Flavonolignans As a Novel Class of Sodium Pump Inhibitors

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388971%3A_____%2F16%3A00462025" target="_blank" >RIV/61388971:_____/16:00462025 - isvavai.cz</a>

Alternative codes found

RIV/61989592:15310/16:33160062

Result on the web

<a href="http://dx.doi.org/10.3389/fphys.2016.00115" target="_blank" >http://dx.doi.org/10.3389/fphys.2016.00115</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3389/fphys.2016.00115" target="_blank" >10.3389/fphys.2016.00115</a>

Result language

angličtina

Original language name

Flavonolignans As a Novel Class of Sodium Pump Inhibitors

Original language description

We examined the inhibitory effects of three flavonolignans and their dehydro-derivatives, taxifolin and quercetin on the activity of the Na+/K+-ATPase (NKA). The flavonolignans silychristin, dehydrosilychristin and dehydrosilydianin inhibited NKA with IC50 of 110 +/- 40 mu M, 38 +/- 8 mu M, and 36 +/- 14 mu M, respectively. Using the methods of molecular modeling, we identified several possible binding sites for these species on NKA and proposed the possible mechanisms of inhibition. The binding to the extracellular- or cytoplasmic C-terminal sites can block the transport of cations through the plasma membrane, while the binding on the interface of cytoplasmic domains can inhibit the enzyme allosterically. Fluorescence spectroscopy experiments confirmed the interaction of these three species with the large cytoplasmic segment connecting transmembrane helices 4 and 5 (C45).

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CE - Biochemistry

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2016

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Frontiers in physiology

ISSN

1664-042X

e-ISSN

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Volume of the periodical

7

Issue of the periodical within the volume

Mar 30

Country of publishing house

CH - SWITZERLAND

Number of pages

12

Pages from-to

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UT code for WoS article

000372965100001

EID of the result in the Scopus database

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