)from hops and daidzein, formononetin, biochanin A, and genistein from red clover were comparedusing a variety of in vitro estrogenic assays. The IC50 values for the estrogen receptor 
and 
bindingassays were 15 and 27 
g/mL, respectively, for hops and 18.0 and 2.0 g/mL, respectively, for thered clover extract. Both of the extracts, genistein, and 8-PN activated the estrogen response element(ERE) in Ishikawa cells while the extracts, biochanin A, genistein, and 8-PN, significantly inducedERE-luciferase expression in MCF-7 cells. Hop and red clover extracts as well as 8-PN up-regulatedprogesterone receptor (PR) mRNA in the Ishikawa cell line. In the MCF-7 cell line, PR mRNA wassignificantly up-regulated by the extracts, biochanin A, genistein, 8-PN, and IX. The two extracts hadEC50 values of 1.1 and 1.9 g/mL, respectively, in the alkaline phosphatase induction assay. On thebasis of these data, hops and red clover could be attractive for the development as herbal dietarysupplements to alleviate menopause-associated symptoms.Keywords: Alkaline phosphatase; estrogen receptor; hops; Humulus lupulus; menopause; progesterone receptor; red clover; Trifolium pratense
and bindingassays were 15 and 27 g/mL, respectively, for hops and 18.0 and 2.0 g/mL, respectively, for thered clover extract. Both of the extracts, genistein, and 8-PN activated the estrogen response element(ERE) in Ishikawa cells while the extracts, biochanin A, genistein, and 8-PN, significantly inducedERE-luciferase expression in MCF-7 cells. Hop and red clover extracts as well as 8-PN up-regulatedprogesterone receptor (PR) mRNA in the Ishikawa cell line. In the MCF-7 cell line, PR mRNA wassignificantly up-regulated by the extracts, biochanin A, genistein, 8-PN, and IX. The two extracts hadEC50 values of 1.1 and 1.9 g/mL, respectively, in the alkaline phosphatase induction assay. On thebasis of these data, hops and red clover could be attractive for the development as herbal dietarysupplements to alleviate menopause-associated symptoms.Keywords: Alkaline phosphatase; estrogen receptor; hops; Humulus lupulus; menopause; progesterone receptor; red clover; Trifolium pratense