Sordi Mariane Beatriz, Moreira Thaís Altoé, Montero Juan Felipe Dumes, Barbosa Luis Cláudio, Benfatti César Augusto Magalhães, Magini Ricardo de Souza, Pimenta Andréa de Lima, Souza Júlio César Matias de
Centro de Ensino e Pesquisa em Implantes Dentários, Departamento de Odontologia, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brasil.
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brasil.
J Appl Oral Sci. 2018;26:e20170065. doi: 10.1590/1678-7757-2017-0065. Epub 2018 Feb 22.
Considering oral diseases, antibiofilm compounds can decrease the accumulation of pathogenic species such as Streptococcus mutans at micro-areas of teeth, dental restorations or implant-supported prostheses.
To assess the effect of thirteen different novel lactam-based compounds on the inhibition of S. mutans biofilm formation.
We synthesized compounds based on γ-lactones analogues from rubrolides by a mucochloric acid process and converted them into their corresponding γ-hydroxy-γ-lactams by a reaction with isobutylamine and propylamine. Compounds concentrations ranging from 0.17 up to 87.5 μg mL-1 were tested against S. mutans. We diluted the exponential cultures in TSB and incubated them (37°C) in the presence of different γ-lactones or γ-lactams dilutions. Afterwards, we measured the planktonic growth by optical density at 630 nm and therefore assessed the biofilm density by the crystal violet staining method.
Twelve compounds were active against biofilm formation, showing no effect on bacterial viability. Only one compound was inactive against both planktonic and biofilm growth. The highest biofilm inhibition (inhibition rate above 60%) was obtained for two compounds while three other compounds revealed an inhibition rate above 40%.
Twelve of the thirteen compounds revealed effective inhibition of S. mutans biofilm formation, with eight of them showing a specific antibiofilm effect.
考虑到口腔疾病，抗生物膜化合物可以减少致病变种（如变形链球菌）在牙齿、牙齿修复体或种植体支持的假体微区域的积聚。
评估13种不同的新型内酰胺类化合物对变形链球菌生物膜形成的抑制作用。
我们通过粘氯酸法从红霉内酯合成基于γ-内酯类似物的化合物，并通过与异丁胺和丙胺反应将它们转化为相应的γ-羟基-γ-内酰胺。测试了浓度范围为0.17至87.5μg/mL的化合物对变形链球菌的作用。我们在TSB中稀释指数生长期培养物，并在不同γ-内酯或γ-内酰胺稀释液存在下（37°C）孵育它们。之后，我们通过在630nm处的光密度测量浮游生长，并因此通过结晶紫染色法评估生物膜密度。
12种化合物对生物膜形成有活性，对细菌活力无影响。只有一种化合物对浮游生长和生物膜生长均无活性。两种化合物获得了最高的生物膜抑制率（抑制率高于60%），而其他三种化合物的抑制率高于40%。
13种化合物中的12种显示出对变形链球菌生物膜形成的有效抑制，其中8种显示出特异性抗生物膜作用。
