ANTIBACTERIAL ACTIVITY OF SOME NANO-ANTIMICROBIAL POLY(AMIDOAMINE) (PAMAM) DENDRIMERIC PRODUCTS

C. Caracoti, Ştefan Negrea, Carmen Ana Isabelle Florea
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Abstract

"Dendrimers are synthetic, branched macromolecules. Compared to linear polymers, dendrimers hold multiple advantages as potential carrier molecules: high capacity to incorporate pharmacologically active substances, chemical stability of micelles under physiological conditions, increased bioavailability of active substances covalently or noncovalently bound to dendrimers, due to increased dendrimers capacity to cross biological barriers. The carrier potential of dendrimers has been evaluated in combination with different antibiotics, as an alternative way to address the increasing resistance of Gram-positive and Gram-negative bacteria. This paper presents a study on the intrinsic antibacterial properties of the following poly(amidoamino) (PAMAM) ethylenediamine core dendrimers: PAMAM generation 3.5, PAMAM generation 4.0 and PAMAM-OH generation 4.0. The following bacterial strains were used: Staphylococcus aureus ATCC 29213, Staphylococcus aureus ATCC 6538, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 15442, Enterococcus faecalis ATCC 51299 and a multi-drug resistant (MDR) Acinetobacter baumannii clinical isolate. The dendrimers’ concentrations used in the experiment were established within the range of admissibility obtained following cytotoxicity testing on human cell cultures. The dendrimers’ antibacterial activity varied depending on the concentration and the bacterial species. The antibacterial efficacy was quantified by calculating the percentage and logarithmic reduction of the number of viable microorganisms. The logarithmic reduction varied between 0.06 and 1.10, corresponding to percentage reductions between 13% and 92%. The strongest antibacterial activity of all dendrimers used in this study was registered for the D3.5 dendrimer (50 μg/mL) against Acinetobacter baumannii and Pseudomonas aeruginosa ATCC 15442 reference strain. For A. baumannii, a logarithmic reduction of bacterial activity of 1.10 log10 (percentage reduction in the number of CFU of 92%) was registered, while for P. aeruginosa ATCC 15442 the logarithmic reduction was 0.75 log10 (percentage reduction of 82%)."
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一些纳米抗菌聚氨基胺(pamam)树突产物的抑菌活性
“树状大分子是合成的支链大分子。与线性聚合物相比,树状大分子作为潜在的载体分子具有多种优势:具有较高的结合药理学活性物质的能力,在生理条件下胶束的化学稳定性,由于树状大分子跨越生物屏障的能力增加,活性物质与树状大分子共价或非共价结合的生物利用度增加。树状大分子的载体潜力已被评估与不同的抗生素联合使用,作为解决革兰氏阳性和革兰氏阴性细菌日益增加的耐药性的替代方法。本文研究了聚氨基氨基(PAMAM)乙二胺核心树状大分子PAMAM 3.5代、PAMAM 4.0代和PAMAM- oh 4.0代的固有抗菌性能。采用金黄色葡萄球菌ATCC 29213、金黄色葡萄球菌ATCC 6538、大肠埃希菌ATCC 25922、铜绿假单胞菌ATCC 15442、粪肠球菌ATCC 51299和耐多药鲍曼不动杆菌临床分离株。实验中使用的树突分子浓度是在对人类细胞培养物进行细胞毒性测试后获得的可接受范围内建立的。树状大分子的抑菌活性随浓度和细菌种类的不同而不同。通过计算活菌数量的百分比和对数减少来量化抗菌效果。对数减少在0.06和1.10之间变化,对应于13%和92%之间的百分比减少。D3.5树状大分子(50 μg/mL)对鲍曼不动杆菌和铜绿假单胞菌ATCC 15442的抑菌活性最强。对于鲍曼假单胞菌,细菌活性的对数降低为1.10 log10 (CFU数量减少92%),而对于铜绿假单胞菌ATCC 15442,细菌活性的对数降低为0.75 log10(百分比减少82%)。”
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