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作为天然抗菌产品的酚类化合物:抵抗耐甲氧西林金黄色葡萄球菌、耐万古霉素肠球菌和其他耐药菌株的新武器。

Phenolic Compounds from as Natural Antimicrobial Products: New Weapons in the Fight against Methicillin Resistant , and Strains.

机构信息

EA 7394-ICV, Charles Viollette Research Institute, SFR Condorcet FR CNRS 3417, Univ. Lille, INRA, ISA-Yncréa, Univ. Artois, University Littoral Côte d'Opale, 3 rue du Professeur Laguesse, 59000 Lille, France.

Pharmacognosy Research group, Louvain Drug Research Institute, Université Catholique de Louvain, 1200 Brussels, Belgium.

出版信息

Molecules. 2019 Mar 14;24(6):1024. doi: 10.3390/molecules24061024.

Abstract

New anti-infective agents are urgently needed to fight microbial resistance. Methicillin-resistant (MRSA) strains are particularly responsible for complicated pathologies that are difficult to treat due to their virulence and the formation of persistent biofilms forming a complex protecting shell. Parasitic infections caused by and are also of global concern, because of the mortality due to the low number of safe and effective treatments. Female inflorescences of hop produce specialized metabolites known for their antimicrobial effects but underexploited to fight against drug-resistant microorganisms. In this study, we assessed the antimicrobial potential of phenolic compounds against MRSA clinical isolates, and . By fractionation process, we purified the major prenylated chalcones and acylphloroglucinols, which were quantified by UHPLC-UV in different plant parts, showing their higher content in the active flowers extract. Their potent antibacterial action (MIC < 1 µg/mL for the most active compound) was demonstrated against MRSA strains, through kill curves, post-antibiotic effects, anti-biofilm assays and synergy studies with antibiotics. An antiparasitic activity was also shown for some purified compounds, particularly on (IC < 1 to 11 µg/mL). Their cytotoxic activity was assessed both on cancer and non-cancer human cell lines.

摘要

急需新的抗感染药物来对抗微生物耐药性。耐甲氧西林金黄色葡萄球菌 (MRSA) 菌株由于其毒性和持久生物膜的形成,形成复杂的保护壳,导致复杂的病理难以治疗,是特别令人关注的。和引起的寄生虫感染也引起了全球关注,因为安全有效的治疗方法数量较少,导致死亡率较高。啤酒花的雌性花序产生的特殊代谢物具有抗菌作用,但尚未充分利用来对抗耐药微生物。在这项研究中,我们评估了酚类化合物对 MRSA 临床分离株、和的抗菌潜力。通过分级分离过程,我们纯化了主要的prenylated chalcones 和 acylphloroglucinols,并通过 UHPLC-UV 在不同植物部位进行定量分析,表明它们在活性花提取物中的含量更高。通过杀菌曲线、抗生素后效应、抗生物膜测定和与抗生素的协同研究,证明了它们对 MRSA 菌株具有很强的抗菌作用(最活跃化合物的 MIC < 1 µg/mL)。一些纯化的化合物也显示出抗寄生虫活性,特别是对(IC < 1 至 11 µg/mL)。还评估了它们对癌细胞和非癌细胞人细胞系的细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac41/6472001/57647b692da1/molecules-24-01024-g001.jpg

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