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三种新合成查耳酮的抗菌活性及与抗生素对耐甲氧西林金黄色葡萄球菌临床分离株的协同作用

Antibacterial activity of three newly-synthesized chalcones & synergism with antibiotics against clinical isolates of methicillin-resistant Staphylococcus aureus.

作者信息

Božić Dragana D, Milenković Marina, Ivković Branka, Ćirković Ivana

机构信息

Departments of Microbiology & Immunology, University of Belgrade-Faculty of Pharmacy, Belgrade, Serbia.

出版信息

Indian J Med Res. 2014 Jul;140(1):130-7.

Abstract

BACKGROUND & OBJECTIVES: Multidrug-resistance of methicillin-resistant Staphylococcus aureus (MRSA) is a serious therapeutical problem. Chalcones belong to a group of naturally occurring flavonoids, usually found in various plant species, and have potent antibacterial, antiviral and antifungal activities. The goal of this study was to evaluate the antibacterial effect of three newly-synthesized chalcones against clinical isolates of MRSA, and their synergism with β-lactam and non-β-lactam antibiotics.

METHODS

Antimicrobial activity of the three newly-synthesized chalcones was tested against 19 clinical isolates of MRSA and a laboratory control strain of MRSA (ATCC 43300). The synergism with β-lactams: cefotaxime (CFX), ceftriaxone (CTX), and non-β-lactam antibiotics: ciprofloxacin (CIP), gentamicin (GEN) and trimethoprim/sulphamethoxazole (TMP-SMX) was investigated by checkerboard method.

RESULTS

All evaluated compounds showed significant anti-MRSA activity with MIC values from 25-200 μg/ml. Observed synergism with antibiotics demonstrated that chalcones significantly enhanced the efficacy of CIP, GEN and TMP-SMX.

INTERPRETATION & CONCLUSIONS: Our study demonstrated that three newly-synthesized chalcones exhibited significant anti-MRSA effect and synergism with non-β-lactam antibiotics. The most effective compound was 1,3-Bis-(2-hydroxy-phenyl)-propenone. Our results provide useful information for future research of possible application of chalcones in combination with conventional anti-MRSA therapy as promising new antimicrobial agents.

摘要

背景与目的

耐甲氧西林金黄色葡萄球菌(MRSA)的多重耐药是一个严重的治疗难题。查尔酮属于一类天然存在的黄酮类化合物,常见于多种植物中,具有强大的抗菌、抗病毒和抗真菌活性。本研究旨在评估三种新合成的查尔酮对MRSA临床分离株的抗菌作用,以及它们与β-内酰胺类和非β-内酰胺类抗生素的协同作用。

方法

测试了三种新合成查尔酮对19株MRSA临床分离株和一株MRSA实验室对照菌株(ATCC 43300)的抗菌活性。采用棋盘法研究了它们与β-内酰胺类抗生素头孢噻肟(CFX)、头孢曲松(CTX)以及非β-内酰胺类抗生素环丙沙星(CIP)、庆大霉素(GEN)和甲氧苄啶/磺胺甲恶唑(TMP-SMX)的协同作用。

结果

所有评估的化合物均显示出显著的抗MRSA活性,MIC值为25 - 200μg/ml。观察到的与抗生素的协同作用表明,查尔酮显著增强了CIP、GEN和TMP-SMX的疗效。

解读与结论

我们的研究表明,三种新合成的查尔酮具有显著的抗MRSA作用,并与非β-内酰胺类抗生素具有协同作用。最有效的化合物是1,3-双(2-羟基苯基)丙烯酮。我们的结果为未来研究查尔酮作为有前景的新型抗菌剂与传统抗MRSA疗法联合应用提供了有用信息。

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