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Elaboration of antibiofilm surfaces functionalized with antifungal-cyclodextrin inclusion complexes

机译:精细化功能化的抗真菌-环糊精包合物的抗生物膜表面

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摘要

To tackle the loss of activity of surfaces functionalized by coating and covalently bound molecules to materials, an intermediate system implying the noncovalent immobilization of active molecules in the inner cavity of grafted cyclodextrins (CDs) was investigated. The antifungal and antibiofilm activities of the most stable complexes of Anidulafungin (ANF; echinocandin) and thymol (THY; terpen) in various CDs were demonstrated to be almost the same as the free molecules. The selected CD was covalently bond to self-assembled monolayers on gold surfaces. The immobilized antifungal agents reduced the number of culturable Candida albicans ATCC 3153 attached to the surface by 64 ± 8% for ANF and 75 ± 15% for THY. The inhibitory activity was persistent for THY-loaded samples, whereas it was completely lost for ANF-loaded surfaces after one use. However, reloading of the echinocandin restored the activity. Using fluorescent dying and confocal microscopy, it was proposed that the ANF-loaded surfaces inhibited the adherence of the yeasts, whereas the activity of immobilized THY was found fungicidal. This kind of tailored approach for functionalizing surfaces that could allow a progressive release of ANF or THY gave promising results but still needs to be improved to display a full activity.
机译:为了解决通过将分子共价键合并涂覆到材料上而功能化的表面失去活性的问题,研究了一种中间体系,该体系暗示了活性分子在嫁接的环糊精(CD)内腔中的非共价固定。各种CD中最稳定的Anidulafungin(ANF; echinocandin)和百里酚(THY; terpen)的复合物的抗真菌和抗生物膜活性已证明与游离分子几乎相同。所选的CD与金表面上的自组装单层共价键合。固定的抗真菌剂使附着在表面的可培养白色念珠菌ATCC 3153的数量对ANF减少了64±8%,对THY减少了75±15%。对于THY负载的样品,抑制活性是持久的,而一次使用后,对于ANF负载的表面则完全丧失了抑制活性。然而,棘皮菌素的重新加载恢复了该活性。使用荧光染色和共聚焦显微镜,有人提出ANF加载表面抑制酵母菌的粘附,而固定化THY的活性被认为是杀真菌的。这种可以使ANF或THY逐步释放的功能化表面的量身定制方法给出了可喜的结果,但仍需要改进以显示出完整的活性。

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