Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells

Lempereur, Maëlle; Majewska, Claire; Brunquers, Amandine; Wongpramud, Sumalee; Valet, Bénédicte; Janssens, Philippe; Dillemans, M.; Nedervelde, Laurence Van; Gallo, Dominique

doi:10.1155/2016/9747863

Cited by 4 publications

(4 citation statements)

References 48 publications

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“…It has long been known that secondary metabolites, which are secreted from the lupulin glands of female hop cones (but are also present in male inflorescences at a low concentration), are groups of compounds that are not synthesized by humans but are valuable to human life, especially for the beer-brewing industry and human health. , Among these metabolites, the resinous compounds can be classified as bitter acids, polyphenols, and volatile oil. The volatile oil comprises mainly terpenoids and possesses moderate antibacterial effects against the Gram-positive bacteria Enterococcus , Bacillus subtilis , and Staphylococcus aureus and the Gram-negative bacteria Escherichia coli , Clostridium perfringens , Enterococcus faecalis , and Staphylococcus aureus subs , as well as an antifungal effect against the fungus Trichophyton interdigitale and the yeast Candida albicans . , However, the present review focuses on the effects of hop bitter acids and lupulin-associated polyphenols (especially xanthohumol), which have been reported to exert a wide range of anticancer effects and to prevent chronic diseases, as a chemotherapeutic modality, both in vitro and in vivo. − …”

Section: Identification Of Nutritional Factors In H Lupulusmentioning

confidence: 99%

“…Oral administration of 0.1% tetrahydro- or hexahydro-iso-α-acids for 6 weeks to diethyl nitrosamine-induced male Wistar rats (body weight 180–190 g) with hepatocellular carcinoma, which is the third leading cause of cancer-related deaths globally, because of alcohol, nonalcoholic steatohepatitis, hepatitis B, and hepatitis C infection, resulted in the reduction of the transformation marker glutathione- S -transferase-positive areas and tumor numbers in the liver compared to the diethylnitrosamine treated control rats. , In another study, tetrahydro-iso-α-acids inhibited estrogen receptor-alpha transcriptional activity, induced a 75% decrease in metabolic activity measured by the MTT assay, and reduced the proliferation of Michigan Cancer Foundation-7 (MCF-7) breast cancer cells, based on the reversal of the effect of 17β-estradiol on cell cycle progression and then a slowdown of the cell cycle . Rho-iso-α-acids, prepared from a modified hop extract, have been shown to potently and selectively inhibit iCOX-2-stimulated prostaglandin E 2 biosynthesis, with minimal effects on cyclooxygenase (COX)-1 or COX-2, in lipopolysaccharide-induced mouse macrophage RAW 264.7 cells (IC 50 of COX-1 was 289 μg/mL, IC 50 of COX-2 was 1.3 μg/mL) (Hall et al, 2008).…”

Section: Bitter Acidsmentioning

confidence: 99%

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Role of Characteristic Components of Humulus lupulus in Promoting Human Health

Lin

Xiang

Chen

et al. 2019

J. Agric. Food Chem.

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Over the next 50 years, the prevention and control of chronic diseases, such as obesity, cardiovascular disease, Alzheimer's disease, and many cancers, will be one of the most critical challenges in human health. Plant biochemistry and phytonutrient supplements are a promising complementary therapy for the management of chronic disease. Among them, Humulus lupulus has attracted special attention throughout the world because it contains numerous dietary phytochemicals that not only contribute to the aroma and flavor of beer but may also be used for medicinal purposes, as its properties include antiseptic, (an)aphrodisiac, anticancer, antiplatelet, antibacterial, antidiuretic, anti-inflammatory, sedative, hypnotic, and stomachic properties. This review sought to identify and understand the risk factors for chronic disease with a focus on two types of phytochemicals, bitter acids and xanthohumol. The goal was to understand how their metabolites promote human health and reduce the risk of chronic disease.

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Section: Identification Of Nutritional Factors In H Lupulusmentioning

confidence: 99%

Section: Bitter Acidsmentioning

confidence: 99%

Role of Characteristic Components of Humulus lupulus in Promoting Human Health

Lin

Xiang

Chen

et al. 2019

J. Agric. Food Chem.

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“…Both ERα and ERβ bind co-factor proteins through LxxLL motifs. It is reported that tetrahydro-iso-alpha acid inhibits the estrogen-stimulated transcriptional activity of ERs by interfering with the binding of ERs to LxxLL motifs in breast cancer cell line MCF-7 [ 102 , 103 ]. One of the enzothiophenone derivatives also has an inhibitory action on the binding of ERα to LxxLL, and the compound also represses the transcription of the mutant form of ERα gene (ESR1) [ 104 ].…”

Section: Future Perspectives On Exploring Ppi In Hormone-dependentmentioning

confidence: 99%

Exploring Protein–Protein Interaction in the Study of Hormone-Dependent Cancers

Miki

Iwabuchi

Ono

et al. 2018

IJMS

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Estrogen receptors promote target gene transcription when they form a dimer, in which two identical (homodimer) or different (heterodimer) proteins are bound to each other. In hormone-dependent cancers, hormone receptor dimerization plays pivotal roles, not only in the pathogenesis or development of the tumors, but also in the development of therapeutic resistance. Protein–protein interactions (PPIs), including dimerization and complex formation, have been also well-known to be required for proteins to exert their functions. The methods which could detect PPIs are genetic engineering (i.e., resonance energy transfer) and/or antibody technology (i.e., co-immunoprecipitation) using cultured cells. In addition, visualization of the target proteins in tissues can be performed using antigen–antibody reactions, as in immunohistochemistry. Furthermore, development of microscopic techniques (i.e., electron microscopy and confocal laser microscopy) has made it possible to visualize intracellular and/or intranuclear organelles. We have recently reported the visualization of estrogen receptor dimers in breast cancer tissues by using the in situ proximity ligation assay (PLA). PLA was developed along the lines of antibody technology development, and this assay has made it possible to visualize PPIs in archival tissue specimens. Localization of PPI in organelles has also become possible using super-resolution microscopes exceeding the resolution limit of conventional microscopes. Therefore, in this review, we summarize the methodologies used for studying PPIs in both cells and tissues, and review the recently reported studies on PPIs of hormones.

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“…In today’s society, breast cancer is one of the most common and lethal cancers. Estrogen receptors have a close correlation with the development of breast cancer, and according to related studies, estrogen receptor alpha (ERα) in estrogen has a strong promoting effect on the dominant characterization of breast cancer ( Lempereur et al, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

A machine learning-based approach to ERα bioactivity and drug ADMET prediction

Chen

et al. 2023

Front. Genet.

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By predicting ERα bioactivity and mining the potential relationship between Absorption, Distribution, Metabolism, Excretion, Toxicity (ADMET) attributes in drug research and development, the development efficiency of specific drugs for breast cancer will be effectively improved and the misjudgment rate of R&D personnel will be reduced. The quantitative prediction model of ERα bioactivity and classification prediction model of Absorption, Distribution, Metabolism, Excretion, Toxicity properties were constructed. The prediction results of ERα bioactivity were compared by XGBoot, Light GBM, Random Forest and MLP neural network. Two models with high prediction accuracy were selected and fused to obtain ERα bioactivity prediction model from Mean absolute error (MAE), mean squared error (MSE) and R2. The data were further subjected to model-based feature selection and FDR/FPR-based feature selection, respectively, and the results were placed in a voting machine to obtain Absorption, Distribution, Metabolism, Excretion, Toxicity classification prediction model. In this study, 430 molecular descriptors were removed, and finally 20 molecular descriptors with the most significant effect on biological activity obtained by the dual feature screening combined optimization method were used to establish a compound molecular descriptor prediction model for ERα biological activity, and further classification and prediction of the Absorption, Distribution, Metabolism, Excretion, Toxicity properties of the drugs were made. Eighty variables were selected by the model ExtraTreesClassifier Classifie, and 40 variables were selected by the model GradientBoostingClassifier to complete the model-based feature selection. At the same time, the feature selection method based on FDR/FPR is also selected, and the three classification models obtained by the two methods are placed into the voting machine to obtain the final model. The experimental results showed that the model‘s evaluation indexes and roc diagram were excellent and could accurately predict ERα bioactivity and Absorption, Distribution, Metabolism, Excretion, Toxicity properties. The model constructed in this study has high accuracy, fast convergence and robustness, has a very high accuracy for Absorption, Distribution, Metabolism, Excretion, Toxicity and ERα classification prediction, has bright prospects in the biopharmaceutical field, and is an important method for energy conservation and yield increase in the future.

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Tetrahydro-iso-alpha Acids Antagonize Estrogen Receptor Alpha Activity in MCF-7 Breast Cancer Cells

Cited by 4 publications

References 48 publications

Role of Characteristic Components of Humulus lupulus in Promoting Human Health

Role of Characteristic Components of Humulus lupulus in Promoting Human Health

Exploring Protein–Protein Interaction in the Study of Hormone-Dependent Cancers

A machine learning-based approach to ERα bioactivity and drug ADMET prediction

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