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Antibacterial Activity of Nitric Oxide-Releasing Hyperbranched Polyamidoamines
Bioconjugate Chemistry ( IF 4.7 ) Pub Date : 2017-12-15 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00537
Lei Yang 1 , Xingzhi Wang 1 , Dakota J Suchyta 1 , Mark H Schoenfisch 1
Affiliation  

Hyperbranched polyamidoamines (h-PAMAM) were prepared using a one-pot reaction to have similar molecular weight to third generation PAMAM (G3-PAMAM) dendrimers, and then functionalized with N-diazeniumdiolate nitric oxide (NO) donors. A wide range of NO storage capacities (∼1–2.50 μmol mg–1) and NO-release kinetics (t1/2 ∼30–80 min) were achieved by changing the extent of propylene oxide (PO) modification. The therapeutic potential of these materials was evaluated by studying their antibacterial activities and toxicity against common dental pathogens and human gingival fibroblast cells, respectively. Our results indicate that the combination of NO release and PO modification is necessary to yield h-PAMAM materials with efficient bactericidal action without eliciting unwarranted cytotoxicity. Of importance, NO-releasing PO-modified h-PAMAM polymers exhibited comparable biological properties (i.e., antibacterial action and cytotoxicity) to defect-free G3-PAMAM dendrimers, but at a substantially lower synthetic burden.

中文翻译:

释放一氧化氮的超支化聚酰胺胺的抗菌活性

使用一锅反应制备超支化聚酰胺胺 (h-PAMAM),其分子量与第三代 PAMAM (G3-PAMAM) 树枝状聚合物相似,然后用N-二氮烯鎓二醇一氧化氮 (NO) 供体进行功能化。通过改变环氧丙烷(PO)改性程度,可以实现广泛的NO储存容量(∼1–2.50 μmol mg –1)和NO释放动力学(t 1/2 ∼30–80 min)。通过研究它们分别对常见牙科病原体和人类牙龈成纤维细胞的抗菌活性和毒性,评估了这些材料的治疗潜力。我们的结果表明,NO 释放和 PO 修饰的结合对于产生具有有效杀菌作用且不会引起不必要的细胞毒性的 h-PAMAM 材料是必要的。重要的是,释放 NO 的 PO 修饰的 h-PAMAM 聚合物表现出与无缺陷的 G3-PAMAM 树枝状聚合物相当的生物特性(即抗菌作用和细胞毒性),但合成负担却显着降低。
更新日期:2017-12-15
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