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赛瑞妮™(Cyrene™)是二甲基亚砜(DMSO)的绿色替代品,可作为一种溶剂用于发现针对ESKAPE病原体的抗菌药物。

Cyrene™ is a green alternative to DMSO as a solvent for antibacterial drug discovery against ESKAPE pathogens.

作者信息

Camp Jason E, Nyamini Simbarashe B, Scott Fraser J

机构信息

Department of Chemical Sciences , University of Huddersfield , Queensgate , Huddersfield , UK.

Department of Chemistry , University of Bath , Bath , UK.

出版信息

RSC Med Chem. 2019 Dec 17;11(1):111-117. doi: 10.1039/c9md00341j. eCollection 2020 Jan 1.

Abstract

Dimethyl sulfoxide (DMSO) is currently employed across the biomedical field, from cryopreservation to assays, despite the fact that it has been shown to have an assortment of biologically relevant effects. The amphiphilic nature of DMSO along with its relatively low toxicity at dilute concentrations make it a challenging solvent to replace. A possible alternative is Cyrene™ (dihydrolevoglucosenone), an aprotic dipolar solvent that is derived from waste biomass. In addition to being a green solvent, Cyrene™ has comparable solvation properties and is reported to have low toxicity. Herein the abilities of the two solvents to solubilize drug compounds and to act as non-participatory vehicles in drug discovery for antibacterials are compared. It was demonstrate that the results of standardised antimicrobial susceptibility testing do not differ between drugs prepared from either Cyrene™ or DMSO stock. Moreover, in contrast to DMSO, Cyrene™ does not offer protection from ROS mediated killing of bacteria and may therefore be an improvement over DMSO as a vehicle in antimicrobial drug discovery.

摘要

二甲基亚砜(DMSO)目前在生物医学领域广泛应用,从冷冻保存到各种检测,尽管已表明它具有一系列与生物学相关的效应。DMSO的两亲性质以及其在稀浓度下相对较低的毒性使其成为一种难以替代的溶剂。一种可能的替代品是Cyrene™(二氢左旋葡萄糖酮),一种源自废弃生物质的非质子偶极溶剂。除了是一种绿色溶剂外,Cyrene™具有类似的溶剂化性质,并且据报道毒性较低。本文比较了这两种溶剂溶解药物化合物的能力以及在抗菌药物发现中作为非参与性载体的作用。结果表明,用Cyrene™或DMSO储备液制备的药物之间,标准化抗菌药敏试验的结果没有差异。此外,与DMSO不同,Cyrene™不能保护细菌免受活性氧介导的杀伤,因此在抗菌药物发现中作为载体可能比DMSO有所改进。

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