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[溶酶体促渗剂的生物活性]

[The biological activity of lysosomotropic agents].

作者信息

Obłąk Ewa, Krasowska Anna

机构信息

Instytut Genetyki i Mikrobiologii, Uniwersytet Wrocławski, 51-148 Wrocław.

出版信息

Postepy Hig Med Dosw (Online). 2010 Oct 13;64:459-65.

PMID:20966503
Abstract

Lysosomotropic agents have antitumor, antifungal and antimicrobial properties. These small, amphiphilic compounds, as weak bases, readily penetrate the lipid bilayer and diffuse into acidic subcellular compartments such as lysosomes or vacuoles. The mechanism of action of lysosomotropic compounds can be distinct, depending on their chemical structure and/or the kind of cells influenced. Our investigations of the influence of lysosomotropic agents on Saccharomyces cerevisiae have lead to a partial explanation of their mechanism of action. The amphiphilic character enables the compounds to penetrate the lipid bilayer and disturb its structure and functions and can inhibit the activity of plasma membrane H+ATPase. The accumulation of the compounds in yeast vacuoles, disrupting them and killing yeast cells, is another mechanism of action. Lysosomotropic agents can be substrates for ABC transporters in Saccharomyces cerevisiae cells.

摘要

溶酶体亲和剂具有抗肿瘤、抗真菌和抗菌特性。这些小分子两亲化合物作为弱碱,很容易穿透脂质双层并扩散到酸性亚细胞区室,如溶酶体或液泡中。溶酶体亲和化合物的作用机制可能因化学结构和/或受影响的细胞类型而异。我们对溶酶体亲和剂对酿酒酵母影响的研究部分解释了它们的作用机制。两亲特性使这些化合物能够穿透脂质双层,扰乱其结构和功能,并能抑制质膜H⁺ATP酶的活性。这些化合物在酵母液泡中的积累,破坏液泡并杀死酵母细胞,是另一种作用机制。溶酶体亲和剂可以是酿酒酵母细胞中ABC转运蛋白的底物。

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