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金鸡纳生物碱衍生物对金黄色葡萄球菌的抗菌及抗生物膜活性评估

Evaluation of antibacterial and anti-biofilm activities of cinchona alkaloid derivatives against Staphylococcus aureus.

作者信息

Skogman Malena E, Kujala Janni, Busygin Igor, Leinob Reko, Vuorela Pia M, Fallarero Adyary

机构信息

Pharmaceutical Sciences, Department of Biosciences, Abo Akademi University, Artillerigatan 6A, FI-20520 Turku, Finland.

出版信息

Nat Prod Commun. 2012 Sep;7(9):1173-6.

Abstract

Bacterial biofilms are resistant to most of the commonly available antibacterial chemotherapies. Thus, an enormous need exists to meet the demands of effective anti-biofilm therapy. In this study, a small library of cinchona alkaloids, including the naturally occurring compounds cinchonidine and cinchonine, as well as various synthetic derivatives and analogues was screened for antibacterial and anti-biofilm activity against the Staphylococcus aureus biofilm producing strain ATCC 25923. Two methods were used to evaluate activity against biofilms, namely crystal violet staining to measure biomass and resazurin assay to measure biofilms viability. Cinchonidine was found to be inactive, whereas a synthetic derivative, 11-triphenylsilyl-10,11-dihydrocinchonidine (11-TPSCD), was effective against planktonic bacteria as well as in preventing biofilm formation at low micromolar concentrations. Higher concentrations were required to eradicate mature biofilms.

摘要

细菌生物膜对大多数常用的抗菌化疗药物具有抗性。因此,满足有效抗生物膜治疗的需求迫在眉睫。在本研究中,对一个包含天然存在的化合物辛可尼定和辛可宁以及各种合成衍生物和类似物的金鸡纳生物碱小型文库,进行了针对金黄色葡萄球菌生物膜产生菌株ATCC 25923的抗菌和抗生物膜活性筛选。使用了两种方法来评估对生物膜的活性,即结晶紫染色法测量生物量和刃天青测定法测量生物膜活力。发现辛可尼定无活性,而一种合成衍生物11-三苯基硅基-10,11-二氢辛可尼定(11-TPSCD)在低微摩尔浓度下对浮游细菌有效,并且能防止生物膜形成。根除成熟生物膜则需要更高的浓度。

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