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一种针对从外耳道炎分离出的临床菌株的双(吡唑基)甲烷衍生物。

A bis(pyrazolyl)methane derivative against clinical strains isolated from otitis externa.

作者信息

Ocaña Ana V, Aguilera-Correa John J, Domínguez-Jurado Elena, Pérez-Martínez Francisco C, Pérez-Tanoira Ramón, López-Carretero Yaiza, Masiá-Mondejar Jesús, Castro-Osma José Antonio, Esteban Jaime, Alonso-Moreno Carlos, Molina-Alarcón Milagros, Seguí Pedro

机构信息

Instituto de Investigación en Discapacidades Neurológicas (IDINE) University of Castilla-La Mancha Albacete Spain.

Clinical Microbiology Department IIS-Fundacion Jimenez Diaz-UAM Madrid Spain.

出版信息

Laryngoscope Investig Otolaryngol. 2022 Jan 18;7(1):283-290. doi: 10.1002/lio2.722. eCollection 2022 Feb.

DOI:10.1002/lio2.722
PMID:35155809
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8823158/
Abstract

OBJECTIVE

The purpose of this study was to evaluate the in vitro antibacterial effects of a Cymene-based bis(pyrazolyl)methane derivative (SC-19) to advance in developing alternative therapeutic compounds to fight against bacterial isolates from patients with otitis externa (OE).

METHODS

Eighteen swab specimens were collected from patients aged over 18 years diagnosed with OE within at least 7 days of symptom onset, contaminated by only one bacterium type: ( = 5); ( = 8); ( = 2); ( = 1); ( = 2). To appraise antibacterial activity, minimal inhibitory concentration (MIC), minimal bactericidal concentration (MBC), minimum biofilm inhibitory concentration (MBIC), and minimum biofilm eradication concentration (MBEC) assays were run at different SC-19 concentrations.

RESULTS

When using SC-19, strains showed less bacterial growth, but no bactericidal effect was observed. The MIC and MBC of SC-19 were 62.5 and 2000 μg/ml against and were >2000 μg/ml against the other isolates obtained from OE, respectively. In addition, the MBICs and MBECs of SC-19 against were 125 and >2000 μg/ml, respectively.

CONCLUSION

Nowadays the acquired antibiotic resistance phenomenon has stimulated research into novel and more efficient therapeutic agents. Hence, we report that, helped by the structural diversity fostered herein by a range of bis(pyrazolyl)methane derivatives, SC-19 can be a promising alternative therapeutic option for treating OE caused by given the observed effects on both planktonic state and biofilm.

LEVEL OF EVIDENCE

IV.

摘要

目的

本研究旨在评估一种基于对伞花烃的双(吡唑基)甲烷衍生物(SC-19)的体外抗菌作用,以推动开发替代治疗化合物,用于对抗外耳道炎(OE)患者分离出的细菌。

方法

从18岁以上、症状出现至少7天内被诊断为OE的患者中收集18份拭子标本,每份标本仅被一种细菌污染:金黄色葡萄球菌(n = 5);铜绿假单胞菌(n = 8);肺炎克雷伯菌(n = 2);鲍曼不动杆菌(n = 1);奇异变形杆菌(n = 2)。为评估抗菌活性,在不同SC-19浓度下进行了最小抑菌浓度(MIC)、最小杀菌浓度(MBC)、最小生物膜抑制浓度(MBIC)和最小生物膜根除浓度(MBEC)测定。

结果

使用SC-19时,金黄色葡萄球菌菌株的细菌生长较少,但未观察到杀菌作用。SC-19对金黄色葡萄球菌的MIC和MBC分别为62.5和2000μg/ml,对从OE分离出的其他菌株的MIC和MBC均>2000μg/ml。此外,SC-19对金黄色葡萄球菌的MBIC和MBEC分别为125和>2000μg/ml。

结论

如今,获得性抗生素耐药现象促使人们对新型、更高效的治疗药物进行研究。因此,我们报告,鉴于观察到的对浮游状态和生物膜的影响,在一系列双(吡唑基)甲烷衍生物在此产生的结构多样性的帮助下,SC-19可能是治疗由金黄色葡萄球菌引起的OE的一种有前景的替代治疗选择。

证据水平

IV级。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cc03/8823158/4f861d590cbc/LIO2-7-283-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cc03/8823158/4f861d590cbc/LIO2-7-283-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cc03/8823158/4f861d590cbc/LIO2-7-283-g002.jpg

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