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新型槐糖脂季铵盐的内分泌干扰效力和毒性。

Endocrine disrupting potency and toxicity of novel sophorolipid quaternary ammonium salts.

机构信息

Institute of Environmental Engineering and Building Installations, Lodz University of Technology, Al. Politechniki 6, 90-924, Lodz, Poland.

Faculty of Bioscience Engineering, Department of Green Chemistry and Technology, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium.

出版信息

Ecotoxicology. 2021 May;30(4):658-666. doi: 10.1007/s10646-021-02378-6. Epub 2021 Mar 17.

Abstract

A new class of biosurfactants, namely quaternary ammonium sophorolipids (SQAS), suitable for pharmaceutical applications, was tested for the evaluation of their (anti)estrogenic and (anti)androgenic potency with the help of YES/YAS assays. Also their toxicity towards yeasts (Saccharomyces cerevisiae) and bacteria (Escherichia coli) was checked. The results achieved for SQAS, which can be regarded as potential micropollutants, were compared with those obtained for two well-known micropollutants diclofenac and 17α-ethinylestradiol subjected to the same testing procedures. This work demonstrated that acetylation of the hydroxyl group of the carbohydrate head of SQAS decreased the toxicity of this class of biosurfactants towards Saccharomyces cerevisiae. Furthermore, it contributed to the decrease of their endocrine disrupting potency. None of the SQAS studied showed clear agonist activity for female or male hormones. SQAS1 and SQAS2 revealed weak antiestrogenic and antiandrogenic potency. All of these properties were weaker, not only to the potency of the appropriate positive control in the antagonists bioassays, but also compared to the potency of other tested compounds, i.e. DCF and EE2. SQAS3 possessed most probably inhibitory activity towards male hormones. Moreover, cytotoxicity of two out of four studied SQAS at the highest concentrations towards the strains of Saccharomyces cerevisiae interfered with the endocrine disruption activity. It would be also worth studying it with the use of another endocrine activity test.

摘要

一类新型生物表面活性剂,即季铵化槐糖脂(SQAS),适合于药物应用,在 YES/YAS 测定的帮助下,对其(抗)雌激素和(抗)雄激素活性进行了测试。还检查了它们对酵母(酿酒酵母)和细菌(大肠杆菌)的毒性。可以将 SQAS 视为潜在的微污染物,其结果与在相同测试程序下进行的两种著名的微污染物双氯芬酸和 17α-乙炔雌二醇的结果进行了比较。这项工作表明,SQAS 碳水化合物头部的羟基乙酰化降低了此类生物表面活性剂对酿酒酵母的毒性。此外,它有助于降低其内分泌干扰活性。所研究的 SQAS 均未显示出对女性或男性激素的明显激动活性。SQAS1 和 SQAS2 表现出较弱的抗雌激素和抗雄激素活性。所有这些特性不仅比拮抗剂生物测定中适当阳性对照的活性弱,而且比其他测试化合物(即 DCF 和 EE2)的活性弱。SQAS3 可能对雄性激素具有抑制活性。此外,在最高浓度下,四种研究的 SQAS 中有两种对酿酒酵母菌株的细胞毒性会干扰内分泌干扰活性。使用另一种内分泌活性测试进行研究也将是值得的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1685/8060166/88d96f525190/10646_2021_2378_Fig1_HTML.jpg

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