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新合成查耳酮对耐甲氧西林金黄色葡萄球菌黏附及生物膜形成的抑制作用

Newly-synthesized chalcones-inhibition of adherence and biofilm formation of methicillin-resistant Staphylococcus aureus.

作者信息

Bozic Dragana D, Milenkovic Marina, Ivkovic Branka, Cirkovic Ivana

机构信息

Department of Microbiology and Immunology University of Belgrade-Faculty of Pharmacy Belgrade Serbia.

Department of Pharmaceutical Chemistry University of Belgrade-Faculty of Pharmacy Belgrade Serbia.

出版信息

Braz J Microbiol. 2014 May 19;45(1):263-70. doi: 10.1590/s1517-83822014000100038. eCollection 2014.

Abstract

Biofilm formation and adherence of bacteria to host tissue are one of the most important virulence factors of methicillin-resistant strains of Staphylococcus aureus (MRSA). The number of resistant strains is seriously increasing during the past years and bacteria have become resistant, not only to methicillin, but also to other commonly used antistaphylococcal antibiotics. There is a great need for discovering a novel antimicrobial agent for the treatment of staphylococcal infections. One of the most promising groups of compounds appears to be chalcones. In present study we evaluated the in vitro effect of three newly synthesized chalcones: 1,3- Bis-(2-hydroxy-phenyl)-propenone, 3-(3-Hydroxy-phenyl)-1-(2-hydroxy-phenyl)-propenone and 3-(4-Hydroxy-phenyl)-1-(2-hydroxy-phenyl)-propenone on glycocalyx production, biofilm formation and adherence to human fibronectin of clinical isolates and laboratory control strain of MRSA (ATCC 43300). Subinhibitory concentrations of the tested compounds reduced the production of glycocalyx, biofilm formation and adherence to human fibronectin of all MRSA strains. Inhibition of biofilm formation was dose dependent and the most effective was 1,3- Bis-(2-hydroxy-phenyl)-propenone. In our study we demonstrated that three newly-synthesized chalcones exhibited significant effect on adherence and biofilm formation of MRSA strains. Chalcones may be considered as promising new antimicrobial agents that can be used for prevention of staphylococcal infections or as adjunct to antibiotics in conventional therapy.

摘要

细菌生物膜的形成以及细菌对宿主组织的黏附是耐甲氧西林金黄色葡萄球菌(MRSA)最重要的毒力因子之一。在过去几年中,耐药菌株的数量急剧增加,细菌不仅对甲氧西林耐药,而且对其他常用的抗葡萄球菌抗生素也产生了耐药性。迫切需要发现一种新型抗菌剂来治疗葡萄球菌感染。最有前景的一类化合物似乎是查耳酮。在本研究中,我们评估了三种新合成的查耳酮:1,3 - 双 -(2 - 羟基 - 苯基) - 丙烯酮、3 -(3 - 羟基 - 苯基) - 1 -(2 - 羟基 - 苯基) - 丙烯酮和3 -(4 - 羟基 - 苯基) - 1 -(2 - 羟基 - 苯基) - 丙烯酮对临床分离株和MRSA实验室对照菌株(ATCC 43300)的胞外多糖产生、生物膜形成以及与人纤连蛋白黏附的影响。受试化合物的亚抑菌浓度降低了所有MRSA菌株的胞外多糖产生、生物膜形成以及与人纤连蛋白的黏附。生物膜形成的抑制呈剂量依赖性,最有效的是1,3 - 双 -(2 - 羟基 - 苯基) - 丙烯酮。在我们的研究中,我们证明了三种新合成的查耳酮对MRSA菌株的黏附和生物膜形成具有显著影响。查耳酮可被视为有前景的新型抗菌剂,可用于预防葡萄球菌感染或作为传统治疗中抗生素的辅助药物。

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Antibiotic resistance of bacterial biofilms.细菌生物膜的抗生素耐药性。
Int J Antimicrob Agents. 2010 Apr;35(4):322-32. doi: 10.1016/j.ijantimicag.2009.12.011. Epub 2010 Feb 10.
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Trends in utilization of the pharmacological potential of chalcones.查耳酮药理潜力的利用趋势。
Curr Clin Pharmacol. 2010 Feb;5(1):1-29. doi: 10.2174/157488410790410579.
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Staphylococcus aureus host cell invasion and post-invasion events.金黄色葡萄球菌宿主细胞入侵和入侵后事件。
Int J Med Microbiol. 2010 Feb;300(2-3):170-5. doi: 10.1016/j.ijmm.2009.08.019. Epub 2009 Sep 24.
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Management of methicillin-resistant Staphylococcus aureus infections.耐甲氧西林金黄色葡萄球菌感染的管理
Clin Microbiol Infect. 2009 Feb;15(2):125-36. doi: 10.1111/j.1469-0691.2009.02701.x.
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Chalcones and their potential role in inflammation.查耳酮及其在炎症中的潜在作用。
Mini Rev Med Chem. 2008 Oct;8(12):1224-42. doi: 10.2174/138955708786141034.
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Antiangiogenic effects of flavonoids and chalcones.黄酮类化合物和查耳酮的抗血管生成作用。
Pharmacol Res. 2008 Apr;57(4):259-65. doi: 10.1016/j.phrs.2008.02.005. Epub 2008 Feb 23.

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