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硒代三甘油脂通过活性氧物质和 Nrf2 转录因子的参与来影响 CYP1A1 和 QR 的活性。

Selenitetriglicerydes affect CYP1A1 and QR activity by involvement of reactive oxygen species and Nrf2 transcription factor.

机构信息

National Medicines Institute, Chełmska 30/34, PL 00-725 Warszawa, Poland.

出版信息

Pharmacol Rep. 2010 Mar-Apr;62(2):352-61. doi: 10.1016/s1734-1140(10)70275-9.

Abstract

Selenitetriglycerides are a group of compounds that contain selenium (Se) (IV). In this paper, we present the results of examinations of three structurally-related selenitetriglicerydes that contain various Se concentrations: 2%, 5% and 7% Selol. The present study concentrates on the effect of Selol on phase 1 and 2 enzyme activity and the implications of free radicals and the nuclear erythroid 2-related factor 2 (Nrf2)-antioxidant response element (ARE) pathway in the activity of this compound. The cytotoxic and cytostatic activities of the three kinds of Selol were evaluated; however, the cytotoxic effect was observed only for 7% Selol. Our results show that 2% Selol acts as a monofunctional inducer of phase 2 enzyme activity, and the induction is mediated by the Nrf2 transcription factor. Selol 7% acts in an opposite manner and induces phase 1 with simultaneous inhibition of phase 2 enzyme activity. The differential effect can be associated with the increase in Se content, leading to a change in the structure of the compound.

摘要

硒代三酰甘油是一组含有硒(IV)的化合物。在本文中,我们介绍了三种结构相关的硒代三酰甘油的检测结果,它们含有不同浓度的硒:2%、5%和 7%Selol。本研究集中于 Selol 对 1 相和 2 相酶活性的影响,以及自由基和核红细胞 2 相关因子 2(Nrf2)-抗氧化反应元件(ARE)途径在该化合物活性中的作用。评估了三种 Selol 的细胞毒性和细胞抑制活性;然而,只有 7%Selol 表现出细胞毒性作用。我们的结果表明,2%Selol 作为一种单功能诱导物作用于 2 相酶活性,诱导作用是通过 Nrf2 转录因子介导的。Selol 7%以相反的方式起作用,诱导 1 相,同时抑制 2 相酶活性。这种差异效应可能与硒含量的增加有关,导致化合物结构发生变化。

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