Antibacterial and Antibiofilm Activities of Makaluvamine Analogs.
Antibacterial and Antibiofilm Activities of Makaluvamine Analogs.
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马卡伐胺类似物的抗菌和抗生素活性。
DOI：
10.3390/microorganisms2030128
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发表时间：
2014
期刊：
影响因子：
4.5
通讯作者：
Velu SE
中科院分区：
文献类型：
--
作者：
Nijampatnam B;Nadkarni DH;Wu H;Velu SE
变形链球菌是龋病的主要致病菌。主要的毒力因子是其形成生物膜的能力。抑制S.变形菌生物膜为龋齿的治疗和预防提供了治疗前景。本研究评价了14种海洋生物碱makaluvamine类似物对S.变形链球菌及其抑制S.变形菌生物膜形成。所有类似物均含有Makaluvamines的三环吡咯亚氨基醌核心。类似物的结构变化是在环的7位上的氨基取代基和在Makaluvamine核心的吡咯环N上包含甲苯磺酰基。Makaluvamine类似物显示出生物膜抑制作用，IC 50值范围为0.4 μM至88 μM。此外，发现大多数类似物的观察到的杀菌活性与抗生物膜活性一致，从而得出结论，这些类似物的抗生物膜活性源于它们杀死S的能力。变种人然而，三种最有效的N-甲苯磺酰基类似物显示生物膜IC 50值比杀菌活性低至少一个数量级，表明这些类似物的生物膜活性更具选择性，可能与杀菌活性无关。
Streptococcus mutans is a key etiological agent in the formation of dental caries. The major virulence factor is its ability to form biofilms. Inhibition of S. mutans biofilms offers therapeutic prospects for the treatment and the prevention of dental caries. In this study, 14 analogs of makaluvamine, a marine alkaloid, were evaluated for their antibacterial activity against S. mutans and for their ability to inhibit S. mutans biofilm formation. All analogs contained the tricyclic pyrroloiminoquinone core of makaluvamines. The structural variations of the analogs are on the amino substituents at the 7-position of the ring and the inclusion of a tosyl group on the pyrrole ring N of the makaluvamine core. The makaluvamine analogs displayed biofilm inhibition with IC50 values ranging from 0.4 μM to 88 μM. Further, the observed bactericidal activity of the majority of the analogs was found to be consistent with the anti-biofilm activity, leading to the conclusion that the anti-biofilm activity of these analogs stems from their ability to kill S. mutans. However, three of the most potent N-tosyl analogs showed biofilm IC50 values at least an order of magnitude lower than that of bactericidal activity, indicating that the biofilm activity of these analogs is more selective and perhaps independent of bactericidal activity.