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

European Pharmaceutical Journal Pub Date : 2019-11-01 DOI:10.2478/afpuc-2019-0016

N. Tsiferova, O. Khamidova, A. Amonov, M. Rakhimova, S. Rustamova, R. S. Kurbannazaova, P. Merzlyak, N. Abdulladjanova, R. Sabirov

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引用次数: 3

Abstract

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.

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单宁，体积调节和体积敏感阴离子通道的新型抑制剂

体积敏感的向外整流阴离子通道(VSOR)是非等渗条件下细胞存活的关键体积调节系统的关键组成部分。本研究的目的是测试四种特定成分的单宁提取物对细胞体积调节和VSOR的影响。制剂I(从苏木叶中分离98%的可水解单宁)和制剂II(从阔叶大车前草叶中分离100%的可水解单宁)完全不可逆地消除HCT116细胞肿胀激活的VSOR电流。两种制剂均能较好地抑制胸腺细胞的体积调节，半最大作用分别为40.9 μg/ml和12.3 μg/ml。在较低的浓度下抑制更有效，但在较高的剂量下由于可能的非特异性膜渗透活性而恢复。制剂III和IV(分别从Fergana spurge Euphorbia ferganensis B.Fedtch的根和地上部分分离得到54.7%和54.3%的水解单宁)以部分可逆的方式抑制了VSOR活性，并抑制了体积调节，其半最大剂量分别为270和278 μg/ml，在高剂量下无二次逆转作用。水解单宁是一类新型的VSOR通道抑制剂，具有抑制细胞体积调节机制的能力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

0.60

自引率

0.00%

发文量

期刊介绍： European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.