Are flavonoids agonists or antagonists of the natural hormone 17β‐estradiol?

Marino, Maria; Galluzzo, Paola

doi:10.1002/iub.34

Cited by 7 publications

(3 citation statements)

References 31 publications

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“…The extract contains flavonoids like luteolin and apigenin that indicated have strong estrogenicity and progestational activity, respectively. 12 Flavonoids are phytoestrogens that can bind to estrogen receptors (ERα and ERβ) and active many signaling pathways in estrogen-target cells. Phytoestrogens can be a favourable alterrnative to synthetic estrogen.…”

Section: Discussionmentioning

confidence: 99%

Effects of tanacetum parthenium l hydroalcoholic extract on sexual hormones and some liver enzymes

Ramezani¹

2019

MOJWH

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Introduction: Tanacetum parthenium L. is one of the most ancient and well-known medicinal plants that its role in the treatment of a wide range of diseases has been studied. This study assessed the probable effects of hydroalcoholic extract of Tanacetum parthenium L. on liver enzymes, including Alkaline phosphatase (ALP)/ Aspartate aminotransferase (AST). Furthermore sexual hormones (progesterone and estrogen) were evaluated in female mice.Materials and methods: 40 female mice with the mean weight of 30-40 gr were divided into three groups: control, sham, and experimental groups control group did not receive any drug. Sham group only received normal saline. The experimental groups were injected by 25, 50, and 100 mg/kg doses of Tanacetum parthenium extract intraperitoneally for 15 consecutive days. Finally, animals were anesthetized using ether, blood serum was extracted and the serum concentration of AST, ALP, estrogen and progesterone was measured. Data were analyzed by one-way ANOVA. Results:The mean serum level of estrogen and progesterone was significantly higher in the experimental groups 50 and 100 mg/kg compared to the sham and control groups. Serum levels of and AST and ALP indicated significant decrease only at 50 and 100 mg/kg doses of extract. Conclusion:Active ingredients of Tanacetum parthenium L. may act as an antioxidant to decrease production of free radicals or liver enzymes releasing into the blood through stabilization of hepatocyte membrane. On the other hand, Tanacetum parthenium L. extract may have some effects on hormone concentration that is due to phytoestrogen components, and can increase the estrogen and progesterone levels.

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Section: Discussionmentioning

confidence: 99%

Effects of tanacetum parthenium l hydroalcoholic extract on sexual hormones and some liver enzymes

Ramezani¹

2019

MOJWH

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“…As such they are of great clinical interest (Romano et al, 2013) and despite their low bioavailability and metabolic stability (Martinez-Perez et al, 2016), flavones containing remedies are being assessed for suitability in menopausal estrogen deficiency symptoms treatment (Rahte et al, 2013;Seo et al, 2006), or in breast cancer prevention (Martinez-Perez et al, 2016). Nevertheless, the literature reports that the activity of pure compounds varies significantly due to experimental design (Marino and Galluzzo, 2008;Ramos, 2007) with flavones rich plant extracts presenting an even bigger challenge due to varied, complementary and/or overlapping biological activities that flavones may exert in mixtures (Marino and Galluzzo, 2008;Xu et al, 2013). What is more, less attention is paid to flavones' conjugated forms which are frequently detected in herbal extracts including oregano, thyme, agrimony, sage and yarrow (Garritano et al, 2005;Innocenti et al, 2007;Rahte et al, 2013) with reported in vitro estrogenic activities detected in their extracts being shown to be the main constituents responsible for estrogenic responses (Gutiérrez-Grijalva et al, 2017;Innocenti et al, 2007;Lee et al, 2012;Nagy et al, 2011;Rahte et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

The origin of in-vitro estrogen-like activity in oregano herb extracts

Wielogórska

Błaszczyk

Chevallier

et al. 2019

Toxicology in Vitro

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Global market of herbs has been struggling with food adulteration issues. A number of assays have been developed to aid the detection of the tampered samples and ensure high quality of the marketed products. However, herbs are marketed not only for their culinary applications but also as remedies due to high levels of biologically active constituents. Nevertheless, there is no information in the literature about the influence of herbs adulteration on the biological activity of the final product. Current study aims at assessing the influence of oregano adulteration on its in-vitro estrogen-like activity. High responses in a mammalian reporter gene assay have been detected in pure and adulterated samples, translating to 21-7,409 ng of 17β-estradiol equivalents per gram of oregano. The origin of those responses was assessed by combining fractionation and UHPLC-HRMS. Three flavones were proposed as the most active extract constituents i.e. luteolin-glucoside, luteolin-and apigenin-glucuronides all of which have been previously identified in other herbal extracts with estrogenic activity. This study underlines challenges of biological activity assessment in complex herbal extracts as well as the need for further assessment of such supplement administrations in the case of postmenopausal women and breast cancer patients undergoing hormone therapy. Highlights:  Oregano extracts exhibit estrogen-like activity in-vitro  Conjugated flavonoids are the origin of the detected biological activity  Combining bio-and chemical assays is a fast tool for detecting bioactive compounds

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“…Since ERα is a major target for the treatment and prevention of breast cancer, many anti-breast cancer compounds have been designed to bind ERα to produce different pharmacological profiles. Hence, the discovery of natural product compounds that could potentially act as antagonists of estrogen in breast tissue would be useful 13,14…”

Section: Introductionmentioning

confidence: 99%

<p>Cytotoxicity Of Chalcone Of <em>Eugenia aquea</em> Burm F. Leaves Against T47D Breast Cancer Cell Lines And Its Prediction As An Estrogen Receptor Antagonist Based On Pharmacophore-Molecular Dynamics Simulation</p>

Muchtaridi

Syahidah

Subarnas

et al. 2019

AABC

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BackgroundThe 2ʹ,4ʹ-dihydroxy-6-methoxy-3,5-3-dimethylchalcone (ChalcEA) isolated from Eugenia aquea Burm f. leaves has potential anticancer activity against human breast-adenocarcinoma cell lines (MCF-7) with an IC50 value of 250 µM. However, its apoptotic activity on the T47D breast cancer cell lines which is involving caspase-3 has not been investigated.Materials and methodsTherefore, this study aims to evaluate the cytotoxicity of ChalcEA on the T47D cell lines using the 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium (WST) method and to predict its possible antagonistic activity on the human estrogen receptor alpha (hERα) using pharmacophore and molecular dynamics (MD) methods. The in vitro test of 10 synthesized ChalcEA derivatives was also performed as an insight into the further development of its structure as an anticancer agent.ResultsIt is shown that ChalcEA has an IC50 of 142.58 ± 4.6 µM against the hERα-overexpressed T47D breast cancer cell lines, indicating its possible mechanism of anticancer activity as an antagonist of hERα. Pharmacophore study showed that ChalcEA shares similar features with the known hERα antagonist, 4-hydroxytamoxifen (4-OHT), which has hydrogen bond donor (HBD), hydrogen bond acceptor (HBA), ring aromaticity (RA), and hydrophobicity (Hy) features. Molecular docking showed that ChalcEA formed hydrogen bonds with Glu353 and Arg394, and hydrophobic interactions in a similar manner with 4-OHT. Moreover, MD simulations showed that ChalcEA destabilized the conformation of His524, a remarkable behavior of a known hERa antagonist, including 4-OHT. Furthermore, the 10 best chalcone derivatives resulted from pharmacophore- and docking-based screening, were tested against the T47D cell lines. None of the derivatives have better activity than ChalcEA. It is suggested that the functional groups at the B-ring of ChalcEA are interesting to be further optimized in the next studies.ConclusionChalcEA might act as an antagonist toward hERα, thus warranting further investigation as a potential anticancer agent.

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Are flavonoids agonists or antagonists of the natural hormone 17β‐estradiol?

Cited by 7 publications

References 31 publications

Effects of tanacetum parthenium l hydroalcoholic extract on sexual hormones and some liver enzymes

Effects of tanacetum parthenium l hydroalcoholic extract on sexual hormones and some liver enzymes

The origin of in-vitro estrogen-like activity in oregano herb extracts

<p>Cytotoxicity Of Chalcone Of <em>Eugenia aquea</em> Burm F. Leaves Against T47D Breast Cancer Cell Lines And Its Prediction As An Estrogen Receptor Antagonist Based On Pharmacophore-Molecular Dynamics Simulation</p>

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