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铜(II)席夫碱配合物对耐甲氧西林金黄色葡萄球菌的抗菌和抗生物膜活性。

Antimicrobial and antibiofilm activities of Cu(II) Schiff base complexes against methicillin-susceptible and resistant Staphylococcus aureus.

机构信息

Department of Microbiology, School of Medicine, International Medical University, Kuala Lumpur, Malaysia.

School of Medicine, International Medical University, Kuala Lumpur, Malaysia.

出版信息

Ann Clin Microbiol Antimicrob. 2021 Sep 24;20(1):67. doi: 10.1186/s12941-021-00473-4.

Abstract

BACKGROUND

Methicillin-resistance S. aureus (MRSA) possesses the ability to resist multiple antibiotics and form biofilm. Currently, vancomycin remains the last drug of choice for treatment of MRSA infection. The emergence of vancomycin-resistant S. aureus (VRSA) has necessitated the development of new therapeutic agents against MRSA. In this study, the antimicrobial and antibiofilm activities of two copper-complexes derived from Schiff base (SBDs) were tested individually, and in combination with oxacillin (OXA) and vancomycin (VAN) against reference strains methicillin-susceptible and methicillin-resistant Staphylococcus aureus. The toxicity of the SBDs was also evaluated on a non-cancerous mammalian cell line.

METHODS

The antimicrobial activity was tested against the planktonic S. aureus cells using the microdilution broth assay, while the antibiofilm activity were evaluated using the crystal violet and resazurin assays. The cytotoxicity of the SBDs was assessed on MRC5 (normal lung tissue), using the MTT assay.

RESULTS

The individual SBDs showed significant reduction of biomass and metabolic activity in both S. aureus strains. Combinations of the SBDs with OXA and VAN were mainly additive against the planktonic cells and cells in the biofilm. Both the compounds showed moderate toxicity against the MRC5 cell line. The selectivity index suggested that the compounds were more cytotoxic to S. aureus than the normal cells.

CONCLUSION

Both the SBD compounds demonstrated promising antimicrobial and antibiofilm activities and have the potential to be further developed as an antimicrobial agent against infections caused by MRSA.

摘要

背景

耐甲氧西林金黄色葡萄球菌(MRSA)具有抵抗多种抗生素和形成生物膜的能力。目前,万古霉素仍然是治疗 MRSA 感染的首选药物。耐万古霉素金黄色葡萄球菌(VRSA)的出现促使人们开发针对 MRSA 的新治疗药物。在这项研究中,分别测试了两种源自席夫碱(SBD)的铜配合物的抗菌和抗生物膜活性,并与苯唑西林(OXA)和万古霉素(VAN)联合用于测试对耐甲氧西林敏感和耐甲氧西林金黄色葡萄球菌的参考菌株。还在非癌细胞系上评估了 SBD 的毒性。

方法

使用微量稀释肉汤测定法测试了浮游金黄色葡萄球菌细胞的抗菌活性,而使用结晶紫和 Resazurin 测定法评估了抗生物膜活性。使用 MTT 测定法在 MRC5(正常肺组织)上评估了 SBD 的细胞毒性。

结果

单独的 SBD 对两种金黄色葡萄球菌菌株的生物量和代谢活性均有显著降低作用。SBD 与 OXA 和 VAN 的组合对浮游细胞和生物膜中的细胞主要表现为相加作用。两种化合物对 MRC5 细胞系均显示出中等毒性。选择性指数表明,与正常细胞相比,化合物对金黄色葡萄球菌的细胞毒性更大。

结论

两种 SBD 化合物均表现出有希望的抗菌和抗生物膜活性,有潜力进一步开发为针对 MRSA 感染的抗菌药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8158/8464119/a685a355b448/12941_2021_473_Fig1_HTML.jpg

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