Bisphenol A Inhibits Voltage-Activated Ca<sup>2+</sup> Channels in Vitro: Mechanisms and Structural Requirements

Deutschmann, André U.; Hans, Michael; Meyer, Rainer; Häberlein, Hanns; Swandulla, Dieter

doi:10.1124/mol.112.081372

Cited by 64 publications

(52 citation statements)

References 46 publications

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“…It states that estrogens act by binding directly on parts of ion channels. It was based mostly on precise single-channel recordings (mostly from excised inside-out patches, see references in Table 4), but also on other methods, such as binding studies [1-3], site mutations [4], pharmacological and biophysical analysis [5], kinetics of estrogen effects [6], etc. Results from such studies are presented in Table 4.…”

Section: Direct Rapid Estrogen Actions On Ion Channelsmentioning

confidence: 99%

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Kow

Pfaff

2016

Steroids

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A survey of nearly two hundred reports shows that rapid estrogenic actions can be detected across a range of kinds of estrogens, a range of doses, on a wide range of tissue, cell and ion channel types. Striking is the fact that preparations of estrogenic agents that do not permeate the cell membrane almost always mimic the actions of the estrogenic agents that do permeate the membrane. All kinds of estrogens, ranging from natural ones, through receptor modulators, endocrine disruptors, phytoestrogens, agonists, and antagonists to novel G-1 and STX, have been reported to be effective. For actions on specific types of ion channels, the possibility of opposing actions, in different cases, is the rule, not the exception. With this variety there is no single, specific action mechanism for estrogens per se, although in some cases estrogens can act directly or via some signaling pathways to affect ion channels. We infer that estrogens can bind a large number of substrates/receptors at the membrane surface. As against the variety of subsequent routes of action, this initial step of the estrogen's binding action is the key.

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Section: Direct Rapid Estrogen Actions On Ion Channelsmentioning

confidence: 99%

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Kow

Pfaff

2016

Steroids

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“…The blockade of hNa v 1.5 by BPA had similar properties as that by local anesthetics; the two share a common binding site on hNa v 1.5 involving amino acid F1760. Later, Deutschmann et al reported that BPA inhibited the L-type Ca 2+ channels in isolated mouse ventricular myocytes in a dose-dependent manner with an IC 50 of 2.5 × 10 −5 M [62]. The blockade was fully reversible, and BPA likely exerted its action by binding to channels at the resting state.…”

Section: Impact Of Bpa On the CV System—experimental Studiesmentioning

confidence: 99%

Impact of Bisphenol A on the Cardiovascular System — Epidemiological and Experimental Evidence and Molecular Mechanisms

Gao

Wang

2014

IJERPH

144

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Bisphenol A (BPA) is a ubiquitous plasticizing agent used in the manufacturing of polycarbonate plastics and epoxy resins. There is well-documented and broad human exposure to BPA. The potential risk that BPA poses to the human health has attracted much attention from regulatory agencies and the general public, and has been extensively studied. An emerging and rapidly growing area in the study of BPA’s toxicity is its impact on the cardiovascular (CV) system. Recent epidemiological studies have shown that higher urinary BPA concentration in humans is associated with various types of CV diseases, including angina, hypertension, heart attack and coronary and peripheral arterial disease. Experimental studies have demonstrated that acute BPA exposure promotes the development of arrhythmias in female rodent hearts. Chronic exposure to BPA has been shown to result in cardiac remodeling, atherosclerosis, and altered blood pressure in rodents. The underlying mechanisms may involve alteration of cardiac Ca2+ handling, ion channel inhibition/activation, oxidative stress, and genome/transcriptome modifications. In this review, we discuss these recent findings that point to the potential CV toxicity of BPA, and highlight the knowledge gaps in this growing research area.

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“…An electrophysiological study has reported that Ca 2+ currents through native L-, N-, P/Q-, T-type Ca 2+ channels in rat endocrine GH3 cells, mouse dorsal root ganglion neurons or cardiac myocytes, and recombinant human R-type Ca 2+ channels expressed in HEK cells, were rapidly and reversibly inhibited by high doses of BPA with similar potency (EC 50 values: 26-35 µM), acting directly on the channel protein [33]. In another study, the mRNA expression of an auxiliary subunit of the high threshold voltage-gated Ca 2+ channel, Cacnα2δ2, was decreased in the left ventricle of male mice with low doses of BPA (1 nM) [26].…”

Section: Bpa Actions Onmentioning

confidence: 99%

Effects of Bisphenol A on ion channels: Experimental evidence and molecular mechanisms

et al. 2016

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Please cite this article as: Soriano, S., Ripoll, C., Alonso-Magdalena, P., Fuentes, E., Quesada, I., Nadal, A., Martinez-Pinna, J., Effects of Bisphenol A on ion channels: experimental evidence and molecular mechanisms, Steroids (2016), doi: http://dx.doi.org/10. 1016/j.steroids.2016.02.020 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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Bisphenol A Inhibits Voltage-Activated Ca²⁺ Channels in Vitro: Mechanisms and Structural Requirements

Cited by 64 publications

References 46 publications

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Impact of Bisphenol A on the Cardiovascular System — Epidemiological and Experimental Evidence and Molecular Mechanisms

Effects of Bisphenol A on ion channels: Experimental evidence and molecular mechanisms

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Bisphenol A Inhibits Voltage-Activated Ca2+ Channels in Vitro: Mechanisms and Structural Requirements

Cited by 64 publications

References 46 publications

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Rapid estrogen actions on ion channels: A survey in search for mechanisms

Impact of Bisphenol A on the Cardiovascular System — Epidemiological and Experimental Evidence and Molecular Mechanisms

Effects of Bisphenol A on ion channels: Experimental evidence and molecular mechanisms

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Product

Resources

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Bisphenol A Inhibits Voltage-Activated Ca²⁺ Channels in Vitro: Mechanisms and Structural Requirements