8-Prenylnaringenin, inhibits estrogen receptor-α mediated cell growth and induces apoptosis in MCF-7 breast cancer cells

Brunelli, Elisa; Minassi, Alberto; Appendino, Giovanni; Moro, Laura

doi:10.1016/j.jsbmb.2007.04.003

Cited by 41 publications

(40 citation statements)

References 38 publications

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“…Growth inhibition within 24 h was more pronounced after treatment with 6-PN than after treatment with the two control HDACi at similar or even higher concentrations. Our results are in line with previous reports that showed induction of cytotoxicity at similar concentrations for the breast, renal and prostate cancer cell lines after single treatment [10,13,16,17,19].…”

Section: Discussionsupporting

confidence: 93%

“…Flavonoids, including the prenylflavonoids, also show anticancer activities [7,10]. In particular, 8-PN inhibits angiogenesis induced by basic fibroblast growth factor and vascular endothelial growth factor in a three-dimensional collagen gel in vitro and in chorioallantoic membrane assays in vivo [11], mimics the effects of 17β-estradiol on MCF-7 breast cancer cells [12] and induces apoptosis in MCF-7 cells [13] and in a multi drug-resistant leukemia blast [14]. Inhibition of multi drug resistance-associated transporters P-glycoprotein and MRP1 by 8-PN was demonstrated [15].…”

Section: Introductionmentioning

confidence: 98%

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6- and 8-Prenylnaringenin, Novel Natural Histone Deacetylase Inhibitors Found in Hops, Exert Antitumor Activity on Melanoma Cells

Venturelli

Niessner

Sinnberg

et al. 2018

Cell Physiol Biochem

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Background/Aims: Prenylnaringenins are natural prenylflavonoids with anticancer properties. However, the underlying mechanisms have not been elucidated yet. Here we report a novel mode of action of 6- and 8-prenylnaringenin (PN) on human melanoma cells: Inhibition of cellular histone deacetylases (HDACs). Methods: We performed in silico and in vitro analyses using 6-PN or 8-PN to study a possible interaction of 6-PN or 8-PN with HDAC as well as Western blot and FACS analyses, real-time cell proliferation and cell viability assays to assess the impact of 6-PN and 8-PN on human metastatic melanoma cells. Results: In silico, 6-PN and 8-PN fit into the binding pocket of HDAC2, 4, 7 and 8, binding to the zinc ion of their catalytic center that is essential for enzymatic activity. In vitro, 100 µmol/L of 6-PN or 8-PN inhibited all 11 conserved human HDAC of class I, II and IV. In clinical oncology HDAC inhibitors are currently investigated as new anticancer compounds. In line, treatment of SK-MEL-28 cells with 6-PN or 8-PN induced a hyperacetylation of histone complex H3 within 2 h. Further, 6-PN or 8-PN mediated a prominent, dose-dependent reduction of cellular proliferation and viability of SK-MEL-28 and BLM melanoma cells. This effect was apoptosis-independent and accompanied by down-regulation of mTOR-specific pS6 protein via pERK/pP90 in SK-MEL-28 cells. Conclusion: The identification of a broad inhibitory capacity of 6-PN and 8-PN for HDAC enzymes with antiproliferative effects on melanoma cells opens the perspective for clinical application as novel anti-melanoma drugs and the usage as innovative lead structures for chemical modification to enhance pharmacology or inhibitory activities.

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Section: Discussionsupporting

confidence: 93%

Section: Introductionmentioning

confidence: 98%

6- and 8-Prenylnaringenin, Novel Natural Histone Deacetylase Inhibitors Found in Hops, Exert Antitumor Activity on Melanoma Cells

Venturelli

Niessner

Sinnberg

et al. 2018

Cell Physiol Biochem

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“…It is possible that 8-prenylnaringenin is able to diffuse across the plasma membrane and reach intracellular compartments, so it may inhibit Kv1.3 channels in the mitochondria. Brunelli et al showed that 8-prenylnaringenin induces apoptosis of MCF-7 cells when applied at 10 and 100 M concentrations [11]. Our study showed that a 10 µM concentration of the flavonoid is high enough to completely inhibit Kv1.3 channels in the plasma membrane.…”

Section: Discussionsupporting

confidence: 54%

The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells

Gąsiorowska

Teisseyre

Uryga

et al. 2012

Cellular and Molecular Biology Letters

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Abstract:Using the whole-cell patch-clamp technique, we investigated the influence of 8-prenylnaringenin on the activity of the voltage-gated Kv1.3 potassium channels in the human leukemic T lymphocyte cell line Jurkat. 8-prenylnaringenin is a potent plant-derived phytoestrogen that has been found to inhibit cancer cell proliferation. The results show that it inhibited the Kv1.3 channels in a concentration-dependent manner. Complete inhibition occurred at concentrations higher than 10 M. The inhibitory effect of 8-prenylnaringenin was reversible. It was accompanied by a significant acceleration of channel inactivation without any pronounced change in the activation rate. Of the naringenin derivatives tested to date, 8-prenylnaringenin is the most potent inhibitor of the Kv1.3 channels. The potency of the inhibition may be due to the presence of a prenyl group in the molecule of this flavonoid. The inhibition of the Kv1.3 channels might be involved in the antiproliferative and pro-apoptotic effects of 8-prenylnaringenin that have been observed in cancer cell lines expressing these channels.

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“…Thus, nutritional compounds could act as antagonists of ERa-evoked rapid responses and agonists of ERb-dependent proapoptotic signaling (4). Remarkably, the interference with the ERa-associated PI3K pathway has recently been proposed as a mechanism underlying the antiestrogenic inhibition of survival and proliferation by 8-prenyl-naringenin in MCF-7 cells (30).…”

Section: Paolo Ascenzimentioning

confidence: 99%

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

Marino¹,

Galluzzo²

2008

IUBMB Life

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8-Prenylnaringenin, inhibits estrogen receptor-α mediated cell growth and induces apoptosis in MCF-7 breast cancer cells

Cited by 41 publications

References 38 publications

6- and 8-Prenylnaringenin, Novel Natural Histone Deacetylase Inhibitors Found in Hops, Exert Antitumor Activity on Melanoma Cells

6- and 8-Prenylnaringenin, Novel Natural Histone Deacetylase Inhibitors Found in Hops, Exert Antitumor Activity on Melanoma Cells

The influence of 8-prenylnaringenin on the activity of voltage-gated kv1.3 potassium channels in human jurkat t cells

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

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