Humulus

Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

The female flowers of hops are used throughout the world as a flavoring agent for beer. Recently, there has been increasing interest in the potential estrogenic properties of hop extracts. Among the possible estrogenic compounds in hops, 8-prenylnaringenin is perhaps most significant due to its high in vitro potency exceeding that of other known phytoestrogens. Since data regarding the pharmacokinetic properties of this compound are lacking, we investigated the in vitro metabolism of 8-prenylnaringenin by human liver microsomes.

Author(s): 
Nikolic, Dejan
Li, Yongmei
Chadwick, Lucas R.
Grubjesic, Simonida
Schwab, Pia
Metz, Peter
van Breemen, Richard B.
Publication Title: 
Journal of Agricultural and Food Chemistry

Because the prevailing form of hormone replacement therapy is associated with the development of cancer in breast and endometrial tissues, alternatives are needed for the management of menopausal symptoms. 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.

Author(s): 
Overk, Cassia R.
Yao, Ping
Chadwick, Lucas R.
Nikolic, Dejan
Sun, Yongkai
Cuendet, Muriel A.
Deng, Yunfan
Hedayat, A. S.
Pauli, Guido F.
Farnsworth, Norman R.
van Breemen, Richard B.
Bolton, Judy L.
Publication Title: 
Phytomedicine: International Journal of Phytotherapy and Phytopharmacology

As the population ages, there is an ever-increasing need for therapeutic agents that can be used safely and efficaciously to manage symptoms related to postmenopausal estrogen deficiency. Endogenous estrogens, e.g., 17beta-estradiol, of exogenous mammalian origin, e.g., horses, have long been used to manage such symptoms. There are more than 20 different classes of phytochemicals that have demonstrated affinity for human estrogen receptors in vitro.

Author(s): 
Chadwick, L. R.
Pauli, G. F.
Farnsworth, N. R.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

The female flowers of hops (Humulus lupulus L.) are used in the brewing of beer and are under investigation for use in dietary supplements for the management of menopausal symptoms in women. Hop extracts contain the weakly estrogenic compound isoxanthohumol (IX), proestrogenic xanthohumol, and the potent estrogen 8-prenylnaringenin (8PN). Because IX can be metabolized in the human liver to form 8PN, the specific cytochrome P450 (P450) enzymes responsible for this O-demethylation reaction were identified.

Author(s): 
Guo, Jian
Nikolic, Dejan
Chadwick, Lucas R.
Pauli, Guido F.
van Breemen, Richard B.
Publication Title: 
Pharmaceutical Research

PURPOSE: The absorption potential and metabolism of 8-prenylnaringenin (8-PN) from hops (Humulus lupulus L.) were investigated. 8-PN is a potent estrogen with the potential to be used for the relief of menopausal symptoms in women. METHODS: Monolayers of the human intestinal epithelial cancer cell line Caco-2 and human hepatocytes were incubated with 8-PN to model its intestinal absorption and hepatic metabolism, respectively.

Author(s): 
Nikolic, Dejan
Li, Yongmei
Chadwick, Lucas R.
van Breemen, Richard B.
Publication Title: 
Combinatorial Chemistry & High Throughput Screening

A high throughput screening assay for the identification of ligands to pharmacologically significant receptors was developed based on magnetic particles containing immobilized receptors followed by liquid chromatography-mass spectrometry (LC-MS). This assay is suitable for the screening of complex mixtures such as botanical extracts. For proof-of-principle, estrogen receptor-alpha (ER-alpha) and ER-beta were immobilized on magnetic particles functionalized with aldehyde or carboxylic acid groups.

Author(s): 
Choi, Yongsoo
van Breemen, Richard B.
Publication Title: 
Chemico-Biological Interactions

The lack of a safe and reliable alternative to hormone therapy (HT) for treating menopausal symptoms underscores the need for alternative therapies. OBJECTIVE: The purpose of this study was to assess the in vivo estrogenic effects of the botanical dietary supplements Trifolium pratense (red clover) and Humulus lupulus (hops), and two compounds obtained from H. lupulus, isoxanthohumol and 8-prenylnaringenin (8-PN) using the ovariectomized uterotrophic adult rat model. A H. lupulus extract and a 30% isoflavone extract of T.

Author(s): 
Overk, Cassia R.
Guo, Jian
Chadwick, Lucas R.
Lantvit, Daniel D.
Minassi, Alberto
Appendino, Giovanni
Chen, Shao-Nong
Lankin, David C.
Farnsworth, Norman R.
Pauli, Guido F.
van Breemen, Richard B.
Bolton, Judy L.
Publication Title: 
Planta Medica

The use of chromatographic assays to assess the residual complexity of materials that are purified from natural sources by chromatographic means is, in a sense, a case of the fox watching the henhouse. Beside their static residual complexity, which is intrinsic to their metabolic origin, biologically active natural materials can also be involved in chemical reactions that lead to dynamic residual complexity.

Author(s): 
Chen, Shao-Nong
Lankin, David C.
Chadwick, Lucas R.
Jaki, Birgit U.
Pauli, Guido F.
Publication Title: 
Molecular Nutrition & Food Research

Hop-derived products may contain xanthohumol (XN), isoxanthohumol (IX), and the potent phytoestrogen 8-prenylnaringenin (8-PN). To evaluate the potential health effects of these prenylflavonoids on breast tissue, their concentration, nature of metabolites, and biodistribution were assessed and compared with 17beta-estradiol (E(2)) exposure. In this dietary intervention study, women were randomly allocated to hop (n=11; 2.04 mg XN, 1.20 mg IX, and 0.1 mg 8-PN per supplement) or control (n=10).

Author(s): 
Bolca, Selin
Li, Jinghu
Nikolic, Dejan
Roche, Nathalie
Blondeel, Phillip
Possemiers, Sam
De Keukeleire, Denis
Bracke, Marc
Heyerick, Arne
van Breemen, Richard B.
Depypere, Herman
Publication Title: 
Analytical Chemistry

Inhibitors of quinone reductase-2 (NQO2; QR-2) can have antimalarial activity and antitumor activities or can function as chemoprevention agents by preventing the metabolic activation of toxic quinones such as menadione. To expedite the search for new natural product inhibitors of QR-2, we developed a screening assay based on ultrafiltration liquid chromatography-mass spectrometry that is compatible with complex samples such as bacterial or botanical extracts.

Author(s): 
Choi, Yongsoo
Jermihov, Katherine
Nam, Sang-Jip
Sturdy, Megan
Maloney, Katherine
Qiu, Xi
Chadwick, Lucas R.
Main, Matthew
Chen, Shao-Nong
Mesecar, Andrew D.
Farnsworth, Norman R.
Pauli, Guido F.
Fenical, William
Pezzuto, John M.
van Breemen, Richard B.
van Breemen, Richard R.

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