PDF(Pubmed)
Abstract：
Antimicrobial Resistance is a serious public health problem, which is aggravated by the ability of the microorganisms to form biofilms. Therefore, new therapeutic strategies need to be found, one of them being the use of cationic dendritic systems (dendrimers and dendrons).
The aim of this study is to analyze the in vitro antimicrobial efficacy of six cationic carbosilane (CBS) dendrimers and one dendron with peripheral ammonium groups against multidrug-resistant bacteria, some of them isolated hospital strains, and their biofilms. For this purpose, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), minimum biofilm inhibitory concentration (MBIC) and minimum eradication biofilm concentration (MBEC) studies were carried out. In addition, the cytotoxicity on Hela cells of those compounds that proved to be the most effective was analyzed.
All the tested compounds showed in vitro activity against the planktonic forms of methicillin-resistant Staphylococcus aureus and only the dendrimers BDSQ017, BDAC-001 and BDLS-001 and the dendron BDEF-130 against their biofilms. On the other hand, only the dendrimers BDAC 001, BDLS-001 and BDJS-049 and the dendron BDEF-130 were antibacterial in vitro against the planktonic forms of multidrug-resistant Pseudomonas aeruginosa, but they lacked activity against their preformed biofilms. In addition, the dendrimers BDAC-001, BDLS-001 and BDSQ-017 and the dendron BDEF-130 exhibited a good profile of cytotoxicity in vitro.
Our study demonstrates the possibility of using the four compounds mentioned above as possible topical antimicrobials against the clinical and reference strains of multidrug-resistant bacteria.
The aim of this study is to analyze the in vitro antimicrobial efficacy of six cationic carbosilane (CBS) dendrimers and one dendron with peripheral ammonium groups against multidrug-resistant bacteria, some of them isolated hospital strains, and their biofilms. For this purpose, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), minimum biofilm inhibitory concentration (MBIC) and minimum eradication biofilm concentration (MBEC) studies were carried out. In addition, the cytotoxicity on Hela cells of those compounds that proved to be the most effective was analyzed.
All the tested compounds showed in vitro activity against the planktonic forms of methicillin-resistant Staphylococcus aureus and only the dendrimers BDSQ017, BDAC-001 and BDLS-001 and the dendron BDEF-130 against their biofilms. On the other hand, only the dendrimers BDAC 001, BDLS-001 and BDJS-049 and the dendron BDEF-130 were antibacterial in vitro against the planktonic forms of multidrug-resistant Pseudomonas aeruginosa, but they lacked activity against their preformed biofilms. In addition, the dendrimers BDAC-001, BDLS-001 and BDSQ-017 and the dendron BDEF-130 exhibited a good profile of cytotoxicity in vitro.
Our study demonstrates the possibility of using the four compounds mentioned above as possible topical antimicrobials against the clinical and reference strains of multidrug-resistant bacteria.
摘要：
■抗菌素耐药性是一个严重的公共卫生问题，微生物形成生物膜的能力加剧了这种情况。因此,需要找到新的治疗策略，其中之一是使用阳离子树枝状系统（树枝状聚合物和树突）。
■本研究的目的是分析六种阳离子碳硅烷（CBS）树枝状聚合物和一个具有外周铵基团的树突对多药耐药细菌的体外抗菌功效，其中一些是分离的医院菌株，和他们的生物膜。为此,最小抑制浓度（MIC），最小杀菌浓度（MBC），进行了最小生物膜抑制浓度（MBIC）和最小根除生物膜浓度（MBEC）研究。此外,分析了那些被证明是最有效的化合物对Hela细胞的细胞毒性。
■所有测试的化合物都显示出针对耐甲氧西林金黄色葡萄球菌的浮游形式的体外活性，仅树枝状聚合物BDSQ017，BDAC-001和BDLS-001以及树突BDEF-130针对其生物膜。另一方面,只有树枝状聚合物BDAC001，BDLS-001和BDJS-049和树突BDEF-130在体外对多药耐药的铜绿假单胞菌的浮游形式具有抗菌作用，但是他们缺乏对预先形成的生物膜的活性。此外,树枝状聚合物BDAC-001，BDLS-001和BDSQ-017以及树突BDEF-130在体外表现出良好的细胞毒性。
■我们的研究证明了使用上述四种化合物作为针对多药耐药细菌的临床和参考菌株的可能的局部抗微生物剂的可能性。
■本研究的目的是分析六种阳离子碳硅烷（CBS）树枝状聚合物和一个具有外周铵基团的树突对多药耐药细菌的体外抗菌功效，其中一些是分离的医院菌株，和他们的生物膜。为此,最小抑制浓度（MIC），最小杀菌浓度（MBC），进行了最小生物膜抑制浓度（MBIC）和最小根除生物膜浓度（MBEC）研究。此外,分析了那些被证明是最有效的化合物对Hela细胞的细胞毒性。
■所有测试的化合物都显示出针对耐甲氧西林金黄色葡萄球菌的浮游形式的体外活性，仅树枝状聚合物BDSQ017，BDAC-001和BDLS-001以及树突BDEF-130针对其生物膜。另一方面,只有树枝状聚合物BDAC001，BDLS-001和BDJS-049和树突BDEF-130在体外对多药耐药的铜绿假单胞菌的浮游形式具有抗菌作用，但是他们缺乏对预先形成的生物膜的活性。此外,树枝状聚合物BDAC-001，BDLS-001和BDSQ-017以及树突BDEF-130在体外表现出良好的细胞毒性。
■我们的研究证明了使用上述四种化合物作为针对多药耐药细菌的临床和参考菌株的可能的局部抗微生物剂的可能性。
