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顺式阿曲库铵对氟康唑耐药分离株的抗真菌活性及其抗生物膜作用。

Antifungal activity of cisatracurium against fluconazole-resistant isolates and its antibiofilm effects.

机构信息

School of Pharmacy, Federal University of Ceará, Fortaleza, CEP, 60.430-372, Brazil.

Drug Research and Development Center, Federal University of Ceará, Fortaleza, CE, Brazil, CE, CEP, 60.430-275, Brasil.

出版信息

Future Microbiol. 2023 Jul;18:649-660. doi: 10.2217/fmb-2022-0224. Epub 2023 Jul 31.

DOI:10.2217/fmb-2022-0224
PMID:37522164
Abstract

To evaluate the antifungal activity of cisatracurium against spp. resistant to fluconazole strains in planktonic and biofilm forms, in addition to determining its mechanism of action. Antifungal activity and pharmacological interactions were determined using broth microdilution methods and the mechanism of action was evaluated by flow cytometry and molecular docking. Cisatracurium presented antifungal activity against spp. planktonic cells due to alterations of mitochondrial transmembrane potential leading to cellular apoptosis in addition to interacting with important targets related to cellular respiration, membrane and cell wall evidenced by molecular docking. Furthermore, the drug both prevented biofilm formation and impaired mature biofilms. Cisatracurium exhibits potential antifungal activity against spp.

摘要

为了评估顺式阿曲库铵对氟康唑耐药株的抗真菌活性,我们分别在浮游和生物膜形式下,对其进行了研究,此外还确定了其作用机制。采用肉汤微量稀释法测定抗真菌活性和药物相互作用,用流式细胞术和分子对接评估其作用机制。顺式阿曲库铵对浮游细胞中的念珠菌具有抗真菌活性,这是由于线粒体跨膜电位的改变导致细胞凋亡,此外,分子对接还表明,顺式阿曲库铵与与细胞呼吸、膜和细胞壁相关的重要靶标相互作用。此外,该药物既能预防生物膜的形成,又能破坏成熟的生物膜。顺式阿曲库铵对念珠菌具有潜在的抗真菌活性。

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