<abstract xmlns="http://www.w3.org/1999/xhtml">

<p>The volume-sensitive outwardly rectifying anion channel (VSOR) is a key component of volume regulation system critical for cell survival in non-isosmotic conditions. The aim of the present study was to test the effects of four tannin extracts with defined compositions on cell volume regulation and VSOR. Preparation I (98% of hydrolysable tannins isolated from leaves of sumac <italic>Rhus typhina L.</italic>) and Preparation II (100% of hydrolysable tannins isolated from leaves of broadleaf plantain <italic>Plantago major L</italic>) completely and irreversibly abolished swelling-activated VSOR currents in HCT116 cells. Both preparations profoundly suppressed the volume regulation in thymocytes with half-maximal effects of 40.9 μg/ml and 12.3 μg/ml, respectively. The inhibition was more efficient at lower concentrations but reverted at higher doses due to possible non-specific membrane-permeabilizing activity. Preparations III and IV (54,7% and 54.3% of hydrolysable tannins isolated, respectively, from roots and aboveground parts of Fergana spurge <italic>Euphorbia ferganensis B.Fedtch</italic>) inhibited VSOR activity in a partially reversible manner and suppressed the volume regulation with substantially higher half-maximal doses of 270 and 278 μg/ml, respectively, with no secondary reversion at higher doses. Hydrolysable tannins represent a novel class of VSOR channel inhibitors with the capacity to suppress the cell volume regulation machinery.</p>
</abstract>

The volume-sensitive outwardly rectifying anion channel (VSOR) is a key component of volume regulation system critical for cell survival in non-isosmotic conditions. The aim of the present study was to test the effects of four tannin extracts with defined compositions on cell volume regulation and VSOR. Preparation I (98% of hydrolysable tannins isolated from leaves of sumac Rhus typhina L.) and Preparation II (100% of hydrolysable tannins isolated from leaves of broadleaf plantain Plantago major L) completely and irreversibly abolished swelling-activated VSOR currents in HCT116 cells. Both preparations profoundly suppressed the volume regulation in thymocytes with half-maximal effects of 40.9 μg/ml and 12.3 μg/ml, respectively. The inhibition was more efficient at lower concentrations but reverted at higher doses due to possible non-specific membrane-permeabilizing activity. Preparations III and IV (54,7% and 54.3% of hydrolysable tannins isolated, respectively, from roots and aboveground parts of Fergana spurge Euphorbia ferganensis B.Fedtch) inhibited VSOR activity in a partially reversible manner and suppressed the volume regulation with substantially higher half-maximal doses of 270 and 278 μg/ml, respectively, with no secondary reversion at higher doses. Hydrolysable tannins represent a novel class of VSOR channel inhibitors with the capacity to suppress the cell volume regulation machinery.

Tannins, novel inhibitors of the volume regulation and the volume-sensitive anion channel

European Pharmaceutical Journal

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

The volume-sensitive outwardly rectifying anion channel (VSOR) is a key component of volume regulation system critical for cell survival in non-isosmotic...

Tannins, novel inhibitors of the volume regulation and the volume-sensitive anion channel

Pubblicato online: 28 gen 2020

Pagine: 37 - 44

Ricevuto: 19 giu 2019

Accettato: 16 ott 2019

DOI: https://doi.org/10.2478/afpuc-2019-0016

Parole chiave
Tannins, plant polyphenols, thymocytes, cell volume regulation, volume-sensitive anion channel

© 2019 N.A. Tsiferova et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Tannins, novel inhibitors of the volume regulation and the volume-sensitive anion channel

Pubblicato online: 28 gen 2020

Pagine: 37 - 44

Ricevuto: 19 giu 2019

Accettato: 16 ott 2019

DOI: https://doi.org/10.2478/afpuc-2019-0016

Parole chiaveTannins, plant polyphenols, thymocytes, cell volume regulation, volume-sensitive anion channel

© 2019 N.A. Tsiferova et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Parole chiave
Tannins, plant polyphenols, thymocytes, cell volume regulation, volume-sensitive anion channel