Flavanones

Publication Title: 
Journal of Agricultural and Food Chemistry

Baicalein is a major compound of extracts derived from Scutellaria baicalensis Lamiaceae, which are used as food supplements. Baicalein possesses a high radical scavenging activity and decreases intracellular reactive oxygen species in Hct116 human colon carcinoma cells and in Caenorhabditis elegans . It activates Nrf2, a key transcription factor that binds to the antioxidant responsive element (ARE): Baicalein causes a nuclear accumulation of Nrf2, increases ARE-dependent luciferase activity, and enhances the expression of heme oxygenase-1 in Hct116 cells.

Author(s): 
Havermann, Susannah
Rohrig, Ricarda
Chovolou, Yvonni
Humpf, Hans-Ulrich
W‰tjen, Wim
Publication Title: 
Bioscience Trends

Hepatitis B induced by hepatitis B virus (HBV) remains a major public health problem worldwide. Although several antiviral drugs have been approved for hepatitis B, they cause significant dose-dependent side-effects (interferon-alpha) and drug resistance (lamivudine, etc.). Safe and potent new anti-HBV drugs are urgently needed. Traditional Chinese medicine (TCM) is an established segment of the health care system in China and widely used for hepatitis B in China and many parts of the world.

Author(s): 
Cui, Xiaoyan
Wang, Yueling
Kokudo, Norihiro
Fang, Dingzhi
Tang, Wei
Publication Title: 
American Journal of Physiology. Heart and Circulatory Physiology

Flavonoids within Scutellaria baicalensis may be potent antioxidants on the basis of our studies of S. baicalensis extract. To further this work, we studied the antioxidative effects of baicalein, a flavonoid component of S. baicalensis, in a chick cardiomyocyte model of reactive oxygen species (ROS) generation during hypoxia, simulated ischemia-reperfusion, or mitochondrial complex III inhibition with antimycin A. Oxidant stress was measured by oxidation of the intracellular probes 2',7'-dichlorofluorescin diacetate and dihydroethidium.

Author(s): 
Shao, Zuo-Hui
Vanden Hoek, Terry L.
Qin, Yimin
Becker, Lance B.
Schumacker, Paul T.
Li, Chang-Qing
Dey, Lucy
Barth, Eugene
Halpern, Howard
Rosen, Gerald M.
Yuan, Chun-Su
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: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

Flavonoids represent a diverse group of natural pigments widely distributed in the plant kingdom and are an important component of human diet due to their high content in fruits and vegetables. Since many flavonoids have been shown to be potent inhibitors, substrates, and even inducers of various cytochrome P450 isoforms, there is considerable interest in studying interactions of this class of molecules with the cytochrome P450 enzyme system. In this study, the metabolism of several simple flavanones by rat liver microsomes was investigated and compared.

Author(s): 
Nikolic, Dejan
van Breemen, Richard B.
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: 
The Journal of Pharmacy and Pharmacology

Ritonavir, a protease inhibitor drug, is commonly used in AIDS therapy. As with other chemotherapeutic drugs that cause gastrointestinal adverse effects, ritonavir treatment is associated with significant nausea and vomiting. This study investigated whether Scutellaria baicalensis, and its active flavonoid constituent, baicalein, attenuate the gastrointestinal effects of ritonavir. The effects of herb administration were evaluated in ritonavir-treated rats using a rat pica model, which simulates nausea and vomiting in humans.

Author(s): 
Mehendale, Sangeeta
Aung, Han
Wang, Chong-Zhi
Tong, Robin
Foo, Adela
Xie, Jing-Tian
Yuan, Chun-Su
Publication Title: 
Molecular and Cellular Endocrinology

After the Women's Health Initiative found that the risks of hormone therapy outweighed the benefits, a need for alternative drugs to treat menopausal symptoms has emerged. We explored the possibility that botanical agents used in Traditional Chinese Medicine for menopausal symptoms contain ERbeta-selective estrogens. We previously reported that an extract containing 22 herbs, MF101 has ERbeta-selective properties. In this study we isolated liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, which is one of the plants found in MF101.

Author(s): 
Mersereau, Jennifer E.
Levy, Nitzan
Staub, Richard E.
Baggett, Scott
Zogovic, Tatjana
Zogric, Tetjana
Chow, Sylvia
Ricke, William A.
Tagliaferri, Mary
Cohen, Isaac
Bjeldanes, Leonard F.
Leitman, Dale C.
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.

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